Bactroban^® (Ointment) Instructions for Use

ATC Code

D06AX09 (Mupirocin)

Active Substance

Mupirocin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antibiotic for external use

Pharmacotherapeutic Group

Antibiotics and antimicrobial agents used in dermatology; antibiotics for topical use; other antibiotics for topical use

Pharmacological Action

Broad-spectrum antibiotic for external and topical use.

Mupirocin is a new antibiotic obtained by fermentation of Pseudomonas fluorescens. Mupirocin inhibits isoleucyl-transfer-RNA synthetase, blocking protein synthesis in the bacterial cell.

Due to its specific mechanism of action and unique chemical structure, Mupirocin is not characterized by cross-resistance with other antibiotics used in clinical practice.

When applied topically at minimum inhibitory concentrations (MIC), Mupirocin has bacteriostatic properties, and at higher concentrations, it has bactericidal properties.

Activity

Mupirocin is an antibacterial substance for topical use, demonstrating in vivo activity against Staphylococcus aureus (including methicillin-resistant strains), S. epidermidis, and β-hemolytic strains of Streptococcus species.

The in vitro activity spectrum includes the following bacteria.

Susceptible species Staphylococcus aureus^1,2; Staphylococcus epidermidis^1,2; coagulase-negative Staphylococci^1,2; Streptococcus species¹; Haemophilus influenzae; Neisseria gonorrhoeae; Neisseria meningitidis; Moraxella catarrhalis; Pasteurella multocida.

¹ – Clinical efficacy has been demonstrated for isolates of susceptible bacteria for the registered clinical indications for use.

² – Including β-lactamase-producing strains and methicillin-resistant strains.

Resistant species Corynebacterium species; Enterobacteriaceae; gram-negative non-fermenting rods; Micrococcus spp.; anaerobes.

Mupirocin susceptibility breakpoint concentrations (MIC) for Staphylococcus spp.

• Susceptible – ≤ 1 µg/ml;
• Intermediate susceptibility – from 2 to 256 µg/ml;
• Resistant – > 256 µg/ml.

Resistance mechanisms

Low-level resistance in staphylococci (MIC from 8 to 256 µg/ml) has been shown to be due to changes in the native isoleucyl-transfer-RNA synthetase enzyme. High-level resistance in staphylococci (MIC ≥ 512 µg/ml) has been shown to be due to a specific plasmid-encoded isoleucyl-transfer-RNA synthetase enzyme. The natural resistance of gram-negative bacteria, such as Enterobacteriaceae, may be due to the low level of antibiotic penetration into the bacterial cell.

Pharmacokinetics

Absorption

Mupirocin is poorly absorbed through intact human skin.

Metabolism

Mupirocin is intended for external use only. If absorbed through damaged skin, Mupirocin is rapidly metabolized to an inactive monic acid.

Excretion

Mupirocin is rapidly eliminated from the body by metabolic conversion to an inactive metabolite, monic acid, which is rapidly excreted by the kidneys.

Indications

• Treatment of primary skin infections: impetigo, folliculitis, furunculosis (including boils of the external auditory canal and auricle), ecthyma;
• Treatment of secondary skin infections: infected eczema, infected trauma (abrasions, insect bites), minor (not requiring hospitalization) wounds and burns;
• Prevention of bacterial infections in minor wounds, cuts, abrasions and other uncontaminated skin lesions.

ICD codes

Dosage Regimen

Ointment

For intranasal use.

Adults and children over 12 years

A cotton swab should be used as an applicator for applying the ointment.

A small amount of ointment, approximately the size of a match head (approximately 30 mg of ointment), should be applied to the nasal mucosa in each nostril 2 times/day for 5 days.

After applying the ointment, the nose should be firmly squeezed several times from both sides simultaneously to ensure even distribution of the ointment over the mucosa.

Hands should be washed before and after applying the drug.

