Loxidon^® (Capsules) Instructions for Use

Marketing Authorization Holder

Pharmasintez, JSC (Russia)

ATC Code

J04AK03 (Terizidone)

Active Substance

Terizidone (Rec.INN registered by WHO)

Dosage Forms

	Loxidon®	Capsules 150 mg: 10, 20, 30, 50, 60 or 100 pcs.
		Capsules 250 mg: 10, 20, 30, 50, 60 or 100 pcs.
		Capsules 300 mg: 10, 20, 30, 50, 60 or 100 pcs.

Dosage Form, Packaging, and Composition

Capsules hard gelatin No. 1, white body, orange cap; capsule contents – white or white with a yellowish tint powder.

Excipients : lactose – 15 mg, talc – 5 mg, colloidal silicon dioxide (aerosil) – 4 mg.

Composition of hard gelatin capsules (“Capsugel”, Belgium):
body: titanium dioxide – 2%, gelatin — up to 100%;
cap: dye ponceau 4R — 0.22401%; titanium dioxide — 1.5004%; dye sunset yellow — 1.2753%; gelatin — up to 100%.

10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (2) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.
10 pcs. – contour cell packaging (6) – cardboard packs.
10 pcs. – contour cell packaging (10) – cardboard packs.
30 pcs. – polymer jars^x (1) – cardboard packs.
50 pcs. – polymer jars^x (1) – cardboard packs.
100 pcs. – polymer jars^x (1) – cardboard packs.

^xwith first opening control

Capsules hard gelatin, No. 0, white body, blue cap; capsule contents – white or white with a yellowish tint powder.

Excipients : lactose – 25 mg, talc – 8.3 mg, colloidal silicon dioxide (aerosil) – 6.7 mg.

Composition of hard gelatin capsules (“Capsugel”, Belgium):
body: titanium dioxide – 2.05%, gelatin — up to 100%;
cap: dye brilliant blue — 0.15%; titanium dioxide — 1.1252%; gelatin — up to 100%.

10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (2) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.
10 pcs. – contour cell packaging (6) – cardboard packs.
10 pcs. – contour cell packaging (10) – cardboard packs.
30 pcs. – polymer jars^x (1) – cardboard packs.
50 pcs. – polymer jars^x (1) – cardboard packs.
100 pcs. – polymer jars^x (1) – cardboard packs.

^xwith first opening control

Capsules hard gelatin No. 00, white body, yellow cap; capsule contents – white or white with a yellowish tint powder.

Excipients : lactose – 30 mg, talc – 10 mg, colloidal silicon dioxide (aerosil) – 8 mg.

Composition of hard gelatin capsules (“Capsugel”, Belgium):
body: titanium dioxide – 2%, gelatin — up to 100%;
cap: dye quinoline yellow – 1.4343%, titanium dioxide — 2.6%, dye sunset yellow — 0.0057%; gelatin — up to 100%.

10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (2) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.
10 pcs. – contour cell packaging (6) – cardboard packs.
10 pcs. – contour cell packaging (10) – cardboard packs.
30 pcs. – polymer jars^x (1) – cardboard packs.
50 pcs. – polymer jars^x (1) – cardboard packs.
100 pcs. – polymer jars^x (1) – cardboard packs.

^xwith first opening control

.

Clinical-Pharmacological Group

Antituberculosis drug

Pharmacotherapeutic Group

Antitubercular agent

Pharmacological Action

Antituberculosis antibiotic. It has a broad spectrum of antimicrobial activity. Acts bacteriostatically.

Active against Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium avium, as well as Staphylococcus aureus and Staphylococcus epidermidis. Enterococcus faecalis, Escherichia coli, Citrobacter spp., Enterobacter spp., Morganella morganii, Klebsiella pneumoniae and Pseudomonas aeruginosa are also sensitive.

Development of secondary resistance is rare. Cross-resistance with other antituberculosis drugs is not observed.

Pharmacokinetics

Absorption from the gastrointestinal tract – 70-90% (food intake does not affect the absorption rate). Time to reach C_max – 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.

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

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

Metabolized insignificantly.

T_1/2 – 21 hours. Excreted by the kidneys (unchanged – 60-70%), by the 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 meals: adults and children over 14 years of age and weighing less than 60 kg – 300 mg 2 times/day (600 mg/day); with a body weight of 60-80 kg – 300 mg 3 times/day (900 mg/day). Adults weighing more than 80 kg – 600 mg 2 times/day (1200 mg/day). Taken for 3-4 months.

If creatinine clearance is less than 30 ml/min, the dose and frequency of administration are 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.

Other: allergic reactions.

Contraindications

Organic diseases of the central nervous system (including cerebroarteriosclerosis), epilepsy, mental disorders, alcoholism, pregnancy, lactation period, children under 14 years of age, hypersensitivity to terizidone.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and during the lactation (breastfeeding) period.

Use in Renal Impairment

Use with caution in chronic renal failure.

Pediatric Use

Contraindicated in children under 14 years of age.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

Use with caution in patients with chronic heart failure, in chronic renal failure, in elderly patients.

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.

Patients should avoid consuming ethanol, because 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 mechanisms

During treatment, it is necessary to refrain from driving vehicles and engaging in 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 central nervous system (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.