Nicergoline

alkaloid · nervous · cardiovascular · immune-hematologic · Oral

Nicergoline, an alkaloid. Semisynthetic ergoline. An alpha-1-adrenoceptor antagonist producing cerebral vasodilation and increased arterial flow, which also enhances…

Semisynthetic ergoline. An alpha-1-adrenoceptor antagonist producing cerebral vasodilation and increased arterial flow, which also enhances cholinergic and catecholaminergic transmission, inhibits platelet aggregation, raises oxygen and glucose utilisation, and has neurotrophic and antioxidant activity. Rapidly hydrolysed after absorption to the alcohol MMDL, which CYP2D6 then N-demethylates to MDL; poor CYP2D6 metabolisers accumulate MMDL roughly sixfold and form essentially no MDL. Marketed for mild-to-moderate dementia and balance disorders.

PubChem CID 34040 (C24H26BrN3O3). What PMID:8971425 actually reports, verbatim, after a single oral 30 mg: "mean MMDL Cmax 59 nmol l-1 and AUC (0, th) 144 nmol l-1h, mean MDL Cmax 183 nmol l-1 and AUC 2627 nmol l-1h" in extensive debrisoquine metabolisers against "mean MMDL Cmax 356 nmol l-1 and AUC 10512 nmol l-1h, MDL concentrations below limit of quantitation" in poor metabolisers — metabolite exposures only, which is why the record is pk_unauthored. Dose range is verbatim from the Winblad 2008 review (PMID:18666801): "nicergoline (30 mg twice daily)" and "commonly applied doses (60 mg/day)". immune-hematologic is tagged for the platelet-aggregation inhibition that review names. NOTE FOR ANY FUTURE PK PASS: this is a prodrug shape — if a parameter is ever sourced it will almost certainly describe MMDL or MDL, not nicergoline, so it needs pk_analyte: active-metabolite and pk_analyte_name set, and mw_g_mol switched to the analyte's mass per the catalog convention. The 484.4 stored here is the parent and is correct only while no PK exists.

Sources: PMID:18666801, PMID:8971425