Hydrolysis of Cefamandole Nafate to Cefamandole in Vivo

The hydrolysis of cefamandole nafate, and the O-formyl ester of cefamandole, to cefamandole was studied in vivo in dogs and normal human subjects. After administration of cefamandole nafate to dogs or humans, the parent compound disappeared rapidly from plasma. Disappearance was slightly faster in d...

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Bibliographic Details
Published in:The Journal of infectious diseases 1978-05, Vol.137 (Supplement), p.S17-S24
Main Authors: Wold, J. S., Joost, R. R., Black, H. R., Griffith, R. S.
Format: Article
Language:English
Subjects:
Animals
Antibiotics
Bicarbonates - administration & dosage
Blood
Blood plasma
Cefamandole - administration & dosage
Cefamandole - analogs & derivatives
Cefamandole - metabolism
Cephalosporins - metabolism
Chemistry and in vitro Studies
Dogs
Dosage
Drug Combinations
Excretion
Female
Half-Life
Human resources
Humans
Hydrolysis
Intravenous injections
Male
Pharmacokinetics
Sodium - administration & dosage
Urine
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Summary:The hydrolysis of cefamandole nafate, and the O-formyl ester of cefamandole, to cefamandole was studied in vivo in dogs and normal human subjects. After administration of cefamandole nafate to dogs or humans, the parent compound disappeared rapidly from plasma. Disappearance was slightly faster in dogs (half-life [t½], 4–6 min) than in humans (t½, 6–9 min). The calculated rate constant for hydrolysis of cefamandole nafate was also higher in dogs than in humans, yielding t½ values of 6–7 min and 10–17 min, respectively. The rapid hydrolysis of cefamandole nafate to cefamandole in vivo, combined with the partial hydrolysis of cefamandole nafate in vitro before administration (caused by Na2CO3 in the formulation), resulted in circulating levels of cefamandole nafate lower than those of cefamandole. In humans the disappearance of cefamandole nafate was not significantly altered after administration of large (4.0 g) or multiple (4.0 g every 6 hr) doses of cefamandole nafate.
ISSN:0022-1899
1537-6613
DOI:10.1093/infdis/137.Supplement.S17