Pharmacokinetics

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Presentation Transcript

Slide 1: 

Mr. Amol Khedkar B. Pharm M.Tech(Biotech) A Presentation on ……. Pharmacokinetics

Slide 2: 

What is Pharmacology? Derived form Greek word Pharmakon Logos Drug Study + + } Pharmacology

Why Study Pharmacokinetics (PK) : 

Why Study Pharmacokinetics (PK) Individualize patient drug therapy Monitor medications with a narrow therapeutic index Decrease the risk of adverse effects while maximizing pharmacologic response of medications Evaluate PK/PD as a diagnostic tool for underlying disease states

Slide 4: 

Branches of Pharmacology Pharmacokinetics: Study of ADME i.e. What body does to drug 2) Pharmacodynamics: Study of Mechanism of action of drug i.e. what drug does to the body 3) Therapeutic Index = 4) Toxicology: Study of poisons 5) Chemotherapy: Concerned with the effect of drug upon microorganism and parasites

Slide 5: 

Sources of DRUG: I) Plant: e.g. Morphine, digoxin II) Animal: e.g. Insulin, Heparin III) Synthetic:e.g. Aspirin, Procaine IV) Mineral: e.g. Liquid paraffin, Kaolin V) Microorganism: e.g. Penicillin VI) Genetic Engineering: rDNA e.g. Human insulin and hGH

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Routes of Administration

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Routes of Administration 1) Enteral: a) Oral b) Sublingual c) Enema: i) Evacuant ii) Retention 2) Paraenteral: a) Inhalation b)Injection: Intradermal Subcutaneous Intramuscular Intravenous Intraarterial Intrathecal Intraperitoneal Intramedullary Intraarticular 3) Local Application

Absorption : 

Absorption Passive diffusion : 1) Diffusion

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2) Facilitated diffusion

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3) Filtration

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4) Osmosis

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http://www.northland.cc.mn.us/biology/BIOLOGY1111/animations/active1.swf Active Transport

Slide 14: 

Pinocytosis

Slide 15: 

Pharmacokinetics

Time to Peak Concentration : 

Time to Peak Concentration

Slide 17: 

http://www.youtube.com/watch?v=8zYIEiXvSZY Drug Distribution: Drug distribution refers to the movement of drug to & from the blood & Various tissues of the body e.g. fat, muscle, brain tissue & the relative proportions of drug in the tissue. Drug dissolves in water (water soluble drug) e.g atenolol tend to stay within blood and fluid surrounds the cells. Drug dissolves in fat (fat soluble drug) e.g halothane tend to concentrate in fatty tissue. Some drug molecule bound to plasma protein, deposit in muscle, bone

Distribution : 

Distribution Membrane permeability cross membranes to site of action Plasma protein binding bound drugs do not cross membranes malnutrition = albumin =  free drug Lipophilicity of drug lipophilic drugs accumulate in adipose tissue Volume of distribution

Metabolism : 

Metabolism Drugs and toxins are seen as foreign to patients bodies Drugs can undergo metabolism in the lungs, blood, and liver Body works to convert drugs to less active forms and increase water solubility to enhance elimination

Metabolism : 

Metabolism Liver - primary route of drug metabolism Liver may be used to convert pro-drugs (inactive) to an active state Types of reactions Phase I (Cytochrome P450 system) Phase II

Phase I reactions : 

Phase I reactions Cytochrome P450 system Located within the endoplasmic reticulum of hepatocytes Through electron transport chain, a drug bound to the CYP450 system undergoes oxidation or reduction Enzyme induction Drug interactions

Phase I reactions types : 

Phase I reactions types Hydrolysis Oxidation Reduction Demethylation Methylation Alcohol dehydrogenase metabolism

Phase II reactions : 

Phase II reactions Polar group is conjugated to the drug Results in increased polarity of the drug Types of reactions Glycine conjugation Glucuronide conjugation Sulfate conjugation

Elimination : 

Elimination Pulmonary = expired in the air Bile = excreted in feces Renal glomerular filtration tubular reabsorption tubular secretion

Pharmacokinetic Principles : 

Pharmacokinetic Principles Steady State: the amount of drug administered is equal to the amount of drug eliminated within one dosing interval resulting in a plateau or constant serum drug level Drugs with short half-life reach steady state rapidly; drugs with long half-life take days to weeks to reach steady state

Steady State Pharmacokinetics : 

Steady State Pharmacokinetics Half-life = time required for serum plasma concentrations to decrease by one-half (50%) 4-5 half-lives to reach steady state

Loading Doses : 

Loading Doses Loading doses allow rapid achievement of therapeutic serum levels Same loading dose used regardless of metabolism/elimination dysfunction

Linear Pharmacokinetics : 

Linear Pharmacokinetics Linear = rate of elimination is proportional to amount of drug present Dosage increases result in proportional increase in plasma drug levels

Nonlinear Pharmacokinetics : 

Nonlinear Pharmacokinetics Nonlinear = rate of elimination is constant regardless of amount of drug present Dosage increases saturate binding sites and result in non- proportional increase/decrease in drug levels

Pharmacogenetics : 

Pharmacogenetics Science of assessing genetically determined variations in patients and the resulting affect on drug pharmacokinetics and pharmacodynamics Useful to identify therapeutic failures and unanticipated toxicity

Slide 33: 

:- References:- 1) Pharmacology and Pharmacotheraprutics by Satoskar & Bhandarkar, 15th edition, Popular publication, Mumbai. 2) The pharmacological basis of therapeutics by Goodman & Gilman 9th edition, International publication. 3) Essentials of Medical Pharmacology by K.D. Tripathi, 5th edition, by Jaypee brothers, New Delhi. 4)http://www.youtube.com 5)http://www.northland.cc.mn.us/biology/BIOLOGY1111/animations/active1.swf 6) http://www.wikipedia.org

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THANK YOU