Category: pharmacological
Aliases: Azilect, TVP-1012
Selective irreversible MAO-B inhibitor for Parkinson disease (monotherapy in early disease or adjunct to levodopa). Propargylamine class — same pharmacophore family as selegiline but no amphetamine-like metabolites (rasagiline metabolizes to 1-aminoindan, which is neuroprotective in some preclinical models — vs selegiline → methamphetamine + amphetamine). Once-daily 0.5-1 mg PO. CYP1A2 substrate (fluvoxamine + ciprofloxacin DDIs documented in label, but no abstract-verbatim AUC ratio per v1.1 GAPS). Selectivity for MAO-B is dose-dependent — at supratherapeutic doses loses selectivity, raises tyramine hypertensive crisis risk. PK (Azilect label, 1 mg PO qd SS): Cmax 2.5 ng/mL, Tmax 1 h, t½ 3 h SS, F 36%, Vss 87 L, protein binding 88-94%. Pharmacokinetics doesn't correlate with pharmacodynamics — irreversible MAO-B inhibition outlasts plasma exposure by weeks (target re-synthesis dictates effect duration). High-fat meal ↓Cmax 60%, ↓AUC 20%.
PO: 3h