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Lecture Aids
Pharmacology & Toxicology -PB 4503
Dr. Mike Perryman
PHARMACOLOGY LECTURE OUTLINE
I) GENERAL PRINCIPLES OF PHARMACOLOGY
A) PHARMACOLOGY - Definition
1. Subdivisions of Pharmacology
a. Pharmacodynamics
b. Pharmacokinetics
c. Pharmacotherapeutics
d. Toxicology
2. Related Fields
a. Pharmacy
b. Chemotherapy
c. Pharmacognosy
3. Related Terms
a. Drug, Medicine, Medication
b. Placebo
c. Synergism
d. Antagonism
e. Hyperactivity
f. Hyporeactivity
Tolerance
Tachyphylaxis
g. Side Effects
h. Adverse Reactions
i. Contraindications
j. Habituation
k. Addiction
l. Bioavalability
m. First-Pass effect
B) DRUG SAFETY & EFFECTIVENESS
1. Factors influencing drug safety and effectiveness
a. Patient-related factors include:
1. Weight and/or body surface area
2. Age
3. Sex
4. Physiological Variables
5. Pathological/Disease states
6. Nutritional status
7. Allergy-Hypersensitivity rxn.
8. Enzyme induction
9. Hormonal factors
10. Patient Compliance
b. Drug-related factors include:
1. Side effects/toxicity (Dyscrasias, Hepato/Nephro/Oto-, Teratogenicity, etc.)
2. Pharmacokinetic factors
3. Concomitant drugs (synergism, antagonism)
a. Iatrogenic Factors
2. Steps in Development & Evaluation of New Drugs
a. Sources of New Drugs
b. Tests in Animals
1. Ed50, LD50, TI, routes of administration
2. Toxicity (acute, subacute, chronic) evaluation
c. Tests in Man
1. Investigational New Drug (IND) permit
2. Clinical Trials: Phase I, II, III
3. Submit New Drug Application
3. Information on New Drugs and Further Evaluation
a. Package Insert
b. Physicians Desk Reference (PDR)
c. The Medical Letter
d. United States Pharmacopeia (USP)
e. Rational Drug Therapy
f. Various journals
4. Drug Nomenclature
a. Nonproprietary
b. Proprietary
C) PHARMACODYNAMICS
1. Nature and Mechanism of Drug Effects
a. Structure - Activity Relationships
b. Actions of Drugs: Physiological/Biochemical Level
2. Drug-Receptor Concept
a. Receptors
b. Drug-Receptor combinations
c. Drug-Receptor bonds (Covalent, ionic, Van der Waals)
3. Dose-Response Relationship
a. Dose-response curve (arithmetic vs. logarithmic scale)
b. Parameters of dose-response curves
(Potency, Slope, Maximal Efficacy, Variability)
c. Median Effective Dose - ED50
d. Median Lethal Dose - LD50
e. Therapeutic Index - T.I. = LD50/ED50 (margin of safety)
4. Drug Antagonism
a. Competitive vs. Non-Competitive Antagonism
b. Chemical Antagonism
c. Functional Antagonsim
D) PHARMACOKINETICS (Absorption, Distribution, Metabolism, Excretion)
1. Principles of Absorption: definition
a. Mechanisms of Absorption
1. Diffusion
2. Filtration
3. Specialized Transport
Active Transport
Facilitated Transport
4. Pinocytosis, Phagocytosis
b. Influence of pH on Drug absorption
c. Properties of biological membranes that influence drug absorption
d. Absorption of GIT (Enteral)
1. Oral
2. Sublingual / Buccal
3. Stomach & Small Intestine
4. Large Intestine
5. Rectum
e. Factors affecting GI absorption
f. Absorption from lungs (Inhalation)
g. Absorption thru skin (Transdermal)
h. Absorption thru Parenteral administration (IV, IM, S.C.)
