Phthisoactive (Phthizoactiv)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceIsoniazid + PyridoxineIsoniazid + Pyridoxine
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  • Phthisoactive
    pills inwards 
    FARMASINTEZ, JSC (Irkutsk)     Russia
    • Dosage form: & nbsppills
    Composition:
    1 tablet contains:
    Active substances:
    Isoniazid 100 mg 150 mg 200 mg 300 mg 300mg
    Pyridoxine hydrochloride 5 mg 7.5 mg 10 mg 15 mg 60 mg
    Excipients:
    starch potato variety "Extra" 2.52 mg / 3.78 mg / 5.0 mg / 7.56 mg / 7.56 mg, povidone (medium-molecular weight polyvinylpyrrolidone, collidon 25) 1.08 mg / 1.62 mg / 2 , 1 mg / 3.24 mg / 3.24 mg, magnesium stearate 1.00 mg / 1.5 mg / 2.0 mg / 3.00 mg / 3.00 mg, silicon dioxide colloid (aerosil
    grade A-300) 0.20 mg / 0.30 mg / 0.40 mg / 0.60 mg / 0.60 mg, talc 0.20 mg / 0.30 mg / 0.40 mg / 0.60 mg / 0.60 mg.


    Description:
    For dosages of 100 mg + 5 mg, 200 mg + 10 mg, 300 mg + 15 mg, 300 mg + 60 mg: tablets are round, biconvex white or
    white with a yellowish tint of color.
    For dosage of 150 mg + 7.5 mg: tablets are round, biconvex, white or white with a yellowish tinge of color, with a risk on one side.
    Pharmacotherapeutic group:anti-tuberculosis drug
    ATX: & nbsp

    J.04.A.C.51   Isoniazid in combination with other drugs

    Pharmacodynamics:
    Isoniazid has a bactericidal effect on the actively dividing cells of Mycobacterium tuberculosis. The mechanism of its action is the inhibition of the synthesis of mycolic acids, which are a component of the cell wall of mycobacteria. For mycobacteria tuberculosis, the minimum inhibitory concentration of the drug is 0.025-0.05 mg / l. Isoniazid has a moderate effect on slowly and rapidly growing atypical mycobacteria.
    Pyridoxine (vitamin B6). Participates in the metabolism. It is necessary for the normal functioning of the central and peripheral nervous system. With tuberculosis infection, there is a deficiency of pyridoxine. In this regard, the daily dose of vitamin increases to 60 mg. With the simultaneous administration of pyridoxine inwards with isoniazid, lomefloxacin, pyrazinamide and ethambutol, no interaction of these drugs is observed at the pharmacokinetic and microbiological levels. Reduces the neurotoxicity of anti-tuberculosis drugs.
    Pharmacokinetics:
    Isoniazid. Taking isoniazid in together with pyridoxine, which is a part of "Phthisoactive", does not affect the rate of its absorption from the gastrointestinal tract. Penetrates isoniazid in many tissues and fluids, including cerebrospinal fluid. Time to reach the maximum concentration of the drug in the blood (TCam) - 2 hours, the value of Cmax -6.6 mg / l, half-life (T1 / 2) - 5.8 hours. Isoniazid practically does not bind to plasma proteins. Isoniazid up to 80-90% is excreted in the urine and 10% with feces during the day. The main products of isoniazid metabolism are N-acetylisoiniazide and isonicotinic acid.
    Pyridoxine absorbed rapidly throughout the small intestine, a larger amount is absorbed in the jejunum. Metabolised in the liver with an educated pharmacologically active metabolites (pyridoxal phosphate and pyridoxamino phosphate). Pyridoxal phosphate with plasma proteins binds to 90%. It penetrates well into all tissues; accumulates mainly in the liver, less - in the muscles and central nervous system. Penetrates through the placenta, is secreted with breast milk. The half-life is 15-20 days. It is excreted by the kidneys.
    Indications:
    Tuberculosis (any localization, in adults and children, treatment and prevention, including as part of combination therapy).

