Adenuric (febuxostat) coated tablets 120 mg. №28

Description

Composition

active substance: febuxostat;

1 film-coated tablet contains febuxostat 120 mg;

auxiliary substances: lactose monohydrate, hydroxypropyl cellulose, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, colloidal aqueous silicon dioxide, polyvinyl alcohol, titanium dioxide (E 171), polyethylene glycol, talc, iron oxide yellow (E 172).

Pharmacodynamics

Uric acid is the end product of purine metabolism in humans and is produced by the following reaction: hypoxanthine → xanthine → uric acid. Xanthine oxidase catalyzes both steps of this reaction. Febuxostat is a derivative of 2-arylthiazole. Its therapeutic effect is associated with a decrease in the concentration of uric acid in the blood serum by selective suppression of xanthine oxidase. Febuxostat is a potent and selective non-purine inhibitor of xanthine oxidase (NP-SIXO) with an in vitro inhibitory constant (Ki) of <1 nanomolar. Febuxostat has been shown to significantly inhibit the activity of both the oxidized and reduced forms of xanthine oxidase. At therapeutic concentrations, febuxostat does not affect other enzymes involved in the metabolism of purines or pyrimidines, such as guanine deaminase, hypoxanthine guanine phosphoribosyl transferase, orotate phosphoribosyl transferase, orotidine monophosphate decarboxylase, or purine nucleoside phosphorylase.

Indications

Adenuric treatment of chronic hyperuricemia in patients with diseases accompanied by the deposition of urate crystals, including those with tophi and / or gouty arthritis at present or in history.

Treatment and prevention of hyperuricemia in adult patients undergoing chemotherapy for hematologic malignancies at moderate or high risk of tumor lysis syndrome (TLS).

Dosage

Gout. The recommended dose of ADENURIK® is 80 mg once a day orally, regardless of food intake.

If the concentration of uric acid in the blood serum exceeds 6 mg/dl (357 μmol/l) after 2–4 weeks of treatment, an increase in the dose of ADENURIK® to 120 mg 1 time per day should be considered.

The effect of the drug appears quickly enough, which makes it possible to re-determine the concentration of uric acid after 2 weeks. The goal of treatment is to reduce the concentration of uric acid in the serum and maintain it at a level of less than 6 mg/dL (357 μmol/L). The duration of prevention of gout attacks is recommended to be at least 6 months. Tumor lysis syndrome (TLS).

The recommended dose Febuxostat is 120 mg once a day orally, regardless of food intake. The use of ADENURIK® should be started two days before the start of cytotoxic therapy and continued for at least 7 days; however, the duration of therapy can be extended up to 9 days according to the duration of chemotherapy and clinical evaluation.

Elderly patients. No dose adjustment is required for this category of patients.

Kidney failure. In patients with severe renal impairment (creatinine clearance <30 ml/min), the efficacy and safety of the drug have not been sufficiently studied. No dose adjustment is required for patients with mild or moderate renal impairment.

Liver failure. The efficacy and safety of febuxostat in patients with severe hepatic impairment (Child-Pugh Class C) have not been studied.

Gout. In mild liver dysfunction, the recommended dose is 80 mg. The experience of using the drug in moderate liver function disorders is limited. Tumor lysis syndrome (TLS). Only subjects with severe hepatic impairment were excluded from the pivotal phase III study (FLORENCE). For patients included in the study, dose adjustment due to liver function is not required.

Contraindications

Hypersensitivity to the active substance or any other auxiliary component of the drug.