Bactopic

Each gram of ointment contains: Mupirocin BP 20 mg (2% w/w).
Excipients/Inactive Ingredients: Polyethylene glycol 3350 & Polyethylene glycol 400.

Pharmacotherapeutic Group: Antibiotics and chemotherapeutics for dermatological use. ATC code: D06AX09.
Pharmacology: Pharmacodynamics: Mupirocin is a novel antibiotic produced through fermentation by Pseudomonas fluorescens. Mupirocin inhibits isoleucyl transfer-RNA synthetase, thereby arresting bacterial protein synthesis.
Mupirocin has bacteriostatic properties at minimum inhibitory concentrations and bactericidal properties at the higher concentrations reached when applied locally.
Mechanism of Resistance: Low-level resistance in staphylococci is thought to result from point mutations within the usual staphylococcal chromosomal gene (ileS) for the target isoleucyl tRNA synthetase enzyme. High-level resistance in staphylococci has been shown to be due to a distinct, plasmid encoded isoleucyl tRNA synthetase enzyme.
Intrinsic resistance in Gram negative organisms such as the Enterobacteriaceae could be due to poor penetration of the outer membrane of the Gram negative bacterial cell wall.
Due to its particular mode of action, and its unique chemical structure, mupirocin does not show any cross-resistance with other clinically available antibiotics.
Microbiological Susceptibility: The prevalence of acquired resistance may vary geographically and with time for selected species, and local information on resistance is desirable, particularly when treating severe infections. As necessary, expert advice should be sought when the local prevalence of resistance is such that the utility of the agent in at least some types of infection is questionable.
Commonly susceptible species: Staphylococcus aureus*, Streptococcus pyogenes*, Streptococcus spp. (β-haemolytic, other than S. pyogenes).
Species for which acquired resistance may be a problem: Staphylococcus spp., coagulase negative.
Inherently resistant organisms: Corynebacterium spp., Micrococcus spp.
* Activity has been satisfactorily demonstrated in clinical studies.
Pharmacokinetics: After topical application of Mupirocin (Bactopic) ointment, mupirocin is only very minimally absorbed systemically and that which is absorbed is rapidly metabolised to the antimicrobially inactive metabolite, monic acid. Penetration of mupirocin into the deeper epidermal and dermal layers of the skin is enhanced in traumatised skin and under occlusive dressings.
Elderly patients: No restrictions unless there is evidence of moderate or severe renal impairment (see Precautions).

Mupirocin (Bactopic) ointment is an RNA synthetase inhibitor antibacterial indicated for the topical treatment of impetigo due to susceptible isolates of Staphylococcus aureus and Streptococcus pyogenes.

Dosage: Adults (including elderly/hepatically impaired) and children: Two to three times a day for up to ten days, depending on the response.
Renally impaired: See Contraindications.
Mode of administration: Topical.
A small quantity of Mupirocin (Bactopic) ointment should be applied to cover the affected area.
The treated area may be covered by a dressing.
Any product remaining at the end of treatment should be discarded.
Do not mix with other preparations as there is a risk of dilution, resulting in a reduction of the antibacterial activity and potential loss of stability of the mupirocin in the ointment.
Not for intranasal, ophthalmic, or other mucosal use.

Signs and Symptoms: There is currently limited experience with overdosage of mupirocin.
Treatment: There is no specific treatment for an overdose of mupirocin. In the event of overdose, the patient should be treated supportively with appropriate monitoring as necessary. Further management should be as clinically indicated or as recommended by the national poisons centre, where available.

Hypersensitivity to the active substance or to any of the excipients.
Mupirocin (Bactopic) ointment formulation is not suitable for ophthalmic or intranasal use.

