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Transcript
MINISTRY OF HEALTH OF UKRAINE
Vinnitsa National Medical Univercity after N.I.Pirogov
“Approved”
on methodological conference
Clinical pharmacy and clinical
Pharmacology department
Head of department
______prof. Yakovleva О.A.
«___»___________20___y.
Guidelines for students for practical lessons (seminar)
Academic discipline
Clinical pharmacology
Informal module №2
Subject classes № 9
Clinical pharmacology of drugs that affect the bronchial
patency. Anti-inflammatory drugs.Antibacterial drugs
Anti-inflammatory drugs.
Course
5-th
Faculty
Medical
Vinnitsya – 2013
Anti-inflammatory drugs
1. Background:
Non-steroidal anti-inflammatory drugs used to treat inflammation, reduce fever
and as anesthetics.
Inflammation is a universal reaction of the organism to the action of various
exogenous and endogenous destructive factors, which include the causative agents of
bacterial, viral and parasitic infections, and allergens, physical and chemical stimuli.
Drug eliminate inflammation by acting on the prostanoids (prostaglandins and
thromboxane). Analgesic effect associated with inhibition of the enzyme
cyclooxygenase and decreasing the synthesis of prostaglandins.
Glucorticosteroids have various effects on the body. The biological activity of
glucocorticoids can use them in the most difficult clinical situations. Often they
include a set of emergency measures of assistance in urgent situations.
Specific Tasks:
1. Analyze the causes of inflammation, the mechanism bolvogo feeling rise in body
temperature.
2. Analyze the mechanisms of action of nonsteroidal anti-inflammatory drugs that
eliminate signs of inflammation, especially depending on the selectivity.
3. To analyze the pharmacological effects of nonselective nonsteroidal antiinflammatory drugs.
4. To analyze the pharmacological effects of selective NSAIDs.
5. To analyze the pharmacological effects of highly selective non-steroidal antiinflammatory drugs.
6. To characterize the pharmacological effects of nonsteroidal anti-inflammatory
drugs.
7. Interpreting the indications for use of NSAIDs different groups.
8. Analyze the possibility of side effects of medicines to prevent them.
9. To make the algorithm of care to patients with fever, bolvomu syndrome.
10. Write down and analyze recipes for Drug, used to reduce elevated body
temperature, elimination of inflammation and reduce pain.
11. Analyze the mechanism of action and physiological effects of glucocorticoids.
12. To analyze the pharmacokinetics of natural glucocorticoids.
13. Analyze the pharmacokinetics of synthetic glucocorticoids.
14. To analyze the pharmacokinetics of inhaled glucocorticoids.
15.
Interpreting
the
evidence
and
the
administration
schedule
systemic
glucocorticoids.
16. Interpreting the evidence and the administration schedule of inhaled
glucocorticoids.
17. Analyze the contraindications and side effects of glucocorticoids.
18. To make the algorithm of care to patients with anaphylactic shock, asthmatic
status.
2.
Basic knoledges, skills, practices to study (interdisciplinary integration).
Name of previous courses
1. Latin
These skills
Section "Pharmacological and medical terminology."
Posses ability to write correct Latin names of drugs
according to grammar. Know about endings of nouns and
adjectives of different declinations in genitive case when
writing drug in recipes
2.Physiology
Section «The body temperature and its regulation»,
section «Physiology of the endocrine and respiratory
systems» - apply the knowledge in this section.
3. Biological Chemistry
Determine the role of the enzyme cyclooxygenase
and metabolism of arachidonic acid, glucocorticoids
in humans. Apply knowledge of this section when
considering the mechanisms of action of individual
drug.
4. Pharmacology
Section «Pharmacology of anti-inflammatory
drugs». Section «Pharmacology of hormonal drugs».
Apply knowledge of this section when considering
the pharmacodynamics and pharmacokinetics of the
individual drug.
