Mupirocin

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Cream, External, as calcium [strength expressed as base]:

Bactroban: 2% (15 g [DSC], 30 g [DSC])

Generic: 2% (15 g, 30 g)

Kit, External:

Centany AT: 2% [contains propylene glycol monostearate]

Ointment, External:

Bactroban: 2% (22 g [DSC])

Centany: 2% (30 g) [contains propylene glycol monostearate]

Generic: 2% (15 g, 22 g)

Ointment, Nasal, as calcium [strength expressed as base]:

Bactroban Nasal: 2% (1 g [DSC])

Pharmacology

Mechanism of Action

Binds to bacterial isoleucyl transfer-RNA synthetase resulting in the inhibition of protein synthesis

Pharmacokinetics/Pharmacodynamics

Absorption

Topical ointment and cream: Penetrates outer layers of skin; systemic absorption minimal through intact skin

Intranasal: Adults: ~3%; Neonates and premature infants: Absorption may be significant

Metabolism

Rapidly metabolized to monic acid (inactive)

Excretion

Urine (as monic acid [inactive])

Half-Life Elimination

17 to 36 minutes

Protein Binding

>97%

Use: Labeled Indications

Topical infection:

Intranasal: Eradication of nasal colonization with methicillin-resistant S. aureus (MRSA) in adult and pediatric patients ≥12 years of age and health care workers as part of a comprehensive infection control program to reduce the risk of infection among patients at high risk of MRSA infection during institutional outbreaks of infections with this microorganism

Limitations of use: Insufficient data for use as part of an intervention program to prevent autoinfection of high-risk patients from their own S. aureus nasal colonization or for general prophylaxis of any infection in any patient population.

Topical cream: Treatment of secondary infected traumatic skin lesions (up to 10 cm in length or 100 cm² in area) due to susceptible isolates of S. aureus and S. pyogenes

Topical ointment: Treatment of impetigo due to S. aureus and S. pyogenes

Use: Off Label

Surgical prophylaxis in methicillin-resistant S. aureus (MRSA) carriers (intranasal administration)a

Data from one prospective, controlled, multicenter, interventional cohort study and one randomized, double-blind, placebo-controlled, multicenter study support the use of mupirocin (twice daily in both nares for 5 days) along with other colonization reduction measures in MRSA carriers to reduce MRSA clinical cultures and infection rates Bode 2010, Lee 2013.

Contraindications

Hypersensitivity to mupirocin or any component of the formulation

Dosage and Administration

Dosing: Adult

Impetigo: Topical: Ointment: Apply to affected area 3 times daily; re-evaluate after 3 to 5 days if no clinical response

Secondary skin infections: Topical: Cream: Apply to affected area 3 times daily for 10 days; re-evaluate after 3 to 5 days if no clinical response

Elimination of MRSA colonization: Intranasal: Approximately one-half of the ointment from the single-use tube should be applied into one nostril and the other half into the other nostril twice daily (morning and evening) for 5 days

Surgical prophylaxis in methicillin-resistant S. aureus (MRSA) carriers (off-label use): Intranasal: Approximately one-half of the ointment from the single-use tube should be applied into one nostril and the other half into the other nostril twice daily for 5 days (Bode, 2010; Lee, 2013)

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

MRSA decolonization, nasal: Topical: Intranasal ointment:

Infants and Children: Limited data available: Apply a small amount twice daily for 5 to 10 days (IDSA [Liu 2011])

Children ≥12 years and Adolescents: Apply 500 mg (¹/₂ of unit-dose tube) twice daily for 5 to 10 days (IDSA [Liu 2011])

MRSA or impetigo, treatment; minor skin infection or a limited number of infected lesions: Infants, Children, and Adolescents: Topical: Cream, Ointment: Apply small amount 3 times daily for 5 to 10 days; patients not showing clinical response after 5 days should be reevaluated (IDSA [Liu 2011]; IDSA [Stevens 2014])

Administration

Intranasal ointment: After application into nostrils, press sides of nose together and gently massage to spread ointment throughout the insides of the nostrils for ~1 minute. Packaged in single-use tubes; discard after use; do not re-use. Not for use in eyes. In case of accidental contact in or near eyes, rinse well with water. Do not apply concurrently with any other intranasal products. Wash hands before and after application.

