Download Cardiovascular - PHARMACEUTICAL REVIEW

Pharmaceutics
General
Abbreviations
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
–
Cata
Dis
Infra
Ultra
Meso
Retro
Cephal
Celi
Colo
Chole
Card - Cor
Cost
Intra-articular
Intra-synovial
Intra-thecal
a. c.
p. c.
i. c.
c. c.
H. S.
Man
No Oct
P.R.N
S.O.S
B.I.D (or bd)
T.I.D (or tds)
Q.I.D (or qds)
Q.D (QA, OD, or qd)
Q.O.D
Q.H
O. U
O. S
O. D
A. U
A. S
A. D
BNF





































Downward.
Apart.
Below.
Above.
Middle.
Backward.
Head (cephalgia = headache)
Abdominal (celiotomy).
Large intestine (coloprotitis) colon + rectum.
Gall bladder (cholecystectomy = removal).
Heart (pericardium = over the heart).
Ribs (intercostals)
Parentral administration in the joint.
Parentral administration in the synovial fluid.
Parentral administration in the spinal cord.
Before meals
After meals
Between meals
With meals
At bed time
In the morning
At night
When necessary
When needed
Twice daily
Thrice daily
Four-times daily
Every day (once daily)
Every other day
Every hour
Both eyes
Left eye
Right eye
Both ears
Left ear
Right ear
Caustic solution / irritating vapor
Abbreviations
– ad or add
– div
– d.t.d.
– ft. or Fiat
– M
– Solv.
– Q.S.
– a.a. or aa
– s.s.
– e. t.
– Cum or c
– S.
– Rep
– Non-rep
– Sat
– Ut dict.(ud or emp)
– Cong. Or c
– Octarious or o 
– Sig.
– Caps
– ung.
– gtt.
– P.O
Roman numbers:
–
–
–
X = 10
L = 50
C = 100

















Pint.





Add.
Divide.
Give of such doses.
Make.
Mix.
Dissolve.
A sufficient quantity.
Of each.
A half.
and
With.
Without.
Repeat.
Do not repeat.
Immediately.
Use as directed.
Gallon.
Write, let it be marked.
Capsules
Ointment.
Drops.
Per oral / by mouth
Some Common Names of Disease
–
St. Vitus Disease

Chorea
–
Down’s Syndrome

Mongolism
–
Honsen’s Disease

Leprosy (caused by Mycobacterium lepra)
–
Shingles Disease

Herpes Zoster
–
Cooley’s Disease

Familial erythroplastic anemia
–
Grave’s Disease ‘Goiter’ 
Enlargement of thyroid gland 
hyperthyroidism  exophthalmoses
–
Myxodema ‘Gull’s Disease’ 
Caused by $ secretion of the thyroid gland
(hypothyroidism)
–
Paget’s Disease

Hyperparathyroidism
–
Hodgkin’s Disease

Enlargement of the lymph nodes
–
Acromegaly (after puberty) 
–
Klinefelter’s Syndrome
–
Stein Leventhal Syndrome 
–
Cushing Syndrome

# cortisol levels secreted from adrenal cortex 
moon face, buffalo hump & HT.
–
Addison’s Disease

Hypofunction of adrenal cortex.
–
Adam’s Stokes Disease

Affects the heart & causes sudden heart block
–
Bright’s Disease

Affects the kidney (glomerulonephritis).
–
Albright’s Disease

Fibrous dysplasia of bone & cartilages.
–
Mysthenia Gravis

Weakness of the muscles due to lack of
acetylcholine (# cholinesterase).
–
Reynold's Disease

Cyanosis of fingers & toes.
–
Crohn’s Disease

Inflammation of layers of the intestinal tract 

# in pituitary gland secretions, ttt  bromocriptine
$ development of seminiferous tubules of testis.
Increased levels of androgens in ovaries
regional enteritis or ileitis & ulcerative colitis
(due to infection/irritating food)
–
Menier’s Disease

Tinnitus, dizziness & deafness.
–
Herpes Simplex

Watery blisters on skin & mucous memb. (lips)
–
STY

Staphylococcal infection of one or more of the
glands of Zeis or moll (p 263)
Some Common Disease Terms
–
Blepharitis

Inflammation of the eye lid.
–
Gastritis

Inflammation of the stomach wall.
–
Glossitis

Inflammation of the tongue.
–
Stomatitis

Inflammation of the oral mucosa.
–
Cholecystitis

Inflammation of the gall bladder (usually due to stones)
–
Cholestasis

obstruction of bile flow due to ppt of bile pigment 
calculi. There is # plasma bile acids
(serum bilirubin).
–
Polyphagia

Excessive carving for food.
–
Dysphagia

Difficulty in swallowing.
–
Alopecia

Baldness.
– Hirsutism

Abnormal hairiness (hair distribution).
–
Hives

Common name for urticaria.
–
Nystagmus

Rapid movement of the eye ball which may be:
horizontal, vertical, rotatory or mixed.
–
Hypertrophy

Enlargement or over growth of an organ.
–
Atrophy

Diminishing of an organ.
–
Hyperhydrosis

Excessive sweating.
– Hyperkinesia

Increased motor activity.
–
Hyperthesia

Excessive sensitivity to stimulation.
–
Anesthesia

Diminished sensitivity to stimulation.
–
Myalgia

Muscle pain.
–
Myositis

Inflammation of the voluntary (skeletal) muscles.
–
Spondylitis

Inflammation of the vertebrae.
–
Amyloidosis

Deposition of amyloid (complex protein) in various organs
–
Phlebitis

Inflammation of the vein.
–
Embolism

An obstruction in the vessel.
–
Stenosis

A constriction or narrowing of the blood vessel.
–
Tricuspid stenosis 
–
Aneurism
Narrowing of veins.

A weakened, bulging portion of artery (circumscribed
dilatation of artery due to BP  blood-
– Epistaxis

Bleeding from the nose.
–
Ascitis

Accumulation of serous fluids peritoneal cavity (treated
by spironolactone in absence of renal insufficiency).
–
Oedema

Excessive accumulation of interstitial fluids.
containing sac)
–
Pyelonephritis

Inflammation of the kidney.
–
Emphysema

Airflow obstruction disease with distention of all
air spaces distal to terminal bronchioles with
alveolar destruction
–
Necrosis

Localized death of a part of the tissue
surrounded by healthy tissue (death in mass)
–
Necrobiosis

Gradual degeneration in the depth of tissues.

A substance obtained from inflamed tissue, it
induces inflammatory changes in normal tissue
– Necrosin
Side Effects of Certain Drugs
•
–
Methyl dopa / Ascorbic acid
 Positive Coomb’s test.
–
Penicillins / Cephalosporins
 Positive Coomb’s test.
–
Diazoxide (vasodilator)
 Na+ retention.
–
Guanethidine
 Inhibits ejaculation
–
Guanethidine & Hydralazine
 Orthostatic hypotension.
–
Hydralazine in large doses
 Systemic Lupus Erythmatosis (SLE).
–
Procainamide
 Systemic Lupus Erythmatosis (SLE).
–
Prazocin (Minipress) (a blocker)
Tachycardia
 Postural hypotension (syncope) &
–
Sulfa-isoxazole / Succinamides
 Steven’s Johnson’s Syndrome.
–
Isoniazide (INH)
 Peripheral neuritis.
–
Chlorpromazine (phenothiazine)
 extra-pyramidal side effects + occulocutaneous pigmentation
–
Xss Bromides (as hypnotics)
 Acne-type rash on excessive use.
–
Morphine, Atropine, Al(OH)3
 Constipation
–
Digitalis, Oral contracep., Mg(OH)2
 Diarrhea
–
Phenylbutazone (NSAID)
 Blood dyscrasis on excessive use.
–
Acetaminophen
 Hepatic necrosis.
Agranulocytosis (Type II hypersensitivity mechanism): is a condition characterized by
marked leucopenia & neutopenia. It occurs as a hypersensitivity reaction to many drugs:
–
Phenyl butazone
– Thiouracil derivatives
–
Chloramphenicol
– Sulfonamides
–
Trimethadione (petit mal)
– Gold preparations
–
Chloropromazine (major tranquilizer)
– Thiazide diuretics
Some Tests
 Rats.
–
Cod liver oil
–
Heparin & Protamine  Sheep.
–
Insulin

