Metronidazole pills 250mg №10

Mechanism of action

Anti-protozoan and antimicrobial drug, a derivative of 5-nitroimidazole. The mechanism of action is the biochemical reduction of the 5-nitro group by intracellular transport proteins of anaerobic microorganisms and protozoa. The restored 5-nitro group interacts with the DNA of microbial cells, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active at respect Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis. Giardia intestinalis, Lamblia spp., As well as obligate anaerobes Bacteroidcs spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotamicron, Bacleroides vulgatus), Fusobacterium spp., Veillonela spp., Prevotella (P. bivia, P. buccae, P. bislacterium spp., Vevonela spp., Prevotella (P. bivia, P. buccae, P. bacistora spp., Veillonela spp., Prevotella (P. bivia, P. buccae, P. bacis, Sac. ocerosis, Bacteroides distasonis, Bacteroides distasonis, Bacteroides distasonis) Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.). The minimum inhibitory concentration for these strains is 0.125-6.25 mcg / ml. In combination with Amoxicillin, it is active against Helicobacter pylori (amoxicillin inhibits the development of metronidazole resistance).

To metronidazolenot sensitive aerobic microorganisms and facultative anaerobes, but in the presence of mixed flora (aerobic and anaerobic) metronidazole acts synergistically with antibiotics that are effective against conventional aerobes.

Increases the sensitivity of tumors to radiation, causes sensitization to alcohol (disulfiramopodobnoe action), stimulates reparative processes.

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 and placental barrier. V_d in adults, approximately 0.55 l / kg; in newborns, 0.54–0.81 l / kg. C_max drug in the blood ranges from 6 to 40 μg / ml depending on the dose. Time to reach C_max - 1-3 hours. Plasma protein binding - 10-20%. In the body, about 30-60% of metronidazole is metabolized by hydroxylation, oxidation and glucuronidation. The main metabolite (2-hydroxymetronidazole) also has an antiprotozoal and antimicrobial effect. T_1/2 with normal liver function - 8 hours (from 6 to 12 hours), with alcoholic liver damage - 18 hours (from 10 to 29 hours), for newborns born during gestation 28-30 weeks - about 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 mstronidazole 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 (T_1/2 reduced to 2.6 h). With peritoneal dialysis is displayed in small quantities.

Indications

- protozoal infections: extraintestinal amebiasis, including amebic liver abscess, intestinal amebiasis (amoebic dysentery), trichomoniasis, giardiasis, balantidiasis, cutaneous leishmaniasis, trichomonas vaginitis, trichomonas urethritis;

- infections caused by Bacteroides spp. (including V. fragilis, B. distasonis, B. ovatus, V. thetaiotaomicron, B. vulgalus): infections of bones and joints, infections of the central nervous system (including meningitis, brain abscess), bacterial endocarditis, pneumonia empyema and lung abscess;

- an infection caused by Bacteroides species, including group B. fragilis, species Clostridium, Peptococcus and Peptostreptococcus: abdominal infections (peritonitis, liver abscess), pelvic infections (endometritis, endomyometritis, abscess, fallopian tubes and ovaries, vaginal cuff infections after surgery ) skin and soft tissue infections;

- infections caused by Bacteroides species, including the B. fragilis group and Clostridium species: sepsis;

- pseudomembranous colitis (associated with the use of antibiotics);

- gastritis or duodenal ulcer associated with Helicobacter pylori;

- alcoholism;

- prevention of postoperative complications (especially interventions on the colon, near-rectal area, appendectomy, gynecological surgery);

- radiation therapy of patients with tumors - as a radiosensitizing agent, in cases where the resistance of the tumor is due to hypoxia in the tumor cells.

Dosage and administration

Inside, during or after a meal, (or squeezed milk), not liquid.

Attrichomoniasis - 250 mg 2 times / day for 10 days or 400 mg 2 times / day for 5-8 days. Women need to additionally appoint Metronidazole in the form of vaginal suppositories or tablets.If necessary, you can repeat the treatment or increase the dose to 0.75-1 g / day. Between courses, you should take a break of 3-4 weeks with repeated laboratory tests. An alternative treatment regimen is the appointment of 2 g once a patient and his sexual partner.Children 2-5 years - 250 mg / day;5-10 years - 250-375 mg / day,over 10 years old - 500 mg / day. The daily dose should be divided into 2 doses. The course of treatment is 10 days.

Atgiardiasis - 500 mg 2 times / day for 5-7 days.Children up to 1 year - 125 mg / day,2-4 years - but 250 mg / day,5-8 years - 375 mg / day,over 8 years old - 500 mg / day (in 2 doses). The course of treatment is 5 days.

Atgiardiasis - 15 mg / kg / day in 3 doses for 5 days.

For adults: atasymptomatic amebiasis (if a cyst is detected) the daily dose is 1-1.5 g (500 mg 2-3 times / day) for 5-7 days.

