CLASSES
Topical Antibacterial Agents, Other
Topical Nasal Anti-infectives
DESCRIPTION
Unique topical antibiotic produced from Pseudomonas fluorescens; active against gram positive organisms like S. aureus and Strept. pyogenes; used for skin infections like impetigo; also in an intranasal ointment to eradicate nasal colonization of MRSA.
COMMON BRAND NAMES
Bactroban, Centany, Centany AT
HOW SUPPLIED
Bactroban/Centany/Centany AT/Mupirocin Topical Ointment: 2%
Bactroban/Mupirocin/Mupirocin Calcium Topical Cream: 2%
DOSAGE & INDICATIONS
For the treatment of impetigo and other skin and skin structure infections due to susceptible strains of Staphylococcus aureus or Streptococcus pyogenes.
For the treatment of impetigo.
Topical dosage (ointment)
Adults, Children, and Infants 2 months and older
Apply a small amount to the affected area(s) 3 times daily. The area(s) may be covered with a sterile gauze dressing. Therapy is usually continued for 1 to 2 weeks. If a response is not evident within 3 to 5 days, the infection should be reevaluated. Studies evaluating use of mupirocin for the treatment of impetigo have found the ointment produces similar cure rates to oral erythromycin.
For the treatment of secondarily infected traumatic skin lesions (up to 10 cm in length or 100 cm2 in area).
Topical dosage (cream)
Adults, Children, and Infants 3 months and older
Apply a small amount to the affected area(s) 3 times daily for 10 days. If a response is not evident within 3 to 5 days, the infection should be reevaluated.
For methicillin-resistant S. aureus nasal carriage eradication to reduce the risk of infection among high-risk patients during institutional outbreaks.
Intranasal dosage
Adults
Apply a small amount (500 mg) into each nare 2 times daily for 5 to 10 days.
Children and Adolescents 12 to 17 years
Apply a small amount (500 mg) into each nare 2 times daily for 5 to 10 days.
Infants† and Children 1 to 11 years†
Apply a small amount (500 mg) into each nare 2 times daily for 5 to 10 days.
For the treatment of mild methicillin-resistant Staphylococcus aureus (MRSA)-associated infectious neonatal pustulosis†.
Topical dosage (ointment)
Neonates and Infants younger than 3 months
Apply a small amount to the affected area(s) 3 times daily. Clinical practice guidelines support the use of mupirocin for mild cases with localized disease.
For the treatment of infected eczema† due to susceptible strains of Staphylococcus sp. or Streptococcus sp..
Topical dosage (ointment)
Adults, Adolescents, Children, and Infants
Apply a small amount to the affected area(s) 2 to 3 times daily for 1 to 2 weeks. Topical mupirocin ointment has similar or superior efficacy when compared with systemic antibiotics (i.e., erythromycin, ampicillin, flucloxacillin) for secondary skin infections, including infected eczema.
For the treatment of folliculitis† due to susceptible strains of Staphylococcus sp. or Streptococcus sp..
Topical dosage (ointment)
Adults, Adolescents, and Children
Apply a small amount to the affected area(s) 3 times daily for 5 to 14 days. Topical mupirocin ointment has similar or superior efficacy when compared with systemic antibiotics (i.e., ampicillin, cloxacillin, erythromycin) for primary skin infections, including folliculitis.
For the prevention of postoperative nosocomial Staphylococcus aureus infections† (i.e., bacterial infection prophylaxis†).
Intranasal dosage
Adults
Apply a small amount to each nare topically twice daily for up to 5 days pre-operatively. Use in combination with chlorhexidine baths once daily.
†Indicates off-label use
MAXIMUM DOSAGE
Adults
Intranasal, 5 days of twice daily therapy; Topical, maximum dosage information is not available.
Geriatric
Intranasal, 5 days of twice daily therapy; Topical, maximum dosage information is not available.
Adolescents
Intranasal, 5 days of twice daily therapy; Topical, maximum dosage information is not available.
Children
12 years: Intranasal, 5 days of twice daily therapy; Topical, maximum dosage information is not available.