Rabbits.
–
Oxytocin 
Chicken.
1.
What is chilblains:
a. It is a frost-bite due to extreme exposure to cold  freezing of the skin &
superficial tissue which looks as if burnt (congestion/swelling)  may lead to
gangrene
2.
Bed sores are due to:
a. Pressure atrophy
3.
1 T q.i.d. , P.C & HS means
a. One tablet four times daily after meals and at bed time.
3.
How to minimize parallex when measuring liquids:
a. By looking straight directly through.
b. By looking at an angle of 45.
4.
5.
Long-term treatment with corticosteroids causes:
a. Cushing syndrome
# cortisone
b. Addison’s syndrome
$ cortisone
What is IDA:
a. It is the reference book for formulations
6.
7.
SLE is a side effect of:
a. Procainamide
c. Hydralazine
b. Digitalis
d. Methyl dopa
Emphesima is:
a. Permanent alveolar space destruction in the lungs.
Poisoning
•
In accidental drug poisoning use:
–
Ipeca syrup to induce vomiting first.
–
Hence, activated charcoal to adsorb the remaining poison.
–
Do not give them together as the charcoal may adsorb the alkaloid of ipeca.
•
Cyanide, DDT, boric acid & FeSO4: are not adsorbed on activated charcoal.
•
Ipeca: is used as an emetic (15-30 mg/day in one dose) & expectorant (0.25-0.5 mg TID).
It is used only in adults & is not recommended in children under 6 years.
•
Universal Antidote: is a mixture of:
d Activated charcoal.
•
d MgO
d Tannic acid
Overdose treatment:
–
Amphetamines: these are bases.
d Urine acidification to enhance excretion.
d Barbiturates or chlorpromazine to control CNS stimulation.
d Beta-blockers to control hypertension.
–
Barbiturates: these are acids.
d Urine alkalanization to enhance excretion.
d Forced diuresis & artificial kidney (hemodialysis).
d IV dextran to control hypotension.
d Artificial respiration.
–
Benzodiazepines (non-barbiturate hypnotics): are safe up to 50-100 X therapeutic dose.
Antidote for benzodiazepines is flumezanil. Activated charcoal is used to $ absorption.
–
Narcotics:
d 0.4 mg Naloxone IV.
–
Acetaminophen (paracetamol): N-acetyl p-aminophenol.
d Treated with N-acetyl cystine given IV within the first 12 hours.
d Charcoal reduces absorption.
•
Acetyl salicylic acid toxicity is characterized by:
d Bleeding
d Headache
d
Dimness of vision
d Hyper-ventilation
d Tinnitus
d
Mental confusion
d Sweating
d Thirst
–
Salicylates: are acids, thus treatment of toxicity involves:
d Urine alkalanization to enhance excretion.
d Gastric lavage with NaHCO3.
d Haemodialysis in severe cases.
•
Organo-phosphorus compounds poisoning: these are commonly found in insecticides /
pesticides (e.g. diazians, dichlorons, parathion). They act as cholinesterase inhibitors (form
very stable compound with acetylcholine esterase enzyme). Symptoms of poisoning include:
d Salivation
d Hypotension
d Muscle twitches.
d Diarrhea & vomiting
d Abdominal spasm
d Miosis
d Increased sweating
d Bronchospasms
It is treated with:
d Atropine injection to antagonize the muscarinic effects.
d Pralidoxime (PAM) which forms a complex with phosphorus, preventing it from
reaching the enzyme
d Barbiturates to treat convulsions.
•
d Blood transfusion.
Organic solvents toxicity:
d Inhalation of # conc. of gasoline vapors in confined quarters  sudden death.
d The CNS effects experienced by those engaging in drug abuse phenomenon of glue
sniffing are related to the action of tolune.
d Gasoline vapors, like other hydrocarbons, may sensitize the myocardium to catecholamines leading to ventricular fibrillations, rapid CNS deprivation & respiratory failure.
d Inhalation of kerosene vapors is less hazardous than is the ingestion of kerosene.
•
Methanol poisoning: methanol is converted by alcohol dehydrogenase to formaldehyde then
formic acid demyelination of optic nerve  blindness. It is treated by giving ethanol. Also
for ethylene glycol toxicity  ethanol
•
Treatment of hyperkalemia: there are 3 methods:
•
–
If there are ECG changes, Ca++ is given to counteract the effect of excess K+ on heart.
–
HCO3 or “glucose + insulin” can be used to rapidly shift K+ from the extracellular to the
intracellular compartment.
–
If there are no ECG changes: Exchange resin (e.g. kayexolate) or dialysis can be used to
remove excess K+ from the body. The most appropriate option is the administration of
kayexolate enema (rectally) containing 50 gm in sorbitol solution.
Cyanide poisoning: is one of the most rapidly acting poisons.
–
It has very # affinity for the Fe3+ state, reacting directly with iron of cytochrome oxidase
in the mitochondria, cellular respiration is thus inhibited & cytotoxic hypoxia results.
–
Diagnosis of cyanide poisoning may be facilitated by the characteristic odour of bitter
almonds with which the physician should be familiar.
–
Cyanide poisoning is treated by Na dicobalt ededate, amyl nitrite inhalation (or Na
nitrite IV injection), Na thiosulfate. This converts Hb to methemoglobin, which has
greater affinity for cyanide thus releasing cytochrome oxidase.
•
•
•
•
CO toxicity: CO has much higher affinity for Hb than O2  carboxy Hb (responsible for the
cherry red cyanosis seen in CO toxicity); carboxy Hb is incapable of carrying O2 to tissues.
–
The toxic reactions resulting from exposure to CO are primarily the result of tissue
hypoxia produced by the inability of blood to transport sufficient oxygen.
–
Anemic persons are more susceptible to CO poisoning than normal individuals.
–
Although the formation of carboxy Hb decreases the oxygen carrying capacity of blood
it does not decrease the PO2 of arterial blood & as a result there is no stimulation of
chemoreceptors.
–
Carboxy Hb is a compound that dissociates most rapidly in presence of O2 which
displaces CO in the Hb molecule & converts carboxy Hb to Oxy Hb. Thus, CO toxicity
can be treated through maintenance of respiration, removal from exposure source, blood
transfusion, administration of 100% oxygen, or hyperbaric O2 when applicable.
Lead Poisoning: may be acute or chronic, yet acute poisoning is relatively infrequent.
–
Organic lead compounds are more likely to produce CNS symptoms, while aberrations
in Hb synthesis are more apt to be associated with inorganic lead poisoning.
–
Exposure to lead produces unmistakable, progressive mental deterioration in children.
–
Pb toxicity can be treated with chelating agents: EDTA, penicillamine, or dimercaprol
(BAL); of which penicillamine only is effective by the oral route.
Mercury Poisoning: 3 major forms of Hg must be distinguished: Hg vapor (elemental Hg),
salts of Hg & organic mercurials.
–
Hg has special affinity for the S atom in thiol gps of enzymes to inactivate them, which
is ultimately responsible for its toxicity.
–
Hg may be absorbed through the GIT, respiratory system or the skin.
–
The upper limit for Hg conc. in blood is 0.01-0.03 mg/ml.
–
The kidney is the target organ for inorganic Hg while the CNS is the target for elemental
Hg & organic Hg compounds.
Arsenic Toxicity: both organic & inorganic forms of As are readily available in industrial &
medicinal products. Pathways & byproducts of As biotransformation are not yet identified.
–
As produces dilatation of capillaries & increases the permeability of capillary walls.
–
It does not cross the BBB.
–
Symptoms include: blood, casts & protein in urine, vesicoes under intestinal mucosa,
peripheral neuropathy & facial edema (it does not produce polycythemia).
–
BAL is the 1ry agent used for As toxicity.
•
Pepto-Bismol (Bismuth subsalicylate) is toxic if absorbed  colors stools black.
•
BAL & penicillamine are antidotes for heavy metals (Hg, Cu, Gold, As & antimony).
•
EDTA: is used as a chelating agent in heavy divalent metal poisoning. (e.g. Pb, Zn, Ca).
•
Deferoxamine is the antidote for Fe poisoning.
•
Vomiting is contra-indicated in poisoning with: (as it might cause aspiration pneumonitis)
– Bleaching liquid. – Organic acids
– INH
– Gasoline.
– Liquid petroleum.
1. What is the antidote for phenylephrine poisoning?
a) Phentolamine
c) Isoprotrenol
b) Atropine
d) Histamine
2. What is the pharmacology of CO poisoning?
a) Interaction with Hb
b) Interaction with cytochrome oxidase.
3. What is the max time after which we can give N-acetyl cystine for acetaminophen toxicity :
a) 3 – 12 hrs.
c. 24 hrs
b) 2 – 6 hrs
d. 48 hrs
4. Grayish mouth & loss of teeth are symptoms of :
a. Lead poisoning
c. Iron poisoning
b. Copper poisoning
EDTA is the antidote,
also for As & Zn
5. EDTA can chelate Ca2+ & Fe3+ in the following proportions:
a. One mole of Ca 2+ + one mole of Fe 3+.
b. 2 moles of Ca 2+ + 2 moles of Fe 3+.
c. 2 moles of Ca 2+ + 3 mole of Fe 3+.
d. 3 moles of Ca 2+ + 3 moles of Fe 3+.
e. None of the above.
6. Which CNS poison is selectively toxic to the retina:
a. Methanol
c. Disulfuram
b. Arsenic
d. CCl4
e. Warfarin
7. Methanol toxicity is due to its conversion in the body to:
a. Ethanol
c. Acetaldehyde
b. Carbonic
d. Formic acid / formaldehyde
8. Methanol toxicity may cause:
a. Blindness
b. Deafness
9. Overuse of digitalis may result in:
a. Habituation
b. Tolerance
c. Addiction
d. Cumulative poisoning
10. The first toxic symptoms of digitalis toxicity are:
a. GIT irritation
c. AV block
b. Cerebral excitement d. Undue depression of heart
e. Flushing
11. Which of the following symptoms is not associated with digitalis poisoning?
a) AV block
c) Vomiting
e) Constipation
b) Ventricular tachycardia
d) Vagal arrest of the heart
12. Because the action of warfarin (dicumarol) persists for several days, its continued use may
lead to cumulative poisoning which can be counteracted with?
a) Vitamin K
c) Protamine sulfate
b) Prothrombin.
d) Heparin
13. Organic pesticides (malathion) may be effectively counteracted with?
a) PAM (an emergency antidote)
c) Charcoal
b) Pentaoline
d) Dopamine
14. The greatest threat for morphine poisoning is:
a. Respiratory depression
c. Renal shut down
b. Paralysis of spinal chord
d. CV collapse
15. Among the signs of barbiturate poisoning are:
a. Hypotension.
b. Diuresis.
b. Decreased respiratory volume.
e. Alkalosis.
16. Which of the following could be used as antidote for curarae poisoning:
a. Neostegmine
c. Atropine
b. Homatropine
d. Hexamethonium.
17. What is the disadvantage of fluorinated drinking water:
a. It may cause mottling of teeth.
18. Poison ivy is treated by:
a. Calamine lotion
c. Hydrocortisone (0.5% systemic)
b. Burrow’s solution
d. Silver nitrate
19. Mechanism of action of dimercaprol & penicillamine in heavy metal poisoning:
a. Formation of a chelate (stable complex) that is non toxic & easily excreted (more
water soluble)
20. Atropine poisoning causes all except:
a) Diarrhea.
21. Ca EDTA is used as an antidote for:
a. Pb poisoning (any divalent metal poisoning)
22. BAL (dimercaprol) is used as an antidote for:
a. Hg poisoning
23. A chelating agent used in Ca toxicity & in rheumatoid arthritis:
a. Penicillamine
b. EDETA
Solutions, Syrups, Elixirs & Tinctures
•
Preparations containing sugar are syrups & elixirs.
•
Preparations containing alcohol are tinctures, spirits & elixirs.
•
Essential oils: are used in perfume industry.
•
Methyl- & Propyl-paraben (preservatives) are used in combination to $ amount needed of
each (achieve solubility, no ppt). The combination has strong antiseptic action (synergistic
effect); also effective over a wide pH range. Their activity is $ in presence of non-ionic SAA.
•
Benzyl alcohol: in a conc. of < 1% is used as a preservative.
•
Benzyl alcohol: In a conc. of > 1% (3-5%) is used as a co-solvent.
•
Aluminium subacetate & Aluminium subgalate are used as astringents (in hemorrhoids).
•
Burrow’s solution: is an Al acetate solution. This is a topical solution with antiseptic &
astringent properties, used as a mouth wash.
•
Flexible Collodion: is prepared by dissolving 2% camphor & 3% castor oil in collodion.
•
Salicylic acid Collodion: is prepared by dissolving salicylic acid in flexible collodion; it is
used for removal of callous (warts).
•
Coal Tar solution: also called LCD (Liquor Carbonis detergent). It contains:
d Coal tar
d alcohol
d Polysorbate 80.
Polysorbate 80 is included to disperse the water insoluble coal tar which may ppt if mixed
with water.
•
Sand is used during manufacturing of coal tar, to # its surface area & dissolution in alcohol.
•
Acidulin: releases HCl in vitro.
•
Rubitussin: contains glyceryl guaiacoate – an antitussive substance.
•
Coricidin: contains an anti-histaminic – chlorpheniramine maleate.
•
Formula 44 syrup: contains the active ingredient cetamlum.
•
Panalba: contains albamycin combined with tetracycline.
•
Organic solvents for internal use include:
–
Glycerol / Ethanol  for oral preparations
–
Vegetable oils (linseed, peanut & cotton seed oil)  as vehicles for parentrals.
•
Reading of a solution: the measure should be held at the level of the eye, to prevent paralox.
•
Controlled room temperature: temp between 15oC - 30oC (59oF - 86oF)
•
Cool place: temp between 8oC - 15oC (46oF - 59oF)
•
Cold place: temp between 2oC - 8oC (36oF - 46oF) e.g. refrigerator.
Emulsifying Agents
•
Any compound that $ the interfacial tension & forms a film at the interface can function as
an emulsifying agent. (Also known as wetting agents or surfactants).
•
The effectiveness of a compound depends on its:
•
d
Chemical structure
d Conc.
d Solubility
d
Physical properties
d pH
d Electrostatic effects.
Emulsifying agents can be classified as:
– True emulsifiers: 1ry agents, capable of forming / stabilizing emulsions by themselves.
–
•
Stabilizers: auxiliary agents, do not form acceptable emulsions when used alone, but do
assist 1ry agents in stabilizing the product by # viscosity.
Emulsifying agents can also be classified as:
–
Natural: Acacia, tragacanth, agar, pectin, gelatin, methyl-, carboxy-methyl-cellulose.
–
Synthetic EAs:
d Non-ionic SA: (the molecule has no tendency to migrate to either pole) are resistant
to the addition of acids & electrolytes; e.g.
A Sorbitan esters (Spans): hydrophobic (HLB < 9)  w/o emulsions.
A Polysorbates (Tweens): hydrophilic (HLB 11 – 20)  o/w emulsions.
Spans & tweens can be used in combination to produce EA with total conc. 2% w/v.
d Anaionic SA:
Triethanolamine
is an anionic
surfactant
A Sulphuric acid esters: e.g. Na lauryl sulfate (HLB < 9) (7-9)
A Sulphonic acid derivatives: e.g. dioctyl sodium sulfo-succinate.
A Soaps: these are for external use only, have high pH & are sensitive to the
addition of electrolytes & acids.
. Alkali soaps: hydrophilic  o/w emulsions.
. Metallic soaps: water insoluble  w/o emulsions.
. Monovalent soaps:  o/w emulsions.
. Polyvalent soaps:  w/o emulsions.
d Cataionic SA: e.g.
A Benzalkonium chloride: used in conc. of 1% & is incompatible with soaps.
A Cetyl pyredinium chloride.
•
The Critical Micellar Conc.: of a surfactant is the conc. above which the surface tension
remains constant (does not decrease).
•
•
Hydrophilic – Lipophilic Balance System: is used to classify thousands of non-ionic
surfactants. These are given numerical designations between 1-20 depending on the relative
hydrophilic – lipophilic portions of the molecule.
–
Emulsifiers with HLB < 9 are more lipophilic  w/o emulsions
–
Emulsifiers with HLB > 11 are more hydrophilic  o/w emulsions
–
Emulsifiers with HLB 9-11 can give both types of emulsions.
HLB:
–
0–3

Anti-foaming
–
3–6

W / O emulsion
–
7–9

Wetting agent (SAA)
–
9 – 18

O / W emulsion
–
9 – 15

Detergent
–
15 – 18

Solubilizing Agent
]
]
W/O
O/W
•
< 10, a compound is said to have a low HLB, >10 the compound is said to have a high HLB
•
Egg yolk (phospholipid): may be used in some pharmaceuticals as an emulsifying agent.
•
Lecithin (phospholipid): is a natural emulsifying agent.
•
Creaming: is the concentration of an emulsion resulting in accumulation of the concentrate
at the top of the emulsion. Reagitation reconstitutes the emulsion again.
–
It is a reversible process, & is increased by the # in droplet size. Surfactants $ creaming.
Suspensions
•
A suspension is a 2 phase system: in which the internal (or dispersed) phase is a solid & the
external (or continuous) phase is a liquid.
•
Aggregation of the suspending agent: is called micelles (also one of the ultra-microscopic
structure of the protoplasm – a colloidal structure).
•
Surface active agents (e.g. Na lauryl sulfate) promote wetting of solids.
•
If the contact angle is less than 90  the substance can be wetted.
•
If the contact angle is equal to zero  the substance is wetted.
•
In a suspension, settling of particles can be overcome by:
–
Adding non-ionic SAA.
– Reducing particle size.
–
Increasing viscosity (by adding shear thinning agents).
•
Calamine: consists of 98% ZnO + 2% ferric oxide (Fe2O3).
•
Acetyl sulfa-isoxazole: is insoluble & tasteless, thus is ideal for flavored oral suspensions.
•
Propoxyphen napsylate: a narcotic analgesic, is a water insoluble powder which forms
stable suspension. Propoxyphen HCl is soluble but unstable for commercial use.
Ointments
•
Yellow ointment: consists of 5% yellow wax (bees wax) in white petrolatum.
•
White ointment: consists of 5% white wax in petrolatum. It is hydrophobic (has a low water
number). Thus aqueous solutions cannot be incorporated as a w/o phase in white ointment.
•
Hydrophilic petrolatum contains cholesterol which acts as an emulsifier, thus can be used to
make a w/o emulsion.
•
Vaginal preparations:
–
Most commercial vaginal suppositories use a base of polyethylene glycol (PEG) (O/W).
–
An excellent choice of a diluent for compressed vaginal tablets would be lactose.
•
Coal tar ointment: Coal tar is mixed with polysorbate (as base), then added to ZnO paste.
•
Sulphur ointment: is used in the treatment of mild cases of scabies.
•
Calamine ointment: contains ZnO to protect the skin from further infections (protection).
•
Ziradyl: contains zirconium salt and is used as a protectant.
•
Compound undecylenic acid ointment consists of:
–
5% free undecylenic acid
- 20% Zn undecylenate
- Poly ethylene glycol as a base.
•
Desenex: contains Zn undecylenate and is used as antifungal in athlete’s foot.
•
Seborrhea is a disease of the scalp, face & other areas of the body causing scaly scalp. It is
treated with 0.01% cortisone e.g. betamethazone valerate (Betnovate).
•
Ointment bases:
–
Oleaginous bases: are good bases for oil insoluble ingredients (e.g. white ointment,
petrolatum, lanoline derivatives, glyceryl monostearate & isopropyl palmitate).
–
W/O emulsion bases: e.g. cold cream, lanoline, eucerine.
–
O/W emulsion bases: e.g. vanishing cream, Lubriderm & hydrophilic ointment.
–
Water soluble bases: polyethylene glycol, propylene glycol & cetaphil.
–
Absorption bases: Aquaphor, hydrophilic petrolatum, wool fat (anhydrous lanoline).
•
Trituration: is the process of grinding a substance to a very fine powder.
•
Pulverization by intervention is the process of reducing the particle size of a substance to
fine powder by utilizing a solvent which can be removed easily, e.g. camphor + alcohol.
•
Levigation: A process of reducing a powdered drug to a smooth paste using a levigating
agent which should be compatible with the powdered drug. It is a process of wetting &
smoothing. E.g. the incorporation of powder into ointment base by adding a wetting agent
(oleaginous vehicles e.g. mineral oil; hydrophilic vehicle e.g. glycerol).
•
Precipitated sulphur: is used in preparing ointments as it has finer particle size & greater
surface area than other forms of sulphur. It produces a smooth ointment.
•
A gel structure can be formed by Bentonite, Agar, or Accacia.
Other Formulations
•
Percolation: is an extraction process of the desired constituent of a powdered drug by the
descend of a suitable solvent at a controlled rate through a column of the drug.
•
Maceration: is an extraction process of the desired constituent of a powdered drug by
soaking in a suitable solvent.
•
Lyophalization (freeze drying): loss of moisture under low temp. It involves rapidly freezing
a substance (below eutectic point) & dehydration under low pressure (# vacuum).
•
Micrometrics: it is the study of all aspects of small particles e.g. particle size, separation of
particles, etc.
–
Impalpable: refers to a substance that is imperceptible to the touch.
d In order to apply powder to the skin, a particle size of < 50m is desirable.
d Particle size for aerosols

