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Pharmacokinetics and Sedative Effect of Midazolam in Connection with Caesarean Section Performed Under Epidural Analgesia
Author(s) -
Kanto J.,
Aaltonen L.,
Erkkola R.,
Äärimaa L.
Publication year - 1984
Publication title -
acta anaesthesiologica scandinavica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.738
H-Index - 107
eISSN - 1399-6576
pISSN - 0001-5172
DOI - 10.1111/j.1399-6576.1984.tb02024.x
Subject(s) - midazolam , sedative , medicine , pharmacokinetics , anesthesia , volume of distribution , benzodiazepine , hypnotic , sedation , pharmacology , receptor
Midazolam, the new investigational 1,4‐benzodiazepine derivative with highly water‐soluble salts, was studied as an anaesthesiological adjuvant in 11 patients undergoing elective caeserean section under epidural analgesia. I.v. administered midazolam, 0.075 mg/kg after delivery, caused a rapid and marked sedative effect, lastingfor about 2–3 h. Short‐lasting anterograde amnesia of about 30 to 60 min was reported as well. The serum levels of the parent drug and its active metabolites were determined in six cases by a radioreceptor assay and pharmacokinetic parameters were calculated on the basis of these levels by a two‐compartment open model. Up to 3 h after midazolam administration, good correlation between the sedative effect and serum drug levels was found. The rapid but short‐lasting action can be explained by the pharmacokinetic parameters of midazolam: a short distribution phase half‐life (4.19 min), and a short elimination phase half‐life (67.85 min) due to a high clearance value (13.18 ml/min/kg) and a moderate distribution volume (1.20 1/kg).