i. Miscellaneous routes (Intraneural, Intracisternal, Intrathecal, Epidural)
j. Rate of Absorption
1. Zero-order kinetics
2. First-order kinetics
2. Principles of Drug Distribution - definition
a. Factors affecting drug distribution and concentration
1. Capillary membranes
2. Cell membranes
3. BBB
4. Placenta, Mammary gland
b. Factors affecting distribution in various compartments and tissues
1. Relative rates of blood flow
2. pH
3. Lipid solubility
4. Protein binding
5. Apparent volume of distribution
3. Principles of Drug Metabolism - definition
a. Production of active/inactive metabolites
b. Factors influencing drug metabolism
1. Stimulation and depression
2. Effects of concomittant drug use on metabolism
3. Other factors affecting drug metabolites
Age
Sex
Nutritional status
Liver disease
c. Pathways of Drug Metabolism
1. Phase I: definition
a. Hydrolysis = Ex: Esters
Amides
b. Microsomal oxidation: Ex: Acyclic oxidation
Aromatic Hydroxylation
N-Hydroxylation
Dealkylation (O-, N-, S-)
Deamination
c. Non-Microsomal oxidations: Ex: Oxidative Deamination
Monoamine Oxidase (MAO)
d. Reduction: Ex: Nitrogroups
Ketones and Aldehydes
2. Phase II: definition
a. Glucuronide formation
b. Acetylation
c. Sulfate conjugation
d. Methylation
e. Desulfuration
3. Principles of Drug Excretion - definition
1. Major Pathway
a. Mechanisms
Glomerular filtration
Passive tubular transfer
Active tubular transfer
Effect of urine pH
b. Renal Clearance of drugs
Clearance = UV / p
Inulin = GFR = 125ml / min.
2. Minor Pathways
a. Biliary Excretion
Factors affecting
Hepatobiliary circulation of a drug
b. Pulmonary Excretion
c. Excretion in sweat, milk, saliva
4. Principles of Drug Elimination - definition
First-order kinetics
Implications of first-order drug elimination
Determining blood levels based on half-life (t1/2)
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E) DRUG DELIVERY SYSTEMS
1. Oral Medications
Solutions
Suspensions
Capsules
Powders
Tablets
Lozenges
Elixir
Buccal and Sublingual
Rectal: Suppository
Topical (Ointment, Liniment)
Subcutaneous
Inhalation
Prolonged release medication (time release)
F) SYSTEMS OF MEASUREMENT
Metric: Basic units - Meter, Liter, Gram
Apothecary: Pints, quarts, gallons, pound, feet, mile
Household: Drops, teaspoon, tablespoon, cups, glasses
G) PHARMACOLOGICAL ETHICS
Five (5) R s
II) AUTONOMIC DRUGS
A) PHYSIOLOGICAL ORGANIZATION OF PERIPHERAL ANS
1) Differences between ANS and Somatic Nervous System
B) THE AUTONOMIC NERVOUS SYSTEM
1) Autonomic Ganglia
2) Pre vs. Postganglionic neurons
3) Autonomic neurotransmitters
a) Acetylcholine (Ach)
b) Epinephrine (Epi) AND Norepinephrine (NE)
4) Autonomic Receptors
a) Cholinergic
Muscarinic
Nicotinic
b) Adrenergic
Alpha 1
Beta 1
Beta 2
5) Basic effects of ANS on select neuroeffector tissues
C) THERAPEUTIC OVERVIEW OF PHARMACOLOGICAL AGENTS
Effects include: Inhibit Neurotransmitter synthesis
Promotion /Inhibition of Neurotransmitter release
Interference with Neurotransmitter storage
Inhibit neuronal re-uptake of Neurotransmitters
Inhibit Neurotransmitter metabolism
Stimulation /Blockade of Autonomic receptors
Ganglionic Blockers
D) DIRECT ACTING CHOLINOMIMETIC DRUGS (Receptor Agonists)
1) Choline esters: Acetylcholine
Bethanechol (Urecholine)
Carbachol
Mechanism of Action
Clinical Indications
Side Effects /ADR
2) Alkaloids: Pilocarpine
Muscarine
Mechanism of Action
Clinical Indications
