Leflunomide Canon pills 20mg, 30pcs

Composition

Active ingredient:

leflunomide 20 mg;

Auxiliary substances:

hyprolose (hydroxypropylcellulose) 6.7 mg,

calcium hydrophosphate dihydrate 72 mg,

corn starch 31.7 mg,

croscarmellose sodium (primellose) 7.5 mg,

magnesium stearate 1.5 mg,

microcrystalline cellulose 40.6 mg;

Shell composition:

Selecoate AQ-02003 6 mg, including:

hypromellose (hydroxypropylmethylcellulose)  3.6 mg,

macrogol 6000 (polyethylene glycol 6000) 1.2 mg,

titanium dioxide 1.2 mg

Pharmacological action

Leflunomide Canon is a drug with antiproliferative, immunomodulatory (immunosuppressive) and anti-inflammatory effects. The active metabolite of leflunomide A 771726 inhibits the enzyme dehydroorotate dehydrogenase and has an antiproliferative effect. a771726 inhibits mitogen-induced proliferation and synthesis of T-lymphocyte DNA in vitro.

The therapeutic effect of leflunomide has been shown in several experimental models of autoimmune diseases, including rheumatoid arthritis.

Pharmacokinetics

After oral use, the absorption is 82-95%. Food intake does not affect the absorption of leflunomide.

Leflunomide is rapidly metabolized in the intestinal wall and liver to one major (A 771726) metabolite and several minor metabolites, including 4-trifluoromethylalanine. Cmax of metabolite A 771726 is determined within 1-24 hours after a single dose. In plasma, A 771726 binds rapidly to albumin. The unbound fraction A of 771726 is 0.62%.

The biotransformation of leflunomide to A 771726 and the subsequent metabolism of A 771726 itself are controlled by several enzymes and occur in microsomal and other cellular fractions.

Trace amounts of leflunomide are detected in plasma, urine, and feces. Elimination of A771726 is slow and is characterized by a clearance of 31 ml / h. T1 / 2 – about 2 weeks.

In patients undergoing hemodialysis, excretion is faster and T1 / 2 decreases.

Indications

Basic therapy of rheumatoid arthritis to reduce the symptoms of the disease and delay the development of structural joint damage.

Use during pregnancy and lactation

Leflunomide Canon is contraindicated in pregnancy, lactation and children under 18

Contraindications

Liver function disorders, severe immunodeficiency conditions (including AIDS); severe bone marrow hematopoiesis disorders or anemia, leukopenia, thrombocytopenia due to other causes (except rheumatoid arthritis), severe infections, moderate or severe renal failure (due to little clinical experience), severe hypoproteinemia (including nephrotic syndrome), pregnancy, lactation, children and adolescents under 18 years of age, hypersensitivity to leflunomide.

Side effects

From the cardiovascular system:  often-increased blood pressure.

From the digestive system:  often – diarrhea, nausea, vomiting, anorexia, lesions of the oral mucosa (aphthous stomatitis, ulceration of the lips), abdominal pain, increased levels of liver enzymes (especially ALT, less often – GGT, alkaline phosphatase, bilirubin); rarely – hepatitis, jaundice, cholestasis; in some cases – liver failure, acute liver necrosis.

Musculoskeletal disorders:  often-tendovaginitis; possible-torn ligaments.

Dermatological reactions:  often – hair loss, eczema, dry skin; possible-Stevens-Johnson syndrome, Lyell’s syndrome, erythema multiforme.

From the hematopoietic system:  often-leukopenia (leukocytes more than 2000 / µl); possible-anemia, thrombocytopenia (platelets less than 100 000/µl); rarely-eosinophilia, leukopenia (leukocytes less than 2000/µl), pancytopenia; in some cases-agranulocytosis. The risk of developing hematological disorders increases with recent, concomitant and subsequent use of myelotoxic drugs.

Allergic reactions:  often-rash (including macular-papular), pruritus; atypical-urticaria; in some cases-anaphylactic reactions.

From the side of exchange processes:  mild hyperlipidemia, hypophosphatemia, decreased uric acid levels. Laboratory data (not clinically confirmed) indicate a slight increase in LDH, CPK.

Other services:  in some cases-the development of severe infections and sepsis; possible development of rhinitis, bronchitis and pneumonia. When using immunosuppressive drugs, the risk of developing malignant and some lymphoproliferative processes increases. It is impossible to exclude the possibility of a reversible decrease in the concentration of sperm, the total number of spermatozoa and their motility.

Interaction

An increase in adverse reactions may occur in the case of recent or concomitant use of hepatotoxic or hematotoxic drugs, or when these drugs are started after treatment with leflunomide without a “wash” procedure.

In vitro studies have shown that the leflunomide A metabolite 771726 inhibits the activity of the CYP2C9 isoenzyme. When used concomitantly with drugs that are metabolized by this enzyme system (phenytoin, warfarin, tolbutamide), the development of undesirable drug interaction effects cannot be excluded.

How to take, course of use and dosage

Inside, the initial dose is 100 mg once for 3 days, then they switch to maintenance treatment-10-20 mg once a day.

Tablets should be swallowed whole, washed down with a sufficient amount of liquid.

Overdose

Treatment: colestyramine or activated charcoal. Colestyramine, taken orally at 8 g 3 times a day during the day, reduces the content of a771726 in plasma by about 40% after 24 hours and by 49-65% after 48 hours.

use of activated carbon (as a suspension) orally or through a gastric tube (50 g every 6 hours during the day) reduces the concentration of the active metabolite A 771726 in plasma by 37% after 24 hours and by 48% after 48 hours.

Special instructions

Application is possible only after a thorough medical examination of the patient.

Before starting treatment, you should keep in mind the possibility of increasing the number of side effects in patients who have previously received other basic drugs for the treatment of rheumatoid arthritis, which have a hepatotoxic and hematotoxic effect.

The active metabolite of leflunomide A 771726 is characterized by a long T1 / 2. Therefore, side effects may occur even after discontinuation of leflunomide treatment. If such cases of toxicity occur or when switching to another basic drug after treatment with leflunomide, the “washing” procedure should be performed (after stopping treatment with leflunomide, colestyramine is prescribed at a dose of 8 g 3 times / day for 11 days or 50 g of activated carbon, ground into powder,4 times/day for 11 days).

It should be borne in mind that with the development of severe dermatological side effects, severe infections, leflunomide should be discontinued and the “washing”procedure should be started immediately.

Patients with tuberculin reactivity should be monitored because of the risk of tuberculosis activation.

Given the long T1 / 2 of leflunomide, live vaccination is not recommended during treatment.

Composition

Tablet Form of production

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Leflunomide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets