Vecuronium inhibits histamine N-methyltransferase

Although there have been clinical reports of significant hypotension and flushing associated with the use of vecuronium, it produces minimal cardiovascular effects in the vast majority of patients. In addition, there is no evidence that vecuronium stimulates the release of histamine. The authors per...

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Bibliographic Details
Published in:Anesthesiology (Philadelphia) 1988-07, Vol.69 (1), p.92-96
Main Authors: FUTO, J, KUPFERBERG, J. P, MOSS, J, FAHEY, M. R, CANNON, J. E, MILLER, R. D
Format: Article
Language:English
Subjects:
Anesthetics. Neuromuscular blocking agents
Biological and medical sciences
Histamine N-Methyltransferase - antagonists & inhibitors
Humans
Medical sciences
Methyltransferases - antagonists & inhibitors
Neuropharmacology
Pharmacology. Drug treatments
Vecuronium Bromide - pharmacology
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Summary:Although there have been clinical reports of significant hypotension and flushing associated with the use of vecuronium, it produces minimal cardiovascular effects in the vast majority of patients. In addition, there is no evidence that vecuronium stimulates the release of histamine. The authors performed in vitro kinetic studies to determine the effect of vecuronium on histamine N-methyltransferase (HNMT), the primary catabolic enzyme for histamine in humans. They also examined plasma from patients who had received vecuronium (0.1 or 0.2 mg/kg) to determine whether clinically used concentrations of the drug could inhibit HNMT. It was determined that vecuronium is a strong inhibitor of HNMT; apparent Ki = 1 microM. The inhibition is competitive with respect to methyl-donor and noncompetitive with respect to histamine. Vecuronium, in doses greater than or equal to 0.1 mg/kg, may delay the metabolism of histamine by HNMT in vitro.
ISSN:0003-3022
1528-1175
DOI:10.1097/00000542-198807000-00014