Composition, form of production and packaging
Ointment nasal white or almost white.
1 g
mupirocin calcium 21.5 mg,
which corresponds to the content of mupirocin 20 mg
Excipients: paraffin white soft - 929.6 mg, softzan 649 - 48.9 mg.
3 g - aluminum tubes (1) with a plastic tip and a screw cap made of polyethylene - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
PHARMACHOLOGIC EFFECT
Antibiotic of a wide spectrum of action for external and local application.
Mupirocin is a new antibiotic that is obtained by fermentation of Pseudomonas fluorescens. Mupirocin inhibits isoleucyl transfer-RNA synthetase by blocking protein synthesis in a bacterial cell.
Due to the specific mechanism of action and the unique chemical structure, mupirocin is not characterized by cross-resistance with other antibiotics used in clinical practice.
With topical application in minimal suppressive concentrations (MIC), mupirocin has bacteriostatic, and in higher concentrations - bactericidal properties.
Activity
Mupirocin is an antibiotic for topical use demonstrating in vivo activity against Staphylococcus aureus (including methicillin-resistant strains), S. epidermidis and? -hemolytic strains of Streptococcus species.
The in vitro activity spectrum includes the following bacteria:
Sensitive species: Staphylococcus aureus 1,2 ; Staphylococcus epidermidis 1,2 ; coagulase-negative Staphylococci 1,2 ; Streptococcus species 1 ; Haemophilus influenzae; Neisseria gonorrhoeae; Neisseria meningitidis; Moraxella catarrhalis; Pasteurella multocida.
1 - Clinical efficacy was demonstrated for isolates of sensitive bacteria according to registered clinical indications for use.
2 - Including strains producing? -lactamase, and methicillin-resistant strains.
Stable species: Corynebacterium species; Enterobacteriaceae; gram-negative non-fermenting sticks; Micrococcus spp .; anaerobes.
Boundary sensitivity concentrations for mupirocin (IPC) for Staphylococcus spp.
- sensitive -? 1 Ојg / ml;
- intermediate sensitivity - from 2 to 256 mcg / ml;
- stable -> 256 Ојg / ml.
Mechanisms of resistance
It was shown that a low level of resistance of staphylococci (MIC from 8 to 256 μg / ml) is due to changes in the native enzyme isoleucyl transfer-RNA synthetase. It was shown that a high level of resistance of staphylococci (MIC of ≤ 512 μg / ml) is due to a certain plasmid encoding of the enzyme isoleucyl transfer-RNA synthetase. The natural resistance of gram-negative bacteria, such as Enterobacteriaceae, may be due to the low penetration of the antibiotic into the bacterial cell.
PHARMACOKINETICS
Suction
Absorption of mupirocin through the damaged and healthy mucous membrane of the nose is insignificant (less than 1% of the applied dose is excreted in urine in the form of monic acid).
Metabolism
The drug is intended for topical use only. In case of absorption through the damaged skin, mupirocin is rapidly metabolized to inactive monic acid.
Excretion
Mupirocin is rapidly excreted from the body by metabolic transformation into an inactive metabolite, monium acid, which is rapidly excreted by the kidneys.
INDICATIONS
- carriage of staphylococcal infection in the nasal cavity, including carriage of Staphylococcus aureus (including methicillin-resistant strains);
- Prevention of infection of Staphylococcus aureus patients on hemodialysis or continuous ambulatory peritoneal dialysis.
DOSING MODE
For intranasal use.
Adults and children over 12 years of age
To apply the ointment as an applicator, you should use a cotton swab.
It is necessary to apply a small amount of ointment volume approximately from the match head (approximately 30 mg of ointment) to the nasal mucosa in each nasal passage 2 times / day for 5 days.
After applying the ointment, the nose should be tightened several times simultaneously from both sides, which ensures an even distribution of the ointment over the mucous membrane.
Wash hands before and after applying the product.
Usually nasal carriage disappears for 3-5 days of treatment. Do not use the drug for more than 5 days.
