Tiberal

Tiberal is a medicine used for amebiasis and other infections of the protozoal type. It is a derivative of nitroimidazole, contains the active element ornidazole.

Ornidazole is an antibacterial antiprotozoal substance derived from the element 5-nitroimidazole. The principle of the therapeutic effect of a DNA-tropic agent is based on a selective effect relative to microbes that have enzyme systems that can restore the nitro group and, at the same time, catalyze protein interactions in the category of nitro compounds with ferridoxins. [1]

Indications Tiberal

It is used for trichomoniasis, , amebiasis or giardiasis .

Release form

The release of the medication is made in the form of tablets - 10 pieces inside a cell package; inside a pack - 1 such package.

Pharmacodynamics

Demonstrates activity in relation to Trichomonas vaginalis, dysentery amoeba, Giardia intestinalis, and in addition to individual anaerobes (clostridia, bacteroids, fusobacteria) and anaerobic cocci.

When a drug enters the bacterial cell, it begins to act, restoring the nitro group under the influence exerted by microbial nitroreductases, and also stimulating the activity of the previously reduced nitroimidazole. Further, the products of this process form bonds with DNA, leading to its degradation, and also destroy DNA transcription and replication. [2]

Along with this, the metabolic components of the drug have a cytotoxic effect and destroy the cellular respiration of bacteria.

Pharmacokinetics

Absorption.

Orally administered ornidazole is absorbed at high speed inside the gastrointestinal tract. The average absorption rate is 90%. The drug reaches the intraplasmic Cmax level within a period of 3 hours.

Distribution processes.

The indicator of protein synthesis of ornidazole is 13%. The active ingredient gets into the cerebrospinal fluid and other fluids, as well as into the tissues.

Plasma values of the drug are in the range of 6-36 mg / l (this is the optimal level when using drugs). With repeated use of Tiberal (with a 12-hour interval) in portions of 0.5 and 1 g, the accumulation coefficient of the substance in volunteers is 1.5-2.5.

Exchange processes.

The drug is involved in intrahepatic metabolism with the formation of metabolic elements such as 2-hydroxymethyl and α-hydroxymethyl. These components have a weaker activity relative to vaginal Trichomonas and anaerobes (in comparison with unchanged ornidazole).

Excretion.

The half-life is 13 hours. With a single intake of drugs, 85% of the portion is excreted during the first 5 days, mainly in the form of metabolic components. Approximately 4% of the administered dose is excreted unchanged through the kidneys.

Dosing and administration

Tiberal is consumed orally, after a meal.

Trichomoniasis treatment.

Tablets with a volume of 0.5 g are used in schemes with 1-time intake or 5-day treatment.

It should be borne in mind that the introduction of ornidazole can provoke some disturbances (fever, redness, vomiting, numbness and nausea; as well as ear noise or hypotension). Also, for a period of at least 3 days after the use of drugs, it is forbidden to drink alcohol.

With a single use of the drug, a dosage of 1.5 g should be taken (3 tablets per 1 dose, in the evening). During a 5-day course, 2 tablets are consumed per day (1-well - in the morning, and the 2nd - in the evening).

To prevent the likelihood of relapse, the patient's sexual partner should undergo a similar course.

The size of the 1-fold daily dosage for a child is 25 mg / kg.

Use for amoebiasis.

With such a disease, the following treatment regimens can be used: with amoebic dysentery, a 3-day cycle of therapy is carried out; for other types of amebiasis, a 5-10-day treatment cycle is required.

With a 3-day therapeutic course, children weighing over 35 kg and adults should take 3 tablets per 1 evening intake (persons weighing over 60 kg need to use 4 tablets - 2 in the morning and in the evening). For a child weighing less than 35 kg, the size of a single serving is 40 mg / kg.

In the case of a 5-10-day cycle for a child weighing more than 35 kg and an adult, 2 tablets are required per day (1 in the morning and in the evening). For a child weighing less than 35 kg - 1 serving is 25 mg / kg.

Therapy for giardiasis.

A 1-2-day cycle of therapy is carried out. For the day, adults and children weighing more than 35 kg take 3 tablets (for 1 evening use). The daily serving size for children weighing less than 35 kg is 40 mg / kg.

Use in persons with liver failure.

In case of a severe form of violation, it is necessary to double the interval of application of the medication.

• Application for children

The medication can be used in pediatrics.

Use Tiberal during pregnancy

In experimental testing of drugs, there was no development of toxic or teratogenic effects on the fetus.

Due to the lack of controlled tests of the drug with the participation of pregnant women, it is allowed to use it at an early stage of gestation or with hepatitis B only if there are strict indications, in cases where the likely benefits of taking Tiberal are more expected than the risks of negative consequences for the fetus / infant.

Contraindications

The main contraindications:

• severe intolerance to the active ingredient or other elements of the drug or other nitromidazole derivatives;
• lesions affecting the central nervous system (brain damage, epilepsy, multiple sclerosis);
• blood diseases or other hematological pathologies.

Side effects Tiberal

Among the side effects:

• lesions associated with the hematopoietic system and lymph: neutro- or leukopenia and signs of exposure to the bone marrow;
• disorders affecting the work of the NA: headaches, rigidity, ataxia, drowsiness and fatigue, and in addition, convulsions, tremors, disorientation in space, coordination disorder and polyneuropathy. Confusion, transient loss of consciousness and agitation are also noted;
• systemic disorders: chills, dyspnea, fever and systemic weakness;
• problems with the gastrointestinal tract: metal taste, diarrhea, taste upset, loss of appetite, vomiting, dry mouth, coated tongue, epigastric pain and nausea;
• symptoms associated with the hepatobiliary system: an increase in liver enzymes, jaundice, hepatotoxicity and a disorder of the biochemical level of hepatic function;
• immune lesions: signs of intolerance, including Quincke's edema and anaphylaxis;
• disorders affecting the subcutaneous layer of the epidermis: urticaria, itching, epidermal rashes and skin hyperemia;
• invasions with infections: exacerbation of candidiasis;
• others: violations associated with the work of the CVS (among them a decrease in blood pressure values), and darkening of the shade of urine.

Overdose

In case of poisoning, side effects of drugs with a more pronounced intensity can develop.

Symptomatic procedures are performed; the drug has no anitdote. In case of convulsions, diazepam should be administered to the patient.

Interactions with other drugs

It is forbidden to take alcoholic beverages during the period of therapy, as well as during the next at least 3 days after its end.

Ornidazole potentiates the activity of oral coumarin anticoagulants, which is why their dosage must be adjusted.

The use in combination with phenobarbital and other enzyme inducers reduces the term of the intra-serum circulation of ornidazole; at the same time, enzyme inhibitors (among them cimetidine), on the contrary, increase it.

Ornidazole prolongs the muscle relaxant effect of vecuronium bromide.

Storage conditions

Tiberal must be kept in a dark place, out of the reach of small children. Temperature indicators - no more than 30 ° С.

Shelf life

Tiberal can be used for a 5-year term from the date of manufacture of the medicinal product.

Analogs

Analogues of drugs are Novizol, Flagil with Naxogin, Ornisid and Orgil with Tiniba.