Description
Release form
Vaginal gel.
Packaging
tube 50g
Pharmacological action
antimicrobial combination agent (antimicrobial and antiprotozoal agent + antifungal agent).
ATX code [G01AF20]
Pharmacological properties of
Pharmacodynamics. A combined preparation for intravaginal use, the effectiveness of which is due to the presence of two components in its composition: metronidazole and clotrimazole.
Metronidazole is highly active against protozoa: Entamoeba histolytica, Giardia lamblia, Trichomonas vaginalis, and gram-negative anaerobes: Bacteroides fragilis, Fusobacterium spp., Prevotella (P. bivia, P. buccae, P. disiere, and others) Gram-positive microorganisms: Clostridium perffringens, Clostridium difficile, Peptococcus spp., Peptostreptococcus spp. The minimum inhibitory concentration for these strains is 0.125 – 6.25 μg / ml.
Clotrimazole is an imidazole derivative. It has a fungicidal and bactericidal effect. Inhibits the biosynthesis of ergosterol, which regulates the permeability of the cell wall of microorganisms. It acts fungistatically in small concentrations, and fungicidal in large concentrations. In fungicidal concentrations, it interacts with mitochondrial and peroxidase enzymes, resulting in an increase in the concentration of hydrogen peroxide to a toxic level, which also leads to the death of fungi. It has high activity against fungi: Blastomyces dermatitidis, Candida spp., Coccidioides immitis, Cryptococcus neoformans, dermatophytes (Trichophyton mentagrophytes, Microsporum canis, Epidermophyton floccosum), Histoplasma capsulatum, Paracoccidioides bras Sporothrix schenckii protozoa: Trichomonas vaginalis gram-positive bacteria: Streptococcus spp., Staphylococcus spp., Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Proteus mirabilis.
Pharmacokinetics. After intravaginal administration, metronidazole undergoes systemic absorption (about 56%). The relative bioavailability of the vaginal gel is 2 times higher than the bioavailability of a single dose (500 mg) of vaginal metronidazole tablets. Penetrates into breast milk and most tissues, passes through the blood-brain barrier and placenta. After a single intravaginal administration of 5 g of gel (50 mg of metronidazole), the average maximum concentration in the blood serum of healthy women is 237 ng / ml, which is 2% of the average maximum concentration of metronidazole when ingested with a dose of 500 mg. The time to reach maximum concentration is 6-12 hours. Communication with plasma proteins is less than 20%. It is metabolized in the liver by hydroxylation, oxidation and glucuronidation. The activity of the main metabolite (2-oxymethronidazole) is 30% of the activity of the starting compound. It is excreted by the kidneys – 60-80% of the dose of the systemic drug (20% of this amount unchanged), by the intestines – 6-15% of the dose of the systemic drug.
When using clotrimazole, no more than 3-10% of the administered dose is intravaginally absorbed. High concentrations in vaginal secretions and low concentrations in the blood persist for 48-72 hours. In the liver, clotrimazole is rapidly metabolized to inactive metabolites.
Indications
Bacterial vaginoses of various etiologies, confirmed by clinical and microbiological data, candida vulvitis and vulvovaginitis, urogenital trichomoniasis.
Contraindications
Hypersensitivity to the components of the drug. Leukopenia (including a history of) organic damage to the central nervous system (including epilepsy), liver failure. Pregnancy I trimester.
Use during pregnancy and lactation
Use of the drug in the II and III trimester of pregnancy is possible only under strict medical indications and under the supervision of a doctor (without the use of an applicator). When prescribing the drug during lactation, it is necessary to stop breastfeeding.
Special instructions
Alcohol is contraindicated during treatment (disulfiram-like reactions may occur: spastic abdominal pain, nausea, vomiting, headache, sudden rush of blood to the face).
Metronidazole can immobilize treponema and lead to a false positive Nelson test. For intravaginal use only! Avoid contact with eyes!
During the course of treatment, it is necessary to abstain from sexual activity.
Composition of
One gram of gel contains:
Metronidazole 10 mg
Clotrimazole 20 mg
and excipients: methylhydroxybenzoate, propylhydroxybenzoate, disodium edetate, propylene glycol 9, sodium hydroxide, carbomer Opalescent homogeneous gel of white or almost white color
Dosage and administration of
Intravaginally. The recommended dose is 5 g (one full applicator) 2 times a day (morning and evening). The course of treatment is 5 days. If necessary, the course of treatment can be repeated after 2 weeks.
Side effects
Local reactions: burning sensation or frequent urination in the sexual partner – burning sensation or irritation of the penis.
Perhaps the development of systemic effects: dizziness, headache, nausea, spastic pain in the abdominal cavity.
Allergic reactions: skin rash, urticaria.
In case of any unwanted side effects, stop treatment and consult a doctor!
Drug Interactions
Similarly to disulfiram, it causes ethanol intolerance.
Enhances the effects of indirect anticoagulants, It is not recommended to combine with non-depolarizing muscle relaxants (vecuronium).
When taken with lithium preparations, the concentration of lithium in the blood plasma may increase.
Phenobarbital accelerates the metabolism of metronidazole due to the induction of microsomal liver enzymes, cmitidine – reduces.
Amphotericin B, nystatin, natamycin reduce the effectiveness of clotrimazole while using it.
overdose
No overdose has been reported with the recommended doses at the recommended doses
Storage Conditions
At a temperature not exceeding 25 C, out of the reach of children.
Shelf life
2 years.
Do not use after the expiration date printed on the package.
Pharmacy conditions
without prescription
Dosage form
gel vaginal
Unique Pharmaceutical, India