3.List of base terms, parameters, characteristics that students should learn in
preparation for the lession
Term
NSAIDs
Finding
Drugs used to relieve depression and signs of inflammation,
relieve pain and fever. For the treatment of patients using drugs
of different chemical groups.
COX
Enzymes that involved in the formation of prostaglandins from
arachidonic acid. Inhibition of this enzyme leads to increased
utilization of arachidonic acid by lipoxygenase path and
improve formation leukotrienes and limit exudation.
Aspirin-induced The result of preferential formation of leukotrienes and
asthma
thromboxane A2 from arachidonic acid. In the case of this
complication prescribe ozagrelya hydrochloride, the decrease of
formation tromboxane synthetase, reduces the formation of
thromboxane A2.
Reye's syndrome Toxic encephalopathy, acute fatty degeneration of the liver,
brain and kidney.
Glucocorticoids
group of drugs that are structural and functional analogs of
hormones that are synthesized in zona fasciculata of the adrenal
cortex.
Pulse-therapy
scheme ultrahigh doses of corticosteroids administration for shortterm patients with severe and life threatening diseases or
conditions (eg, systemic collagen, vasculitis, severe rheumatoid
arthritis with a lesion of the internal orgnans, multiple sclerosis).
Drug of choice is methylprednisolone.
Chronotherapy Section of Medicine, which is based on the improvement of
patient care by reducing the one-time, daily, course of doses of
medicines, reducing the severity of side effects, taking into
account the variability of pharmacodynamic, pharmacokinetic
parameters, depending on the time factor (period of day, month,
season, etc.).
4. Theoretical questions to lesson.
1. Signs of inflammation, the effect on each link of inflammation.
2. Classification of non-steroidal anti-inflammatory drugs, depending on the chemical
origin, anti-inflammatory activity, analgesic activity, antipyretic activity.
3. Classification of NSAIDs according to the selectivity of action on COX.
4. The mechanism of action of nonsteroidal anti-inflammatory drugs, unlike antiinflammatory effects of GCS.
6. Pharmacological effects of nonsteroidal anti-inflammatory drugs and their practical
application in clinics.
7. The pharmacokinetics of NSAIDs.
8. The interaction of NSAIDs with drugs from other groups.
9. Side effects of NSAIDs and the ways of its treatment and prevention.
10. Indications for use of NSAIDs.
11. Criteria of evaluating the effectiveness and safety of NSAIDs.
12. Classification of glucocorticoides.
13. Regulation of the functions of the hypothalamic-pituitary-adrenal system.
14. The mechanism of action and physiological effects of glucocorticoids.
15. Pharmacokinetics of systemic and inhaled glucocorticoides.
16. Impressions and administration schedule of systemic and inhaled glucocorticoids.
17. Contraindications and side effects of glucocorticoides.
18. Interaction of glucocorticoides with drugs of other groups.
5. Practice.
This stage provides for carring out without assistance by each student following
practical work.
A. Materials for self-control
Task 1
Prescription and to hold their pharmacotherapeutic analysis (indicate group
membership, indications for use, possible complications)
1. Ibuprofen tablets
2. Diclofenac sodium intablets and capsules
3. Paracetamol in tablets and suppositories
4. Nimesulide
5. Celecoxib in tablets
6. Rofecoxib in tablets
7. Meloxicam in tablets
8. Hydrocortisone in ampule
9. Prednisolone in tablets and capsules
10. Methylprednisolone in tablets and capsules
11. Triamcinolone in tablets and capsules
12. Dexamethasone in tablets and capsules
13. Beclomethasone dipropionate for inhalation
14. Flunisolide for inhalation
15. Budesonide for inhalation
16. Fluticasone for inhalation.
Task 2
Look through the training drug collection on the subject, to determine their beloning to the
pharmacological group, and indications for use.
Task 3
Confirm the choice of the drug, its pharmaceutical form, dosage, concentration and
route of drug introduction.