Side Effects /ADR
E) INDIRECT ACTING CHOLINOMIMETICS (Cholinesterase Inhibitors)
1) Three Types: Carbamates (reversible)
Physostigmine (Antilirium)
Neostigmine (Prostigmin)
Quanternary Amines (reversible)
Edrophonium (Tensilon)
Organophosphates (irreversible)
Isoflurophate (Floropryl)
Chlorpyrifos
Parathion
Malathion
Soman, Sarin (nervegases)
Mechanism of Action
Clinical Indicstions
Side Effects /ADR
F) MUSCARINIC BLOCKERS
Example: Atropine (added to Lomotil, Donnatal)
Scopolamine (Transderm Scop)
Mechanism of Action
Clinical Indications
Side Effects /ADR
G) ADRENOMIMETIC DRUGS
1) Direct Acting Sympathomimetics (Agonists)
a) Nonselective: Epinephrine
Norepinephrine (Levophed)
Isoproterenol (Isuprel)
b) Alpha Agonists: Phenylephrine (Neosynephrine, Dristan)
c) Beta1 agonists: Dobutamine (Dobutrex)
d) Beta2 agonists: Albuterol (Proventil, Ventolin)
Metaproterenol (Alupent)
Terbutaline (Brethine, Bricunyl)
Ritodrine (Yutopar)
2) Indirect Acting Sympathomimetics (Agonists)
D-Amphetamine (Dexedrine, Biphetamine)
Phenylpropanolamine (Traiminic, Acutrim)
Ephedrine
Pseudoephedrine (Sudafed)
Mechanism of Action
Clinical Indications /usage
Side Effects /ADR
3) Sympatholytic Drugs (Antagonists)
a) Nonselecive Beta blockers: Propranolol (Inderal) Nadolol (Corgard)
b) Beta1 Blockers: Metoprolol (Lopressor)
Atenolol (Tenormin)
c) Alpha Blockers: Prazosin (Minipress)
Phentolamine (Regitine)
Mechanism of Action
Clinical Indications /usage
Side Effects /ADR
4) Centrally Acting Sympatholytic Drugs
Examples: Methyldopa (Aldomet)
Clonidine (Catapres)
Mechanism of Action
Clinical Indications
Side Effects /ADR
III) DRUGS AFFECTING THE CNS
A) PHYSIOLOGICAL ORGANIZATION OF CNS
1) Cellular Types: Neurons (Unipolor, Bipolar, Multipolar)
Neuroglia (Astrocytes, Oligodendrocytes, Microglia)
2)Neuronal Membrane Properties
a) Pumps
b) Channels
c) Resting Membrane Potential
3) Synaptic Transmission Properties
4) Neurotransmitters
a) Synthesis, Storage, Release, Inactivation
b) Excitatory vs. Inhibitory types
c) Postsynaptic Actions of Neurotransmitters
Cholinergic Receptors
Adrenergic Receptors
d) Neuronal Circuit Types
Hierarchical vs. Diffuse
e) Pharmacologist?s view of the brain
Class of CNS drug ?Cellular Target
B) ANTIPSYCHOTIC AGENTS (Neuroleptics)
1) Therapeutic overview
2) Classifications of Neuroleptic Agents
Phenothiazines: Chlorpromazine (Thorazine)
Trifluoperazine (Stelazine)
Thioridazine (Mellaril)
Butyrophenones: Haloperidol (Haldol)
Thioxanthenes: Thiothixene (Navane)
Mechanism of Action
Clinical Indications /Usage
Side Effects /Toxicity /Adverse Rxns.
C) AGENTS FOR MOOD-AFFECTIVE DISORDERS
1) Therapeutic Overview
2) Classification of Antidepressants
a) Tricyclics: Amitriptyline (Elavil)
Nortriptyline (Pamelor, Aventyl)
Imipramine (Toframil)
Desipramine (Norpramin)
*Clomipramine (Anafranil)
Mechanism of Action
Clinical Indications /Usage
Side Effects /ADR
b) Monoamine Oxidase Inhibitors: Phenelzine (Nardil)
Tranylcypromine(Parnate)
Mechanism of Action
Clinical Indications /Usage
Side Effects /ADR
c) Selective Serotonin Reuptake Inhibitors: Fluoxetine (Prozac)
Sertraline (Zoloft)
Paroxetine (Paxil)
Mechanism of Action
Clinical Indications /Usage
Side Effects /ADR
d) Misc. Agents
Trazodone (Desyrel)
Bupropion (Wellbutrin)
3) Antimanic Agents
Therapeutic Overview
Antimanic Drugs: Lithium salts(Eskalith, Lithonate, Lithobid)
Carbamazepine (Tegretol)
Mechanicam of Action
