Metronidazole pills 250 mg, 50 pcs.

Composition

Per tablet:

Active ingredient: metronidazole – 250 mg.

Excipients: potato starch, stearic acid, povidone (polyvinylpyrrolidone low molecular weight medical 12600±2700, plasdon K-17), sucrose (powdered sugar).

Pharmacological action

Pharmacotherapeutic group: antimicrobial and antiprotozoal agent

ATX Code: J01XD01

Pharmacological Properties

Pharmacodynamics

Metronidazole is a derivative of 5-nitroimidazole. The mechanism of action of metronidazole is the biochemical reduction of the 5-nitro group of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group of metronidazole interacts with the deoxyribonucleic acid (DNA) of the microbial cell, inhibiting the synthesis of their nucleic acids, which leads to the death of microorganisms.

Active against Trichomonas vaginalis, Entamoeba histolytica, and gram-negative anaerobes Bacteroides spp. (including B. fragilis, B. distasonis, B. ovatus, B. thetaiotaomicron, B. vulgatus), Fusobacterium spp., and some Gram-positive anaerobes (sensitive strains of Eubacterium spp., Clostridium spp., Peptococcus niger., 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 suppresses 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.

Pharmacokinetics

When taken orally, metronidazole is rapidly and almost completely absorbed (approximately 80% in 1 hour). Food intake does not affect the absorption of metronidazole. Bioavailability is at least 80%. After oral administration of metronidazole at a dose of 500 mg, its concentration in blood plasma is 10 mcg / ml after 1 hour,13.5 mcg / ml after 3 hours. Binding to blood proteins is insignificant and does not exceed 10-20%. Metronidazole quickly penetrates into the tissues (lungs, kidneys, liver, skin, bile, cerebrospinal fluid, saliva, seminal fluid, vaginal secretions), into breast milk and passes through the placental barrier. About 30-60% of metronidazole is metabolized by hydroxylation, oxidation, and glucuronidation. Main metabolite (2-oxymetronidazole) it also has an antiprotozoal and antimicrobial effect.

40-70% of metronidazole is excreted by the kidneys (in unchanged form-about 35% of the dose taken). The elimination half-life is 8-10 hours.

In patients with impaired renal function, a course of taking metronidazole may increase its concentration in the blood serum.

Indications

Protozoal infections: extra-intestinal amoebiasis (including amoebic liver abscess), intestinal amoebiasis (amoebic dysentery), trichomoniasis.

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

Infections caused by Clostridium spp., Peptococcus niger and Peptostreptococcus spp. : abdominal infections (peritonitis, liver abscess), pelvic infections (endometritis, fallopian tube and ovarian abscess, vaginal vault infections).

Pseudomembranous colitis associated with the use of antibiotics.

Gastritis or duodenal ulcer associated with Helicobacter pylori (as part of complex therapy).

Prevention of postoperative complications (especially after operations on the colon, pararectal area, appendectomy, gynecological operations).

Use during pregnancy and lactation

Since metronidazole passes through the placental barrier and its effect on the organogenesis of the human fetus is unknown, the use of the drug during pregnancy is contraindicated.

Metronidazole penetrates into breast milk, so the use of the drug during breastfeeding is contraindicated.

Contraindications

– hypersensitivity to metronidazole and other nitroimidazole derivatives, to imidazoles or other ingredients;

organic CNS lesions (including epilepsy);

– leukopenia (including in the anamnesis);

– liver failure (in case of appointment of high doses);

– pregnancy;

– the period of breastfeeding;

– children up to age 6 years;

– deficiency of sucrase/isomaltase, fructose intolerance, glucose-galactose malabsorption.

With caution

– hepatic encephalopathy;

– acute and chronic diseases of the peripheral and central nervous system (risk of aggravation of neurological symptoms);

– renal failure.

Side effects

Gastrointestinal disorders

– Epigastric pain, nausea, vomiting, diarrhea.

– Inflammation of the oral mucosa (glossitis, stomatitis), taste disorders (“metallic” taste in the mouth), decreased appetite, anorexia, dryness of the oral mucosa, constipation.

– Pancreatitis (reversible cases).

– Discoloration of the tongue/ “overlaid” tongue (due to excessive growth of fungal microflora).

Immune system disorders

– Angioedema, anaphylactic shock.

Nervous system disorders

– Peripheral sensory neuropathy.

– Headache, cramps, dizziness.

– Encephalopathy (e. g., confusion) and subacute cerebellar syndrome (impaired coordination and synergy of movements, ataxia, dysarthria, gait disorders, nystagmus and tremor) have been reported to reverse after metronidazole withdrawal.

– Aseptic meningitis.

Mental disorders

– Psychotic disorders, including confusion, hallucinations.

– Depression, insomnia, irritability, increased excitability.

Visual disturbances

– Transient visual disturbances, such as diplopia, myopia, blurred vision, decreased visual acuity, and color perception disorders.

– Neuropathy/neuritis of the optic nerve.

Hearing disorders and labyrinth disorders

– Hearing disorders/hearing loss (including sensorineural deafness).

– Tinnitus.

Disorders of the blood and lymphatic system

– Agranulocytosis, leukopenia, neutropenia and thrombocytopenia.

Liver and biliary tract

disorders – Increased activity of “liver” enzymes (aspartate aminotransferase (AST)Studies of liver function should be performed before starting treatment, during therapy, and after it ends until liver function indicators reach normal values, or until the initial values of these indicators are reached. If liver function indicators are significantly exceeded during treatment, the drug should be discontinued.

Patients with Cockayne’s syndrome should be advised to immediately report any symptoms of potential liver damage to their doctor and discontinue the use of metronidazole.

It should be taken into account that metronidazole can immobilize treponemes, which leads to a false positive Nelson test.

Influence on the ability to drive vehicles and mechanisms

Taking into account the risk of developing such adverse reactions as confusion, dizziness, hallucinations, visual disturbances, it is recommended to refrain from driving during treatment, from engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

In a dark place at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Metronidazole

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Weight

Weight: 35 gr.