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METRONIDAZOLE 50 tablets / МЕТРОНИДАЗОЛ - 50 таблеток
Pharmachologic effect
Antiprotozoal and antimicrobial drug derived from 5-nitroimidazole. The mechanism of action consists in the biochemical reduction of the 5-nitro group by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group interacts with the DNA of the cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.
Active against 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 thetaiotaomicron, Bacleroides vulgatus), Fusobacterium spp., Veillonela spp., Prevotella (P.bivia, P.buccae, microorganisms and P..dismpos) Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.). The minimum inhibitory concentration for these strains is 0.125-6.25 μg / ml. In combination with amoxicillin, it is active against Helicobacter pylori (amoxicillin inhibits the development of resistance to metronidazole).
Aerobic microorganisms and facultative anaerobes are not sensitive to metronidazole, but in the presence of mixed flora (aerobes and anaerobes), metronidazole acts synergistically with antibiotics that are effective against conventional aerobes.
Increases the sensitivity of tumors to radiation, causes sensitization to alcohol (disulfiram-like action), stimulates reparative processes.
Pharmacokinetics
Absorption - high (bioavailability at least 80%). Possesses high penetrating ability, reaching bactericidal concentrations in most tissues and body fluids, including lungs, kidneys, liver, skin, cerebrospinal fluid, brain, bile, saliva, amniotic fluid, abscess cavities, vaginal secretions, semen, breast milk, penetrates through blood-brain and placental barrier. Vd in adults is about 0.55 l / kg, in newborns - 0.54-0.81 l / kg. Cmax of the drug in the blood ranges from 6 to 40 μg / ml, depending on the dose. Time to reach Cmax - 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-oxymetronidazole) also has antiprotozoal and antimicrobial effects. T1 / 2 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 with a gestational age of 28-30 weeks - about 75 hours, 32 35 weeks - 35 hours, 36-40 weeks - 25 hours. Excreted by the kidneys 60-80% (20% unchanged), through the intestines - 6-15%. Renal clearance - 10.2 ml / min.
In patients with impaired renal function, after repeated administration, accumulation of mstronidazole in the blood serum may be observed (therefore, in patients with severe renal insufficiency, the frequency of administration should be reduced).
Metronidazole and the main metabolites are rapidly removed from the blood during hemodialysis (T1 / 2 is reduced to 2.6 hours). With peritoneal dialysis, it is excreted in small quantities.
Indications for Metronidazole
- protozoal infections: extraintestinal amebiasis, including amoebic liver abscess, intestinal amebiasis (amoebic dysentery), trichomoniasis, giardiasis, balantidiasis, cutaneous leishmaniasis, trichomonas vaginitis, trichomonas urethritis;
- infections caused by Bacteroides spp. (including B. fragilis, B. distasonis, B. ovatus, B. 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;
- infections caused by Bacteroides species, including the B. fragilis group, Clostridium, Peptococcus and Peptostreptococcus species: infections of the abdominal cavity (peritonitis, liver abscess), infections of the pelvic organs (endometritis, endomyometritis, abscess of the fallopian tubes and ovaries, infections of the vaginal vault after surgery) , infections of the skin and soft tissues;
- 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 region, appendectomy, gynecological operations);
- radiation therapy for patients with tumors - as a radiosensitizing agent, in cases where tumor resistance is due to hypoxia in tumor cells.
Dosage regimen
Inside, during or after meals, (or with milk), without chewing.
With trichomoniasis - 250 mg 2 times / day for 10 days or 400 mg 2 times / day for 5-8 days. Women need to additionally prescribe Metronidazole in the form of vaginal suppositories or tablets. If necessary, you can repeat the course of treatment or increase the dose to 0.75-1 g / day. Between courses, you should take a break of 3-4 weeks with repeated control laboratory tests. An alternative therapy regimen is the appointment of 2 g once to the patient and his sexual partner. Children 2-5 years old - 250 mg / day; 5-10 years old - 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.
With giardiasis - 500 mg 2 times / day for 5-7 days. Children under 1 year old - 125 mg / day, 2-4 years old - but 250 mg / day, 5-8 years old - 375 mg / day, over 8 years old - 500 mg / day (in 2 divided doses). The course of treatment is 5 days.
With giardiasis - 15 mg / kg / day in 3 doses for 5 days.
Adults: with asymptomatic amebiasis (if a cyst is detected), the daily dose is 1-1.5 g (500 mg 2-3 times / day) for 5-7 days.
In chronic amebiasis, the daily dose is 1.5 g in 3 divided doses for 5-10 days.
In acute amoebic dysentery - 2.25 g in 3 divided doses until symptoms stop.
With liver abscess - the maximum daily dose is 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 old - 1/4 adult dose, 3-7 years old - 1/3 adult dose, 7-10 years old - 1/2 adult dose.
