Drug information of Tacrolimus
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
Tacrolimus acts by inhibiting interleukin-2 and used in organ transplant to avoid rejection. It is also used in atopic dermatitis .
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.
• 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 contraindicationshypersensitivity to this drug
InteractionsAmphotericin B , Bromocriptin , Erythromycin , Omeprazole , Pamidronate , Pneumovax , Daunorubicin , Cyclosporine , Troleandomycin , Glycerol Phenylbutyrate , Gadofosveset , Blinatumomab , Betrixaban , Foscarnet , Apalutamide , Crizotinib , Edoxaban , Ustekinumab , Alefacept , Letermovir , Adenovirus types 4 and 7 live, oral , Diatrizoate (Amidotrizoic acid) , Olsalazine , Baricitinib , Dabrafenib , Netilmicin , Halofantrine , Grepafloxacin , Canakinumab , Basiliximab , Canagliflozin , Efavirenz , Aceclofenac , Sulindac , Ibandronate , lumacaftor and Ivacaftor , Golimumab , Anagrelide , Hib vaccine , Triamterene , brigatinib , Parecoxib , Afatinib , Tofacitinib , vandetanib , Indinavir , Mesoridazine , Mefloquine , Toremifene , methylene blue , saquinavir , mitotane , Meglumine Compound , Mifepristone , Methylprednisolone , Naproxen , Vincristin , Rifabutin , Kanamycin , Pentamidine , Diltiazem , Rifampin , Cimetidine , Cisplatin , Phenobarbital , Phenytoin , Metoclopramide , Carbamazepine , Clarithromycin , Ethinyl Estradiol
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.