Home > Drugs A – Z > Tacrolimus (By mouth)

Tacrolimus (By mouth)

Prevents your body from rejecting an organ after transplant.

What works?

Learn more about the effects of these drugs. The most reliable research is summed up for you in our featured article.

Brand names include
Astagraf XL, Envarsus XR, Novaplus Tacrolimus, Prograf
Other forms
By injection, On the skin, Oral route
Drug classes About this
Immune Suppressant

What works? Research summarized

Evidence reviews

Tacrolimus is superior to cyclosporin in improving graft survival and preventing acute rejection after kidney transplantation, but increases post‐transplant diabetes and other side effects

Kidney transplantation is the treatment of choice for most patients with end‐stage renal disease (ESRD). Strategies to increase donor organ availability and to prolong the transplanted kidney's survival have become priorities in kidney transplantation. Standard immunosuppressive therapy consists of initial treatment and maintenance regimes to prevent rejection and short courses of more intensive immunosuppressive therapy to treat episodes of acute rejection. This review compared tacrolimus and cyclosporin used as primary immunosuppression for kidney transplant recipients. Thirty studies (4102 patients) were included. Tacrolimus was shown to be superior to cyclosporin in improving graft survival and preventing acute rejection after kidney transplantation, but increases post‐transplant diabetes, neurological and gastrointestinal side effects. There was insufficient information to assess the cost of tacrolimus versus cyclosporin, and there was a general failure to consider global quality of life (QOL) for transplant recipients which may inform our understanding of patient preference and compliance.

Tacrolimus is superior to cyclosporin in improving patient survival, graft survival, and in preventing acute rejection after liver transplantation, but increases post‐transplant diabetes

Almost every liver transplant recipient takes either cyclosporin or tacrolimus to prevent rejection of the graft. This is a review of the clinical trials that compared patients initially prescribed one of the two anti‐rejection drugs after liver transplantation. Sixteen trials (3813 participants) were included. The review shows that tacrolimus is marginally better than cyclosporin at preventing patient death and graft loss. Tacrolimus is substantially better than cyclosporin at preventing rejection. No differences were seen between the drugs with respect to adverse events (renal failure, lymphoproliferative disorder) except for diabetes mellitus, which was more common with tacrolimus. After liver transplantation more patients stayed on tacrolimus than on cyclosporin. Tacrolimus is more beneficial than cyclosporine and should be considered the treatment of choice after liver transplantation. This review does not evaluate the benefit or harm of switching from one anti‐rejection drug to another.

Tacrolimus for treatment of active treatment resistant ulcerative colitis

One study that tested the effectiveness of tacrolimus as therapy for treatment resistant ulcerative colitis was reviewed. Ulcerative colitis is a relapsing inflammatory disease restricted to the colon. Symptoms include bloody diarrhea, passage of pus and/or mucus and abdominal cramping during bowel movements. Tacrolimus is an immunosuppressant that may inhibit transcription of the interleukin 2 gene required for T cell activation thereby suppressing the inflammation associated with ulcerative colitis. The study compared two dosing regimens of tacrolimus (high serum concentration and low serum concentration) with placebo (inactive pill) and found that tacrolimus was effective for improving the symptoms of ulcerative colitis at two weeks. No benefit for induction of remission was noted. Patients in the high serum concentration group were significantly more likely than placebo patients to experience side effects related to treatment. Most of the side effects that occurred during the study were mild and included finger tremor, sleepiness, hot flush, headache, queasiness, stomach discomfort, hypomagnesemia and kidney problems. Two patients developed serious side effects during the study. One patient in the high serum concentration group developed serious viral gastroenteritis. A patient in the low serum concentration group developed Acinetobacter sepsis. Tacrolimus treatment was withdrawn in these patients and both patients recovered after medical therapy. Other side effects that have been associated with tacrolimus in other studies included liver problems, seizures, hypertension, diabetes mellitus, hyperkalemia, itching, insomnia, confusion, loss of appetite, hyperglycemia, weakness, depression, cramps, neuropathy, and infections. Tacrolimus may be effective for short‐term improvement in symptoms in patients with treatment resistant colitis. There are no data from controlled trials to allow conclusions with regard to long term safety and effectiveness. The use of tacrolimus needs to be weighed against the potential risk of serious side effects. More data from well designed and controlled studies are needed to determine the long‐term safety and effectiveness of tacrolimus.

