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

microcrystalline - 42.00 mg; croscarmellose sodium - 25.00 mg; Povidone K-30 - 14.00 mg; silicon dioxide colloid - 7,00 mg; calcium stearate - 7.00 mg; sodium lauryl sulfate - 4,00 mg;

film sheath: [hypromellose - 15.00 mg, talc - 5.00 mg, titanium dioxide - 2.75 mg, macrogol 4000 (polyethylene glycol 4000) - 2.25 mg] or [dry mixture for film coating containing hypromellose (60%) , talc (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)] - 25.00 mg.

Description:

Round biconvex tablets covered with a film coat of white or white with a yellowish hue.

Pharmacotherapeutic group:An antiprotozoal agent.

ATX: & nbsp

G.01.A.F.06 Ornidazole

Pharmacodynamics:

Ornidazole is an antiprotozoal and antimicrobial drug, a derivative of 5-nitroimidazole. The mechanism of action is the biochemical reduction of the 5-nitro group of ornidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. Reduced 5-nitro group of ornidazole. interacts with DNA cells of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active with respect to Trichomonas vaginalis, Giardia lamblia (Giardia intestinalis), Entamoeba histolytica, as well as obligate anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicronron, Bacteroides vulgatus), Fusobacterium spp., Clostridium spp., and anaerobic cocci Peptostreptococcus spp., Peptococcus spp.

Orniferous microorganisms are not sensitive to ornidazole.

Pharmacokinetics:

Suction

After oral administration ornidazole quickly absorbed in the gastrointestinal tract (GIT), absorption is an average of 90%. The maximum concentration (C_mOh) of ornidazole in blood plasma is observed 3 hours after taking the drug. Distribution

The binding of ornidazole to plasma proteins is about 13%. Ornidazole penetrates into breast milk and most tissues, cerebrospinal fluid, other body fluids, passes through the blood-brain barrier and the placenta. Concentrations of ornidazole in the blood plasma are in the range of 6-36 mg / l, that is, at a level considered optimal for different indications for the use of the drug. After repeated use of 500 mg or 1000 mg of the drug by healthy volunteers every 12 hours, the cumulation coefficient was 1.5-2.5. Metabolism

It is metabolized in the liver by hydroxylation, oxidation and glucuronation with the formation of mainly 2-hydroxymethyl- and alpha-hydroxymethylmetabolites. Both metabolites are less active in relation to Trichomonas vaginalis and anaerobic bacteria than unchanged ornidazole.

Excretion

The half-life (T1/2) is 12-14 hours. After a single application of the drug, 85% of the dose is taken within the first 5 days, mainly in the form of metabolites: 60-70% kidney and 20-25% intestine.In unmodified form it is excreted by the kidneys (4%). Cumulates.

Pharmacokinetics in specific patient groups Patients with hepatic impairment

T1/2 Ornidazole in cirrhosis increases to 22 hours, creatinine clearance is reduced to 35 ml / min compared with healthy.

Patients with impaired renal function

In renal dysfunction, the pharmacokinetics of ornidazole does not change, so dose adjustments are not required.

Ornidazole is excreted during hemodialysis. Before the beginning of hemodialysis it is necessary to take an additional ornidazole (50% of the prescribed dose).

Childhood

The pharmacokinetics of ornidazole in children is similar to the pharmacokinetics of adults.

Indications:

- trichomoniasis;

- amebiasis: amoebic dysentery, intestinal and extra-intestinal amebiasis (including amoebic liver abscess);

- giardiasis;

- prevention of infections caused by anaerobic bacteria, in operations on the colon and in gynecology.

Contraindications:

- hypersensitivity to ornidazole and other nitroimidazole derivatives;

- organic diseases of the central nervous system (CNS);

- pathological changes in blood and abnormalities of blood cells;

- deficiency of lactase, galactose intolerance, glucose-galactose malabsorption;

- pregnancy (I trimester);

- the period of breastfeeding;

- children under 3 years old and body weight less than 20 kg.

Carefully:

- impaired liver function;

- alcoholism;

- patients of advanced age;

- pregnancy (II and III trimesters).

Pregnancy and lactation:

Pregnancy

During the study ornidazole did not show teratogenic or toxic effects on the fetus. Since no controlled studies have been conducted with pregnant women, it is possible to prescribe the drug during pregnancy (II and III trimester) only in the presence of absolute indications, when the possible benefits of using the drug for the mother exceed the potential risk to the fetus. Ornidazole contraindicated in the first trimester of pregnancy.

Breastfeeding period

If it is necessary to use the drug Ornidazole during breastfeeding should stop breastfeeding. Renewal of breastfeeding is possible no earlier than 48 hours after the last dose of the drug.

Dosing and Administration:

Inside, after eating, squeezed a little water.

