Pharmacology: Pharmacodynamics: Cloxacillin exerts a bacterial action against susceptible microorganisms during the stage of active multiplication. It acts through the inhibition of biosynthesis of cell wall mucopeptides.
Cloxacillin demonstrates activity against strains of beta-hemolytic streptococci, pneumococci, penicillin G sensitive staphylococci and, due to its resistance to penicillinase, penicillin G resistant (β-lactamase producing) staphylococci. Cloxacillin displays less intrinsic antibacterial activity and a narrower spectrum than penicillin G.
Pharmacokinetics: Cloxacillin is stable in an acid medium and is approximately 50% absorbed orally. After an oral dose of 500 mg cloxacillin, a peak serum level of about 8 micrograms/mL is reached in about 1 hour. The serum level after i.m. cloxacillin is approximately twice that obtained when the same dose is given orally to fasting adults. Food in the stomach or small intestine reduces absorption and peak serum levels are approximately 50% those obtained after fasting. As with other penicillins, concurrent administration of probenecid enhances the serum concentration.
Once absorbed, approximately 94% are bound to plasma proteins. After oral administration, roughly 20% of the dose is excreted in the urine, together with one or more active metabolites as yet unidentified. The half life of elimination is about 30 minutes.
Toxicology: Preclinical safety data: No further information of relevance to add.
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