Artiflex

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ARTEFLEX (ARTIPHLEX)

Composition:

Active substance: glucosamine;

1 sachet contains sodium chloride glucosamine sulfate (equivalent to 1.5 g of glucosamine sulfate and 0.384 g of sodium chloride) – 0.384 g;

Excipients: sorbitol (E 420), anhydrous citric acid, aspartame (E 951), polyethylene glycol 4000.

Medicinal form. Powder for oral solution.

Main physicochemical properties: crystalline powder from white to off-white.

Pharmacotherapeutic group. Other non-steroidal anti-inflammatory and antirheumatic agents.

ATC code M01AX05.

Pharmacological properties.

Pharmacodynamics.

The active ingredient is a salt of the aminomonosaccharide glucosamine sulfate, which is naturally present in the human body and is used together with sulfates for the biosynthesis of hyaluronic acid in synovial fluid and glycosaminoglycans of the ground substance of articular cartilage.

The mechanism of action of glucosamine sulfate is stimulation of glycosaminoglycan synthesis and, consequently, of articular proteoglycans. In addition, glucosamine exhibits anti-inflammatory properties and slows down the degradation processes of articular cartilage primarily due to its metabolic activities and ability to inhibit the activity of interleukin-1 (IL-1), thus contributing both to symptomatic relief in osteoarthritis and to delaying structural joint damage, as evidenced by long-term clinical studies.

The efficacy of glucosamine sulfate in osteoarthritis becomes apparent within 2–3 weeks after the initiation of treatment.

Data from clinical studies on daily continuous treatment over 3 years indicate progressively increasing efficacy of glucosamine sulfate in terms of symptom relief and slowing structural joint damage, as confirmed by radiographic findings.

Glucosamine sulfate has demonstrated good tolerability. No significant effects of glucosamine sulfate on the cardiovascular, respiratory, autonomic, or central nervous systems have been observed.

Pharmacokinetics. 90% of the dose of glucosamine sulfate is rapidly and completely absorbed from the gastrointestinal tract, passes through biological barriers, and penetrates into tissues, predominantly into articular cartilage. Bioavailability is 26%. T½ is 68 hours.

Clinical Characteristics.

Indications. For relief of symptoms in mild to moderate knee osteoarthritis.

Contraindications. Hypersensitivity to the components of the medicinal product. Liver and kidney dysfunction in the decompensated stage, tendency to bleeding. Allergy to shellfish (the active substance is derived from shellfish).

Interaction with other medicinal products and other forms of interaction. Data on drug interactions with glucosamine are limited; however, an increase in INR (international normalized ratio) has been observed when glucosamine is used concomitantly with oral vitamin K antagonists. Therefore, patients receiving oral vitamin K antagonists should be closely monitored when initiating or discontinuing glucosamine therapy. Concomitant treatment with glucosamine may enhance the absorption and, consequently, the serum concentration of tetracyclines. However, the clinical significance of this interaction is likely limited.

Due to the fact that only limited data are available regarding potential interactions with glucosamine, particular attention should be paid to any altered response related to changes in serum concentrations of concomitantly administered medicinal products.

Special precautions for use.

Before using the medicine, consult a physician to rule out the presence of joint diseases for which other treatment methods are indicated.

Patients with impaired glucose tolerance should use glucosamine with caution. Diabetic patients are advised to monitor blood glucose levels more closely and, if necessary, determine insulin requirements both before starting and periodically during treatment.

In patients with known risk factors for cardiovascular diseases, monitoring of blood lipid levels is recommended, since hypercholesterolemia has been observed in several cases among patients receiving glucosamine.

The medicine should be used with caution in patients with asthma, as such patients may be more prone to allergic reactions to glucosamine, potentially leading to exacerbation of their disease symptoms.

The medicine contains aspartame (E 951), a phenylalanine derivative, which poses a risk for patients with phenylketonuria.

The medicine contains sorbitol. If a patient has known intolerance to certain sugars, medical advice should be sought before taking this medicine.

This medicine contains 6.57 mmol (or 151 mg)/dose of sodium (1 sachet of the medicine). Caution is advised when administering to patients on a sodium-restricted diet.

Use under medical supervision in patients with hepatic or renal impairment (except in decompensated stages) and in patients with thrombophlebitis.

Use in children and adolescents. Glucosamine should not be used in children and adolescents (under 18 years of age), as the safety and efficacy of the medicine in this patient group have not been established.

Use in elderly patients. No specific studies involving elderly patients have been conducted; however, based on clinical experience, dose adjustment is not required in this patient group.

Use in patients with renal and/or hepatic impairment. Dosage recommendations cannot be provided for patients with impaired renal and/or hepatic function, as no studies have been conducted in these populations.

Use during pregnancy or breastfeeding. Data on the use of the medicine during pregnancy or breastfeeding are lacking; therefore, use during these periods is contraindicated.

Ability to affect reaction speed when driving or operating machinery. Studies on the effect of the medicine on the ability to drive or operate machinery have not been conducted. Caution is advised when driving vehicles or performing tasks requiring attention. If drowsiness, fatigue, dizziness, or visual disturbances occur, driving and operating machinery are prohibited.

Method of administration and dosage.

For oral use.

Adult and elderly patients: the contents of 1 sachet, equivalent to 1.5 g of glucosamine sulfate, should be dissolved in a glass of water and taken once daily, preferably during meals.

Glucosamine is not intended for the treatment of acute pain symptoms. Symptomatic relief (particularly pain relief) may occur only after several weeks of treatment, and in some cases, even later.

If no symptomatic improvement occurs after 2–3 months of treatment, the therapy should be re-evaluated.

Children. Do not use in children and adolescents (under 18 years of age), as the safety and efficacy of the medicinal product in these patient groups have not been established.

Overdose. Cases of overdose have not been reported. Available data from acute and chronic toxicity studies in animals indicate that toxic symptoms are unlikely even at doses 200 times higher than the therapeutic dose. However, in cases of overdose, an intensification of adverse reactions is possible; therefore, symptomatic treatment aimed at restoring fluid and electrolyte balance should be administered.

Adverse reactions.

The most commonly reported adverse reactions associated with the use of glucosamine are nausea, abdominal pain, dyspepsia, flatulence, constipation, diarrhea, headache, fatigue, and somnolence. These adverse reactions are generally transient and mild in severity.

Immune system disorders: Allergic reactions (hypersensitivity).

Nervous system disorders: Headache, somnolence, dizziness.

Eye disorders: Visual disturbances.

Vascular disorders: Flushing.

Respiratory, thoracic and mediastinal disorders: Asthma, exacerbation of asthma.

Gastrointestinal disorders: Abdominal pain, flatulence, dyspepsia, diarrhea, constipation, nausea, vomiting.

Hepatobiliary disorders: Jaundice.

Skin and subcutaneous tissue disorders: Exanthema, erythema, pruritus, rash, angioneurotic edema, urticaria.

General disorders: Fatigue, edema, peripheral edema.

Investigations: Increased levels of liver enzymes.

In patients with diabetes mellitus, a negative effect on blood glucose monitoring may occur.

There have been reports of isolated spontaneous cases of hypercholesterolemia; however, a causal relationship has not been established.

Shelf life. 3 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging. 4 g in sachets, 10 sachets per pack, 20 sachets per box.

Category of release. Prescription only.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVYA".

Manufacturer's address and place of business. Ukraine, 61013, Kharkiv region, city of Kharkiv, Shevchenka Street, building 22.