Human experience of cetiedil, a new vasodilator with anticholinergic properties

Abstract

Cetiedil, a new vasodilating drug with anticholinergic properties, was shown to be metabolised very rapidly in man after intravenous and oral administration of the 14C-compound. Higher concentrations of labelled compound after oral than after intravenous administration at the same sampling time, and proportional differences in urinary excretion, suggest that metabolic handling of the drug differs depending on the route of administration. Experiments in which inhibition of saliva secretion was measured indicated that (an) active metabolite(s) probably was (were) responsible for the action of the drug. As an anticholinergic drug, cetiedil is at least 400 times weaker than atropine.

Cetiedil, a Drug That Inhibits Acetylcholine Release in Torpedo Electric Organ

“…Cetiedil is also known to be an inhibitor of the calcium-activated potassium channel (Bookchin and Lew, 1983;Christophersen and Vestergaard-Bogin, 1985;Sarkadi et al, 1985) in cell membranes, and a role in neuromuscular transmission has been proposed for the calciumactivated potassium current observed in motor nerve terminals (Mallart, 1985). Adverse reactions to cetiedil, such as dryness of mouth, blurred vision, and disorientation, have been attributed to anticholinergic properties (Soeterboek et al, 1977;Boissier et al, 1978;Cho et al, 1979;Haringet al, 1980;Mankad et al, 1983). Eserine was recommended for preventing these adverse reactions (Linquette et al, 1973).…”