Envarsus (tacrolimus) tablets with prolonged release 4 mg. №30

Description

Envarsus Storage
active substance: tacrolimus (as a monohydrate); 1 tablet contains 0.75 mg, 1 mg or 4 mg of tacrolimus (as a monohydrate);

Envarsus excipients:

hypromellose; lactose monohydrate; macrogol 6000; poloxamer 188; magnesium stearate; tartaric acid (E 334); butylhydroxytoluene (E 321); dimethicone 350.

Envarsus Dosage form
Prolonged-release tablets.

Basic physical and chemical properties:

0.75 mg:

oval, white to off-white, uncoated tablets, engraved with 0.75 on one side and TCS on the other.

1 mg:

oval, white to off-white, uncoated tablets, engraved with “1” on one side and “TCS” on the other side.

4 mg:

oval, white to off-white, uncoated tablets engraved with “4” on one side and “TCS” on the other side.

Pharmacotherapeutic group
Immunosuppressants, calcineurin inhibitors. ATX code: L04A D02.

Pharmacological properties

Pharmacodynamics.

Mechanism of action

At the molecular level, the effects of tacrolimus are due to binding to the cytosolic protein (FKBP12), which is responsible for the intracellular accumulation of the compound. The FKBP12-tacrolimus complex specifically and competitively binds to and inhibits calcineurin, leading to calcium-dependent inhibition of T cell signaling transduction pathways, thereby preventing the transcription of a discrete set of cytokine genes.

Pharmacodynamic effects

2 Tacrolimus is a highly active immunosuppressive agent, the activity of which has been proven in in vitro and in vivo experiments.

In particular, tacrolimus inhibits the formation of cytotoxic lymphocytes, which are mainly responsible for graft rejection. Tacrolimus inhibits T-cell activity and T-helper-dependent B-cell proliferation, as well as the formation of lymphokines (such as interleukins-2, -3 and γ-interferon) and the expression of the interleukin-2 receptor.

Indication
Prevention of renal or liver allograft rejection in adult recipients. Treatment of allograft rejection resistant to treatment with other immunosuppressive drugs in adult patients.

Contraindication
Hypersensitivity to the active substance or to any of the excipients. Hypersensitivity to other macrolides.

Storage conditions
Store in the original aluminum foil bag for protection from light at a temperature not exceeding 25 ° C. Keep out of reach of children.