Terizidone-Mac (Capsules) Instructions for Use

Marketing Authorization Holder

Macleods Pharmaceuticals Ltd. (India)

ATC Code

J04AK03 (Terizidone)

Active Substance

Terizidone (Rec.INN registered by WHO)

Dosage Form

Terizidone-Mac

Capsules 250 mg: 10, 50 or 100 pcs.

Dosage Form, Packaging, and Composition

10 pcs. – non-cell contour packs (1) – cardboard packs.
10 pcs. – non-cell contour packs (5) – cardboard packs.
10 pcs. – non-cell contour packs (10) – cardboard packs.

Clinical-Pharmacological Group

Antituberculosis drug

Pharmacotherapeutic Group

Antitubercular agent

Pharmacological Action

Broad-spectrum bacteriostatic antibiotic, active against Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium avium, as well as Staphylococcus aureus and Staphylococcus epidermidis.

Also sensitive are: Enterococcus faecalis, Escherichia coli, Citrobacter spp., Enterobacter spp., Morganella morganii, Klebsiella pneumoniae, and Pseudomonas aeruginosa.

The development of secondary resistance is rare. No cross-resistance with other antituberculosis drugs is observed.

Pharmacokinetics

Absorption from the gastrointestinal tract is 70-90% (food intake does not affect the absorption rate). Time to reach C_max is 2-3 hours. Effective C_min: for Mycobacterium tuberculosis – 10-40 mg/L, for staphylococci – 8-32 mg/L, for gram-negative bacteria (of clinical significance) – 20-250 mg/L.

Distributes well in body tissues and fluids ( lungs, bile, ascitic fluid, pleural effusion, synovial fluid, lymph, sputum).

Penetrates into the CSF ( 80-100% of the serum concentration), a higher concentration in the CSF is achieved with inflammatory changes in the meninges.

Metabolized insignificantly.

T_1/2 – 21 hours. Excreted by the kidneys (unchanged – 60-70%), intestines (a small amount unchanged and as metabolites).

Indications

Tuberculosis of various forms and localizations as part of complex therapy for resistant forms of the disease.

ICD codes

Dosage Regimen

Orally, regardless of food intake: for adults and children over 14 years of age and weighing less than 60 kg – 300 mg 2 times/day (600 mg/day); for those weighing 60-80 kg – 300 mg 3 times/day (900 mg/day). For adults weighing more than 80 kg – 600 mg 2 times/day (1200 mg/day). Taken for 3-4 months.

In case of CrCl less than 30 ml/min, the dose and frequency of administration should be reduced.

Adverse Reactions

From the nervous system headache, dizziness, increased excitability, tremor, insomnia, feeling of intoxication; in isolated cases – epileptiform convulsions, depression, psychosis.

From the digestive system rarely – abdominal pain, flatulence, diarrhea.

Allergic reactions.

Contraindications

Hypersensitivity (including to cycloserine); organic diseases of the CNS (including cerebrovascular sclerosis); epilepsy; mental disorders; alcoholism; pregnancy; lactation period; childhood (under 14 years).

With caution elderly age, chronic heart failure, chronic renal failure.

Use in Pregnancy and Lactation

Contraindications: pregnancy; lactation period.

Use in Renal Impairment

With cautionchronic renal failure.

In case of CrCl less than 30 ml/min, the dose and frequency of administration should be reduced.

Pediatric Use

Contraindication — childhood (under 14 years).

For children over 14 years of age and weighing less than 60 kg, 300 mg 2 times/day (600 mg/day) is prescribed; for those weighing 60-80 kg – 300 mg 3 times/day (900 mg/day).

Geriatric Use

With caution elderly age.

Special Precautions

Terizidone may cause cyanocobalamin and/or folic acid deficiency, appropriate examination and treatment are necessary.

Blood and urine parameters, liver function ( ALT, AST, bilirubin) should be monitored monthly.

Avoid consumption of ethanol, as simultaneous use with terizidone increases the frequency of side effects (up to the development of convulsions).

Due to the possibility of developing side reactions from the nervous system (depression, behavior change), it is necessary to monitor the patient’s mental status.

Effect on ability to drive vehicles and machinery

During treatment, it is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Ethanol increases the risk of epileptic seizures.

When used concomitantly with ethionamide, the risk of side effects from the CNS (especially convulsions) increases.

Concomitant use with isoniazid increases the frequency of dizziness and drowsiness.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°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.