Ftizamax (Ftizamax)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceIsoniazid + Pyrazinamide + RifampicinIsoniazid + Pyrazinamide + Rifampicin
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    FARMASINTEZ, JSC (Irkutsk)     Russia
  • Ftizamax
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    McLeodz Pharmaceuticals Co., Ltd.     India
    • Dosage form: & nbspdispersible tablets
    Composition:
    1 tablet contains:
    Active substances: Isoniazid 30.0 mg / 150.0 mg Pyrazinamide 150.0 mg / 375.0 mg Rifampicin 60.0 mg / 150.0 mg
    Excipients: cellulose microcrystalline (25.0 mg / 105.5 mg), crospovidone (15.0 mg / 0), crospovidone (type A) (0 / 35.0 mg), povidone-KZO (5.0 mg / 9.5 mg), shellac (1.0 mg / 2.0 mg), croscarmellose sodium (7.0 mg / 15.0 mg), aspartame (2.0 mg / 3.5 mg), magnesium stearate (2.0 mg / 10.0 mg), a strawberry flavoring (3.0 mg / 4.5 mg).

    Description:
    Tablets with a dosage of 30 mg + 150 mg + 60 mg: Round flat tablets are orange-brown in color, with dark and light impregnations, with a facet on both sides, with a weak characteristic odor.
    Tablets with a dosage of 150 mg + 375 mg + 150 mg: Biconvex tablets of capsular form are orange-brown in color, with dark and light impregnations, with a smooth surface on both sides, with a weak characteristic odor.
    Pharmacotherapeutic group:Anti-tuberculosis means combined
    ATX: & nbsp

