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Tacrolimus

Brand name is Prograf by Fujisawa. Also called FK-506

Discovered in Japan in 1984, tacrolimus is a potent immunosuppressant. Recent trials show it to be effective in managing heart transplant patients and it may be used instead of Neoral. A lower dose can be used than with cyclosporine. Prograf should not be used at the same time as cyclosporine. The current drug should be stopped at least 24 hours before beginning the other one. Some studies suggest that Prograf may cause less atherosclerosis in heart transplant patients than cyclosporine and that it may do more to offset organ mismatches.
     Prograf comes in two capsule forms and as an IV (intravenous) solution. The capsules contain 1 or 5mg anhydrous tacrolimus. The solution contains 5 mg tacrolimus/mL in castor oil and alcohol. Tacrolimus should be used with steroids. It is also used for "rescue" immunosuppression in heart transplant patients. Rescue is drug use to suppress serious episodes of rejection.

Tacrolimus Dose

This is highly individual and depends in part on how close a match your new heart is to your own body. Side effects are more closely related to blood levels than dose, so you will be closely monitored through blood testing to keep your blood levels in that narrow range between effectiveness and poison. Don't get too scared by this - remember that many of the drugs you took for heart failure had the potential to really mess you up but didn't.
     After the surgery, your blood will be tested at least every 2 to 3 days. After you go home, your blood levels of transplant drugs - including tacrolimus - will be measured at each clinic visit, which is usually twice a week for the first 2 months, once a week for 2 more months, and once a month for the rest of the first year with your new heart.
     The blood test used to measure your tacrolimus levels is called "Tacrolimus Level/Whole Blood TDX." High level increases risk of infection and may damage other organs like your kidneys. Low level invites organ rejection. Normal = 6 to 15 ng/ml. With cyclosporine, one component of your blood is tested for drug level: plasma. With tacrolimus, whole blood drug level is measured rather than just drug level in one part of your blood.
     Like cyclosporine, children need to take a higher dose of tacrolimus to get the same effect. Black patients may also need a higher dose to maintain proper blood levels.

Possible Side Effects

You will not get all, or even most, of these side effects, but they are possible. This is not a complete list. The main concerns with tacrolimus use is kidney damage, diabetes, and high blood pressure. The most common side effects are tremors, headache, insomnia, diarrhea, high blood pressure, nausea, and kidney damage. Up to 20% of tacrolimus patients may develop adult onset diabetes. Side effects usually appear early in treatment, and may get better as time passes.
     As many as 50% of patients will suffer infection, creatinine increase, headache, diarrhea or hypophosphatemia (a phosphate deficiency that results in bone defects). Do not get any vaccinations while on tacrolimus. Avoid people who have recently taken an oral polio vaccine. Call your doctor if you notice increased thirst, dry mouth, or a fruity odor on your breath. This may signal onset of diabetes, a known side effect.

Drug Interactions With Tacrolimus

Grapefruit juice should be avoided while taking tacrolimus. Drug interactions are no joke for the heart transplant recipient. You must never take any drug or over the counter medicine without checking first with your transplant cardiologist. Period. This is not a complete list.

Drug Interactions
 Raise tacrolimus level   Lower tacrolimus level   Drug interaction 
diltiazem
clotrimazole
nicardipine
nifedipine
verapamil
clarithromycin
erythromycin
troleandomycin
fluconazole
itraconazole
ketoconazole
cisapride
metoclopramide
bromocriptine
cimetidine
cyclosporine
danazol
methylprednisolone
protease inhibitors
carbamazepine
rifabutin
phenobarbital
rifampin
phenytoin
aluminum hydroxide
aminoglycosides
amphotericin B
cisplatin
cyclosporine
ganciclovir
ritonavir
vaccines
Diet and Food

Diet Food slows absorption of tacrolimus into your system. High fat foods slow it the most, but hey, you're not eating that stuff anymore anyway, are you?! ;-)
Mothers and children Prograf use during pregnancy may cause dangerously high potassium levels and kidney dysfunction in the unborn child. Tacrolimus is found in breast milk of mothers taking the drug, so nursing should be avoided.


Material taken from manuals given to potential transplant recipients at transplant centers in the USA, and from online drug monographs, the manufacturer, and medical dictionaries - Updated April 26, 2002

All information on this site is opinion only. All concepts, explanations, trials, and studies have been re-written in plain English and may contain errors. I am not a doctor. Use the reference information at the end of each article to search MedLine for more complete and accurate information. All original copyrights apply. No information on this page should be used by any person to affect their medical, legal, educational, social, or psychological treatment in any way. I am not a doctor. This web site and all its pages, graphics, and content copyright © 1997, 1998, 1999, 2000, 2001, 2002, 2003, 2004 Jon C.

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