01 general pharmacology_history_introduction_


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01 general pharmacology_history_introduction_

  1. 1. 1GENERALPHARMACOLOGY1) HISTORY OF MEDICINE2) INTRODUCTION TO PHARMACOLOGY3) PHARMACOKINETIC•ABSORPTON•DISTRIBUTION•BIOTRANSFORMATION•ELIMINATION•CLINICAL PHARMACOKINETIC4) PHARMACODYNAMIC5) DRUG INTERACTIONS6) FACTORS THAT MODIFY DRUG ACTIONS7) CLINICAL PHARMACOLOGY8) DRUG TOXICOLOGY9) PHARMACOGENETIC10)HISTORY OF MEDICINE• As old as the history of human being• As old as the age of pain an sufferings• So, PAIN and sufferings were the first sensed alarm reactions thatdrew the attention of human being.Thus, surge was focused on how to combat with theseleading symptomsBy experience, the analgesic power of certain plants wasexplored accidentally first• HISTORICAL DEVELOPMENTa) PRE-EXPERIMENTAL PERIOD (might be up to 1789)b) EXPERIMENTAL PERIOD• PRE-XPERIMENTAL PERIOD:Depends on experience rather than experimentationMostly uses trial and error methodUnder strict influence of religious and traditional beliefsNo experimentation at allNo questioning by what, why and howCurative potential of plants was discovered accidentally
  2. 2. 2The reason of illnesses was widely believed to be due to badspirits which were dismissed from body by magiciansSO, magicians were the first medical men who were also thereligious leader who were conducting ritual ceremoniesBelief in the curative powers of plants and certainsubstances was exclusively depending upon traditionalknowledge which was empirical rather than subject tocritical examinationThe effects of Opium, Belladonnae, Rauwolfia, Digitalis,Curare etc. were discovered by experience accidentally andwere used empirically• EXPERIMENTAL PERIOD:Questioning with what, how and whyNot under religious and traditional false beliefsDepending on experimental resultsReached by revolution in the brain cortex• CHRONOLOGICAL BACKGROUNDFirst informations on opium and other curative plants appear inthe Sumerian and Egyptian manuscripts or tabletsFirst documental knowledge on drugs are deduced from EBERSPAPYRUS written in 1550 B.C.1sth. Century A.C.: DIOSCORIDES assembled that far knowndrugs in a book which is considered the first PHARMACOPEA2nd. Century A.C.: CLAUDIUS GALEN (129-200 A.C.)He says: “All is found, is in part be experience and in parttheory. Neither experience nor theory alone apt todiscover all”He described the ways to prepare drug forms from plants, eg.powder, tincture, decoction, extract etc. which are calledGALENIC PREPARATIONS.MIDDLE AGE:Orientation to polypharmacy. A pharmaceutical formpossessing more than 100 active principle in it is calledTHERIACA or TRIACADevelopment in chemistry and synthesis of newsubstances increased therapeutic facilities. Thus, newsubstances were introduced into the therapy.- John Rudolph Glauber (1604-1688): Na sulphate-Aureolus Theophrastus Bombastus (PARACELSUS)from Hochenheim (1493-1541): Iron and Arsenic- He rejected irrational medicaments ofmedieval medicine
  3. 3. 3- He prescribed chemically definedsubstances with success onlyThe influence of magic and religion (i.e. church) werecrushed down.Experimental results and rationalism became the leadingapproach for the treatment.Johan Jacob Wepfer (1620-1695) was the first toverify th pharmacologic and toxic actions of drugs byanimal experimentationSerturner isolated morphine from opium milkEmil Fisher synthesized barbital, a hypnoticPaul Ehrlich by trying more than 500 bacteria dyesand 606 newly synthesized chemicals on animals,discovered the first useful chemotherapeuticsOswald Schmiedeberg (1838-1921)-Insisted on -structure activity relationship-drug receptors-selective toxicology-With his