Tacrolimus (Prograf)

• Type of Drug: Immunosuppressant.
• Prescribed for: Preventing the rejection of transplanted organs.

Tacrolimus (Prograf) General Information

Tacrolimus, formerly known as FK506, is derived from a bacterium. It has been shown to prolong the survival of transplanted liver, kidney, heart, bone marrow, small bowel and. pancreas, lungs and trachea, skin, cornea, and limbs in animal studies. In people, the drug is used in liver transplants and has been studied in kidney, bone marrow, heart, pancreas, and small bowel transplants, among others.

Tacrolimus works by inhibiting the activation of T-cells, an essential element of the body’s immune response, producing immune-system suppression.

Tacrolimus (Prograf) Cautions and Warnings

Transplant patients who are sensitive or allergic to Tacrolimus should be given another drug. Some people may also be allergic to chemically modified castor oil, which is used in Tacrolimus injection.

Tacrolimus can cause kidney damage, especially when taken in high doses. This effect has been noted in 33 to 40 percent of liver transplant patients. To avoid excess kidney damage, this drug should not be taken together with Cyclosporine, another organ transplant drug. These drugs should be separated by at least 24 hours.

Mild elevations of blood potassium were noted in 10 to 44 percent of liver transplant patients.

Tremors, headaches, muscle function changes, changes in mental state and sense perception, or other nervous-system problems occur in about half of people receiving a liver transplant. Seizures have also occurred. In some cases, these side effects may be associated with large amounts of Tacrolimus in the blood.
As with other immune suppressants, people taking Tacrolimus have a better chance of developing a lymphoma or other malignancy. The chance increases with the degree of immune suppression and the length of time that the drug is taken. A disorder related to Epstein-Barr virus (EBV) infection has also been reported.

People with kidney disease should receive lower doses of Tacrolimus. People who experience post-transplant reduction in liver function can develop kidney damage.

Mild to moderate high blood pressure is a common side effect of Tacrolimus and can be a sign of kidney damage. People taking this drug should measure their blood pressure regularly.

Tacrolimus (Prograf) Possible Side Effects

• Most common: headache, tremors, sleeplessness, tingling in hands or feet, diarrhea, nausea, constipation, loss of appetite, vomiting, liver or kidney abnormalities, high blood pressure, urinary infection, infrequent urination, anemia, increased white-blood-cell counts, reduced blood-platelet counts, changes in blood-potassium level, reduced blood-magnesium, high blood-sugar, fluid in the lungs and other lung problems, difficulty breathing, itching, rash, abdominal pains, pain, fever, weakness, back pains, abdominal fluid buildup, and retention of fluid.
• Less common: abnormal dreaming, anxiety, confusion, depression, dizziness, instability, hallucination, poor coordination, muscle spasms, psychosis, tiredness, unusual thoughts, double vision or other visual disturbances, ringing or buzzing in the ears, upset stomach, yellow discoloration of skin or whites of the eyes, trouble swallowing, stomach gas, stomach bleeding, fungus infection of the mouth, bloody urine, chest pain, rapid heartbeat, low blood pressure, diabetes, black-and-blue marks, muscle and joint aches, leg cramps, muscle weakness, asthma, bronchitis, coughing, sore throat, pneumonia, stuffy and runny nose, sinus irritation, voice changes, sweating, skin rashes, and herpes infections.

Tacrolimus (Prograf) Drug Interactions

• Tacrolimus should not be taken at the same time as other immune suppressants so as to avoid excessive suppression of the immune system.
• Tacrolimus may cause more kidney damage when taken together with other drugs that also cause kidney problems, including aminoglycoside antibiotics, Amphotericin B, Cisplatin, and Cyclosporine.
• Antifungal drugs, Bromocriptine, calcium channel blockers, Cimetidine, Clarithromycin, Danazol, Diltiazem, Erythromycin, Methylprednisolone, and Metoclopramide can increase Tacrolimus blood levels and possible drug side effects.
• Carbamazepine, Phenobarbital, Phenytoin, Rifampin, and Rifampicin can reduce the amount of Tacrolimus in the blood.
• Vaccination may be less effective during Tacrolimus use. Live vaccines (measles, mumps, rubella, oral polio, BCG, yellow fever, and TY 21 typhoid) should be avoided.

Food Interactions

Food interferes with the absorption of Tacrolimus into the blood. Take this drug either 1 hour before or 2 hours after meals.

Usual Dose

Adult and Child: 0.075 to 0.15 mg per pound per day divided into 2 doses. Your dosage will be reduced to the lowest effective dose. Children may require larger doses than adults. Dosing is usually started, at the high end of the recommended dose and then reduced to the lowest effective level.

Overdosage

Tacrolimus overdose can be expected to produce exaggerated drug side effects. Overdose victims should be taken to a hospital emergency room for treatment. ALWAYS bring the medicine bottle with you.

Tacrolimus (Prograf) Special Information

It is extremely important for you to take this medicine exactly as prescribed. If you do forget a dose of Tacrolimus, take it as soon as you remember. If it is almost time for your next dose, skip the forgotten dose and continue with your regular schedule. Do not take a double dose, and call your doctor if you forget 2 or more doses in a row.

People taking Tacrolimus require regular testing to monitor their; progress.

Call your doctor at the first sign of fever; sore throat; tiredness; weakness; nervousness; unusual bleeding or bruising; tender or swollen gums; convulsions; irregular heartbeat; confusion; numbness or tingling of your hands, feet, or lips; difficulty breathing; severe stomach pains with nausea; or bloody urine. Other drug effects are less serious but should be brought to your doctor’s attention, particularly if they are unusually bothersome or persistent.

It is important to maintain good dental hygiene while faking Tacrolimus and to use extra care when using your toothbrush or dental floss because the drug may make you more susceptible to dental infections. Tacrolimus suppresses the normal body systems that fight infection. See your dentist regularly while taking this medicine.

This medicine should be continued as long as prescribed by your doctor. Do not stop faking it because of side effects or other problems. If you cannot tolerate the oral form, this drug can be given by injection, though the oral capsules are preferable.

Tacrolimus (Prograf) Special Populations

Pregnancy/Breast-feeding
In animal studies using half the human dose, this drug was lethal to embryos and affected the ability of females to become pregnant. Malformations were seen at higher doses. The drug passes into the blood of the developing fetus and should be used during pregnancy only if absolutely necessary. Babies born to mothers taking this drug have had high blood potassium and poor kidney function.
Tacrolimus passes into breast milk. Nursing mothers who must take this drug should bottle-feed their babies.

Seniors
Older adults may take this drug, but their dose may have to be reduced to accommodate normal loss of kidney function.