Clinical Indications /Usage
Side Effects /ADR
D) ANXIOLYTIC AGENTS
1) Therapeutic Overview
2) Classification of Anxiolytics
a) Benzodiazepines: Clordiazepoxide (Librium)
Diazepam (Valium)
Alprazolam (Xanax)
Lorazepam (Ativan)
Mechanism of Action
Clinical Indications /Usage
Side Effects / ADR
b) Non-Benzodiazepine: Buspirone (Buspar)
Mechanism of Action
Clinical Indications /Usage
Side Effects
E) ANTIEPILEPTIC AGENTS
1) Therapeutic overview of seizure types
2) Generalized Siezures
Tonic-Clonic (Grand Mal)
Absence (Petit Mal)
Myoclonic (Atypical Absence)
3) Antiepileptics according to seizure type
a) Both Tonic/Clonic and Simple /Complex Partial Seizures:
Carbamazepine (Tegretol)
Phenytoin (Dilantin)
Phenobarbital (Luminal)
b) Absence Seizures
Ethosuximide (Zarontin)
*Valproate (Depakene, Depakote)
c) Myoclonic: Clonazepam (Klonopin)
*Valproate (Depakene, Depakote)
Mechanism of Action
Clinical Indications /Usage
Side Effects /ADR
4) Misc. Conditions
a) Status Epilepticus
b) Febrile Seizures
F) AGENTS FOR MOVEMENT DISORDERS
1) Therapeutic Overview
2) Hypokinetic Disorders
a) Idiopathic Parkinson?s Disease
Clinical Features, Etiology, Pathology
Antiparkinsonian Agents
Carbidopa /L-DOPA (Sinemet)
Bromocriptine (Parlodel)
Benztropine (Cogentin)
Trihexyphenidyl (Artane)
b) Iatrogenic Parkinsonian Syndrome
Extrapyramidal Symptons (EPS)
3) Hyperkinetic Disorders
a) Tourette?s Syndrome
Clinical Features, Treatment
b) Huntington?s Disease
Clinical Features, Treatment
c) Myoclonus
d) Dystonias
e) Tardive Dyskinesia
f) Attention Deficit Hyperactivity Disorder
Clinical Features
Treatment: Methylphenidate (Ritalin)
Pemoline (Cylert)
G) SEDATIVE-HYPNOTIC AGENTS
1) Therapeutic Overview
a) Stages of sleep
I - IV: (NREM)
V: (REM)
b) Neurotransmitters of Sleep-Awake Cycle
c) Classification of Sleep Disorders
Insomnia
Hypersomnia
Parasomnia (Initial, Middle, Latent)
2) Treatment for Insomnia Disorders
Drug Therapy:
Benzodiazepines
1) Triazolam (Halcion)
2) Flurazepam (Dalmane)
3) Quazepam (Doral)
Barbiturates
1) Secobarbital (Seconal)
2) Amobarbital (Amytal)
Antihistamines
1) Diphenhydramine (Benadryl, Sominex)
2) Doxylamine (Unisom)
IV) OPIOID ANALGESICS
A) THERAPEUTIC OVERVIEW
1) Types of pain (Somatic vs. Visceral)
2) Opioid receptors: delta, Kappa, mu
3) Opioid peptides: Enkephalins
Endorphins
B) OPIOID ANALGESIC AGENTS
1) Primary Agonists
Morphine
Hydromorphone (Dilaudid)
Meperidine (Demerol)
Oxycodone (Percodan)
Codeine
Hydrocodone (Vicodin, Lortab)
Methadone (Dolophine)
Fentanyl (Sublimaze)
Mechanism of Action
Clinical Indications /Usage
Side Effects /ADR
2) Mixed Agonist/Antagonist Opiate Analgesics
Mentazocine (Talwin)
Butorphanol (Stadol)
Nalbuphine ( Nubain)
Mechanism of Action
Clinical Indications /Usage
Side Effects / ADR
3) Opiates used as Primary Antagonists
Naloxone (Narcan)
Neltrexone (Trexan)
Mechanism of Action
Clinical Indications /Usage
C) CLINICAL PROBELMS ASSOCIATED WITH OPIATES
Tolerance
Abuse Liability
Physical Dependence
V) GENERAL ANESTHETICS
A) THERAPEUTIC OVERVIEW
B) TYPES OF GENERAL ANESTHESIA
1) Inhalation: Methoxyflurane
Halothane
Nitrous Oxide
Mechanism of Action
MAC
Oil: Gas Partition Coefficient
Blood: Gas Partition Coefficient
Clinical Effects, ADR
2) Intravenous: Thiopental (Pentothal)
Ketamine (Ketalar)
Diazepam
Mechanism of Action
Clinical Effects / ADR
3) Local Anesthesia / Analgesia
Therapeutic Overview
