Metronidazol-Zdorovye, the tab. on 250 mg No. 10х2

General characteristics. Structure:

International and chemical names: metronidazole, 2 (2-methyl-5-nitro-1H-imidazole-1-silt) ethanol;
main physical and chemical properties: tablets of color, white or white with a yellowish-greenish shade, a ploskotsilindrichesky form, with risky and a facet;
structure: 1 tablet contain metronidazole 250 mg;
excipients: starch prezhelatinizirovanny, gidroksipropilmetil-cellulose (gipromeloza), sodium of a kroskarmelloz, microcrystallic cellulose, stearic acid.

Pharmacological properties:

Pharmacodynamics. Antibacterial, antipro-tozoynoye (trikhomonatsidny) agent. Derivative nitroimidazole.
The mechanism of action is caused by penetration in a drug molecule microorganism, embedding of its nitrogroup in a respiratory chain of protozoa and anaerobe bacterias that breaks respiratory processes and causes death of cells. At some species of anaerobe bacterias suppresses synthesis of DNA and causes its degradation (a rupture of threads).
The action spectrum includes protozoa: Trichomonas vaginalis, Entamoeba histolytica, Lamblia, Leishmania; anaerobic gram-negative microorganisms: bacteroids, including the Bacteroides fragilis group (B. fragilis, B. caccae, B. uniformis, B. distasonis, B. ovatus, B. thetaiotaomicron, B. vulgatus); Prevotella fuzobakteriya (P. bivia, P. buccae, P. disiens); anaerobic gram-positive sticks: Clostridium, sensitive strains of Eubacterium; anaerobic gram-positive cocci: Peptococcus spp., Peptostreptococcus spp. Trikhomonatsidny action (death about 99% of the above-stated protozoa) is observed at concentration of drug of 2,5 mkg/ml during the 24th hour. For anaerobic microorganisms the minimum bacteriostatic concentration causing 90% of their death makes 8 mkg/ml. Mycoplasma hominis, the elementary Balantidium coli is active concerning Mobiluncus.
In combination with amoxicillin shows activity concerning Helicobacter pylori (amoxicillin suppresses development of resistance to metronidazole).
Facultative anaerobes and obligate aerobes, but in the presence of the mixed flora are steady against metronidazole (aerobes and anaerobe bacterias) metronidazole works synergy with antibiotics, effective against usual aerobes. It is inactive concerning types of Actinomyces, Candida albicans.
At patients with an alcoholism creates disgust for alcohol (causes an antabusopodobny syndrome). Stimulates reparative processes.

Pharmacokinetics. After intake it is quickly and completely soaked up from digestive tract. The concomitant use of food does not influence drug absorption. Bioavailability – not less than 80%. The maximum concentration in blood is reached in 1 – 3 h after reception and makes from 6 to 40 mkg/ml depending on the accepted dose (after intake of doses of 250 mg, 500 mg and 2 g the maximum concentration in blood serum makes 6, 12 and 40 mkg/ml respectively). Linkng with proteins of plasma insignificant – less than 20%. Well gets into fabrics and liquids of an organism, creating bactericidal concentration in the majority of fabrics and liquids, including lungs, kidneys, a liver, skin, cerebrospinal fluid, a brain, bile, saliva, semen, a vulval secret, amniotic liquid, cavities of abscesses; gets through hematoencephalic and placental barriers, and also into breast milk. Is exposed to biotransformation in a liver by a hydroxylation, oxidation and conjugation with glukuronovy acid; forms inactive and active metabolites. The main metabolite (2 oxymetronidazole) also possesses antiprotozoan and antimicrobic action. The elimination half-life at normal function of a liver – 6 – 12 h, at alcoholic damage of a liver is extended to 10 – 29 h. It is excreted by kidneys (60 - 80% of the accepted dose) and intestines (6 – 15%); in not changed look about 20% are removed.
At repeated receptions it can kumulirovatsya, especially at patients with a renal failure.
Metronidazole and its main metabolites quickly are removed from blood at a hemodialysis. At peritoneal dialysis it is removed by kidneys in insignificant quantities.