2 – 6 m.
d Particle size for inhalation

0.1 m.
•
The powder surface area: can be determined by the adsorption of a gas.
•
In a crystallization process: Addition of a reactant with vigorous stirring will lead to the
formation of crystals with solvent embedded in it or very fine filterable powder.
•
Freon II: a fluorinated hydrocarbon used as a propellant in aerosols; as it has harmful effects
on environment, is currently replaced by flouro-hydrocarbons. It is used only in deodorants.
•
Nicorette: marketed as a chewing gum, each piece containing 2 mg of nicotine-resin
complex. It is used to help physically dependant cigarette smokers to quit smoking. It does
not eliminate the desire to smoke. It is contraindicated in pregnancy & cardiac problems.
Tablets
•
The Wurster Process: can be used to coat tablets.
•
Tablets are coated: to mask bad taste & / or unpleasant odor.
•
Picking: is said to occur when poorly manufactured tablets have small particles on the
surface (due to tablet powder sticking to the punch face).
•
Mottling: is uneven color distribution of tablets due to poor mixing of tablet granulations.
•
Shellac is sometimes included as a sealing subcoat in the production of sugar coated tablets.
It prevents the tablet from absorbing water from subsequent coating solutions.
•
Methyl stearate is used as a lubricant, while talc is used as a glidant in tableting.
•
Fillers in tablet manufacturing: Mannitol, Lactose, Cellulose & Ca3 (PO4) 2.
•
Disintegrants in tablet manufacturing: Mannitol, Lactose, Cellulose & Ca3 (PO4) 2.
•
Mannitol (in manufacturing) has 2 functions:
–
It possesses characteristics that make it almost a sweetener for chewable tablets.
– It is included in many lyophilized (freeze dried) products as a bulking agent as the cake.
1.
Liquid droplets dispersed in another liquid is called:
a. Emulsion
2.
3.
b. Suspension
Which of the following vehicles is suitable for internal use:
a. Ethylene glycol
c. Butanol
e. Methanol
b. Ethanol
d. Isopropanol
f. Propylene glycol
Addition of mineral oil to sulphur is:
a. Trituration (powder with powder) c. Levigation
b. Milling
4.
5.
6.
c. Antioxidant.
b. Suspending agent.
d. Buffer.
e. Solubilizer.
Polyoxyethylene sorbitan monooleate is used in a mouth wash as:
a. Flavoring agent
c. Preservative
b. Oil solubilizer
d. Buffer.
e. Antioxidant.
Which of the following agents is used as anti-oxidant in aqueous solutions:
Na lauryl sulfate is a
b. Vitamin C
c. EDTA
surfactant:
b. Non-ionic
c. Cataionic
What is the use of cellulose in tablet formulation:
a. As a diluent
9.
d. Pulverization
a. Wetting agent.
a. Anaionic
8.
e. Attrition
Menthioglycerol in a parentral procaine penicillin suspension is:
a. Na bisulphite (Na thiosulfate)
7.
c. Gel
b. As a lubricant
c. As a glidant
b. As a lubricant
c. As a glidant
What is the use of talc in a formulation:
a. As a diluent
10. Methyl cellulose is a(n)
a. Anaionic
surfactant:
b. Non-ionic
c. Cationic
11. Which of the following has a phospholipid structure:
a. Lecithin
c. bile acid
c. Cardiolipin
12. Aquaphor is:
a. Anhydrous ointment base ???
b. Hydrophilic petrolatum ???
13. Lanoline 900 gm + Fatty acid (oil) + Cetyl alcohol + Water 500 ml, the resulting formula is:
a. O/W emulsion
14. A sustained release formulation has no value in:
a. Drugs having long half-life.
b. Drugs having short half-life.
15. Which of these suppository bases can be used for both oil- & water-soluble drugs:
a. PEG (carbowax)
c. Cocoa butter
b. Glycerin
d. Glycerinated gelatin
16. The sedimentation rate of a poorly soluble drug in a suspension can be decreased by adding:
a. Non-ionic surfactant
d. Thyxotropic gel
b. Shear thickening gel
e. Dilatant colloidal clay
c. An agent that increases the viscosity.
17. Levigation depends upon:
a. Ointment base
b. Particle size
c. Both
18. Which of the following is true about enteric coated tablets:
a. Protected from moisture
b. Protected from gastric juice
19. What is bentonite magma:
a. A preservative
b. A suspending agent
20. A substance has an HLB of 10 – 18 forms:
a. Good W/O
c. Is good for solubilization
b. Good O/W
d. None of the above
21. Which of the following can be used as an emulsifying agent for O/W parentral emulsions:
a. Lecithin
22. Burrow’s solution is used as :
a. Astringent
b. Keratolytic
23. Fereon, which is used as a propellant in aerosols,:
a. has a harmful effect on the environment (Ozone)
24. In tablet manufacturing, Mg stearate is used as:
a. Lubricant
b. Glidant
c. Diluent.
25. Which is not a suitable suspending agent in clear gel preparations:
a. Bentonite.
26. Which compound is used as a preservative & antibacterial:
a. Benzalconium chloride
b. Propylene glycol.
27. Hydrophilic petrolatum employs wool alcohol to:
a. Render petrolatum emulsifyable.
28. Arrangement of surfactant molecules in a sphere is called:
a. Micelle
c. Benzoyl alcohol.
29. Which drugs are used in smoking cesation:
a. Nicoderm
d. Nicorette
g. Nicotrol
b. Regitine
e. Bupropione (Zyban)
h. Clonidil
c. Rivia
f. Normatol
30. On the label of Nicorette gum resin it should be indicated:
a. Do not take more than 20 mg per day
b. Not used for patients under 18, pregnant nor lactating women
c. Do not throw into the garbage (toxic to animals)
d. Chew, park against the cheek then chew again
31. What advice do you give to a patient taking Nicorette gum resin:
a. The number of chewing gums should not exceed 10 per day
b. Changing the site of chewing.
c. Park against the cheek every 15 min.
32. Which is not considered a tablet processing problem:
a. Peeling
c. Sticking
b. Capping
d. Picking.
e. Mottling
33. Which is true about surfactants:
a. Have hydrophylic, lipophylic properties
b. Are either anaionic, cataionic or non-ionic
c. Are amphiphobic
d. React as acids & bases (Amphoteric)
34. The physical stability of a solution can be determined by:
a. Precipitation
b. Odor
c. Viscosity
35. A flocculated sediment has:
a. Has a large volume of sediment c. Easily re-dispersed by shaking
b. Has a clear supernatant
36. Diazepam, ethanol & phenol, phenol is:
a. Cosolvent
37. Cimetidine HCl, water & phenol, phenol is:
a. Preservative
38. The process by which a substance accumulates on the surface of a body is:
a. Adsorption
b. Absorption
39. Which is not in suspension:
a. Adsorption
c. Aggregation
b. Flocculation
d. Crystal growth
40. Fluorinated hydrocarbons (Fereon) are replaced by:
a. Hydrocarbons
c. Chlorofluorocarbons (CFCs)
b. Inert gas
d. Hydrofluoroalkanes (Hydrofluorocarbons)
41. Which of the following happens when a tablet reaches the stomach:
a. Absorbs water
c. Swells
b. Undergoes hydrolysis
42. Which is true about sedimentation:
a. Larger particles have higher sedimentation rates
b. Decreasing particle density decreases sedimentation rate
c. Sedimentation increases with the decrease in viscosity
43. Which increases wetting of powders:
a. Polysorbate 80
b. Benzyl alcohol.
44. Which is used to prepare O/W emulsion:
a. Accacia
c. PEG
b. Methyl cellulose
d. Polysorbate
45. Which is used as a base for vaginal suppositories:
a. Propylene glycol
b. Cocoa butter
46. The removal of tablet surface material by a punch is called:
a. Picking
b. Mottling
47. Which is not included as an emulsion problem:
a. Cracking
48. Creaming in an emulsion is due to:
a. Increasing droplet size
49. Diazipam + Alcohol + Propylene glycol (or ethylene glycol) 45% in a Rx is:
a. Co-solvent
c. Preservative
b. Antioxidant
d. Solvent
50. Gel preparations can include all except:
a. Carageenan
c. Accacia
b. PEG
d. Agar
51. Elixirs are:
a. Sweetened hydro-alcoholic formulations
52. Tri-ethanolamine is used as:
a. Emulsifying agent
53. Which is used as a humectant:
a. Glycerol
Ophthalmic Preparations
•
The cornea of the eye: consists of 3 layers:
–
Outermost layer  the corneal epithelium.
–
Substantia propria  the stroma.
–
Inner layer  the corneal endothelium.
•
Stroma is the deepest & most hydrophilic & least lipophilic layer.
•
The capacity of the precorneal area: for instilling eye drops is ~ 0.01 – 0.02 ml. (the normal
tears volume is ~ 0.007 ml).
•
A wetting agent is used for contact lenses: to prevent dryness (e.g. Na lauryl sulfate).
•
On using soft lenses: An antimicrobial preservative for ophthalmics is considered adequately
effective if it re-sterilizes the solution within 1 hr.
•
A combination of benzalkonium chloride & EDTA (0.01% of each) is effective against
most common micro-organisms including strains of P. aeruginosa that are resistant to
benzalkonium chloride alone.
•
Benzalkonium chloride, in addition to its use as a preservative is also used to adjust the pH
of nasal drops to reduce irritation.
•
Thiomersal: is used as a preservative in contact lenses’ solution.
•
Pabin is a proteolytic enzyme used in contact lens solutions as a protein remover to dissolve
proteinaceous residues that slowly build up on lenses. It is present in protein removal tablets.
•
Collyrium means an eye wash (may contain boric acid).
•
Liquifilm is an ophthalmic vehicle containing polyvinyl alcohol to increase the viscosity &
thus increase contact time with the corneal surface.
•
Methyl cellulose, carboxymethyl cellulose & hydroxypropyl methylcellulose are used to
increase viscosity of eye drops.
•
A red dispensing cap or top in eye drops identifies mydriatic drugs (as atropine, mydriacil).
•
A green dispensing cap or top in eye drops identifies miotic drugs (as pilocarpine).
•
Nasal & ophthalmic solutions: should have low or mild buffer capacity so that the natural
buffer system can overcome any pH difference otherwise it will cause irritation.
–
They should have an acidic pH (5.5 – 7.5)  use phosphate buffer.
–
They should be isotonic.
–
They should have an antimicrobial preservative.
•
Difference between pilocarpine & beta-blockers (Timoptic) in treatment of glaucoma
Difference
Pilocarpine
Timoptic
Mode of action
Contraction of sphincter muscle
of the pupil leads to drainage of
aqueous humor & $ IOP
Decrease the production of
aqueous humor  $ IOP
Onset of action
2 – 4 hrs
1 – 2 hrs
Duration of action
4 – 8 hrs
24 hrs
Vision
Accommodation of near vision
due to miosis.
No effect on vision because
there is no miosis.
•
Narrow angle glaucoma: is treated by pilocarpine, timolol, phospholine iodine,
pheostegmine ( anticholine esterase) or carbacol 0.5 - 1% (which is similar to acetylcholine).
•
Advantages of timolol maleate (Timoptic) over pilocarpine
–
Reduces the elevated IOP through $ production of aqueous humor.
–
Exerts its maximal effect within 1 – 2 hours.
–
Maintains significant effect for 24 hrs after one single dose.
–
Little or no effect on visual accuracy or accommodation.
–
Little or no effect on pupil size.
•
Pilocarpine: the miotic effect of pilocarpine is observed 5-30 min after installation in the eye
& the intraocular pressure is reduced within 2 – 4 hours.
•
Phospholine Iodine: is an anti-cholinesterase drug (# acetylcholine) & used to treat
glaucoma. Prolonged use of this drug, reduces the activity of pseudo-cholinesterase.
•
Epinephrine (adrenaline) is contraindicated for narrow angle glaucoma: since dilatation
of the pupil may lead to blindness. It may be used in open angle glaucoma as it increases the
drainage, & reduces the production of aqueous humor.
•
Similarly, phenylephrine, guanithidine, antazoline & hematropine are contraindicated
for narrow angle glaucoma: as they cause mydriasis.
•
90% of glaucomas are open (wide) angle glaucoma.
•
Filters used in ophthalmics have pose size = 0.2m.
1.
Methyl cellulose is used in ophthalmic solutions to:
a. Increase contact time of solution in the eye.
c. Increase infiltration
b. Increase drop size
2.
Drugs of choice for the treatment of narrow angle glaucoma include:
a. Physostigmine (eserine), pilocarpine, phospholine, iodine
myosis.
b. Carbachol (0.5 – 1% eye drops).
c. Demecarium (reversible cholinesterase inhibitor).
d. Hematropine (atropine derivative)
3.
The Rx shown is:
a. Suspension
Phospholine is an irreversible
cholinesterase inhibitor.
Rx Atropine sulphate
Carboxymethyl cellulose (# viscosity)
Benzalkonium chloride (Preservative)
Na3PO4 / Na2HPO4 (Buffer)
Aqua
c. Cream
b. Ophthalmic solution
4. The English name of collyrium is:
a. Eye wash.
c. Clear solution.
b. Ointment.
5.
What is the effect of beta-blockers (Timolol) on the intra-ocular pressure :
a. Increase the intra-ocular pressure
b. Decrease the intra-ocular pressure
6.
90% of the cases of glaucoma are:
a. Narrow angle glaucoma
b. Wide (open) angle glaucoma
7.
To increase the bioavailability of ophthalmic solutions:
a. Increase conc. of drug
c. Add mono-ploymer
b. Increase the retention time (by increasing viscosity).
8.
Hydroxy methyl cellulose in atropine eye drops is used to:
a. Inhibit bacterial growth
b. Increase corneal contact time.
9.
Which agent is used in otic solutions to increase bioavailability:
a. Ethyl alcohol
c. Methyl alcohol
b. Glycerol.
10. A sympathomemetic drug will $ IOP by:
a. Decreasing synthesis of aqueous humor.
b. Increasing drainage of aqueous humor.
11. Which is the most lipophilic barrier of the eye:
a. Cornea.
c. Conjunctiva
b. Eye lids
d. Aqueous humor.
12. All of the following are used in eye allergy except:
a. Xalatan (eye pressure)
13. Side effects of Xalatan (Catamaprost) include:
a. Pigmentation (eyes are more black)
b. Increased thickness of eye lashes
14. In ophthalmic preparations, the absolute bioavailability is:
a. Zero %
c. 50%.
b. 75%.
15. The rate limiting step in an ophthalmic preparation is:
a. Corneal penetration
16. A solution of phenyl ephrine & boric acid is:
a. Hypertonic
b. Isotonic
17. Which is correct about ophthalmic solutions:
a. Methyl & propyl parabens (preservatives) are not used in ophthalmic preparations
b. Polyvinyl alcohol increases viscosity in ophthalmic preparations.
c. Surface active agents are used in lens solutions to increase wetting.
d. Percentage bioavailability is zero.
18. Best way of application of eye drops is to:
a. Make an occular sac in which to insert drops.
b. Insert drops in the cap.
c. Close the eye & apply pressure on the internal corner.
19. Which agent is used in otic solutions to increase bioavailability:
a. Ethyl alcohol
c. Methyl alcohol
b. Glycerol.
20. A sympathomemetic drug will $ IOP by:
a. Decreasing synthesis of aqueous humor.
b. Increasing drainage of aqueous humor.
Parentrals
•
The gauge number of needles (G): this number refers to the external diameter of the
cannula. The larger the gauge number the smaller the diameter of the cannula.
•
Hypodermic Needle: is a small needle used to inject a drug under the skin. It consists of:
–
Hub: the extension of the needle that fits onto the syringe.
–
Bevel: Portion of the needle that is ground for sharpness.
–
Heel: the back portion of the bevel
– Cannula: the shaft portion of the needle (made of steel)
–
Lumen: the cavity in the needle through which drug is injected.
•
A short bevel needle: is preferred for IV injection as it reduces the possibility of perforating
the back wall of the vein.
•
A very short bevel needle: is preferred for ID injections.
•
Insulin preparations: have low viscosity & small volumes to inject. Thus small pore (25G –
26G) & short (1/2 or 5/8``) needles are adequate for SC injection. (Insulin is given SC
because of good absorption from this site, ease of self-administration & to $ tissue damage).
•
Winged needle (Butterfly): consists of a stainless steel needle with 2 flexible plastic winglike projections that serve 2 purposes during IV injection:
–
They ease manipulation of the needle during insertion in the vein.
–
Allow the needle to be anchored to the skin with a tape.
•
A Busher Automatic Injector: is a metal device in which the patient places a filled
hypodermic syringe & needle. It automatically administers the injection.
•
Becton-Dickinson (B-D): supplies insulin syringes with 0.5 ml volume.
•
Autoclaving: sterilization under steam & pressure (15 min at 121oC).
•
Propylene syringes are autoclavable while other plastic syringes must be gas sterilized
(using ethylene oxide). Vials are also sterilized using ethylene oxide.
•
Venoclysis is the IV administration of large volume parentrals by infusion. (= IV infusion).
•
Hypodermoclysis: is the intentional administration of IV fluids in the SC tissue (e.g. in
infants & obese women).
•
LVPs: means large volume parentral solutions.
•
Piggy pack: saves the patient from multiple injections (as intermittent therapy of antibiotics).
•
IV infusion: maximum volume / day is 4 L otherwise it might cause fluid overload.
•
Diazepam should not be added to IV infusions as it will precipitate.
•
IV admixture must be used within 24 hrs (when refrigerated 2-8oC to limit microbial growth)
Needle Gauge: 13 – 27  largest number:
S.C.