1. Drug for removal of headache.
2. Drug for removal of pain in the joints.
3. Drug to lower elevated body temperature.
4. Drug for the relief of pain with radiculitis.
5. Drug of NSAIDs to contra aggregate e of the patient's coronary artery disease.
6. Drug to stimulate the closure of the open Bottalo's duct in preterm infants
provided left-right shunt.
7 Drug for emergency assistance by anaphylactic shock.
8. Drug for emergency care for asthmatic status.
9. Drug for emergency care for cerebral edema.
10. Drug for local therapy in articular syndrome.
11. Drug substitution therapy for adrenal insufficiency.
Task 4
Indicate NSAIDs:
• contraindicated for use for children
• contraindicated in pregnant women
• contraindicated in patients older through hondrotoksichnist
B. Tasks for self-control.
Task 1
Mode of action of acetylsalicylic acid:
a) Anti-inflammatory, hemostatic, uricosuric
b) Antipyretic, anti-inflammatory, fibrinolytic
c) Antipyretic, anti -inflammatory, contra -aggregate
d) Wound healing, anti -inflammatory
Task 2
NSAIDs are used for:
a) Arthritis, radiculitis, myalgia, neuritis, connective tissue diseases
b) Connective tissue diseases, neuritis, colic, toothache
c) Radiculitis, arthritis, myalgia, thrombosis, spastic states
d) Bleeding, colic
Task 3
Suppositories with anti-inflammatory, analgesic and antipyretic action:
a) Metindol, revodin, paracetamol
b) Anuzol
c) Voltaren
d) Posterizan, Ekonazol-HL
Task 4
Combined NSAIDs include:
a) Diclocaine, reopyrin
b) Reopyrin, meloxicam
c) Piroxicam, diclocaine
d) Voltaren, mefenamic acid
Task 5
For NSAIDs include:
a) Meloxicam, diclofenac sodium, analgin, paracetamol, and prednisone
b) Indomethacin, mefenamic acid, piroxicam, movalis, voltaren
c) Piroxicam, indomethacin, Sedalgin, tramadol
d) Retabolil, ephedrine hydrochloride, tramadol
Task 6
Diseases in which contraindicated the use of NSAIDs:
a) Stomach ulcer, myocardial damage, bleeding in the digestive tract
b) Stomach ulcer, diabetes, arthritis
c) Hyperacid gastritis, bleeding from the gastrointestinal tract, bronchial asthma,
stomach ulcer
d) Diabetes mellitus, myocardial infarction
Task 7
Distinctive feature of NSAIDs selective inhibitors of COX-2 is less expressed:
a) Anti-inflammatory action
b) Ulcerogenic effect
c) Antipyretic action
d) Analgesic actions
Task 8
With simultaneous use of NSAIDs and alcohol increases the risk:
a) Bronchospasm
b) Nephrotoxicity action
c) Allergic reaction
d) Ulcerogenic effect
Task 9
Of the group of anti-inflammatory action of NSAIDs during pregnancy allowed
to use:
a) Ibuprofen
b) Aspirin
c) Acetaminophen
d) Analgin
Task 10
Drugs of natural glucocorticoids are biologically inactive. Activated in the liver,
turning into hydrocortisone and have a short-term effects. In comparison with other
glucocorticoids is most pronounced mineralocorticoid action. Name the drug and the
dominant display to use it. (Answer: Cortisone)
Task 11
Natural glucocorticoid on glucocorticoid activity in 4 weaker than prednisolone at
mineralocorticoid - a few ahead of him.
Name the drug. How is not recommended to assign to patient this drug. (Answer:
Hydrocortisone)
Task 12
Drug, which is fluorinated glucocorticoids, 7 times more glucocorticoid activity
of prednisolone, has no mineralocorticoid activity. Cause significant inhibition of the
hypothalamic-pituitary-adrenal system. Call the drug, and particularly the testimony to
its destination. (Answer: Dexamethasone)
Task 13
The synthetic glucocorticoid,which in comparison with prednisolone has a few
more (20%) of glucocorticoid activity, minimal mineralocorticoid effects. Indicate the
drug, especially its use. (Answer: Methylprednisolone)
Task 14.
