Ergoloid mesylates

alkaloid · nervous · cardiovascular · Oral

Ergoloid mesylates, an alkaloid. Fixed mixture of four dihydrogenated ergot alkaloids — dihydroergocornine, dihydroergocristine, and the alpha and beta isomers of…

Fixed mixture of four dihydrogenated ergot alkaloids — dihydroergocornine, dihydroergocristine, and the alpha and beta isomers of dihydroergocryptine — in a 3:3:2:1 ratio by the USP monograph. As a class they are partial agonists and antagonists at alpha-adrenergic, dopaminergic and serotonergic receptors, with the hydrogenation removing the vasoconstrictor action of the parent ergots. This was the first agent approved in the United States for "idiopathic decline in mental capacity" in the elderly and is the archetype of the cerebral-insufficiency class that nicergoline and the racetams followed; its mechanism of benefit was never established, and the indication itself is a diagnosis modern practice does not use.

No mw_g_mol: four alkaloids have four masses, and PubChem CID 6420006 (679.8) is the mesylate of one congener rather than the product. NO composition[] EITHER, deliberately. That block needs a mg_per_g_extract per constituent and each constituent present as its own compound with its own PK; none of the four is in this catalog, and the only human data for any of them is a single-subject Cmax from a paper that calls itself "preliminary results". Four stubs expanding into four unsolvable curves would add rows without adding information, so the USP ratio is recorded in the mechanism prose instead, where it reads as what it is rather than as a solver input. Revisit if any congener ever gets its own PK — dihydroergocristine is the likeliest, since it is marketed alone in some markets. What PMID:4091992 does establish, and what is worth keeping even without a stored number: twelve healthy males, three oral formulations, plasma "exceeded 200 pg ml-1 for approximately 5 h and decayed in a biphasic manner", with the retard capsule reaching half the solution's Cmax at similar overall bioavailability — so this is a low-concentration, biphasic, formulation-sensitive drug, none of which a one-compartment curve would have represented honestly. Dose range is the marketed 1 mg three times daily up to the 12 mg/day used in the older dementia trials; PMID:17941060 used a single 27 mg dose to get measurable concentrations at all, which is itself a comment on the exposure.

Sources: PMID:17941060, PMID:4091992