Should a possible sensitisation reaction or severe local irritation occur with the use of Mupirocin (Bactopic) Ointment, treatment should be discontinued, the product should be washed off and appropriate therapy instituted.
As with other antibacterial products, prolonged use may result in overgrowth of non-susceptible organisms.
Pseudomembranous colitis has been reported with the use of antibiotics and may range in severity from mild to life-threatening. Therefore, it is important to consider its diagnosis in patients who develop diarrhoea during or after antibiotic use. Although this is less likely to occur with topically applied mupirocin, if prolonged or significant diarrhea occurs or the patient experiences abdominal cramps, treatment should be discontinued immediately and the patient investigated further.
Renal impairment: Polyethylene glycol can be absorbed from open wounds and damaged skin and is excreted by the kidneys. In common with other polyethylene glycol based ointments, Mupirocin (Bactopic) ointment should not be used in conditions where absorption of large quantities of polyethylene glycol is possible, especially if there is evidence of moderate or severe renal impairment.
Mupirocin (Bactopic) ointment is not suitable for: Ophthalmic use, Intranasal use, Use in conjunction with cannulae and At the site of central venous cannulation.
Avoid contact with the eyes. If contaminated, the eyes should be thoroughly irrigated with water until the ointment residues have been removed.
Effects On Ability to Drive and Use Machines: No adverse effects on the ability to drive or operate machinery have been identified.

Pregnancy: Risk Summary: There are insufficient human data to establish whether there is a drug-associated risk with Mupirocin ointment in pregnant women. Systemic absorption of mupirocin through intact human skin is minimal following topical administration of mupirocin ointment. No developmental toxicity was observed in rats or rabbits treated with mupirocin subcutaneously during organogenesis at doses of 160 or 40 mg per kg per day, respectively (22 and 11 times the human topical dose based on calculations of dose divided by the entire body surface area).
The estimated background risk of major birth defects and miscarriages for the indicated population is unknown.
Data: Animal Data: Developmental toxicity studies have been performed with Mupirocin administered subcutaneously to rats and rabbits at doses up to 160 mg per kg per day during organogenesis. This dose is 22 and 43 times, respectively, the human topical dose (approximately 60 mg Mupirocin per day) based on calculations of dose divided by the entire body surface area.
Maternal toxicity was observed (body weight loss/decreased body weight gain and reduced feeding) in both species with no evidence of developmental toxicity in rats. In rabbits, excessive maternal toxicity at the high dose precluded the evaluation of fetal outcomes. There was no developmental toxicity in rabbits at 40 mg per kg per day, 11 times the human topical dose based on calculations of dose divided by the entire body surface area.
Mupirocin administered subcutaneously to rats in a pre- and postnatal development study (dosed during late gestation through lactation) was associated with reduced offspring viability in the early postnatal period at a dose of 106.7 mg per kg, in the presence of injection site irritation and/or subcutaneous hemorrhaging. This dose is 14 times the human topical dose based on calculations of dose divided by the entire body surface area. The no-observed adverse effect level in this study was 44.2 mg per kg per day, which is 6 times the human topical dose.
Lactation: Risk Summary: It is not known whether mupirocin is present in human milk, has effects on the breastfed child, or has effects on milk production. However, breastfeeding is not expected to result in exposure of the child to the drug due to the minimal systemic absorption of mupirocin in humans following topical administration of Mupirocin ointment. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for Mupirocin ointment and any potential adverse effects on the breastfed child from Mupirocin ointment or from the underlying maternal condition.
Clinical Considerations: To minimize oral exposure of the drug to children, a breast and/or nipple being treated with Mupirocin ointment should be thoroughly washed prior to breastfeeding.
Fertility: There are no data on the effects of mupirocin on human fertility. Studies in rats showed no effects on fertility.

Adverse reactions are listed as follows by system organ class and frequency. Frequencies are defined as: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10,000, <1/1000), very rare (<1/10,000), including isolated reports.
Immune system disorders: Very rare: Systemic allergic reactions including anaphylaxis, generalised rash, urticaria and angioedema have been reported with mupirocin Ointment.
Skin and subcutaneous tissue disorders: Common: Burning localised to the area of application.
Uncommon: Itching, erythema, stinging and dryness localised to the area of application.
Cutaneous sensitisation reactions to Mupirocin or the ointment base.

No drug interactions have been identified.

Store at temperatures not exceeding 30°C.

Topical Antibiotics

D06AX09 - mupirocin ; Belongs to the class of other topical antibiotics used in the treatment of dermatological diseases.

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