Tinidazolum

General characteristics. Structure:

Active agent: Tinidazolum of 500 mg

Excipients: kernel: cellulose microcrystallic - 80,0 mg, potato starch - 17,0 mg, povidone (polyvinylpirrolidone) - 32,0 mg, croscarmellose sodium of-15,0 mg, magnesium stearate - 6,0 mg; cover: a gipromelloza - 12,0 mg, a macrogoal of-2,5 mg, titanium dioxide - 5,0 mg, talc (magnesium hydrosilicate) - 0,5 mg.

Pharmacological properties:

Antiprotozoan drug with antimicrobic action. Entamoeba histolytica, Lamblia spp is active concerning Trichomonas vaginalis. Has bactericidal effect concerning the following anaerobic microorganisms: Bacteroides spp., (including Bacteroides fragilis, Bacteroides melaninogenicus), Clostridium spp., Eubacterium spp., Fusobacterium spp., Peptococcus spp., Peptostreptococcus spp. The mechanism of action is caused by oppression of synthesis and damage of structure of DNA of activators.

Pharmacokinetics. Absorption — high, bioavailability — about 100%. Communication with proteins of plasma — 12%. The maximum concentration (Stakh) in a blood plasma is reached after intake of 2 g — 40-51 mkg/ml, in 24 h — 11-19 mkg/ml, in 72 h — 1 mkg/ml. Time of achievement of the maximum concentration — 2 h. Distribution volume — 50 l. Gets through a blood-brain barrier, a placenta. It is allocated with breast milk during 72 h after reception. It is metabolized in a liver with formation pharmacological of active hydroxylated derivatives which suppress growth of anaerobic microorganisms and can strengthen action of Tinidazolum. An elimination half-life (T1/2) — 12-14 h. It is removed with bile — 50%, kidneys — 25% (in not changed look) and 12% (in the form of metabolites). Is exposed to the return absorption in renal tubules.

Indications to use:

— trichomoniasis (colpitises, endometritises, ovarian and tubovarialny abscesses);
— lambliasis;
— amebiasis (including intestinal and hepatic form);
— the infections caused by anaerobic bacteria (at pneumonia, a pleura empyema, abscess of a lung, an infection of skin and soft tissues, at an acute ulocace);
— the mixed aerobic-anaerobic infections (in a combination with antibiotics);
— Helicobacter pylori eradikation (in a combination with drugs of bismuth and antibiotics).
Drug is used for prevention of the postoperative infectious complications caused by anaerobe bacterias.

Route of administration and doses:

Pill is taken inside in time or after food.
At trichomoniasis and a lambliasis drug appoint once adult on 2 g/days; to children at the rate of 50-75 mg/kg of body weight a day. If necessary administration of drug can be repeated in the same dose. At an intestinal amebiasis the daily dose for adults makes 2 g, drug is accepted by 2-3 days. To children Tinidazolum is appointed at the rate of 50-60 mg/kg/days; a course of treatment — 3 days.
At a hepatic amebiasis the adult drug appoint 1,5-2 g/days in an initial dose. The course of treatment — 3 days, if necessary duration of therapy can be increased up to 6 days. The course dose depending on weight of an infection makes 4,5-12 g. To children Tinidazolum is appointed in doses at the rate of 50-60 mg/kg/days; therapy duration — 5 days. At treatment of the infections caused by anaerobe bacterias adult in the first day of treatment appoint 2 g/days in 1 reception, then on 1 g/days. Treatment is continued by 5-6 days. For prevention of postoperative complications by the adult appoint 2 g once in 12 hours prior to operation. Safety and efficiency of use of drug for treatment and prevention of mephitic gangrenes at children are younger than 12 years are not established.

Features of use:

At treatment of genital trichomoniasis it is necessary to carry out simultaneous treatment of sexual partners. In the course of treatment it is necessary to abstain from the ethanol use (a possibility of development of disulfiramopodobny reactions).
Causes dark coloring of urine. At appointment more than 6 days control of a picture of peripheral blood is necessary. During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

- From digestive tract: anorexia, dryness and unpleasant taste in a mouth, nausea, vomiting, diarrhea are possible.
- From the central nervous system: headache, dizziness, ataxy, peripheral neuropathy; seldom — spasms.
- Allergic reactions: urticaria, skin itch, skin rash, Quincke's disease.
- Other: seldom — a tranzitorny leukopenia, weakness.

Interaction with other medicines:

Strengthens effect of indirect anticoagulants (for reduction of risk of development of bleedings the dose is reduced by 50%) and effect of ethanol (disulfiramopodobny reactions). Let's combine with streptocides and antibiotics (aminoglycosides, erythromycin, rifampicin, cephalosporins). It is not recommended to appoint with Etioniamidum. Phenobarbital accelerates metabolism.
 

Contraindications:

Hypersensitivity to drug or other derivative 5-nitroimidazo-la, organic diseases of the central nervous system, oppression of a marrowy hemopoiesis, the I trimester of pregnancy, the lactation period, children's age (up to 12 years).

USE DURING PREGNANCY AND DURING FEEDING BY THE BREAST
Drug is contraindicated to use in the I trimester of pregnancy. Use in II and III trimesters is possible only when the estimated advantage for mother exceeds potential risk for a fruit. In need of use of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination. It is necessary to consider that Tinidazolum is defined in breast milk during 72 h after reception.

Overdose:

Symptomatic treatment. The specific antidote does not exist. Tinidazolum is removed at dialysis.

Storage conditions:

List B. To store in the dry, protected from light place at a temperature not above 25 °C.
To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 500 mg.
On 4, 10 tablets place in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.
On 4, 10, 16, 20, 30 or 50 tablets place in a container polymeric for medicines. One container or 1, 2, 3, 4 or 5 blister strip packagings together with the application instruction place in a pack from a cardboard.