Metronidazole pills 250mg №20

Tradename:

Metronidazole.

International non-proprietary name:

Metronidazole / Metronidazole.

Dosage Form:

250 mg tablets.

Description:

tablets of white with a greenish-yellow shade of color, flat-cylindrical, with riska and a facet.

Composition:

each pill contains: the active substance - metronidazole - 250 mg; excipients - talc, stearic acid, polyvinyl alcohol, potato starch.

Pharmacotherapeutic group:

Antimicrobial agents for systemic use.

Pharmacological properties

Pharmacodynamics

Anti-protozoan and antibacterial drug derived from 5-nitro-imidazole. The mechanism of action is the biochemical reduction of the 5-nitro group of metronidazole with intracellular transport proteins of anaerobic microorganisms and protozoa. The recovered 5-nitro group of metronidazole interacts with the microbial cell DNA, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

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 MIC for these strains is 0.125 - 6.25 mcg / ml.

It is active against Helicobacter pylori (however, in 40% of cases, the presence of metronidazole-resistant strains is possible).

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

Increases the sensitivity of tumors to radiation, causes disulfiram-like reactions

Pharmacokinetics

Absorption - high (bioavailability of at least 80%). It has a high penetrating ability, reaching bactericidal concentrations in most tissues and body fluids, including lungs, kidneys, liver, skin, cerebrospinal fluid, brain, bile, saliva, amniotic fluid, abscesses, vaginal secretions, seminal fluid, breast milk, passes through blood-brain barrier and placental barrier. The volume of distribution: adults - about 0.55 l / kg, newborns - 0.54 - 0.81 l / kg.

Cmax ranges from 6 to 40 mcg / ml, depending on the dose, and is achieved in 1–3 h. Communication with plasma proteins is 10–20%.

Metabolized ≈ 30 - 60% of metronidazole by hydroxylation, oxidation and glucuronidation. The main metabolite (2-hydroxymetronidazole) also has an antiprotozoal and antimicrobial effect.

T½ with normal liver function - 8 hours (from 6 to 12 hours), with alcoholic liver damage - 18 hours (from 10 to 29 hours), in newborns: born during the gestation period - 28 - 30 weeks - approximately 75 hours, 32 - 35 weeks - 35 hours, 36 - 40 weeks - 25 hours. 60 - 80% (20% unchanged) are excreted by the kidneys, 6 - 15% through the intestines.

Renal clearance - 10.2 ml / min. In patients with impaired renal function, after repeated administration, cumulation of metronidazole in serum may be observed (therefore, in patients with severe renal insufficiency, the frequency of administration should be reduced).

Metronidazole and the major metabolites are rapidly removed from the blood during hemodialysis (T1 / 2 is reduced to 2.6 hours). With peritoneal dialysis is displayed in small quantities.

Indications for use

In order to avoid the development of resistance of microorganisms, metronidazole should be used only for the treatment of infections caused by metronidazole-sensitive strains (according to material microbiological research or epidemiological data).

Clinical symptoms of trichomoniasis - in women and men in the case of laboratory confirmation of the diagnosis (smear and / or culture).

Asymptomatic trichomoniasis - in women with endocervicitis, cervicitis, or cervical erosion. Since the presence of Trichomonas can interfere with an accurate assessment of cytological smears, additional smears should be performed after parasite eradication.

Treatment of a spouse without clinical manifestations. Partners without symptoms should be treated at the same time in order to prevent re-infection. The decision on the treatment of a male partner without clinical manifestations, in which Trichomonas are not found (or the analysis was not performed), is taken by a doctor. When re-infection spouses must be treated with metronidazole at the same time.

Amebiasis. Treatment of acute intestinal amebiasis (amoebic dysentery) and liver abscess caused by amoebae (including aspiration or drainage of abscess).

Anaerobic bacterial infections, including infections caused by Bacteroides, including the species B. fragilis (B. fragilis, B. diastasonis, B.ovatus, B.thetalotaomicron, B. vulgatus), Clostridium spp., Eubacterium spp., Peptococcus niger and Peptostreptococcus. Treatment of severe infections caused by sensitive anaerobic bacteria in combination with surgical treatment. In the case of mixed aerobic and anaerobic infections, antibacterial agents that are active against aerobic bacteria are additionally used.

