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Pharmacokinetics

Pharmacokinetics. Dr. M. Yulis Hamidy, MKes, MPdKed. Definition. Pharmacodynamics = the effects of the drug on the body Pharmacokinetics = the way the body affects the drug with time absorption distribution biotransformation / metabolism excretion of drugs. Passage of drugs through body.

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Pharmacokinetics

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  1. Pharmacokinetics Dr. M. Yulis Hamidy, MKes, MPdKed

  2. Definition • Pharmacodynamics=the effects of the drug on the body • Pharmacokinetics = the way the body affects the drug with time • absorption • distribution • biotransformation / metabolism • excretion of drugs

  3. Passage of drugs through body • Administration • Absorption • Distribution • Metabolism • Excretion

  4. Drug Administration parental, oral, topical Plasma Compartment Bound Free drug drug Excretion urine, feaces, expelled air Storage fat, cytoplasm, bone Metabolism liver, GIT, lung Site of drug action

  5. Routes of administration • Oral • Parental • Topical • buccal • vaginal • anal • dermal • ocular • nasal First pass metabolism

  6. Plasma levels after different routes of administration IV Oral Topical Plasma concentration Time (hrs)

  7. Drug Distribution • molecular size • lipophilicity • plasma binding • blood flow to different organs • lean:fat body weight

  8. pKa of drug and pH of environment distribution

  9. Plasma binding distribution

  10. Blood Flow distribution

  11. Drug Biotransformation

  12. Metabolism • most drugs • Phase 1 • Phase 2 • ind/inh • tissues • prodrugs

  13. Elimination • First order • zero order • intermediate

  14. Pharmacokinetics • One-compartment model

  15. Two-compartment model

  16. Steady state concentration

  17. Age, Sex, Race • Age • infants • children • elderly • Sex • Race

  18. Drug Interactions • pharmacokinetic basis • pharmacodynamic basis

  19. Effect of Disease on Drug Action • cardiovascular disease • liver function • celiac disease • viral infections • renal disease • asthma • Alzheimer-type dementia

  20. Bioavailability • Bioavailability is defined as the fraction of unchanged drug reaching the systemic circulation following administration by any route. • The area under the blood concentration-time curve (area under the curve, AUC) is a common measure of the extent of bioavailability for a drug given by a particular route. • For an intravenous dose of the drug, bioavailability is assumed to be equal to unity. For a drug administered orally, bioavailability may be less than 100% for two main reasons—incomplete extent of absorption and first-pass elimination.

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