    Contraindications:Hypersensitivity to any component of the drug. Medicinal hepatitis and hepatic insufficiency (against the background of the previous treatment of isoniazid), liver disease in the acute stage, convulsive syndrome, children under 3 years old.
    Carefully:peptic ulcer of the stomach and duodenum,ischemic heart disease, alcoholism, hepatic insufficiency, renal failure, convulsive seizures, age over 35, depleted patients, cancellation of isoniazid therapy in history, peripheral neuropathy, HIV infection, decompensated diseases of the cardiovascular system (angina, hypertension), hypothyroidism .
    Pregnancy and lactation:When lactation and pregnancy is not prescribed in a dose of more than 10 mg / kg for isoniazid.
    Dosing and Administration:
    Inside, after eating, 600-900 mg / day isoniazid in 1-3 divided doses, the maximum single dose - 600 mg isoniazid, daily - 900 mg isoniazid; children older than 3 years - 5-15 mg / kg / day isoniazid, the frequency of admission -1 -2 times a day, the maximum dose - 500 mg / day isoniazid.
    For the prevention of adults and children older than 3 years - inside, 5-10 mg / kg / day of isoniazid in two divided doses per day for 2 months. During pregnancy and severe forms of pulmonary heart failure, severe atherosclerosis, ischemic heart disease and hypertension should not be prescribed in doses greater than 10 mg / kg isoniazid.
    Side effects:
    From the nervous system: headache, dizziness, paresthesia, numbness of the extremities, peripheral neuropathy; rare - excessive fatigue or weakness, irritability, euphoria, insomnia, optic neuritis, polyneuritis, toxic psychosis, emotional lability, depression, convulsions, toxic neuropathy, memory impairment.
    From the cardiovascular system: heart palpitations, angina, increased blood pressure.
    From the digestive system: nausea, vomiting, gastralgia; an increase in the activity of alanine aminotransferase and aspartate aminotransferase, hypobilirubinemia, bilirubinuria, jaundice; rarely - toxic hepatitis, incl. with a lethal outcome.
    From the hematopoiesis: agranulocytosis, hemolytic, sidroblastic or aplastic anemia, thrombocytopenia, eosinophilia. Allergic reactions: skin rash (cortex, maculopapular, exfoliative, purpura), itching, fever, arthralgia, lymphadenopathy, vasculitis.
    From the side of metabolism: hypovitaminosis pyridoxine (vitamin B6), pellagra, hyperglycemia, metabolic acidosis, gynecomastia.Other: very rarely - menorrhagia, a tendency to bleeding and hemorrhage.
    Associated with pyridoxine.
    Allergic reactions, hypersecretion of hydrochloric acid, numbness, the appearance of a feeling of compression in the limbs - a symptom of "stocking" and "gloves", rarely - a skin rash, itching of the skin.

    Overdose:
    Symptoms occur within 0.5-3 h after administration: nausea, vomiting, dizziness, blurred speech, visual impairment, visual hallucinations. With severe overdose: respiratory distress syndrome, central nervous system depression rapidly shifting from stupor to coma, severe non-curable convulsions, severe metabolic acidosis, acetonuria, hyperglycemia. Treatment: in severe overdose (80-150 mg / kg), insufficient therapy leads to neurotoxicity with a fatal outcome. With adequate therapy, the prognosis is favorable.
    With asymptomatic overdose: Activated carbon, gastric lavage. When taken in a dose of more than 80 mg / kg in the same dose intravenously administered pyridoxine, if the dose of isoniazid is unknown, then 5 g of pyridoxine are administered intravenously to adults, 80 mg / kg for children within 30-60 minutes.At clinical displays: adequate ventilation, maintenance of activity of cardiovascular system, prevention of aspiration of gastric contents. If the dose of isoniazid is known, the same amount of pyridoxine is administered intravenously bolus within 3-5 minutes. If the dose of isoniazid is unknown, then 5 g of pyridoxine are injected intravenously, 80 mg / kg for children. If the convulsions do not stop, the dose can be repeated. It is rare to prescribe a dose of more than 10 g. The maximum safe dose of pyridoxine in case of an overdose with isoniazid is unknown. If pyridoxine is ineffective, diazepam.
    It is necessary to control the content of electrolytes, urea, glucose and partial pressure of gases in the blood. With the development of metabolic acidosis sodium hydrogen carbonate can enhance hypercapnia (continuous monitoring is necessary).
    Dialysis is prescribed if seizures and acidosis are not stopped by pyridoxine, diazepam and sodium bicarbonate.