Adverse effects of glucocorticoids include:
a) Osteoporosis
b) Hypotension
a) Glaucoma
d) Dysphonia
d) Hyperkalemia
Task 15.
What pharmacodynamic effects typical of glucocorticoids?
E) Neutrophilic leukocytosis.
b) Increase blood pressure
a) Lymphocytopenia
c) Eosinopenia
d) Decrease in circulating blood
e) Inhibition of basal secretion of hydrochloric acid
B. Problems for self-control
The final stage - 15 min.
Active ultimate test control
The problem according to the base Krok 2 Test Center MoH Ukraine
NSAIDs
1. The patient, 46 years, with exacerbation of rheumatoid arthritis, who has spent
NSAIDs revealed leukopenia. What drug could cause this effect is most likely?
A. Ibuprofen
B. butadion
C. Meloxicam
D. Celecoxib
E. Diclofenac sodium
2. By the pharmacist asked the patient, which recommended acceptance of
acetylsalicylic acid as antiaggregants. What is the daily dose should be recommended
for continuous use?
A. 0,1-0,3
B. 0,5-1,0
C. 1,0-2,0
D. 2,0-3,0
E. More than 4,0
3. Which of the pharmacodynamic effects are not characteristic of non-steroidal
anti-inflammatory drugs?
A. Inhibition of exudative manifestations of inflammation
B. Inhibition of synthesis of interleukin-2
C. Inhibition of synthesis of thromboxane A2
D. Inhibition making macroergastic substrates
E. Inhibition of synthesis of hyaluronidase
4. What complication may arise in the prescribing of acetylsalicylic acid, a
patient with deficiency of glucose-6-phosphodiesterase?
A. Lyell’s syndrome
B. Anaphylaxis
C. Asthma
D. Intravascular hemolysis
E. Thrombocytopenic purpura
5. In the pharmacy turned a pregnant woman with a fever. Recommend safest
drug.
A. Diclofenac sodium
B. Acetylsalicylic acid
C. Paracetamol
D. Ibuprofen
E. Indomethacin
6. In the pharmacy called mother of 3 month-old baby, with a request to extradite
antipyretic drug. Which drug you recommend for a child?
A. Coldrex
B. Panadol
C. Acetylsalicylic acid
D. Indomethacin
E. Diclofenac sodium
7. A pregnant woman (III trimester), which the flu for 3 days, in order to reduce
the temperature took acetylsalicylic acid on 0,5 twice a day. What side effects may
result acetylsalicylic acid on the fetus?
A. Violation of protein metabolism
B. Teratogenic
C. Embryotoxicity
D. Violation of carbohydrate metabolism
E. Violation of fat metabolism
8. Newborn E., admitted to the neonatal center with the diagnosis: Pulmonary
hypertension, premature closure of the Strait Batalova. What kind of friend that were
applied a woman during pregnancy could cause these complications?
A. Chloroquine
B. Penicillamine
C. Vitamin E
D. Indomethacin
E. Chlorpromazine
9. Patient P., aged 38, of rheumatoid arthritis in adjuvant therapy took diclofenac
sodium 0.01 g / day. Evaluating the effectiveness of nonsteroidal anti-inflammatory
agents occurs in all except the following criteria?
A. Index nabryaklivosti sites joints
B. Power compression hand
C. Laboratory tests
D. Range of motion in joints
E. The emergence of agranulocytosis
10. The activity of cyclooxygenase can be inhibited by the application of certain
drugs. Which of them has an irreversible inhibitory effect on this enzyme?
A. norsulfazol
B. Diclofenac sodium
C. Sulfodimezin
D. Aspirin
E. Tocopherol
Glucorticosteroids
11. The woman, 38 years, 6 years suffer from asthma. Works in the room where
the walls are covered with mold. Allergy to aspirin, analginum, Tylenol. At the present
time - 4 attacks of breathlessness at night, often at night. Nasal breathing is difficult. In
the lungs, breathing weakened, dry rales on vidosi. Cutaneous allergic to house dust
samples - +, feather pillows on - "on maple and alder - +. Assign treatment with regard
to the shape and severity of the disease.
