AbstractThe aim of this investigation was to assess the pharmacokinetics and bioavailability of ergometrine in six human male subjects after an oral dose of 0·200 mg and after an intravenous dose of 0·075 mg of ergometrine maleate. A large variation in bioavailability of between 34% and 117% in the six volunteers was observed. The lag time was also subject dependent and ranged between 0·0073 h (0.4 mm) and 0·47 h (28 min). After intravenous administration, the pharmacokinetic profile can be described by a twocompartment model. The distribution half‐lifet1/2αis 0·18 ± 0·20 h, the elimination half‐lifet1/2βis 2·0 ± 0·90 h, the total body clearance (CL) amounts to 35·9 ± 13·41 h−1and the steady‐state volume (Vss) of distribution is 73·4 ± 22·01. After oral administration, the pharmacokinetic profile can be described by a one‐compartment model. The absorption half‐lifet1/2absis 0·19 ± 0·22 h, and the elimination half‐lifet1/2β1·90 ± 0·16 h. This study with oral ergometrine shows such a large interindividual variability in bioavailability that the oral route of administration does not seem not to be the most reliable means of accurate dosing