Tiberal

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

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

Indications Tiberal

It is used for trichomoniasis, amebiasis or giardiasis.

Release form

The medicine is released in the form of tablets - 10 pieces in a cell package; there is 1 such package in a pack.

Pharmacodynamics

It demonstrates activity against vaginal trichomonas, dysenteric amoeba, Giardia intestinalis, and also against individual anaerobes (clostridia, bacteroides, fusobacteria) and anaerobic cocci.

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

At the same time, 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 in the gastrointestinal tract. The average absorption rate is 90%. The drug reaches the intraplasmic Cmax level within 3 hours.

Distribution processes.

The protein synthesis rate of ornidazole is 13%. The active component enters the cerebrospinal fluid and other fluids, as well as into tissues.

Plasma values of the drug are within 6-36 mg/l (this is the optimal level when using the drug). With repeated use of Tiberal (with a 12-hour interval) in a portion 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 such metabolic elements as 2-hydroxymethyl and α-hydroxymethyl. These components have weaker activity against vaginal trichomonads and anaerobes (in comparison with unchanged ornidazole).

Excretion.

The half-life is 13 hours. With a single dose of the drug, 85% of the dose 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 taken orally, after meals.

Treatment of trichomoniasis.

Tablets with a volume of 0.5 g are used in regimens with a single dose or 5-day treatment.

It is necessary to take into account that the introduction of ornidazole can provoke some disorders (heat, redness, vomiting, numbness and nausea; as well as tinnitus or hypotension). Also, it is forbidden to drink alcohol for at least 3 days after using the drug.

When using the medicine once, you should take a dosage of 1.5 g (3 tablets per dose, in the evening). During a 5-day course, take 2 tablets per day (1 in the morning, and the 2 in the evening).

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

The size of a single daily dose for a child is 25 mg/kg.

Use in amebiasis.

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

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

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

Therapy for giardiasis.

A 1-2-day therapy cycle is carried out. Adults and children weighing more than 35 kg take 3 tablets per day (for 1 evening use). The daily portion size for children weighing less than 35 kg is 40 mg/kg.

Use in individuals with liver failure.

In severe cases of the disorder, the interval between medication administration should be doubled.

• Application for children

The medication can be used in pediatrics.

Use Tiberal during pregnancy

During experimental testing of the drug, no toxic or teratogenic effects on the fetus were observed.

Due to the lack of controlled tests of the drug involving pregnant women, its use in the early stages of pregnancy or during breastfeeding is permitted only in the presence of strict indications, in cases where the probable benefit from taking Tiberal is more expected than the risks of negative consequences for the fetus/infant.

Contraindications

Main contraindications:

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

Side effects Tiberal

Side effects include:

• lesions associated with the hematopoietic system and lymph: neutro- or leukopenia and signs of impact on the bone marrow;
• disorders affecting the functioning of the nervous system: headaches, rigidity, ataxia, drowsiness and fatigue, as well as 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 gastrointestinal function: metallic taste, diarrhea, taste disorder, loss of appetite, vomiting, xerostomia, coated tongue, pain in the epigastric region and nausea;
• symptoms related to the hepatobiliary system: increased liver enzyme levels, jaundice, hepatotoxicity and abnormal biochemical liver function;
• immune disorders: signs of intolerance, including Quincke's edema and anaphylaxis;
• disorders affecting the subcutaneous layer with the epidermis: urticaria, itching, epidermal rashes and skin hyperemia;
• invasions with infections: exacerbation of candidiasis;
• Others: disorders associated with the functioning of the cardiovascular system (including a decrease in blood pressure) and darkening of the urine color.

Overdose

In case of poisoning, more severe side effects of the drug may develop.

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

Interactions with other drugs

It is prohibited to consume alcoholic beverages during the therapy period, as well as for at least 3 days after its completion.

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

Use in combination with phenobarbital and other enzyme inducers reduces the intraserum circulation term of ornidazole; at the same time, enzyme inhibitors (including cimetidine), on the contrary, increase it.

Ornidazole prolongs the muscle relaxant effect of vecuronium bromide.

Storage conditions

Tiberal should be stored in a dark place, out of the reach of small children. Temperature indicators - no more than 30 ° C.

Shelf life

Tiberal can be used for a period of 5 years from the date of manufacture of the medicinal product.

Analogues

Analogues of the drug are the medications Novizol, Flagyl with Naxodgin, Ornisid and Orgil with Tiniba.