24 – 25
Comp. Parentrals

18 – 20

I.M.
12 – 19
Needle length:
¼ - 6 inches
I.D.

¼ - 5/8 inches
S.C.

½ - 5/8 inches
Compound Parentrals

1.5 inches
I.V.
Intra-cardiac

1.25 – 1.5 inches

3.5 inches
Filters:
Depth Filters: Fritted glass or unglazed porcelain.
Serum Filters: Cellulose ester or ….. or ……
Parentral Solvents & Solutions
•
Purified water USP: The method of preparation must be indicated on the label (i.e.
distillation, ion-exchange, …etc.).
•
Water for injection (WFI): is a pyrogen-free water, freshly prepared by careful treatment of
distilled water. It must be used within 24 hrs as it may get contaminated with microorganisms.
During manufacturing of parentrals, WFI is most commonly used, & is sterilized near the end
of the manufacturing process.
•
Test for pyrogen-free water: is made by measuring the temp. of tested animals. If the water
is pyrogenic
a
increase in body temp. of tested animals.
•
The Limulus test: is an in vitro test for pyrogen. It is more rapid, sensitive & simple than the
rabbit (in vivo) test.
•
Sterile water for injection: is used to reconstitute penicillin, ampicillin, erythromycin,…etc.
•
Oily injections have vegetable oil (e.g. linseed, cotton seed, sesame, peanut or corn oil but
never olive, castor, mineral or theobroma oil) as solvent.
•
Parentral stability: for parentral admixture (e.g. ampicillin) normal saline is more stable
(8 hrs at room temp) than 5% dextrose (4 hrs at room temp). Thus normal saline is preferred.
•
Erythromycin precipitates if reconstituted with normal saline.
•
Garamycin (Gentamycin sulfate): is one of the soluble antibiotics & is stable in aqueous
solution for 2 years; thus it is available as a solution ready for injection.
•
Dextran is a plasma expander (# extracellular fluid volume).
•
The acetonide salt: is used to improve the solubility characteristics of some drugs; e.g.
triamcinolone acetonide (Kenacort) & fluocinolone acetonide (Synalar).
•
SC injections must particularly be isotonic as these come in contact with nerve endings &
stay for a long time; otherwise they will be painful.
•
IV injections must not be in suspension form otherwise it might block the blood vessel.
•
IM injections are sometimes preferred over IV injections to avoid capillary damage.
•
Parental formulations should be:
d Pyrogen free
d Particle free
d Sterile (preserved)
d Isotonic (to prevent irritation / hemolysis)
•
Inert gases sometimes replace oxygen to improve stability of the injection. Unless otherwise
specified, they are not indicated on the label.
•
Quantities of all ingredients in parentral solution should be specified on the label including:
d Antimicrobials,
d Antioxidants
d Chelating agents
d Isotonic adjustors
N.B: pH adjustors (HCl / NaOH) are not specified as the amount needed varies between batches.
Parental Electrolytes
•
IV fluid system (Glass bottles): can be divided into 2 types based on the presence or absence
of an airway tube.
–
Baxter: utilize a plastic airway tube through the stopper to above the fluid surface when
inverted for administration.
–
Abbott: utilized a filtered airway in the administration set.
•
The isotonicity of blood is equal to 0.9% NaCl solution or 5% dextrose solution w/v.
•
Parentral electrolytes: their conc. is usually expressed in mEq.
•
Sodium Cation: is the most prevalent cation in the extracellular fluid of humans, present as
Cl-. (135 – 145 mEq / L).
•
Potassium Cation: is the most prevalent cation in the intracellular fluid of humans, present
as PO4. (3.5 – 5.5 mEq / L).
•
Potassium PO4 is used as a source of PO4 & if only K is needed use KCl or K acetate.
•
Calcium PO4 & CO3 have limited solubility & thus may precipitate in parentral admixtures.
•
To reduce the possibility of pptn in a mixture of K3 PO4 & Ca gluconate we must:
–
Lower the conc. to 20 mEq / L for each.
–
Dissolve K3 PO4 first then add Ca gluconate slowly while stirring.
•
Since K3 PO4 is available as a mixture of monobasic (KH2PO4) & dibasic (K2HPO4) it is
more suitable to express the conc. in mmoles/L (rather than mEq/L) based on K average.
•
Adults need 10 – 15 mM of phosphorous / day.
•
Ringer’s injection: is an isotonic electrolyte solution of Na+, K+, Ca++ & Cl-, in a balanced
physiologic preparation.
•
Lactated Ringer’s injection (Hartmann’s solution) is considered to be the most closely
related to the extracellular fluid of the human body.
•
Heparin Na: should not be given IM as it is painful & may cause localized haematoma.
•
Ascorbic acid injection: is highly acidic, thus alkali as NaOH, NaHCO3, Na2CO3 are used to
adjust the pH between 5.5 & 7.
•
Liposyn & Intralipid: are parentral emulsions intended to provide fatty acids. These should
be administered separately & should not be admixed with other drugs / solutions.
•
Narrow safety margin drugs: given by slow IV infusion to maintain constant therap. conc.
•
Extravascular blood (blood donation): blood is prevented from clotting by removing the
Ca++ cation by adding a mixture of citrate salts (Na, K, NH4) which will react with the Ca in
blood to form Ca citrate. Upon administration to a recipient, citrate is rapidly metabolized in
the liver releasing free Ca & blood is capable of clotting normally.
Albumin & Globulin
•
Inradermal test with gamma-globulin: will cause localized inflammation (incorrectly
interpreted as +ve reaction) & treated with epinephrine which should be available.
•
Serum globulin contains 17% gamma-globulin. (serum hepatitis is seldom reported).
•
Normal Human Serum-albumin USP 5% or 25%: is a sterile preparation of serum albumin
used to treat shock or hemorrhage. It is stable to heat & is stored at room temp.
•
Serum albumin: is a protein in plasma which controls blood volume through its water
containing capacity.
•
The label of biologicals: should specify the storage temp (2 - 8oC with few exceptions).
Types of Glass
•
The water resistance of glass containers: is measured by testing the amount of alkali
released into water (which # the pH & may $ stability).
•
Type I glass: is made of barosilicate. It is the best material; more resistant to water attack.
•
Type II glass: is specially treated with SO2 & is called treated soda-lime glass.
•
Type III glass: is typical soda-lime glass & is for non-parentral use (not for injections).
•
Leaching: means the release of a container’s ingredient into the product; e.g. Zn is released
(or leached) from a rubber closure of a vial into the drug.
•
Adsorption: When 2 substances are taken up and one is attached superficially to the other, it
is said to be adsorbed (this is a reversible process). The term is used to refer to binding of a
substance on the surface of the container.
•
Diffusion: is the passage of a substance through a 2nd substance (e.g. volatile oil or a dye
through the walls of the container).
•
Porosity: indicates small holes through which a substance can pass.
Sustained Release Formulations
•
Advantages:
–
Less frequent dosing is more convenient for patients & nurses.
–
Maintains therapeutic effect for longer period of time (vs. conventional dosage forms)
– Eliminates the fall of serum levels below the minimum effective level (MEL)  the
patient is receiving therapeutically adequate amount of the drug at all times.
–
The maxima (peaks) in drug conc. (seen with multiple dose administration of
conventional dosage) are eliminated  more economic use of the drug & $ side effects
(since higher blood levels  higher side effects).
–
Elimination of maxima decreases the total amount of drug needed to achieve MEL.
1.
Parentrals should be:
a. Sterile
2.
b. Particle free
c. Pyrogen free
In an IM injection, which is least required :
a.
Plastic
c. Pseudo-plastic
b. Dilatant (# shear stress  # viscosity  # resistance to flow)
3.
Which of the following organic solvents is used to prepare internal use injections:
a.
Glycerol
c. Alcohol
d. Acetone
b. Vegetable oil (peanut, sesame or cotton seed oil but neither olive nor theobroma oil)
4.
At the site of injection, the rate of absorption is decreased by:
a.
Friction.
c. Heating.
d. Cooling.
b. Injection of adrenaline. ( vasoconstriction  $ absorption  prolonged effect)
5.
In a parentral Rx of hormone, adrenaline is used as:
a.
6.
Vasoconstrictor.
Blood substitution after injury or surgery is with:
a. Plasma.
7.
8.
c. 5% dextrose.
Which of the following statements concerning immune serum globulin is true:
a.
immune serum globulin contains ~ 50% gamma globulin.
b.
Serum hepatitis is one of the most common reported adverse effects.
c.
Skin test should not be performed before injection.
d.
Virus infections attenuated by gamma globulin are non-infecting.
Where is Limulus amebecytes used:
a.
9.
b. 0.9% NaCl.
Test for pyrogen
The major contaminant in parentrals is from:
a.
Raw materials
b. Equipments
c. Personnel
d. Atmosphere
10. Intra-articular injection means:
a.
In the synovial fluid
b. In the joint or the synovial space
11. For the preparation of LVPs we use:
a.
Purified water for injection USP b. Sterile water for injection USP ???
12. Testosterone is sterilized by:
a.
Dry heat sterilization
b. Gas sterilization
13. To improve the stability of parentrals we use:
a.
Inert gas instead of oxygen.
14. Type II glass:
a. Is best for parentrals
b. Prepared by de-alkalizing Type III glass by SO2  more resistant to water
c.
Specially treated soda-lime glass
15. Castor oil has :
a.
Very low I2 value (almost zero)
16. Dry heat sterilization is used for:
a.
Mineral oil
b. Testosterone
17. In ethylene oxide sterilization,:
a.
You must first aireate the substance to be sterilized.
18. In parentrals, phenol is used as:
a.
Preservative (0.5%).
19. Extravasation is a problem with IV injections, it describes:
a.
Escape of blood to the surrounding tissue.
b. Escape of injected fluid to the surrounding tissue.
c.
A clot at the end of the needle.
20. Ethylene oxide sterilization:
a.
Has high penetration power for sealed plastic containers
b. Is used for the sterilization of chemical waste products
21. Where is Limulus amebecytes used:
a.
Test for pyrogen
22. The major contaminant in parentrals is from:
a.
Raw materials
b. Equipments
c. Personnel
d. Atmosphere
23. Intra-articular injection means:
a.
In the synovial fluid
b. In the joint or the synovial space
24. For the preparation of LVPs we use:
a.
Purified water for injection USP b. Sterile water for injection USP ???
25. Testosterone is sterilized by:
a.
Dry heat sterilization
b. Gas sterilization
26. To improve the stability of parentrals we use:
a.
Inert gas instead of oxygen.
Acids & Alcohol
•
Glacial acetic acid: 100% w/w. It is the highest conc. & the strongest acid.
•
Acetic acid USP: 36 – 37% w/w.
•
Diluted acetic acid: 6% w/v.
•
Phosphoric acid BNF: 85 – 88% w/w.
•
Diluted phosphoric acid: 10% w/v.
•
HCl USP: 35% w/w.
•
Absolute alcohol USP: 100% v/v ethanol.
•
Alcohol USP (grain alcohol): contains 95% ethanol (94.9% v/v = 92.3% w/w).
•
Proof alcohol: 50% v/v.
•
Dilute alcohol is 49% v/v ethanol.
•
Rubbing alcohol is 70% v/v ethanol.
•
The volume of alcohol: is determined at a temp of 15.6oC (60oF).
•
A cough syrup is labeled as containing 20% alcohol by volume, this is equivalent to 20 ml
absolute alcohol in every 100 ml of syrup.
•
Its proof strength is calculated by doubling the % v/v, thus it will be 40%.
•
Shrinkage: It occurs when alcohol is mixed with purified water & is primarily due to
hydrogen bonding (attraction forces between H atoms & electro –ve atoms as O / N /F).
•
Mineral oil is immiscible with alcohol & with castor oil.
•
Acetic acid: is used as a bladder irrigator.
•
Boric acid: is a mild antiseptic used in eye washes or in topical / vaginal preparations.
•
Tannic acid: is an astringent used in burns & wounds.
•
Undecylenic acid (Desenex): is a fungistatic agent used in treating ring worm (athlete's foot).
•
Trans-retinoic acid (Acutane) (iso-retinol): is used topically for the treatment of acne.
•
Para-amino benzoic acid (PABA): is used as a sun screen & in Enrlish test.
Antiseptics
•
Iodine solution USP: contains I2 & NaI. They react to form Na I3, a water soluble complex
(hydrotrophy) without loss of antibacterial activity.
•
Iodine Tincture & Solution: both contain 2% I2 & 2.4% NaI, but differ in the vehicle:
– The solution is prepared using purified water USP.
–
The tincture is prepared using diluted alcohol USP (49% alcohol).
•
In the Tincture: NaI is not added to help solubilize I2 in alcohol (I2 is readily soluble in
alcohol) but to prevent pptn. if water is added.
•
Official hydrogen peroxide solution: is 3% solution of H2O2; this is also called 10 volume
solution meaning that 1 ml of solution liberates 10 volumes of O2.
•
20 volume (6%) H2O2 solution: is considered too strong for medicinal use. It is used to
bleach hair & fabrics.
•
The antiseptic properties of H2O2 solution: is dependent on the catalaze enzyme which
breaks
2 H2O2  2 H2O + 2 O. The nascent oxygen oxidizes the bacterial cell.
•
Hydrogen peroxide is used in cleansing wounds & diluted 1:1 with water & used as a mouth
wash, to treat Vincent angina (Trench mouth).
•
Sodium hypochlorite solution (NaOCl): Known as Dakin’s solution (Clorox). It is a
disinfectant & not an antiseptic, because of its high alkalinity which is too strong to be
applied to living tissue.
•
Benisone Gel: contains beta-methazone benzoate (steroid) & is used as an anti-inflammatory
in dermatitis. It does not contain benzoyl peroxide. (Betnovate is beta-methazone valerate)
•
Benzoyl peroxide is used topically to treat acne.
The Law of Pharmacy Practice
•
Patients have the right to know the effects of the drug from the pharmacist.
•
When filling a Rx: to get maximum patient satisfaction, the patient should receive both oral
& written counseling (instructions).
•
Vicarious Liabilities of the pharmacist: An innocent master may be held responsible for the
harm caused to a 3rd person by the torsion acts of his servants while they are acting within the
cope of their employment, HE WHO ACTS THROUGH OTHERS, ACTS HIMSELF.
i.e. the pharmacist has responsibility of all subordinates working in the pharmacy.
•
Authorization: It is the responsibility of the pharmacist who handles this authorization.
•
Negligence: is less than average pharmacy care.
•
The main reason for keeping a low inventory is to decrease the cost of inventory.
•
The % turn over for a good business is 5%.
Anti-emetics
•
Metoclopramide (Primperan): is a dopamine antagonist that stimulates the motility of the