students: T. Frazer from ScothlandLangley from EnglandP, Ehrlich from GermanyJ. Clark from EnglandWas the first a) to propose receptor theoriesb) to apply law of mass action todrug-receptor interaction-Published the first journal of pharmacologyJohn Abel, a student of O. Schmiedeberg, was the first topublish J Pharmacol Exp Ther in USAPharmacology developed within physiology aspharmacodynamic by experimentation of drugs on animalsThe first pharmacologists were in fact physiologists-Rudolph Bucheim (1846) in Dorpat Medical Facultywas appointed as pharmacology lecturer for the fist time.He investigated certain effects of atropine and ergotalkaloids.-Claud Bernard investigated the effects of curare andmorphineO. Schmiedeberg was appointed as the director ofpharmacology department in Strasburg for the first time.-Otto Loewi and Guddum improved biological essaymethods and developed comparative pharmacology-Most recently gene cloning technology was developed
  4. 4. 4By this way, pharmacology became an independent disciplinein medicine.COCLUSION: Cordial respect to those who did their bestfor human being.INTRODUCTION TO PHARMACOLOGY• PARMACOLOGY = Pharmacon + LogosDrug Scıence= Drug Science= The science that deals with the interaction of livingsystems with chemicals (endogenous or exogenous)• SUBDIVISION OF PHARMACOLOGY:1) MEDICAL PHARMACOLOGY:Deals with materials used to prevent, diagnose and treat diseases.2) PHARMACOTHERAPY:Employment of drugs for the prevention and treatment ofdiseases.Its scope: -Indications-Contraindications-Drug interactions-Rational therapy design (art of therapy planning)-Good prescribingTHERAPY: i) Radical (full healing)ii) Symptomatic(treatment of symptoms only)iii)Prophylactic (eg. contraception, vaccine)3) CLINICAL PHARMACOLOGY:Deals with: -the discovery and development of new drug molecules-evaluation of these on healthy and diseased human beingafter enough experimentation on animals-should not be mixed with pharmacotherapy andart of prescription writings4) CHEMOTHEREAPY:Deals with the treatment of infectious and neoplastic disorders5) PHARMACOKINETIC:Deals with how the body handles a drug.Its scope: - Absorption- Distribution- Biotransformation (metabolism)- Elimination
  5. 5. 56) PHARMACODYNAMIC:-Deals with how drug handles the body-Deals with the biochemical and physiological effects(beneficial or toxic) of drugs and their mechanism of actionin human being.7) PHARMACOGENETIC:Deals with:- the influence of genetic on the mode of drug actions(eg. metabolism)- and biological variations of drug responses8) BIOPHARMACEUTIC:Deals with: - the production of drug forms- and the relationship between the pharmacokinetic ofthese forms and their effects9) PHARMACOGNOSIA:Deals with plants possessing active principlesEg. Digitalis purpureaAtropa belladonnaePapaver somniferum10) IMMUNOPHARMACOLOGYDeals with drugs that can bring about an effect by acting on immuneSystem: - Immunosuppressive agents used in organ transplantationand in autoimmune disorders- Immunomodulators like immunostimulants used inimmune deficiencies11) TOXİCOLOGY:Deals with undesirable or adverse effects of chemicals inbiological systems.Drug EffectsDesirable Undesirable(therapeutic)Non-deleterious Deleterious(side effects) (toxic effects)-Pharmacologic-Pathologic-Genotoxic(nitrogen mustard)Liver: AcetaminopheneLung: Paraquat (herbesite)Phototoxicity: Sulfonamides, tetracyclines
