PowerPoint PresentationDefinitionsSlide 3History of PharmacologySlide 5HomeopathySlide 7Slide 8Slide 9New Drug DiscoverySlide 11Slide 12Slide 13Patent Protection of new DrugsOrphan DrugsDrug NomenclatureDrug ApprovalSlide 18Slide 19Drug QualityDrug EfficacyDrug Efficacy - Dietary Supplements?Slide 23CosmeticsEstablishing Safety and EfficacyPreclinical StudiesSlide 27Slide 28Toxicity TestingSlide 30Slide 31Slide 32Premarketing Clinical Studies: Phase I-III TrialsPhase I StudiesSlide 35Phase II StudiesPhase III StudiesSlide 38Slide 39Phase IV studies:Adverse Reactions to DrugsBIMM118“One of the features which is thought to distinguish man from other animals is his desire to take medicines”(Sir William Osler, 1849-1919)QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118Definitions•Pharmacology is the science of the interaction of chemicals with living systems at all levels•Pharmacokinetics investigates the effects of the biological system on drugs (absorption, distribution, elimination…)•Pharmacodynamics describes the fundamental action of a drug on a physiological, biochemical or molecular level •Pharmacogenetics examines the effects of genetic factors to variations in the drug response (“Asian Flush”, Codeine “resistance”)•Toxicology studies the undesirable effects of chemicals on living systems (includes poisons, antidotes and unwanted side effects of drugs)•Pharmacy is the art of preparing, compounding and dispensing chemicals for medicinal useBIMM118Definitions•Prophylactic refers to a drug or procedure aimed to prevent disease•Palliative refers to a drug or procedure aimed to relieve symptoms•Therapeutic refers to a drug or procedure aimed to cure disease•Tolerance is the increased resistance to the usual effects of an established dose of a particular drug•Effective dose (ED50) is the concentration at which 50% of the subject show a predefined response•Efficacy refers to the inherent capability of a drug to produce a desired effect•Potency compares the relative effectiveness of drugs to produce a desired effecte.g. Drug A requires fewer milligrams than Drug B to achieve the same pharmacological response --> Drug A has the higher potency, yet, both drugs have the same efficacy.BIMM118History of Pharmacology•Initially most medicines were of botanical or zoological origin•Since 1950’s, large increase in synthetic organic chemicals•Recent introduction of recombinant DNA technology has extended synthesis to molecules of human originQuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118History of Pharmacology•Early agents were naturally occurring inorganic salts and plant alkaloids–Opium –Foxglove–Mercury, arsenic or lead compounds•Most ineffective or actually dangerous•Standardization of dose very difficult–Narrow therapeutic index with foxgloveQuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118Homeopathy•1790-96: Dr. Samuel Hahnemann:To discover the true mode of action by which cinchona bark cured malaria, he ingested cinchona juice twice daily for a few days. To his great astonishment, he very soon developed symptoms very similar to malarial fever.–Postulated a new principle of treatment: “Likes cure likes”–Drug is called the remedy, obtained through serial dilutions of the chemical The remedy is mainly extracted from the plants, animals and minerals. The medicinal extract is diluted and potentiated to such an extent that not even an atom of the mother material can be detected in the remedy by the time it reaches the 12th potency. Dilutions are done in steps. For example: In the centi scale, one drop of mother tincture is mixed with 99 drops of alcohol and shaken rigorously using pre-determined strokes. This is termed as 1c. From this, one drop is mixed with 99 drops of alcohol and is termed as 2c and so on. The higher the dilution, the more powerful the remedy. It was proposed recently that the magnetic aura of the remedy increases with potency (supposedly, this had been proven with Kirlian photography). Since the remedies are used after diluting several times, it cannot have chemical effects on the body to create a long standing side effect.QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118History of Pharmacology•Major advance in safe use of naturally derived agents was the isolation, purification and chemical characterization of the active compound:–Allowed administration of a controlled dose–Allowed administration of the active component of herbal mixtures to be given alone–Identification and characterization of active component allowed definition of mechanism of action, leading to synthesis of improved agents with greater selectivity, potency, altered duration of action, etc.BIMM118History of Pharmacology•Aspirin® - first synthetic drug–Hippocrates: pain relief treatments with powder made from the bark and leaves of the willow tree (Salix sp.)–Johann Buchner (1829): isolated Salicin as the active ingredient in Meadowsweet (Spiraea ulmaria)(hydrolyzed into glucose and Salicyl-aldehyde ->oxidyzed to Salicylic Acid)Salicylic Acid is very tough on the stomach->–Felix Hoffman (1898-9): Chemist at Bayersynthezised Acetyl-Salicylic Acid, (process discovered originally by Charles Gerhardt in 1853)and tested it on his arthritis-suffering father!–March 6, 1899: Bayer receives patent for Aspirin®–Sales today exceed 50 billion pills per yearQuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118History of Pharmacology•20th Century: Dramatic change in antimicrobial therapy–Survival of patients with severe infections with historically high mortality–Introduction of sulfonamides (Gelmo 1908: Sulfanilamide) and arsenic compounds (Ehrlich 1908/10: arsephenamine= Salvarsan) and subsequently penicillins (Fleming 1928/29)QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.QuickTime™ and aTIFF (LZW) decompressorare needed to see this picture.BIMM118New Drug Discovery•Analogues to existing drugs–Usually shows only minor changes in potency, absorption, duration of action•New applications for existing drugs–Occasionally unexpected additional properties may become evident when the compounds are tested
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