Nasal carriage usually disappears on the 3rd-5th day of treatment. The drug should not be used for more than 5 days.

Children and adolescents over 12 years dose adjustment is not required.

Elderly patients dose adjustment is not required.

Patients with renal impairment dose adjustment is not required.

Patients with hepatic impairment dose adjustment is not required.

Adverse Reactions

The adverse reactions listed below are presented according to the affected organs and organ systems and frequency of occurrence. Frequency is defined as follows: very common (≥1/10), common (≥1/100 and <1/10), uncommon (≥1/1000 and < 1/100), rare (≥1/10,000 and < 1/1000), very rare (<1/10,000), including isolated cases.

The prevalence of common and uncommon adverse reactions was established based on pooled safety data from 12 clinical studies involving 1573 patients.

The prevalence of very rare adverse reactions was established primarily from post-marketing data and therefore represents the reporting frequency of such reactions rather than the true frequency of occurrence.

Immune system disorders very rare – systemic allergic reactions (including anaphylaxis, generalized rash, urticaria and angioedema).

Skin and subcutaneous tissue disorders common – burning at the application site; uncommon – itching, erythema, tingling, dryness at the application site. Skin allergic reactions to Mupirocin or the ointment base.

Contraindications

• Hypersensitivity to mupirocin or any other component of the drug in the history.

Use with caution in patients with moderate and severe renal failure, and in elderly patients.

Use in Pregnancy and Lactation

There are no data on the use of the drug during pregnancy and breastfeeding.

Animal studies have not revealed signs of reproductive toxicity.

However, as with the use of other drugs, the use of Bactroban^® during pregnancy and breastfeeding is possible only if the intended benefit to the mother outweighs any potential risk to the fetus.

Breastfeeding should be discontinued during the use of the drug for the prevention of bacterial infection of nipple fissures.

Use in Renal Impairment

Use with caution in patients with moderate and severe renal failure.

Pediatric Use

There are no restrictions on the use of the drug in children.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

Avoid getting the ointment into the eyes. If it gets into the eyes, rinse with plenty of water until the ointment residue is completely removed.

In rare cases, the use of the drug may cause a hypersensitivity reaction or severe local irritation. In such a case, treatment should be discontinued, the drug should be removed from the treated surface if possible, and alternative therapy for the infection should be prescribed.

As with other antibacterial drugs, prolonged use of mupirocin carries the risk of overgrowth of non-susceptible microorganisms.

Cases of pseudomembranous colitis have been described with the use of antibiotics, the severity of which can range from mild to life-threatening. Therefore, it is important to consider this diagnosis in patients who develop diarrhea during or after antibiotic use. Although the likelihood of this phenomenon with topical use of mupirocin is lower, if prolonged or severe diarrhea or abdominal cramps develop, treatment should be stopped immediately and the patient should be further examined.

The drug should not be used in ophthalmology, intranasally, in combination with the use of catheters, or at the site of central venous catheter insertion.

Polyethylene glycol (macrogol) can be absorbed through an open wound surface or other skin lesions and excreted by the kidneys. Like other macrogol-based ointments, Bactroban^® ointment should not be used in conditions where large amounts of macrogol may be absorbed, especially in moderate or severe renal failure.

Do not use the ointment remaining in the tube at the end of treatment for the next course of treatment.

There are no restrictions for elderly patients (in the absence of symptoms of moderate or severe renal failure).

Effect on ability to drive vehicles and mechanisms

Not studied.

Overdose

Symptoms Currently, there is limited data on mupirocin overdose.

Treatment There is no specific treatment for mupirocin overdose. In case of overdose, supportive therapy and appropriate monitoring of the patient’s condition are indicated if necessary.

Drug Interactions

The drug should not be mixed with other drugs to avoid dilution of the ointment and, consequently, a decrease in antibacterial activity or possible changes in the stability of mupirocin.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 2 years. Do not use after the expiration date printed on the package.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.