Фтизоэтам® B6

General characteristics. Structure:

Active ingredients: 150 mg of an isoniazid, 400 mg of Ethambutolum of a hydrochloride, 15 mg of a pyridoxine of a hydrochloride.

Excipients: phosphate calcium dihydrate, povidone, кросповидон, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. The isoniazid has bactericidal effect on actively sharing Mycobacterium tuberculosis cells. The mechanism of its action consists in oppression of synthesis of the mikoliyevy acids which are a component of a cell wall of mycobacteria. For tuberculosis mycobacteria the minimum overwhelming concentration (MOC) makes 0,025 - 0,05 mg/l. The isoniazid possesses moderate action on slowly - and fast-growing atypical mycobacteria.

Ethambutolum. Ethambutolum - bacteriostatic drug, is effective concerning typical and atypical mycobacteria of tuberculosis. The mechanism of effect of drug is connected with disturbance of synthesis of RNA in bacterial cells, it suppresses synthesis of a cell wall, blocking inclusion in it of mikoliyevy acids. Ethambutolum is active in the relation quickly - and slow-growing atypical mycobacteria. MPK of Ethambutolum makes - 0,78-2,0 mg/l. On not tubercular pathogenic microorganisms Ethambutolum does not work.

Pyridoxine hydrochloride. Vitamin means. Participates in a metabolism. It is necessary for normal functioning of the central and peripheral nervous system. Antitubercular drugs cause a peripheral polyneuropathy which emergence can reduce a pyridoxine. In this regard the daily dose of vitamin raises to 60 mg. At a concomitant use of a pyridoxine inside with an isoniazid and Ethambutolum interaction of these drugs at the pharmacokinetic and microbiological levels is not observed.

Pharmacokinetics. Isoniazid. Reception of an isoniazid inside together with the drugs which are a part ^{of Ftizoetama®} of B6 does not influence the speed of its absorption from the digestive tract (DT). The isoniazid gets into many fabrics and liquids of an organism, including cerebrospinal fluid (SMZh). Time of achievement of the maximum concentration of drug in blood (TCmax) - 2 hours, the size Cmax - 6,6 mg/l, an elimination half-life (T1/2) - 5,8 hours. The isoniazid is acetylated and hydrolyzed in a liver. Acetylation is the main way of metabolism of an isoniazid. Speed of acetylation depends on specific features of the patient. Metabolites of an isoniazid have no antimicrobic activity.

Within 24 hours with urine 75-95% of the entered dose in the form of metabolites are removed (N-atsetilizoniazid, etc.). A part of an isoniazid is removed with urine in the changed look: to 12% at bystry acetylation and to 27% at slow acetylation. At the expressed renal failure at patients with slow acetylation drug accumulation is possible.

Ethambutolum. After reception ^{of Ftizoetama®} of B6 of Cmax of Ethambutolum reaches 6,4-7,6 mg/l. High Cmax of Ethambutolum is explained by delay of its excretion under the influence of an isoniazid. Drug Cmax in plasma (60%) is reached in 2 h. Ethambutolum is excreted with urine of 70% in not changed look; 30% in the form of aldehydic and carboxyl inactive metabolites. On average 25% of drug contact proteins of plasma.

Pyridoxine hydrochloride. It is soaked up quickly throughout a small intestine, the bigger quantity is absorbed in a jejunum. It is metabolized in a liver with formation pharmacological of active metabolites (пиридоксаль phosphate and пиридоксаминофосфат). Piridoksal phosphate contacts proteins of plasma for 90%. Well get into all fabrics; collects preferential in a liver, it is less - in muscles and the central nervous system (CNS).

Gets through a placenta, cosecretes with breast milk. T1/2 - 15-20 days. It is removed by kidneys.

Indications to use:

^{Фтизоэтам®} B6 is shown for treatment of all forms and localizations of tuberculosis caused by sensitive mycobacteria to an isoniazid and Ethambutolum. ^{Фтизоэтам®} B6 can be applied to chemoprophylaxis of tuberculosis and performing antirecurrent therapy.

Route of administration and doses:

^{The drug Ftizoetam® B6} is used inside after food, once a day. Dosing ^{of Ftizoetama®} of B6 is carried out on an isoniazid: for adults and children 12 years of 5-10 mg/kg of body weight are more senior. Drug is used daily in the period of an intensive care (3-4 months), in the subsequent time - every other day.

The general course dose ^{of Ftizoetama®} of B6 for everyone is individual and depends on the nature of a disease, efficiency of treatment and portability.

Features of use:

During treatment by drug patients have to abstain from alcohol intake.

In some cases, especially patients with attacks have gouts in the anamnesis, it is recommended to control periodically the level of uric acid in blood serum.

Ethambutolum can exert negative impact on sight. Sight is usually normalized after timely cancellation of Ethambutolum. In rare instances normalization of sight can happen within a year and more. It is necessary to check visual acuity of each eye separately and both eyes together; visual acuity is checked prior to treatment and periodically in the course of treatment. At any change of visual acuity patients should see a doctor at once. If decrease in visual acuity is revealed, drug is cancelled.