Trichomoniasis

Adults and children weighing more than 35 kg - 0.5 g (1 tablet) 2 times a day (morning and evening) for 5 days.

To eliminate the possibility of re-infection, the sexual partner should in all cases receive the same treatment.

The daily dose for children weighing 20-35 kg is 25 mg / kg of body weight and is prescribed in one session (in the evening), for 5 days.

Intestinal amebiasis

Adults and children weighing over 35 kg - 1.5 g (3 tablets) once a day (in the evening), with a body weight of over 60 kg - 2 g (4 tablets) per day once, for 3 days; children older than 3 years and with a body weight of 20-35 kg - 40 mg / kg per day once, for 3 days. Extraintestinal amebiasis

Adults and children over 12 years of age - 500 mg (1 tablet) in the morning and evening for 5-10 days; children older than 3 years and with a body weight of 20-35 kg - 40 mg / kg per day once. Duration of treatment is 5-10 days.

Lambliasis

Adults and children weighing over 35 kg - 1.5 g (3 tablets) per day once in the evening; children older than 3 years and with a body weight of 20-35 kg - 40 mg / kg per day once. Duration of treatment is 1-2 days.

Prevention of anaerobic infection during surgery

For 0.5-1 g (1-2 tablets) for 1-2 hours before surgery, after surgery - 0.5 g (1 tablet) 2 times a day for 3-5 days.

Side effects:

From the nervous system:

- tremor, muscle stiffness, impaired coordination of movements, convulsions, temporary loss of consciousness, signs of sensory or mixed peripheral neuropathy, dizziness, drowsiness, fatigue, headache.

From the digestive system:

- disorders of the gastrointestinal tract, including nausea, vomiting, diarrhea, perversion of taste sensations, a "metallic" taste in the mouth, a change in the activity of "liver enzymes."

On the part of the organs of hematopoiesis:

- oppression of bone marrow hematopoiesis, neutropenia.

From the urinary system.

- polyuria.

Allergic reactions:

- manifestations of skin reactions and hypersensitivity reactions (rash, itching, urticaria, angioedema).

Overdose:

Symptoms

In case of an overdose, there may be: loss of consciousness, headache, dizziness, shivering, convulsions, dyspeptic disorders and the occurrence of other dose-related symptoms as indicated in the "Side effect" section, but in a more pronounced form. Treatment

Treatment is symptomatic, a specific antidote is unknown. To remove ornidazole from the body, gastric lavage or hemodialysis is recommended.In case of convulsions, intravenous diazepam is administered.

Interaction:

Strengthens the effect of anticoagulants coumarinic series, which requires appropriate correction of their dose; prolongs the miorelaksiruyuschee action of vecuronium bromide.

Compatible with ethanol (does not inhibit acetaldehyde dehydrogenase), unlike other imidazole derivatives (metronidazole).

Joint reception with phenobarbital and other inducers of hepatic enzymes reduces T1/2 Ornidazole from blood plasma, while co-administration with inhibitors of microsomal liver enzymes (eg, cimetidine) increase T1/2.

Special instructions:

When treating trichomoniasis, simultaneous treatment of sexual partners should be carried out.

In the course of treatment, there may be a worsening of the course of diseases of the peripheral nervous system. When symptoms of peripheral neuropathy, ataxia, dizziness or confusion arise, treatment should be suspended.

Patients receiving lithium therapy should monitor the concentration of lithium, electrolytes and creatinine in the blood plasma during treatment with ornidazole.

There is a certain risk in patients with liver damage, brain abusing alcohol (see the section "With caution"),

In the case of hemodialysis, the reduction T1 \ 2 and prescribe additional doses of the drug before or after hemodialysis (see section "Pharmacological properties").

The effect of other drugs may increase or decrease during the period of application of the drug.

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

Given the potential for the development of adverse reactions from the nervous system (dizziness, headache, drowsiness, fatigue, impaired coordination, temporary loss of consciousness), with the drug Ornidazole should refrain from transport management and the performance of potentially hazardous activities that require increased attention and speed of response.

Form release / dosage:

Tablets, film-coated, 500 mg.

Packaging:

3 or 5 tablets in a planar cell box made of a polyvinylchloride film and aluminum foil.

3 or 10 tablets in a can of high-density polyethylene.

1 contour squad package of 3 tablets, 2 out-of-round packs of 5 tablets or one bank, along with instructions for use in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005125/08

Date of registration:01.07.2008

The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia

Manufacturer: & nbsp

VERTEKS, AO Russia

Representation: & nbspVERTEKS CJSC VERTEKS CJSC Russia

Information update date: & nbsp29.06.2015

Illustrated instructions

Instructions

Ornidazole (Ornidazole)