MUPIROCIN CALCIUM- mupirocin calcium cream
Prasco Laboratories
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HIGHLIGHTS OF PRESCRIBING INFORMATIONThese highlights do not include all the information needed to use Mupirocin Calcium Cream safely and effectively. See full prescribing information for Mupirocin Calcium Cream.
Mupirocin calcium cream, for topical use Initial U.S. Approval: 1997 INDICATIONS AND USAGEMupirocin calcium cream is an RNA synthetase inhibitor antibacterial 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 and Streptococcus pyogenes. (1) DOSAGE AND ADMINISTRATION
DOSAGE FORMS AND STRENGTHSCream: 2.15% w/w mupirocin calcium (equivalent to 2% mupirocin free acid) in 15-gram and 30-gram tubes. (3) CONTRAINDICATIONS
WARNINGS AND PRECAUTIONS
ADVERSE REACTIONS
To report SUSPECTED ADVERSE REACTIONS, contact GlaxoSmithKline at 1-888-825-5249 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling. Revised: 12/2015 |
Mupirocin calcium 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 calcium cream is a white cream that contains 2.15% w/w mupirocin calcium (equivalent to 2% mupirocin free acid) in an oil- and water‑based emulsion supplied in 15-gram and 30-gram tubes.
Mupirocin calcium cream is contraindicated in patients with known hypersensitivity to mupirocin or any of the excipients of Mupirocin calcium cream.
Systemic allergic reactions, including anaphylaxis, urticaria, angioedema, and generalized rash have been reported in patients treated with formulations of mupirocin, including Mupirocin calcium cream [see Adverse Reactions (6.2)].
Avoid contact with the eyes. In case of accidental contact, rinse well with water.
In the event of a sensitization or severe local irritation from Mupirocin calcium cream, usage should be discontinued, and appropriate alternative therapy for the infection instituted.
Clostridium difficile-associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.
C. difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin-producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibacterial drug use. Careful medical history is necessary since CDAD has been reported to occur over 2 months after the administration of antibacterial agents.
If CDAD is suspected or confirmed, ongoing antibacterial drug use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibacterial treatment of C. difficile, and surgical evaluation should be instituted as clinically indicated.
The following adverse reactions are discussed in more detail in other sections of the labeling:
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice.
In 2 randomized, double‑blind, double‑dummy trials, 339 subjects were treated with topical Mupirocin calcium cream plus oral placebo. Adverse reactions occurred in 28 (8.3%) subjects. The following adverse reactions were reported by at least 1% of subjects in connection with the use of Mupirocin calcium cream in clinical trials: headache (1.7%), rash (1.1%), and nausea (1.1%).
Other adverse reactions which occurred in less than 1% of subjects were: abdominal pain, burning at application site, cellulitis, dermatitis, dizziness, pruritus, secondary wound infection, and ulcerative stomatitis.
In a supportive trial in the treatment of secondarily infected eczema, 82 subjects were treated with Mupirocin calcium cream. The incidence of adverse reactions was as follows: nausea (4.9%), headache, and burning at application site (3.6% each), pruritus (2.4%), and 1 report each of abdominal pain, bleeding secondary to eczema, pain secondary to eczema, hives, dry skin, and rash.
In addition to adverse reactions reported from clinical trials, the following reactions have been identified during postmarketing use of Mupirocin calcium cream. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made. These reactions have been chosen for inclusion due to a combination of their seriousness, frequency of reporting, or potential causal relationship to Mupirocin calcium cream.
Immune System Disorders
Systemic allergic reactions, including anaphylaxis, urticaria, angioedema, and generalized rash [see Warnings and Precautions (5.1)].
Pregnancy Category B.
There are no adequate and well-controlled studies of Mupirocin calcium cream (contains equivalent of 2% mupirocin free acid) 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.
Developmental toxicity studies have been performed with mupirocin administered subcutaneously to rats and rabbits at doses up to 160 mg per kg per day in both species. This dose is 22 and 43 times, respectively, the human topical dose (approximately 60 mg mupirocin per day) based on body surface area. There was no evidence of fetal harm due to mupirocin.
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 Mupirocin calcium cream is administered to a nursing woman.
The safety and effectiveness of Mupirocin calcium cream have been established in the age-groups 3 months to 16 years. Use of Mupirocin calcium cream in these age-groups is supported by evidence from adequate and well‑controlled trials of Mupirocin calcium cream in adults with additional data from 93 pediatric subjects studied as part of the pivotal trials in adults [see Clinical Studies (14)].
In 2 adequate and well‑controlled trials, 30 subjects older than 65 years were treated with Mupirocin calcium cream. No overall difference in the efficacy or safety of Mupirocin calcium cream was observed in this patient population when compared with that observed in younger patients.
Mupirocin calcium cream, 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 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 is:
Figure 1. Structure of Mupirocin Calcium
Mupirocin calcium cream is a white cream that contains 2.15% w/w mupirocin calcium (equivalent to 2% 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.
