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Active ingredients
Metronidazole
Release form
Gel
Composition
In 1 g of gel: metronidazole 10 mg. Excipients: propyl hydroxybenzoate, propylene glycol, carbomer-940, disodium edetate, sodium hydroxide, purified water.
Pharmacological effect
Metronidazole has a high activity against Trichomonas vaginalis, Gardnerella vaginalis, Giardia intestinalis, Entamoeba histolytica, and obligate anaerobes Bacteroides spp. (Including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides viilgatus), Fusobacterium spp., Veillonela spp., Prevotella (P. bivia, P. buccae. P.disiens), and some gram-positive bacteria ( Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp., Mobiluncus spp.). The minimum inhibitory concentration for these strains is 0.125–6.25 mcg / ml; The mechanism of action of Metrogyl consists in the biochemical reduction of the 5-nitro group of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. The recovered 5-nitro group of metronidazole interacts with the microbial cell DNA, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.
Pharmacokinetics
After a single intravaginal administration of 5 g of Metrogyl, the average Cmax of the drug in serum is 237 ng / ml, which is 2% of the average Cmax of metronidazole when a dose of 500 mg is taken inside the dose. The time to reach Cmax is 6-12 hours after intravaginal administration of a single dose of 5 g and 1-3 hours after oral administration of metronidazole at a dose of 500 mg. After intravaginal administration, the drug undergoes systemic absorption (about 56%). Penetrates into breast milk and most tissues, passes through the blood-brain barrier and the placenta. Plasma protein binding is less than 20%. Metabolized in the liver by hydroxylation, oxidation and glucuronidation. The activity of the main metabolite (2-hydroxymetronidazole) - 30% of the activity of the parent compound .; The relative bioavailability of the vaginal gel is 2 times higher than the bioavailability of a single dose (500 mg) of vaginal pills metronidazole, due to the high penetrating ability of the drug into the vaginal fluid. Therefore, the therapeutic effect after intravaginal administration is achieved at low concentrations of metronidazole .; It is excreted by the kidneys - 60-80% of the dose of the systemic drug (20% - unchanged), the intestine - 6-15% of the dose of the systemic drug.
Indications
Bacterial vaginosis of various etiologies, confirmed by clinical and microbiological data; urogenital trichomoniasis.
Contraindications
Leukopenia (includingin history); lack of coordination of movements; organic lesions of the central nervous system (including epilepsy); liver failure; pregnancy - I term; hypersensitivity (including to nitroimidazole derivatives).
Use during pregnancy and lactation
Perhaps the use of the drug in the II and III trimesters of pregnancy. When prescribing the drug during lactation, it is recommended to stop breastfeeding.
Dosage and administration
Intravaginally. The recommended dose is 5 g (1 full applicator) 2 times / day (morning and evening). The course of treatment is 5 days.
Side effects
Local reactions: burning sensation or frequent urination, vulvitis; at the sexual partner - a burning sensation or irritation of the penis. After discontinuation of the drug - the development of vaginal candidiasis .; Possible development of systemic effects: dizziness, headache, dry mouth, changes in taste, including metallic taste, nausea, vomiting, loss of appetite, spastic abdominal pain, constipation or diarrhea, dark urine staining, leukopenia or leukocytosis .; Allergic reactions: skin rash, urticaria .; In the event of any undesirable side effects, you must stop treatment and consult a doctor.
Overdose
Cases of overdose when prescribed at recommended doses were not observed.
Interaction with other drugs
Similar to disulfiram, it causes intolerance to ethanol; It enhances the effect of indirect anti-coagulants; it is not recommended to combine with non-depolarizing muscle relaxants (vecuronium) .; When taken simultaneously 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, cimetidine - reduces.
special instructions
Metrogil; can immobilize treponema and lead to a false-positive Nelson test; During the course of treatment it is necessary to refrain from sex .; Avoid contact with eyes.