Professional Information
Mupirocin (Nasal)
VA CLASSIFICATION
Primary: NT900
Commonly used brand name(s): Bactroban Nasal.
Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).
Category:
Antibacterial (nasal)—
Indications
Accepted
Staphylococcus aureus, methicillin-resistant (treatment)—Intranasal mupirocin calcium is indicated for the eradication of nasal colonization with methicillin-resistant S. aureus in adult patients and health care workers as part of a comprehensive infection control program to reduce the risk of infection among patients at high risk of methicillin-resistant S. aureus infection during institutional outbreaks of infections with this pathogen {01}.
—In clinical trials, more than 90% of persons treated with intranasal mupirocin had eradication of nasal colonization 2 to 4 days after completion of therapy, as compared with 5 to 30% of persons administered the vehicle only. In one study, recolonization in approximately 30% of patients was reported within 4 weeks after completion of therapy as compared with 85 to 100% cases of recolonization with administration of the vehicle only. {01}
Acceptance not established
There are insufficient data to establish that intranasal mupirocin calcium is safe and effective as part of an intervention program to prevent autoinfection of high-risk patients from their own nasal colonization with S. aureus {01}.
There are insufficient data to recommend use of intranasal mupirocin calcium for general prophylaxis of any infection in any patient population {01}.
Unaccepted
The safety and efficacy of using intranasal mupirocin calcium for more than 5 days have not been established. There are no human clinical or animal data to support the use of this product for more than 5 days or in ways not described in this monograph {01}.
Pharmacology/Pharmacokinetics
Physicochemical characteristics:
Source—
Produced by fermentation of Pseudomonas fluorescens {01}.
Molecular weight—
Mupirocin calcium: 1075.36 {02}
Mupirocin free acid: 500.6 {01}
Mechanism of action/Effect:
Mupirocin inhibits bacterial protein synthesis by reversibly and specifically binding to bacterial isoleucyl transfer-RNA synthetase. Because of this process, mupirocin does not demonstrate in vitro cross-resistance with other classes of antimicrobial agents {01}.
The type of mupirocin resistance that may occur appears to result from the production of a modified isoleucyl transfer-RNA synthetase. High-level plasmid-mediated resistance (minimum inhibitory concentration [MIC] > 1024 mcg per mL) has been reported in some strains of Staphylococcus aureus and coagulase-negative staphylococci {01}.
Mupirocin is bactericidal at concentrations achieved by topical intranasal administration. However, the minimum bactericidal concentration (MBC) against relevant intranasal pathogens is generally eightfold to thirtyfold higher than the MIC. In addition, mupirocin is highly protein-bound, and the effect of nasal secretions on the MIC of intranasal mupirocin has not been determined {01}.
Mupirocin has been shown to be active against most strains of methicillin-resistant S. aureus , both in vitro and in clinical studies of the eradication of nasal colonization {01}.
Absorption:
Repeated intranasal applications of 0.2 gram of mupirocin calcium ointment three times a day for 3 days to five adult males resulted in no evidence of systemic absorption of mupirocin. For up to 72 hours after the nasal applications, concentrations of mupirocin in urine and of monic acid in urine and serum were below the limits of determination of the assay. The lower detectable limits of the assay were 50 nanograms per mL of mupirocin in urine, 75 nanograms per mL of monic acid in urine, and 10 nanograms per mL of monic acid in serum. Extrapolation of the detectable limit of the urine assay for monic acid yields a mean of 3.3% (range, 1.2 to 5.1%) of the applied dose that could possibly be absorbed systemically from the nasal mucosa of adults {01}.
Protein binding:
Very high (> 97%) {01}.
Biotransformation:
Mupirocin is rapidly metabolized following intravenous or oral administration {01}. The principal metabolite is monic acid, which has no antibacterial activity {01}.
Half-life:
A study of seven men who were administered intravenous mupirocin reported an elimination half-life of 20 to 40 minutes for mupirocin and 30 to 80 minutes for monic acid {01}.
Elimination:
Predominately renal as monic acid after intravenous administration of mupirocin {01}.
Precautions to Consider
Carcinogenicity
Long-term animal studies have not been done {01}.
Mutagenicity
The following in vitro or in vivo tests, using either mupirocin calcium or mupirocin sodium, did not show any mutagenic potential: 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 {01}.
Pregnancy/Reproduction
Fertility—
No evidence of impaired fertility was found in reproductive studies in rats administered mupirocin sodium subcutaneously at doses that were comparable (on a mg-per-square-meter [mg/m 2] basis) to up to 40 times the human intranasal dose of approximately 20 mg of mupirocin per day {01}.
Pregnancy—
Adequate and well-controlled studies in humans have not been done {01}.
No evidence of harm to the fetus was found in reproductive studies in rats and rabbits administered mupirocin (salt not disclosed) subcutaneously at doses that were comparable (on a mg-per-square-meter [mg/m 2] basis) to up to 65 and 130 times, respectively, the human intranasal dose of approximately 20 mg of mupirocin per day {01}.