stomach & is used in:
–
Diabetic gastro-paresis (delayed gastric emptying) in diabetics
–
Gastro-esophageal reflux disorder (GERD)
–
Antiemetic in cancer chemotherapy where it acts through 2 mechanisms:
•
Centrally: central antiemetic effect (being a dopamine antagonist)
•
Peripheral: cholinomimetic effect
•
Chlorpromazine: a phenothiazine (major tranquilizer) is used as anti-emetic.
•
Emetrol is also used as anti-emetic.
•
Nabilone: a cannabinol used as anti-emetic for nausea & vomiting in cancer chemotherapy.
•
Anti-cancer drugs induce nausea & vomiting by stimulation of the chemoreceptor trigger
zone (CTZ) & vomiting center.
Antacids
•
Antacids relief pain. They are more effective if given 2-3 hours after meals. If given hourly
their dose must be reduced.
•
NaHCO3 (baking soda): has alkaline pH when dissolved in water, thus used as antacid. It
has poor alcohol solubility. When heated, it produces a more alkaline carbonate solution.
•
Antacids hinder the absorption of penicillin, tetracyclines, INH & iron preparations.
•
Aluminium hydroxide & magnesium hydroxide (milk of magnesia) are antacids that
hinder the absorption of penicillin & must be given 4 hrs before or after penicillin dosing.
Also hinder the absorption of tetracyclines & INH.
–
The most common side effect of Al(OH)3 is constipation.
•
Antacids should be taken 1-3 hour PC & HS: as they neutralize HCl secreted in response to
eating. They should be repeated 3-4 times daily. (PC = after meals HS = at bed time)
•
Sucralfate (Sulcrate): is used in treating duodenal ulcers, it forms a complex with ulcerated
area protecting it from gastric acids & enzymes  healing of ulcer; given before meals.
•
H2 receptor antagonists (Cimetidine): are used to treat peptic ulcers.
•
The ideal antacid is that which raises the pH of the stomach contents to ~ 3.5 - 5. This will
neutralize 90% of the acid & greatly reduce the proteolytic activity of pepsin.
–
Buffering to higher pH serves unuseful purposes.
–
At pH 4 pepsin will be completely inhibited.
Anti-diarrheals
•
Kaopectate: contains Kaolin + pectin  treats diarrhea.
•
Polycarbophil: is the safest anti-diarrheal drug. It absorbs large amounts of water leading to
stool formation. It has no effect on the digestive enzymes & nutrients. It is not absorbed.
•
Bismuth subsalicylate (Pepto-Bismol): used in chronic diarrhea, & traveler’s diarrhea; its
mechanism of action is:
•
–
Inhibit protein by local action
–
Has adsorbent properties
–
Salicylate portion has anti-diarrheal action due to inhibition of prostaglandin synthesis
which may be a mediator of intestinal secretions.
–
Blacken the stool due to inhibition of bisulphite.
–
GIT hemorrhage.
In diarrhea:
– Activated charcoal is a good adsorbent, but is not used as it has a laxative effect.
–
Kaolin & attapulgite (adsorbent clays – Mg & Al silicate) adsorb alkaloids, toxins,
bacteria; but as they also adsorb enzymes/nutrients, are only used in mild diarrhea.
Diphenoxylate (Lomotil)
Loperamide (Imodium)
•
It is a Meperidine analogue.
•
•
CNS depressant (poteniates barbiturates,
alcohol & neuroleptics).
Related to diphenoxylate & haloperidol
but is not a Meperidine analogue.
•
Should not be used for > 5 days in adults
& is not recommended for children.
No CNS depression (does not stimulate
opiate receptors).
•
No tolerance, no dependence
•
Decrease GIT propulsion.
•
Decrease GIT propulsion.
•
No analgesic activity.
•
No analgesic activity.
•
Short duration of action, given QID.
•
•
Lomotil contains diphenoxylate +
atropine to prevent its abuse as a
narcotic, thus it does not cause addiction.
More potent, rapid onset & prolonged
duration of action, given BID - TID.
•
No withdrawal symptoms.
•
Laxatives
•
MgSO4, Mg citrate, Na2HPO4, Na3PO4: laxatives with a purgative, non-systemic cathartic
effect, used to # peristalsis of intestine by # bulk of stools (laxation by osmosis, like enemas).
•
Paraffin oil is used as a lubricant cathartic (soften the stool by lubrication).
•
Sodium docusate (stool softener) is the best laxative in old age.
•
Poloxamer 188: is a surfactant, it softens the stool by reducing surface tension.
•
Bisacodyl (Dulcolax): stimulates the intestinal wall. It is manufactured as enteric coated
tablets (to avoid gastric irritation). It should not be taken within 1 hr of ingestion of milk or
antacids (as these may cause premature dissolution  gastric irritation).
•
Psyllium & Carbophils: produces bulky stool.
•
Lactulose: is a synthetic disaccharide used in the treatment of chronic constipation.
Additionally it is used to decrease NH3 from blood.
•
Senokot: is a laxative containing senna powder.
•
Some Laxatives Include:
–
Neolid: 76% castor oil in aqueous emulsion.
– Agoval: Mineral oil + phenolphthalein.
•
–
Kondremul: Mineral oil + cliondrus.
–
Petrogolar: Mineral oil in aqueous emulsion.
–
Neo cultol: chocolate flavored mineral oil jelly.
For elderly patients suffering from constipation: advise a stool softener, if found
ineffective you can advise: Moderate exercise, Warm water & Fibrous diet.
Urinary Tract
•
Cunning ham clamp: is a device used to stop urine flow in an incontinent male to prevent
nocturnal enuresis (involuntary discharge of urine during sleep).
•
Pyridium: is a red dye (azodye) used as a urinary analgesic. It causes discoloration of urine.
•
Acidification of urine can be done with NH4Cl, which, when ingested, the NH4+ dissociates
to NH3 and H+. NH3 is converted into urea which has osmotic properties. H+ is buffered & Clis filtered along with Na+, thus maintaining electrical neutrality to the extent that urinary Na+
is not replaced by H+ in renal tubules. Na+ & water are lost in urine.
•
Alkalanization of urine can be done with NaHCO3 to # excretion of phenobarbitone &
salicylates.
1. Which of the following agents is used to acidify urine (or to # excretion of an alkaline drug):
a. NH4Cl
c. Vitamin C
b. Sodium citrate
d. NaHCO3
2. Mineral oil is not used as a laxative because:
a. It interferes with the absorption of fat soluble vitamins.
b. It can cause lipid pneumonia if it gains access to the lungs.
c. It is indigestible.
3. Which agent is used in non-infective diarrhea:
a. Loperamid (Imodium).
b. Peptobismol (Bisthmus subsalicylate) ( used in traveler's diarrhea).
c. Atropine (is incorporated with diphenoxylate in Lomotil to discourage abuse).
4. Which of the following agents block or decrease the action of penicillin:
a. Probenecid
b. Salicylate
c. Aluminium hydroxide
5. A 50 year old patient makes bowl movement 3 times / week. What do you advise him to take:
a. Stimulant laxative.
b. Advise to exercise.
c. Advise to take more fiber diet.
d. Stool softener
e. Drink warm water T.I.D.
6. Which of the following is a non-systemic laxative antacid:
a. Al(OH)3.
c. Mg(OH)2.
b. NaHCO3
d. CaCO3.
7. A person comes to the pharmacist complaining of hard stool after every 2 – 3 days, what
should be advised:
a. Stool softener
c. Warm water
b. Fiber diet
d. Dulcolax
8. Gastric antacids inhibit (delay) the absorption of iron :
a. Fe 2+  Fe 3+ thus $ absorption.
9. For a patient with gastric ulcer, antacids should be given :
a. 1 hr before meals & 3-4 hrs afterwards & at bed time.
b. Maximum 7 times a day
10. Which f the following antacids causes rebound acidity:
a. CaCO3
b. Na2CO3
c. NaHCO3
11. Hexyl resorsinol (an antiseptic) is better adsorbed (more powerful) than resorsinol because:
a. It has larger molecular size.
b. It has a higher O/W partition coefficient.
12. All of the following can increase gastric secretions except:
a. Stomastatin ($ gastric secretions).
b. Protein.
13. All of the following drugs can be given with or without food except :
a. Sucralfate (must be given on empty stomach with plenty of water).
14. Which drugs must be given with plenty of water:
a. Allopurinol
b. Fosimax
c. Cotrimoxazole.
15. The antacid used in hyperphosphatemia is:
a. Al(OH)3.
c. Mg(OH)2.
16. Excessive antacid use will lead to:
a. Rebound hyperacidity (Xss antacid  # pH of stomach  # release of gastrin  #
HCl release  # acidity)
17. Chronic use of Al(OH)3 will lead to:
a. Hypophosphatemia.
b. Hyperphosphatemia
18. Mg trisilicate is used as:
a. A laxative (similar to MgSO4 & Mg(OH)2
19. What is true about mineral oil:
a. Chronic use  $ absorption of fat soluble vitamins.
b. Used as a laxative.
c. Sterilized by dry heat
c. Has slow absorption from the GIT.
20. Acne is treated by:
a. Benizone Gel.
c. Persagel
b. Benzagel
d. Desquan ???
21. Which of the following agents is bacteriostatic not bactericidal:
a. Boric acid
c. Iodine
b. Trichloro-ethanol
d. Benzalkonium chloride
22. Emetrol is:
a. Phosphate / carbohydrate solution containing levulose & dextrose & ortho
phosphoric acid with controlled pH.
b. Used to treat motion sikness
c. Given 15 – 30 ml q 15 min not more than 7 doses.
Disorders of the Thyroid Gland
•
Hyperparathyroidism (Paget’s disease): leads to decreased Ca metabolism  increased
decalcification of bone, hypercalcemia & hypophosphatemia, thus:
–
Stimulation of osteoblasts, osteocytes, chromocytes  bone dystrophy
It is treated with Calcitonin to decrease Ca++ in blood
•
Hypoparathyroidism: is a metabolic disorder of Ca metabolism in which serum Ca levels of
patient $ (hypocalcemia), & serum phosphate levels # in an inversely proportional manner.
•
Grave’s Disease: (hyperthyroidism) characterized by exophthalmoses & enlargement of
thyroid; treated by antithyroid drugs (thiouracil, propyl thiouracil, methimazole, carbimazole)
•
Mechanism of action of anti-thyroid drugs:
•
–
Inhibit organ function
–
–
Inhibit coupling of iodo-tyrosine to free tyrosine
–
Inhibit periferal deiodination of T4  T3
Inhibit oxidation of I2.
Conditions leading to hyperthyroidism include:
–
Graves Disease (Diffuse toxic goiter)
–
Plummer’s disease (Nodular toxic goiter)
–
Multi-nodular toxic goiter
–
Tri-iodo-thyronine toxicosis (T3 toxicosis)
•
Elderly patients with chronic disease should be screened for thyroid disease.
•
Myxodema (Gull’s Disease): is a disease due to hypothyroidism & is treated by L-thyroxin
(Eltroxin, Synthroid) or desicated thyroid preparation (less common).
•
Hashimato’s thyroiditis is a cause of hypothyroidism.
•
The dose of L-thyroxin is determined by:
•
–
Age, weight, height.
– Duration of hypothyroidism
–
Pretreatment TSH levels.
– Presence of other chronic disease
Myxodema is characterized by:
a. Skin dryness
c. Slow pulse
b. Loss of hair
d. Low body temp
e. Impaired mental function
•
Myoxedema coma: is a life threatening condition of hypothyroidism, treated by a loading
dose of L-throxin (400 mg IV bolus) followed by oral iodo-thyronine 25mg OD till the
patient improves, hence shift to oral L-thyroxin.
•
Lugol’s I2: a strong I2 solution taken orally as a preoperative preparation for thyroidoctomy.
It inhibits the synthesis of iodotyrosine, iodothyroxin & antagonizes the effect of thyrotropine
on endocytosis, proteolysis & thyroid hormone secretion.
•
Euthyroid: refers to a person with normal thyroid function.
1.
2.
Which of the following disorders is related to hypothyroidism:
a. Cushing syndrome.
(Increased secretion of cortisone)
b. Addison disease.
(decreased secretion of cortisone)
c. Grave disease
(Increased thyroxin secretion  exophthalmoses)
d. Myasthenia gravis
(decreased secretion of acetylcholine)
e. Myxodema or Gull’s disease
(decreased thyroxin secretion)
Mechanism of action of methimizole:
a. Inhibits iodination of tyrosine & mono-iodotyrosine
b. Inhibits coupling of iodotyrosines
3.
Hypothyroidism is due to:
a. Treatment with I 131
c. Grave’s disease
b. Hashimato’s goiter
4.
Calcitonin:
a. Decreases Ca in blood
5.
b. Increases Ca in blood
Hyperparathyroidism (Paget’s disease) leads to:
a. Decreased Ca & increased P in blood
b. Increased Ca & decreased P in blood (treated with calcitonin)
6.
Thiouracil is used to treat:
a. Graves’ disease
b. Jodbasedow’s disease ???
b. Plummer’s disease
7.
Mechanism of action of propyl thiouracil:
a. Inhibits organification of iodine
b. Inhibits conversion of T4  T3
c. Inhibits encoupling of iodotyrosine to free thyroxin
Bronchial Asthma
•
•
Selective b 2 Stimulants (also known as adrenergic anti-histaminics):
–
Salbutamol (Ventoline)
– Terbutaline (Bricanyl)
– Albuterol
–
These, being selective are better agents than isoprotrenol in treating bronchial asthma.
–
Isoprotrenol (Isoprenaline), a non-selective b-agonist, stimulates the heart  cardiac
arrest / cardiac shock. It has no a-agonist effect.
Cromolyn disodium or cromoglycate sodium (Intal inhaler):
–
Stabilizes the sensitized mast cells  $ histamine release.
–
Not effective in acute asthmatic attacks
–
Is used as a prophylactic agent in asthma
–
Is used in chronic asthma as adjuvant to cortisone
–
Is used as a prophylactic agent in allergic rhinitis.
•
Choledyl: is a partially enteric coated theophylline.
•
H1 receptor antagonists (antihistaminics): are used to treat asthma & nausea.
•
In acute asthma (status asthmaticus) & anaphylactic shock adrenaline is used.
•
Epinephrine is vasoconstrictor if used locally, it is a bronchodilator if injected SC  it is the
drug of choice for allergy-induced bronchospasm.
1.
What is the drug of choice in allergy-induced bronchospasms?
a. Adrenaline
2.
What is the drug of choice in acute asthma?
a. Adrenaline
3.
b. Salbutamol (or albuterol)
Episodic cough & wheezing that improves on treatment is:
a. Asthma
4.
b. Sodium cromoglycate
b. Chronic bronchitis
All the following factors affect asthma except:
a. Food additives
c. Staying away from dust
c. Taking inhalation regularly
5.
6.
Asthma is triggered by:
a. Smoke
c. Stress
c. Fresh painting
d. Cold weather
Cromylene disodium is used as:
a. A prophylactic agent in allergic rhinitis
7.
Shake well before use is a direction for:
a. Flovent
c. Ibrotonium (Atrovent)
c. Pulmicort (Pulmihaler)
8.
A patient on fluticasone (Flexonaze) & salmetrol has worsened asthma, advise him to:
a. Take oral cortecosteroids
c. Take inhaled corticosteroids
b. Take ibratonium
9.
Antiasthmatics (adrenergic antihistaminics) are mainly:
a. B2 agonists
3.
Episodic cough & wheezing that improves on treatment is:
a. Asthma
4.
b. B2 antagonists
b. Chronic bronchitis
All the following factors affect asthma except:
a. Food additives
c. Staying away from dust
c. Taking inhalation regularly
5.
6.
Asthma is triggered by:
a. Smoke
c. Stress
c. Fresh painting
d. Cold weather
Cromylene disodium is used as:
