Perchlozon^® (Tablets) Instructions for Use

Marketing Authorization Holder

Pharmasintez, JSC (Russia)

ATC Code

J04AK (Other antituberculosis drugs)

Dosage Forms

	Perchlozon®	Film-coated tablets, 200 mg: 50 or 100 pcs.
		Film-coated tablets, 400 mg: 50 or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets from yellow to dark yellow in color, round in shape, biconvex, with an engraving “PHZ” on one side; on the cross-section, the tablet is from light yellow to yellow with a slight greenish tint.

Excipients: colloidal silicon dioxide (aerosil) – 5 mg, crospovidone (kollidon CL) – 17.5 mg, magnesium stearate – 2.5 mg, povidone (medium molecular weight polyvinylpyrrolidone, kollidon 25) – 6.65 mg, microcrystalline cellulose 101 – 58.35 mg.

Film coating composition: hypromellose E5 (hydroxypropyl methylcellulose 5) – 0.35 mg, hypromellose E15 (hydroxypropyl methylcellulose 15) – 6 mg, iron oxide yellow dye – 0.4 mg, macrogol 6000 (polyethylene glycol 6000) – 1.25 mg, talc – 1 mg, propylene glycol – 0.5 mg, titanium dioxide – 0.5 mg.

10 pcs. – contour cell packaging (5) – cardboard packs.
10 pcs. – contour cell packaging (10) – cardboard packs.
50 pcs. – jars (1) – cardboard packs.
100 pcs. – jars (1) – cardboard packs.

Film-coated tablets from yellow to dark yellow in color, oval in shape, biconvex, with an engraving “PHZ” on one side; on the cross-section, the tablet is from light yellow to yellow with a slight greenish tint.

Excipients: colloidal silicon dioxide (aerosil) – 1 mg, crospovidone (kollidon CL) – 35 mg, magnesium stearate – 5 mg, povidone (medium molecular weight polyvinylpyrrolidone, kollidon 25) – 13.3 mg, microcrystalline cellulose 101 – 116.7 mg.

Film coating composition: hypromellose E5 (hydroxypropyl methylcellulose 5) – 0.7 mg, hypromellose E15 (hydroxypropyl methylcellulose 15) – 12 mg, iron oxide yellow dye – 0.8 mg, macrogol 6000 (polyethylene glycol 6000) – 2.5 mg, talc – 2 mg, propylene glycol – 1 mg, titanium dioxide – 1 mg.

10 pcs. – contour cell packaging (5) – cardboard packs.
10 pcs. – contour cell packaging (10) – cardboard packs.
50 pcs. – jars (1) – cardboard packs.
100 pcs. – jars (1) – cardboard packs.

Clinical-Pharmacological Group

Antituberculosis drug

Pharmacotherapeutic Group

Agents active against mycobacteria; antituberculosis agents; other antituberculosis agents

Pharmacological Action

Antituberculosis agent. The mechanism of action has not been established. Active against Mycobacterium tuberculosis and Mycobacterium bovis. It has a pronounced inhibitory effect on the viability of tuberculosis mycobacteria, including those resistant to other antituberculosis drugs.

Perchlozon^® is a low-toxicity substance, does not cause significant structural and functional disorders of vital organs and systems, and does not have an irritating effect on the mucous membranes of the gastrointestinal tract.

The mechanism of action has not been definitively established, studies are ongoing.

Pharmacokinetics

After oral administration, Perchlozon^® is rapidly absorbed in the gastrointestinal tract. The time to reach maximum blood concentration (T_max) is 1.5-3 hours. After a single oral administration in doses of 400 mg, 800 mg, 1200 mg and 1600 mg, the maximum blood concentration (C_max) is 2.61±0.34 µg/ml, 5.07±0.69 µg/ml, 5.42±0.65 µg/ml and 8.17±1.91 µg/ml, respectively.

The half-life is 12-27 hours. The time to reach steady-state concentration (C_ss) of the active substance in the blood with prolonged use is 14 days. The concentration of the active substance in the blood during a course of the drug (once a day), measured 15 minutes before the next dose, is 23.4 µg per 1 ml of blood plasma.

The pathways of metabolism of the active substance have not been established, studies are ongoing.

Indications

• Pulmonary tuberculosis, including with multidrug-resistant Mycobacterium tuberculosis (as part of combination therapy).

ICD codes

Dosage Regimen

Administer orally, once daily, after a meal.

Determine the daily dose for adults based on body weight, using the range of 9.5-12.5 mg/kg/day.

For a body weight of less than 50 kg, prescribe 400-600 mg per day.

For a body weight of 50-80 kg, prescribe 800-1000 mg per day.

For a body weight exceeding 80 kg, do not exceed a maximum daily dose of 1200 mg.

Always use as part of a combination antituberculosis therapy regimen.

Limit the total duration of therapy to a maximum of three months.

Monitor patients for the development of adverse reactions, particularly neuropsychiatric effects, hepatotoxicity, and allergic phenomena.

In case of significant adverse reactions, consider reducing the dose to 400 mg/day or discontinuing treatment.

Do not use sodium metamizole (analgin) to manage drug-induced fever.

Advise patients that side effects like dizziness and drowsiness may impair the ability to drive or operate machinery.

Adverse Reactions

Nervous system disorders: dizziness, headache, weakness, drowsiness, loss of consciousness, neuropsychiatric reactions (aggression, depression).

Cardiovascular system disorders: tachycardia, palpitations, decreased blood pressure.

Digestive system disorders: epigastric pain, increased activity of “liver” transaminases, nausea, vomiting.

Allergic reactions: itching, rash, skin hyperemia, toxic-allergic reactions, angioedema.

Other: bronchospasm, fever, eosinophilia, sensation of heat.

Contraindications

• Hypersensitivity to the active substance or to any components of the drug;
• Impaired liver and/or kidney function (the possibility of using the drug in this category of patients has not been studied);
• Pregnancy;
• Breastfeeding period;
• Childhood (under 18 years of age).

With caution

Elderly age.

Use in Pregnancy and Lactation

The drug is contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Contraindicated in cases of impaired liver function (the possibility of using the drug in this category of patients has not been studied).

Use in Renal Impairment

Contraindicated in cases of impaired kidney function (the possibility of using the drug in this category of patients has not been studied).

Pediatric Use

Contraindicated for children under 18 years of age.

Geriatric Use

Use with caution in elderly persons.

Special Precautions

If allergic reactions develop, it is recommended to discontinue the drug. Do not use sodium metamizole (analgin) to relieve fever. In case of development of other aforementioned adverse reactions, the possibility of reducing the dose to 400 mg/day or discontinuing the drug should be considered.

Effect on ability to drive vehicles and machinery

No special studies have been conducted on the effect of Perchlozon^® on the ability to drive a car and operate machinery. Such side effects of the drug as dizziness, weakness, drowsiness may impair reaction ability and concentration. During treatment with Perchlozon^®, it is not recommended to drive vehicles or engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

There are no data on acute overdose with Perchlozon^® in humans.

Treatment: specific antidote is unknown. In case of overdose, general supportive therapy with monitoring of basic physiological parameters should be carried out.

Gastric lavage and administration of activated charcoal are recommended.

Drug Interactions

Interaction with other medicinal products has not been sufficiently studied.

When Perchlozon^® is used concomitantly with other antituberculosis drugs (isoniazid, amikacin, rifabutin, rifampicin), an increase in activity against tuberculosis mycobacteria is noted, and the possibility of mutual potentiation of side effects should be taken into account.

Storage Conditions

In a dry, light-protected place at a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Shelf Life

Shelf life – 2 years.

Dispensing Status

By prescription.

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.