Metrogil - instructions for use, dose, side effects, contraindications

Excipients: corn starch 57.5 mg, methylparahydroxybenzoate sodium 0.5 mg, magnesium stearate 1.0 mg, silicon dioxide colloid 1.5 mg, castor oil hydrogenated 1.0 mg.

Film coating: Opaprai II pink 85G54815 7,875 mg (polyvinyl alcohol, partially hydrolyzed 3,465 mg, talc 1,575 mg, titanium dioxide 1,473 mg, macrogol 3000 0,973 mg, lecithin 0.276 mg, crimson dye [Ponso 4 R] (aluminum varnish) 0.114 mg)

1 tablet, film-coated, with a dosage of 400 mg contains:

Active substance: metronidazole 400 mg;

Excipients: corn starch 35.0 mg, methylparahydroxybenzoate sodium 1.0 mg, povidone 10.0 mg, magnesium stearate 2.0 mg, silicon dioxide colloid 3.0 mg, croscarmellose sodium 10.0 mg.

Film coating: Opaprai II orange 85G53070 14.0 mg (polyvinyl alcohol, partially hydrolyzed 6.160 mg, talc 2.80 mg, titanium dioxide 2.618 mg, macrogol 3000 1.729 mg, lecithin 0.490 mg, dye sunset yellow (aluminum lacquer) 0.227 mg)

Description:

Tablets with a dosage of 200 mg: Round, biconvex tablets, covered with a film shell of pink color.

Tablets with a dosage of 400 mg: Round, biconvex tablets, covered with a film shell of orange color.

Pharmacotherapeutic group:Antimicrobial and antiprotozoal drug

ATX: & nbsp

P.01.A.B Nitroimidazole derivatives

P.01.A.B.01 Metronidazole

Pharmacodynamics:

Antiprotozoal and antimicrobial drug, a derivative of 5-nitroimidazole.The mechanism of action 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 reacts with the DNA of a cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active with respect to Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., as well as obligate anaerobes Bacteroides spp. (in t.ch. Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella (Prevotella bivia, Prevotella buccae, Prevotella disiens) and some Gram-positive microorganisms (Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.). The MIC for these strains is 0.125-6.25 μg / ml.

In combination with amoxicillin shows activity against Helicobacter pylori (amoxicillin suppresses the development of resistance to metronidazole).

Metronidazole is insensitive Aerobic microorganisms and facultative anaerobes, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against conventional aerobes.

Pharmacokinetics:

Absorption is high (bioavailability is not less than 80%). It has a high penetrating ability, reaching bactericidal concentrations in most tissues and body fluids, including lungs, kidneys, liver, skin, cerebrospinal fluid, brain, bile, saliva, amniotic fluid, abscess cavities, vaginal secretion, seminal fluid, breast milk; penetrates through the blood-brain and placental barrier. After ingestion of a single dose of the drug 200 mg, 400 mg metronidazole quickly and completely absorbed, reaching a peak concentration in the blood plasma (6 μg / ml, 12 μg / ml) after 2 hours. The average area under the pharmacokinetic curve "Concentration-time" is 35 μg / ml / h and 69 μg / ml / hour, respectively. Connection with blood plasma proteins - 10-20%.

In the body, about 30-60% of metronidazole is metabolized by hydroxylation, oxidation and glucuronation. The main metabolite (2-oxymetronidazole) also has antiprotozoal and antimicrobial effects.

It is excreted by the kidneys (60-80% of the dose), 20% the drug is withdrawn unchanged. Half-life with normal liver function is an average of 8 hours; with alcoholic liver damage - an average of about 18 hours (from 10 to 29 hours). Kidney clearance is about 10 ml / min.

In patients with impaired renal function after repeated administration of the drug may be observed cumulation metronidazole in blood plasma (therefore, in patients with severe renal failure, the daily dose of metronidazole should be reduced).

Metronidazole and the main metabolites are rapidly removed from the blood plasma during hemodialysis (the elimination half-life is reduced to 2.6 hours). When peritoneal dialysis is withdrawn in small quantities.