FDA Pregnancy Category B {01}.
Breast-feeding
It is not known whether mupirocin is distributed into breast milk {01}. However, problems in humans have not been documented.
Pediatrics
Safety and efficacy have not been established {01}. Appropriate studies on the relationship of age to the effects of mupirocin have not been performed in children up to 12 years of age. However, a report of a pharmacokinetic study in neonates and premature infants indicated that significant systemic absorption occurred following administration of intranasal mupirocin {01}.
Geriatrics
Appropriate studies on the relationship of age to the effects of mupirocin have not been performed in the geriatric population. However, no geriatrics-specific problems have been documented to date.
Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):
Note: Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.
» Intranasal products, other (concurrent use of mupirocin with other intranasal products has not been studied and is not recommended until studies are done {01})
Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).
Except under special circumstances, this medication should not be used when the following medical problem exists:
» Sensitivity to mupirocin{01}
Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:
Those indicating need for medical attention
Incidence less frequent
Cough{01}
respiratory disorder, including upper respiratory tract congestion{01} (chest congestion)
Incidence rare
Ear pain{01}
Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
Headache{01}
Incidence less frequent or rare
Burning or stinging in the nose{01}
pharyngitis{01} (sore throat)
pruritus{01} (itching)
rhinitis{01} (stuffy or runny nose)
taste perversion{01} (change in taste)
Overdose
There was no evidence of systemic absorption following repeated intranasal applications of mupirocin calcium in adults {01}. (See Absorption .) In addition, intravenous infusions of 252 mg of mupirocin and single oral doses of 500 mg of mupirocin have been well tolerated in adults {01}.
Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Mupirocin (Nasal) .
In providing consultation, consider emphasizing the following selected information (» = major clinical significance):
Before using this medication
» Conditions affecting use, especially:
Sensitivity to mupirocin
Use in children—Safety and efficacy have not been established in children up to 12 years of age; in addition, a report of a pharmacokinetic study in neonates and premature infants indicated that significant systemic absorption occurred following administration of intranasal mupirocin
Other medications, especially other intranasal products
Proper use of this medication
» Proper administration: First washing hands; applying approximately one half of the ointment from single-use tube directly from tube into nostril; applying the remainder of ointment directly into other nostril; closing nostrils by pressing sides of nose together and then releasing them repeatedly for approximately 1 minute to help spread medication throughout inside of nostrils; another method is pressing sides of nose together and gently massaging nose; being careful not to touch eyes; discarding tube after using; washing hands afterwards to remove any medication that may be on them
» Proper dosing
Missed dose: Using as soon as possible; not using if almost time for next dose; not doubling doses
» Proper storage
Precautions while using this medication
» Keeping medication away from eyes; medication may cause severe burning and tearing of eyes that may last days or weeks; contacting physician if this occurs
» Not using any other medication in your nose without checking with physician
» Discontinuing medication and checking with physician if severe nasal irritation occurs
Side/adverse effects
Signs of potential side effects, especially cough; respiratory disorder, including upper respiratory tract congestion; and ear pain
General Dosing Information
The single-use tube should not be reused, but should be discarded immediately after use {01}.
If sensitization or a severe local irritation develops, treatment with mupirocin should be discontinued {01}.
Patients should be cautioned to keep mupirocin away from the eyes. Under test conditions, application of mupirocin nasal ointment to the eye caused severe symptoms, such as burning and tearing, that resolved over days to weeks {01}.
Nasal Dosage Forms
MUPIROCIN CALCIUM NASAL OINTMENT
Usual adult and adolescent dose
Antibacterial, nasal
Intranasal, approximately one half of the ointment from a single-use tube applied into each nostril two times a day (morning and evening) for five days. {01}
Usual adult and adolescent prescribing limits
Five days of twice-daily treatment {01}.
Usual pediatric dose
Antibacterial, nasal
Children up to 12 years of age: Safety has not been established {01}.
Children 12 years of age and older: See Usual adult and adolescent dose .
Usual geriatric dose
Antibacterial, nasal
See Usual adult and adolescent dose .
Strength(s) usually available
U.S.—
2% (Rx) [Bactroban Nasal{01} (2.15% w/w mupirocin calcium equivalent to 2% mupirocin free acid) (paraffin) (glycerin esters mixture [Softisan 649])]
Packaging and storage:
Store at or below 25 ºC (77 ºF) {01}. Protect from freezing.
Auxiliary labeling:
• For the nose.
• Keep away from eyes {01}.
Developed: 11/04/1997
References
- Bactroban package insert (SmithKline Beecham—US), Issued 9/95, Rec 5/96.
- Canada JR, editor. USAN 1998. USP dictionary of USAN and international drug names. Rockville, MD: The United States Pharmacopeial Convention, Inc; 1997. p. 490.
- Product Information: Bactroban ®Nasal, mupirocin calcium ointment. SmithKline Beecham, Philadelphia, PA (PI revised 3/1998) PI reviewed 5/2001
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