Examples: Lidocaine (Xylocaine, Solarcaine)
Procaine (Novacaine)
Benzocaine (Anbesol, Auralgan, Oragel, Lanacane)
Cocaine HCI
Mechanism of Action
Clinical Indications /Usage
Side Effects / ADR
VI) ANALGESIA VIA THE NON-STEROIDAL ANTIINFLAMMATORY DRUGS (NSAIDS)
A) THERAPEUTIC OVERVIEW
B) CLINICAL INDICATIONS TO BE CONSIDERED
C) CLASSIFICATIONS of NSAIDS
1) Carboxylic acids: Acetylsalicylic Acid (ASA, aspirin)
Mechanism of Action
Clinical Inidcations
Side Effects / ADR / Toxicity
2) Propionic Acids: Ibuprofen (Motrin, Advil, Nuprin)
Ketoprofen (Orudis, Actron)
Fenoprofen (Nalfon)
Naproxen (Naprosyn, Anaprox, Aleve)
Mechanism of Action
Clinical Indications
Side Effects / ADR, Toxicity
3) Acetic acids: Indomethacin (Indocin)
Mechanism of Action
Clinical uses
Side effects
4) Misc. Agents:
Ketorolac Trimethamine (Toradol) Pyrrole Group
Mechanism of Action,
Clinical Indications
Side Effects / ADR
Phenylbutazone (Butazolidine) Pyrazolone Group
Piroxican (Feldene) Oxican Group
Mefenamic acid (Ponstel) Fenamate Group
D) AGENTS USED IN TREATMENT of GOUT
1) Clinical complications of Gout
2) Treatment of Acute Gout
3) Treatment of Chronic Gout
Probenicid (Benemid)
Mechanism of Action
Allopurinol (Zyloprim)
Mechanism of Action
Colchicine
Mechanism of Action
E) ACETAMINOPHEN (Tylenol, Tempra)
Mechanism of Action
Clinical Indications / Usage
Side Effects / ADR
Toxicity
VII) STEROIDAL ANTIINFLAMMATORY AGENTS (Adrenocorticotropic Hormones)
A) ANATOMY AND PHYSIOLOGY of ADRENAL CORTEX
B) CORTICOSTEROID SYNTHESIS
1) Glucocorticords
Cortisol (Cortogen, Cortef)
Prednisone
Triamcinolone (Aristocort, Kenalog)
Betamethasone (Diprolene, Maxivate)
Dexamethasone (Decadron)
Mechanism of Action
Clinical Indications /Uses
Side Effects /ADR
VIII) PRINCIPLES OF ANTIMICROBIAL THERAPY
A) HISTORICAL PERSPECTIVES
B) EFFECTS of ANTIBIOTICS ON CELLULAR BIOCHEMICAL PATHWAYS
Mechanisms of Action:
1) Inhibition of synthesis or damage to cell wall
2) Inhibition of synthesis or damage to cytoplasmic membrane
3) Modification in synthesis / metabolism of nucleic acids
4) Inhibition / Modification of protein synthesis
5) Modification of energy synthesis
C) FACTORS AFFECTING SELECTION OF ANTIMICROBIALS
1) Identification of Organism
2) Antimicrobial suseptibility of Organism
3) Bacteriocidal vs. Bacteriostatic
4) Host Status: Allergy History
Age
Pharmacokinetics
Renal Function
Hepatic Function
Pregnancy Status
Genetic Factors
Anatomical Siteofinfection
Host Defenses, WBC Function
5) Antimicrobial Combinations
Responses: Indifferent
Synergistic
Antagonistic
D) ANTIMICROBIAL CLASSIFICATIONS BY MECHANISM OF ACTION
1) Inhibition of Cell Wall Synthesis
a) Penicillins (Beta Lactam Antibiotics)
Narrow Spectrum: Penicillins G/V, Phenethicillin
Broad Spectrum: Ampicillin, Amoxillin, Carbenicillin
Penicillinase-Resistant: Methicillin, Naficillin, Cloxacillin, Piperacillin
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects / ADR
b) Cephalosporins (Beta Lactam Antibiotics)
Cephalexin (Keflex)
Cefadroxil (Duricef)
Cefaclor (Ceclor)
Cefzil
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects /ADR
c) Vancomycin (Vancocin)
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects / ADR
d) Bacitracin
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects / ADR
2) Inhibition /Damage to synthesis of Cytoplasmic Membrane
a) Polymixins
Polymixin B (Aerosporin)
Polymixin E (Coly-mycin)