With balantidiasis - 750 mg 3 times / day for 5-6 days.
For ulcerative stomatitis, adults are prescribed 500 mg 2 times / day for 3-5 days; in this case, the drug is not indicated for children.
With pseudomembranous colitis - 500 mg 3-4 times / day.
For the eradication of Helicobacter pylory - 500 mg 3 times / day for 7 days (as part of a combination therapy, for example, a combination with amoxicillin 2.25 g / day).
In the treatment of anaerobic infection, the maximum daily dose is -1.5-2 g.
In the treatment of chronic alcoholism, 500 mg / day is prescribed for a period of up to 6 (no more) months.
For the prevention of infectious complications - 750-1500 mg / cyt in 3 doses 3-4 days before the operation, or once 1 g on the 1st day after the operation. 1-2 days after surgery (when oral administration is already allowed) - 750 mg / day for 7 days.
In severe renal impairment (CC less than 10 ml / min), the daily dose should be halved.
Side effect
From the digestive system: diarrhea, anorexia, nausea, vomiting, intestinal colic, constipation, metallic taste in the mouth, dry mouth, glossitis, stomatitis, pancreatitis.
From the nervous system: dizziness, impaired coordination of movements, 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, red-brown urine staining.
Others: neutropenia, leukopenia, flattening of the T wave on the ECG.
Contraindications for use
leukopenia (including history);
organic lesions of the central nervous system (including epilepsy);
hepatic impairment (in the case of the appointment of large doses);
pregnancy (I trimester);
lactation period;
hypersensitivity.
With caution - pregnancy (II, III trimesters), renal / hepatic failure.
Application during pregnancy and lactation
Contraindicated in the first trimester of pregnancy and lactation. Use with caution in the II and III trimesters of pregnancy.
Application for violations of liver function
Contraindicated in liver failure (in the case of large doses).
It is prescribed with caution for violations of liver function, liver failure.
Application for impaired renal function
Prescribed with caution in renal failure.
In case of severe renal impairment (CC less than 10 ml / min), the daily dose should be halved.
Application in children
Inside, during or after meals, (or with milk), without chewing.
With trichomoniasis, children 2-5 years old - 250 mg / day; 5-10 years old - 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.
With giardiasis - children under 1 year old - 125 mg / day, 2-4 years old - but 250 mg / day, 5-8 years old - 375 mg / day, over 8 years old - 500 mg / day (in 2 doses) ... The course of treatment is 5 days.
With liver abscess - children 1-3 years old - 1/4 adult dose, 3-7 years old - 1/3 adult dose, 7-10 years old - 1/2 adult dose.
In case of ulcerative stomatitis, the drug is not indicated for children.
Special instructions
During the period of treatment, ethanol is contraindicated (a disulfiram-like reaction may develop: spastic abdominal pain, nausea, vomiting, headache, sudden flush of blood to the face).
In combination with amoxicillin, it is not recommended for use in patients under 18 years of age.
With prolonged therapy, it is necessary to control the blood picture.
With 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.
May immobilize treponemas and lead to false positive Nelson's test.
Stains urine dark.
When treating Trichomonas vaginitis in women and Trichomonas urethritis in men, it is necessary to abstain from sexual activity. Simultaneous treatment of sexual partners is mandatory. Treatment does not stop during menstruation. After trichomoniasis therapy, control tests should be carried out for three successive cycles before and after menstruation.
After treatment of giardiasis, if symptoms persist, after 3-4 weeks, conduct 3 fecal analyzes at intervals of several days (in some successfully treated patients, lactose intolerance caused by invasion may persist for several weeks or months, resembling the symptoms of giardiasis).
Drug interactions
Enhances the action of indirect anticoagulants, which leads to an increase in the time of prothrombin formation.
Similar to disulfiram, it causes intolerance to ethanol.
Simultaneous use with disulfiram can lead to the development of various neurological symptoms (the interval between appointments is at least 2 weeks).
Cimetidine inhibits the metabolism of metronidazole, which can lead to an increase in its concentration in the blood serum and an increased risk of side effects.
The simultaneous administration of drugs that stimulate enzymes of microsomal oxidation in the liver (phenobarbital, phenytoin) can accelerate the elimination of metronidazole, as a result of which its concentration in plasma decreases.
When taken simultaneously with lithium preparations, the concentration of the latter in the plasma may increase and the development of symptoms of intoxication.
It is not recommended to combine with non-depolarizing muscle relaxants (vecuronium bromide).
Sulfonamides enhance the antimicrobial effect of metronidazole.
Storage conditions of the drug Metronidazole
List B. The drug is stored in a dry, dark place, out of the reach of children, at a temperature not exceeding 25 ° C.
Shelf life of the drug Metronidazole
Shelf life is 2 years. It is recommended to use before the expiration date indicated on the package.
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