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

Auxiliary substances: propylene glycol; carbomer (carbopol); propyl parahydroxy benzoate (nipazole, propylparaben); disodium edetate (disodium ethylenediaminetetra acetic acid, trilon B); sodium hydroxide; purified water - up to 100 g.

Description:

Colorless or with a yellowish or yellowish-greenish shade of gel.

Pharmacotherapeutic group:Antimicrobial and antiprotozoal drug

ATX: & nbsp

P.01.A.B Nitroimidazole derivatives

P.01.A.B.01 Metronidazole

Pharmacodynamics:

Antiprotozoal and antimicrobial drug, a derivative of 5-nitroimidazole. 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 (DNA) of a cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active with respect to Trichomonas vaginalis, Gardnerella vaginalis, Giardia intestinalis, Entamoeba histolytica, Lamblia spp., as well as obligate anaerobes Bacteroides spp. (incl. Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella (Prevotella bivia, Prevotella buccae, Prevotella disiens) and some Gram-positive microorganisms (Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp., Mobiluncus spp.). The minimum inhibitory concentration for these strains is 0.125-6.25 μg / ml.

To Metronidazole insensitive aerobic microorganisms.

Pharmacokinetics:

After intravaginal administration, it undergoes systemic absorption (about 56%). The relative bioavailability of the vaginal gel is 2 times higher than the bioavailability of a single dose (500 mg) of vaginal metronidazole tablets.

It penetrates into breast milk and most tissues, passes through the blood-brain barrier and the placenta. The connection with plasma proteins is 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) of the vaginal gel is 6-12 hours.

It is excreted by the kidneys - 60-80% of the dose of the systemic action drug (20% of this quantity in the unchanged form), the intestine - 6-15% of the dose of the systemic action drug.

Indications:

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

Contraindications:

Hypersensitivity (incl.to derivatives of nitroimidazole), leukopenia, disorders of coordination of movements, organic lesions of the central nervous system (including epilepsy), liver failure (in the case of high doses), pregnancy (I trimester), lactation period, and history of leukopenia.

Carefully:

Pregnancy (II-III trimesters).

Dosing and Administration:

Intravaginally recommended dose is 5 g (one complete applicator) 2 times a day (morning and evening). The course of treatment is 5 days.

Side effects:

Allergic reactions: urticaria, skin rash.

Local Reactions: burning sensation or irritation of the penis in the sexual partner, a burning sensation or frequent urination, vulvitis (itching, burning pain or hyperemia of the mucosa in the external genital area).

It is possible to develop systemic effects: changes in taste sensations, including "metallic" smack, dizziness, headache, dry mouth, nausea, vomiting, decreased appetite, abdominal cramps, constipation or diarrhea, dark urine staining, leukopenia or leukocytosis .

After the withdrawal of the drug - the development of candidiasis of the vagina.

Overdose:

Data on overdose are absent.

Interaction:

Similarly to disulfiram, causes intolerance ethanol.

Simultaneous application with disulfiram may lead to the development of various neurological symptoms (should not be prescribed metronidazole patients who took disulfiram in the last 2 weeks).

Strengthens the effect of indirect anticoagulants (warfarin), it is not recommended to combine with nondepolarizing muscle relaxants (vecuronium bromide).

With simultaneous reception with drugs lithium may increase the concentration of the latter in the plasma.

Phenobarbital accelerates the metabolism of metronidazole due to the induction of microsomal liver enzymes; cimetidine - reduces, which can lead to an increase in its concentration in the serum and an increased risk of side effects.

Special instructions:

Only for intravaginal application!

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

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

Form release / dosage:Vaginal gel, 1%.

Packaging:

30 grams per tube aluminum.

Each tube with an applicator for intravaginal administration and instruction for use is placed in a pack of cardboard.

Storage conditions:

In a dry, dark place at a temperature of 15 to 25 ° C. Freezing is not allowed.

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:LSR-000796/09

Date of registration:06.02.2009

Expiration Date:Unlimited

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

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp25.04.2018

Illustrated instructions

Instructions

Metronidazole (Metronidazole)