Composition, form of production and packaging
Tablets are white or white with a yellowish-greenish to light yellow with a greenish tinge color, flat-cylindrical, with a facet on both sides and a risk on one side.
1 tab.
metronidazole 250 mg
Excipients: corn starch, microcrystalline cellulose, glycerol, povidone, talc, silicon dioxide colloid, magnesium stearate.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
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 restored 5-nitro group of metronidazole interacts with the DNA of a cell of microorganisms, inhibiting the synthesis of nucleic acids, which leads to the death of microorganisms.
It is active against Trichomonas vaginalis, Entamoeba hystolitica, Gardnerella vaginalis, Giardia intestinalis, and obligate anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides distasonis, 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.). The MIC for these strains is 0.125 Ојg / ml. In combination with amoxicillin shows activity against Helicobacter pylori (amoxicillin suppresses the development of resistance to metronidazole).
Metronidazole is insensitive to aerobic microorganisms and facultative anaerobes, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against conventional aerobes.
Increases the sensitivity of tumors to radiation, causes disulfiram-like reactions, stimulates reparative processes.
PHARMACOKINETICS
Suction
When you take the drug inside the absorption is high. Bioavailability - not less than 80%. C max in blood plasma is from 6 to 40 Ојg / ml, depending on the dose. Tmax is 1-3 hours.
Distribution
Has a high penetrating ability, reaching bactericidal concentrations in most tissues and body fluids, including. in the lungs, kidneys, liver, skin, cerebrospinal fluid, brain, bile, saliva, amniotic fluid, abscess cavity, vaginal secretions, seminal fluid, breast milk, penetrates the BBB and the placental barrier.
V d for adults is approximately 0.55 l / kg, for newborns 0.54-0.81 l / kg. Binding to plasma proteins - 10-20%.
Metabolism
About 30-60% of the administered dose of metronidazole is metabolized by hydroxylation, oxidation and glucuronidation. The main metabolite (2-oxymetronidazole) also has antiprotozoal and antimicrobial effects.
Excretion
T 1/2 with normal liver function - 8 hours (6 to 12 hours). Kidney clearance - 10.2 ml / min. It is excreted by the kidneys 60-80% (20% - unchanged), 6-15% is excreted through the intestine.
Pharmacokinetics in special clinical cases
T 1/2 for alcoholic liver damage - 18 hours (from 10 to 29 hours), in newborns born at the gestational age of 28-30 weeks. - approximately 75 hours, at a time of 32-35 weeks. - 35 hours, at a period of 36-40 weeks. - 25 hours.
With severe renal dysfunction, metronidazole cumulation in serum can be observed after repeated administration of the drug. Therefore, in patients with severe renal insufficiency, the frequency of drug intake should be reduced.
Metronidazole and major metabolites are rapidly removed from the blood during hemodialysis (T 1/2 is reduced to 2.6 h). When peritoneal dialysis is withdrawn in small quantities.
INDICATIONS
- protozoal infections: extraintestinal amoebiasis, incl. amoebic liver abscess, intestinal amoebiasis (amoebic dysentery), trichomoniasis (including trichomonas vaginitis, trichomoniasis urethritis), balantidiasis, giardiasis, cutaneous leishmaniasis;
- infections caused by Bacteroides spp. (including Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides distasonis, Bacteroides vulgatus): 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 Clostridium spp., Peptococcus spp., Peptostreptococcus spp .: infections of the abdominal cavity (peritonitis, liver abscess), infections of the pelvic organs (endometritis, abscess of the fallopian tubes and ovaries, vaginal vaginal infection after surgery), skin infections and soft tissues;
- pseudomembranous colitis (associated with the use of antibiotics);
- gastritis or duodenal ulcer associated with Helicobacter pylori;
- prevention of postoperative complications (especially after interventions on the colon, near-rectal area, appendectomy, and after gynecological operations);
- Radiation therapy of patients with tumors - as a radiosensitizer in cases where tumor resistance is due to hypoxia in tumor cells.
DOSING MODE
The drug is taken orally during or after a meal (with milk), without chewing.
Trichomoniasis: adults are prescribed 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 course of treatment or increase the dose to 0.75-1 g / day. Between the courses should be a break in 3-4 weeks with the conduct of repeated control laboratory tests.
An alternative scheme of therapy is the appointment of 2 g once to the patient and his sexual partner.
Children aged 2-5 years, the drug is prescribed at a dose of 250 mg / day, at the age of 5-10 years - 250-375 mg / day; over 10 years - 500 mg / day. The daily dose should be divided into 2 divided doses. The course of treatment is 10 days.
Giardiasis: adults are prescribed 500 mg 2 times / day for 5-7 days.
Children older than 8 years - 500 mg / day (in 2 divided doses), at the age from 5 to 8 years - 375 mg / day, at the age of 3 years and older - 250 mg / day; the daily dose should be divided into 2 divided doses; course of treatment - 5 days. The dose of the drug can be 15 mg / kg / day in 3 divided doses for 5 days.
Asymptomatic amebiasis (if cyst is detected): adults are prescribed in a daily dose of 1-1.5 g (500 mg 2-3 times / day) for 5-7 days.
Chronic amoebiasis: 1.5 g / day in 3 divided doses for 5-10 days.
Acute amoebic dysentery: 2.25 g / day in 3 divided doses before the symptoms stop.
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 as part of complex therapy.
