Clinical and pharmacological group: & nbsp

Interferons

Other synthetic antibacterial agents

Antifungal means

Included in the formulation
  • Vagiféron®
    suppositories the vagina. 
    FIRN M, ZAO     Russia
  • АТХ:

    G.01.A.F.20   Combinations of imidazole derivatives

    Pharmacodynamics:

    Interferon alfa-2b inhibits the replication of viruses, disrupts the synthesis of viral DNA, RNA and viral proteins. The drug increases the phagocytic activity of macrophages, potentiates the cytotoxic effect of lymphocytes. It shows pronounced antitumor activity due to antiproliferative properties.

    Metronidazole - the drug is active against Gardnerella vaginalis, Trichomonas vaginalis, Giardia lamblia, Entamoeba histolytica, as well as for anaerobic bacteria. The drug is resistant to aerobic microorganisms.

    Enzyme systems of anaerobic bacteria and microaerophilic intracavitary parasites restore the nitro group of metronidazole (the nitro group of the metronidazole molecule is the electron acceptor). Refurbished metronidazole is built into the respiratory chain of protozoa and anaerobes, preventing the action of flavoproteins - carriers of electrons. As a result, respiratory processes are violated, which leads to cell death. In addition, in some species of anaerobes and protozoa in the reduction of the nitro group metronidazole promotes the formation of free radicals that damage DNA.

    Fluconazole is an antifungal agent. The triazole derivative exhibits an antifungal effect by blocking the biosynthesis of the ergosterol of the fungal cell membrane. "Target" for the action of the drug - enzyme 14-α-demethylase. 14-α-demethylase is part of a group of enzymes known collectively "cytochrome P450 ". All enzymes of the cytochrome P450 group contain a hematinic iron-containing pigment. Fluconazole binds to the iron atom of the hematinic group and inactivates 14-α-demethylase, which leads to a disruption in the synthesis of ergosterol and the accumulation of lanosterol and other sterols. Their incorporation into the membrane instead of ergosterol significantly disrupts the structure and function of the fungal cell membrane.

    The decrease in the synthesis of ergosterol, as well as the accumulation of 14α-methylsterols, destroys the densely packed acyl chains of the phospholipids of the fungal membranes. Destabilization of the fungal membrane leads to dysfunction of membrane enzymes, including those involved in the electron transport chain, and ultimately to cell death.

    Fluconazole has a highly specific fungicidal (antifungal) action. It is active in mycosis, including caused by Candida spp.(including generalized forms of candidiasis on the background of immunodepression), Cryptococcus neoformans and Coccidioides immitis, Microsporum spp., Blastomyces dermatitidis. When intravaginal application is particularly active in relation to Candida albicans, to a lesser extent - in relation to Candida glabrata.

    Pharmacokinetics:

    After intravaginal administration, the bioavailability of metronidazole is 20% compared to oral administration. After intravaginal administration, it undergoes systemic absorption (about 56%). Metabolized in the liver by hydroxylation, oxidation and glucuronation. The activity of the main metabolite (2-hydroxymethonidazole) is 30% of the activity of the parent compound. Half-life is 6 to 12 hours. Output is 40-70% (about 20% unchanged) through the kidneys. The pharmacokinetics of interferon and fluconazole for intravaginal application has not been studied.

    Indications:

    Bacterial vaginitis (nonspecific).

    Bacterial vaginosis.

    Vaginitis caused by a mixed infection (Trichomonases, gardnerelli, yeast-like fungi, herpes simplex virus type 1 and type 2, mycoplasma, ureaplasma) as part of complex therapy.

    I.A30-A49.A49.3   Infection caused by mycoplasma, unspecified

    I.A50-A64.A59   Trichomoniasis

    I.A50-A64.A59.0   Urogenital trichomoniasis

    I.A50-A64.A60   Anogenital herpetic viral infection [herpes simplex]

    I.A50-A64.A63.8   Other specified diseases, mainly sexually transmitted

    I.B35-B49.B37.3   Candidiasis of the vulva and vagina (N77.1 *)

    XIV.N70-N77.N76   Other inflammatory diseases of the vagina and vulva

    XIV.N70-N77.N76.8   Other specified inflammatory diseases of the vagina and vulva

    XIV.N70-N77.N77.1 *   Vaginitis, vulvitis and vulvovaginitis in infectious and parasitic diseases classified elsewhere

    Contraindications:

    Age to 18 years.

    Pregnancy.

    Hypersensitivity.

    Carefully:

    No data.

    Pregnancy and lactation:

    The drug is not used in pregnancy. Metronidazole penetrates into breast milk. Breastfeeding during the period of taking the drug should be canceled. Renew breastfeeding should not be earlier than 48 hours after the end of the drug.

    Dosing and Administration:

    The drug is taken intravaginally, 1 suppository in the evening (before bedtime) once a day for 10 days. (1 suppository - interferon alpha-2b human recombinant not less than 50000 IU, fluconazole 200 mg, metronidazole 150 mg).

    Side effects:

    Allergic reactions.

    Ataxia.

    Convulsions.

    Constipation.

    Headache.

    Nausea.

    Pain and cramping in the abdomen.

    Dryness in the mouth.

    Increased fatigue.

    Leukopenia.

    Changes in the psyche (anxiety, lability of mood).

    Diarrhea.

    Dizziness.

    Loss of appetite.

    Vomiting.

    Change of taste.

    "Metallic" or unpleasant aftertaste in the mouth.

    Overdose:

    Cases of drug overdose have not been identified.

    Metronidazole

    Symptoms: nausea, vomiting, abdominal pain, diarrhea, itching, metallic taste in the mouth, ataxia, dizziness, paresthesia, convulsions, leukopenia, dark staining of urine.

    Interaction:

    Do not combine with nondepolarizing muscle relaxants.

    Possible a joint use with dzhozamycin (antibiotic-macrolide systemic action).

    Special instructions:

    During the treatment period, refrain from having sexual intercourse.

    During the treatment period, do not consume ethanol.

    In the case of using the drug in conjunction with metronidazole for oral administration, especially in the second course, control of the picture of peripheral blood (danger of leukopenia) is necessary. During the period of treatment, ethanol intake is contraindicated (development of disulfiram-like reactions is possible - abdominal pain of spastic nature, nausea, vomiting, headache,a sudden rush of blood to the face). Do not assign metronidazole patients who took disulfiram during the last 2 weekspruce.

    Impact on the ability to manage motor transport and other technical devices

    The drug does not affect the ability to drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

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