Indications:

- Protozoal infections (amoebiasis, trichomoniasis, giardiasis, amoebic dysentery);

- anaerobic infections caused by Bacteroides spp. (incl. Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus): infections of bones and joints, infections of the central nervous system, incl. meningitis, abscess of the brain, lower respiratory tract (pneumonia, pleural empyema, lung abscess, bacterial endocarditis).

- Infections caused by the species Clostridium spp., Peptococcus and Peptostreptococcus: infection of the abdominal cavity (peritonitis, liver abscess), pelvic infection (endometritis, abscess of fallopian tubes and ovaries, vaginal vaginal infection).

- Prevention of postoperative complications (especially with interventions on the colon, near-rectal area, appendectomy, gynecological operations).

Contraindications:

Hypersensitivity to metronidazole or components included in the preparation, as well as to other derivatives of nitroimidazole; I trimester of pregnancy, lactation period, organic lesions of the central nervous system (including epilepsy), leukopenia (incl.in the anamnesis), hepatic insufficiency (in case of appointment of the big doses); children's age up to 3 years.

In combination with amoxicillin it is not recommended to use in patients younger than 18 years.

Carefully:

Renal or hepatic insufficiency.

Pregnancy and lactation:

II and III trimesters of pregnancy - only for life indications; breastfeeding mothers - according to indications, with simultaneous cessation of breastfeeding.

Dosing and Administration:

Inside with food or after eating, without chewing (or squeezed milk).

The dose of the drug and the course of treatment is determined by the nature of the infection:

- trichomoniasis: adults - 400 mg twice a day for 5-8 days; women should be additionally appointed metronidazole in the form of vaginal suppositories or vaginal ointments. If necessary, you can repeat the course of treatment or increase the dose to 750-1000 mg / day. Between the courses should be a break in 3-4 weeks with the conduct of repeated control laboratory tests. An alternative scheme of therapy is the appointment of 2 g once to the patient and his sexual partner.

- giardiasis - adults: 200 mg, maximum - 4 times a day, for 5 days.After the completion of treatment after 2-3 months, it is necessary to study the completeness of the cure.

- amebiasis: adults with asymptomatic flow (if a cyst is detected) - a daily dose of 1.0-1.5 g, divided into several doses, for 5-7 days.

- chronic amoebiasis: adults - 1.5 grams per day in 3 divided doses, for 5-10 days. Children 30-40 mg / kg / day in 3 divided doses. The course of treatment is 7-10 days.

- amoebic liver abscess: the maximum daily dose is 2.5 g in one or 2-3 doses, for 3-5 days in combination with antibiotics (tetracycline or other antibiotics); children from 3 to 7 years - 1/3 of the dose of an adult, from 7 to 10 years - 1/2 dose of an adult.

- anaerobic bacterial infections: adults - the maximum daily dose - 1,5-2 g; children 7 mg / kg every 8 hours. The course of treatment is 7-10 days.

- for the prevention of infectious complications: 750-1500 mg / day in 3 divided doses 3-4 days prior to surgery or 1 g once a day after the operation, then 200 mg 3 times a day for 7 days.

Side effects:

Disorders from the gastrointestinal tract: pain in the epigastrium, nausea, vomiting, diarrhea, glossitis, stomatitis, "metallic" taste in the mouth, decreased appetite, anorexia, pseudomembranous colitis, dryness of the oral mucosa, constipation, pancreatitis (reversible cases),change in the color of the tongue / "lined tongue" (due to the growth of fungal microflora).

Immune system disorders: angioedema, anaphylactic shock.

Impaired nervous system: peripheral sensory neuropathy, headache, convulsions, dizziness, reported on the development of encephalopathy and subacute cerebellar syndrome (impaired coordination and synergy of movements, ataxia, dysarthria, gait disturbance, nystagmus, tremor) that are reversible after metronidazole withdrawal, aseptic meningitis.

Disorders of the psyche: psychotic disorders, including disorders and confusion, hallucinations; depression, insomnia, irritability, increased excitability.

Disorders from the side of the organ of vision: transient visual impairments, such as diplopia, myopia, vagueness of contours of subjects, reduced visual acuity, violation of color perception; Neuropathy / optic neuritis.