Children from 3 years old - 1/4 of the adult dose, at the age of 3-7 years - 1/3 of the adult dose, at the age of 7-10 years - 1/2 dose of an adult.
Balantidiasis: 750 mg 3 times / day for 5-6 days.
Ulcerative stomatitis: adults are prescribed 500 mg 2 times / day for 3-5 days. Children in this case, the drug is not shown.
Pseudomembranous colitis: 500 mg 3-4 times / day.
For the eradication of Helicobacter pylori: 500 mg 3 times / day for 7 days (as part of combination therapy, for example, in combination with amoxicillin 2.25 g / day).
Treatment of anaerobic infection: the maximum daily dose is 1.5-2 g.
Treatment of chronic alcoholism: prescribed in a dose of 500 mg / day for a period of up to 6 (not more) months.
For the prevention of infectious complications: 750-1500 mg / day in 3 divided doses 3-4 days before surgery, or once a dose of 1 g in the first day after the operation.In 1-2 days after the operation (when already allowed ingestion) - 750 mg / day for 7 days.
In severe renal dysfunction (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, dry mouth, "metallic" taste in the mouth, glossitis, stomatitis, pancreatitis.
From the side of the central nervous system and peripheral nervous system: dizziness, impaired coordination of movements, ataxia, confusion, irritability, depression, increased excitability, weakness, insomnia, headache, convulsions, peripheral neuropathy, hallucinations.
From the urinary system: dysuria, cystitis, polyuria, urinary incontinence, urine staining in red-brown color.
From the hemopoietic system: neutropenia, leukopenia.
From the cardiovascular system: a decrease in the amplitude of the T wave on the ECG.
Allergic reactions: urticaria, skin rash, skin hyperemia, nasal congestion, fever, arthralgia.
Other: Candidiasis.
CONTRAINDICATIONS
- organic lesions of the central nervous system (including epilepsy);
- hepatic insufficiency (in case of prescribing the drug in high doses);
- Lakopenia (including in the anamnesis);
- I trimester of pregnancy;
- the period of lactation (breastfeeding);
- Children under 3 years of age (for this dosage form);
- Hypersensitivity to the components of the drug.
With caution: II and III trimesters of pregnancy, renal / hepatic impairment
PREGNANCY AND LACTATION
The drug is contraindicated for use in the first trimester of pregnancy and during breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
Data on the use of the drug in patients with impaired renal function are not provided.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
When violations of liver function, metabolism of metronidazole slows down, which leads to cumulation of the drug in the body. In these cases, the dose of the drug should be reduced.
APPLICATION FOR CHILDREN
With giardiasis :
Children under the age of 1 year at 125 mg / day (1/2 tablets), children between 2 and 4 years of age at 250 mg / day (1 tab.), Children aged 5 to 8 years 375 mg / day (1 1/2 tablets), children over the age of 8 years 500 mg / day (1 tablet 2 times / day) after eating for 5 days.
With amoebiasis :
Children aged 7 to 10 years are prescribed a dose equal to half the dose for adults, children aged 3 to 7 years - one third of the dose for adults, children aged 1 to 3 years - a quarter of the dose for adults.
Children with gangrenous stomatitis use Clion is not shown.
APPLICATION IN ELDERLY PATIENTS
There is no data on the use of the drug in elderly patients.
SPECIAL INSTRUCTIONS
During the period of treatment, alcohol use is contraindicated (it is possible to develop a disulfiram-like reaction: spasmodic abdominal pain, nausea, vomiting, headache, sudden rush of blood to the face).
With prolonged therapy, it is necessary to monitor 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.
Metronidazole is able to immobilize treponema, which leads to Nelson's false test.
In the treatment of trichomonas vaginitis in women and trichomoniasis in men, patients should abstain from sexual activity. It is necessary to simultaneously treat sexual partners. Treatment does not stop during menstruation. After trichomoniasis therapy, control tests should be performed for three consecutive cycles before and after menstruation.
After treatment of lambliasis, if symptoms persist, after 3 to 4 weeks, 3 feces should be analyzed at intervals of several days (in some successfully treated patients lactose intolerance caused by invasion can persist for several weeks or months, recalling the symptoms of giardiasis).
Stains urine in a dark color.
Use in Pediatrics
In combination with amoxicillin it is not recommended to use in children and adolescents under 18 years of age .
OVERDOSE
Symptoms: nausea, vomiting, ataxia.
Treatment: there is no specific antidote. Symptomatic therapy is performed.
DRUG INTERACTION
Strengthens the effect of oral anticoagulants, which leads to an increase in prothrombin time.
Similarly to disulfiram, causes intolerance to ethanol. Simultaneous use with disulfiram can lead to the development of various neurologic symptoms (the interval between appointments is at least 2 weeks).
Cimetidine inhibits metronidazole metabolism, which can lead to an increase in serum concentrations and an increased risk of adverse reactions.
Inducers of microsomal liver oxidation enzymes (phenytoin, phenobarbital) can accelerate the elimination of metronidazole, which leads to a decrease in its concentration in the blood plasma.
With simultaneous administration with lithium preparations, an increase in plasma concentration in the plasma and the development of symptoms of intoxication are possible.
It is not recommended to use in combination with nondepolarizing muscle relaxants (vecuronium bromide).
Sulfonamides increase the antimicrobial effect of metronidazole.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, protected from light at a temperature of 15 В° to 30 В° C. Shelf life - 5 years.