    J.04.A.M   Combinations of antituberculous drugs

    J.04.A.M.05   Isoniazid in combination with pyrazinamide and rifampicin

    Pharmacodynamics:
    The drug Ftizamax is a combined antituberculous drug containing fixed amounts of isoniazid, pyrazinamide and rifampicin, is active against Mycobacterium tuberculosis at various stages of its development. The combined use of active substances included in the preparation reduces the risk of resistance of mycobacteria tuberculosis. Pharmacodynamics
    Isoniazid.
    Isoniazid has a bactericidal effect on the actively dividing cells of Mycobacterium tuberculosis, inhibiting the synthesis of mycolic acids, which are a component of the cell wall of mycobacteria. For Mycobacterium tuberculosis, the minimum inhibitory concentration (MIC) of isoniazid is 0.05-0.025 mg / L.
    Pyrazinamide acts bactericidal on intracellular mycobacteria, as well as Micobacterium tuberculosis at different stages of its development, it penetrates well into the centers of tuberculous lesion. The minimum inhibitory concentration (MIC) of pyridinamide is 20 mg / l. Pyrazinamide does not affect atypical mycobacteria.
    Rifampicin - broad-spectrum antibiotic, inhibits DNA-dependent RNA polymerase. With tuberculosis rifampicin has bactericidal action, both on intracellular and extracellular microorganisms.When monotherapy is characterized by rapid development of resistance of mycobacteria.
    Pharmacokinetics:
    Isoniazid. Isoniazid quickly and completely absorbed when ingested, food reduces absorption and bioavailability, the value of which is greatly influenced by the effect of "first passage" through the liver. The value of the maximum concentration in the blood plasma after ingestion of a single dose of 300 mg - 3-7 μg / ml. The connection with proteins is insignificant - up to 10%. The volume of distribution is 0.57-0.76 l / kg. Well distributed throughout the body, penetrating all tissues and fluids, including cerebrospinal, pleural, ascites; high concentrations are created in the lung tissue, kidneys, liver, muscles, saliva and sputum. Penetrates through the placental barrier and into breast milk. It is metabolized in the liver by acetylation with the formation of inactive products. The liver is acetylated with N-acetyltransferase to form N-acetylisoiniazide, which is then converted to isonicotinic acid and monoacetylhydrazine, which has a hepatotoxic effect by forming a cytochrome P450 system upon N-hydroxylation of the active intermediate metabolite.The rate of acetylation is genetically determined; in people with "slow" acetylation, there is little N-acetyltransferase. Is the inducer of the isoenzyme CYP2E1. The half-life (T1 / 2) for "fast acetylators" is 0.5-1.6 hours; for "slow" - 2-5 hours. In case of renal insufficiency, Tm can increase to 6.7 hours. The value of T1 / 2 varies considerably depending on the individual intensity of the acetylation processes, the average value of T1 / 2 is 3 hours (ingestion of 600 mg) and 5.1 hours (900 mg). With the course of admission, T \ a is shortened to 2-3 hours. It is excreted mainly by the kidneys: within 75 hours 75-95% of the drug is excreted in the form of inactive metabolites - N-acetylisiniazide and isonicotinic acid. Small amounts are excreted with feces. Isoniazid is removed from the blood during hemodialysis. Passes through the hematoplacental barrier, is determined in fetal blood plasma at concentrations comparable to or higher than the concentration in the mother's blood plasma. Perhaps the emergence of myelomeningocele and hypospadias, hemorrhages in the fetus, may further lead to a delay in the psychomotor development in the child. An animal embryotoxic effect was shown in animal experiments.Penetrates into breast milk, reaching concentrations comparable to the concentration in the blood plasma. The child receives 0.75-2.3% of the dose taken by the mother. The elderly are more likely to develop hepatitis (2.6% of patients, compared with 0.3% - young people); the risk of peripheral neuritis is higher in people older than 65, pregnant women with diabetes, chronic renal failure, alcoholism, and people taking anticonvulsants.
    Pyrazinamide. Quickly and completely absorbed in the gastrointestinal tract with reaching the maximum concentration in the plasma after 1-2 hours. The connection with plasma proteins is 10-20%. It penetrates well into tissues and organs. Metabolised in the liver, where an active metabolite, pyrazinic acid, is first formed, which later becomes an inactive metabolite, 5-hydroxypyrazinic acid. The half-life is 8-9 hours. It is excreted by the kidneys: in unchanged form - 3%, in the form of pyrazinic acid - 33%, in the form of other metabolites - 36%. Removed during hemodialysis. Pyrazinamide in small amounts excreted in breast milk.
    Rifampicin. Absorption - fast, eating reduces the absorption of the drug.When administered on an empty stomach 600 mg the maximum concentration (Cmax) - 10 μg / ml is achieved after 2-3 hours. In case of reception with absorption of rifampicin, decreases by 30%. Approximately 60-80% of the dose is associated with plasma proteins. Quickly distributed to organs and tissues (the highest concentration in the liver and kidneys), penetrates into the bone tissue, the concentration in the saliva - 20% of the concentration in the plasma. The apparent volume of distribution is 1.6 l / kg in adults and 1.1 l / kg in children. Penetrates through the placenta (concentration in fetal plasma - 33% of the concentration in the mother's plasma) and excreted in breast milk (breast-fed children receive about 1% of the dose of the drug). Metabolised in the liver with the formation of pharmacologically active metabolite - 25-O-deacetyltrifampicin. After several days of intake, the bioavailability decreases and the half-life (T1 / 2) after repeated administration of 600 mg is shortened to 1-2 hours. It is excreted primarily with bile, 80% - in the form of a metabolite; kidneys - 20%. The amount of rifampicin excreted by the kidney in unchanged form depends on the value of the dose taken and is 4-20% of the dose taken.
    Indications:Tuberculosis (any localization in the first period of intensive treatment).
    Contraindications:
    Hypersensitivity to the drug.
    Pulmonary heart failure of II - III degree.
    Dysfunction of the liver.
    Acute liver disease, jaundice, acute hepatitis.
    Impaired renal function.
    Gout, hyperuricemia.
    Purpura.
    Phenylketonuria.
    Pregnancy (I trimester), lactation.
    Children weighing less than 7 kg.