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects /ADR
3) Inhibition of Protein Synthesis (at ribosomes)
a) Macrolides
Ex: Erthromycin (E-mycin, PCE, EES, Ery Ped)
Azythromycin (Zithromax)
Clarithromycin (Biaxin)
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects /ADR
b) Chloramphenicol (Chlormycetin)
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects / ADR
c) Lincomycin (Lincocin) and Clindamycin (Cleocin)
Source and Chemistry
Mechanism of Aaction
Pharmaco Kinetics
Clinical Indications
Side Effects /ADR
d) Tetracyclines
Ex: Tetracycline (Achromycin)
Doxycycline (Vibramycin)
Minocycline (Minocin)
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects /ADR
e) Aminoglycosides
Ex: Streptomycin
Gentamycin (Garamycin)
Kanamycin (Kantrex)
Neomycin
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects/ ADR
4) Modify Energy Metabolism in Cytoplasm (at folate cycle)
a) Sulfonamides
Sulfisoxazole (Gantrisin)
Sulfamethoxazole (Gantanol)
Sulfamethoxazole + Trimethoprim (Septra, Bactrim)
Sulfamethoxazole + Erythromycin (Pediazole)
Silver Sulfadiazine (Silvadene cream)
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects / ADR
b) Trimethoprim
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects / ADR
5) Modify Nucleic acid / DNA Synthesis
a) Nitrofurans: Nitrofurantoin (Macrodantin, Furadantin)
Nitrofurazone (Furacin)
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indicatons
Side Effects / ADR
b) Fluroquinolones
Ciprofloxacin (Cipro)
Ofloxacin (Floxin)
Cinoxacin (Cinobac)
Nalidixicacid (NegGam)
Source and Chemistry
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects / ADR
6) Methenamine Mandelate (Mandelamine)
Mechanism of Action
Pharmaco Kinetics
Clinical Indications
Side Effects / ADR
E) ANTITUBERCULOSIS AGENTS
Isoniazid (INH)
Rifampin
Ethambutol
Mechanism of Action
Clinical Indications
Side Effects / ADR
F) ANTILEPROSY AGENTS
Dapsone
Mechanism of Action
Clinical Indications
Side Effects / ADR
G) ANTIFUNGAL AGENTS
1) Dermatophytic Agents
Undecylenic acid (Desenex)
Tolnaftate (Tinactin)
Miconazole (Micatin, Monistat)
Mechanism of Action
Clinical Indications
Side Effects / ADR
2) Systemic Antifungal Agents
Griseofulvin (Fulvicin)
Amphotericin B (Fungizone)
Miconazole (Monistat)
Mechanism of Action
Clinical Indications
Side Effects / ADR
3) Candidiasis (Candida Albicans)
Mycostatin (Nystatin)
Mechanism of Action /Uses
Side Effects / ADR
H) ANTIVIRAL AGENTS
1) Amantidine (Symmetrel)
Mechanism of Action
Clinical Indications
Side Effects / ADR
2) Acyclovir (Zovirax)
Mechanism of Action
Clinical Indications
Side Effects / ADR
3) Idoxuridine (Herplex)
Mechanism of Action
Clinical Indications
Side Effects / ADR
4) Interferon (Roferon)
Mechanism of Action
Clinical Indications
Side Effects / ADR
IX) TREATMENT OF RESPIRATORY DISORDERS
A) AGENTS USED TO TREAT ASTHMA and COPD
1) Bronchodilators (Beta2 Agonists)
Albuterol (Ventolin, Proventil)
Metaproterol (Alupent)
Terbutaline (Brethine, Brethaire, Bricanyl)
Ephedrine (Primatene, Bronchaid)
Mechanism of Action
Clinical Indications
Side Effects / ADR
2) Methylxanthines
Theophylline (Theodur, Slopyllin)
Aminophylline
Mechanism of Action
Clinical Indications
Side Effects / ADR
3) Cromones
Cromolyn Sodium (Intal)
Nedocromil (Tilade)
Mechanism of Action
Clinical Indications
Side Effects / ADR
4) Inhaled Steroids
Flunisolide (Aerobid)
Beclomethasone (Vanceril, Beclovent)
Mechanism of Action
Clinical Indications