A. Deksametozon and teopek inside
B. Claritin eufillina intravenously and orally.
C. Implementation of specific desensitization to the allergen house dust and
feather pillows.
D. Ingakort to 2 inhalations, 2 times a day after preliminary inhalation
ofFenoterol.
E. Teofedrin inside and astmopent in ingalyatsyayah in attack
12. The patient, 23 years old, suffers from lupus, acute with the passage of a
primary lesion of the myocardium, kidney, esophagus, designed pathogenetic
treatment. In the analysis of blood erythrocytes - 3,8 * 102 / l, Hb - 120 g / l, WBC 2 *
109 / l, platelets - 150 * 109 / l, bilirubin - 19 mEq / liter. Select the correct Variant
treatment.
A. Prednisone - 60 mg / day
B. Cyclophosphamide 200 mg / day in a
C. Timalin - 10 mg / m daily
D. Laferon 5 million / m 2 twice a week
E. Levamisole 150 mg / day according to the scheme
13. Patient, 20 years after zhaleniya axis developed angioedema, rash on the
trunk appeared in the form of blisters, papules. Emergency aid should begin with:
A. Norepinephrine, mezaton
B. Reopolyglukine, gemodez
C. Epinephrine, prednisolone, antihistamines, drugs
D. Fresh frozen plasma, E-aminocaproic acid
E. Hypothiazid, furosemide
14. According to WHO recommendations, the daily dose of inhaled
corticosteroids for persistent mild bronchial asthma in adults is?
A. 150-300 mcg
B. 200-500 mg
C. 800-2000 mcg
D. More than 2000 mcg
15. The patient, 28 years old, 2 months after suffering from angina. Complaints
of morning stiffness, pain, proximal interphalangeal II and III of the fingers, knees,
elbows. In laboratory examination - hypochromic anemia, ESR 40 mm / h, the reaction
Vaaler-Rose 1:128. Which drug should be used for local therapy?
A. Kenalog-40
B. Afluton
C. Arteparon
D. Rumalon
E. Lidasa
16. The patient K., age 28, was admitted in serious condition in the nephrology
department, a fast-diagnosed idiopathic glomerulonephritis, nephrotic syndrome
(proteinuria of up to 12 g / day), secondary hypertension. Which of the proposed
treatment regimens must assign the patient:
A. Prednisone 1 mg / kg / day 8 weeks. + Cyclophosphamide 2 mg / kg / day for
8 weeks.
B. Trimethoprim-sulfamethoxazole 160/800 mg 2 times a day for 14 days.
C. Cefazolin 2 g / 3 times a day for 10 days.
D. Methylprednisolone 30 mg / kg (up to 3g) in / in a day NN3, then prednisone
2 mg / kg oral for 2 months.
E. Kidney.
17. Female patient, 30 years, during the year received substitution treatment
prednisolone (10 mg / day after meals) on the chronic adrenal insufficiency. Following
the discovery of focal pulmonary tuberculosis worsened appetite in zvyazku reception
than with prednisolone was stopped. The next day there adynamia, vomiting, psychotic
disorders (disorientation). Glycemia 3.1 mmol / l, blood pressure 110/80 mm Hg.
Required treatment:
A. Hydrocortisone gemisuktsinat, rn sodium chloride 0.9%, glucose 5% / drip,
treatment of tuberculosis.
B. Mineralocorticoid Drug (ftorgidrokortizon inside), ftivazid.
C. Only TB therapy with corticosteroids after removal of tuberculous
intoxication.
D. 40% rr glucose and 10% p-r sodium chloride w / jet, treatment of tuberculosis.
E. Drug potassium and specific TB treatment.
18. Patients with bronchial asthma, which for years had been treated Bekotid and
SEREVENT emerged redness and swelling of the gums, white patches on the tongue.
