Macroside 500

Macroside 500 is an antimicrobial drug for systemic use.

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Indications Macroside 500

Among the indications: a remedy for tuberculosis of any form (as part of a combination therapy with other anti-tuberculosis drugs).

Release form

Produced in the form of tablets. One blister contains 10 tablets. The package contains 10 blister plates.

Pharmacodynamics

Pyrazinamide belongs to the pharmacotherapeutic category of the second-line anti-tuberculosis drugs. It effectively affects the location of the foci of tuberculosis. The activity of the substance does not decrease in conditions of an acidic environment of purulent masses, as a result of which it is often used to treat purulent lymphadenitis, purulent-pneumonic processes, and tuberculosis.

When treated with pyrazinamide alone, tuberculosis mycobacteria can quickly adapt to it, so it is usually prescribed in conjunction with other anti-tuberculosis drugs.

Pharmacokinetics

Pyrazinamide is almost completely absorbed from the digestive tract. After oral administration of 1 g of the drug, the concentration of the drug in the blood plasma reaches 45 μg / ml after 2 hours, and decreases to 10 μg / ml after 15 hours. In the process of hydrolysis, pyrazinamide passes into the active product of decomposition (pyrazinic acid), and after this - into the inactive. The half-life (if the kidneys function normally) is 9-10 hours.

Through the kidneys, 70% of the active substance is excreted. The elimination process takes 24 hours, the drug is excreted mainly in the form of decay products.

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Dosing and administration

You need to drink the pill after eating - drink with water and swallow. To calculate the daily dosage, it is necessary to use the BMI indicators.

Children 15+ years, as well as adults - the dosage is calculated within 15-30 mg / kg for 1 reception. Drug use should be 1-3 times a day (the exact figure depends on how the patient tolerates it). For a day you can take no more than 2 grams of the drug.

Elderly patients (due to a possible worsening of the liver or kidneys) should prescribe the drug in dosages for adults, close to the minimum limit of 15 mg / kg.

Patients with moderate disorders in the work of the kidneys should be prescribed a daily dosage within the range of 12-20 mg / kg. In this case, patients who have a creatinine cleansing factor of less than 50 ml / min should give up treatment with pyrazinamide.

Patients who undergo peritoneal dialysis or hemodialysis procedures can be given a standard adult dosage. But it is recommended to take the tablets before dialysis (for 24 hours).

Since pyrazinamide begins to accumulate in patients with a disorder in liver function when taking standard dosages, it should be consumed in reduced doses of 15 mg / kg. Before starting treatment, you need to perform a functional liver test, and then repeat this procedure throughout the therapy (every 2-4 weeks).

The duration of the treatment course depends on how the disease progresses, and also on how the patient transfers the medicine. Exact terms are appointed by the doctor (basically it's about 6-8 months).

[4], [5]

Use Macroside 500 during pregnancy

Use of the drug during pregnancy is prohibited.

Contraindications

Among the contraindications: individual sensitivity to the components of the drug or other, close to it by chemical structure, LS - isoniazid, ethionamide, and also niacin. In addition, hepatic insufficiency is also severe, hyperuricemia without symptoms, and exacerbated gout.

Side effects Macroside 500

Among the side reactions to the drug:

