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Active ingredients
Metronidazole
Release form
Pills
Composition
Metronidazole 250 mg. Adjuvants: corn starch, microcrystalline cellulose, glycerol, povidone, talc, colloidal silicon dioxide, magnesium stearate.
Pharmacological effect
Antimicrobial, antiprotozoal, antibacterial.
Pharmacokinetics
Absorption When taking the drug inside absorption is high. Bioavailability - at least 80%. Cmax in blood plasma ranges from 6 to 40 mcg / ml depending on the dose. Тmax - 1-3 hours. Distribution: It 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, passes through the BBB and placental barrier. Vd for adults is about 0.55 l / kg, for newborns 0.54-0.81 l / kg. Plasma protein binding - 10-20%. Metabolism About 30-60% of the administered dose of metronidazole is metabolized by hydroxylation, oxidation and glucuronidation. The main metabolite (2-hydroxymetronidazole) also has an antiprotozoal and antimicrobial effect. Excretion of T1 / 2 with normal liver function is 8 hours (from 6 to 12 hours). Renal clearance - 10.2 ml / min. 60-80% are excreted by the kidneys (20% - unchanged), 6-15% are excreted through the intestines. The pharmacokinetics in special clinical cases of T1 / 2 for alcoholic liver damage is 18 hours (10 to 29 hours), for newborns born to gestation 28-30 weeks. - about 75 hours, for a period of 32-35 weeks. - 35 hours, for a period of 36-40 weeks. - 25 hours. In cases of marked impaired renal function, patients may experience cumulation of metronidazole in the blood serum after repeated administration of the drug. Therefore, in patients with severe renal failure, the frequency of taking the drug should be reduced. Metronidazole and the main metabolites are quickly removed from the blood during hemodialysis (T1 / 2 is reduced to 2.6 hours). With peritoneal dialysis is displayed in small quantities.
Indications
Protozoal infections: extraintestinal amebiasis, incl. amebic liver abscess, intestinal amebiasis (amoebic dysentery), trichomoniasis (including trichomonas vaginitis, trichomonas urethritis), balantidiasis, giardiasis, cutaneous leishmaniasis; infections caused by Bacteroides spp. (includingBacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides distasonis, Bacteroides vulgatus): infections of bones and joints, infections of the central nervous system (including meningitis, abscess of the brain), bacterial endocarditis, pneumonia, empyema, and abdominal infections, absiema, and abs. 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, infection of the vaginal fornix after surgery), infections of the skin and soft fabrics; 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 radiosensitizing agent in cases when tumor resistance is due to hypoxia in the tumor cells.
Contraindications
Organic lesions of the central nervous system (including epilepsy); liver failure (in the case of the appointment of the drug in high doses); leukopenia (including in history); I trimester of pregnancy; lactation period (breastfeeding); children's age up to 3 years (for this dosage form); hypersensitivity to the drug. With care: II and III trimesters of pregnancy, renal / hepatic failure
Use during pregnancy and lactation
The drug is contraindicated for use in the first trimester of pregnancy and during breastfeeding.
Dosage and administration
Tablets are taken orally during or after a meal (squeezed 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 should also be prescribed metronidazole in the form of vaginal suppositories or pills. 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 aged 2-5 years, the drug is prescribed in a dose of 250 mg / day, at the age of 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. Giardiasis: adults are prescribed 500 mg 2 times / day for 5-7 days.Children over 8 years old - 500 mg / day (in 2 doses), at the age of 5 to 8 years old - 375 mg / day, at the age of 3 and older - 250 mg / day; the daily dose should be divided into 2 doses; The course of treatment is 5 days. The dose of the drug may be 15 mg / kg / day in 3 doses for 5 days. Asymptomatic amebiasis (if a cyst is detected): Adults are given a daily dose of 1-1.5 g (500 mg 2-3 times / day) for 5-7 days. Chronic amebiasis: 1.5 g / day in 3 divided doses for 5-10 days. Acute amebic dysentery: 2.25 g / day in 3 divided doses until symptoms cease. 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 dose of an adult, at the age of 3-7 years - 1/3 doses of an adult, 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 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 doses for 3-4 days before surgery, or once a dose of 1 g in the first day after surgery. 1-2 days after surgery (when oral administration is already allowed) - 750 mg / day for 7 days. In cases of pronounced impaired renal function (CC less than 10 ml / min), the daily dose should be halved.
Side effects
On the part of 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, incoordination, ataxia, confusion, irritability, depression, irritability, weakness, insomnia, headache, convulsions, peripheral neuropathy, hallucinations. On the part of the urinary system: dysuria, cystitis, polyuria, urinary incontinence, urine staining in red-brown color. From the hematopoietic system: neutropenia, leukopenia. Since the cardiovascular system: a decrease in the amplitude of the T wave on the ECG. Allergic reactions: urticaria, skin rash, skin flushing, nasal congestion, fever, arthralgia. Other: candidiasis.
Overdose
Symptoms: nausea, vomiting, ataxia. Treatment: there is no specific antidote. Symptomatic therapy is carried out.
Interaction with other drugs
Enhances the action of oral anticoagulants, which leads to an increase in prothrombin time. 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 adverse reactions. The inducers of enzymes of microsomal oxidation of the liver (phenytoin, phenobarbital) are able to accelerate the elimination of metronidazole, which leads to a decrease in its concentration in blood plasma. When taken simultaneously with lithium preparations, it is possible to increase the concentration of the latter in plasma and the development of symptoms of intoxication. Not recommended in combination with non-depolarizing muscle relaxants (vecuronium bromide). Sulfonamides enhance the antimicrobial action of metronidazole.
special instructions
During treatment, alcohol is contraindicated (a disulfiram-like reaction may develop: spastic abdominal pain, nausea, vomiting, headache, sudden flushing). 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. Metronidazole is able to immobilize treponemas, which leads to a false Nelson test. When treating Trichomonas vaginitis in women and Trichomonas urethritis in men, patients should refrain 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 feces analyzes 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). It paints urine in a dark color. Use in pediatrics In combination with amoxicillin is not recommended for use in children and adolescents under 18 years of age.