Mupirocin is an RNA synthetase inhibitor antibacterial [see Microbiology (12.4)].
Absorption
Systemic absorption of mupirocin through intact human skin is minimal. The systemic absorption of mupirocin was studied following application of Mupirocin calcium 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 calcium 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.
Special Populations
Renal Impairment: The pharmacokinetics of mupirocin have not been studied in individuals with renal insufficiency.
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.
Mechanism of 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 Testing
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
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 genotoxicity: 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.
Reproduction studies were performed with mupirocin administered subcutaneously to male and female rats at doses up to 100 mg per kg per day which is 14 times the human topical dose (approximately 60 mg mupirocin per day) based on body surface area. Neither evidence of impaired fertility nor impaired reproductive performance attributable to mupirocin was observed.
The efficacy of topical Mupirocin calcium cream for the treatment of secondarily infected traumatic skin lesions (e.g., lacerations, sutured wounds, and abrasions not more than 10 cm in length or 100 cm2 in total area) was compared with that of oral cephalexin in 2 randomized, double‑blind, double‑dummy clinical trials. Clinical efficacy rates at follow‑up in the per-protocol populations (adults and pediatric subjects included) were 96.1% for Mupirocin calcium cream (n = 231) and 93.1% for oral cephalexin (n = 219). Pathogen eradication rates at follow‑up in the per-protocol populations were 100% for both Mupirocin calcium cream and oral cephalexin.
Pediatrics
There were 93 pediatric subjects aged 2 weeks to 16 years enrolled per protocol in the secondarily infected skin lesion trials, although only 3 were younger than 2 years of age in the population treated with Mupirocin calcium cream. Subjects were randomized to either 10 days of topical Mupirocin calcium cream 3 times daily or 10 days of oral cephalexin (250 mg 4 times daily for subjects greater than 40 kg or 25 mg per kg per day oral suspension in 4 divided doses for subjects less than or equal to 40 kg). Clinical efficacy at follow‑up (7 to 12 days post-therapy) in the per-protocol populations was 97.7% (43 of 44) for Mupirocin calcium cream and 93.9% (46 of 49) for cephalexin.
Mupirocin calcium cream, 2% is supplied in 15‑gram and 30‑gram tubes.
Mupirocin calcium cream is a white cream that contains 2.15% w/w mupirocin calcium (equivalent to 2% mupirocin free acid) in an oil- and water-based emulsion.
NDC 66993-942-15 (15-gram tube)
NDC 66993-942-31 (30-gram tube)
Store at or below 25°C (77°F). Do not freeze.
Advise the patient to read the FDA-approved patient labeling (Patient Information).
Advise the patient to administer Mupirocin calcium cream as follows:
Manufactured for:
Prasco Laboratories
Mason, OH 45040 USA
MUC-PS:5PI
PHARMACIST‑DETACH HERE AND GIVE INSTRUCTIONS TO PATIENT
Mupirocin calcium cream
What is Mupirocin calcium cream?
Mupirocin calcium cream is a prescription medicine used on the skin (topical use) to treat certain skin infections caused by bacteria called Staphylococcus aureus and Streptococcus pyogenes.
It is not known if Mupirocin calcium cream is safe and effective in children under 3 months of age.
Who should not use Mupirocin calcium cream?
Do not use Mupirocin calcium cream if:
What should I tell my healthcare provider before using Mupirocin calcium cream?
Before using Mupirocin calcium cream, tell your healthcare provider about your medical conditions including, if you:
Tell your healthcare provider about all of the medicines you take, including prescription and over-the-counter medicines, vitamins and herbal supplements. Do not mix Mupirocin calcium cream with other lotions, creams, or ointments.
How should I use Mupirocin calcium cream?
Mupirocin calcium cream may cause serious side effects, including:
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The most common side effects of Mupirocin calcium cream include:
These are not all the possible side effects of Mupirocin calcium cream. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
How should I store Mupirocin calcium cream?
General information about the safe and effective use of Mupirocin calcium cream.
Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use Mupirocin calcium cream for a condition for which it was not prescribed. Do not give Mupirocin calcium cream to other people, even if they have the same symptoms that you have. It may harm them. You can ask your pharmacist or healthcare provider for information about Mupirocin calcium cream that is written for health professionals.
What are the ingredients in Mupirocin calcium cream?
Active Ingredient: mupirocin calcium
Inactive Ingredients: benzyl alcohol, cetomacrogol 1000, cetyl alcohol, mineral oil, phenoxyethanol, purified water, stearyl alcohol, and xanthan gum.
Manufactured for:
Prasco Laboratories
Mason, OH 45040 USA
MUC-PS:1PIL
For more information, call 1-888-825-5249
MUPIROCIN CALCIUM
mupirocin calcium cream |
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Labeler - Prasco Laboratories (065969375) |
Registrant - GlaxoSmithKline LLC (167380711) |