Side Effects /ADR
5) Mucolytics
Acetylcysteine (Mucomyst)
Mechanism of Action
Clinical Uses
Side Effects /ADR
B) ANTIHISTAMINES / DECONGESTANTS
1) Histamine 1 Receptor Blockers
Examples: Diphenhydramine (Benadryl)
Chlorpheniramine (Chlortrimeton)
Brompheniramine (Bromfed, Dimetapp)
Clemastine (Tavist)
Triprolidine (Actifed)
Terfenadine (Seldane)
Mechanism of Action
Clinical Indications
Side Effects / ADR
2) Nasal Decongestants
Examples: Phenylpropanolamine (Entex, Naldecon, Acutrim, Dexatrim)
Phenylephrine (Dristan, Neosynephrine)
Oxymetazoline (Afrin)
Pseudoephedrine (Sudafed)
Ephedrine
Mechanism of Action
Clinical Indications
Side Effects / ADR
3) Expectorants
Guaifenesin (Robitussin)
Iodine -Potassium Iodide
Mechanism of Action
Clinical Uses
Side Effects / ADR
4) Antitussives
Dextromethorphan (Non-Narcotic)
Codeine (Narcotic)
Hyrocodone (Narcotic)
Mechanism of Action
Clinical Indications
Side Effects / ADR
5) Combination Products
Allerest, Triaminic (Chlorpheniramine, Phenylpropanolamine)
Actifed Plus (Pyrolidine, Pseudoephedrine)
Sudafed Plus (Pseudoephedrine, Chlorpheniramine)
Nyquil: ultimate respiratory cocktail
Doxylamine
Pseudoephedrine
Guaifenesin
Dextromethorphan
Acetaminophen
Alcohol (20 proof)
X) AGENTS AFFECTING ENDOCRINE SYSTEMS
A) OVERVIEW OF ENDOCRINE SYSTEM PHYSIOLOGY
B) ENDOCRINE PATHOPHYSIOLOGY
1) Diabetes Mellitus
a) Types of Diabetes Mellitus
Insulin-Dependent D.M. (Type I, Juvenileonset)
Non-Insulin Dependent D.M.(Type II, Adultonset)
b) Clinical Features of Diabetes Mellitus
c) Clinical Emergency Situations
Diabetic Ketoacidosis
Insulin Shock
d) Hypoglycemics
Oral (Sulfonylureas)
Tolbutamide (Orinase)
Chlorpropamide (Diabinese)
Mechanism of Action
Clinical Indications
Side Effects / ADR
Parenteral
Insulin (Short, intermediate, long-acting)
Mechanism of Action
Clinical Indications
Side Effects / ADR
C) THYROID DISORDERS
1) Graves Disease (Hyperthyroidism)
a) Clinical features
b) Therapeutic Interventions
Surgery
Radioactive Iodine
Antihyperthyroid Agents
Propylthiouracil
Methimazole
Mechanism of Action
Clinical Indications
Side Effects / ADR
2) Myxedema (Hypothyroidism)
a) Clinical Features
b) Therapeutic Interventions
Liotrix (Thyrolar, Euthyroid)
Liothyronine (Cytomel, T3)
Thyroxine (Leuothyroid, Synthroid, T4)
Armour Thyroid
Mechansim of Action
Clinical Indications
Side Effects / ADR
XI) CARDIOVASCULAR AGENTS
A) Definition: BP=(CO)(PR), C)=(HR)(SV)
B) THERAPEUTIC OVERVIEW of HYPERTENSION
C) CLINICAL COMPLICATIONS
D) THERAPY
1) Non-Pharmacological
Dietary: Decrease Na, ETOH, Weight, Smoking, Saturated Fats
Activity: Increase Exercise, Biofeedback, Relaxation
2) Pharmacological (According to Organ System)
Heart, Beta blockers force /rate of CO
Peripheral Sympatholytics contraction
Kidneys, Diuretics, Blood Volume,CO
ACE inhibitors
Beta Blockers
Smooth Muscle, Peripheral Sympatholytics, Relax vascular, TPR
ACE inhibitors smooth muscle
Ca2+Channel blockers
Brain, Centrally Acting Sympatholytics, Sympathetic, CO
Beta Blockers flow, TPR
E) BETA BLOCKERS (Adrenergic Receptor Antogonists)
1) Nonselective (B1, B2)
Propranolol (Inderal)
Nadolol (Corgard)
2) Selective (B1) Firstpass effect
Atenolol (Tenormin)
Metoprolol (Lopressor)
Mechanism of Action
Clinical Indications
Side Effects / ADR
F) ALPHA BLOCKERS
Prazosin (Minipres)
Mechanism of Action
Clinical Indications
Side Effects / ADR
G) DIRECT VASODILATIORS
