Opioid metabolism

Results in the production of active and inactive metabolites.

Active metabolites may be more potent than the parent compound.

First pass metabolism reduces the opioid’s bioavailability.

Opioids cross cell membranes because of their lipophilic activity so they can reach target tissues.

Drug metabolism increases the hydrophilic activity of the opioid drug and increases excretion in the urine.

Occurs primarily in the liver.

The liver produces enzymes that metabolize opioid drugs.

Liver enzymes promote phase 1 and phase 2 metabolism.

Phase 1 metabolism allows oxidative r hydrolytic metabolism.

Phase 1 involves cytochrome P450 (CYP) enzymes that facilitate multiple reactions.

Phase 2 metabolism conjugates opioids to hydrophilic substances.

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