Bupropion
Bupropion. Norepinephrine + dopamine reuptake inhibitor with nicotinic-ACh-receptor antagonism (mechanism behind smoking-cessation indication).… Oral half-life 21 h.
Norepinephrine + dopamine reuptake inhibitor with nicotinic-ACh-receptor antagonism (mechanism behind smoking-cessation indication). Active hydroxybupropion metabolite contributes. No sexual side effects and mild weight-neutral-to-loss profile → often chosen when SSRI sexual dysfunction is a problem.
PK: A 6.5-TO-8.4x UNDER-PREDICTION ON A CITATION THAT CARRIES NOTHING. Its source states none of the four values — only metabolite ratios, a simulated partial-AUC range and a metabolite half-life range — and was not even in refs[]. F 0.06 has no traceable origin: no indexed abstract states an absolute bioavailability for bupropion, the frequently quoted ~87% is canine and could not be verified in any abstract either, and 0.06 sits on cbd, dronabinol, ganciclovir and oxybutynin where six percent is real. Since no absolute F exists the volume is necessarily apparent, so F is pinned to 1. THE HALF-LIFE WAS A RANGE ENDPOINT AND THE STATED VALUE WAS ALREADY IN ITS OWN refs[]: "biphasic elimination with an elimination half-life of 11 - 14 hours" was stored as 14, while a reference the record already carried says "Bupropion is extensively metabolized by the liver (t(1/2), approximately 21 hours)". The volume becomes the one reproducing a verbatim "apparent oral clearance of 221 L/h", which is disclosed as derived AND as measured at 60.9 kg rather than this registry 70. ka 0.5 is kept because it is formulation-coherent, reproducing the extended-release peak; a scalar ka can represent only one of three marketed forms and this record is declared XL. A STRUCTURAL LIMIT IS LOGGED: hydroxybupropion runs an "AUC ... approximately 10-fold greater" than the parent, so a parent-only curve cannot represent this drug pharmacology. INTERACTIONS: BOTH AFFINITIES INVERT THROUGH 1.0 µM, from a fivefold exposure rise in each case. A caveat carried from the record own notes: the inhibition is attributed to bupropion together with its hydroxy metabolite, so a constant expressed against the parent plasma curve alone understates the perpetrator.
Pharmacokinetics
- Oral — t½ 21 h · F 100% · ka 0.6194 h⁻¹ · Vd 6695 L
Related compounds
- Atomoxetine — major
- Desipramine — major
Sources: PMID:16368442, PMID:27518170, PMID:18420781, PMID:27255113, PMID:30520001, PMID:14515060