a. A prophylactic agent in allergic rhinitis
7.
Shake well before use is a direction for:
a. Flovent
c. Ibrotonium (Atrovent)
c. Pulmicort (Pulmihaler)
Vitamins & Minerals
•
Vitamin B complex: Consists of vitamin B1 (thiamine) + B2 (Riboflavin) + B6 (Pyridoxine) +
B12 ( cyanocobolamine).
•
Macrocytic Megaloplastic Anemia is treated by: vitamin B12 & folic acid.
•
Perinaceous anemia: failure of vitamin B12 absorption due to lack of gastric intrinsic (Castle)
factor (secreted by parietal cells of stomach & essential for absorption of B12 – the extrinsic
factor). Castle’s factor binds with ingested B12, preventing its destruction in the upper GIT.
– Parietal cells of the stomach secrete HCl & intrinsic factor.
•
Perinaceous (Addisonian) anemia is treated by vitamin B12 (IV, IM or deep SC injection).
•
Folic acid is never given alone to treat perinaceous anemia (as it will mask the symptoms).
•
Vitamin C, EDTA & Na bisulfite are used as antioxidants in aqueous solutions (EDTA is a
chelating agent for heavy metals).
•
Vitamin E (or alternatively butylated hydroxy toluene) is used as antioxidant in oily
solutions. (Anti-oxidant = reducing agent).
•
Chronic use of mineral oil decreases absorption of fat sol. vitamins
•
Vitamin K occurs in 2 forms:
–
Vitamin K1 = phytonadione  natural from plant origin.
–
Vitamin K2 = Menaquinione  natural (synthesized by G +ve bacteria).
–
Vitamin K3 = Menadione  synthetic, water soluble.
•
Warfarin inhibits vitamin K synthesis.
•
Carotene: is the precursor of vitamin A (Retinol).
•
Vitamin A (retinol): is useful in the treatment of acne vulgaris.
•
a hypovitaminosis.
–
13 trans-retinoic acid is used topically in the treatment of acne vulgaris.
–
13 cis-retinoic acid is used orally in the treatment of acne vulgaris.
Vitamin D is important for the regulation of Ca++ & P metabolism (# Ca, $ P) similar to
the parathyroid hormone. This action is opposed by calcitonin, which is used to treat
hyperparathyroidism.
Iron
•
Iron deficiency (& lead toxicity) leads to:
–
Microcytic anemia (small RBCs).
–
Hypochromic anemia (low hemoglobin content).
•
Imferon: is an iron-dextran injection (ferric hydroxide) for the treatment of iron deficiency
anemia resistant to oral iron administration.
•
Iron deficiency anemia: is more prevalent in females.
•
The best dose for iron deficiency is: 300 mg / day IM (imferon) for 6-12 months
–
Continue oral therapy after remission for 6 – 12 months.
–
Iron will cause black discoloration of the stool.
•
Iron: after oral administration is absorbed from the duodenum by an active transport process.
•
Vitamin C is added to iron preparations to enhance its absorption & also as a reducing
agent to maintain iron in the soluble ferrous state & to form a soluble absorbable chelate with
iron in the ferric state.
•
Antacids $ GIT absorption of iron, thus it is advisable to take the iron preparation 1 hr
before the antacid. Lower pH (acidity) of the intestine favors iron absorption.
•
Hemochromatosis: is the excessive storage of iron in parenchymal tissue  tissue damage,
bronzy skin, cirrhosis, diabetes mellitus.
Potassium
•
KCl is an obvious substitute for NaCl since:
d It has the same salty taste.
d
It is crystalline.
d It is an electrolyte that already exists in the body.
•
KCl is contraindicated in severe kidney disease & oligurea. It is not given by IV bolus (IV
injection of high conc. of KCl may cause cardiac arrest).
•
Symptoms of Na depletion include weakness, nausea & muscle cramps.
•
Slow K: is a potassium source. It is composed of KCl embedded in wax matrix.
•
Koachlor, Kaon & Kayciel are potassium sources too.
•
Isochlor: is not a K source. It contains 2 mg chlorpheniramine maleate + 12.5 mg pseudoephedrine HCl / teaspoonful. It is used in URTIs & bronchial congestion.
1.
Which of the following agents is keratolytic (in acne treatment):
a. Retinoic acid.
c. Retinol.
b. Vitamin C.
2.
Symptoms of perinaceous anemia are treated by:
a. Folic acid
b. Iron preparation.
b. Vitamin B12 IM / IV or SC
3.
Acne is treated by :
a. Retinoic acid
b. Retinol
c. Tocopherol acetate (Vitamin E)
4.
In iron deficiency anemia which is not true:
a. More prevalent in females.
b. Over dose can cause liver damage.
c. Causes microcytic, hypochromic anemia.
d. Oral iron preparations are better than parentral ones.
e. Oral iron preparations are similar parentral ones.
5.
Which vitamin is occasionally used as an anti-oxidant:
a. Vitamin D
d. Vitamin E
b. Vitamin K
e. Vitamin B3
c. Vitamin B1
6.
7.
Which vitamin is necessary for collagen synthesis:
a. Vitamin D
c. Vitamin C
b. Vitamin K
d. Vitamin A
Vitamin A deficiency results in:
a. Keratinization
8.
b. Night blindness
Vitamin D important for:
a. Regulation of Ca & phosphorus levels in the body (it acts as a hormone)
9.
The intrinsic factor (glycoprotein) that helps in vitamin B12 absorption is secreted from:
a. Pareital cells
b. Globet cells
10. What is the effect of antacids on iron absorption:
a. Decreases absorption
b. Increases absorption.
11. What is the effect of Vitamin C on iron absorption:
a. Decreases absorption
b. Increases absorption.
12. Which vitamin acts as a para-hormone:
a. Vitamin D3.
b. Vitamin A. c. Vitamin C.
13. Which vitamin contains a quinone structure:
a. Vitamin D
b. Vitamin E
c. Vitamin K.
b. Purine ring
c. Pyrimidine ring
14. The Structure of nicotinic acid is:
a. Pyridine ring
15. Which form of vitamin E is the most active as an anti-oxidant:
a. Alpha.
b. Beta
c. Delta.
16. Smokers suffer from deficiency of:
a. Vitamin D
b. Vitamin Cc. Vitamin E
17. Which is not true about vitamin D3:
a. Hydroxylation at C25 occurs in the liver.
18. Hypercalcemia occurs due to all except:
a. Granulomatous disease
b. #ed exposure to sun light (# vitamin D)
19. Vitamin E deficiency results in:
a. Anemia in neonates.
20. Large doses of iron leads to:
a. Liver collapse
21. Thiamine (Vitamin B1) deficiency leads to:
a. Beriberi
b. Nerve degeneration.
22. Breast fed children need which vitamin as a supplement:
a. Vitamin Drops.
23. Which is true about vitamin K:
a. Is deficient in new born
b. Is essential for synthesis of clotting factors II, VII, IX, X
c. Is essential for protein synthesis & transformation
24. Which is true about vitamins:
a. Inorganic nutrients
b. Organic nutrients that act as co-enzymes in metabolic processes
25. Which mineral (metal) is present in the body in largest amount:
a. Mg
c. Zn
b. Fe
d. Cu
Obstetrics & Gynecology
•
Terratogenisity is critical at week 3-8, 1st trimester (fetus resists terratogenisity  day 1-20).
•
Terratogenic drugs  damage to embryo: CNS, eyes, axial skeleton, lower limbs & heart.
•
The placenta is fully functioning in 2nd week, umbilical cord is formed at the 2nd – 3rd week.
•
There is no direct communication between mother’s blood & fetus.
•
Blood supply to the fetus is through the umbilical artery  providing nutrients.
•
Micronor is a contraceptive containing progestin only. It is administered daily &
continuously so long as contraception is required.
•
Ovral is a combination of estrogen + progestin & is administered on a cyclical regimen for
21 days starting from the 5th day of the menstrual cycle.
•
Progesta-sert system: is an intra-uterine device (IUD) inserted in the uterus as a
contraceptive. It undergoes zero-order release of progesterone for a 1 year period.
•
Estrogens in contraceptive pills: may cause embolism (thrombus formation).
– Smoking with oral contraception may aggravate embolism.
•
Benefits with contraceptive pills use outweigh the risks:
Benefits:
Protection from the risk of pregnancy.
Protection against iron deficiency anemia.
Alleviation of dysmenorrhea.
$ incidence of ectopic pregnancy.
Alleviation of premenstrual tension.
$ incidence of benign breast disease.
Alleviation of heavy & irregular menses.
$ incidence of ovarian & endometrial cancer.
Protection from pelvic inflammatory disease due to thickening of cervical mucous
secretion. Stronger uterine contraction prevent ascend of bacteria in uterus & fallopian tube.
Risks:
CV complications (venous thrombosis, IHD, cerebral stoke)
•
Diethyl Stelbesterol (estrogen): is used in treating senile vaginitis.
•
Premature labor: may be prevented by using terbutaline (Bricanyl), a sympathomemetic
b 2 selective agonist.
•
PGE2 + tamoxifen (Nolvadex) (anti-estrogen) are used to terminate pregnancy.
•
Pregnant women with deep venous thrombosis (DVT): can be treated only with heparin
(also used in prophylaxis of thrombosis & arterial embolism); warfarin is contraindicated.
•
Factors affecting drug excretion in breast milk:
–
PKa
–
Partition coefficient.
–
Lipid solubility.
–
Conc. of the drug.
–
Nursing schedule.
Obstetrics & Gynecology
•
The main source of newborn eye infections is from the vagina (Chlamydia)  ttt AgNO3.
•
Corpus albican: is a mass of fibrous tissue that replaces the regressing corpus luteum
following rapture of the graffian follicle. It forms a white sac which gradually decreases in
size & finally disappears.
•
Corpus albican: is present in non-pregnant women of child bearing age.
•
Corpus luteum: is present in pregnant women.
Geriatric Patients
•
In elderly patients there is a decrease in:
–
Cardiac output & Creatinin clearance & GFR.
–
Total body fluids.
–
Blood flow to various organs.
–
Plasma albumin conc. (although total plasma protein conc. does not change
significantly).
–
Muscle mass & brain weight.
–
Kidney, spleen, pancreas, lungs & liver become smaller.
–
Blood vessels lose elasticity.
Dehydration
•
Lytren: is an orally administered electrolyte solution containing dextrose (or glucose), K, Na,
Ca, Mg & Cl. It is used to supply glucose & electrolytes in balanced proportions in order to
avoid serious deficits from occurring in patients suffering from mild-to-moderate fluid loss.
1. Anti-estrogens include:
a. Clopiphene
b. Tamoxifen (also anti-cancer)
2. In post-menoposal therapy, :
a. Conjugated estrogen carries the risk of endometrial cancer.
b. Progesterone combined with estrogen reduces the chance of cancer.
c. Progesterone alone is effective but does not help vaginal itching & dryness.
3. When corpus albicans is found in the uterus, it can be said that
a. Woman is of child bearing age (Non-pregnant).
b. Woman is at puberty.
c. Woman is experiencing menopause.
d. Woman is pregnant.
4. What is Gravida:
a. It is the number of times a woman became pregnant.
5. What is the role of estrogen & progestins in managing post-menopausal symptoms esp. with
respect to bleeding:
a. Estrogen reduces bleeding.
b. Progestins reduce side effects.
6. In menopause, The management therapy includes:
a. Conjugated estrogen 0.3 – 1.25 mg/day.
7. During ovulation the secreted hormones include (reach maximum level):
a. FSH.
b. LH.
8. During Fertilization which of the following hormones has maximum effect:
a.
# levels of progesterone & estrogens (stimulate human chorionic gonadotropine).
9. Oral contraception is contra-indicated in all except:
a. Breast cancer
d. Pregnancy
g. Hypertension
b. Deep venothrombosis
e. Depression
h. Diabetes
c. Liver cirrhosis
f. Seizures / Epilepsy
10. Conjugated estrogens carry the risk of:
a. Endometrial cancer
b. Progestrone reduces the risk of estrogen
c. Progestrone affects blood vessels but is not effective in vaginal hypertrophy
11. All of the following parameters may decrease in elderly patients except:
a. Serum Creatinine
c. BUN
e. Skin hydration
b. Albumin
d. GFR
f. Lean body mass
12. The effect of oral contraceptives is decreased by:
a. Antibiotics
13. Which drug does not interact with oral contraseptives:
a. Phenytoin
c. Carbamazipime.
b. Warfarin
d. None of the above
14. Which is not true about the placenta:
a. Contains enzymes for biotransformation.
b. Contains blood vessels that transfer drugs & nutrients.
15. Clomiphen:
a. Increases the secretion of LH, GH, FSH from anterior pituitary & adrenal glands.
b. Blocks estrogen receptors in the hypothalamus (anti-estrogen)
16. In post-menopausal therapy, the use of:
a. Estrogen alone # possibility of carcinoma
b. Progesterone alone may not prevent symptoms.
c. Estrogen + progesterone prevents the development of cancer.
17. Side effects of oral contraceptives include:
a. Fluid retention.
c. Depression
b. Hypotension & CV problems
d. Acne
e. Diarrhea
18. Which of the following hormones is used in menopose:
a. Progesterone + estrogens.
19. In menopose:
a. Estrogen & progestrone are given to guard against side effects of $ estrogen
b. To guard against cancer
c. To guard against bleeding
20. Which is not contraindicated with oral contraceptives:
a. Warfarin
b. Antibiotics
c. Phenytoin
21. All of the following parameters may decrease in elderly patients except:
a. Serum Creatinine
c. BUN
e. Skin hydration
b. Albumin
d. GFR
f. Lean body mass
Balance Tests
–
Arm Ratio: to confirm that the 2 arms of the balance are equal in length.
–
Rider test: to confirm the accuracy of the calibrated beam or dial at both 500 mg & 1 g
positions.
–
Shift test: to check the balance construction especially arm & lever.
–
Sensitivity requirements: sensitivity is the minimum wt. that will shift the indicator
point 1 unit or mark.
–
Sensitivity requirement = minimum weight that can be weighed X permissible error
–
SR for class A is 6 mg; SR for class B is 30 mg.
•
The rest point: where the indicator stops & this can be shifted by adjusting the leveling
screws. This is not a balance test.
•
The accuracy of weights is expressed in tolerance that are +ve or –ve deviation from the
stated wt.
•
–
Class Q weights have tolerance smaller than the sensitivity requirements of class A
balance. These are used in pharmacy.
–
Class P weights: are more accurate than Q, used in balance tests & to check other wts.
–
P > Q > A >B
National bureau of standards (NBS): specifies that:
–
A measure shall have an initial interval of not less than 1/5 nor more than 1/4 of the
capacity of the graduate. E.g. 100 ml graduated measure, the initial intervals should be
20 ml or 25 ml.
– Measures holding 10 ml or less should be cylindrical & not conical (less accurate).
•
Protect from light: indicates storage in a light resistant container that reduces light
transmission in the range of 290 – 450 nanometer. Amber glass or plastic are suitable.
•
Expiry date: means the length of time in which the product should continue to meet the
specified requirements. If the expiry date is June 2005, this means dispensing the drug before
June 30, 2005.
