Theraflex^® (Capsules) Instructions for Use

Marketing Authorization Holder

Bayer Consumer Care, AG (Switzerland)

Manufactured By

Makiz-Pharma, LLC (Russia)

Contact Information

BAYER AG (Germany)

ATC Code

M01BX (Anti-inflammatory and antirheumatic agents in combination with other drugs)

Active Substances

Chondroitin sulfate sodium (Ph.Eur. European Pharmacopoeia)

Glucosamine (Rec.INN WHO Registered)

Dosage Form

Theraflex®

Capsules 500 mg+400 mg: 60, 100, or 200 pcs.

Dosage Form, Packaging, and Composition

Capsules transparent hard gelatin, size #00; capsule contents – powder white or white with a yellowish tint with crystalline particles.

Excipients : stearic acid – 10 mg, magnesium stearate – 5 mg, manganese sulfate – 1 mg.

Gelatin capsule composition gelatin – 120 mg.

60 pcs. – high-density polyethylene bottles^× (1) – cardboard packs.
100 pcs. – high-density polyethylene bottles^× (1) – cardboard packs.
200 pcs. – high-density polyethylene bottles^× (1) – cardboard packs.

^× with a screw-on polypropylene cap sealed with a protective polymer film; under the cap, the bottle neck is sealed with a multilayer membrane; the free space of the bottle is filled with a cotton wick.

Clinical-Pharmacological Group

Tissue repair stimulant

Pharmacotherapeutic Group

Tissue repair stimulant

Pharmacological Action

A drug that stimulates the repair of cartilage tissue.

Glucosamine and chondroitin sulfate are involved in the synthesis of connective tissue, helping to prevent cartilage destruction processes and stimulating tissue regeneration. The introduction of exogenous glucosamine enhances the production of cartilage matrix and provides nonspecific protection against chemical damage to cartilage. Another possible action of glucosamine is the protection of damaged cartilage from metabolic destruction caused by NSAIDs and corticosteroids, as well as its own moderate anti-inflammatory action.

Chondroitin sulfate serves as an additional substrate for the formation of a healthy cartilage matrix. It stimulates the formation of hyaluronan, the synthesis of proteoglycans and type II collagen, and also protects hyaluronan from enzymatic breakdown (by suppressing hyaluronidase activity); maintains the viscosity of synovial fluid, stimulates the mechanisms of cartilage tissue repair and suppresses the activity of those enzymes (elastase, hyaluronidase) that break down cartilage. In the treatment of osteoarthritis, it alleviates the symptoms of the disease and reduces the need for NSAIDs.

Pharmacokinetics

Glucosamine

Absorption

The bioavailability of glucosamine when taken orally is 25% (due to the “first-pass” effect through the liver).

Metabolism

After absorption, radioactively labeled glucosamine is first detected in plasma and later penetrates into tissues. The highest concentrations are found in the liver, kidneys, and articular cartilage. About 30% of the administered dose persists for a long time in bone and muscle tissues.

Excretion

It is excreted mainly by the kidneys unchanged, partially through the intestines. T_1/2 – 68 h.

Chondroitin sulfate

Absorption

When chondroitin sulfate is taken orally once at a dose of 0.8 g (or 0.4 g twice/day), the plasma concentration increases over 24 hours. The absolute bioavailability is 12%.

Metabolism

It is metabolized by desulfation.

Excretion

It is excreted by the kidneys. T_1/2– 310 min.

Indications

• Degenerative-dystrophic diseases of the joints and spine: osteoarthritis stages I-III, osteochondrosis.

ICD codes

Dosage Regimen

Orally. Adults and children over 15 years are prescribed 1 caps. 3 times/day for the first 3 weeks; subsequent days – 1 caps. 2 times/day, regardless of food intake, with a small amount of water. The recommended duration of the treatment course is from 3 to 6 months.

If necessary, repeated courses of treatment can be carried out, the duration of which is determined individually.

Adverse Reactions

Theraflex^® is well tolerated by patients.

From the digestive system pain in the epigastric region, flatulence, diarrhea, constipation.

From the nervous system dizziness, headache, drowsiness, insomnia.

From the cardiovascular system tachycardia.

Other allergic reactions, leg pain and peripheral edema.

Contraindications

• Hypersensitivity to the drug components;
• Severe chronic renal failure;
• Pregnancy;
• Lactation period;
• Age under 15 years.

With caution: diabetes mellitus (it is recommended to periodically monitor blood glucose levels, especially at the beginning of treatment), bronchial asthma, cardiac and/or renal failure (isolated cases of edema development have been described when taking chondroitin), hypersensitivity to seafood.

Use in Pregnancy and Lactation

Clinical data on the efficacy and safety of Theraflex^® use during pregnancy and breastfeeding are not available.

Use in Renal Impairment

Contraindicated in severe renal failure.

Pediatric Use

The use of the drug is contraindicated in children under 15 years of age.

Special Precautions

If adverse effects from the gastrointestinal tract occur, the drug dose should be reduced by half, and if there is no improvement, the drug should be discontinued.

Overdose

Overdose cases are unknown.

Symptoms with an overdose of chondroitin sulfate, hemorrhagic rash, nausea, and vomiting are possible.

Treatment gastric lavage, symptomatic therapy.

Drug Interactions

The drug improves the absorption of tetracyclines and reduces the effect of semi-synthetic penicillins and chloramphenicol.

The drug is compatible with NSAIDs and corticosteroids.

There is limited data on a possible interaction between glucosamine and warfarin, which may lead to an increase in INR and the risk of bleeding. Therefore, when taken concomitantly, blood coagulation parameters should be monitored.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years. Do not use after the expiration date.

Dispensing Status

The drug is available without a 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.