• organs of the digestive tract: dyspepsia, pain in the stomach, as well as epigastrium, loss of appetite, the appearance of vomiting with nausea, diarrhea, ulcer development, the presence of metallic taste in the oral cavity;
• organs of the digestive system: a disorder in the work of the liver, an increase in the number of transaminases of the liver, and in addition bilirubin, as well as an increase in the rate of timoloneval test and the development of hepatomegaly. In rare cases, liver atrophy (acute) and jaundice (depending on the dose) may begin;
• organs of the urinary system: tubulointerstitial nephritis; single - myoglobinuric form of renal failure due to rhabdomyolysis, and besides dysuria and the appearance of painful sensations when urinating;
• organs of the National Assembly: headaches with dizziness, trouble with sleep, depression, a feeling of increased excitability; in rare cases, the appearance of convulsions, and in addition to hallucinations and paresthesias, it is also possible to develop a peripheral form of neuropathy and confusion;
• organs of the lymphatic and hematopoietic systems: anemia, and in addition porphyria and thrombocytopenia, increased accumulation of iron in the serum, eosinophilia, sideroblastic form of anemia, erythrocyte vacuolation, increased blood coagulability, tendency to thrombogenesis, and in addition splenomegaly;
• musculoskeletal structure: rhabdomyolysis, joint or muscle pain, exacerbation of gout, edema of joints, sensation of joint stiffness;
• skin with subcutaneous tissue: rashes, itching, development of urticaria or hyperemia, photosensitivity, toxicodermia and acne;
• immune reactions: Quincke edema, fever, various anaphylactoid reactions, very rarely anaphylaxis can be observed;
• organs of the respiratory system: dyspnea, difficulty breathing, and in addition dry cough;
• other: a state of general weakness or malaise, the development of pellagra, hyperuricemia or hyperthermia syndrome.

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Overdose

Sometimes, an overdose is observed in the liver, and there is an increase in the level of transaminases. Symptoms disappear after the drug is withdrawn. In addition, hyperuricemia, arousal, manifestations of dyspepsia, and side effects symptoms may occur.

As a treatment - requires washing the stomach and taking activated charcoal, and then monitoring the liver and determining the level of urate in the blood serum. Symptomatic therapy is also performed. The patient should drink plenty of fluids. Effective and use of hemodialysis.

Interactions with other drugs

When pyrazinamide is combined with ethionamide, the possibility of liver damage increases, especially for diabetics. When combined treatment of these drugs must constantly monitor the work of the liver. If you have any symptoms of a violation, you should immediately stop treatment in this combination.

Pyrazinamide lowers the metabolic rate of cyclosporine, and at the same time reduces its concentration in blood serum. Patients treated with cyclosporine should constantly monitor the indices of this substance during the entire course of treatment with pyrazinamide, as well as the first time after its completion.

Pyrazinamide is able to weaken the effectiveness of drugs used in the treatment of gout, as well as drugs that help remove uric acid from the body (such drugs as allopurinol and colchicine, and in addition probenecid with sulfinpyrazone). Indices of the concentration of uric acid in the blood serum of patients suffering from gout and treated with pyrazinamide may increase. If you use the above drugs in conjunction with pyrazinamide, you need to adjust their dose - to control hyperuricemia.

In the case of combination of pyrazinamide with allopurinol, the metabolism of the degradation products of pyrazinamide is slowed down, but the metabolism of the active substance itself does not change significantly.

As a result of the compound with zidovudine, the value of pyrazinamide in the blood serum is reduced, which increases the risk of anemia.

Pyrazinamide can be combined with many anti-tuberculosis drugs (eg, isoniazid). If a destructive chronic form of pathology develops, it should be used together with rifampicin (a higher effect) or ethambutol (this combination is better tolerated). Due to the combination with tuberculosis blocking drugs, the rate of their elimination can be slowed down, and the toxic reaction can be intensified.

The drug increases the anti-tuberculosis properties of ofloxacin, as well as lomefloxacin. When pyrazinamide is combined with isoniazid, the latter can be reduced in blood serum (especially in patients who have a slow metabolism of this substance).

When pyrazinamide is combined with phenytoin, the latter may be elevated in the blood serum, so that the symptoms of phenytoin poisoning may appear. If, with the combined use of these two substances, side reactions occur in the CNS (for example, such as ataxia or nystagmus, hyperreflexia or tremor) - in this case, you need to cancel their reception. Further, it is required to determine the level of phenytoin in the blood serum, and then to select the appropriate dosage of this drug.

Pyrazinamide is able to enhance the effectiveness of hypoglycemic drugs.

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Storage conditions

Keep the medicine in a place that is not accessible to children. Optimum temperature conditions - maximum 30 ˚С.

Shelf life

Macroside 500 is recommended to be used for 3 years from the date of manufacture of the drug.