Indications to use:

Protozoan infections: abenteric amebiasis (including amoebic abscess of a liver), intestinal amebiasis (amoebic dysentery), trichomoniasis, balanthidiasis, lambliasis, skin leushmaniosis, mecotic vaginitis, mecotic urethritis.
The infections caused by anaerobic bacteria: infections of an abdominal cavity (peritonitis, liver abscess), infections of bodies of a small pelvis (an endometritis, an endomyometritis, abscess of fallopian pipes and ovaries, infections of a vault of the vagina after surgeries), infections of bones and joints, the central nervous system (including meningitis, brain abscess), a bacterial endocarditis, pneumonia, an empyema and abscess of lungs, infections of skin and soft tissues, sepsis.
The pseudomembranous colitis connected using antibiotics.
Peptic ulcer of a stomach or duodenum (in combination with drug of bismuth and an antibiotic, for example, amoxicillin).
Prevention of postoperative complications (especially interventions on a colon, okolorektalny area, appendectomy, gynecologic operations). At patients from groups of the increased risk – in combination with intravenous or intramuscular administration of cefazolin.

Route of administration and doses:

Appoint inside, in time or after food, without chewing.
Amebiasis. To adults and children 13 years are more senior appoint 250 mg (1 tablet) 3 times a day within 8 – 10 days.
To children at the age of 2 – 12 years appoint 35 – 50 mg/kg of the body weight divided into 3 receptions within 8 – 10 days in a daily dose.
Giardiazis. Appoint the adult in a dose 15 mg/kg of body weight a day for 3 receptions, within 5 days.
Trichomoniasis. Appoint the adult 500 mg (2 tablets) 2 times a day within 5 – 8 days or on 250 mg (1 tablet) 3 times a day within 10 days or 2 g (8 tablets) once. Carry out simultaneous treatment of both partners. Women need to appoint in addition metronidazole in the form of vaginal candles. If necessary after the repeated laboratory researches in 4 – 6 weeks conduct a repeated course or raise a dose to 750 – 1000 mg (3 – 4 tablets) a day.
To children appoint in a daily dose: 2 – 5 years – 250 mg (1 tablet), 5 – 10 years – 250 – 375 mg (1 – 1½ tablets), are more senior than 10 years – 500 mg (2 tablets); the daily dose is divided into 2 receptions. A course of treatment for children – 10 days.
Lambliasis. Appoint to adults and children 13 years on 500 mg (2 tablets) 2 times a day within 5 – 7 days or on 250 mg (1 tablet) 3 times a day within 10 days are more senior.
To children appoint in a dose: 2 – 5 years – on 125 mg (½ tablets) 2 times a day, 6 – 10 years – on 125 mg (½ tablets) 3 times a day, are more senior than 10 years – on 250 mg (1 tablet) 2 times a day. A course of treatment for children – 5 days.
After the termination of a course of treatment it is necessary to conduct several control laboratory researches. If necessary the course of treatment can be repeated in 4 – 6 weeks and after completion of treatment in 2 – 3 months conduct a control research on completeness of treatment.
Amebiasis. At an asymptomatic amebiasis (at detection of a cyst) the adult appoint 500 mg (2 tablets) 2 – 3 times a day within 5 – 7 days. At a chronic amebiasis the adult appoint 500 mg (2 tablets) 3 times a day within 5 – 10 days; at acute amoebic dysentery – on 750 mg (3 tablets) 3 times a day before disappearance of symptoms. At liver abscess the adult appoint in a dose not higher than 2,5 g (10 tablets) for 1 or 2 – 3 receptions, within 3 – 5 days in combination with antibiotics (tetracyclines) and other methods of therapy.
To children appoint: 2 – 3 years – ¼ doses for adults, 3 – 7 years – 1/3 doses for the adult, 7 – 10 years – ½ doses for the adult.
Skin leushmaniosis. Appoint the adult 250 mg (1 tablet) 3 – 4 times a day, to children – on 125 mg (½ tablets) 3 times a day within 7 days. Then after a 7-day break the adult – on 250 mg (1 tablet) 3 times a day, to children – on 125 mg (½ tablets) 2 times a day within 14 days.
Balanthidiasis. The adult appoint 750 mg (3 tablets) 3 times a day within 5 – 6 days.
Stomacace. The adult appoint 500 mg (2 tablets) 2 times a day within 3 – 5 days. Drug is not shown to children.
Pseudomembranous colitis. The adult appoint 500 mg (2 tablets) 3 – 4 times a day.
Peptic ulcer of a stomach or duodenum. Appoint the adult 500 mg (2 tablets) 3 times a day within 7 days, it is obligatory in combination with other drugs (for example, a combination with amoxicillin of 2,25 g/days).
At children and teenagers aged up to 18 years it is not recommended to apply in combination with amoxicillin.
Mephitic gangrene. Appoint to adults and children 12 years on 250 – 500 mg (1 - 2 tablets) 3 times a day within 7 – 10 days are more senior. To children of 2 - 12 years appoint 7,5 mg/kg of body weight 3 times a day.
Prevention of the infectious complications caused by anaerobic bacteria. For adults and children 12 years the first single dose are more senior makes 1 g (4 tablets), then appoint 250 mg (1 tablet) 3 times a day during 3 – 4 previous operations of days (prior to preoperative starvation). To children of 5 - 12 years before operation each 8 h within 2 days appoint 125 mg (½ tablets).
The alternative scheme for adults: once 1 g (4 tablets) in the first days after operation. In the next 6 days appoint 750 mg (3 tablets) in a daily dose.
The maximum daily dose for adults – 4 g.
The maximum daily dose for patients with a chronic renal failure and clearance of creatinine less than 30 ml/min. and/or a liver failure – 1 g (4 tablets) 2 times a day.

