METRONIDAZOLE

Active material: Metronidazol
When ATH: G01AF01
CCF: Antiprotozoal drug with antibacterial activity
ICD-10 codes (testimony): A59, N76
When CSF: 07.01.03
Manufacturer: Synthesis of (Russia)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

◊ Vaginal gel 1% colorless or yellowish or zheltovato-greenish tint.

Excipients: propylene glycol, karʙomer (Carbopol), propilparagidroksibenzoat (nipazol, propyl), disodium эdetat (disodium edetate, Trilon b), Sodium hydroxide, Purified water.

30 g – aluminum tuba (1) complete with applikatorom for intravaginal introduction – packs cardboard.

Pharmacological action

Protivoprotozojnyj and antibacterial, 5-nitroimidazole derivative. The mechanism of action consists in biochemical restoration of 5-nitro group of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. The recovered 5-nitro group of metronidazole is reacted with the cellular DNA of microorganisms, inhibiting the synthesis of nucleic acids, that leads to the death of the bacteria.

It is active against protozoa: Trichomonas vaginalis, Giardia intestinalis, Entamoeba histolytica, Lamblia spp., as well as obligate gramotricationah anaerobov: Bacteroides spp. (incl. Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Gardnerella vaginalis, Veillonella spp., Prevotella spp. (Prevotella crossroads, Prevotella mouth, Prevotella disiens) and some grampolaugitionah anaerobic microorganisms: Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp., Mobiluncus spp. Minimum overwhelming concentration for these strains is 0.125-6.25 ug / ml.

Metronidazole insensitive aerobic microorganisms.

Pharmacokinetics

Absorption

After intravaginal introduction exposed systemic absorption (about 56 %). Relative bioavailability of metronidazole vaginal gel in the form in 2 times higher bioavailability of vaginal tablets in a one-time dose 500 mg. C_max When you apply a vaginal gel is 237 ng / ml achieved after 6-12 no.

Distribution

Plasma protein binding – less 20%. Metronidazole penetrate most body tissues, GEB and placental barrier. Provided with breast milk.

Metabolism

Metabolised in the liver by gidrauxilirovania, oxidation and glukuronirovania. Active metabolita (2-oksimetronidazol) is 30% source activity compounds.

Deduction

When taking metronidazole in dosage form for systemic use 60-80% dose appears kidneys (20% This quantity – in unchanged form), through the intestine – 6-15%.

Testimony

-urogenital trichomoniasis (incl. uretrit, vaginitis);

— baby vaginitis of different etiology (confirmed clinical and microbiological data).

Dosage regimen

Appoint intrawaginalno. The recommended dose is 5 g (one full applicator) 2 times / day (in the morning and in the evening). A course of treatment – 5 days.

Side effect

Allergic reactions: hives, skin rash.

Local reactions: stinging or irritation of the penis to sexual partner, sensation of burning or frequent urination, vulvyt (itch, searing pain or hyperemia mucous membranes in the field of external genital organs). After the drug may develop candidiasis of vagina.

Systemic reactions: possible change of taste sensations, including “metal” smack, dizziness, headache, dry mouth, nausea, vomiting, decreased appetite, cramping in the abdomen, constipation or diarrhea, staining of urine a dark color, leukopenia or leukocytosis.

Contraindications

- Leukopenia (incl. history);

— violation of coordination of movements,

- Organic CNS (incl. epilepsy);

- Liver failure (in the case of the appointment of high doses);

- I trimester of pregnancy;

- Lactation;

- Hypersensitivity to the drug;

-hypersensitivity to derivative nitrohimidazola.

FROM caution apply in groups II and III trimestrah pregnancy.

Pregnancy and lactation

The drug is contraindicated for use in the I trimester of pregnancy and lactation (breast-feeding). Be wary of in II and III trimestrah pregnancy.

Cautions

The drug is intended only for intravaginal application.

In waginite, caused by Trichomonas vaginalis, It is advisable to simultaneous treatment of sexual partner oral metronidazole.

In the case of use of the drug in conjunction with oral metronidazole, especially when repeated course, necessary to monitor patterns of peripheral blood (the danger of radiation).

During the period of treatment is contraindicated in ethanol intake (development disulfiramopodobnyh reactions: abdominal pain, spastic nature, nausea, vomiting, headache, a sudden rush of blood to the face).

During the course of treatment, patients should be avoided sexual contact.

Overdose

There are no data on overdose.

Drug Interactions

Similar disulfiramu, causes an intolerance to ethanol.

The simultaneous use of disulfiram can lead to a variety of neurological symptoms (nor should appoint metronidazole for patients, who have taken disulfiram in the past 2 weeks).

It enhances the effect of indirect anticoagulants (warfarin).

Do not combine with non-depolarizing muscle relaxants (vekuroniya bromide).

Together with the drug lithium can increase the concentration of plasma.

Phenobarbital accelerates the metabolism of metronidazole due to induction mikrosomaionah liver enzymes, cimetidine – decreases, which may lead to an increase in its concentration in the serum and an increased risk of side effects.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children, dry, dark place at a temperature of 15 ° to 25 ° C; Do not freeze. Shelf life – 2 year.