Children and adolescents over 12 years of age do not need a dose adjustment.
Older patients do not need a dose adjustment.
Patients with renal dysfunction do not need dose adjustment.
Patients with a violation of liver function correction of the dose is not required.
SIDE EFFECT
The undesirable reactions presented below are listed in accordance with the damage to organs and organ systems and frequency of occurrence. Frequency of occurrence is defined as follows: very often (? 1/10), often (? 1/100 and <1/10), infrequently (? 1/1000 and <1/100), rarely (? 1/10 000 and < 1/1000), very rarely (<1/10 000), including individual cases. Frequency categories were formed on the basis of clinical studies of the drug and post-registration surveillance.
The prevalence of infrequent adverse reactions was established on the basis of general safety data obtained from 12 clinical trials involving 422 patients. The prevalence of very rare undesirable reactions was determined mainly on the basis of post-registration data and therefore is the frequency of reports of such reactions, rather than the true frequency of occurrence of these reactions.
From the immune system: very rarely - local reactions of hypersensitivity, systemic allergic reactions (including anaphylaxis, generalized rash, hives and angioedema).
On the part of the respiratory system: infrequently - reactions from the mucous membrane of the nose (itching, redness, burning, tingling).
CONTRAINDICATIONS
- hypersensitivity to mupirocin or any other component included in the preparation, in the anamnesis;
- use of the drug in children under the age of 12 years (safety and efficacy assessment in children under 12 years of age has not been carried out, so the drug is not recommended for this age group).
PREGNANCY AND LACTATION
There is no data on the use of the drug during pregnancy and breastfeeding.
In animal studies, no signs of reproductive toxicity were found.
However, as with the use of other drugs, the use of the drug Bactroban В® during pregnancy and during breastfeeding is possible only if the intended benefit to the mother exceeds any potential risk to the fetus and the baby.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with renal dysfunction do not need dose adjustment.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Patients with a violation of liver function correction of the dose is not required.
APPLICATION FOR CHILDREN
Contraindicated the use of the drug in children under the age of 12 years (safety and efficacy in children under 12 years old was not performed, so the drug is not recommended for this age group).
APPLICATION IN ELDERLY PATIENTS
Older patients do not need a dose adjustment.
SPECIAL INSTRUCTIONS
The drug is not intended for use in ophthalmic practice.
Avoid contact with ointment in the eyes. In case of contact with eyes, rinse immediately with plenty of water until the remnants of the ointment are completely removed.
In rare cases, the use of the drug may cause a reaction of increased sensitivity or severe local irritation. In this case, it is required to stop treatment, if possible, remove the drug from the mucosa and prescribe an alternative therapy for the infection.
As with other antibacterial drugs, with prolonged use of mupirocin, there is a risk of excessive growth of insensitive microorganisms.
With the use of antibiotics, cases of pseudomembranous colitis have been described, the severity of which can vary from mild to life-threatening. Thus, it is important to consider the possibility of such a diagnosis in patients with diarrhea on the background or after the use of antibiotics. Although the probability of developing this phenomenon with local application of mupirocin is less, in case of prolonged or severe diarrhea or abdominal cramps, treatment should be stopped immediately and an additional examination of the patient should be carried out.
For elderly patients there are no restrictions (in the absence of symptoms of moderate or severe renal failure).
Do not use the ointment left in the open tube at the end of treatment for the next course of treatment.
Impact on the ability to drive vehicles and manage mechanisms
According to the described side effects, the use of the drug does not adversely affect the ability to drive vehicles or mechanisms.
OVERDOSE
Symptoms: At the moment there are limited data on overdose of mupirocin.
Treatment: there is no specific treatment for overdose with mupirocin. In case of an overdose, supportive therapy is indicated and appropriate monitoring of the patient's condition, if necessary.
DRUG INTERACTION
Do not mix the drug with other medicinal products to avoid dilution of the ointment and, consequently, decrease in antibacterial activity or a possible change in the stability of mupirocin.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years. Do not take the drug after the expiration date indicated on the package.
