Metronidazole, vaginal suppositories 500 mg 10 pcs

Pharmgroup:

Antimicrobial and antiprotozoal agent.

Pharmic action:

An antiprotozoal and antibacterial drug, a 5-nitroimidazole derivative. Mechanism of action consists in biochemical reduction of 5-nitrogroup of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitrogroup of metronidazole interacts with the DNA of the microbial cell, inhibiting the synthesis of their nucleic acids, which leads to the death of the bacteria.

It is active against Trichomonas vaginalis, Entamoeba histolytica as well as Gram-negative anaerobes Bacteroides spp. (including B. fragilis, B. distasonis, B. ovatus, B. thetaiotaomicron, B. vulgatus), Fusobacterium spp. and some Gram-positive anaerobes (sensitive strains of Eubacterium spp, Clostridium spp., Peptococcus niger, Peptostreptococcus spp.). The MPC for these strains is 0.125-6.25 µg/ml.

The aerobic microorganisms and facultative anaerobes are insensitive to metronidazole, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against common aerobes.

Pharmacokinetics:

After intravaginal administration it undergoes systemic absorption (about 56%).

The relative bioavailability of vaginal gel is 2 times greater than the bioavailability of a single dose (500 mg) of metronidazole vaginal tablets.

Passes into breast milk and most tissues, passes through the HEB and placenta. Binding to plasma proteins is less than 20%. Metabolized in the liver by hydroxylation, oxidation and glucuronidation. The activity of the main metabolite (2-oxymetronidazole) is 30% of the activity of the parent compound. TCmax (237 ng/ml) of vaginal gel is 6-12 hours.

Extracted by the kidneys – 60-80% of the dose of the drug of systemic action (20% of this amount in unchanged form), by the intestine – 6-15% of the dose of the drug of systemic action.

Indications

Urogenital trichomoniasis (including urethritis, vaginitis), nonspecific vaginitis of various etiologies, confirmed by clinical and microbiological data.

Active ingredient

How to take, the dosage

Intravaginally, once 2 g or as a course of treatment 500 mg/day 2 times a day (morning and evening) for 10 days.

At the time of treatment, sexual intercourse should be avoided.

Interaction

Similar to disulfiram, it causes ethanol intolerance.

Simultaneous use with disulfiram may lead to the development of various neurological symptoms (metronidazole should not be administered to patients who have taken disulfiram in the last 2 weeks).

It increases the effect of indirect anticoagulants (warfarin), it is not recommended to combine with nondepolarizing myorelaxants (vecuronium bromide).

Simultaneous use with Li+ drugs may increase the concentration of the latter in plasma.

Phenobarbital accelerates metabolism of metronidazole due to induction of microsomal liver enzymes; cimetidine decreases it, which may cause increase of its concentration in serum and increase the risk of side effects.

Special Instructions

The simultaneous treatment of sexual partners is recommended.

When treating trichomonas vaginitis in women and trichomonas urethritis in men it is necessary to refrain from sexual intercourse.
In vaginitis caused by Trichomonas vaginalis it is advisable to treat the sexual partner with oral metronidazole simultaneously.

In case of concomitant treatment with oral metronidazole, especially if repeated, peripheral blood counts should be monitored (risk of leukopenia).

Ethanol administration is contraindicated during treatment (development of disulfiram-like reactions is possible: spastic abdominal pain, nausea, vomiting, headache, sudden rush of blood to the face).

Contraindications

Hypersensitivity (including to nitroimidazole derivatives), leukopenia, movement coordination disorders, organic CNS lesions (including epilepsy), liver failure (in case of high doses), pregnancy (I trimester), lactation.

With caution. Pregnancy (II-III trimesters), leukopenia in anamnesis.

Side effects

Allergic reactions: urticaria, skin rash.

Local reactions: burning sensation or irritation of the penis in the sexual partner, burning sensation or increased frequency of urination, vulvitis (itching, burning pain or hyperemia of the mucous membrane in the area of the external genitalia).

Possible systemic effects include change in taste, including metallic taste, dizziness, headache, dry mouth, nausea, vomiting, decreased appetite, spastic abdominal pain, constipation or diarrhea, dark urine coloring, leukopenia or leukocytosis.

After withdrawal of the drug, the development of vaginal candidiasis.

Overdose

Symptoms: nausea, vomiting, ataxia.

Treatment: no specific antidote, symptomatic and supportive therapy.

Similarities