metronidazole (Metronidazole)
Russian Name: Metronidazole
Latin name: Metronidazole
Chemical name: 2-Methyl-5-nitro-1H-imidazole-1-ethanol
Gross-formula: C6H9N3O3
Code CAS: 443-48-1
Characterization
White or slightly greenish crystalline powder. It is soluble in water and insoluble in alcohol.
Pharmacology
Mode of action - antibacterial, protivoprotozoynoe, trihomonatsidnoe, antiulcer, antialcoholic. Nitro group of the molecule, an electron acceptor, embedded in the respiratory chain of the simplest and anaerobes (competes with elektrontransportiruyuschimi proteins - Flavoprotein, etc.) that violate the respiratory processes and causes cell death. In addition, some species of anaerobic bacteria has the ability to suppress the synthesis of the DNA and induce its degradation.
Once inside quickly and completely absorbed from the gastrointestinal tract (bioavailability nearly 100%). Cmax achieved within 1-2 h and from 6 to 40 mg / ml depending on the dose. Protein binding of plasma small - less than 20%. Well into the tissues and body fluids, creating a bactericidal concentration in saliva, semen, vaginal secretions, penetrates the BBB and placental barrier, is secreted in breast milk. Repeated receptions cumulating. Biotransformation in the liver by oxidation of the side chain and conjugation with glucuronic acid with the formation of inactive and active - 2-hydroxymethyl-metabolites. Excreted by the kidneys (60-80% of applied dose) and intestine (6-15%), with about 20% unchanged.
The range comprises of protozoa: Trichomonas vaginalis, Entamoeba histolytica; anaerobic gram-negative microorganisms: bacteroids, including a group of Bacteroides fragilis (B. fragilis, B. caccae, B. uniformis, B. distasonis, B. ovatus, B. thetaiotaomicron, B. vulgatus) ; fuzobakterii Prevotella (P. bivia, P. buccae, P. disiens); anaerobic Gram-positive bacilli: Clostridium, Eubacterium; anaerobic Gram-positive cocci: Peptococcus, Peptostreptococcus; trihomonatsidnoe effect (loss of 99% above the simplest) was observed at concentrations of the drug 2,5 ug / ml for 24 h. For anaerobic microorganisms MPK90 is 8 ug / ml.
Shows activity against Helicobacter pylori.
With the appointment of people suffering from chronic alcoholism, and forms they have an aversion to alcohol (causes antabuspodobny Syndrome).
Metronidazole
Amoebiasis, trichomoniasis, giardiaz, lambliasis, intra-abdominal infections (peritonitis, abscess), anaerobic infections of bones and joints and skin and soft tissue, female genital tract (endometritis, ovarial abscess), CNS (meningitis, brain abscess), lower respiratory tract (pneumonia , empyema, lung abscess,), endocarditis, pseudomembranous colitis and eradication of Helicobacter pylori, chronic alcoholism, prevention of postoperative anaerobic infections. For external and topical use: pink and acne vulgaris, bacterial vaginosis, long-term non-healing wounds, trophic ulcers.
Contraindications
Hypersensitivity (incl. other nitroimidazole derivatives), pregnancy, lactation, infancy (excluding cases of amoebiasis).
Restrictions on the use
Diseases of the liver dysfunction (possible cumulation), the central and peripheral nervous system.
Side effects
Nausea, vomiting, abdominal pain, diarrhea, unpleasant metallic aftertaste, headache, dizziness, syncopal states, ataxia, impaired consciousness, seizures, neutropenia (leukopenia), erythematous rash, itching, staining of urine a dark color, allergic reactions, thrombophlebitis (when in / implementation).
Interaction
Enhances the effects of indirect anticoagulants and lithium salts. Phenytoin and phenobarbital reduce the effect (due to the activation of liver microsomal system and accelerate the metabolism and excretion), and cimetidine enhances (inhibits the enzyme systems of liver and, consequently, slow biotransformation). Incompatible with alcohol (by sharing a growing antabuspodobny syndrome).
Overdose
Symptoms: nausea, vomiting, ataxia, in severe cases - peripheral neuropathy and seizures.
Treatment: symptomatic, there is no specific antidote.
Dosing and Administration
Inside, during or after a meal. Amoebiasis: adults - 600-800 mg 3 times daily for 8-10 days; children - 35-50 ppm / day in 3 divided doses for 8-10 days.
Giardiazis: 15 mg / kg / day in 3 divided doses for 5 days.
Trichomoniasis: adults - by mouth, 400 mg 2 times a day for 5-8 days (if necessary repeat the course in 4-6 weeks) or a single 2.0 g or 250 mg 2 times a day for 10 days, held together treatment of both partners. Children: 2-5 years - 250 mg / day, 5-10 years - 250-375 mg / day, more than 10 years - 500 mg / day by mouth, while the daily dose is divided into 3.
Giardiasis: Adults - at 400 mg 3 times daily for 5 days or 250 mg 2 times a day for 10 days; children: 2.5 years - 250 mg / day, 5-10 years - 250-375 mg / day, over 10 years - 500 mg / day orally, in 3 divided doses. After completion of treatment in 2-3 months is control study on the completeness of healing.
Eradication of Helicobacter pylori: 500 mg 3 times daily for 7 days, always in combination with other drugs.
Anaerobic infection: adults - 400 mg 3 times daily for 7-10 days, children under 12 years - 7.5 mg / kg 3 times a day.
In severe cases, medication given by injection (IV drip) adult 500 mg in 100 ml of solvent, the children - at the rate of 7.5 mg / kg in the same amount of solvent. Infusion carried out at a rate of 5 ml / min at intervals of 8 h.
To prevent the development of postoperative anaerobic infections: a 1-second day after surgery - 1 g of the drug once, later on 200 mg 3 times daily for 7 days.
Chronic alcoholism: inside, at 0,5 g / d for 6 (not more) months.
Vaginal: 500 mg at night for 10 days.
Externally: apply two times a day, the dose is determined individually.
Trading names of drugs with active ingredient
Deflamon
Klion
Metrovagin ®
Subway
Metrogil ®
Metroksan
Metron
Metronidazole
Metronidazole / v Brown
Metronidazole Nycomed
Metronidazole-Akos
Metronidazole-Altfarm
Metronidazole-UBF
Metronidazole-chicks
Metronidazole gemisuktsinat
Metronidazole gemisuktsinat injection
Metronidazole tablets
Metroseptol
Orvagil
Rozamet
Rozeks
Trichomes-PIN ®
Trihobrol ®
Trykhopol ®
Trihosept
Flags ®
Efloran
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