Supirocin, ointment 15 g

Mechanism of action

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

Mupirocin has no cross-resistance with other antibiotics used in clinical practice due to its specific mechanism of action and unique chemical structure.

Mupirocin has bacteriostatic properties at minimal suppressive concentrations (MPC) when applied topically and bactericidal properties at higher concentrations.

Pharmacodynamic Effects

Activity

Mupirocin is a topical antibacterial agent that demonstrates in vivo activity against Staphylococcus aureus (including methicillin-resistant strains), S. epidermidis and beta-haemolytic strains of Streptococcus species.

The spectrum of in vitro activity includes the following bacteria:

Sensitive species:

– Staphylococcus aureus1,2;

– Staphylococcus epidermidis1,2;

– Coagulazonegative staphylococci1,2;

– Streptococcus species1;

– Haemophilus influenzae;

– Neisseria gonorrhoeae;

– Neisseria meningitidis;

– Moraxella catarrhalis;

– Pasteurella multocida.

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

2 Including beta-lactamase-producing strains and methicillin-resistant strains.

Resistant species

– Corynebacterium species;

– Enterobacteriaceae;

– Gram-negative non-fermenting bacilli;

– Micrococcus species;

– Anaerobes.

Sensitivity limit concentrations to mupirocin (MPC) for Staphylococcus spp.

Sensitive: less than or equal to 1 µg/mL.

Intermediate sensitivity: 2 to 256 µg/mL.

Resistant: above 256 µg/mL.

Betamethasone is a glucocorticosteroid for external use.

It has local anti-inflammatory, anti-allergic, anti-edema and antiproliferative effects. It has stronger vasoconstrictor action than other fluorine derivatives of glucocorticosteroids; the systemic effects are expressed insignificantly due to limited absorption through the skin. When exposed to the skin, there is prevention of marginal accumulation of neutrophils, which leads to decrease of exudation, cytokines production, inhibition of macrophages migration, resulting in final reduction of infiltration and granulation processes.

Mupirocin is poorly absorbed through intact human skin.

If absorbed through damaged skin, mupirocin is rapidly metabolized to inactive monic acid.

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

Betamethasone dipropionate is a lipophilic substance and is easily absorbed through the stratum corneum without biotransformation. Absorption is increased when applied to the skin in body folds, on skin with damaged epidermis or on the area of inflammation, when using the drug frequently or after application over a large area of skin. Absorption of betamethasone dipropionate through the skin in children is faster than in adults.

Indications

Treatment of primary and secondary skin infections caused by mupirocin-sensitive microorganisms including:

Prevention of bacterial infections in minor wounds cuts abrasions and other uncontaminated skin injuries.

Active ingredient

Composition

100 g of ointment for topical and external use contains:

acting ingredients:

mupirocin – 2.0g.

Excipients:

MacroGol 400 (polyethylene glycol 400),

MacroGol 4000 (polyethylene glycol 4000).

How to take, the dosage

Applied to the affected skin surface 2-3 times a day with a cotton or gauze tampon.
Thereafter a simple gauze or occlusive bandage may be applied to the application area.
Frequency of application and duration of treatment depend on the dynamics of the clinical picture.
The drug should not be used for more than 10 days.
In case of no effect after 5 days of treatment it is recommended to reconsider further treatment tactics taking into account the dynamics of clinical parameters.
Hands should be washed before and after application of the drug.

Special Instructions

To avoid getting the ointment in the eyes. In case of contact with the eyes – rinse with plenty of water until complete removal of residual ointment.
In rare cases, when using the drug, a reaction of hypersensitivity or severe local irritation may occur. In such cases, it is necessary to discontinue treatment, if possible remove the drug from the treated surface and prescribe an alternative therapy for the infection.
As with other antibacterial drugs, there is a risk of excessive growth of insensitive microorganisms with long-term use of mupirocin.
In cases of pseudomembranous colitis, the severity of which can vary from mild to life-threatening, have been described with the use of antibiotics. Thus, it is important to consider the possibility of this diagnosis in patients who develop diarrhea on or after the use of antibiotics. Although there is less chance of this occurring with topical administration of mupirocin, if prolonged or severe diarrhea or abdominal cramps develop, treatment should be stopped immediately and the patient should be further evaluated.
The drug should not be used in ophthalmology, intranasally, combined with catheter use, or at the site of central venous catheter insertion.
Polyethylene glycol (macrogoal) may be absorbed through open wound surfaces or other skin injuries and excreted by the kidneys.
Compared with other macrogoal-based ointments, Supirocin Ointment should not be used in conditions where large amounts of macrogoal may be absorbed.
Do not mix the ointment with other medicines to avoid dilution of the ointment and consequently a decrease in antibacterial activity or a possible change in stability of mupirocin.
The ointment remaining in the tube at the end of treatment may not be used for the next course of treatment
Special patient groups
Patients of advanced age
No restrictions (if there are no symptoms of moderate or severe renal failure).
Impact on the ability to drive vehicles and other mechanisms:
Have not been studied.

Contraindications

Side effects

The undesirable reactions presented below are listed according to organ and system involvement and frequency of occurrence.

The frequency of occurrence is defined as follows: very common (>1/10) common (>1/100 < 1/10) infrequent (>1/1000 < 1/100) rare (>1/10000 < 1/1000) very rare (< 1/10000) including individual cases.

Infrequent adverse reactions

Immune system disorders

Very rare: systemic allergic reactions (including anaphylaxis generalized rash urticaria and angioedema).

Dermal and subcutaneous tissue disorders

Often: burning at the site of application.

Infrequent: itching erythema tingling dryness at the application site. Skin allergic reactions to mupirocin or the base of the ointment.

Overdose

Symptoms

There are currently limited data on mupirocin overdose.

Treatment

There is no specific treatment for mupirocin overdose. In cases of overdose, supportive therapy and appropriate patient monitoring is indicated if necessary.

Pregnancy use

Similarities