See all (122)

Summaries for consumers

Tacrolimus is superior to cyclosporin in improving graft survival and preventing acute rejection after kidney transplantation, but increases post‐transplant diabetes and other side effects

Kidney transplantation is the treatment of choice for most patients with end‐stage renal disease (ESRD). Strategies to increase donor organ availability and to prolong the transplanted kidney's survival have become priorities in kidney transplantation. Standard immunosuppressive therapy consists of initial treatment and maintenance regimes to prevent rejection and short courses of more intensive immunosuppressive therapy to treat episodes of acute rejection. This review compared tacrolimus and cyclosporin used as primary immunosuppression for kidney transplant recipients. Thirty studies (4102 patients) were included. Tacrolimus was shown to be superior to cyclosporin in improving graft survival and preventing acute rejection after kidney transplantation, but increases post‐transplant diabetes, neurological and gastrointestinal side effects. There was insufficient information to assess the cost of tacrolimus versus cyclosporin, and there was a general failure to consider global quality of life (QOL) for transplant recipients which may inform our understanding of patient preference and compliance.

Tacrolimus is superior to cyclosporin in improving patient survival, graft survival, and in preventing acute rejection after liver transplantation, but increases post‐transplant diabetes

Almost every liver transplant recipient takes either cyclosporin or tacrolimus to prevent rejection of the graft. This is a review of the clinical trials that compared patients initially prescribed one of the two anti‐rejection drugs after liver transplantation. Sixteen trials (3813 participants) were included. The review shows that tacrolimus is marginally better than cyclosporin at preventing patient death and graft loss. Tacrolimus is substantially better than cyclosporin at preventing rejection. No differences were seen between the drugs with respect to adverse events (renal failure, lymphoproliferative disorder) except for diabetes mellitus, which was more common with tacrolimus. After liver transplantation more patients stayed on tacrolimus than on cyclosporin. Tacrolimus is more beneficial than cyclosporine and should be considered the treatment of choice after liver transplantation. This review does not evaluate the benefit or harm of switching from one anti‐rejection drug to another.

Tacrolimus for treatment of active treatment resistant ulcerative colitis

One study that tested the effectiveness of tacrolimus as therapy for treatment resistant ulcerative colitis was reviewed. Ulcerative colitis is a relapsing inflammatory disease restricted to the colon. Symptoms include bloody diarrhea, passage of pus and/or mucus and abdominal cramping during bowel movements. Tacrolimus is an immunosuppressant that may inhibit transcription of the interleukin 2 gene required for T cell activation thereby suppressing the inflammation associated with ulcerative colitis. The study compared two dosing regimens of tacrolimus (high serum concentration and low serum concentration) with placebo (inactive pill) and found that tacrolimus was effective for improving the symptoms of ulcerative colitis at two weeks. No benefit for induction of remission was noted. Patients in the high serum concentration group were significantly more likely than placebo patients to experience side effects related to treatment. Most of the side effects that occurred during the study were mild and included finger tremor, sleepiness, hot flush, headache, queasiness, stomach discomfort, hypomagnesemia and kidney problems. Two patients developed serious side effects during the study. One patient in the high serum concentration group developed serious viral gastroenteritis. A patient in the low serum concentration group developed Acinetobacter sepsis. Tacrolimus treatment was withdrawn in these patients and both patients recovered after medical therapy. Other side effects that have been associated with tacrolimus in other studies included liver problems, seizures, hypertension, diabetes mellitus, hyperkalemia, itching, insomnia, confusion, loss of appetite, hyperglycemia, weakness, depression, cramps, neuropathy, and infections. Tacrolimus may be effective for short‐term improvement in symptoms in patients with treatment resistant colitis. There are no data from controlled trials to allow conclusions with regard to long term safety and effectiveness. The use of tacrolimus needs to be weighed against the potential risk of serious side effects. More data from well designed and controlled studies are needed to determine the long‐term safety and effectiveness of tacrolimus.

See all (27)

PubMed Health Blog...

read all...