What could it be? What not to do ill and what to do?
A. Glossitis, stomatitis due to stimulation of the oral cavity.
B. Side effects SEREVENT. Cancel drug.
C. Allergic reaction to Bekotid. Cancel drug
D. Gribkov impression of the oral cavity as a result of prolonged use Bekotid.
Arose from the fact that the patient does not rinse your mouth after inhaling Bekotid. In
the next (after treatment of mycosis), this should be done.
E. Not associated with asthma disease. It should be thoroughly examined
patients.
19. A man aged 36, who suffers from bronchial asthma, severe persistent
currents, for 16 years and regularly took salbutamol during seizures, Formoterol 2 times
per day, Bekotid 400 mg 2 times / day, Teotard 1 time per day, there was severe
asthma. On-no: cyanosis, heart rate = 95/hv, BH = 28/hv. Dry whistling rales are heard
at a distance, auscultation - "silent" light. Condition was bought w / the introduction of
hydrocortisone and eufillina. What is the further patient treatment in the future is most
appropriate?
1. Go to hydrocortisone tablets
2. Take salbutamol regularly
3. Increase the dose of beclomethasone
4. Exchange w / introduction eufillina
5. Increase number of intakes formotorelu
20. A man aged 36, who suffers from bronchial asthma, severe persistent
currents, for 16 years and regularly took salbutamol during seizures, Formoterol 2 times
per day, Bekotid 400 mg 2 times / day, Teotard 1 time per day, there was severe
asthma. On-no: cyanosis, heart rate = 95/hv, BH = 28/hv. Dry whistling rales are heard
at a distance, auscultation - "silent" light. What type of glucocorticoid therapy is the
most shown in this situation?
A. Inhalation therapy
B. Intensive short-term
C. Alrenating therapy
D. Intermittent therapy
E. Pulse therapy
Solve a pharmacological problem (10) and write in the form of recipes
1. Drug for relieving headache.
2. Drug for removal of joint inflammation in rheumatoid arthritis.
3. Drug for reducing elevated body temperature in lactating women.
4. Antiagregantnymi effect of NSAIDs.
5. Drug for the elimination of acute inflammation in gouty arthritis.
6. Highly selective NSAIDs for the treatment of inflammation in patients with
stomach ulcer in the anamnesis.
7. Highly selective NSAIDs, caution should be taken for the elderly with
cardiovascular pathology.
8. Gel to relieve pain syndrome of the cervical spine with pain and antiinflammatory effect.
9. NSAIDs for the treatment of the manifestations of dysmenorrhea.
10. Drug for the treatment of inflammation and pain in osteoarthritis.
11. Drug group of SCS to provide emergency assistance in anaphylactic shock.
12. Glucorticosteroid for emergency care of asthmatic status.
13. Glucorticosteroid for emergency care of cerebral edema.
14. Glucorticosteroid for local therapy of articular syndrome.
15. Glucorticosteroid for substitution therapy of adrenal insufficiency.
At the end of the session to review and analysis of our results with the exhibiting
relevant points and assessment.
Algorithm for evaluating students' knowledge
1. Baseline knowledge
2. The final level of knowledge.
- Tests for KROK-2
- Prescribing of recipes and solving of pharmacological problems
3. Situational problem
Students learning activities assess by a 4-point traditional scale, which then
converted into points by «Scale convertion of traditional marks in rating points for
discipline that finish by final module control», approved by Academic Council of
VNMU.
1.
2.
3.
Recommended literature:
Basic & Clinical Pharmacology/ edited by Bertram G. Katzung. - 10th edition. –
USA, 2007.
Goodman & Gilman's the pharmacological basis of therapeutics / edited by
Laurence L. brunton. - 11th ed. – USA, 2006.
Color atlas of Pharmacology/ edited by Heinz Lullmann, Klaus Mohr, Albrecht
Ziegler, Detlef Bieger. - 2nd edition. - New York, 2000.