    Carefully:
    During pregnancy.
    The elderly.
    With chronic alcoholism and psychosis.

    Pregnancy and lactation:
    The appointment is possible only if absolutely necessary and under strict medical supervision. Contraindicated in the first trimester of pregnancy. Pregnant women in the II and III trimesters can be prescribed if the expected benefit to the mother exceeds the risk to the fetus.
    When used in the last weeks of pregnancy, it is possible to develop postpartum hemorrhage in the mother or bleeding in a newborn.
    Application in the period of breastfeeding. The decision on the abolition of breastfeeding or the cessation of drug treatment should be taken taking into account the value of treatment with the drug for the mother.

    Dosing and Administration:
    It is taken orally 1-2 hours before meals, usually once a day at a dose, depending on the body weight and age of the patient.
    The required number of tablets of the drug Ftizamax (as directed by a doctor) is dissolved in one glass of boiled water at room temperature immediately before taking. Shake before use.
    The daily dose of the drug and the duration of treatment is determined only by the doctor. The dose of the drug is calculated from rifampicin:
    Adults with a body weight, less than 50 kg - 450 mg per day, 50 kg or more - 600 mg per day. Children-10-15 mg / kg per day, the maximum daily dose - 450 mg.
    It is possible to use the drug in combination with other anti-TB drugs.

    Side effects:
    Side effects in the treatment of the drug Ftizamax determined by its constituent active substances.
    Isoniazid.
    From the nervous system: headache, dizziness, rarely (> 1/10000, <1/1000) - excessive fatigue or weakness, irritability, euphoria, insomnia, paresthesia, numbness of limbs, peripheral neuropathy, optic neuritis, polyneuritis, psychosis, mood change, depression, memory impairment. Seizures can occur in patients with epilepsy.
    From the side of the cardiovascular system: heart palpitations, angina, increased blood pressure.
    From the digestive system: gastralgia, nausea, vomiting, toxic hepatitis, including fatal, increased activity of liver transaminases, hyperbilirubinemia, bilirubinemia, jaundice.
    From the hematopoiesis: agranulocytosis, hemolytic, sideroblastic or aplastic anemia, thrombocytopenia, eosinophilia.
    Allergic reactions: skin rash, itching, hyperthermia, arthralgia, lymphadenopathy, vasculitis.
    From the side of metabolism: hypovitaminosis pyridoxine hydrochloride (vitamin Bb), pellagra, hyperglycemia, metabolic acidosis.
    Other: gynecomastia in men and menorrhagia in women, a tendency to bleeding and hemorrhage.

    Pyrazinamide.
    From the digestive system: nausea, vomiting, diarrhea, "metallic" taste in the mouth, impaired liver function (decreased appetite, liver soreness, hepatomegaly, jaundice, yellow atrophy of the liver); exacerbation of peptic ulcer.
    From the nervous system: dizziness, headache, sleep disturbances, increased excitability, depression; very rarely (<1/10000) - hallucinations, convulsions, confusion.
    On the part of the organs of hematopoiesis and the system of hemostasis: thrombocytopenia, sideroblastic anemia, erythrocyte vacuolization, porphyria, hypercoagulation, splenomegaly.
    From the musculoskeletal system: arthralgia, myalgia. From the side of the urinary system: dysuria, interstitial nephritis.
    Allergic reactions: skin rash, hives.
    Other: hyperthermia, acne, hyperuricemia, exacerbation of gout, photosensitivity, increased concentration of iron in plasma.

    Rifampicin.
    From the digestive system: nausea, vomiting, diarrhea, decreased appetite, erosive gastritis, pseudomembranous colitis; increased activity of "hepatic" transaminases in blood plasma, hyperbilirubinemia, hepatitis.
    From the central nervous system: headache, decreased visual acuity, ataxia, disorientation.
    From the urinary system: nephronecrosis, interstitial nephritis.
    Allergic reactions: urticaria, eosinophilia, angioedema, bronchospasm, arthralgia, fever.
    Other: leukopenia, dysmenorrhea, induction of porphyria, myasthenia gravis, hyperuricemia, exacerbation of gout.