1 to 11 years: Maximum dosage information is not available for topical ointment or cream. Safety and efficacy not established for intranasal ointment; however, intranasal ointment has been used off-label.
Infants
3 months and older: Maximum dosage information is not available for topical ointment or cream. Safety and efficacy not established for intranasal ointment; however, intranasal ointment has been used off-label.
2 months: Maximum dosage information is not available for topical ointment. Safety and efficacy not established for topical cream or intranasal ointment; however, intranasal ointment has been used off label.
younger than 2 months: Safety and efficacy not established; however, topical and intranasal ointment have been used off-label.
Neonates
Safety and efficacy not established; however, topical ointment has been used off-label.
DOSING CONSIDERATIONS
Hepatic Impairment
No dosage adjustment needed.
Renal Impairment
No dosage adjustment needed.
ADMINISTRATION
Topical Administration
Cream/Ointment/Lotion Formulations
Apply to affected area. Treated area may be covered with sterile gauze dressing if desired.
Avoid contact with the eyes and mucosal surfaces.
Topical cream and ointment products are not FDA-approved for nasal use.
Other Administration Route(s)
Nasal Administration
Apply ointment inside the nose.
After application, close the nostrils by pressing together and releasing the sides of the nose repetitively for approximately 1 minute. This will spread the ointment throughout the nares.
Avoid contact with the eyes.
Do not apply concurrently with any other intranasal product.
STORAGE
Bactroban:
- Store at controlled room temperature (between 68 and 77 degrees F)
Centany:
- Store at controlled room temperature (between 68 and 77 degrees F)
Centany AT :
- Store at controlled room temperature (between 68 and 77 degrees F)
CONTRAINDICATIONS / PRECAUTIONS
General Information
Prolonged use of mupirocin is not recommended because of possible overgrowth of resistant organisms including fungi. This overgrowth can cause superinfection.
Burns, renal impairment
Normal undamaged epithelial surfaces inhibit the absorption of polyethylene glycol, the vehicle for mupirocin skin ointment. Damaged epithelial surfaces allow absorption of polyethylene glycol. Mupirocin skin ointment should not be used on burns (especially extensive burns), open wounds, or other damaged skin. Increased absorption of polyethylene glycol should be avoided, especially if there is evidence of moderate to severe renal impairment.
Children, infants, neonates
The intranasal form of mupirocin is not for use in neonates, infants, or children < 12 years old. Safe use and pharmacokinetic properties have not been studied in these groups. The safety and efficacy of mupirocin topical cream have not been established in pediatric patients less than 3 months and the safety and efficacy of the topical ointment have not been established in pediatric patients less than 2 months of age.
Ocular exposure, ophthalmic administration
Mupirocin is not for ophthalmic administration. Avoid ocular exposure of mupirocin as ocular contact produces severe burning and tearing.
Pregnancy
There are insufficient human data to establish a drug-associated risk with mupirocin use during pregnancy. Systemic absorption of mupirocin through intact skin is minimal after topical administration of mupirocin. No developmental toxicity was observed in rats or rabbits given mupirocin subcutaneously at doses 11 and 22 times the human topical dose based on calculations of dose divided by the entire body surface area.
Breast-feeding
It is not known whether mupirocin is present in human breast milk, has effects on the breast-fed child, or has effects on milk production. However, breast-feeding is not expected to result in exposure of the child to mupirocin due to the minimal systemic absorption of mupirocin after topical administration. Consider the benefits of breast-feeding along with the mother's clinical need for mupirocin and any potential adverse effects on the breast-fed child from mupirocin or the underlying maternal condition. To minimize oral exposure of the drug to the breast-feeding child, thoroughly wash a breast and/or nipple being treated with mupirocin prior to breast-feeding.
C. difficile-associated diarrhea, diarrhea, pseudomembranous colitis
Consider pseudomembranous colitis in patients presenting with diarrhea after antibacterial use. Careful medical history is necessary as pseudomembranous colitis has been reported to occur over 2 months after the administration of antibacterial agents. Almost all antibacterial agents, including mupirocin, have been associated with pseudomembranous colitis or C. difficile-associated diarrhea (CDAD) which may range in severity from mild to life-threatening. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.
