Penicillin

(penicillinase-
resistant)
Indications
Treatment of infections caused by penicillinase-producing staphylococci. May be used to initiate therapy in suspected
cases of resistant staphylococcal infections prior to the availability of laboratory test results.
Oral
Staphylococcal infections resistant to benzylpenicillin
Adult: 250-500 mg 4 times daily.
Child: 50-100 mg/kg in divided doses every 6 hr.
Incompatibility: Incompatible with aminoglycosides and a number of other antimicrobials.
Contraindications
Hypersensitivity to penicillins.
Warnings /
Precautions
Serious and occasionally fatal hypersensitivity (anaphylactic shock with collapse) reactions reported; initiate only after a
comprehensive drug and allergy history has been obtained. Caution with history of allergy and/or asthma. Should not be
relied upon in patients with severe illness, N/V, gastric dilatation, cardiospasm, or intestinal hypermotility. May result in
bacterial resistance with prolonged use or use in the absence of a proven/suspected bacterial infection or a prophylactic
indication; take appropriate measures if superinfection develops. Change to another active agent if culture tests fail to
demonstrate the presence of staphylococci. Monitor organ system functions (eg, renal, hepatic, and hematopoietic)
periodically with prolonged use. If renal impairment is suspected/known, reduce dose and monitor blood levels. Monitor
for possible liver function abnormalities.
Adverse Reactions
Allergic reactions, N/V, diarrhea, stomatitis, black or hairy tongue, GI irritation, agranulocytosis, rash, Sore mouth or
tongue.
Potentially Fatal: Neuromuscular hypersensitivity; pseudomembranous colitis; anaphylaxis.
Drug Interactions
Co-admin of probenecid or disulfiram may result in higher cloxacillin concentration. Chloramphenicol and tetracycline
antagonise bactericidal effect of penicillins.
Potentially Fatal: Increased hypoprothrombinaemic effects of oral anticoagulants.
Lab Interactions
Interferes with urinary glucose tests using cupric sulfate. False-positive results in urine and serum protein, uric acid and
urinary steroid tests.
Food Interactions
Delayed absorption in the presence of food.
Mechanism of Actions
Cloxacillin is resistant to degradation by penicillinases. It is particularly useful against penicillinase-producing
staphylococci. Highly active against S aureus, S pyogenes, S viridans and S pneumoniae.
Absorption: Incompletely absorbed from the GI tract with peak plasma concentrations after 1-2 hr (oral); may be
reduced in the presence of food. Completely absorbed with peak plasma concentrations after 30 min (IM).
Distribution: Pleural and synovial fluids and bone (therapeutic concentrations), CSF (small amounts except when the
meninges are inflamed; crosses the placenta and enters the breast milk. Protein-binding: 94%
Metabolism: Minimal metabolism.
Excretion: Via the urine by glomerular filtration and renal tubular secretion (35% of an oral dose); via the bile (Up to
10%). Not removed by dialysis; 0.5-1 hr (elimination half-life).
Assesment
Assess for drug hypersensitivity, history of allergy/asthma, severe illness, N/V, gastric dilatation, cardiospasm, renal
impairment, intestinal hypermotility, pregnancy/nursing status, and possible drug interactions. Obtain bacteriologic
studies with susceptibility testing, blood cultures, WBC, and differential cell count prior to therapy.
Monitoring
Monitor for hypersensitivity reactions, development of superinfection, new infection, and renal/hepatic impairment.
Monitor organ system function periodically during prolonged therapy. Monitor blood cultures, WBC and differential cell
count weekly. Monitor BUN, urinalysis, creatinine, ALT, and AST periodically.
Patient Counselling
Counsel that drug should only be used to treat bacterial, and not viral, infections (eg, common cold). Advise to take
exactly ud; inform that skipping doses or not completing full course may decrease effectiveness and increase resistance.
Advise not to take drug if with previous allergic reaction to PCN and to inform physician of any allergies or previous
allergic reactions to any drugs. Advise to take 1 hr ac or 2 hrs pc. Advise to d/c and notify physician if SOB, wheezing,
skin rash, mouth irritation, black tongue, sore throat, N/V, diarrhea, fever, swollen joints, or any unusual bleeding or
bruising occurs. Advise to notify physician if taking additional medications, including nonprescription drugs.
Administration
Should be taken on an empty stomach. (Take on an empty stomach 1 hr before or 2 hr after meals.)
Pregnancy Category
B: Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-
controlled studies in pregnant women OR Animal studies have shown an adverse effect, but adequate and well-
controlled studies in pregnant women have failed to demonstrate a risk to the fetus in any trimester.