Applications of Pharmacokinetic Principles

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Chapter: Biopharmaceutics and Pharmacokinetics : Bioavailability and Bioequivalence

The time course of drug concentration in the body after its administration can be defined by a number of pharmacokinetic parameters.

Applications of Pharmacokinetic Principles

The time course of drug concentration in the body after its administration can be defined by a number of pharmacokinetic parameters. Often, the information gained about the pharmacokinetics of one drug helps in anticipating the pharmacokinetics of another. The knowledge of pharmacokinetic behaviour of a drug coupled with important pharmacodynamic parameters like therapeutic index can be put to several applications:

1.        Design and development of new drugs with greatly improved therapeutic effectiveness and fewer or no toxic effects

2.        Design and development of an optimum formulation for better use of the drug

3.        Design and development of controlled/targeted release formulation

4.        Design an appropriate multiple dosage regimen

5.        Select the appropriate route for drug administration

6.        Select the right drug for a particular illness

7.        Predict and explain drug-food and drug-drug interactions

8.        Therapeutic drug monitoring in individual patients

9.        Dosage adjustment in situations of altered physiology and drug interactions.

The applications of pharmacokinetic principles are mainly aimed at achieving the therapeutic objective. The therapeutic objective is often control or cure of the condition in shortest possible time with minimum side effects by the use of least amount of drug. New drug development or chemical modification is frequently done to improve pharmacokinetic properties and increase efficacy. Drug product design is aimed at optimising bioavailability or better control/cure of illness through controlled- or targeted-release. Proper choice of route of administration is necessary to ensure that the drug moves to the site of action at a sufficiently rapid rate and amount. Selection of a suitable drug is based on achieving optimal therapy by balancing the desirable and undesirable effects. Co-administration of several drugs to a patient may lead to changes in the pharmacokinetic profile of a drug which is indicative of interactions between drugs. Such an understanding of interaction makes possible more rational use of drugs that have to be co-administered.

Clinically, the two most important applications of pharmacokinetic principles are:

1. Design of an optimal dosage regimen, and

2. Clinical management of individual patient and therapeutic drug monitoring.

Such applications permit the physician to use certain drugs more safely and sensibly.

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