Hydralazine (Apresoline)
Minoxidil (Loniten, Rogaine-topical)
Diazoxide (Hyperstat)
Sodium Nitroprusside (Nipride)
Mechanism of Action
Clinical Indications
Side Effects / ADR
H) ACE INHIBITORS
Renin-Angiotensin -Aldosterone System
Examples: Captopril (Capoten)
Benazepril (Lotensin)
Mechanism of Action
Clinical Indications
Side Effects / ADR
I) CNS-ACTING SYMPATHOLYTICS
Methyldopa (Aldomet)
Clonidine (Catapres)
Mechanism of Action
Clinical Indications
Side Effects / ADR
J) PNS-ACTING SYMPATHOLYTICS
Reserpine (Serpasil)
Guanethidine (Ismelin)
Mechanism of Action
Clinical Indications
Side Effects / ADR
K) DIURETICS
1) Loop Diuretics
Furosemide (Lasix)
Bumetanide (Bumex)
Mechanism of Action
Clinical Indications
Side Effects / ADR
2) Potassium-Sparing Diuretics
Spironolactone (Aldactone)
Triamterine (Dyrenium)
Mechanism of Action
Clinical Uses
Side Effects / ADR
3) Thiazide
Chlorothiazide (Diuril)
Chlorthalidone (Hygroton)
Mechanism of Action
Clinical Uses
Side Effects / ADR
4) Carbonic Anhydrase Inhibitors
Acetazolamide (Diamox)
Mechanism of Action
Clinical Uses
Side Effects / ADR
5) Osmotic Diuretics
Mannitol
Glycerin
Mechanism of Action
Clinical Uses
Side Effects / ADR
XII) CONGESTIVE HEART FAILURE (CHF)
A) THERAPEUTIC OVERVIEW of CHF
B) DIGITALIS (Glycoside) THERAPY
Digoxin
Digitoxin
Mechanism of Action
Clinical inidcations
Side Effects / ADR
C) ANGINA PECTORIS
Therapeutic Overview of Angina
Clinical Forms: Stable
Variant (Prinzmetal?s )
Unstable
Pharmacological Interventions
1) Calcium Channel Blockers
Verapamil (Calan, Isoptin)
Nifedipine (Procardia)
Diltiazem (Cardizem)
Mechanism of Action
Clinical Indications
Side Effects / ADR
2) Vasodilators
Nitroglycerin
Isosorbide Dinitrate (Isordil)
Mechanism of Action
Clinical Indications
Side Effects / ADR
XIII) GASTROINTESTINAL AGENTS
A) THERAPEUTIC OVERVIEW
B) SUMMARY of AGENTS USED TO TREAT PEPTIC ULCER DISEASE (PUD)
1) Histamine2 Receptor Antagonists
Cimetidine (Tagamet)
Ranitidine (Zantac)
Famotidine (Pepsid)
Nizatidine (Axid)
Mechanism of Action
Clinical Indications
Side Effects / AADR
2) Mucosal Strengtheners (Protectants)
Sucralfate ( Carafate)
Mechanism of Action
Clinical Indications
Side Effects / ADR
3) Antacids
Magnesium Oxide / Hydroxide (Milk of Magnesia, Haley?s Mo)
Aluminum Hydroxide (Amphogel)
Calcium Carbonate (Tums, Rolaids)
Magaldrate (Riopan)
Magnesium Trisolate, Alum. Hydroxide (Gaviscon)
Mechanism of Action
Clinical Indications
Side Effects / Adr
4) Laxatives
Therapeutic Overview
a) Irritants / Stimulants
Phenolphthalein (Correctol, ExLax)
Castor Oil (Ricinoleicacid)
Bisacodyl (Dulcolax)
Anthraquinones
Cascara Segrada (Fletcher?s Castoria)
Senna (Senokot)
Mechanism of Action
Clinical Indications
Side Effects / ADR
b) Fecal Softeners
Docusate (Colace, Surfak)
Mineral Oil
Mechanism of Action
Clinical Indications
Side Effects /ADR
c) Bulk Laxatives
Psyllium (Metamucil, Fiberall, Perdiem)
Methylcellulose (Citrucel)
Mechanism of Action
Side Effects / ADR
d) Saline Laxatives
Magnesium Sulfate (Epsom Salts)
Magnesium Citrate
Sodium phosphate (Fleet enema)
Mechanism of Action
Side Effects / ADR
5) Antidiarrheals
a) Therapeutic Overview
b) OTC Preparations
Bismuch Subsalicylate (Pepto Bismol)
Kaolin (Kaopectate)
Loperamide (Immodium-AD)
Attapulgite (Donnagel)
Lactobacillus
c) Rx Preparations
Diphenoxylate (Lomotil)
Parapectolin (Paragoric)
Mechanism of Action
Clinical Indications
Side Effects / ADR