Features of use:

Restriction to use of drug are liver diseases with disturbance of its function, a disease of the central and peripheral nervous systems.
At the expressed renal failures (clearance of creatinine less than 10 ml/min.) the daily dose has to be lowered twice.
At a leukopenia the possibility of continuation of treatment depends on risk of development of infectious process.
Any deterioration in the neurologic status of the patient (emergence of an ataxy, dizziness, etc.) demands the treatment termination.
At treatment of a mecotic vaginitis at women and a mecotic urethritis at men it is necessary to refrain from sex life. Simultaneous treatment of sexual partners is obligatory. During periods treatment is not stopped. After treatment of trichomoniasis it is necessary to carry out control tests during 3 next cycles before and after periods.
At treatment of the infections caused by anaerobic bacteria, drug can be used both in the form of monotherapy, and in combination with other antibacterial agents.
After treatment of a lambliasis in case of preservation of symptoms it is necessary to carry out in 3 – 4 weeks 3 analyses a bucketed calla in several days (some successfully treated patients have a lactose intolerance caused by an invasion, can remain within several weeks or months, reminding lambliasis symptoms).
The interval between purposes of metronidazole and Disulfiramum has to make not less than 2 weeks.
It is necessary to avoid simultaneous use of metronidazole and indirect anticoagulants. In need of their joint appointment it is necessary to control carefully a prothrombin time and to pick up the corresponding dose of anticoagulant.
With care it is necessary to apply metronidazole together with lithium drugs, at the same time it is necessary to control concentration of lithium and creatinine in serum.
At administration of drug more than 10 days careful clinical and laboratory monitoring is recommended.
During treatment by metronidazole reception of alcoholic beverages since development of disulfiramopodobny reaction is possible is contraindicated (spastic abdominal pains, nausea, vomiting, a headache, sudden rush of blood to the person).
Metronidazole can immobilize treponemas and lead to the false positive TPI test (Nelson test). Obtaining false results when determining activity of transaminases of a liver, a lactate dehydrogenase, level of triglycerides and glucose in a blood plasma is also possible.
In order to avoid irritation of a mucous membrane of digestive tract drug should be accepted in time or right after food.
It is necessary not to pass doses and to accept them at regular intervals. At the admission of a dose it is necessary to accept it as soon as possible; not to accept if almost there came time of reception of the following dose; not to double a dose.
Treatment by metronidazole can be combined with streptocides and antibiotics.
At overdevelopment of fungal flora of a vagina (candidiasis) during treatment purpose of antifungal drugs (nystatin) is required by metronidazole.
Use during pregnancy and feeding by a breast. Drug is contraindicated in І a pregnancy trimester. Purpose of drug in ІІ – ІІІ trimesters of pregnancy is possible only if the expected advantage for mother exceeds potential risk for a fruit. In need of use in the period of a lactation, feeding by a breast should be stopped. Feeding by a breast can be resumed not earlier than in 24 - 48 hour after completion of treatment.
Influence on a possibility of control of vehicles and mechanisms. Due to a possibility of development of dizziness at administration of drug patients whose activity requires special attention and speed of psychomotor reactions should be careful.

