BACTROBAN

BACTROBAN- mupirocin calcium cream
Lake Erie Medical & Surgical Supply DBA Quality Care Products LLC

DESCRIPTION

BACTROBAN CREAM (mupirocin calcium cream, 2%) contains the dihydrate crystalline calcium hemi-salt of the antibiotic mupirocin. Chemically, it is (αE ,2S ,3R ,4R ,5S)-5-[(2S ,3S ,4S ,5S)-2,3-Epoxy-5-hydroxy-4-methylhexyl]tetrahydro-3,4-dihydroxy-β-methyl-2H -pyran-2-crotonic acid, ester with 9-hydroxynonanoic acid, calcium salt (2:1), dihydrate.

The molecular formula of mupirocin calcium is (C26 H43 O9 )2 Ca•2H2 O, and the molecular weight is 1075.3. The molecular weight of mupirocin free acid is 500.6. The structural formula of mupirocin calcium is:

chemical structure
(click image for full-size original)

BACTROBAN CREAM is a white cream that contains 2.15% w/w mupirocin calcium (equivalent to 2.0% mupirocin free acid) in an oil and water-based emulsion. The inactive ingredients are benzyl alcohol, cetomacrogol 1000, cetyl alcohol, mineral oil, phenoxyethanol, purified water, stearyl alcohol, and xanthan gum.

CLINICAL PHARMACOLOGY

Pharmacokinetics

Systemic absorption of mupirocin through intact human skin is minimal. The systemic absorption of mupirocin was studied following application of BACTROBAN CREAM 3 times daily for 5 days to various skin lesions (>10 cm in length or 100 cm2 in area) in 16 adults (aged 29 to 60 years) and 10 children (aged 3 to 12 years). Some systemic absorption was observed as evidenced by the detection of the metabolite, monic acid, in urine. Data from this study indicated more frequent occurrence of percutaneous absorption in children (90% of patients) compared to adults (44% of patients); however, the observed urinary concentrations in children (0.07 — 1.3 mcg/mL [1 pediatric patient had no detectable level]) are within the observed range (0.08 — 10.03 mcg/mL [9 adults had no detectable level]) in the adult population. In general, the degree of percutaneous absorption following multiple dosing appears to be minimal in adults and children. Any mupirocin reaching the systemic circulation is rapidly metabolized, predominantly to inactive monic acid, which is eliminated by renal excretion.

Microbiology

Mupirocin is an antibacterial agent produced by fermentation using the organism Pseudomonas fluorescens. It is active against a wide range of gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA). It is also active against certain gram-negative bacteria. Mupirocin inhibits bacterial protein synthesis by reversibly and specifically binding to bacterial isoleucyl transfer-RNA synthetase. Due to this unique mode of action, mupirocin demonstrates no in vitro cross-resistance with other classes of antimicrobial agents.

Resistance occurs rarely; however, when mupirocin resistance does occur, it appears to result from the production of a modified isoleucyl-tRNA synthetase. High-level plasmid-mediated resistance (MIC >1024 mcg/mL) has been reported in some strains of Staphylococcus aureus and coagulase-negative staphylococci.

Mupirocin is bactericidal at concentrations achieved by topical application. The minimum bactericidal concentration (MBC) against relevant pathogens is generally 8-fold to 30-fold higher than the minimum inhibitory concentration (MIC). In addition, mupirocin is highly protein bound (>97%), and the effect of wound secretions on the MICs of mupirocin has not been determined.

Mupirocin has been shown to be active against most strains of S. aureus and Streptococcus pyogenes , both in vitro and in clinical studies. (See INDICATIONS AND USAGE.) The following in vitro data are available, BUT THEIR CLINICAL SIGNIFICANCE IS UNKNOWN. Mupirocin is active against most strains of Staphylococcus epidermidis and Staphylococcus saprophyticus.

INDICATIONS AND USAGE

BACTROBAN CREAM is indicated for the treatment of secondarily infected traumatic skin lesions (up to 10 cm in length or 100 cm2 in area) due to susceptible strains of S. aureus and S. pyogenes.

CONTRAINDICATIONS

BACTROBAN CREAM is contraindicated in patients with known hypersensitivity to any of the constituents of the product.

WARNINGS

Avoid contact with the eyes.

In the event of a sensitization or severe local irritation from BACTROBAN CREAM, usage should be discontinued, and appropriate alternative therapy for the infection instituted.

PRECAUTIONS

General

As with other antibacterial products, prolonged use may result in overgrowth of nonsusceptible microorganisms, including fungi. (See DOSAGE AND ADMINISTRATION.)

BACTROBAN CREAM is not formulated for use on mucosal surfaces.

Information for Patients

• Use this medication only as directed by your healthcare provider. It is for external use only. Avoid contact with the eyes.

• The treated area may be covered by gauze dressing if desired.

• Report to your healthcare provider any signs of local adverse reactions. The medication should be stopped and your healthcare provider contacted if irritation, severe itching, or rash occurs.

• If no improvement is seen in 3 to 5 days, contact your healthcare provider.

Drug Interactions

The effect of the concurrent application of topical mupirocin calcium cream and other topical products has not been studied.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term studies in animals to evaluate carcinogenic potential of mupirocin calcium have not been conducted.

Results of the following studies performed with mupirocin calcium or mupirocin sodium in vitro and in vivo did not indicate a potential for mutagenicity: Rat primary hepatocyte unscheduled DNA synthesis, sediment analysis for DNA strand breaks, Salmonella reversion test (Ames), Escherichia coli mutation assay, metaphase analysis of human lymphocytes, mouse lymphoma assay, and bone marrow micronuclei assay in mice.

Fertility studies were performed in rats with mupirocin administered subcutaneously at doses up to 49 times a human topical dose of 1 gram/day (approximately 20 mg mupirocin per day) on a mg/m2 basis and revealed no evidence of impaired fertility from mupirocin sodium.

Pregnancy

Teratogenic Effects: Pregnancy Category B. Teratology studies have been performed in rats and rabbits with mupirocin administered subcutaneously at doses up to 78 and 154 times, respectively, a human topical dose of 1 gram/day (approximately 20 mg mupirocin per day) on a mg/m2 basis and revealed no evidence of harm to the fetus due to mupirocin. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when BACTROBAN CREAM is administered to a nursing woman.

Pediatric Use

The safety and effectiveness of BACTROBAN CREAM have been established in the age groups 3 months to 16 years. Use of BACTROBAN CREAM in these age groups is supported by evidence from adequate and well-controlled studies of BACTROBAN CREAM in adults with additional data from 93 pediatric patients studied as part of the pivotal trials in adults. (See CLINICAL STUDIES.)

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