Universal reference book for medicines
Name of the preparation: FTIZAMAX ® (FTIZAMAX)

Active substance: isoniazid, pyrazinamide, rifampicin

Type: Anti-TB drug

Manufacturer: MACLEODS PHARMACEUTICALS (India)
Composition, form of production and packaging
Tablets are dispersible
orange-brown in color, round, flat, with dark and light impregnations, with a facet on both sides, with a weak characteristic odor.

1 tab.

isoniazid 30 mg

pyrazinamide 150 mg

rifampicin 60 mg

Excipients: microcrystalline cellulose 25 mg, crospovidone 15 mg, povidone (K-30) 5 mg, shellac 1 mg, croscarmellose sodium 7 mg, aspartame 2 mg, magnesium stearate 2 mg, strawberry flavoring 3 mg.

28 pcs.
- blisters (3) - packs of cardboard.
28 pcs.
- Blisters (24) - packs of cardboard.
10 pieces.
- Strips (10) - packs of cardboard.
1000 pcs.
- Three-layer packages (1) - polypropylene containers.
Tablets are dispersible orange-brown in color, round, flat, with dark and light impregnations, with a facet on both sides, with a weak characteristic odor.

1 tab.

isoniazid 150 mg

pyrazinamide 375 mg

Rifampicin 150 mg

Excipients: microcrystalline cellulose 62.5 mg, povidone (K-30) 9.5 mg, crospovidone type A 35 mg, shellac 2 mg, croscarmellose sodium 15 mg, aspartame 3.5 mg, magnesium stearate 10 mg, strawberry flavoring 4.5 mg.

28 pcs.
- blisters (3) - packs of cardboard.
28 pcs.
- Blisters (24) - packs of cardboard.
10 pieces.
- Strips (10) - packs of cardboard.
1000 pcs.
- Three-layer packages (1) - polypropylene containers.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2013.

PHARMACHOLOGIC EFFECT

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 of isoniazid is 0.05-0.025 mg / L.
Pyrazinamide acts bactericidal on intracellular mycobacteria, as well as Micobacterium tuberculosis at various stages of its development, it penetrates well into the centers of tuberculous lesion.
The minimum inhibitory concentration of pyridinamide is 20 mg / l. Pyrazinamide does not act on atypical mycobacteria.
Rifampicin is a broad-spectrum antibiotic that inhibits DNA-dependent RNA polymerase.
With tuberculosis, rifampicin has a bactericidal effect, 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 C max in blood plasma after ingestion of a single dose of 300 mg is 3-7 μg / ml. The connection with proteins is insignificant - up to 10%. V d - 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. T 1/2 for "fast acetylators" is 0.5-1.6 hours; for "slow" - 2-5 hours. In case of renal insufficiency, T 1/2 can increase to 6.7 hours. The value of T 1/2 varies considerably depending on the individual intensity of the acetylation processes, the average value of T 1/2 is 3 hours (ingestion 600 mg) and 5.1 h (900 mg). At the course of admission T 1/2 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 development of 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 into the digestive tract with the attainment of C max in 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 formed at the beginning, which later becomes an inactive metabolite, 5-hydroxypyrazinic acid. T 1/2 - 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 C max - 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. Apparent V d 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 a few days of intake, the bioavailability decreases and T 1/2 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 kidneys in an 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).

DOSING MODE

It is taken orally 1-2 hours before meals, usually 1 time / day in 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 / day, 50 kg or more - 600 mg / day.
Children - 10-15 mg / kg / day, the maximum daily dose - 450 mg.
It is possible to use the drug in combination with other anti-TB drugs.

SIDE EFFECT

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 the extremities, peripheral neuropathy, optic neuritis, polyneuritis, psychosis, mood changes, depression, memory impairment.
Seizures can occur in patients with epilepsy.
From the cardiovascular system: a feeling of heartbeat, angina, an increase in blood pressure.

