Isoniazid
IsoniazidPharmacological action
Is the basic representative of derivatives of the isonicotinic acid, found application as antituberculous remedies. Other preparations of this group (Ftivazidum, etc.) can be surveyed as derivatives of Hydrazidum of isonicotinic acid.
Isoniazid possesses high bacteriological activity concerning tuberculosis micobacteria (tuberculosis originators). On other widespread originators of infectious diseases it does not render the expressed chemotherapeutic action.
The preparation is well soaked up from a gastroenteric tract. The maximum concentration of a preparation in blood is found out through 1-4 h after intake; during 6-24 h after reception of a single dose in blood concentration (the concentration of medical products causing the termination of vital activity of bacteria of a tuberculosis) remains. The preparation easily gets through a hematoencephalic barrier (a barrier between blood and a brain tissue) and it is found out in various tissues and organism liquids. It is deduced mainly by kidneys.
Indications to Isoniazid application
Apply Isoniazid to treatment of all forms and localisations of an active tuberculosis at adults and children; it is most effective at fresh, acutely proceeding processes.
Prescribe in a combination with other antituberculous preparations. At a multi-infection it is necessary to accept simultaneously with Isoniazid other antibacterial preparations: antibiotics (a wide spectrum of action), Sulfanilamidums.
Way of application and dose
At appointment of Isoniazid and other preparations - Hydrazidum derivatives acids should be considered, that in an organism these preparations are inactivated (in full or in part lose biological activity) with different speed. Degree define under the maintenance of active Hydrazidum of isonicotinic acid in blood and urine. The faster the preparation is inactivated in blood, the more it it is required for maintenance to concentration in blood, therefore to patients in which organism there is a fast inactivation, give a preparation in a little bit big doses. To "fast inactivator" carry the patients allocating a day with urine to 10 % of active Isoniazid in relation to the accepted dose, and to "slow (weak)" - 10 % allocating more.
Apply Isoniazid inside, in a cavity formed owing to a necrosis of a tissue, intramusculary, intravenously, inhalationly.
Inside prescribe Isoniazid to adults and children in a daily dose of 5-15 mg to 1 kg of mass of a body in 1 - 3 receptions (after meal). The Daily dose establish individually depending on character and the form of disease, inactivation and shipping degree. Treatment long.
Intramusculary (and intravenously) Isoniazid enter at active forms of a tuberculosis if the patient experiences difficulties at intake (diseases of a gastroenteric tract, intolerance). To adults and teenagers enter 10 % a solution on 5-12 mg/kg a day within 2-5 months For reduction of side effects prescribe a pyridoxine which accept inside on 0,06-0,1 g (60-100 mg), simultaneously with an injection of Isoniazid or enter intramusculary on 0,1-0,125 g (100-125 mg) through 30 mines after an injection.
Intravenously enter Isoniazid to adults and teenagers at widespread forms of a pulmonary tuberculosis. Enter 10 % a solution on 0,01-0,015 g (10-15 mf) on 1 kg of mass of a body a day. Course of treatment - 30-150 injections (depending on efficiency and shipping). To the prevention and reduction of side effects apply a pyridoxine.
At intravenous introduction of Isoniazid of the patient should observe after an injection a confinement to bed during 1-1 1/2 h.
For preventive maintenance of a tuberculosis Isoniazid accept only inside on 5-10 mg/kg a day in 1-2 receptions; a preventive course - 2 months
Isoniazid Side effect
At application of Isoniazid and other preparations of this number (Ftivazidum, Methazidum, etc.) The headache, giddiness, nausea, vomiting, painful sensations in the field of heart, dermal allergic reactions can be observed. Euphoria (causeless complacent mood), dream deterioration, in rare instances - psychosis development, and also occurrence of a peripheric neuritis (an inflammation of peripheric nerves) with occurrence of an atrophy of muscles (reduction of mass of muscles with weakening of their function as a result of disturbance of a food of a muscular tissue) and a paralysis of extremities are possible. The medicinal hepatitis (the inflammation of a liver caused by reception of Isoniazid) is occasionally observed. Very seldom at treatment by Isoniazid at men become perceptible a gynecomastia (augmentation of mammary glands), at women - menorrhagias (uterine bleedings). At sick of an epilepsy attacks can become frequent. Usually side effects pass at reduction of a dose or a time break in preparation reception. For reduction of by-effects, besides a pyridoxine, are recommended Thiaminum solutions-intramusculary 1 ml of a solution of Thiamini chloridum of 5 % or 1 ml of a solution of Thiamini bromidum of 6 % (at paresthesias/feeling of a numbness in extremities/), Atriphosum.
Contraindications
An epilepsy and predilection to convulsive attacks; earlier transferred poliomyelitis (an infectious disease head and a spinal cord), disturbances of functions of a liver and the kidneys, the expressed atherosclerosis. It is not necessary to accept Isoniazid in a dose over 10 mg/kg at pregnancy, a pulmonary heart of III stage, an idiopathic hypertensia II - III stage, ischemic illness of heart, a widespread atherosclerosis, diseases of nervous system, a bronchial asthma, a psoriasis, an eczema in an exacerbation phase, a myxedema (sharp oppression of function of a thyroid gland). Intravenous introduction of Isoniazid is contraindicative at a phlebitis (an inflammation of veins).
Release forms
Tablets on 0,1; 0,2 or 0,3 g; a powder; 10 % a solution in ampoules on 5 ml.
Storage conditions
B.Poroshok's list - in well corked banks of orange glass; tablets - in the place protected from light; ampoules - at temperature not above +10 With. The solutions prepared from a powder can be stored at temperature not above +10 C no more 48 h.
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