Metronidazole tablets 250mg, No. 24

• Protozoal infections: extraintestinal amebiasis, including amoebic liver abscess, intestinal amebiasis (amoebic dysentery), trichomoniasis (including trichomonas vaginitis, trichomonas urethritis).

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

• Infections caused by the species Clostridium spp., Peptococcus niger and Peptostreptococcus spp .: infections of the abdominal cavity (peritonitis, liver abscess), infections of the pelvic organs (endometritis, abscess of the fallopian tubes and ovaries, infections of the vaginal vault). Pseudomembranous colitis (associated with the use of antibiotics).

• Gastritis or duodenal ulcer associated with Helicobacter pylori.

• Prevention of postoperative complications (especially interventions on the colon, near-rectal region, apendectomy, gynecological operations).

• Radiation therapy for patients with tumors - as a radiosensitizing agent, in cases where tumor resistance is due to hypoxia in tumor cells.

Inside, during or after meals, (or with milk), without chewing. With trichomoniasis - 250 mg 2 times a day. within 10 days or 400 mg 2 times a day. within 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.

Children under 1 year old - 125 mg / day, 2-4 years - 250 mg / day, 5-8 years - 375 mg / day, over 8 years - 500 mg / day. (in 2 steps). The course of treatment is 5 days.

For adults with asymptomatic amebiasis (if a cyst is detected), the daily dose is 1-1.5 g (500 mg 2-3 times a day) for 5-7 days.

In chronic amoebiasis, the daily dose is 1.5 g in 3 doses for 5-10 days, in acute amoebic dysentery - 2.25 g in 3 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.

For ulcerative stomatitis, adults are prescribed 500 mg 2 times a day. within 3-5 days; in this case, the drug is not indicated for children.

With pseudomembranous colitis - 500 mg 3-4 times a day.

For the eradication of Helicobacter pylory - 500 mg 3 times a day. within 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.

For the prevention of infectious complications - 750-1500 mg / day. in 3 divided doses 3-4 days before surgery, or once 1 g on the first day. after operation. 1-2 days after surgery (when ingestion is already allowed) - 750 mg / day. within 7 days.

With severe renal impairment (creatinine clearance less than 10 ml / min), the daily dose should be halved.

Tablets of white or white color with a yellowish-greenish tinge, flat-cylindrical, with a score and a chamfer.

1 tab.

metronidazole 250 mg

Excipients: potato starch, stearic acid, talc.

• Hypersensitivity

• leukopenia (including history),

• organic lesions of the central nervous system (CNS) (including epilepsy),

• hepatic impairment (in the case of large doses),

• pregnancy (I trimester), lactation period.

• With caution: pregnancy (II-III trimesters), renal / hepatic failure.

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 deoxyribonucleic acid (DNA) of microbial cells, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active against Trichomonas vaginalis, Entamoeba histolytica, as well as gram-negative anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp. and some gram-positive anaerobes (sensitive strains Eubacterium spp., Clostridium spp., Peptococcus niger., Peptostreptococcus spp.). The minimum inhibitory concentration for these strains is 0.125-6.25 ?g / 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 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 power, 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 the blood-brain and placental barrier. Vd: adults - about 0.55 l / kg, newborns - 0.54-0.81 l / kg.

Cmax of the drug in the blood ranges from 6 to 40 ?g / ml, depending on the dose. The time to reach Cmax is 1-3 hours. The connection with plasma proteins is 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: those born at a gestational age of 28-30 weeks - about 75 hours, respectively, 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 metronidazole 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.

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 electrocardiogram.

Application during pregnancy and lactation

Contraindicated in the first trimester of pregnancy, during lactation.

With care: pregnancy (II-III trimesters).

Application for violations of liver function

With care: liver failure. In case of liver failure, large doses should not be prescribed.

Application for impaired renal function

With caution: renal failure. With severe renal impairment (creatinine clearance less than 10 ml / min), the daily dose should be halved.

In patients with impaired renal function, after repeated administration, accumulation of metronidazole in the blood serum may be observed (therefore, in patients with severe renal insufficiency, the frequency of administration should be reduced).

Application in children

Application is possible according to the dosage regimen.

In combination with amoxicillin, it is not recommended to use this drug in patients under 18 years of age.

special instructions

During the period of treatment, ethanol is contraindicated (a disulfiram-like reaction may develop: spastic abdominal pain, nausea, vomiting, headache, sudden flushing of 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).

It is recommended to stop breastfeeding during the treatment period.

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.