“Pharmacon / Xenobiotic” “medicine”/ “recreational drug” DISCUSSION POINTS RELATED TO DEFINITIONS The car analogy. QUERY: Drugs vs. foods? (“physiological” vs “pharmacological dose”) Drugs vs. medicines? Drugs vs. poisons? Disinfectants? (Not used on the body. ) Antiseptics?
(Often don’t enter the body. ) NOTE: In general, “medicines” normalize physiology, but any drug in excess = a “poison”. NOTE: Drugs are: 1) often organic compounds 2) often have a MW around 300 Daltons 3) often affect excitable membranes (chemical messenger systems, ion channels) 4) usually act by binding to proteins.
Definition: “Drug Receptor”, “Specific” Drug Receptor II. SUB-FIELDS OF PHARMACOLOGY 1. PHARMACOKINETICS ABSORPTION DISTRIBUTION BIOTRANSFORMATION ELIMINATION 2. PHARMACODYNAMICS MECHANISM OF ACTION III. RELATED DISCIPLINES 1. ACADEMIC BIOCHEMISTRY PHYSIOLOGY 2. REAL WORLD PHARMACOTHERAPEUTICS (THERAPEUTICS) TOXICOLOGY (Toxins are drugs. Pesticides are drugs. )
PHARMACY PHARMACEUTICAL CHEMISTRY (SARs = structure activity relationships) PHARMACOECONOMICS IV. REFERENCES / SOURCES OF INFORMATION 1. THE PHARMACOLOGICAL BASIS OF THERAPEUTICS 11th ed, Hardman et al. (eds. ) (2005):
An excellent handbook, widely used by pharmacologists and doctors. (Generally called “Goodman and Gilman” after the original editors. ) 2. COMPENDIUM OF PHARMACEUTICALS AND SPECIALTIES: Issued annually, this Canadian book is a compendium of product information supplied by the manufacturers. It also contains lists of manufacturers, addresses, etc. (Called the “CPS”. ) 3. PHYSICIANS’ DESK REFERENCE: The American version of the CPS. (Called the “PDR”. ) 4. THE MERCK INDEX: A handbook which describes the physical properties of many chemicals, including drugs.
The place to go for information on molecular weight, melting point, etc. 5. WIKIPEDIA – USE WITH CARE IV. READINGS IN THE COURSE Readings are in Principles of Medical Pharmacology (7th Ed. ), edited by Kalant et al. Chapters for reading are indicated on the lecture schedule. In general, understand what the tables and figures in the text are trying to say, but don’t memorize material in them unless I say so. Do learn the material in table 1-1 (Below). INTRODUCTION II: WHERE DO DRUGS COME FROM? / DRUG NAMES I. SOURCES OF DRUGS 1. NATURAL SOURCES (TRADITIONAL SOURCE) 1. PLANTS (Most Important) Alkaloids (the majority of drugs) Nonalkaloids.
2. ANIMALS Venoms Hormones 3. 4. 2. MINERALS MICRO-ORGANISMS CHEMICAL SYNTHESIS (no molecule in nature) Learn this table from Chapter 1: (note; eserine = physostigmine) SOURCE: Principles of Medical Pharmacology; Kalant, Grant, and Mitchell (Ed. s), Toronto: Elsevier, 2007, pp. 6. II. DRUG CLASSSIFICATION ACCORDING TO SOURCE: (Traditional Drugs) 1. CRUDE NATURAL PREPARATIONS (“galenicals”) ? opium 2.
PURE EXTRACT FROM NATURAL PREPARATIONS ? morphine 3. SEMI-SYNTHETIC ? heroin 4. PURE SYNTHETIC ? meperidine III. MODERN DRUG DEVELOPMENT (Mostly Pure Synthetics These Days – Patenting) A: DRUG SYNTHESIS/DISCOVERY.
Drug Synthesis 1. Purification from natural sources Animal Pharmacology Pharmaceutical Development Acute, Subacute, & Chronic Toxicity Human Pharmacology (Phase I) 2. Modification of existing chemical structures – change pharrmacokinetics – exploitation of side effects) Initial Clinical Trials (Phase I & II) Comparative Clinical Trials (Phase III) Controlled Marketing (Phase IV) Unrestricted Marketing 3. De novo development B: PRECLINICAL TESTING (ANIMAL Drug PHARMACOLOGY) Synthesis Animal Pharmacology Pharmaceutical Development 1. 2. IN VITRO (Test tube) IN VIVO (Animals) Acute, Subacute, & Chronic Toxicity.
Human Pharmacology (Phase I) Initial Clinical Trials (Phase I & II) Comparative Clinical Trials (Phase III) Controlled Marketing (Phase IV) Unrestricted Marketing C: CLINICAL TESTING (HUMAN PHARMACOLOGY) Drug Synthesis 1. Phase I – healthy humans in hospital Animal Pharmacology Pharmaceutical Development 2. Phase II – unhealthy humans – “open studies” Acute, Subacute, & Chronic Toxicity Human Pharmacology (Phase I) Initial Clinical Trials (Phase I & II) 3. Phase III – double blind Comparative Clinical Trials (Phase III) Controlled Marketing (Phase IV) 4. Phase IV – controlled marketing Unrestricted Marketing.
D: POST-MARKETING CONTROLS Drug Synthesis 1) manufacture – pharmacopoeia Animal Pharmacology Pharmaceutical Development Acute, Subacute, & Chronic Toxicity 2) sales – prescription – “OTC” 3) advertising – Canada – The US Human Pharmacology (Phase I) Initial Clinical Trials (Phase I & II) Comparative Clinical Trials (Phase III) Controlled Marketing (Phase IV) Unrestricted Marketing IV. DRUG NAMES (Modern Drugs) 1. 2. DRUG COMPANY CODE 3. NON-PROPRIETARY NAME (approved, official, “generic”) 4. PROPRIETARY NAME 5. V. CHEMICAL NAME COMMON/STREET NAME POINT FOR DISCUSSION: Why are new drugs so expensive?