Plasma and skin blister fluid levels of cefotiam and cefmenoxime after single intramuscular application of 1 g in gonorrhea.
To predict the clinical efficacy of a new antibiotic in uncomplicated gonorrhea, data pertinent to its pharmacokinetics in man are needed. Before starting clinical trials on cefotiam and cefmenoxime, 1 g of each antibiotic was administered intramuscularly as a single dose to 5 healthy volunteers. Both blood and skin blister fluid samples (obtained by suction and cantharides blistering) were repeatedly taken. Peak plasma levels amounted on average to 24.8 and 48.2 micrograms/ml, respectively. 6 h after dose still average plasma concentrations of 3.4 and 6.52 micrograms/ml were found. Suction blister fluid levels essentially paralleled plasma levels, whereas cantharides blister fluid levels increased and decreased more slowly than plasma levels. Cefotiam penetrated more readily into suction blister fluid than cefmenoxime as obtained from area ratios. Thus, the chosen dosage regimens considered apt for gonorrhea led to high initial as well as long-standing drug levels. And this does not only hold true for the plasma. Facing their good in vitro activity on Neisseria gonorrhoeae, cefotiam and cefmenoxime well deserve further studies in this field including clinical trials.
D000328:Adult; D001768:Blister / Q000209:etiology / Q000378:metabolism*; D002193:Cantharidin; D015281:Cefmenoxime; D002439:Cefotaxime / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism; D015310:Cefotiam; D005260:Female; D006069:Gonorrhea / Q000188:drug therapy*; D006801:Humans; D007273:Injections, Intramuscular; D007700:Kinetics; D008297:Male; D013396:Suction
D015310:Cefotiam; D002193:Cantharidin; D015281:Cefmenoxime; D002439:Cefotaxime