From the digestive system: gastralgia, nausea, vomiting, toxic hepatitis, including fatal, increased activity of liver transaminases, hyperbilirubinemia, bilirubinemia, jaundice.

On the part of the organs of 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 B 6 ), pellagra, hyperglycemia, metabolic acidosis.

Other: gynecomastia in men and menorrhagia in women, a tendency to bleeding and hemorrhage.

Pyrazinamide

On the part of the digestive system: nausea, vomiting, diarrhea, "metallic" taste in the mouth, impaired liver function (decreased appetite, liver tenderness, 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 hematopoiesis and hemostasis system: 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, increase in the concentration of iron in the plasma.

Rifampicin

On the part of the digestive system: nausea, vomiting, diarrhea, decreased appetite, erosive gastritis, pseudomembranous colitis;
increased activity of "hepatic" transaminases in blood plasma, hyperbilirubinemia, hepatitis.
From the side of the central nervous system: headache, reduced 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, flu-like syndrome (fever, chills, headache, dizziness, sore throat and soreness of the tongue, myalgia), skin reactions, hemolytic anemia, thrombocytopenic purpura, acute renal failure are possible .

CONTRAINDICATIONS

- hypersensitivity to the drug;

- pulmonary heart failure of II-III degree;

- violations of the liver function;

acute liver disease;

- jaundice;

acute hepatitis;

- impaired renal function;

- gout, hyperuricemia;

- purple;

- phenylketonuria;

- Pregnancy (I trimester), lactation period;

- Children weighing less than 7 kg.

With caution: with 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.
APPLICATION FOR FUNCTIONS OF THE LIVER

Contraindicated in the violation of kidney function.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in violations of liver function, acute liver disease, jaundice, acute hepatitis.

APPLICATION FOR CHILDREN

Contraindicated in children weighing less than 7 kg.

APPLICATION IN ELDERLY PATIENTS

With caution: the elderly.

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 6 additionally.
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 B 12 ) 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, faeces, teardrop, 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.
Impact on the ability to drive vehicles and other mechanisms

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.
OVERDOSE

Symptoms: pulmonary edema, confusion, convulsions, peripheral neuropathy, impaired liver function, nausea, vomiting, impaired vision and hearing, slurred speech, respiratory depression, stupor, coma.

Treatment: gastric lavage, the appointment of activated charcoal;
symptomatic therapy, forced diuresis, artificial ventilation, intravenous short-acting barbiturates, pyridoxine, osmotic diuretics, sodium bicarbonate in the development of metabolic acidosis.
DRUG 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 (Zn 2+ ) in the blood. Isoniazid enhances the action of coumarin, indanedione, benzodeazepins, 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 nephro-toxicity increases.

Isoniazid reduces metabolic transformations and increases the concentration in the blood of alfentanil.

Cycloserine and disulfiram increase the adverse central effects of isoniazid.

The combination of isoniazid with pyridoxine reduces the risk of peripheral neuritis.

Caution should be combined with 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 when combined 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 (pirmenol, quinidine, tokainide), glucocorticosteroids, dapsone, hydantoins (phenytoin), hexobarbital, nortriptyline, benzodiazepines, sex hormones, theophylline, chloramphenicol, intraconazole, cyclosporine A, beta-adrenoblockers, enalapril, cimetidine and oral indirect anticoagulants.

With the simultaneous use of rifampicin (600 mg / day), ritonavir (100 mg 2 times / day) and sanguinavir (1000 mg), it is possible to develop severe hepatotoxicity.When combined, rifampicin significantly reduces plasma concentrations of atazanavir, darunavir, fosamprenavir, sanguinavir and tipranavir, which may lead to a decrease in antiviral activity.

Rifampicin increases the rate of excretion of bromsulfalein.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

Keep out of the reach of children, in a dry and protected from light place, at a temperature of no higher than 25 ° C.

Shelf life - 2 years.
Do not use the drug after the expiry date stated on the package.
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