Pro-tube-3

General characteristics. Structure:

Active ingredients: 75,0 mg of an isoniazid, 150,0 mg of rifampicin, 400,0 mg of Pyrazinamidum; 150,0 mg of an isoniazid, 225,0 mg of rifampicin, 750,0 mg of Pyrazinamidum; 300,0 mg of an isoniazid, 450,0 mg of rifampicin, 1000 mg of Pyrazinamidum.

The combined antitubercular drug operating bakteritsidno on Mycobacterium tuberculosis at different stages of its development.

Pharmacological properties:

Pharmacodynamics. The isoniazid oppresses synthesis of mikoliyevy acids of a cell wall of mycobacteria of tuberculosis, has specific activity concerning MBT, fast-growing extracellular and intracellular, including strains, resistant to other drugs. Rifampicin - a semi-synthetic antibiotic, blocks a DNA-dependent RNA polymerase, is active concerning fast-growing, preryvistorastushchy, intracellular and extracellular activators. Pyrazinamidum affects intracellular mycobacteria, well gets into the centers of tubercular defeat. Its activity does not decrease in acid medium of caseous masses. Depending on a dose renders bactericidal or bacteriostatic effect.

Pharmacokinetics. The isoniazid is well soaked up in a GIT. Meal slows down absorption and reduces bioavailability. Cmax in 1-2 hours after reception, semi-removal time – of 30 minutes till 5 o'clock, depending on the acetylation speed (specific features of an organism). Well gets into various fabrics and liquids of an organism. It is metabolized in a liver. At the same time the active metabolite (pirazinoyevy acid) is formed. It is removed by kidneys generally in the form of inactive metabolites. Rifampicin is soaked up well and quickly. Meal reduces drug absorption. Cmax in 2-2.5 hours. It is quickly distributed on bodies and fabrics, gets into a bone tissue. Gets through a placenta and it is allocated with breast milk. It is metabolized in a liver. T1/2 depends on the accepted dose and makes 2.5-5 h. It is removed with bile and kidneys. At patients with abnormal liver functions increase in concentration of rifampicin in plasma and lengthening of T1/2 is noted. Pyrazinamidum is well soaked up in a GIT. Cmax in 1-2 hours. Well gets into various fabrics and liquids of an organism including in cerebrospinal fluid. Elimination half-life of 8-9 hours. It is allocated with kidneys.

Indications to use:

Tuberculosis of any localization, as a part of a combination therapy in an intensive phase and/or in a phase of continuation of treatment at an out-patient stage.

Route of administration and doses:

Inside, for 1-2 h to food in 1 reception.

At the body weight of the patient less than 40 kg on 1 таб. with a dose of active components of 150 mg + 750 mg + 225 mg.

At the body weight of sick from 40 to 50 kg on 1 таб. with a dose of active components of 300 mg + 1000 mg + 450 mg.

At the body weight of the patient from 50 kg to 64 kg on 4 таб. with a dose of active components of 75 mg + 400 mg + 150 mg.

At the body weight of the patient more than 65 kg on 2 таб. with a dose of active components of 150 mg + 750 mg + 225 mg.

To children of 10-15 mg/kg/days in terms of rifampicin, but no more than 600 mg/days. A course of treatment - 2 months, with further reception of combinations of an isoniazid and rifampicin or an isoniazid and Ethambutolum.

Features of use:

The combination with B6 vitamin is possible. At increase in activity of "hepatic" transaminases drug is cancelled. Resume treatment after normalization of indicators.

Rifampicin paints skin, a phlegm, sweat, kcal, the lacrimal liquid, urine, soft contact lenses in orange-red color. Pyrazinamidum worsens the course of gout and a diabetes mellitus, control of function of kidneys, uric acid is necessary. In case of a resistant hyperuricemia and an exacerbation of gouty arthritis treatment is cancelled.

During treatment it is not necessary to apply the bromsulfaleinovy test (false positive results). At long reception carry out control of function of a liver, kidneys, pictures of peripheral blood and survey of the ophthalmologist. The ethanol use is forbidden.

In the course of treatment additional reception of vitamin D for prevention of disturbances of exchange of calcium and phosphorus is recommended. At appointment in recent weeks pregnancies perhaps puerperal bleeding at mother and bleeding at the newborn (treatment: vitamin K). Women during treatment are recommended to use non-hormonal methods of contraception.

