Biomaterial Database

Dihydroergotoxine kinetics in healthy men after intravenous and oral administration. 1982

B G Woodcock, and W Loh, and W D Habedank, and N Rietbrock

The kinetics of intravenous and oral dihydroergotoxine mesylate determined in eight healthy male subjects with a radioimmunoassay method incorporating a plasma extraction step to obtain maximal sensitivity and specificity. The intravenous plasma concentration-time curve showed an initial rapid decline (half-life[t1/2] = 3.5 min) and could be fitted to a three-compartment model. The high systemic clearance (20.2 to 28.8 ml x min-1 x kg-1) and large distribution volume, (9.9 to 20.41 x kg-1) were associated with a terminal t1/2 of 9.5 to 18.4 hr. The oral absorption was rapid. (t1/2 = 14.8 min). Absolute bioavailability was 5.3% to 12.4%. The terminal t1/2 and bioavailability were considerably lower than earlier estimates and this can be attributed to the use in these investigations of a more sensitive and specific dihydroergotoxine assay method.

UI	MeSH Term	Description	Entries
D007275	Injections, Intravenous	Injections made into a vein for therapeutic or experimental purposes.	Intravenous Injections,Injection, Intravenous,Intravenous Injection
D007700	Kinetics	The rate dynamics in chemical or physical systems.
D008297	Male		Males
D011863	Radioimmunoassay	Classic quantitative assay for detection of antigen-antibody reactions using a radioactively labeled substance (radioligand) either directly or indirectly to measure the binding of the unlabeled substance to a specific antibody or other receptor system. Non-immunogenic substances (e.g., haptens) can be measured if coupled to larger carrier proteins (e.g., bovine gamma-globulin or human serum albumin) capable of inducing antibody formation.	Radioimmunoassays
D004088	Dihydroergotoxine	A mixture of three different hydrogenated derivatives of ERGOTAMINE: DIHYDROERGOCORNINE; DIHYDROERGOCRISTINE; and DIHYDROERGOCRYPTINE. Dihydroergotoxine has been proposed to be a neuroprotective agent and a nootropic agent. The mechanism of its therapeutic actions is not clear, but it can act as an alpha-adrenergic antagonist and a dopamine agonist. The methanesulfonate salts of this mixture of alkaloids are called ERGOLOID MESYLATES.	Co-Dergocrine,Ergot Alkaloids, Hydrogenated,Dihydroergotoxin,Alkaloids, Hydrogenated Ergot,Hydrogenated Ergot Alkaloids
D006207	Half-Life	The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity.	Halflife,Half Life,Half-Lifes,Halflifes
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000284	Administration, Oral	The giving of drugs, chemicals, or other substances by mouth.	Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000328	Adult	A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available.	Adults
D013997	Time Factors	Elements of limited time intervals, contributing to particular results or situations.	Time Series,Factor, Time,Time Factor