Gravagin

General characteristics. Structure:

Active ingredient: metronidazole; 1 suppository contains 500 mg of metronidazole; excipient: lipophilic basis. Main physical and chemical properties: suppositories of white color, with slightly yellowish or yellowish-greenish shade, an ovoid form (ovula).

Pharmacological properties:

Pharmacodynamics. Metronidazole, active ingredient of Gravagin, is derivative 5 nitroimidazoles, possesses a wide range of antimicrobic action in relation to gram-positive and gram-negative anaerobic bacteria, and also protozoa. Drug acts bakteritsidno on Peptostreptococcus spp., Clostridium spp., Bacteroides spp., Fusobacterium spp., Prevotella spp., Veilonella spp., Eubacterium spp., Gardnerella vaginalis, an also oppresses development of the elementary Trichomonas vaginalis, Entamoeba histolytica, Giardia intestinalis (Lamblia intestinalis). The mechanism of effect of metronidazole is connected with disturbance of synthesis of nucleic acids in DNA of microorganisms that leads to their death. Besides, the nitrogroup of a molecule of metronidazole, being an acceptor of electrons, is built in a respiratory chain of protozoa and anaerobe bacterias (competes with elektrontransportiruyushchy proteins — flavoproteins) that breaks respiratory processes and causes death of microorganisms.

Pharmacokinetics. At intravaginalny use drug creates high antimicrobic and anti-protozoan concentration of metronidazole in a vagina, a neck of uterus, a cavity and walls of a uterus, bodies of a small pelvis. System absorption of metronidazole makes 10-15 %, other part is brought out of an organism with vulval allocations for days. The elimination half-life of the metronidazole which got to system blood circulation makes 8-10 hours. 10-20 % of metronidazole contact blood proteins. Gets into most bodies and liquids of an organism, including breast milk, a vaginal secret, through a placenta in the same concentration, as in a blood plasma. It is metabolized in a liver generally by oxidation and conjugation with glucuronic acid, 60-80 % are removed with urine, the rest — through intestines. Metabolites of metronidazole paint urine in red-brown color.

Indications to use:

Mecotic vaginitis, nonspecific vaginita.

Route of administration and doses:

Drug is used for treatment only of adult patients. Suppository is exempted from planimetric packaging and entered deeply into a vagina in a dorsal decubitus with the legs bent in knees and tightened to a breast or "on cards". For treatment of a mecotic vaginitis appoint 500 mg (1 suppository) to night for 10 days in a row once a day. For treatment of nonspecific vaginit appoint 500 mg (1 suppository) for 7 days in a row once a day. Simultaneous treatment of the sexual partner, even in the absence of infection symptoms at it is necessary. The maximum duration of treatment should not exceed 10 days, and quantity of courses of treatment — no more than 3 in a year.

Features of use:

Prolonged use of drug demands control of a blood count. With care it is necessary to use drug at a serious illness of a liver, and also to patients with the permanent or progressing neyropatiya. It is necessary to remember risk of deterioration in the neurologic status of patients with a serious chronic or acute neurologic illness at treatment by metronidazole. It is necessary to stop treatment at emergence of an ataxy, dizziness, hallucinations and at deterioration in the neurologic status of the patient. Metronidazole is capable to immobilize treponemas that can result in false positive results at test of Nelson. Patients have to be warned that during Gravagin's use it is necessary to refuse completely alcohol intake, and also the medicines containing alcohol. At use of vaginal suppository along with condoms or vaginal diaphragms the risk of a rupture of latex can increase.

Ability to influence speed of response at control of motor transport or work with other mechanisms. During Gravagin's use it is not recommended to drive the car and other mechanisms.

Use during pregnancy or feeding by a breast. In the I trimester of pregnancy use of drug is contraindicated. In II and III trimesters use of drug is possible in case the expected positive effect for mother exceeds potential risk for the fruit/child. Metronidazole gets into breast milk therefore for drug use feeding by a breast needs to be stopped.

Children. Drug is used for treatment only of adult patients.

Side effects:

Digestive tract: pain in a stomach, anorexia, taste disturbances, stomatitis, nausea, vomiting, diarrhea, exceptional cases of pancreatitis which have reversible character.

Hypersensitivity reactions: an itch, an erythema, urticaria, fever, isolated cases of pustular rash, a Quincke's disease, in exceptional cases — an acute anaphylaxis.

Peripheral and central nervous system: headache, dizziness, peripheral touch neuropathy, spasms. Very seldom — cases of encephalopathy and a subacute cerebellar syndrome (an ataxy, a dysarthtia, gait disturbance, a nystagmus, a tremor) which pass after drug withdrawal.

Mental disorders: psychotic frustration, including confusion of consciousness, hallucination.

Temporary disturbances of an organ of sight: diplopia, myopia.

Hematology: isolated cases of an agranulocytosis, neutropenia and thrombocytopenia.

Abnormal liver function: isolated cases of an aberration of functional hepatic trials and cholestatic hepatitis which have reversible character. During treatment coloring of urine in henna-red color is possible.

Interaction with other medicines:

Drug inhibits enzyme to an aldegiddegidrogenaz therefore at combined use with alcohol, causes disulfiramopodobny reaction (reddening, vomiting, tachycardia). Reported about cases of psychotic reactions at patients who accepted at the same time metronidazole and Disulfiramum. Gravagin exponentiates effect of indirect anticoagulants therefore in case of need combined use it is necessary to monitorirovat daily MHO (the international normalizing relation) and if necessary to reduce an anticoagulant dose. Lithium level in a blood plasma at simultaneous use with metronidazole can increase. It is necessary to control concentration of lithium, creatinine and electrolytes in a blood plasma at patients who accept lithium and metronidazole. At combined use with Phenytoinum or phenobarbital metronidazole level in a blood plasma can umenshatsya. Metronidazole slows down metabolism of a 5-ftoruratsil, cyclosporine, a busulfan, increasing their plasma concentration and toxicity.

Contraindications:

Hypersensitivity to metronidazole or other components of drug. Hypersensitivity to imidazole derivatives. First trimester of pregnancy and period of feeding by a breast.

Overdose:

The ataxy, vomiting, neuropathy, leukopenia can be observed. There is no specific antidote, a symptomatic treatment. Metronidazole to be removed from an organism when carrying out a hemodialysis.

Storage conditions:

To store at  a temperature from +8 °C to +15 °C. To store in the place, unavailable to children. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

On 5 suppositories in a blister strip packaging from a polyvinyl chloride film. On two blister strip packagings with the application instruction in a cardboard pack.