    With irregular therapy or with the resumption of treatment after a break,possible: flu-like syndrome (fever, chills, headache, dizziness, sore throat and soreness of the tongue, myalgia), skin reactions, hemolytic anemia, thrombocytopenic purpura, acute renal failure.
    Overdose:
    Symptoms: pulmonary edema, confusion, convulsions, peripheral neuropathy, impaired liver function, nausea, vomiting, impaired vision and hearing, slurred speech,
    oppression of breath, stupor, coma.
    Treatment: gastric lavage, the appointment of activated charcoal; symptomatic therapy, forced diuresis, artificial ventilation, intravenous - barbiturates of short action, pyridoxine, osmotic diuretics, sodium bicarbonate in the development of metabolic acidosis.
    Interaction:
    Isoniazid.
    Prednisolone can significantly reduce the concentration of isoniazid in the blood plasma. Antacid medicines (especially aluminum containing) slow down absorption and reduce the concentration of isoniazid in the blood (antacids should be taken no earlier than 1 hour after taking isoniazid).
    Isoniazid increases the frequency and severity of liver function disorders in combination with rifampicin in patients with previous liver disease. Isoniazid increases the concentration of phenytoin in the blood, increasing its side effects, such as drowsiness and ataxia, reduces the effectiveness of oral combined contraceptive drugs, glipizide, tolbutamide, tolazamide, thiamine; suppresses the excretion of triazolam; reduces the content of zinc ions (Zn2 +) in the blood. Isoniazid enhances the action of coumarin derivatives, indanedione, benzodeazepines, carbamazepine, theophylline, as it reduces their metabolism.
    Isoniazid increases the concentration of valproic acid in the blood (monitoring of valproic acid concentration is necessary: ​​correction of the dosing regimen may be required).
    When combining isoniazid with paracetamol, hepato- and nephrotoxicity increases.
    Isoniazid reduces metabolic transformations and increases the concentration in the blood of alfentanil.
    Cycloserine and disulfiram enhance the adverse central effects of isoniazid.
    The combination of isoniazid with pyridoxine reduces the risk of peripheral neuritis.
    Caution should be combined isoniazid with potentially neuro-, hepato- and nephrotoxic drugs because of the risk of side effects.
    Pyrazinamide.
    When used simultaneously with drugs that block tubular secretion, it is possible to reduce their excretion and increase toxic reactions.
    Strengthens the antituberculous action of lomefloxacin.
    The likelihood of developing a hepatotoxic effect increases with joint
    with rifampicin.
    Rifampicin.
    Rifampicin accelerates the metabolism of phenytoin, quinidine, oral anticoagulants and antifungal drugs.
    Anticholinergic drugs and ketoconazole reduce the bioavailability of rifampicin.
    Preparations aminosalitsilovoy acid appoint 4 hours after taking rifampicin. Antacids, opiates reduce the bioavailability of rifampicin.
    Rifampicin reduces the activity of oral hypoglycemic drugs, oral hormonal contraceptives, digitalis preparations, antiarrhythmic drugs (pyrmenol, quinidine, tokainid), glucocorticosteroids, dapsone, hydantoins (phenytoin), hexobarbital, nortriptyline, benzodiazepines, sex hormones, theophylline, chloramphenicol, intraconazole, cyclosporin A, beta adrenoblockers, enalapril, cimetidine and oral indirect anticoagulants.With the simultaneous use of rifampicin (600 mg / day), ritonavir (100 mg twice daily) and sanguinavir (1000 mg), it is possible to develop severe hepatotoxicity. When combined rifampicin significantly reduces the plasma concentrations of atazanavir, darunavir, fosamprenavir, sanguinavir and tipranavir, which can lead to a decrease in antiviral activity. Rifampicin increases the rate of excretion of bromsulfalein.
    Special instructions:
    It is forbidden to drink ethanol and / or alcoholic beverages while taking the drug. Do not interrupt (accidentally or intentionally) taking the drug without consulting a doctor. The consumption of cheese (Swiss and Cheshire), fish (tuna, sardanella, etc.) and some other products with isoniazid may be accompanied by a feeling of fever or chills, redness and itching of the skin, palpitations, sweating, headache, dizziness due to isoniazid metabolism of tyramine and histamine.
