Cloxacillin

MOA:

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.

Drug Label Information | Brands:

Brands of Cloxacillin in Kenya

Cosacillin®, Cosmos
Cloxacillin®, Elys
Kloxy®, Lab & Allied
Cloxapen®, Mac’s
Cloxashel®, Shelys
Cloxazen®, Zenufa
Dawaclox®, Dawa
Medibenin®, Medivet
Mediclox®, Regal
Orbenin®, GSK

INDICATIONS AND CLINICAL USE

The treatment of beta-hemolytic streptococcal and pneumococcal infections as well as staphylococcal infections (including those caused by beta-lactamase producing organisms).

In severe staphylococcal infections (septicaemia, osteomyelitis, endocarditis, pneumonia) or when staphylococci are suspected and treatment is required before sensitivity results are available, parenteral cloxacillin should be administered at once, followed by cloxacillin orally, when indicated. It is not effective against the so called “methicillin-resistant” strains of staphylococcus.

If the results of identification and susceptibility testing indicate that the infection is due to an organism other than a penicillinase producing staphylococcus susceptible to cloxacillin sodium, treatment should be discontinued and therapy with an alternative agent instituted

CONTRAINDICATIONS

Cloxacillin for Injection is contraindicated for use:•in patients who are hypersensitive to this drug, to penicillin, or to cephalosporins

Pharmacokinetics

Cloxacillin is stable in an acid medium and is approximately 50% absorbed orally. After an oral dose of 500mg 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

WARNINGS AND PRECAUTIONS

Hematologic:During long-term therapy, renal, hepatic and hematopoietic functions should be checked periodically.

Hepatic: During long-term therapy, renal, hepatic and hematopoietic functions should be checked periodically.

Immune: Serious and occasionally fatal hypersensitivity (anaphylactoid) reactions have been reported in patients receiving penicillin or cephalosporin therapy. These reactions are more apt to occur in individuals with a history or sensitivity to multiple allergens. Careful inquiry should be made concerning previous hypersensitivity to reactions to penicillins, cephalosporins or other allergens. If allergic or anaphylactic reactions occurs, discontinue treatment and administer the usual agents, e.g. antihistamines, pressor amines, corticosteroids.

Neurologic:The passage of any penicillin from blood into brain is facilitated by inflamed meninges and during cardiopulmonary bypass. In the presence of such factors, particularly in renal failure when high serum concentration can be attained, CNS adverse effects including myoclonia, convulsive seizures and depressed consciousness can be expected. Although this complication has not been reported with cloxacillin, it should be anticipated.

Sensitivity/Resistance: Candidiasis and other superinfections may occur, especially in debilitated and malnourished patients, or those with low resistance to infection due to corticosteroids, immunosuppressors or irradiation. If superinfection occurs, institute appropriate measures.

Renal: During long-term therapy, renal, hepatic and hematopoietic functions should be checked periodically.

ADVERSE REACTIONS

It may be expected the most common untoward reactions will be related to sensitivity. They are more likely to occur in individuals who have previously demonstrated hypersensitivity to penicillins and cephalosporins and in those with a history of allergy, asthma, hay fever or urticaria. All degrees of hypersensitivity, including fatal anaphylaxis, have been reported with penicillin.

Gastrointestinal: Nausea, vomiting, epigastric discomfort, flatulence and loose stools have been noted in some patients.

Hematologic: Eosinophilia, leucopenia, anemia, thrombocytopenia, thrombocytopenic, purpura, neutropenia and agranulocytosis have been reported during therapy with penicillins. These reactions are usually reversible on discontinuation of therapy and are believed to be hypersensitivity phenomena. Thrombophlebitis has occurred during the course of i.v. therapy. Mildly elevated SGOT level (less than 100 units) have been reported. Immune: Allergic reactions (rash, urticaria) including wheezing and sneezing have been reported.

DRUG INTERACTIONS
Drug-Drug Interactions
Probenecid: as with other penicillins, concurrent administration of probenecid enhances the serum concentration of cloxacillin.