Pharmacokinetics of CM 57755, a new histamine H2-receptor antagonist, after single oral doses in man.
The plasma pharmacokinetics and urinary excretion of CM 57755, an H2-receptor antagonist, were studied after administration of single oral doses in a range between a 100 and 700 mg in human volunteers. Pharmacokinetic parameters were calculated model-independent. Absorption of CM 57755 was bimodal and the maximum plasma concentration was reached between 2 and 4 h after dosing. The drug was widely distributed with an apparent volume of distribution between 140 and 200 l. The plasma clearance was between 56 and 69 L/h. The plasma concentrations declined following a monoexponential function with an elimination half-life of 2 h. No modification in the plasma clearance or other pharmacokinetic parameters with these doses was observed. Therefore, a linear pharmacokinetic profile of CM 57755 was proposed. About 40% of the parent drug was unchanged in urine excreted over the 24 h. The drug was compared with cimetidine and ranitidine, the three compounds seemed to exhibit a consistent pharmacokinetic profile.
Necciari
J
J
Mery
D
D
Garriot
P
P
Escourrou
J
J
Cautreels
W
W
D000284:Administration, Oral; D000328:Adult; D006635:Histamine H2 Antagonists / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D008297:Male; D009536:Niacinamide / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism
D006635:Histamine H2 Antagonists; D009536:Niacinamide; C041784:ramixotidine