Biotransformation and Drug Metabolism

Purpose of Biotransformation

• Biotransformation refers to the chemical modification made by an organism on a chemical compound, primarily facilitating the detoxification and elimination of xenobiotics (foreign substances) from the body.

Consequences for Drugs

• For some drugs, biotransformation results in metabolic activation, converting the drug into a more active or potent form, which can enhance therapeutic effects.
• Alternatively, it can lead to inactivation, where drugs are converted into less active forms, impacting efficacy.
• In some cases, biotransformation produces toxic metabolites that can lead to adverse drug reactions or toxicity.

Key Organ for Biotransformation

• The liver is the most important organ for biotransformation processes, playing a critical role in metabolizing drugs and other xenobiotics.

Location of Microsomal Enzymes

• Microsomal enzymes responsible for biotransformation reactions are located in the endoplasmic reticulum of liver cells and other tissues, facilitating drug metabolism.

Function of Non-Microsomal Enzymes

• Non-microsomal enzymes, found in various tissues, primarily function in conjugation reactions, aiding in the further modification of metabolites, enhancing water solubility for excretion.

Test your understanding of biotransformation, the process of biochemical alteration of drugs in the body, and how it affects drug excretion and metabolism in different organs. Explore the site of metabolism and the consequences of biotransformation on drug efficacy and toxicity.