Cefotiam

Antibacterial

ChEBI: A cephalosporin with ({1-[2-(dimethylamino)ethyl]-1H-tetrazol-5-yl}sulfanyl)methyl and (2-amino-1,3-thiazol-4-yl)acetamido substituents at positions 3 and 7, respectively, of the cephem skeleton. A third generation beta-lactam cephalospo in antibiotic, it is active against a broad spectrum of both Gram positive and Gram negative bacteria.

A semisynthetic cephalosporin formulated as the dihydrochloride for injection and as a prodrug ester, cefotiam hexetil, for oral administration. Activity is similar to that of cefuroxime, but it is somewhat more active against a range of enterobacteria .
A 30-min intravenous infusion of the dihydrochloride produces a peak serum concentration of 35 mg/L; the corresponding concentration after a 1 g intramuscular dose is 17 mg/L. Oral absorption of the hexetil ester is around 65%. Food delays absorption of the ester. The plasma half-life is 0.6–1.1 h. Around 40% is bound to plasma protein. Urinary excretion is almost complete 4 h after the end of intravenous infusion, but only 50–67% is recovered unchanged; there is substantial non-renal elimination and some evidence of saturation of renal tubular excretion at doses above 2 g. In anuria the plasma elimination half-life rises to 13 h and plasma and renal clearances parallel creatinine clearance. A small amount is excreted in bile. In patients with cholelithiasis given 0.5 or 1 g intravenously, mean concentrations in gallbladder bile and gallbladder wall 30 min after the dose were around 17 and 32 mg/L, respectively. In patients with normal liver function, hepatic bile concentrations can exceed 1 g/L.
It is generally well tolerated and has been used successfully to treat lower respiratory infections, skin and soft-tissue infection. It is not widely used, but is available in Japan and some other countries.