•
20 capsule of drug are weighed individually & average is calculated. Requirements are met if:
– each individual capsule is within 90 -110% of the average wt.
–
Not > 2 of the net content (powder) have difference > 10% of the average net contents.
–
No one case has difference greater than 25%.
•
25oC is the official temp USP, while the national bureau of standards utilizes 20oK.
•
The BNF warning statement “caution” emphasizes the caustic nature of the solution & the
irritating properties of its vapor; e.g. strong NH3 solution the bottle must be cooled before
opening & covered with a cloth while opening.
1.
The capacity of a buffer to resist changes in pH upon addition of a strong acid or a strong
base is due to:
a. Common ion effect
b. [K] equilibrium remains constant & the reaction shifts towards reactants
c. [K] equilibrium remains constant & the reaction shifts towards products
2.
All of the following properties are classified as colligative properties except:
a. Elevation of boiling point
d. Osmotic pressure
b. Increased conductivity
e. Lowering of freezing point
c. Magnitude of vapor pressure
3.
The colligative properties of a solution are related to:
a. Total number of solute particles
d. pH
b. Ratio of number of ions to number of molecules e. Number of ions
c. Number of non-ionized molecules
4.
The colligative properties are useful in determining:
a. Tonicity of solution
d. pH
b. Solubility
e. Sterility
c. Stability
5.
The solubility of a chemical is influenced by:
b. pKa of the chemical
It is not influenced
by the valency
e. Solubility parameters
c. Volume of the chemical
f. All of the above
a. Dielectric constant
d. pH of solution
6. When the vapor pressure equals the atmospheric pressure, this is the:
a. Melting point
c. Boiling point.
b. Vaporization point.
7.
8.
Of the following agents, which is the most amphyprotic (ampholytic):
a. HCl.
c. H2SO4.
b. CH3CN.
d. Water.
e. Acetic acid.
To increase the rate of a chemical reaction:
a. Remove the resultants as soon as they are formed.
9.
What is true about pseudo-plastic flow:
a. Do not yield unless a certain shear rate is exceeded
b. Examples include gums like bentonite.
c. Follow Newton’s law of flow
10. Slow addition of precipitant with vigorous stirring of hot solution during addition gives:
a. Coarse powder difficult to filtrate.
b. Fine powder difficult to filtrate.
c. Fine powder easy to filtrate.
d. Coarse powder easy to filtrate.
11. Which of the following compounds is not a dipole:
a. CO2
b. O3
c. NH3
(covalent bond, [sharing] have zero dipole also CCl4, Cl2, H2, O2)
12. The pH equals the pKa at which point:
a. Half the neutralization point (50% ionized).
13. NH4 + OH  NH3 + H2O, According to the Bronsted Joury theory this reaction is:
a. Neutralization
b. Ionization
c. Hydrolysis
14. If A + B  AB, what will happen to the reaction rate if A decreases :
a. The reaction rate will decrease.
15. In competitive antagonism, increasing the amount of substrate will:
a.
$ the rate of the reaction
b. # the rate of the reaction
16. The rate of forward reaction decreases when: CH3COOH + H2O D CH3COO- + H3O+
a. Acetic acid is depleted
b. More H3O+ ions are produced.
17. In an azeotropic mixture of 2 volatile liquids, if the azeotrope has higher vapor pressure than
the individual components, then the azeotrope will :
a. Distill slower
b. Distill faster
18. 2 solids melting when mixed at room temperature
a. Eutectics
b. Colloids
c. Crystalloid
19. Removal of a competitive antagonist (inhibitor) from a reaction results in:
a. Increased rate of reaction
b. Decreased rate of reaction
20. In competitive antagonism, increasing the amount of substrate will results in:
a. Increased rate of reaction
b. Decreased rate of reaction
21. When pH = pKa, what % of drug is ionized:
a. 50%
b. 100%
c. 90%
22. The separation of 2 miscible liquids can be done by:
a. Centrifugation & a separating funnel
b. Fractional distillation
23. Co-pptn is due to:
a. Rapidly adding a solvent
b. Rapid cooling
24. Dipole bond exists between:
a. Water & alcohol.
c. Alcohol & alcohol.
b. Ester & ester.
d. Amino-acid & amino acid
25. To obtain the desired pH, what should be added to a salt of weak acid:
a. Salt of weak acid
c. Weak acid
b. Salt of strong acid
26. Benzocaine & caffeine from:
a. A complex.
b. Ion dipole ?????
27. A+B- + A+ this is called:
a. Common ion effect
b. Ionization
c. Hydrolysis
28. Zeta potential is present at:
a. The interface between solid & liquid.
29. For a sparingly soluble compound A+B-, the addition of A+ to the solution will:
a.
$ the solubility
b. Not affect the solubility
30. At the boiling point:
a. The vapor pressure is equal to the atmospheric pressure.
31. Thermodynamic flow is:
a. 2nd flow
b. 1st flow
32. A non-newtonian liquid which exhibits decreased flow rate with increased shearing force is:
a. Dilatant
b. Plastic
33. Bronsted Lowery theory describes:
a. Ionization
34. Oslow’s ripening law states that:
a. Large crystals will increase in size at the expense of smaller crystals
35. Surface tension is:
a. The tendency of a liquid to have the smallest surface area
36. Phenol coefficient is:
a. ???
37. The surface area of a powder can be determined by:
a. Sieving
c. Microscopic examination
b. Adsorption
38. NH3 + HCl  NH4Cl, addition of more NH3 will lead to:
a. Formation of more NH4Cl
b. No Effect ???
39. Electron withdrawing groups have:
a. Low pKa.
b. High pKa
40. What are the characteristics of polymers in matrix diffusion:
a. Salting in / out
41. Fp depression of normal saline is:
b. 0.52oC
a. 0.9%.
42. No of moles =:
a. Weight / Molecular weight
43. No of m moles = :
a. Weight in mg / Molecular weight (Moles X 1000).
44. No of m osmoles =:
a.
m moles X No of ions
45. What is entropy:
a. ????
46. A drug at a dose of:
50 – 200
300
500
is 99% bound to plasma proteins
is 85% bound to plasma proteins
is 65% bound to plasma proteins
This means that:
a. AUC increases ???
c. Renal clearance increases
b. Pharmacokinetics of the drug remain linear
47. Oslow’s ripening law states that:
a. Large crystals will increase in size at the expense of smaller crystals
48. Surface tension is:
a. The tendency of a liquid to have the smallest surface area
49. Phenol coefficient is:
a. ???
50. The surface area of a powder can be determined by:
a. Sieving
b. Adsorption
c. Microscopic examination
Bioavailability
•
The relative bioavailability of various products can be evaluated by comparing their
respective “serum conc. vs. time” curves (serum level curves).
•
The relative bioavailability: is calculated by dividing the AUC of the drug (or the total
amount of drug excreted) by the respective values for the reference standard.
Relative bioavailability = AUC tab / AUC control
•
The peak serum concentration achieved in the said curve approximates the point of time
where the absorption rate = elimination rate (equilibrium is attained).
•
The absolute bioavailability (F value): the F values are calculated for drugs in their dosage
forms by comparing the AUC (or total amount of drug excreted) to the control dose of
reference of an IV bolus dose (284).
•
When comparing the absolute bioavailability of an oral dosage form relative to that of the
same dose given by IV route. It is essential that the IV dose should be given at approx. a rate
= the rate of absorption of the oral dosage form from the GIT.
(F) Value = [AUC oral / Oral dose] / [AUC IV / IV dose]
1- Peak Conc.
2- Peak Time (time of peak conc. or Tmax).
3- AUC indicates the amount of drug absorbed.
N.B: Bioavailability curves measure:
–
Rate of absorption
–
Rate of elimination
Serum Conc.
1- Peak serum conc. (Cmax)
3- AUC
2- Peak
Time
Time
•
Steady state kidney is said when the fraction of drug absorbed = fraction of drug eliminated.
•
Lipid solubility & CNS penetration: Drugs that are poorly lipid soluble & those that are
extensively ionized at the pH of blood, generally have very slow penetration through BBB &
may be eliminated from the body before achieving a significant conc. in the CNS. To
penetrate the BBB a drug must be lipophilic (lipid soluble).
•
Absorption of chewable tablets > suspension.
•
Absorption of solution > suspension > capsules > tablets > enteric coated tablets.
•
To diminish the absorption from the site of injection we use:
–
Adrenaline (as vasoconstrictor).
–
Cooling the site of injection.
•
Ancuriom: it is abnormal distribution.
•
A graph of C = Co e – kt will give a straight line with -ve slope (1st order kinetics).
States of Matter
•
Boyle’s Law: states that the volume of a gas is inversely proportional to the pressure,
provided that the temperature remains constant.
V a 1/P
•
at constant T
Charle’s Law: states that the pressure exerted by a gas is directly proportional to the absolute
temperature, provided that the volume remains constant.
P a T
at constant V
•
Avogadro’s Law: states that equal volumes of gases, under the same conditions of
temperature & pressure, contain the same number of molecules.
•
London Forces: these are weak intermolecular forces & are not true chemical bonds.
•
Van der Val Forces: is the increased attraction between molecules as the number of atoms #.
•
Dipole-Dipole interaction: is the attraction force between the +ve pole of an atom & the –ve
pole of another; H bonding is an example of this force, where a H atom serves as a bridge
between 2 electronegative atoms holding one by covalent bonding & the other by pure
electrostatic force.
H–F…H–F
(electronegative = O, N, F, Cl, Br, I )
•
Amorphous: without definite shape or visible differentiatn. in structure. No crystalline
lattice. The substance is said to be isotropic i.e. has the same properties in all directions.
–
•
Al(OH)3 gel in its amorphous form is a good antacid; however, upon aging it becomes
crystalline & less effective.
Polymorphous: existence of several crystalline forms of the same drug. They will differ in:
d
Melting point
d
X-ray diffraction
d
Stability
d
Solubility
d
IR spectra
d
Density
–
Riboflavin (vitamin B2) has 3 polymorphs with different solubility.
–
Cocoa butter (theobroma oil) exhibits polymorphism. It exists in 4 different polymorphs with different melting pts. It should not be heated > 60oC otherwise it will solidify
(metastasis form). Theobroma oil (b) is ideal for suppository bases as it melts at 34.5oC.
•
Crystaline substances have a definite melting point, crystal lattice, & are anisotropic (i.e.
have different properties in different directions) except for cubic crystals).
•
Sublimation: is the conversion of a solid to a vapor without passing through the liquid phase.
•
Hygroscopics: these are substances that have the ability of to absorb & retain moisture
(glycerol is the most hygroscopic liquid & is thus used as a humectant).
•
Efflorescents: these are substances that have the ability of to lose water (e.g. morphine SO4
looses its water of crystallization).
•
Deliquescents: these are substances that become liquids due to absorption of water from
polymorphs (e.g. cocoa butter).
•
Azeotrophy is the absence of any change in the composition of a mixture of substances when
boiled under a given pressure. Such substances are known as azeotropes.
Rheology is the study of liquids & semisolids & their behavior in the fluid state.
I- Newtonian liquid: If the shearing rate # & the viscosity
remains constant the solution is said to be a true solution
e.g. water & alcohol, & ether & diluted colloids.
II- Non-Newtonian liquids: e.g. plastic, pseudo-plastic &
dilatant.
1- Plastic liquids: All suspension like ZnO/mineral oil
ointment. They need a yield value which is the amount
of force required to breakdown the flocculating plastic
structure of the liquid (i.e. #shear stress $ viscosity
 # rate of flow i.e. shear thinning).
2- Pseudo-plastic liquids: e.g. mucilage, tragacanth, carboxymethyl cellulose (CMC) & polyvinyl pyrolidone (PVP). These do not need yield value. #shear stress $ viscosity.
N.B: Plastic liquids do not flow until a certain minimum shearing stress is applied while pseudoplastic liquids do not require this certain shearing stress to flow.
3- Dilatant: like 50% of non-flocculated suspension of K silicate & starch suspension. Also ZnO
paste. #shear stress  #viscosity (i.e. shear thickening or dilatency).
4- Thixotrophy: Is the reversal isothermal gel-solution transformation. While standing, many plastic systems form a
gel which will breakdown to form a solution if mechanical
agitation is applied. These are non-Newtonian liquids of
plastic & pseudo-plastic type (gel-sol-gel) e.g. bentonite
magma.
5- Anti-thixotrophy: is present only in dilatants (sol-gel-sol).
An eutectic mixture: is a mixture of 2 solids that melt at room temp if mixed together
(e.g. camphor + iodine or camphor + phenol).
At point X 100% of both substances A & B are melted.
•
Y is the temperature at which both A & B are 100% melted.
•
Area 1 contains melted (A+B) together with solid A.
•
Area 2 contains melted (A+B) together with solid B.
•
Area 3 (blue) contains solid A + solid B.
•
The eutectic point is the lowest temp. at which any of the
infinite possible combinations of solids A & B melts.
Or, the lowest temp. at which any of the infinite possible
combinations of 2 liquids freezes.
1
2
Y
Temp.
•
MP of B
MP of A
100% A
3
X
Conc.
100% B
•
Dissolution rate can be # by $ particle size (# surface area), # temp. or stirring
•
Critical solution temp. is the temp. above
which 2 immiscible liquids become miscible & a
homogenous solution is formed regardless of
the conc. of each liquid. E.g. phenol & water.
•
Temp.
X = the critical solution temp.
Homogenous soln.
X
Amphoteric (ampholytic) solvent: contains both +ve
& -ve charges e.g. water (H+, OH-) but not CH3COOH.
1 layer
region
2 layer
region
Conc.
•
An ampholyte is capable of functioning both as acid & base (NaH2PO4, tetracycline, water)
•
Ampheprotic solvent: is one that has weak H+ donor & H+ accepting properties (i.e. can act
as a weak acid or a weak base) e.g. water.
•
Dielectric constant: if we put an ionic reactant in a solvent with a low dielectric constant, the
rate of reaction will be slower than if we put it in a solvent with a high dielectric constant.
•
A binary System: is a system of 2 liquids that are soluble in each other in different
proportions (e.g. water & tri-ethanol).
•
Parts of solvent required for 1 part of solute:
–
Very soluble < 1
– Freely soluble 1 – 10
–
Soluble 10 - 30
