TACROLIMUS

Description: Tacrolimus is an immunosuppressant that inhibits T-lymphocyte activation.

Uses

Tacrolimus is an immunosuppressant used to prevent organ rejection.
Prevention of organ rejection in liver, kidney, or heart transplant.

Warnings

Tacrolimus is assigned to Pregnancy Category C.

This drug is associated with premature delivery risk, neonatal hyperkalemia, and renal dysfunction. Animal studies revealed maternal toxicity, and decreases in pup weight, viability, and live births, and increases in abortions, late resorptions, fetal death in utero, fetal malformations, and developmental variations.

Tacrolimus Breastfeeding Warning

Tacrolimus is excreted into breastmilk and must be discontinued when breastfeeding.

Side Effects

baldness
anemia
loss of appetite
diarrhea
high concentrations of potassium in the blood
high blood pressure
nausea
vomiting
tingling sensation in the extremities
itching
tremor
fever
headache
rash
high blood sugar concentrations
abdominal pain

Other side effects include:

confusion
painful joints
increased sensitivity to light
blurred vision
insomnia
infection
jaundice (yellowing of the skin due to effects on the liver)
kidney injury
swollen ankles
seizures

Precautions

Precautions

Malignancies
Serious Infections
Mortality in female liver transplant recipients

Drug Interactions

Lansoprazole (Prevacid)
omeprazole (Prilosec)
protease inhibitors (for example, nelfinavir [Viracept] and ritonavir [Norvir])
bromocriptine (Parlodel)
cimetidine (Tagamet)
cisapride (Propulsid)
clarithromycin (Biaxin)
cyclosporine (Sandimmune; Neoral)
danazol (Danocrine)
diltiazem (Cardizem, Tiazac)
erythromycin
fluconazole (Diflucan)
itraconazole (Sporanox)
ketoconazole (Nizoral)
metoclopramide (Reglan)
methylprednisolone (Medrol)
nicardipine (Cardene)
troleandomycin (Tao)
verapamil (Calan, Isoptin, Verelan, Covera-HS)
grapefruit juice
carbamazepine (Tegretol), nifedipine (Procardia; Adalat); phenobarbital, phenytoin (Dilantin), St. John’s Wort, rifabutin, and rifampin.

Live virus vaccines and other immunosuppressants should be avoided while receiving tacrolimus.

Overdose & Brands

Dosing

Starting dose: 0.075 mg/kg/day to 0.2 mg/kg/day; taken twice daily.

Taken with food to reduce abdominal pain; but food also reduces its absorption.

Storage: Room temperature between 15 C – 30 C (59 F – 86 F).

Brands

Available Brands

Advagraf [ Astellas ]
Imugraft 0.5 [ Rainbow Life Sciences ]
Prograf [ Astellas ]
Protopic [ Johnson & Johnson ]
Rocimus [ Mega Lifesciences ]
Taclin [ Cathay Drug ]
Tacrocin [ Intas ]
Tacrotec [ United Biotech ]
Tagraf [ DéGa ] Vingraf [ Emcure Pharma ]