Pyzina (Tablets) Instructions for Use

Marketing Authorization Holder

Lupin, Ltd. (India)

ATC Code

J04AK01 (Pyrazinamide)

Active Substance

Pyrazinamide (Rec.INN registered by WHO)

Dosage Form

Pyzina

Tablets 500 mg: 100 pcs.

Dosage Form, Packaging, and Composition

Tablets are white, round, flat, with beveled edges, with the inscription “PYZINA LUPIN” and a break line on one side.

Excipients: calcium phosphate dibasic dihydrate, pregelatinized starch, corn starch, colloidal silicon dioxide, sodium lauryl sulfate, magnesium stearate, purified talc.

10 pcs. – blisters (10) – cartons.
100 pcs. – polyethylene bags (1) – plastic containers.

Clinical-Pharmacological Group

Antituberculosis drug

Pharmacotherapeutic Group

Antitubercular agent

Pharmacological Action

Synthetic second-line antituberculosis drug. The mechanism of action is not precisely known. It has a bacteriostatic or bactericidal effect depending on its concentration and the sensitivity of the microorganism. Penetrates well into foci of tuberculous lesions.

Pharmacokinetics

After oral administration, Pyrazinamide is rapidly absorbed from the gastrointestinal tract. C_max in plasma is reached within 2 hours and is about 35 µg/ml at a dose of 1.5 g and 66 µg/ml at a dose of 2 g. Pyrazinamide is widely distributed in body tissues and fluids, penetrates the blood-brain barrier.

It is metabolized mainly in the liver by hydrolysis to form pyrazinoic acid, the main metabolite, which is gradually hydroxylated to 5-hydroxypyrazinoic acid.

T_1/2 from plasma is about 9-10 hours.

It is excreted mainly by the kidneys via glomerular filtration. About 70% is found in the urine within 24 hours, mainly in the form of metabolites, and 4-14% as unchanged substance.

Indications

Tuberculosis (as part of combination therapy).

ICD codes

Dosage Regimen

Administer orally.

Calculate the dose based on body weight.

For daily administration, use 15-25 mg/kg once per day.

For intermittent therapy, use 50-70 mg/kg two or three times per week.

Do not exceed the maximum daily dose of 2 grams.

Do not exceed the maximum intermittent dose of 3 grams when administered three times weekly or 4 grams when administered twice weekly.

Use only as part of a combination antituberculosis regimen to prevent the development of resistance.

Monitor liver transaminases and serum uric acid levels monthly during prolonged therapy.

Adverse Reactions

From the digestive system: impaired liver function, nausea, vomiting, diarrhea.

Allergic reactions: skin rash, itching, arthralgia.

Other: hyperuricemia, exacerbation of gout; rarely – photosensitivity.

Contraindications

Impaired liver function, hypersensitivity to pyrazinamide.

Use in Pregnancy and Lactation

Adequate and strictly controlled clinical studies on the safety of pyrazinamide use during pregnancy and lactation (breastfeeding) have not been conducted. However, if resistance to isoniazid, rifampicin, and ethambutol develops, the use of pyrazinamide in pregnant women may be considered.

Pyrazinamide is excreted in breast milk in small amounts.

Use in Hepatic Impairment

Contraindicated in impaired liver function.

Pediatric Use

Use is possible according to the dosing regimen.

Special Precautions

With monotherapy, resistance of mycobacteria to pyrazinamide develops rapidly, therefore Pyrazinamide is usually used in combination with other antituberculosis drugs.

Pyrazinamide is removed from the body by dialysis.

With long-term use, it is advisable to regularly (once a month) monitor the activity of liver transaminases and the content of uric acid in the blood.

Drug Interactions

Pyrazinamide reduces plasma concentrations of cyclosporine.

Pyrazinamide increases plasma concentrations of uric acid and reduces the effectiveness of antigout agents (allopurinol, sulfinpyrazone) with simultaneous use.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.