It is recommended to control the ALT and nuclear Heating Plant levels in plasma and to monthly estimate function of a liver. The isoniazid should be cancelled only in those cases if levels of transaminases more than by 3 times exceed the upper bound of norm as asymptomatic passing increase in level of liver enzymes which does not demand the termination of administration of drug is quite often noted. At development of acute or chronic hepatitis drug needs to be cancelled, in the latter case it is impossible to resume therapy by drug.

It is not recommended to drive the car and to work with the difficult equipment.

Side effects:

Isoniazid. From a nervous system: a headache, dizziness, it is rare - extraordinary 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 outside warmly - vascular system (CCC): heartbeat, increase in the arterial pressure (AP), stenocardia.

From the alimentary system: nausea, vomiting, gastralgia, toxic hepatitis.

Allergic reactions: skin rash, itch, hyperthermia, arthralgia.

Others: very seldom - a gynecomastia, a menorrhagia, tendency to bleedings and hemorrhages.

Ethambutolum. From a nervous system and sense bodys: weakness, a headache, dizziness, consciousness disturbance, a disorientation, a hallucination, a depression, peripheral neuritis (paresthesias in extremities, numbness, paresis, an itch), an optic neuritis (decrease in visual acuity, disturbance of color perception, generally green and red colors, color-blindness, scotoma).

From the alimentary system: a loss of appetite, a gastralgia, nausea, vomiting, an abnormal liver function - increase in activity of "hepatic" transaminases.

Allergic reactions: dermatitis, skin rash, itch, arthralgia, fever, anaphylaxis.

Others: hyperuricemia, exacerbation of gout.

Pyridoxine hydrochloride. Allergic reactions, hypersecretion of hydrochloric acid, numbness, emergence of feeling of a prelum in extremities - a symptom of "stockings" and "gloves", it is rare - skin rash, a skin itch.

Interaction with other medicines:

Isoniazid. The isoniazid slows down metabolism of some medicines, including Phenytoinum, carbamazepine, Valproatum. At co-administration with an isoniazid of a dose of the specified drugs it is recommended to reduce.

It is necessary to avoid simultaneous use of an isoniazid and Disulfiramum as it can lead to mental disorders. The mechanism of this interaction is not installed.

The isoniazid increases serumal concentration of carbamazepine and Phenytoinum, reduces concentration in blood of a ketokonazol and cyclosporine.

Antacids reduce absorption of an isoniazid.

Reduces efficiency of peroral contraceptive drugs, a glipizid, Tolbutamidum, theophylline, a tolazomid, B1 vitamin; strengthens side effects of Phenytoinum; suppresses removal of a triazolam, strengthens B1 vitamin excretion; reduces the maintenance of ions of zinc in blood, increases their excretion.

Alcohol intake against the background of therapy by an isoniazid can increase risk of developing of hepatitis.

Ethambutolum. Co-administration of Ethambutolum and the drugs possessing neurotoxic action can increase probability of development of an optic neuritis and peripheral neuritis.

Pyridoxine hydrochloride. A pyridoxine the hydrochloride weakens action a levodopa at their combined use. A pyridoxine the hydrochloride reduces risk of development of toxic effect of antitubercular drugs on the central and peripheral nervous system.

Contraindications:

^{Фтизоэтам®} B6 is contraindicated to children up to 12 years, to patients with hypersensitivity to an isoniazid, Ethambutolum and a pyridoxine. It is contraindicated at the epilepsy and other diseases which are followed by tendency to spasms, uncontrollable arterial hypertension, heavy coronary insufficiency, cirrhosis, acute hepatitises, a myxedema at an optic neuritis, a cataract, a diabetic retinopathy, bronchial asthma, psoriasis, a hyperuricemia, acute gout, a peptic ulcer of a stomach and a 12-perstny gut, pregnancy, a lactation.

With care to appoint drug to persons with a chronic renal failure.

Overdose:

Symptoms: nausea, vomiting, abdominal pains, jaundice, increase in level of liver enzymes, acute fluid lungs, consciousness disturbance, coma, spasms, breath disturbance, hyperglycemia, metabolic ketoacidosis.

Treatment: a gastric lavage with introduction in absorbent carbon, an artificial diuresis, general measures on maintenance of the vital functions, a hemodialysis.

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. Not to use after the expiry date specified on packaging. A period of validity - 2 years. 

Issue conditions:

According to the recipe

Packaging:

On 50 or 100 tablets in bank from polyethylene or in bank from polypropylene. Each can together with the application instruction is placed in a pack from a cardboard. On 500 or 1000 tablets in a package from a film polyethylene; a plastic bag together with the application instruction in a container from polyethylene or from polypropylene (for a hospital). On 25 cans on 100 tablets together with the equal number of application instructions place in a box from a cardboard (for a hospital).