Envarsus (tacrolimus) tablets with prolonged release 0.75 mg. №30

Description

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

Envarsus 0.75 mg. excipients: hypromellose; lactose monohydrate; macrogol 6000; poloxamer 188; magnesium stearate; tartaric acid (E 334); butylhydroxytoluene (E 321); dimethicone 350.

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.

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

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

Interaction with other medicinal products and other forms of interaction
Systemically available tacrolimus is metabolized by hepatic CYP3A4. There is also evidence of gastrointestinal metabolism of CYP3A4 in the intestinal wall. Concomitant use of drugs 5 with an established inhibitory or inducing effect on CYP3A4 may affect the metabolism of tacrolimus and, accordingly, increase or decrease the concentrations of tacrolimus in the blood. When concomitant use of substances that may potentially alter CYP3A4 metabolism or otherwise affect tacrolimus blood levels, it is recommended that blood tacrolimus levels be closely monitored and that renal function and other side effects be monitored and, if necessary, discontinued or modified. dose of tacrolimus, to maintain equivalent tacrolimus exposure (see sections “Method and Dosage” and “Specifics”).