– Sparingly soluble 30 – 100
–
Slightly soluble 100 - 1000
– Very slightly soluble 1000 – 10,000
–
Practically insoluble > 10,000
•
Quantitative statement of solubility: is the ml of solvent required to dissolve 1 gm of solute.
E.g. boric acid 1: 18 means that 1 gm boric acid is soluble in 18 ml of water.
•
Salting out: when water solubility of a non-electrolyte or gas is $ by adding an electrolyte.
•
Salting in: when water solubility of a non-electrolyte or gas is # by adding an electrolyte.
•
The colligative properties are the properties of a solution that depend on the No of particles
of solute & are independent on the chemical structure or nature of the solute. These include:
d Freezing point depression
d
Boiling point elevation
d Osmotic pressure
d
Decreasing vapor pressure
d Any of these properties can be used to determine the tonicity of the solution.
•
Freezing point depression: can be used to determine the m wt of a non-ionic solute. F.p
depression of 0.9% NaCl = 0.52
•
Isotonic solutions: have the same osmotic pressure of blood thus do not cause hemolysis.
•
Hypertonic solutions (having higher osmotic pressure than blood) will cause water to pass
out of RBCs resulting in shrinking & wrinkling (crenation) of cells.
•
Hypotonic solutions will cause water to pass in the cells & cause swelling & rapture with the
release of hemoglobin i.e. hemolysis.
•
In a mixture of different liquids, those with highest vapor pressure will distill first.
•
Molarity: a molar solution is a solution containing 1 gm molecular wt of solute dissolved in
1 L of solution.
•
Equimolar solutions of non-electrolytes will have the same osmotic pressure. Solutions of
the same molarity contain the same number of solute moles & thus have the same osmotic
pressure (provided that both are unionized).
•
The osmotic pressure of 0.1 molar dextrose will be half that of an equimolar solution of NaCl
(0.1 M NaCl) since, in solution, NaCl ionizes into 2 particles.
•
A solution of a single solute may have different molarities for its various ionic components.
Thus 1 M Na2CO3 will contain 2 M Na+ & 1 M CO32-.
•
Molarity changes with temp. Thus it should not be used when properties of a solution are to
be studied at various temperatures.
•
Normality: a normal solution is a solution containing 1 gm equivalent wt of solute dissolved
in 1 L of solution.
–
Equivalent wt of a substance is the wt of that substance that reacts with (or is
produced by its reaction with) 7.999 gm of O2 or 1.008 gm of H2
–
Equivalent weight = molecular wt / valency
•
Normality changes value with temp (as molarity).
•
Molality: a molal solution is a solution containing 1 gm molecular wt of solute dissolved in
1,000 gm of solution.
–
No of moles = gm of the substance / m wt
–
No of millimoles = (gm of the substance / m wt) X 1000
•
Molality does not change with temperature. Thus it is more commonly used than molarity.
•
Osmolarity is expressed in mosm/L.
•
–
mosm/L = [ (mg/L) / m wt ] X No of ions present
–
The conc. in the above formula must be in MILLIGRAMS /LITER.
Calculate the osmolarity of 0.9% NaCl solution if the m wt of NaCl is 58.5.
No of millimoles = ( gm of substance / m wt ) X 1000
= 9 / 58.5 X 1000 = 154 millimoles.
Since NaCl is ionized to 2 ions thus:
mosm / L = 154 X 2 = 308 mosm / L.
•
NaCl equivalent is the wt of NaCl that will produce the same osmotic effect as one gram of a
specified chemical.
•
Surface tension is the tendency of a liquid to have the smallest possible surface area.
•
Partition Coefficient: of a drug is the ratio of its solubility at equilibrium in a non-aqueous
solvent to its solubility in an aqueous solvent.
•
Partition coefficient: if the conc. of (x) in oil = 10, & if the conc. of (x) in water = 5
Thus, o/w partition coefficient of (x) = conc. of (x) in oil / conc. of (x) in water = 10 / 5 = 2
•
Viscosity: is the friction force that tends to retard the movement at a fluid base.
•
Viscosity follows Poiselli law:
V = volume
V = p r4 . t . DP / 8 Ln
where
r = radius of the tube
t = time
DP = Pressure difference at each side of the tube
L = length of the tube
•
From the equation, the volume of a liquid passing through the tube is directly proportional to
the radius of the tube, the time & the pressure difference between the 2 sides of the tube. It is
inversely proportional to the length of the tube & the viscosity of the liquid.
–
•
n = viscosity of the liquid
The radius of the tube has the largest effect (it is raised to the power of four).
Kinematic Viscosity: is the ratio of absolute viscosity to density, i.e.
Kinematic viscosity = Viscosity / density
•
Hydrometer: is used to measure the specific gravity (sp gr) by means of floating in a liquid.
•
Pycnometer: is a container used as a specific gravity bottle. It has a known capacity (usually
10, 25 or 100 ml); thus the weight of water it can contain is already known. The specific
gravity of a give liquid can be calculated as
weight of the liquid (contained in the pycnometer) / weight of water (already known)
•
The specific gravity can also be expressed decimally as the ratio of a volume of a given
liquid : volume of an equal weight of another liquid (taken as a standard) at the same temp.
Water is usually the standard selected for most liquids.
•
The amount of chemical adsorbed per unit of an adsorbent is a log function, thus doubling
the concentration of a chemical will not double the amount of chemical adsorbed. Adsorption
depends on the surface area of the adsorbent and the temp. as temp #, adsorption $.
The Rate Theory of Drug Reaction (Modern Occupancy or Panton Theory)
Drug ( D ) + Receptor ( R )
K1
K3
DR g Effect ( E )
K2
– An active agonist combines with the receptor, but the complex formed (DR) rapidly breaks
down to give the response & free the receptor for further combination with fresh agonist.
– An antagonist-receptor complex breaks down more slowly in such a way that fewer &
fewer receptors finally become available for the action of the agonist, thus:
• When K1 = K2  no complex is formed & K3 will be equal to zero (i.e. zero action
agonist) [equilibrium reaction].
• When K1 > K2 & K3 has a certain value (i.e. K3 is not zero) complex is formed &
competitive agonist reaction will exist.
• When K3 > K1  agonist complex is formed which is rapidly broken down to give
effect (i.e. competitive agonist).
• When K1 > K2 & K3 = zero  complex is formed & competitive antagonist reaction
will exist.
• When K2 > K1 & K3 = zero  i.e. antagonist complex is formed & non-competitive
antagonism will exist, i.e. no effect will result.
• Equilibrium reaction is the point at which: Rate of forward reaction = Rate of backward
reaction.
• Most drugs are weak electrolytes, i.e. not easily ionized.
• Drugs that are weak electrolytes exist in both ionized (salt) & non-ionized (weak acid or
weak base) forms. The extent of ionization depends on both the pKa of the weak electrolyte &
the pH of the solvent.
• The relation between the ionized & the un-ionized forms is described by the Henderson
Hasselbach equation:
– For weak acids:
pH = pKa + log [ Salt / Acid ]
– For weak bases:
pH = pKa + log [ Base / Salt ]
• The ionization constant (Kw) of water at 25oC = 1 X 107 + 1 X 107 = 1 X 1014
• Mechanism of action of a buffer system is through accepting or donating protons (common
ion effect).
• The Bronsted Lowry theory of acid-base states that acids are proton donors while bases are
proton acceptors e.g.
HCl + H2O  Cl - + H3O+
• The Lewis Theory: states that an acid is any moiety capable of accepting electrons, & a base
is any moiety capable of donating electrons.
•
Isotopes: are atomic species having the same No of protons but a different No of neutrons.
•
The radiation used for organ scanning is Gamma radiation.
•
Gamma radiation has the strongest penetration power. a & b have weaker penetration
power (a is the weakest). (g > b > a )
•
Radium (Ra 226): is never used as unsealed internal source of radiation or tracers because:
–
It has extremely long half-life.
–
Its retention time in the body is high.
•
The most commonly used radio-active isotope is cobalt (Co 57, Co 58): used to test for
vitamin B12 deficiency in perinaceous anemia.
•
Technetium (Tc 99): is considered the ideal isotope for medical applications & is
commercially available as a radio-isotope generator. Tc decay is by the emission of g-rays. It
is used to scan lung (aluminum colloid), brain (bisicate), liver (sulfur colloid), kidney
(glucoceptate colloid) & spleen. It is eliminated from lungs within 12 – 14 days.
–
Tc has a physical half-life of 6 – 12 hrs & a physiologic half-life of 30 hrs.
•
Radio-isotope generator: is an ion exchange column on which a nuclide has been adsorbed.
•
N.B: If the question is about radiations you can select a, b or g but never X-rays.
1. For the purpose of organ screening, the agent of scanning is:
a.
Gamma radiation
b.
Alpha radiation (the least penetration power)
c.
Beta radiation
d.
X-ray
N.B: If the question is on
isotopes or radiation, choose
a,b,g, but not X-rays.
2. Which is not true about Tc 99:
a.
Eliminated through the lungs within 30 days (12 – 14 days)
b.
T ½ is 6 – 12 hrs
c.
It is in the form of sodium pertecchniate.
d.
It decays by gamma radiation
e.
It is eluted in a Tc generator from radioactive decay of molybdenum 99.
3. Which is true about Tc 99:
a.
Is used for scanning lungs, liver, brain, & Kidney.
b.
It is short acting
c.
It decays by (emits) gamma radiation
1.
The most common OTC preparations used for weight control are:
a. Phenyl propanolamine.
2.
b. Benzocaine.
Mechanism of action of Orlistat (Zenical):
a. It is a potent & irreversible inhibitor of pancreatic / gastric phospholipase (carboxy
ester lipase) required for the hydrolysis of fats to free fatty acids & glycerol that
can be absorbed (phospholipase inhibitor).
3.
Mechanism of action of Sibutramine (Meridia / Reductil):
a. Inhibits the reuptake of seretonin & NE in the hypothalamus.
4.
Liver cirrhosis is considered in cases of:
a. Bleeding.
b. Ascitis.
5.
b. Jaundice
c. Hemorrhage
Symptoms of alcoholic cirrhosis include:
a. Ascitis
7.
(due to schistosomiasis or alcoholism).
Which of the following is (are) specific complication(s) of cirrhosis:
a. Ascitis
6.
c. Jaundice.
b. Jaundice (# serum bilirubin)
c. Hemorrhage (bleeding)
Which of the following is soluble in water:
a. Glucocorticoid
c. Progesterone
b. Na salt of glucocorticoid
8.
9.
Which of the following drugs is used in treating erectile dysfunction:
a. Propranolol
c. Alprostadil
b. Sildenafil
d. Papaverine
Alkaloids are:
a. Organic basic nitrogenous compounds occurring in plants.
10. Treatment of diaper rash:
a. Barrier creams / ointments (ZnO) f. Ensure nappies are changed frequently
b. Avoid tight fitting wet pants
g. Corticosteroids & antihistaminics
c. Rash may clear when left exposed to air
d. If associated with fungal infections, an antifungal (nystatin) may be helpful
e. A mild corticosteroid (HC 1%) may be useful, but treatment is limited to 1 week or less
11. Diaper rash:
a. Common in breast fed children
b. In neonates under 1 month
c. Is complicated by fungal (monilial) infections
1. A pharmacist can give the following advices except:
a. Dosage & precautions
b. Cross verify diagnosis
2. A patient on metformine wants to quit therapy & control with diet & exercise, you should:
a. Advise him to consult the physician & maintain metformine till then.
b. Assist him plan & implement the dose reduction.
c. Decrease the dose & monitor therapeutic effectiveness.
3. What documents should be submitted to a bank to open a pharmacy:
a. Premises of the pharmacy.
d. The pharmacy act.
b. Criteria of ownership
e. Portfolio of the pharmacy
c. Ontario license of the pharmacist.
4. You refer a patient to the doctor when he as:
a. Red eye
c. Blurred vision
b. Painful eye
5. P.O.S. means:
a. Point of sales
6. Inventory control benefit is:
a. 10%
b. 25%
c. 5%
7. A pharmacy manager making a written note of the various activities of the pharmacy:
a. Scope of business
8. A pharmacy manager distributing work among technicians, cashiers, …etc. is:
a. Job description
b. Job sharing
c. Obligation
9. All are patient drug problems except:
a. Improvement in patient condition upon treatment.
10. A pharmacy manager distributing work among technicians, cashiers, …etc. is:
a. Job description
b. Job sharing
c. Obligation
11. A pharmacy manager distributing work among technicians, cashiers, …etc. is:
a. Job description
b. Job sharing
c. Obligation
12. In case a pharmacist makes a mistake, the court will:
a. Send to the licensing body to prepare a report.
13. Losec 20 mg 1 BID 2 weeks. Which is a dispensing error (results from misreading):
a. Lasix 20 mg 28 tablets
b. Losec 1 tablet twice daily
c. Losec 2 tablets twice daily
14. A director who places certain rules & expects his subordinates to follow them without
exception is:
a. Autocratic
b. Bureaucratic
15. The pharmacist in a pharmacy has to take from which labor representative:
a. The collective bargaining agent.
16. A pharmacist writes job responsibilities & determines tasks, duties & qualifications needed,
this is:
a. Job description.
c. Deligation.
b. Job management.
d. Job positioning
17. The statement describing the difference between revenues & expenses is:
a. Fixed assets
c. Shareholder equity
b. Net income
18. According to the law of pharmacy practice in Canada, which is not considered as pharmacy
ownership:
a. Solo-ownership
c. Partner-ownership
b. Chain ownership
d. Franchise ???
19. Inventory control benefit is:
a. 10%
b. 25%
c. 5%
20. A pharmacy manager making a written note of the various activities of the pharmacy:
a. Scope of business
21. A pharmacy manager distributing work among technicians, cashiers, …etc. is:
a. Job description
b. Job sharing
c. Obligation
22. All are patient drug problems except:
a. Improvement in patient condition upon treatment.
23. A pharmacy manager distributing work among technicians, cashiers, …etc. is:
a. Job description
b. Job sharing
c. Obligation
24. A pharmacy manager distributing work among technicians, cashiers, …etc. is:
a. Job description
b. Job sharing
c. Obligation
25. In case a pharmacist makes a mistake, the court will:
a. Send to the licensing body to prepare a report.
26. Losec 20 mg 1 BID 2 weeks. Which is a dispensing error (results from misreading):
a. Lasix 20 mg 28 tablets
b. Losec 1 tablet twice daily
c. Losec 2 tablets twice daily