Mupirocin – a drug of natural origin, obtained from a culture of Pseudomonas fluorescens. On chemical structure and mechanism of action differs from other ILA. Applies only locally.
Mechanism of action
Antibacterial action of Mupirocin Ointment is associated with inhibition of the enzyme isoleucyl-tRNA synthetase, resulting in disturbed synthesis of bacterial proteins and RNA, to a lesser extent – the synthesis of DNA and cell wall formation. Due to the uniqueness of the mechanism of cross-resistance with other classes of mupirocin ILA absent. However, there is the possibility of selection of resistance to mupirocin using separate AMP (tetracycline, trimethoprim) and antiseptic (triclosan) in the joint transfer of resistance genes. Depending on the concentration of this product may have both bacteriostatic and bactericidal action. Given the high local drug concentration (significantly exceed the IPC), the vast majority of cases it acts bactericidal.
Spectrum of activity
The main clinical significance of this product is in action for most strains of staphylococci, including MRSA, as well as strains resistant to other ILA. By mupirocin susceptible streptococci as A, B, C, G, and some gram-negative bacilli (P.multocida).
Mupirocin is inactive against enterococci, members of the family Enterobacteriaceae, P.aeruginosa, anaerobes. A distinctive feature of mupirocin is low in vitro activity against members of the normal microflora of the skin (Micrococcus spp., Coryne-bacterium spp., Propionibacterium spp.).
Pharmacokinetics
It is practically not absorbed from the surface of intact skin (less than 0.24% of dose) through the nasal mucosa absorption of a few more (1,2-5,1% of dose). Absorption may increase when there is damage. The drug creates a high and stable concentration in the surface layers of the skin. May be subjected to a partial slow inactivation in the skin. Soaked part of mupirocin is rapidly metabolized to form inactive Moniev acid, which is derived primarily by the kidneys. The Ointment is well linked to proteins (97%), so its effect is attenuated in the presence of serum.
Adverse reactions
For external applications: dry skin, burning, itching, pain, rash, redness, swelling.
When intranasal administration: cough, respiratory disorders, ear pain, headache, pharyngitis, rhinitis, affects the flavor.
Statement
Skin infections: furunculosis, folliculitis, impetigo, erysipelas, trophic ulcers, infected eczema, including those caused by MRSA.
Otitis externa (except for malignant).
Prevention of bacterial infections of the skin for wounds, bruises, burns.
Eradication of nasal carriage of MRSA in adult patients and medical staff.
Contraindications
Hypersensitivity to Mupirocin Ointment and / or any component, part of the dosage form.
Warnings:
Pregnancy. Adequate safety studies in pregnant women was conducted. Used in pregnancy is not recommended.
Breast-feeding. Penetration of mupirocin in breast milk has not been studied. In the absence of adequate safety data to use in women, breastfeeding is not recommended.
Pediatrics. According to pharmacokinetic studies in neonates and premature there is significant systemic absorption of Mupirocin Ointment after intranasal administration. Safety of intranasal mupirocin in infants and children up to 12 years has not been studied so intranasal application in these age groups is not recommended.
Renal dysfunction. When applying ointment to a large area of open wounds or burns, the better the absorption of polyethylene glycol included in the ointment base, which can lead to nephrotoxicity, particularly in patients with moderate and severe renal dysfunction.
Information for patients
Use the drug regularly, at about the same time, we can not apply the missed dose if almost time for the application of the next dose, you can not double dose.
Strictly observe the relevant use of the dosage form to the application. You can not enter dermatological ointment intranasally.
Before use, dermatological ointment should wash their hands with soap and thoroughly dry them. A small amount of drug applied to the affected skin and gently rub. If necessary, cover the affected area with gauze bandages.
After each application of nasal ointment should be within 1 minute gently massage the wings of the nose in order to ensure maximum penetration of the drug to the back of the throat.
Not recommended for simultaneous use of nasal Mupirocin Ointment and other drugs administered intranasally.
Avoid getting mupirocin in the eye, as it can cause burning and tearing, which may persist for several days or even weeks.
When a significant irritation, itching, rash, discontinue use of Mupirocin Ointment and seek medical advice.
