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. 1982 Jun;13(6):785–790. doi: 10.1111/j.1365-2125.1982.tb01866.x

Bioavailability of dihydroergotamine in man.

P J Little, G L Jennings, H Skews, A Bobik
PMCID: PMC1402019  PMID: 7093108

Abstract

1 The pharmacokinetics of dihydroergotamine (DHE) in plasma were examined in six normotensive subjects after single acute doses of dihydroergotamine, 10 micrograms/kg i.v. and 10, 20 and 30 mg orally. 2 The mean apparent half-time of elimination was 2.37 +/- 0.29 h and plasma clearance of dHE was 1002 +/- 169 ml/min. 3 Mean apparent absorption of DHE determined from the 10 mg dose was 26.6 +/- 10% and ranged from 8.9 to 60.3%. The oral bioavailability after the 10, 20 and 30 mg doses averaged 0.47 +/- 0.07%, 0.59 +/- 0.13% and 0.52 +/- 0.14% respectively. Inter-patient variability in bioavailability was 6-fold. 4 The results indicate that pre-systemic 'first-pass' extraction of DHE is the main determinant of its oral bioavailability. Oral doses of the drug up to 30 mg do not saturate this extraction process resulting in apparently linear kinetics for the drug.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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