Metabolic induction and metabolic inhibition

B pharmacy notes

Metabolic induction and metabolic inhibition refer to processes that affect the rate of metabolism, primarily in the liver, where many drugs and other substances are metabolized. These processes involve enzymes, particularly the cytochrome P450 (CYP) enzyme system, which plays a crucial role in the metabolism of drugs and endogenous compounds.

B pharmacy important notes


Metabolic induction and metabolic inhibition refer to processes that affect the rate of metabolism, primarily in the liver, where many drugs and other substances are metabolized. These processes involve enzymes, particularly the cytochrome P450 (CYP) enzyme system, which plays a crucial role in the metabolism of drugs and endogenous compounds.

1. Metabolic Induction

Metabolic induction occurs when a substance (like a drug, food, or chemical) increases the activity or production of metabolic enzymes, leading to faster metabolism of drugs or other substances. This can reduce the effectiveness of medications because the body clears them more quickly.

  • Example: Rifampin (an antibiotic) induces CYP450 enzymes. If taken with other drugs, those drugs may be metabolized faster, reducing their therapeutic effects.

  • Effects:

    • Decreased plasma concentration of drugs
    • Reduced drug efficacy
    • May require higher doses of medication for effectiveness

2. Metabolic Inhibition

Metabolic inhibition occurs when a substance decreases the activity of metabolic enzymes, leading to slower metabolism of drugs or other substances. This can result in higher concentrations of drugs in the body, increasing the risk of side effects or toxicity.

  • Example: Grapefruit juice inhibits the CYP3A4 enzyme, slowing the metabolism of certain medications (like statins), which can lead to higher levels of these drugs in the blood and potential toxicity.

  • Effects:

    • Increased plasma concentration of drugs
    • Heightened risk of side effects or toxicity
    • May require lower doses of medication to avoid adverse effects
Both induction and inhibition can significantly impact drug interactions and are important considerations in clinical settings.

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