Metronidazole - instructions for use, dose, side effects, contraindications

Suppositories from white to white with a yellowish hue; torpedoform. On the longitudinal section, there may be an air rod or a funnel-shaped depression.

Pharmacotherapeutic group:Antimicrobial and antiprotozoal drug

ATX: & nbsp

P.01.A.B Nitroimidazole derivatives

P.01.A.B.01 Metronidazole

Pharmacodynamics:

Metronidazole is a 5-nitroimidazole and is a bactericidal-type drug that exhibits tropism for deoxyribonucleic acid. The mechanism of action of metronidazole is 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 reacts with the deoxyribonucleic acid of a cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of microorganisms.

Metronidazole is an effective antimicrobial and antiprotozoal means of a wide spectrum of action.

The drug shows a high activity in relation to: Trichomonas vaginalis, Entamoeba histolytica; as well as against gram-negative anaerobes Bacteroides spp. (including AT. fragilis, AT. ovatus, AT. distasonis, AT. thetaiotaomicron, AT. vulgatus), Fusobacterium spp. and some Gram-positive anaerobes (sensitive strains Eubacterium spp., Clostridium spp., Peptostreptococcus spp., Peptococcus spp.).

To Metronidazole insensitive aerobic microorganisms and facultative anaerobes, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against conventional aerobes.

Pharmacokinetics:

After vaginal administration metronidazole is subject to systemic absorption (about 56%). It penetrates into breast milk and most tissues, passes through the blood-brain barrier and the placenta. Connection with plasma proteins - less than 20%. Metabolized in the liver by hydroxylation, oxidation and glucuronation. Activity of the main metabolite (2-hydroxymethonidazole) - 30% of the activity of the starting compound. The time required to reach the maximum concentration (237 ng / ml) is 6-12 hours. It is excreted by the kidneys - 60-80% (about 20% dose in unchanged form).

Indications:

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

Contraindications:

Hypersensitivity to metronidazole or other nitroimidazole derivatives, leukopenia (including in the anamnesis),disorders of coordination of movements, organic lesions of the central nervous system (including epilepsy), liver failure (in the case of large doses), children under 18 years of age.

Pregnancy and lactation:

The drug is contraindicated in the first trimester of pregnancy (it penetrates the placenta), then it should be used only if the potential benefit to the mother exceeds the possible risk to the fetus.

Metronidazole penetrates into breast milk, so breastfeeding during the period of taking the drug should be canceled. Renew breastfeeding is possible no earlier than 48 hours after the end of the drug.

Dosing and Administration:

Mode of application: vaginally, having previously released the suppository from the contour package using scissors, cutting the film along the contour of the suppository.

Enter deeply into the vagina 1 suppository at 500 mg 2 times a day (morning and evening) for 7-10 days.

During the course of treatment, sexual intercourse should be avoided.

Side effects:

Local side effects: itching, burning, pain and irritation in the vagina; thick, white, mucous discharge from the vagina without smell or with a faint odor;frequent urination; after drug cancellation - development of candidiasis of the vagina is possible; a burning sensation or irritation of the penis in the sexual partner.

From the gastrointestinal tract: change in taste, metallic taste in the mouth, dry mouth, decreased appetite, abdominal cramps, nausea, vomiting, constipation, or diarrhea.

From the nervous system: dizziness, headache.

On the part of the hematopoiesis system: leukopenia or leukocytosis.

Allergic reactions: urticaria, skin rash.

In rare cases, the color of urine can be observed in the red-brown color, due to the presence of a water-soluble pigment formed as a result of metronidazole metabolism.

Overdose:

Symptoms: nausea, vomiting, ataxia.

Treatment: there is no specific antidote, symptomatic and supportive therapy.

Interaction:

Compatible with sulfonamides and antibiotics. When treating metronidazole, avoid drinking alcohol (similar to disulfiram causes alcohol intolerance). Do not combine metronidazole with disulfiram, since the interaction of these drugs may inhibit consciousness, the development of mental disorders.

When used concomitantly with warfarin and other indirect anticoagulants metronidazole intensifies their action, which leads to an increase in prothrombin time. It is not recommended to combine with nondepolarizing muscle relaxants (vecuronium bromide).

Under the influence of barbiturates, the effect of metronidazole may decrease, since its inactivation in the liver is accelerated.

Cimetidine depresses the metabolism of metronidazole, which can lead to an increase in its concentration in the blood serum and an increased risk of developing adverse reactions.

With simultaneous administration with lithium preparations, the concentration of the latter in plasma can increase.

Special instructions:

Treatment with metronidazole should not last more than 10 days and should be repeated more than 2-3 times a year.

During treatment of trichomonas vaginitis in women and trichomoniasis in men, it is necessary to abstain from sexual intercourse.

With vaginitis caused by Trichomonas vaginalis, it is advisable to simultaneously treat the sexual partner metronidazole for oral administration.

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, the intake of ethanol is contraindicated (it is possible to develop a disulfiram-like reaction: spastic abdominal pain, nausea, vomiting, headache, sudden rush of blood to the face).

Effect on the ability to drive transp. cf. and fur:During treatment, care should be taken when managing vehicles, mechanisms, and also engaging in activities requiring rapidity of psychomotor reactions;

Form release / dosage:Vaginal suppositories, 500 mg.

Packaging:

Suppositories of 5 pieces are placed in a contour mesh package made of a polyvinyl chloride film.

Two contour mesh packages together with the instruction for use are placed in. a pack of cardboard.

Storage conditions:

In a dry, dark place at a temperature of no higher than 15 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001286

Date of registration:08.12.2011

Expiration Date:Unlimited

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Representation: & nbspDALHIMFARM, OJSCDALHIMFARM, OJSC

Information update date: & nbsp25.04.2018

Illustrated instructions

Instructions

Metronidazole (Metronidazole)