The pharmacokinetics, urinary and biliary excretion of pipecuronium bromide.
The pharmacodynamics and -kinetics of pipecuronium were studied in 12 patients, six of whom received 100 micrograms kg-1 for laryngectomy (Group L), and six who underwent choledochotomy after insertion of the T-drain and were given 50 micrograms kg-1 (Group C). Onset time and clinical duration were 2.3 and 109 min and 2.8 and 39 min in Groups L and C, respectively. All patients could be sufficiently reversed with neostigmine. Terminal half-lives were 101.5 min (Group L) and 179 min (Group C) in a three-exponent decay; the distribution volumes at steady state 0.339 l kg-1 (Group L) and 0.506 l kg-1 (Group C); the plasma clearance 3.4 ml kg-1 min-1 (Group L) and 2.5 ml kg-1 min-1 (Group C). Within 24 h, 38.6% and 37% were excreted unchanged in the urine and 4.4% and 1% as 3-desacetyl pipecuronium in Groups L and C, respectively. Within 24 h only 2% was excreted into the bile in Group C. Distribution volume and terminal half-life in Group C were positively correlated with pre-operative serum aminotransferase levels (P less than 0.005).
Wierda
J M
JM
Department of Pharmacology and Pharmacotherapeutics, University of Groningen, The Netherlands.
Szenohradszky
J
J
De Wit
A P
AP
Zentai
G
G
Agoston
S
S
Kakas
M
M
Kleef
U W
UW
Meijer
D K
DK
D000410:Alanine Transaminase / Q000097:blood; D015113:Androstane-3,17-diol / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology / Q000652:urine; D000769:Anesthesia, Inhalation; D000771:Anesthesia, Intravenous; D001219:Aspartate Aminotransferases / Q000097:blood; D001646:Bile / Q000378:metabolism*; D001651:Cholestasis, Extrahepatic / Q000378:metabolism; D003135:Common Bile Duct / Q000601:surgery; D005260:Female; D006801:Humans; D007825:Laryngectomy; D008297:Male; D008875:Middle Aged; D009119:Muscle Contraction / Q000187:drug effects; D009466:Neuromuscular Blocking Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000652:urine; D003473:Neuromuscular Nondepolarizing Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000652:urine; D017300:Pipecuronium; D010879:Piperazines / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000652:urine; D013933:Thumb; D013997:Time Factors; D014459:Ulnar Nerve / Q000187:drug effects
D009466:Neuromuscular Blocking Agents; D003473:Neuromuscular Nondepolarizing Agents; D010879:Piperazines; D017300:Pipecuronium; D015113:Androstane-3,17-diol; D001219:Aspartate Aminotransferases; D000410:Alanine Transaminase