Topical cream, ointment: For external use only; not for use in eyes or on mucous membranes (components may be absorbed systemically and cause drying and irritation). Apply small amount to affected area using gauze pad or cotton swab; area may be covered with a gauze dressing if desired. In case of accidental contact in or near eyes, rinse well with water. Wash hands before and after application.

Storage

Intranasal: Store between 20°C and 25°C (68°F and 77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F). Do not refrigerate.

Topical cream: Store at or below 25°C (77°F). Do not freeze.

Topical ointment: Store between 20°C and 25°C (68°F and 77°F).

Drug Interactions

There are no known significant interactions.

Adverse Reactions

1% to 10%:

Central nervous system: Headache (2% to 9%), localized burning (<4%), stinging sensation (<2%)

Dermatologic: Pruritus (≤2%), skin rash (≤1%)

Gastrointestinal: Nausea (1% to 5%), dysgeusia (3%)

Local: Local pain (<2%)

Respiratory: Rhinitis (6%), respiratory congestion (5%), pharyngitis (4%), cough (2%)

<1%, postmarketing, and/or case reports: Abdominal pain, aphthous stomatitis, blepharitis, cellulitis, Clostridioides (formerly Clostridium) difficile-associated diarrhea, contact dermatitis, dermatitis, diarrhea, dizziness, epistaxis, erythema, hypersensitivity reaction, increased wound secretion, localized edema, localized tenderness, otalgia, urticaria, wound infection (secondary), xeroderma, xerostomia

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity: May be associated with systemic allergic reactions, including anaphylaxis, urticarial, angioedema, and generalized rash. If a systemic reaction occurs, discontinue use.
• Irritation: If sensitization or local irritation occurs, discontinue use.
• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.

Disease-related concerns:

• Renal impairment: Topical ointment and intranasal: Use with caution in patients with renal impairment (has not been studied).

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity ("gasping syndrome") in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer's labeling.
• Polyethylene glycol: Potentially toxic amounts of polyethylene glycol contained in some topical products may be absorbed percutaneously in patients with extensive burns or open wounds. Do not use polyethylene glycol-based ointments in conditions where absorption of large quantities of polyethylene glycol is possible, especially in the presence of moderate or severe renal impairment.

Other warnings/precautions:

• Appropriate use: For external use only. Avoid contact with eyes; in case of accidental contact in or near eyes, rinse well with water.

- Intranasal: May cause severe burning and tearing in eyes (resolves within days to weeks after discontinuation). Available in single-use tubes to decrease risk of contamination.

- Topical cream and ointment: Not for ophthalmic or nasal use or use on mucosal surfaces. May cover treated areas with gauze dressing.

• Limitations of use:

- Nasal ointment: There are insufficient data to establish that product 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; should not be used for general prophylaxis of any infection in any patient population; >90% of patients had eradication of nasal colonization within 2 to 4 days after therapy was completed; ~30% recolonization within 4 weeks of therapy was reported in one study.

- Topical ointment: Should not be used with intravenous (IV) cannulae or at central IV sites because of the potential to promote fungal infections and antimicrobial resistance.

Pregnancy

Pregnancy Considerations

Systemic absorption following topical application is minimal.

Patient Education

What is this drug used for?

• It is used to treat a bacteria found in nose passages and stop its spread to others.
• It is used to treat skin infections.

Frequently reported side effects of this drug

• Burning
• Stinging
• Headache
• Runny nose
• Sore throat
• Cough
• Stuffy nose
• Change in taste

Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:

• Clostridioides (formerly Clostridium) difficile-associated diarrhea like abdominal pain or cramps, severe diarrhea or watery stools, or bloody stools.
• Dizziness
• Fast heartbeat
• Abnormal heartbeat
• Application site irritation
• Severe itching
• Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.