  6. 6. 6There is no strict limit between drugs, nutrients and poisonsDRUGNUTRIENT POISONEg. - Water- Vitamines- d-Tubocurarine• DRUGThe main concern of pharmacology.Definitions: 1) Drugs are active chemical principles used in medicine2) WHO: Drug is a compound used to change thephysiological functions or pathophysiological condi-ditions for the benefit of human being.3) MORE GENERAL: Any substance that bring aboutchanges in biological functions through its chemicalaction.4) OR: Drug is any small molecule that alter bodyfunctions by interaction at the molecular level.• Drug actions are mediated by 3 ways:1) By acting on somatic or psychic processes orfunctions.2) By correction of deficiencies3) By toxic action on pathogenic microorganism• Drug effects: - Should be -selective-temporary-dose-related (controllable)- And show close relationship with bioavailability• HOW ARE DRUGS RESPONSES PRODUCED?By interaction with active binding sites called RECEPTORS- Inert binding sites (plasma & tissue proteins) do notbring about a biological response- Drug may be agonist or antagonist for the receptors- Interaction wit receptors may be covalent, electrostatic..- For best fitting, drug size, shape, electrical charges andatomic composition are important- Majority of drug size fall in 100 to 1000-Small molecules are more selective in its action-Large molecules move more slowly (mw 1000)
  7. 7. 7Influence of physical nature of drugsPhysical state: -solid (aspirin)-liquid(nicotine, ethanol) -Determine-Gas route of-Vaporizable liquid forms administrationChemical structure: Protein, lipid, carbohydrateTo be weak acid or weak basePrimary amine : R-NH2Secondary amine: R2-NHTertiary amine : R3-NQuaternary : R4-N+Isomeric forms: (+)d, (-)l, dlDrug-body interactions: -PHARMACOKINETIC-PHARMACOYNAMIC• SOURCES OF DRUGS: 1) NATURAL- Plants- Animals- Bacteria, fungi- Inorganic compounds2) SEMISYNTHETIC3) Synthetic4) DNA recombinant technologyDRUGS FROM PANTS:- Active principles are found in roots, leaves and seeds in2 forms: 1) Glycoside2) AlkaloidTO BE ALKALOİD TO BE GLYCOSIDE-Must be of plant origin -Must be of plant origin-Has a nitrogen atom in a -aglycone-O-carbohydrateheterocyclic ring system linkage-Has bitter taste -Genin (aglycone) is the avtive-Base form is not soluble in componentwater but in alcohol -eg. Digital glycosides-Salt form is soluble in water-eg. Morphine, curare, atropinePharmaceutical forms obtained from plans:(GALENIC PREPARATIONS)1) POWDERS2) EXTRACTS: -Obtained by incubation in solvents- May be soft, semisolid or dry
  8. 8. 83) INFUSIONS: -Obtained by incubation in hot water-eg. Tea- Must be prepared freshly4) DECOCTIONS: -Obtained by boiling in water-eg. Lindon blossom5) TINCTURES: -Obtained by treatment with alcohol-eg. Digital tinctureDRUGS FROM ANIMALS-Hormones like heparin, insulin-Plasma or serum from blood-Gonadotrophines from urine of pregnant womenDRUGS FROM MICROORGANISMS:-Antibiotics-Streptokinase, streptodorinaseINORGANIC METALS:-Iodine-Lithium-Radioactive elements: 131I, 198Au, 60CoSEMISYNTHETIC DRUGS-Semisynthetic penicillins from 6-aminopenicillnicacid-Semisynthetic cephalosporins from 7-aminocephalosporinic acid-LSD from natural lysergic acidDRUGS BY DNA RECOMBINANT TECHNOLOGYCells from animals or human thatproduce active principleIsolation of DNARelease of DNA fragmentsBy endonucleaseTransfer to E-coliby plasmids(Gene cloning)A new E-coli formthat synthesize thethe new substance
  9. 9. 9• CRITERIA FOR DRUG CLASSIFICATION1) Chemical structure: - Cholinester- Organophosphates- Catecholamines2) Locus of action: - Heart glycosides- Autonomic drugs3) Purpose of medication: - Antihypertensive- Diuretic- Antiemetic- Analgesic4) Name of plant: - Opium alkaloids- Digital glycosides Papaver somniferum- Belladonnae alkaloids• DRUG NAMES: 1) General or generic name given by WHO3) Trade name given by the DRUG FIRMS4) Chemical name which is LONG, COMPLEX ANDNOT USED CURRENTLYPapaver somniferum
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