Pharmacokinetics of dihydroergotamine following subcutaneous administration in humans.
The pharmacokinetics of dihydroergotamine was studied following a 1.5-mg subcutaneous dose of the mesylate salt in six healthy volunteers. Plasma and urine dihydroergotamine, determined using a specific radioimmunoassay, were simultaneously fitted to equations consistent with a two-compartment open model. The drug was rapidly absorbed from the injection site; peak plasma concentrations of 3-8 ng/ml were observed within 15-45 min of dosing. Half-lives for the rapid and slow phases of decline in plasma dihydroergotamine were 0.95 and 7.26 h, respectively. The overall volume of distribution was 14.6 l/kg. The plasma clearance and renal clearance values were 1814 and 91 ml/min, respectively, indicating that 5% of the dose was excreted unchanged in the urine. Comparison of the results of the present study to published data confirmed that dihydroergotamine is eliminated from the body predominantly by metabolism.
D000328:Adult; D004087:Dihydroergotamine / Q000008:administration & dosage / Q000378:metabolism*; D006801:Humans; D007279:Injections, Subcutaneous; D007700:Kinetics; D008297:Male; D011863:Radioimmunoassay
D004087:Dihydroergotamine