Pharmacokinetics and bioavailability of ergoloid mesylates.
Article Details
- CitationCopy to clipboard
Schran HF, McDonald S, Lehr R
Pharmacokinetics and bioavailability of ergoloid mesylates.
Biopharm Drug Dispos. 1988 Jul-Aug;9(4):349-61. doi: 10.1002/bod.2510090404.
- PubMed ID
- 3207855 [ View in PubMed]
- Abstract
The pharmacokinetics and bioavailability of ergoloid mesylates following single administrations of various dose levels (3-9 mg), dosage forms (oral swallow and sublingual tablets, solution) and under different dosing conditions (fasted, with meal) were studied in young healthy volunteers. Male and female subjects showed a similar rate and extent of bioavailable ergoloid after drug treatment. The absorption of ergoloid using either the tablet dosage forms or the drug administered as a solution was rapid, with peak levels of about 60-80 pg ml-1 mg-1 dose achieved after 0.6 to 1.3 h. The elimination half-life for ergoloid in plasma was 2-5 h. Administration of drug with food had no effect on the extent of absorption (AUC) but lowered the absorption rate. This resulted in a reduction of (by 25 per cent) and delay in (by 1 h) achieving peak levels (Cmax). Increasing the ergoloid dose caused a proportional increase in the AUC, but a smaller than proportional increase for Cmax. The tablet formulations provided similar AUCs as the solution; the objective of the sublingual tablet formulation to provide improved bioavailability over the swallow tablet via circumvention of first-pass metabolism was therefore not realized. Transient decreases in blood pressure after ergoloid treatment paralleled the plasma level profiles. Higher ergoloid levels were paired with the larger pressure decreases.
DrugBank Data that Cites this Article
- Drugs
- Food Interactions
Drug Interaction Ergoloid mesylate Take with or without food. Taking ergoloid mesylate with food may reduce gastrointestinal upset.