Pharmacokinetics Chapter 4

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Presentation transcript:

Pharmacokinetics Chapter 4 Copyright (c) 2004 Elsevier Inc. All rights reserved.

Pharmacokinetics Four basic pharmacokinetic processes are Absorption Distribution Metabolism Excretion Copyright (c) 2004 Elsevier Inc. All rights reserved.

Factors Affecting Drug Absorption Rate of dissolution Surface area Blood flow Lipid solubility pH partitioning Copyright (c) 2004 Elsevier Inc. All rights reserved.

Routes of Administration Two major groups Enteral Via gastrointestinal tract Parenteral Outside the gastrointestinal tract Usually referred to as “by injection” Common routes—intravenous, subcutaneous, intramuscular Copyright (c) 2004 Elsevier Inc. All rights reserved.

Drug Distribution Factors influencing distribution are Blood flow to tissue – Exiting the vascular system – The blood-brain barrier – Placental drug transfer Copyright (c) 2004 Elsevier Inc. All rights reserved.

Drug Metabolism Biotransformation Enzymatic alteration of drug structure Liver—primary site of drug metabolism P450 system (cytochrome P450) Copyright (c) 2004 Elsevier Inc. All rights reserved.

Drug Metabolism—Implications Therapeutic consequences are Accelerated drug excretion Drug inactivation Increased therapeutic action Activation of prodrugs Toxicity variations Copyright (c) 2004 Elsevier Inc. All rights reserved.

Special Considerations in Drug Metabolism Age Induction of drug-metabolizing enzymes First-pass effect Nutritional status Competition between drugs Copyright (c) 2004 Elsevier Inc. All rights reserved.

Drug Excretion Removal of drug from the body Kidney—via three processes Glomerular filtration Passive tubular reabsorption Active tubular secretion Copyright (c) 2004 Elsevier Inc. All rights reserved.

Time Course of Drug Responses Plasma drug levels Minimum effective concentration (MEC) Toxic concentration Therapeutic range Drug half-life Loading dose Maintenance dose Copyright (c) 2004 Elsevier Inc. All rights reserved.

The time for the amount of drug in the body to decrease by 50% Drug Half-life The time for the amount of drug in the body to decrease by 50% Copyright (c) 2004 Elsevier Inc. All rights reserved.