Infections of the skin and appendages caused by Bacteroides (including B. fragilis), Slostridium spp., Peptococcus niger, Peptostreptococcus spp. and Fusobacterium spp.

Gynecological infections, including endometritis, endomyometritis, tubo-ovarian abscess and infections after gynecological operations caused by Bacteroides (including B. fragilis), Slostridium spp., Peptococcus niger, Peptostreptococcus spp.

Bacterial septicemia caused by Bacteroides (including B. fragilis), Slostridium spp.

Infections of bones and joints caused by Bacteroides species (including B. fragilis), as an additional therapy.

Central nervous system infections, including meningitis and brain abscess, lower respiratory tract infections, including pneumonia, empyema and lung abscess; endocarditis caused by Bacteroides (including B. fragilis).

Contraindications

Hypersensitivity, leukopenia (including a history), organic lesions of the central nervous system (including epilepsy), liver failure (in the case of the appointment of large doses), pregnancy (I term), lactation; children's age (up to 3 years).

Carefully

Pregnancy (II - III trimesters), renal / hepatic failure.

Method of application and dosing regimen

Is taken orally, during or after a meal (or squeezed milk), without chewing.

Trichomoniasis in women and men. The course of treatment is chosen individually.

A one-day course of treatment is 2 grams (8 tablets) as a single dose or separately into two doses of 1 gram (4 tablets) 2 times a day. Day treatment is indicated in cases where there is an assumption that the patient cannot accurately follow the treatment regimen;

The seven-day course of treatment is 250 mg (½ tablet) three times a day for seven days. The cure rate may be higher after a seven-day course of treatment.

Pregnant women taking metronidazole during the first trimester of pregnancy is contraindicated. Conducting a daily course of therapy for pregnant women is contraindicated, since it leads to a high concentration of metronidazole in the blood plasma and can penetrate into the fetus.

With repeated courses of treatment with metronidazole, it is recommended to take a break in 4 - 6 weeks. Before and after these courses, you must perform a blood test for the total number of leukocytes and leukocyte formula.

Amebiasis.

Adults: with intestinal amoebiasis 750 mg (1½ tablets) by mouth three times a day for 5-10 days; with liver abscess 500 mg or 750 mg three times a day for 5 to 10 days. Children: daily dose of 35-50 mg / kg, divided into three orally for 10 days.

For the treatment of severe anaerobic bacterial infections, metronidazole is prescribed at the initial stage. The usual dose for adults is 7.5 mg / kg every six hours by mouth (about 500 mg for a patient weighing 70 kg). The maximum daily dose of 4 g. The duration of treatment from 7 to 10 days (treatment of infections of bones and joints, lower respiratory tract and endocardium may be longer).

In elderly patients, the pharmacodynamics of metronidazole can be changed, monitoring of serum metronidazole is necessary to adjust the dose.

In patients with severe liver disease, cumulation of metronidazole is possible and its doses should be reduced. A careful monitoring of plasma levels of metronidazole and signs of toxicity is recommended. Anuria does not require a dose reduction, since metronidazole and its metabolites are excreted by dialysis.

Side effect

Serious reactions: seizures, encephalopathy, aseptic meningitis , optic and peripheral neuropathy (with numbness or paresthesia of the extremities). If you experience any neurological symptoms, you must stop taking metronidazole and immediately consult a doctor.

Frequent adverse reactions: gastrointestinal disorders (nausea in 12% of patients, vomiting, anorexia, diarrhea, epigastric discomfort, abdominal cramping, constipation) headache.

The following side reactions are also possible:

Oral cavity: a sharp, unpleasant metallic taste in the mouth, a feeling of "unevenness" of the tongue, glossitis, stomatitis. These symptoms may be associated with the growth of Candida fungi during therapy.

Hemopoietic disorders: reversible neutropenia (leukopenia); persistent thrombocytopenia.

Cardiovascular disorders: flattening of the T-wave on the ECG.

Central nervous system disorders: encephalopathy,aseptic meningitis, seizures, optic neuropathy, peripheral neuropathy, dizziness, incoordination, ataxia, confusion, dysarthria, irritability, depression, weakness, insomnia.

