First-pass metabolism and prodrugs
Explains why some drugs don't work orally — and why others only work after being metabolized.
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- Absorption and routes of administration — Oral drugs pass through gut and liver before the brain.
- When enzymes change: induction, inhibition and genetics — Inhibiting the first-pass enzyme changes everything.
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- Half-life and redistribution — With delivery understood, turn to how long drugs last.
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Prodrug – chemical is not initially psychoactive, but active metabolite of chemical is. First-pass metabolism – drug passes through GI tract and/or liver before it reaches brain, causing some amount of the drug to be broken down; this effectively lowers bioavailability. More direct routes into the bloodstream (IV, inhalation, intranasal, sublingual) avoid it.
Términos del curso
Las palabras de tu profesor, tal cual aparecen en las diapositivas. Aprende el término y esta definición; la explicación de abajo solo ayuda a entenderla.
- Prodrug
“Chemical is not initially psychoactive – but active metabolite of chemical is”Diapositivas 04, p. 41
e.g., psilocybin → psilocin; lisdexamfetamine (Vyvanse) → amphetamine.
- First-pass metabolism
“Drug passes through GI tract and/or liver before it reaches brain, causing some amount of the drug to be broken down (metabolized)”Diapositivas 04, p. 42
“This effectively lowers bioavailability of the drug – sometimes massively!”
De tu curso: Course slides 04, pp. 41–43
Consejo: las teclas ← y → recorren la lección.
Lección completa: Prodrugs and first-pass metabolism