Tarzhivort vaginal suppositories, No. 10

• Vulvovaginitis: bacterial, candidal, Trichomonas and / or in association with mixed flora, sensitive to the components of the combination;

• nonspecific vaginitis;

• prevention of urogenital infections before gynecological surgery, diagnostic procedures and the installation of an intrauterine contraceptive.

Intravaginally 1 time / day for 10 days.

Vaginal suppositories from light yellow with a beige or cream shade to yellow with a beige or cream shade, cylindrical conical shape; on the cut, the presence of an air rod or a funnel-shaped depression is allowed.

1 supp.

metronidazole 500 mg

chloramphenicol 200 mg

natamycin 150 mg

hydrocortisone acetate 15 mg

Excipients: semi-synthetic glycerides (Supposir AM) - 1635 mg.

• Hypersensitivity to the components of the combination;

• severe dysfunction of the liver, kidneys;

• pregnancy, breastfeeding period;

• children and adolescents under the age of 18.

  Carefully

• Severe acute or chronic diseases of the central nervous system and peripheral nervous system (including with permanent or progressive neuropathies); violation of hematopoiesis (history of leukopenia).

pharmachologic effect

Combined drug for intravaginal use.

Metronidazole is an antimicrobial and antiprotozoal drug derived from 5-nitroimidazole. The mechanism of action consists in the biochemical reduction of the 5-nitro group of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group of metronidazole interacts with the DNA of the cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria. It is active against Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Mobiluncus spp., As well as against obligate anaerobes: Bacteroides spp., Fusobacterium spp.

Chloramphenicol is a broad-spectrum antibiotic. Has a bacteriostatic effect. The mechanism of action is associated with the suppression of the synthesis of proteins of microorganisms, due to the binding of the 50 8 ribosome subunit and the termination of the formation of the peptide chain. Effective against strains of bacteria resistant to penicillin, tetracyclines, sulfonamides. It is active against many gram-positive and gram-negative bacteria, causative agents of purulent infections, typhoid fever, dysentery, meningococcal infection.

Natamycin is a polyene antibiotic of the macrolide group, has a wide spectrum of antifungal action. Has a fungicidal effect. Natamycin binds sterols of cell membranes, disrupting their integrity and function, which leads to the death of microorganisms. Most pathogenic yeasts, especially Candida albicans, are sensitive to natamycin.

Hydrocortisone - GCS. It has anti-inflammatory, anti-exudative and anti-allergic effects.

Pharmacokinetics

With intravaginal administration, metronidazole is absorbed into the systemic circulation (about 20%). Cmax of metronidazole in the blood is determined after 6-12 hours and is approximately 50% of Cmax, which is achieved (after 1-3 hours) after a single dose of an equivalent dose of metronidazole inside. Plasma protein binding is less than 20%. Metronidazole is metabolized in the liver, hydroxyl metabolites are active. The activity of the main metabolite (2-oxymetronidazole) is 30% of the activity of the parent compound. Metronidazole and oxidized metabolites are excreted mainly by the kidneys (20% unchanged) and, to a lesser extent, through the intestines. Penetrates the BBB and the placental barrier, excreted in breast milk.

The pharmacokinetics of chloramphenicol with intravaginal administration has not been studied.

Natamycin, when administered intravaginally, is not absorbed from the mucous membrane.

With intravaginal administration, hydrocortisone is practically not absorbed from the vaginal mucosa, the plasma concentration is below the detection level.

Side effect

Local reactions: burning sensation, pain, irritation and edema at the injection site, erythema, vaginal dryness, especially at the beginning of treatment, which do not require discontinuation of treatment and are determined by the effect of this agent on the irritated vaginal mucosa.

From the hematopoietic and lymphatic system: a decrease in the number of blood leukocytes (leukopenia).

From the immune system: rash, itching of the skin, urticaria, anaphylactic reactions.

From the side of mental status: anxiety, mood lability.

From the nervous system: headache, with prolonged use of the drug - peripheral neuropathy (feeling of numbness and tingling (paresthesia), convulsions, tremors.

From the vestibular apparatus: movement disorders (ataxia), dizziness.

From the digestive system: pain or cramps in the abdomen, 'metallic' taste in the mouth, change in taste, dry mouth, constipation, diarrhea, loss of appetite, nausea, vomiting.

Application during pregnancy and lactation

Use during pregnancy and breastfeeding is contraindicated.

Application for violations of liver function

Use is contraindicated in severe violations of the liver function.

Application for impaired renal function

It is contraindicated for use in severe disorders of the kidney function.

Application in children

Contraindicated for use in children and adolescents under the age of 18 years.

special instructions

During treatment, it is recommended to refrain from sexual intercourse.

In case of infection of the sexual partner and to exclude the possibility of reinfection, simultaneous treatment of both partners is mandatory

In the case of using this combination together with metronidazole for oral administration, especially with a repeated course, it is necessary to control the picture of peripheral blood (risk of leukopenia) If a decrease in the number of leukocytes is detected, treatment should be discontinued.

If movement disorders, dizziness, confusion, paresthesias or seizures appear during treatment, treatment should be discontinued.

Metronidazole, which is part of the drug, is able to immobilize treponemas, which leads to an erroneous positive Nelson's test.

Influence on the ability to drive vehicles and mechanisms

A possible negative effect on the ability to drive vehicles and potentially dangerous mechanisms cannot be ruled out, therefore, care must be taken during treatment. If side effects from the central nervous system appear, the patient should refrain from driving.

Drug interactions

With simultaneous use with oral anticoagulants (for example, warfarin), it is possible to increase the concentration of anticoagulants in plasma, increase the effect and, therefore, the risk of bleeding; it is necessary to control the level of prothrombin and monitor the prothrombin time; it is necessary to adjust the dose of oral anticoagulants during treatment and within one week after stopping treatment.

With simultaneous use with lithium preparations, an increase in the toxicity of the latter is possible.

With simultaneous use with cyclosporine, it is possible to increase the concentration of cyclosporine in plasma.

With simultaneous use with disulfiram, psychotic reactions are possible (attacks of delirium, confusion); should not be prescribed to patients who have taken disulfiram within the last 2 weeks.

With simultaneous use with drugs containing ethanol, or with the use of ethanol, disulfiram-like reactions may develop (feeling of heat, facial redness, vomiting, tachycardia).

With simultaneous use with busulfan, an increase in the concentration of busulfan in blood plasma is possible.

With simultaneous use with phenobarbital, the concentration of metronidazole in the blood decreases.

With simultaneous use with cimetidine, an increase in the concentration of metronidazole in the blood is possible.