Mupirocin Cream

Mupirocin cream USP, 2% contains the dihydrate crystalline calcium hemi-salt of the RNA synthetase inhibitor antibacterial, 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 USP is (C26H43O9)2 Ca•2H2O, and the molecular weight is 1075.3. The molecular weight of mupirocin free acid is 500.6. The structural formula of mupirocin calcium USP is:

Mupirocin cream USP is a white cream that contains 2.15% w/w mupirocin calcium USP (equivalent to 2% mupirocin free acid) in an oil- and water-based emulsion. The inactive ingredients are benzyl alcohol, glycerol monostearate, mineral oil, phenoxyethanol, polyoxyl 20 cetostearyl ether, purified water and xanthan gum.

Dosage Forms And Strengths

Mupirocin cream USP is a white cream that contains 2.15% w/w mupirocin calcium USP (equivalent to 2% mupirocin free acid) in an oil- and water-based emulsion supplied in 15-gram and 30-gram tubes.

Stronge And Handling

Mupirocin cream USP, 2% is supplied in 15-gram and 30-gram tubes.

Mupirocin cream USP is a white cream that contains 2.15% w/w mupirocin calcium USP (equivalent to 2% mupirocin free acid) in an oil- and water-based emulsion.

NDC 69150-225-01 15-gram tube (1 tube per carton)
NDC 69150-225-03 30-gram tube (1 tube per carton)

Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Do not freeze.

Manufactured by: Biomes Pharmaceuticals LLC.,Lansing, MI 48906. Revised: Mar 2016

Included as part of the "PRECAUTIONS" Section

Mupirocin 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 isolates of Staphylococcus aureus (S. aureus) and Streptococcus pyogenes (S. pyogenes).

Mupirocin Cream USP is a white cream that contains 2.15% w/w mupirocin calcium, USP (equivalent to 2% mupirocin free acid) in an oil-and water-based emulsion supplied in 15-gram and 30-gram tubes.

Mupirocin Cream USP, 2% contains the dihydrate crystalline calcium hemisalt of the RNA synthetase inhibitor antibacterial, 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, USP is (C26H43O9)2Ca•2H2O, and the molecular weight is 1075.3. The molecular weight of mupirocin free acid is 500.6. The structural formula of mupirocin calcium, USP is:

Figure 1. Structure of Mupirocin Cream, USP

Mupirocin Cream USP is a white cream that contains 2.15% w/w mupirocin calcium, USP (equivalent to 2% mupirocin free acid) in an oil-and water-based emulsion. The inactive ingredients are benzyl alcohol, glycerol monostearate, mineral oil, phenoxyethanol, polyoxyl 20 cetostearyl ether, purified water and xanthan gum.

Mechanism of Action

Mupirocin is an RNA synthetase inhibitor antibacterial [see Microbiology (12.4)].

Pharmacokinetics

Absorption

Systemic absorption of mupirocin through intact human skin is minimal. The systemic absorption of mupirocin was studied following application of Mupirocin Cream 3 times daily for 5 days to various skin lesions greater than 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 trial indicated more frequent occurrence of percutaneous absorption in children (90% of subjects) compared with adults (44% of subjects); however, the observed urinary concentrations in children (0.07 to 1.3 mcg per mL [1 pediatric subject had no detectable level]) are within the observed range (0.08 to 10.03 mcg per 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.

The effect of the concurrent application of Mupirocin Cream with other topical products has not been studied [see Dosage and Administration (2)].

Elimination

In a trial conducted in 7 healthy adult male subjects, the elimination half-life after intravenous administration of mupirocin was 20 to 40 minutes for mupirocin and 30 to 80 minutes for monic acid.

Metabolism: Following intravenous or oral administration, mupirocin is rapidly metabolized. The principal metabolite, monic acid, demonstrates no antibacterial activity.

Excretion: Monic acid is predominantly eliminated by renal excretion.

Microbiology

Mupirocin is an RNA synthetase inhibitor antibacterial produced by fermentation using the organism Pseudomonas fluorescens.

Mechanism of Action

Mupirocin inhibits bacterial protein synthesis by reversibly and specifically binding to bacterial isoleucyl-transfer RNA (tRNA) synthetase.

Mupirocin is bactericidal at concentrations achieved by topical administration. Mupirocin is highly protein bound (greater than 97%) and the effect of wound secretions on the minimum inhibitory concentrations (MICs) of mupirocin has not been determined.

Resistance

When mupirocin resistance occurs, it results from the production of a modified isoleucyl-tRNA synthetase, or the acquisition of, by genetic transfer, a plasmid mediating a new isoleucyl-tRNA synthetase. High-level plasmid-mediated resistance (MIC ≥512 mcg/mL) has been reported in increasing numbers of isolates of S. aureus and with higher frequency in coagulase-negative staphylococci. Mupirocin resistance occurs with greater frequency in methicillin-resistant than methicillin-susceptible staphylococci.

Cross Resistance

Due to its mode of action, mupirocin does not demonstrate cross resistance with other classes of antimicrobial agents.

Antimicrobial Activity

Mupirocin has been shown to be active against susceptible isolates of S. aureus and S. pyogenes, both in vitro and in clinical trials [see Indications and Usage (1)]. The following in vitro data are available, but their clinical significance is unknown. Mupirocin is active against most isolates of Staphylococcus epidermidis.

Susceptibility Test Methods

High-level mupirocin resistance (≥512 mcg/mL) may be determined using standard disk diffusion or broth microdilution tests.1,2 Because of the occurrence of mupirocin resistance in methicillin-resistant S. aureus (MRSA), it is appropriate to test MRSA populations for mupirocin susceptibility prior to the use of mupirocin using a standardized method. 3,4,5

Advise the patient to read the FDA-approved patient labeling (Patient Information).

Advise the patient to administer Mupirocin Cream as follows:

• Use Mupirocin Cream only as directed by the healthcare provider. It is for external use only. Avoid contact of Mupirocin Cream with the eyes. If Mupirocin Cream gets in the eyes, rinse thoroughly with water. • Do not use Mupirocin Cream in the nose. • Wash your hands before and after applying Mupirocin Cream. • Use a gauze pad or cotton swab to apply a small amount of Mupirocin Cream to the affected area. The treated area may be covered by gauze dressing if desired. • Report to the healthcare provider any signs of local adverse reactions. Mupirocin Cream should be stopped and the   healthcare provider contacted if irritation, severe itching, or rash occurs. • Report to the healthcare provider or go to the nearest emergency room if severe allergic reactions, such as swelling of the lips, face, or tongue, or wheezing occur [see Warnings and Precautions (5.1)]. • If no improvement is seen in 3 to 5 days, contact the healthcare provider.

Trademarks are the property of their respective owners.

Manufactured by:

Glenmark Pharmaceuticals Ltd.

Colvale-Bardez, Goa 403 513, India

Manufactured for:

Glenmark Pharmaceuticals Inc., USA

Mahwah, NJ 07430

Questions? 1 (888)721-7115

www.glenmarkpharma.com/usa

July 2017