Macrozide 500

Macroside 500 is an antimicrobial drug for systemic use.

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Indications Macrozide 500

Indications include: a therapeutic agent against tuberculosis of any form (as part of combination therapy with other anti-tuberculosis drugs).

Release form

Available in tablet form. One blister contains 10 tablets. The package contains 10 blister strips.

Pharmacodynamics

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

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

Pharmacokinetics

Pyrazinamide is almost completely absorbed from the gastrointestinal tract. After oral administration of 1 g of the drug, its concentration in the blood plasma reaches 45 mcg/ml after 2 hours, and decreases to 10 mcg/ml after 15 hours. During hydrolysis, pyrazinamide turns into an active decay product (pyrazinoic acid), and then into an inactive one. The half-life (if the kidneys are functioning normally) is 9-10 hours.

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

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Dosing and administration

The tablets should be taken after meals - washed down with water and swallowed. To calculate the daily dosage, you need to use BMI indicators.

For children aged 15+ and adults, the dosage is calculated within 15-30 mg/kg per dose. The medicine should be taken 1-3 times per day (the exact figure depends on how the patient tolerates it). No more than 2 grams of the drug can be taken per day.

Elderly patients (due to possible deterioration of liver or kidney function) should be prescribed the drug in adult dosages close to the minimum limit - 15 mg/kg.

Patients with moderate renal impairment should be given a daily dosage of 12-20 mg/kg. However, patients with a creatinine clearance rate of less than 50 ml/min should not receive pyrazinamide treatment.

Patients undergoing peritoneal dialysis or hemodialysis can be prescribed the standard adult dosage. However, it is recommended to take the tablets before dialysis (24 hours).

Since pyrazinamide begins to accumulate in patients with liver dysfunction when taking standard doses, it should be used in reduced doses - 15 mg / kg. Before starting treatment, it is necessary to perform a liver function 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 how the patient tolerates the medication. The exact time frame is prescribed by the doctor (usually it is about 6-8 months).

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Use Macrozide 500 during pregnancy

It is prohibited to use the medicine during pregnancy.

Contraindications

Contraindications include: individual sensitivity to the components of the drug or other drugs close to it in chemical structure - isoniazid, ethionamide, and niacin. In addition, severe liver failure, asymptomatic hypercricemia, and exacerbated gout.

Side effects Macrozide 500

Adverse reactions to the drug include:

• gastrointestinal tract: dyspepsia, pain in the stomach area, as well as epigastrium, loss of appetite, vomiting with nausea, diarrhea, development of ulcers, presence of metallic taste in the mouth;
• digestive system organs: liver dysfunction, increased liver transaminases, and also bilirubin, as well as an increase in the thymoloveronal test and the development of hepatomegaly. In rare cases, liver atrophy (acute) and jaundice (depending on the dose) may begin;
• urinary system organs: tubulointerstitial nephritis; isolated cases – myoglobinuric form of renal failure due to rhabdomyolysis, and in addition dysuria and the appearance of pain during urination;
• organs of the nervous system: headaches with dizziness, sleep problems, depression, feeling of increased excitability; in rare cases, the appearance of seizures, and in addition to hallucinations and paresthesia, the development of peripheral neuropathy and confusion is also possible;
• organs of the lymphatic and hematopoietic systems: anemia, as well as porphyria and thrombocytopenia, increased accumulation of iron in the serum, eosinophilia, sideroblastic form of anemia, vacuolization of erythrocytes, increased blood clotting, tendency to thrombus formation, and in addition splenomegaly;
• musculoskeletal system: rhabdomyolysis, joint or muscle pain, exacerbation of gout, joint swelling, feeling of stiffness in joints;
• skin with subcutaneous tissue: rashes, itching, development of urticaria or hyperemia, photosensitivity, toxicoderma and acne;
• immune reactions: Quincke's edema, fever, various anaphylactoid reactions, very rarely anaphylaxis may be observed;
• respiratory system: dyspnea, difficulty breathing, and also a dry cough;
• other: a state of general weakness or malaise, development of pellagra, hyperuricemia or hyperthermic syndrome.

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Overdose

Sometimes, overdose may cause liver dysfunction and increase transaminase levels. Symptoms disappear after discontinuation of the drug. In addition, hyperuricemia, agitation, dyspepsia, and increased symptoms of side effects may occur.

Treatment involves gastric lavage and activated carbon, followed by monitoring of liver function and determination of serum urate levels. Symptomatic therapy is also performed. The patient should drink plenty of fluids. Hemodialysis is also effective.

Interactions with other drugs

When pyrazinamide is combined with ethionamide, the risk of liver damage increases, especially for diabetics. When combined with these drugs, it is necessary to constantly monitor liver function. If any symptoms of a disorder appear, treatment in this combination should be stopped immediately.

Pyrazinamide decreases the rate of cyclosporine metabolism and, at the same time, decreases its concentration in the blood serum. Patients treated with cyclosporine should have their levels of this substance constantly monitored throughout the course of treatment with pyrazinamide, as well as for the first period after its completion.

Pyrazinamide can reduce the effectiveness of drugs used to treat gout, as well as drugs that help remove uric acid from the body (these are drugs such as allopurinol and colchicine, as well as probenecid with sulfinpyrazone). The concentration of uric acid in the blood serum of patients suffering from gout and treated with pyrazinamide may increase. In the case of using the above drugs in combination with pyrazinamide, their dose will need to be adjusted to control hyperuricemia.

When pyrazinamide is combined with allopurinol, the metabolism of pyrazinamide breakdown products is slowed down, but the metabolism of the active substance itself does not change significantly.

As a result of the combination with zidovudine, the pyrazinamide level in the blood serum decreases, which increases the risk of developing anemia.

Pyrazinamide can be combined with many anti-tuberculosis drugs (for example, isoniazid). In case of development of destructive chronic form of pathology it should be used together with rifampicin (higher effect) or ethambutol (this combination is better tolerated). Due to combination with drugs-blockers of tubular secretion, the rate of their excretion can slow down, and also the toxic reaction can increase.

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

When pyrazinamide is combined with phenytoin, the latter's levels in the blood serum may increase, which may result in symptoms of phenytoin poisoning. If side effects in the central nervous system (such as ataxia or nystagmus, hyperreflexia or tremor) occur when these two substances are used together, they should be discontinued. Next, the phenytoin level in the blood serum should be determined, and then the appropriate dosage of this drug should be selected.

Pyrazinamide can enhance the effectiveness of hypoglycemic drugs.

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Storage conditions

The medicine must be kept in a place out of reach of children. Optimal temperature conditions are a maximum of 30˚С.

Shelf life

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