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

Description:Suppositories cylindrical, from white to white with a yellowish hue of color.On the cut, an air rod or a funnel-shaped depression is allowed.

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 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 bacteria.

Active with respect to protozoa: Trichomonas vaginalis, Giardia lamblia, Entamoeba histolytica, as well as facultative anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella spp. (Prevotella bivia, Prevotella buccae, Prevotella disiens) and some gram-positive obligatory (Clostridium spp.) and facultative (Eubacterium spp., Peptococcus spp., Peptostreptococcus spp., Mobiluncus spp.) anaerobes and facultative airbus - Gardnerella vaginalis.

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

Pharmacokinetics:

Bioavailability of metronidazole for intravaginal administration is 56%. Penetrates into breast milk and most tissues, passes through the placental and blood-brain barrier. Less than 20% binds to plasma proteins. Metabolized in the liver by hydroxylation, oxidation and binding to glucuronic acid. The activity of the main metabolite (2-hydroxymethonidazole) is 30% of the activity of the parent compound.

TS_max is 6-12 hours.

The half-life of metronidazole is about 8 hours.

It is excreted by the kidneys - 40-70% mainly in the form of metabolites (about 20% of the dose in unchanged form).

Indications:

Local treatment of trichomonas vaginitis, bacterial vaginosis and nonspecific vaginitis caused by microorganisms sensitive to metronidazole.

Contraindications:

Hypersensitivity to metronidazole or other derivatives of nitroimidazole; diseases of the blood, leukopenia (including in the anamnesis); violation of coordination of movements, diseases of the central nervous system (including epilepsy); hepatic failure (with appointmentlarge doses); pregnancy (I trimester), lactation period, children under 18 years of age.

Carefully:BVariability (II-III trimesters).

Pregnancy and lactation:

The drug is contraindicated in the first trimester of pregnancy (it penetrates the Placenta), and 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:

Intravaginal in adults.

Trichomonal vaginitis: 1 suppository per day, immediately before bedtime for 7-10 days in combination with taking the drug metronidazole in tablets.

Nonspecific vaginitis, bacterial vaginosis: 1 suppository per day, immediately before bedtime for 7-10 days, if necessary in combination with taking the drug metronidazole in tablets.

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

Preliminarily releasing the suppository from the contour pack using scissors (cut the film along the contour of the suppository), insert it deep into the vagina.

Side effects:

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

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

From the nervous system: headache, dizziness.

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

Allergic reactions: urticaria, itching of the 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:

Overdose is, exceeding the recommended dose, so it is usually not observed when taking the recommended doses. If the recommended dosages are exceeded, the following symptoms: nausea, vomiting, abdominal pain, diarrhea, itching, metallic taste in the mouth, ataxia, dizziness, paresthesia, convulsions, leukopenia, dark staining of urine.

Treatment: symptomatic and supportive therapy, with occasional ingestion - gastric lavage.

Interaction:

When used simultaneously with indirect anticoagulants (for example, warfarin) metronidazole intensifies their action, which leads to an increase in prothrombin time.

It is not recommended to combine with nondepolarizing muscle relaxants (for example, vecuronium bromide).

Similarly to disulfiram, causes intolerance to ethanol.

The simultaneous use of metronidazole with disulfiram can lead to the development of various neurological syndromes (depression of consciousness, development of mental disorders).

Under the influence of barbiturates (for example, phenobarbital) decreases the effectiveness of metronidazole due to the acceleration of its inactivation in the liver.

With simultaneous use with cimetidine, the level of metronidazole in the blood serum can increase and the risk of adverse reactions increases.

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

Special instructions:

When using the drug is recommended 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 treatment period, ethanol intake is contraindicated - it may be intolerant and develop disulfiram-like reactions: abdominal pain of a spastic nature, nausea, vomiting, headache, sudden rush of blood to the face.

With metronidazole, false positive Nelson test results may occurmetronidazole can immobilize treponema).

Having a history of leukopenia associated with influenza or other viral infections is not a contraindication for the use of the drug.

Effect on the ability to drive transp. cf. and fur:Attention should be paid to drivers of vehicles and persons managing other potentially dangerous mechanisms, the possibility of dizziness associated with the use of the drug.

Form release / dosage:

Vaginal suppositories, 500 mg.

Packaging:

5 suppositories per contour cell package.

2 contour squares with instructions for medical use in a pack of cardboard.

Storage conditions:

In a dry, dark place at a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008204/09

Date of registration:16.10.2009 / 20.04.2017

Expiration Date:Unlimited

The owner of the registration certificate:AVEKSIMA, JSC AVEKSIMA, JSC Russia

Manufacturer: & nbsp

FARMAPRIM, LLC The Republic of Moldova

Representation: & nbspAVEKSIMA, JSC AVEKSIMA, JSC Russia

Information update date: & nbsp25.04.2018

Illustrated instructions

Instructions

Metronidazole (Metronidazole)