Description

Pharmacodynamics:

At the molecular level, the effects and intracellular accumulation of tacrolimus are due to binding to a cytosolic protein (FKI3P 12). The FKBP 12-tacrolimus complex specifically and competitively inhibits calcineprin, providing calcium-dependent blocking of T-cell signaling pathways and preventing transcription of a discrete number of lymphokine genes.

Tacrolimus is a highly active immunosuppressant. In experiments in vitro and in vivo, tacrolimus clearly reduced the formation of cytotoxic lymphocytes, which play a key role in the graft rejection reaction. Tacrolimus inhibits the formation of lymphokines (interleukin -2, -3, γ-interferon), T-cell activation, expression of the interleukin-2 receptor, as well as T-helper-dependent B-cell proliferation.

Indications:

Prevention of liver or kidney allograft rejection in adult patients. Treatment of allograft rejection resistant to standard immunosuppressive therapy regimens in adult patients.

Contraindications:

Hypersensitivity to tacrolimus, other macrolides, auxiliary components of the drug. Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Dosage and administration:

Advagraf® is a once-daily oral form of tacrolimus.

Uncontrolled switching of patients from one tacrolimus preparation to another (including switching from regular capsules to extended-release capsules) is unsafe.

If clinical signs of rejection appear, consideration should be given to adjusting the immunosuppressive regimen.

Mode of application

The oral daily dose of Advagraf® is recommended to be taken in the morning once a day. Advagraf® prolonged-release capsules are taken immediately after they are removed from the blister. Patients should be warned about the presence of a desiccant (silica gel sachet) in the package, which is not intended for use. The capsules must be taken whole with a liquid (preferably water). To achieve maximum absorption of Advagraf®, it is recommended to take it on an empty stomach: 1 hour before or 2-3 hours after taking food. The missed dose should be taken as soon as possible, preferably on the same day; do not take a double dose the next morning.

Duration of taking the drug

To prevent transplant rejection, the state of immunosuppression must be maintained constantly; therefore, the duration of therapy is not limited.