Drug Groups

approved

Description

One of the penicillins which is resistant to penicillinase. [PubChem]

Indication

Used to treat infections caused by penicillinase-producing staphylococci which have demonstrated susceptibility to the drug.

Pharmacology

Dicloxacillin is a beta-lactamase resistant penicillin similar to oxacillin. Dicloxacillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of dicloxacillin results from the inhibition of cell wall synthesis and is mediated through dicloxacillin binding to penicillin binding proteins (PBPs). Dicloxacillin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.

Toxicity

Oral LD₅₀ in rat is 3579 mg/kg. Symptoms of overexposure include irritation, rash, labored breathing, hives, itching, wheezing, nausea, chills, and fever.

Affected Organisms

Absorption

Absorption of the isoxazolyl penicillins after oral administration is rapid but incomplete: peak blood levels are achieved in 1-1.5 hours. Oral absorption of cloxacillin, dicloxacillin, oxacillin and nafcillin is delayed when the drugs are administered after meals.

Half Life

The elimination half-life for dicloxacillin is about 0.7 hour.

Protein Binding

Binds to serum protein, mainly albumin.

Elimination

Dicloxacillin sodium is rapidly excreted as unchanged drug in the urine by glomerular filtration and active tubular secretion.

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