    Interaction:
    Isoniazid
    When combined with paracetamol, hepatotoxicity and nephrotoxicity increase; isoniazid induces a system of cytochrome P450,as a result of which the metabolism of paracetamol increases to toxic products. Ethanol increases the hepatotoxicity of isoniazid and accelerates its metabolism. Reduces the metabolism of theophylline, which can lead to an increase in its concentration in the blood.
    Reduces metabolic transformations and increases the concentration in blood of Alfrntanyl. Cycloserine and disulfiram enhance the adverse central effects of isoniazid. Increases hepatotoxicity of rifampicin. Combination with pyridoxine reduces the risk of peripheral neuritis. Caution should be combined with potentially neuro-, hepato- and nephrotoxic drugs because of the risk of side effects. Enhances the action of coumarin and indanedione derivatives, benzodiazepines, carbamazepine, theophylline, as it reduces their metabolism due to the activation of cytochrome P450 isoenzymes. Glc cocorticosteroids accelerate metabolism in the liver and reduce active concentrations in the blood. Suppresses the metabolism of phenytoin, which leads to an increase in its concentration in the blood and increase the toxic effect (correction of the dosing regimen of phenytoin,especially in patients with slow acetylation of isoniazid); should be considered when administered as an anticonvulsant with an overdose of isoniazid. Antacid drugs (especially aluminum-containing drugs) slow down absorption and reduce the concentration of isoniazid in the blood (antacids should be taken no earlier than 1 hour after taking isoniazid). When used simultaneously with enflurane isoniazid can increase education; an inorganic fluoride metabolite with a nephrotoxic effect. When taken together with rifampicin reduces the concentration of ketoconazole in the blood. Increases the concentration of valproic acid in the blood (monitoring of valproic acid concentration is required, correction of the dosing regimen may be required).
    Pyridoxine weakens the action of levodopa when combined. Pyridoxine reduces the risk of developing toxic effects of anti-tuberculosis drugs on the central and peripheral nervous system.
    Special instructions:
    To slow the development of microbial resistance is prescribed together with other antituberculous drugs.
    In some cases, fatal drug hepatitis develops during treatment, which may occur even after several months of use. The risk rises with age (the highest frequency in the age group is 35-64 years), especially with daily consumption of ethanol. Therefore, every month it is necessary to monitor the function of the liver, people over 35 years of age, the function of the liver is further examined before treatment. In addition to ethanol absorption, additional risk factors include chronic liver disease, parenteral use of any medicines and the postpartum period; under these circumstances, monitoring of liver function (laboratory and clinical) should be conducted more often. Patients should be informed of the need to report any manifestations of liver damage (unexplained anorexia, nausea, vomiting, darkening of the urine, jaundice, rash, paresthesia of the hands and feet, weakness, fatigue or fever lasting more than 3 days, abdominal pain, especially in the right upper quadrant ). AT ; In these cases, the drug is immediately withdrawn. Patients who have previously undergone isoniazid hepatitis are prescribed alternative antituberculous drugs.If it is necessary to resume therapy, it begins after complete resolution of clinical and laboratory signs of hepatitis with subsequent monitoring of liver function. With any signs of relapse, the drug is immediately withdrawn. In patients with acute liver disease, the phthisoactive prophylaxis should be postponed.
    In connection with the different metabolic rate before application of Phtisoactive, it is expedient to determine the rate of inactivation of isoniazid by its content in blood and urine. With rapid inactivation, the drug is used in higher doses.
    During the treatment, cheese (especially Swiss and Cheshire), fish (especially tuna, sardinella, skipjack) should be avoided, since the simultaneous use of them with isoniazide may cause reactions (skin hyperemia, itching, a sensation of heat or cold, palpitation, increased sweating, chills, headache, dizziness) associated with inhibition of monoamine oxidase (MAO) and diaminoxidase activity and leading to a disruption of the metabolism of tyramine and histamine contained in fish and cheese.
    It should be borne in mind that isoniazid can cause hyperglycemia with secondary glucosuria; tests with the reduction of copper ions can be false positive, and the enzyme tests for glucose drug does not affect. Simultaneous use of alcohol contributes to the intensification of hepatotoxic reactions.
    Laboratory indices of alanine aminotransferase and aspartate aminotransferase, serum bilirubin concentration can transiently increase without clinical manifestations
    With severe liver damage pyridoxine in large doses can cause a deterioration in its function. When determining urobilinogen using Ehrlich's reagent, it can distort the results.
    Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:
    Tablets 100 mg + 5 mg, 150 mg + 7.5 mg, 200 mg + 10 mg, 300 mg + 15 mg, 300 mg +60 mg.


    Packaging:
    Primary packaging of medicinal product. For 10 tablets in a contoured package of polyvinylchloride film and aluminum foil printed lacquered.For 100, 500 or 1000 tablets (for hospitals) in a can of polymer with a lid pulled with the control of the first opening. Free space is filled with cotton wool.
    Secondary packaging of medicinal product. For 5 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.
    Banks, together with an equal number of instructions for use, are placed in a group package.
    Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:
    4 years. Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-003969/10
    Date of registration:06.05.2010
    The owner of the registration certificate:FARMASINTEZ, JSC (Irkutsk) FARMASINTEZ, JSC (Irkutsk) Russia
    Manufacturer: & nbsp
    Information update date: & nbsp27.05.2014
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