Violations from the blood and lymphatic system: agranulocytosis, leukopenia, neutropenia, thrombocytopenia.

Disorders from the liver and bile ducts: rise activity of "liver" enzymes (aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase), development of cholestatic or mixed hepatitis and hepatocellular liver damage, sometimes accompanied by jaundice; In patients treated with metronidazole in combination with other antibacterial agents, cases of hepatic insufficiency, which required carrying out liver transplantation.

Disturbances from the skin and subcutaneous tissues: rash, itching, skin hyperemia, urticaria, pustular skin rash, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Disorders from the kidneys and urinary tract: staining of urine in a brownish-reddish color due to the presence in the urine of a water-soluble metabolite of metronidazole, dysuria, polyuria, cystitis, urinary incontinence, candidiasis.

General disorders: fever, nasal congestion, arthralgia, weakness.

Laboratory and instrumental data: flattening of the T wave on electrocardiogram.

Overdose:

Symptoms: nausea, vomiting, ataxia, in severe cases - peripheral neuropathy and epileptic seizures.

Treatment: symptomatic, specific antidote is absent.

Interaction:

Increases the effect of indirect anticoagulants, which leads to an increase in prothrombin time.

Similarly, disulfiram can cause intolerance to ethanol.

Cimetidine inhibits metronidazole metabolism, which can lead to an increase in its serum concentration and an increased risk of side effects.

Sulfonamides increase the antimicrobial effect of metronidazole.

Simultaneous administration of drugs stimulating enzymes of microsomal oxidation in the liver (phenobarbital, phenytoin) can accelerate the elimination of metronidazole, as a result of which its concentration in the blood plasma decreases.

With simultaneous administration with lithium preparations, the concentration of lithium in blood plasma and the development of symptoms of intoxication may increase.

It is not recommended to combine with nondepolarizing muscle relaxants (vecuronium bromide).

Special instructions:

During the drug intake, alcohol can not be consumed (it is possible to develop a disulfiram-like reaction: abdominal pain of a spastic nature, nausea, vomiting, headache, sudden rush of blood to the face).

With leukopenia, the possibility of continuing treatment depends on the risk of developing an infectious process.Long-term use of the drug is desirable to be carried out under the control of peripheral blood.

The appearance of ataxia, dizziness and any other deterioration in the neurological status of patients requires discontinuation of treatment.

Can immobilize treponema and lead to Nelson's false positive test.

When treating trichomonadal vaginitis in women and trichomoniasis in men, it is necessary to abstain from sexual activity. It is necessary to simultaneously treat sexual partners. After therapy with trichomoniasis, control tests should be performed for 3 consecutive cycles before and after menstruation.

After treatment of giardiasis, if symptoms persist, 3 feces analysis should be performed at intervals of several days in 3-4 weeks (in some successfully treated patients lactose intolerance caused by invasion can persist for several weeks or months, recalling the symptoms of giardiasis).

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and when engaging in other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions (dizziness, impaired consciousness, hallucinations, convulsions, impaired coordination of movements, ataxia).

Form release / dosage:

The film-coated tablets are 200 mg and 400 mg.

Packaging:

10 tablets per blister Al / PVC.

2 or 10 blisters (20 or 100 tablets) together with instructions for use in a cardboard box.

Storage conditions:

At a temperature of no higher than 30 ° C, in a place protected from light.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N011666 / 03

Date of registration:16.01.2009 / 26.05.2016

Expiration Date:Unlimited

The owner of the registration certificate:Unik Pharmaceutical Laboratories Unik Pharmaceutical Laboratories India

Manufacturer: & nbsp

UNIQUE PHARMACEUTICAL Laboratories India

Representation: & nbsp"UNIC PHARMACEUTICAL LABORATORY (branch of the company" JB Chemicals and Pharmaceuticals Ltd. ")""UNIC PHARMACEUTICAL LABORATORY (branch of the company" JB Chemicals and Pharmaceuticals Ltd. ")"India

Information update date: & nbsp11.05.2018

Illustrated instructions

Instructions

Metrogil® (Metrogyl®)