Hypersensitivity: urticaria, erythematous rash, Stephen-Johnson syndrome, toxic epidermal necrolysis, hot flashes, nasal congestion, dry mouth (vagina or vulva), fever.

Impaired renal function: dysuria, cystitis, polyuria, urinary incontinence, a feeling of tension in the pelvic region. Dark color of urine, probably due to a metabolite (frequency: 1 case out of 100,000).

Others: the growth of Candida fungi in the vagina, dyspareunia, decreased libido, proctitis and short-term joint pain. If you drink alcoholic beverages with metronidazole, abdominal pain, nausea, vomiting, redness of the skin or headache are possible. It is possible to change the taste of alcoholic beverages, rarely - the development of pancreatitis.

In experiments on rats and mice, metronidazole had a carcinogenic effect. In patients with Crohn's disease, gastrointestinal cancer and other variants of extraintestinal cancer may develop (breast and colon cancers may develop when using metronidazole in high doses for a long period of time). Metronidazole is not recommended for use in patients with Crohn's disease.

Drug interaction

It enhances the effect of indirect anticoagulants, which leads to an increase in prothrombin time.

Similarly, disulfiram causes intolerance to ethanol.

Simultaneous use with disulfiram can lead to the development of various neurological symptoms (the interval between doses is at least 2 weeks).

Cimetidine inhibits the metabolism of metronidazole, which can lead to an increase in its concentration in serum and an increase in the risk of side effects.

The simultaneous appointment of microsomal oxidative stimulating agents (phenobarbital, phenytoin) can accelerate the elimination of metronidazole and reduce its concentration in plasma.

When taken simultaneously with lithium preparations (Li +), the concentration of the latter in plasma and the development of symptoms of intoxication may increase.

It is not recommended to combine with non-depolarizing muscle relaxants (vecuronium bromide).

Sulfonamides enhance the antimicrobial action of metronidazole.

special instructions

During treatment, ethanol use is contraindicated (disulfiram-like reactions may develop: abdominal pain of a spastic nature, nausea, vomiting, headache, sudden flushes of blood to the face).

With prolonged therapy, it is necessary to control the picture of peripheral blood. In case of leukopenia, the possibility of continuing treatment depends on the risk of developing an infectious process.

The appearance of ataxia, dizziness, and any other deterioration in the neurological status of patients requires discontinuation of treatment.

It can immobilize treponema and lead to a false-positive Nelson test.

Metronidazole may affect the determination of such biochemical parameters as aspartate aminotransferase (AST), alanine aminotransferase (ALT), lactate dehydrogenase (LDH), triglycerides, glucose hexokinase.

It paints urine in a dark color.

When treating Trichomonas vaginitis in women and Trichomonas urethritis in men, it is necessary to abstain from sex. After therapy, control tests should be carried out for 3 regular cycles before and after menstruation.

Use during pregnancy during lactation

Acceptance of metronidazole during the first trimester of pregnancy is contraindicated. In II - III trimesters, if necessary, metronidazole can be appointed taking into account the benefit / risk. Metronidazole has a teratogenic effect, penetrates the placental barrier and quickly enters the bloodstream of the fetus. Adequate and well-controlled studies in pregnant women have not been conducted. Due to the fact that metronidazole has carcinogenicity in rodents, this tool can be used during pregnancy only if absolutely necessary.

The use of metronidazole for treating trichomoniasis during pregnancy should be limited to cases in which alternative treatment is ineffective.

If necessary, the appointment of metronidazole during lactation should stop breastfeeding. Metronidazole is secreted into human milk at concentrations corresponding to those found in plasma.

Influence on ability to steer the car and potentially dangerous mechanisms

You may develop vertigo, confusion, hallucinations or convulsions associated with taking this drug, which disrupts operator activity.

Overdose

Symptoms: nausea, vomiting, ataxia; when taken as a radiosensitizing agent - convulsions, peripheral neuropathy.

Treatment: no specific antidote, symptomatic and supportive therapy.

Storage conditions

In the place protected from light and moisture, at a temperature not higher than 25 ° C. Keep out of the reach of children.