Atchronic amebiasis daily dose - 1.5 g in 3 doses for 5-10 days.

Atacute amebic dysentery - 2.25 g in 3 divided doses until the cessation of symptoms.

Atliver abscess - maximum daily dose - 2.5 g in 1 or 2-3 doses, for 3-5 days, in combination with antibiotics (tetracyclines) and other methods of therapy.Children 1-3 years - 1/4 adult dose3-7 years - 1/3 adult dose,7-10 years - 1/2 dose of an adult.

Atbalantidiasis - 750 mg 3 times / day for 5-6 days.

At ulcerative stomatitis for adults appoint 500 mg 2 times / day for 3-5 days;for children in this case, the drug is not shown.

Atpseudomembranous colitis - 500 mg 3-4 times / day.

ForHelicobacter pylory eradication - 500 mg 3 times / day for 7 days (as part of combination therapy, for example, a combination with amoxicillin 2.25 g / day).

Attreatment of anaerobic infection maximum daily dose of 1.5-2 g.

Attreatment of chronic alcoholism appoint 500 mg / day for a period of up to 6 (not more) months.

For prevention of infectious complications - 750-1500 mg / cy in 3 doses for 3-4 days before surgery, or once 1 g on the 1st day after surgery. 1-2 days after surgery (when oral administration is already allowed) - 750 mg / day for 7 days.

Atpronounced impaired renal function (CC less than 10 ml / min) daily dose should be halved.

Side effect

Gastrointestinal: diarrhea, anorexia, nausea, vomiting, intestinal colic, constipation, metallic taste in the mouth, dry mouth, glossitis, stomatitis, pancreatitis.

Nervous system: dizziness, incoordination, ataxia, confusion, irritability, depression, irritability, weakness, insomnia, headache, convulsions,hallucinations, peripheral neuropathy.

Allergic reactions: urticaria, skin rash, skin flushing, nasal congestion, fever, arthralgia.

From the genitourinary system: dysuria, cystitis, polyuria, urinary incontinence, candidiasis, urine staining in red-brown color.

Other: neutropenia, leukopenia, flattening of the T wave on the ECG.

Contraindications

- leukopenia (including in 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 period;

- increased sensitivity.

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

Use during pregnancy and lactation

Contraindicated in the first trimester of pregnancy and lactation. With care to apply in II and III trimesters of pregnancy.

Application for violations of the liver

Contraindicated in liver failure (in the case of the appointment of large doses).

Be wary prescribed for abnormal liver function, liver failure.

Application for violations of kidney function

Be wary appointed with renal failure.

In cases of pronounced impaired renal function (CC less than 10 ml / min), the daily dose should be halved.

Use in children

Inside, during or after a meal, (or squeezed milk), not liquid.

Attrichomoniasis children 2-5 years old - 250 mg / day;5-10 years - 250-375 mg / day,over 10 years old - 500 mg / day. The daily dose should be divided into 2 doses. The course of treatment is 10 days.

Atgiardiasis - children under 1 year - 125 mg / day,2-4 years - but 250 mg / day,5-8 years - 375 mg / day,over 8 years old - 500 mg / day (in 2 doses). The course of treatment is 5 days.

Atliver abscess - children 1-3 years old - 1/4 adult dose3-7 years - 1/3 adult dose,7-10 years - 1/2 dose of an adult.

Atulcerative stomatitis for children drug is not shown.

special instructions

Ethanol is contraindicated during the treatment period (a disulfiram-like reaction may develop: spastic abdominal pain, nausea, vomiting, headache, sudden flushing).

In combination with amoxicillin is not recommended for use in patients younger than 18 years.

With prolonged therapy, it is necessary to control the blood picture.

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.

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. Necessarily simultaneous treatment of sexual partners. The treatment does not stop during menstruation. After treatment of trichomoniasis, control tests should be carried out during three regular cycles before and after menstruation.

After giardiasis treatment, if symptoms persist, after 3–4 weeks to perform 3 stool tests at intervals of several days (in some successfully treated patients, lactose intolerance caused by invasion may persist for several weeks or months, recalling the symptoms of giardiasis).

Drug interaction

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

Similar to disulfiram, it causes intolerance to ethanol.

Simultaneous use with disulfiram can lead to the development of various neurological symptoms (the interval between administration 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 drugs that stimulate the enzymes of microsomal oxidation in the liver (phenobarbital, phenytoin), can accelerate the elimination of metronidazole, resulting in a decrease in its concentration in plasma.

When taken simultaneously with lithium preparations, 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.

Terms and conditions of storage

List B. The drug is stored in a dry, dark place, out of reach of children, at a temperature not higher than 25 ° C. It is recommended to use until the time specified on the package.

Pharmacy sales terms

The drug is available on prescription.