Pharmacokinetics and pharmacodynamics of emepronium bromide (Cetiprin) after intravenous administration in man.
Intravenous doses of 1, 5, 10 and 15 mg of emepronium bromide were given to three healthy volunteers. Emepronium serum concentration declined in a triexponential manner with half-lives between 2.2-3.0 min., 1.0-1.6 hours and 5.1-13 hours, respectively. The initial dilution space (volume of the central compartment) varied between 4.1-7.5 l. The area under the serum concentration time curve increased linearly with dose, indicating constancy of total serum clearance (range: 24-38 l/hr) with dose. The renal clearance of emepronium varied with serum concentration; secretion in addition to glomerular filtration was evident. Tubular secretion of emepronium was half-saturated at serum concentrations of approximately 50 nmol/l. No obvious drug-related effect on blood pressure was noted, whereas salivary secretion decreased and heart rate increased with 10-15% at emepronium serum concentrations of about 200 nmol/l. ECG recordings were without abnormalities after slow intravenous injections of emepronium bromide in doses of up to 15 mg. Since no adverse effects were noted, intravenous administration of emepronium bromide may be an alternative in situations where the drug is now used intramuscularly e.g. severe tenesmus in the urinary bladder.
D000284:Administration, Oral; D000328:Adult; D004629:Emepronium / Q000008:administration & dosage / Q000378:metabolism*; D005260:Female; D006339:Heart Rate; D006801:Humans; D007273:Injections, Intramuscular; D007668:Kidney / Q000378:metabolism; D007700:Kinetics; D008297:Male; D008657:Metabolic Clearance Rate; D000644:Quaternary Ammonium Compounds / Q000378:metabolism*; D012463:Saliva / Q000378:metabolism
D000644:Quaternary Ammonium Compounds; D004629:Emepronium