Side effects:

Isoniazid. From a nervous system: a headache, dizziness, it is rare - excessive fatigue or weakness, irritability, euphoria, sleeplessness, paresthesias, numbness of extremities, a peripheral neuropathy, an optic neuritis, a polyneuritis, psychoses, change of mood, a depression. At patients with epilepsy attacks can become frequent. From CCC: heartbeat, stenocardia, increase in the ABP. From the alimentary system: nausea, vomiting, gastralgia, toxic hepatitis. Allergic reactions: skin rash, itch, hyperthermia, arthralgia. Other: very seldom – a gynecomastia, a menorrhagia, tendency to bleedings and hemorrhages.

Rifampicin. From the alimentary system: nausea, vomiting, diarrhea, loss of appetite, erosive gastritis, pseudomembranous coloenteritis; increase in activity of "hepatic" transaminases in blood serum, a hyperbilirubinemia, hepatitis. Allergic reactions: urticaria, eosinophilia, Quincke's disease, bronchospasm, arthralgia, fever. From a nervous system: headache, decrease in visual acuity, ataxy, disorientation. From an urinary system: нефронекроз, intersticial nephrite. Other: leukopenia, dysmenorrhea, induction of a porphyria, myasthenia, hyperuricemia, exacerbation of gout. At irregular reception or when resuming treatment after a break the grippopodobny syndrome (fever, a fever, a headache, dizziness, a mialgiya), skin reactions, hemolitic anemia, a Werlhof's disease, an acute renal failure are possible.

Pyrazinamidum. From the alimentary system: nausea, vomiting, diarrhea, "metal" smack in a mouth, an abnormal liver function (a loss of appetite, morbidity of a liver, a hepatomegalia, jaundice, a yellow hepatatrophia); aggravation of a round ulcer. From TsNS: dizziness, headache, sleep disorders, hyperexcitability, depressions; in some cases - hallucinations, spasms, confusion of consciousness. From bodies of a hemopoiesis and system of a hemostasis: thrombocytopenia, sideroblastny anemia, vacuolation of erythrocytes, porphyria, hypercoagulation, splenomegaly. From a musculoskeletal system: arthralgia, mialgiya. From an urinary system: dysuria, intersticial nephrite. Allergic reactions: skin rash, small tortoiseshell. Other: hyperthermia, acne, hyperuricemia, exacerbation of gout, photosensitization, increase in concentration of serumal Fe.

Interaction with other medicines:

The isoniazid increases concentration of Phenytoinum in blood, reduces efficiency of the peroral combined contraceptive HP, a glipizid, Tolbutamidum, theophylline, a tolazomid, thiamin; strengthens side effects of Phenytoinum; suppresses removal of a triazolam; reduces the maintenance of Zn2 + in blood, increases its removal.

Antacids, opiates, anticholinergic HP and кетоконазол reduce bioavailability of rifampicin. The isoniazid and/or Pyrazinamidum increase the frequency and weight of abnormal liver functions in a combination with rifampicin at patients with a liver disease in the anamnesis.

Rifampicin reduces activity of peroral anticoagulants, peroral hypoglycemic HP, hormonal contraceptives, drugs of a foxglove, antiarrhytmic HP, GKS, Phenytoinum, hexobarbital, a nortriptilin, benzodiazepines, sex hormones, theophylline, chloramphenicol, a ketokonazol, cyclosporine A, beta adrenoblockers, BMKK, enalapril, Cimetidinum.

Rifampicin causes induction of fermental systems of a liver, accelerates metabolism. Antacids reduce absorption of an isoniazid. Pyrazinamidum increases concentration of an isoniazid in blood serum, slowing down its removal.

Strengthens action of an ofloksatsin and lomefloksatsin. At reception together with rifampicin the risk of development of hepatotoxic reactions increases.

Contraindications:

Hypersensitivity, jaundice, acute diseases of a liver of various genesis, pulmonary heart of the II-III Art.; hyperuricemia, gout; purpura; pregnancy (I trimester); lactation period.

Overdose:

Isoniazid. Symptoms: dizziness, a dysarthtia, slackness, a disorientation, a hyperreflexia, a peripheral polyneuropathy, an abnormal liver function, a metabolic acidosis, a hyperglycemia, a glucosuria, a ketonuria, spasms (in 1-3 h after drug use), a coma. Treatment: see the Isoniazid.

Rifampicin. Symptoms: fluid lungs, lethargy, confusion of consciousness, spasm. Treatment: see rifampicin.

Pyrazinamidum. Symptoms: an abnormal liver function, strengthening of expressiveness of side effects from TsNS. Treatment: symptomatic.

 

Storage conditions:

List B. In the dry, protected from light place at a temperature not over 25 ºС.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, on 100 or 500 tablets in bank of polymeric.