Drug information of Tacrolimus


Tacrolimus

Drug group:

Tacrolimus is an immunosuppressive drug .It was discovered in 1984 from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis

Mechanism of effect

Tacrolimus acts by inhibiting the production of interleukin-2, a molecule that promotes the development and proliferation of T cells, which are vital to the body's learned (or adaptive) immune response

Pharmacodynamic

Tacrolimus acts by inhibiting interleukin-2 and used in organ transplant to avoid rejection. It is also used in atopic dermatitis .

Pharmacokinetics

The rate of absorption of tacrolimus is variable with peak blood or plasma concentrations being reached in 0.5 to 6 hours; approximately 25% of the oral dose is bioavailable.
half-life is 12 hours .
The elimination of tacrolimus is decreased in the presence of liver impairment.

Dosage

KIDNEY TRANSPLANT:
In combination with azathioprine: Initial dose: 0.1 mg/kg orally every 12 hours. Initiate within 24 hours of surgery, but delay until renal function has recovered.
-In combination with mycophenolatemofetil (MMF)/interleukin-2 (IL-2) receptor antagonist: Initial dose: 0.05 mg/kg orally every 12 hours. Initiate within 24 hours of surgery, but delay until renal function has recovered.
LIVER TRANSPLANT:
Initial dose: 0.05 to 0.075 mg/kg orally every 12 hours. Initiate no sooner than 6 hours after surgery.
HEART TRANSPLANT:
-Initial dose: 0.0375 mg/kg orally every 12 hours. Initiate no sooner than 6 hours after surgery
Dose Adjustments
Concomitant use of cyclosporine: Avoid concomitant use; discontinue tacrolimus or cyclosporine at least 24 hours prior to initiating the other. In the presence of elevated tacrolimus or cyclosporine concentrations, further delay dosing with the other drug.

Drug contraindications

hypersensitivity to this drug

Alerts

Tacrolimus may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away

Points of recommendation

Before using tacrolimus let your doctor know any following conditions:
*if you are allergic to it; or to other macrolide medications (such as sirolimus); or if you have any other allergies.
*your medical history, especially of: mineral imbalances (such as high potassium), kidney disease, any recent/current infections, cancer, liver disease, high blood pressure, diabetes.
Avoid eating grapefruit or drinking grapefruit juice while taking tacrolimus.

Pregnancy level

C

Related drugs

pimecrolimus , Cyclosporine


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