Biotransformation of Drugs (Metabolism)

BIOTRANSFORMATION OF DRUGS (METABOLISM)

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Introduction

·       Biotransformation of drugs, also known as drug metabolism, refers to the chemical alterations that drugs undergo within the body.

·       This process typically occurs in the liver but can also take place in other organs such as the kidneys, lungs, and intestines.

·       The primary purpose of drug metabolism is to make the drug more water-soluble, facilitating its excretion from the body, and often rendering it less active or completely inactive.

·       Understanding these factors is crucial for predicting and managing drug interactions, optimizing drug therapy, and minimizing the risk of adverse drug reactions.

·       There are two main phases of drug metabolism:

·       Phase I Metabolism:

·       In this phase, the drug molecule is often oxidized, reduced, or hydrolysed by enzymes such as cytochrome P450 enzymes.

·       These reactions introduce or expose functional groups (e.g., hydroxyl, amino, or carboxyl groups) to the drug molecule, making it more reactive and preparing it for further metabolism in phase II.

·       Phase II Metabolism

·       Phase II reactions involve the conjugation of the drug or its metabolites with endogenous molecules such as glucuronic acid, sulphate, glycine, or glutathione.

·       This conjugation typically increases the water solubility of the drug, facilitating its excretion via urine or bile.

Factors Affecting Drug Biotransformation

·       Genetics

·       Genetic variations in drug-metabolizing enzymes, such as cytochrome P450 enzymes, can lead to differences in drug metabolism among individuals.

·       This can result in variations in drug efficacy and toxicity.

·       Age

·       Drug metabolism can be influenced by age, with neonates, infants, and the elderly often exhibiting altered metabolic rates compared to adults.

·       In neonates, the activity of drug-metabolizing enzymes may be low, while in the elderly, it may decline due to decreased liver function.

·       Disease States

·       Certain diseases, such as liver or kidney disease, can impair drug metabolism.

·       Liver diseases like hepatitis or cirrhosis can reduce the activity of drug-metabolizing enzymes, leading to decreased metabolism and potential drug toxicity.

·       Conversely, some diseases can increase drug metabolism due to the induction of drug-metabolizing enzymes.

·       Drug-Drug Interactions

·       Co-administration of multiple drugs can affect drug metabolism through various mechanisms.

·       For example, some drugs may inhibit or induce specific drug-metabolizing enzymes, altering the metabolism of co-administered drugs.

·       This can result in decreased efficacy or increased toxicity of one or both drugs.

·       Nutritional Status

·       Certain nutrients or dietary factors can influence drug metabolism.

·       For example, grapefruit juice contains compounds that inhibit cytochrome P450 enzymes, affecting the metabolism of drugs metabolized by these enzymes.

·       Environmental Factors

·       Environmental factors such as exposure to pollutants or toxins can influence drug metabolism by affecting the activity of drug-metabolizing enzymes.

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