    Care should be taken when using the drug in weakened patients, patients with underweight and elderly age due to an increased risk of toxic events.
    Care should be taken when using the drug in patients with alcoholism or mental illness due to an increased risk of unwanted reactions.
    Before treatment and every 2-4 weeks during treatment, the content of alanine aminotransferase and aspartate aminotransferase is determined. When the level of hepatic enzymes is raised, the drug is canceled. Renewal treatment after the normalization of indicators. It is possible to take vitamin B supplement.
    Pyrazinamide worsens the course of gout and diabetes, monitoring of kidney function and uric acid levels is necessary. In the case of persistent hyperuricemia and exacerbation of gouty arthritis, the drug is canceled.
    During the treatment, microbiological methods are used to determine the concentration of folic acid and cyanocobalamin (vitamin B12) in the blood serum. During the treatment should not be used bromsulfaleinovy ​​test (false positive results).
    With prolonged admission, periodic monitoring of liver and kidney function, peripheral blood picture and examination of the ophthalmologist.
    In the course of treatment, an additional intake of ergocalciferol (vitamin D) is recommended to prevent calcium and phosphorus metabolism disorders.
    With the appointment in the last weeks of pregnancy, postpartum bleeding in the mother and bleeding in the newborn (treatment - vitamin K (sodium bisulfite metadione)) is possible. Women during the treatment period are recommended to use non-hormonal methods of contraception. Rifampicin stains skin, phlegm, sweat, feces, lacrimal fluid, urine, soft contact lenses in orange-red color. The drug does not have the features of the action at the first reception or upon its cancellation. Under no circumstances should it be necessary to prematurely discontinue or temporarily discontinue the treatment course or take the drug irregularly without consulting a doctor.
    If you miss a single dose, if you take the drug once a day, you need to take the next dose of the drug at a time when you remember that you missed taking the drug. If you take the drug more than once a day, if you miss a dose, you need to take the next dose of the drug at the set time. Do not take twice the dose of the drug.
    Effect on the ability to drive transp. cf. and fur:
    The ability of the drug to influence the speed of psychomotor reactions and the ability to control transport or other technical means has not been studied. Care should be taken when dealing with potentially hazardous activities requiring increased attention and rapid psychomotor reactions.
    Form release / dosage:
    Dispersible tablets, 30 mg + 150 mg + 60 mg and 150 mg + 375 mg + 150 mg.


    Packaging:
    28 tablets in a blister pack. 3 or 24 blisters together with instructions for use are placed in a cardboard pack. 10 tablets in a strip. 10 strips together with instructions for use are placed in a cardboard pack.
    1000 tablets in a package of three-layer material (PETF, aluminum foil, paper). The package together with the instruction for use is placed in a polypropylene container. The container is sealed with an aluminum membrane, covered with a polypropylene lid. Packing No. 1000 is intended for hospitals.
    When packing in a Russian company (ZAO "Rafarma") 3 blisters of 28 tablets are placed in a pack of cardboard along with instructions for use.
    Storage conditions:In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:
    2 years.
    Do not use the product after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-001810
    Date of registration:27.08.2012/26.12.2014
    Date of cancellation:2017-08-27
    The owner of the registration certificate:McLeodz Pharmaceuticals Co., Ltd. McLeodz Pharmaceuticals Co., Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspAdvansd Trading, OOOAdvansd Trading, OOO
    Information update date: & nbsp10.05.2016
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