Pharmacokinetics

COURSE CONTENT

(Weekly Detailed Course Content)

Week

Theoretical Topics                                     

Lab content

Study Materials

1

Basic Concepts for Pharmacokinetics (PKs): Definition of ADME processes, time course of drug & metabolites in and outside the body, measurement  and significance of drug concentration in various biological fluids.

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2

Basic Concepts for Pharmacokinetics: Concept of compartment in PKs, definition of linear and nonlinear PKs, mathematical fundamentals for PKs, orders of rate processes (Zero-order, 1st order) and general equations.

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3

Drug Absorption kinetics: Difference between absorption and bioavailability, absorption from  various routes of drug administration and typical plasma profile, first- and zero-order rates of drug absorption, calculation of absolute and relative bioavailability.

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4

Drug Distribution and Protein Binding: Physiologic factors of drug distribution, drug reservoirs (accumulation), rate of drug distribution, extent of distribution (volume of distribution).

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5

Drug Distribution and Protein Binding: Characteristics of drug-plasma protein binding, methods of determining protein binding, kinetics of protein binding (calculation of binding constant and number of binding sites on protein molecule), effect of protein binding on distribution and elimination, clinical significance of drug protein binding.

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6

Drug Elimination: Functions of drug metabolism, sites of metabolism, types of metabolic reactions, factors affecting drug metabolism, mechanism of metabolism induced toxicity, drug excretion by various routes.

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7

Drug Elimination: Determination of relative amount of metabolism and excretion, expressions for elimination rate (clearance), calculation of elimination, excretion and metabolic rate constants, organ clearance model, creatinine clearance, hepatic extraction ratio and classification of drugs on the basis of it, characteristics of high hepatic extraction ratio drugs, determination of renal and hepatic clearance.

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8

Pharmacokinetic Models: Determination of whether body behaves as one- or multi-compartment, IV bolus-one compartment pharmacokinetic model, determination of duration of drug action and volume of distribution, IV bolus-2 and 3- compartment models.

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9

Pharmacokinetic Models: Main reasons for applying drugs as IV infusion, steady-state plasma concentration, IV infusion- one compartment model.

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10

Pharmacokinetic Models: One compartment model for oral administration with 1st and zero-order absorption, calculation of time required to reach peak plasma concentration.

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11

Pharmacokinetic Models: One compartment model for multiple IV bolus dosage administration, one compartment model for multiple IV infusion, one compartment model for multiple oral dosage administration.

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12

Relationship between Pharmacokinetics and Pharmacodynamics: Relation of dose, rate of absorption, distribution and elimination to pharmacologic response, pharmacokinetic drug tolerance, pharmacodynamic models (maximum effect model, sigmoid model) and hysteresis of pharmacodynamic response.

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13

Application of Pharmacokinetic Principles in Clinical Situations: Determination of dose, dosage interval and route of administration, individualization of dosage regimen and therapeutic drug monitoring.

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14

Application of Pharmacokinetic Principles in Clinical Situations: Dosing for infant, children, elderly and obese patients, pharmacokinetic drug interaction, dosage adjustment in renal and hepatic diseases.

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