ADVERSE REACTIONS
Severe
angioedema / Rapid / Incidence not known
anaphylactoid reactions / Rapid / Incidence not known
C. difficile-associated diarrhea / Delayed / Incidence not known
Moderate
erythema / Early / 0-1.0
contact dermatitis / Delayed / 0-1.0
stomatitis / Delayed / 0-1.0
blepharitis / Early / 0-1.0
superinfection / Delayed / Incidence not known
pseudomembranous colitis / Delayed / Incidence not known
Mild
rash / Early / 1.0-10.0
headache / Early / 1.7-9.0
rhinitis / Early / 6.0-6.0
nausea / Early / 0-4.9
pharyngitis / Delayed / 4.0-4.0
skin irritation / Early / 0-3.6
dysgeusia / Early / 3.0-3.0
nasal irritation / Early / 2.0-2.0
cough / Delayed / 2.0-2.0
xerosis / Delayed / 0-1.0
epistaxis / Delayed / 0-1.0
xerostomia / Early / 0-1.0
otalgia / Early / 0-1.0
diarrhea / Early / 0-1.0
pruritus / Rapid / Incidence not known
urticaria / Rapid / Incidence not known
abdominal pain / Early / Incidence not known
dizziness / Early / Incidence not known
infection / Delayed / Incidence not known
DRUG INTERACTIONS
There are no drug interactions associated with Mupirocin products.
PREGNANCY AND LACTATION
Pregnancy
There are insufficient human data to establish a drug-associated risk with mupirocin use during pregnancy. Systemic absorption of mupirocin through intact skin is minimal after topical administration of mupirocin. No developmental toxicity was observed in rats or rabbits given mupirocin subcutaneously at doses 11 and 22 times the human topical dose based on calculations of dose divided by the entire body surface area.
It is not known whether mupirocin is present in human breast milk, has effects on the breast-fed child, or has effects on milk production. However, breast-feeding is not expected to result in exposure of the child to mupirocin due to the minimal systemic absorption of mupirocin after topical administration. Consider the benefits of breast-feeding along with the mother's clinical need for mupirocin and any potential adverse effects on the breast-fed child from mupirocin or the underlying maternal condition. To minimize oral exposure of the drug to the breast-feeding child, thoroughly wash a breast and/or nipple being treated with mupirocin prior to breast-feeding.
MECHANISM OF ACTION
Mupirocin is bacteriostatic at low concentrations and bactericidal at high concentrations. Bacterial protein and RNA synthesis are inhibited when mupirocin reversibly binds to bacterial isoleucyl-tRNA synthetase. This enzyme normally promotes the conversion of isoleucine and tRNA to isoleucyl-tRNA. The epoxide side chain of mupirocin is similar to isoleucine and competes with it for binding sites on the synthetase enzyme. The cellular concentration of isoleucyl-tRNA becomes depleted, subsequently inhibiting bacterial protein and RNA synthesis. Unlike many other antibiotics, mupirocin has little effect on bacterial DNA synthesis and cell wall peptidoglycan formation.
PHARMACOKINETICS
Mupirocin is administered topically to the skin or the nares. Once in systemic circulation, it is rapidly metabolized to inactive monic acid and is excreted via the kidneys. The elimination half-life is 20—40 minutes for mupirocin and 30—80 minutes for monic acid.
Topical Route
Percutaneous absorption through intact skin is minimal in both pediatric and adult patients. Following topical administration, > 97% of the drug is bound to protein. Polyethylene glycol (PEG), the vehicle used for the ointment, can be absorbed from open or damaged skin and may cause renal failure.
Other Route(s)
Intranasal Route
In adults, systemic absorption of intranasally applied mupirocin ointment is minimal. One study suggested 3.3% (range: 1.2—5.1%) of an applied dose may be absorbed from the nasal mucosa of adults. Pharmacokinetic studies have not been conducted in pediatric patients < 12 years of age.