Side effects:

From system of digestion: nausea, vomiting, an abdominal pain, diarrhea, locks, anorexia, unpleasant metal smack and dryness in a mouth, a glossitis, stomatitis, pancreatitis. From the central and peripheral nervous system: headache, dizziness, incoordination of movements, syncopal states, ataxy, confusion of consciousness, irritability, depression, hypererethism, weakness, sleep disorders, spasms, hallucinations, peripheral neuropathy. From system of a hemopoiesis: neutropenia, leukopenia. Allergic reactions: urticaria, skin rash, dermahemia, nose congestion, fever, arthralgias. From urinogenital system: a dysuria, cystitis, a polyuria, an urine incontience, candidiasis, coloring of urine in red-brown color. Other: flattening of a tooth of T on the electrocardiogram.

Interaction with other medicines:

Strengthens effects of indirect coagulants (that leads to lengthening of a prothrombin time) and lithium salts. Effects of metronidazole weaken Phenytoinum and phenobarbital (activating a microsomal oxidation of metronidazole and strengthening its removal); strengthens – Cimetidinum (oppresses metronidazole biotransformation in a liver). Antimicrobic effect of metronidazole is strengthened by streptocides. It is incompatible with alcohol (at joint reception disulfiramopodobny reaction develops). At co-administration with Disulfiramum development of various neurologic symptoms is possible (the interval between purpose of these drugs has to make not less than 2 weeks). It is not recommended to combine with not depolarizing muscle relaxants (a vekuroniya bromide), and also with astemizoly and terfenadiny (changes on an ECG, development of arrhythmia, a heart block, a syncope are possible).

Contraindications:

The increased individual sensitivity to components of drug or other derivatives of a nitroimidazole, a leukopenia (including in the anamnesis), organic lesions of the central nervous system (including epilepsy), a heavy liver failure (at purpose of high doses), pregnancy (especially І a trimester), feeding by a breast, children's age up to 2 years.
It is not recommended to apply in combination with amoxicillin at children and teenagers aged up to 18 years.

Overdose:

Symptoms: nausea, vomiting, ataxy; in hard cases – peripheral neuropathy and epileptic seizures. Treatment: drug withdrawal, symptomatic treatment. The specific antidote is absent.

Storage conditions:

To store in the dry, protected from light place at a temperature from 8 °C to 25 °C. To store in the place, unavailable to children.
Period of validity –3 years.

Issue conditions:

According to the recipe

Packaging:

Tablets on 250 mg No. 10х2 in blisters in a box.