Prograf: Advanced Immunosuppression for Transplant Success
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Synonyms | |||
Prograf (tacrolimus) is a cornerstone immunosuppressive agent specifically formulated to prevent organ rejection in transplant recipients. As a calcineurin inhibitor, it operates by selectively inhibiting T-lymphocyte activation, a critical pathway in the immune response against foreign tissue. This mechanism provides a targeted approach to maintaining graft function while balancing immunosuppressive efficacy with manageable side effect profiles. Its use is integral in heart, kidney, liver, and other solid organ transplantation protocols, often forming part of a multi-drug regimen to optimize patient outcomes and long-term allograft survival.
Features
- Active ingredient: Tacrolimus
- Available formulations: Immediate-release capsules, prolonged-release capsules, injection for intravenous use
- Mechanism: Calcineruin inhibitor, suppressing interleukin-2 synthesis and T-cell proliferation
- Bioavailability: Variable, with approximately 20–25% oral bioavailability
- Half-life: Approximately 12 hours in healthy adults; prolonged in hepatic impairment
- Metabolism: Primarily hepatic, via CYP3A4/5 enzymes
- Excretion: Mostly fecal
Benefits
- Significantly reduces incidence of acute rejection episodes in transplant recipients
- Provides flexible dosing options with both immediate and prolonged-release formulations
- Allows for therapeutic drug monitoring to individualize therapy and improve safety
- Contributes to long-term graft survival when used as part of maintenance immunosuppression
- May enable corticosteroid-sparing regimens in appropriate patient populations
- Established efficacy across multiple organ transplant types
Common use
Prograf is indicated for the prophylaxis of organ rejection in patients receiving allogeneic liver, kidney, or heart transplants. It is used in combination with other immunosuppressants, typically including corticosteroids and sometimes antiproliferative agents. In clinical practice, initiation occurs immediately post-transplantation, with therapy continuing indefinitely as maintenance immunosuppression. Off-label uses may include prevention of rejection in other solid organ transplants, graft-versus-host disease prophylaxis following hematopoietic stem cell transplantation, and treatment of certain autoimmune conditions, though these applications require careful specialist supervision.
Dosage and direction
Dosing must be highly individualized based on transplant type, time since transplantation, concomitant immunosuppression, and therapeutic drug monitoring.
Initial oral dosage:
- Liver transplantation: 0.10–0.15 mg/kg/day in two divided doses
- Kidney transplantation: 0.2 mg/kg/day in two divided doses
- Heart transplantation: 0.075 mg/kg/day in two divided doses
Administration:
- Take consistently with respect to food (either always with food or always on empty stomach)
- Swallow capsules whole with water; do not crush, chew, or break
- Doses should be taken approximately 12 hours apart
- IV administration is reserved for patients unable to take oral medication, with conversion ratio of 1:4 (IV:oral)
Therapeutic trough concentrations are typically maintained at:
- Early post-transplant: 10–15 ng/mL
- Maintenance phase: 5–10 ng/mL
Dosage adjustments are made based on regular therapeutic drug monitoring, clinical response, and toxicity assessments.
Precautions
- Requires careful therapeutic drug monitoring due to narrow therapeutic index
- Increased susceptibility to infections and possible development of lymphoma and other malignancies
- May cause hypertension, which should be monitored and treated appropriately
- Neurotoxic effects, including tremor, headache, and changes in mental status, may occur
- Hyperkalemia and hypomagnesemia are common and require monitoring
- Glucose metabolism should be monitored due to risk of new-onset diabetes mellitus
- Avoid live vaccines during therapy
- Pregnancy Category C: Use only if potential benefit justifies potential risk to fetus
Contraindications
- Hypersensitivity to tacrolimus or any component of the formulation
- Concomitant use with cyclosporine (must discontinue cyclosporine at least 24 hours before initiating tacrolimus)
- Patients with known hypersensitivity to hydrogenated castor oil (for IV formulation)
Possible side effects
Very common (>10%):
- Tremor
- Headache
- Hypertension
- Diarrhea
- Nausea
- Renal dysfunction
- Hyperglycemia
- Hypomagnesemia
- Hyperkalemia
- Insomnia
Common (1-10%):
- Seizures
- Confusion
- Anxiety
- Photosensitivity
- Pruritus
- Rash
- Anemia
- Leukocytosis
- Thrombocytopenia
- Weight gain
Uncommon (<1%):
- Posterior reversible encephalopathy syndrome (PRES)
- Hemolytic uremic syndrome
- Thrombotic thrombocytopenic purpura
- Myocardial hypertrophy
- Pancreatitis
- Hearing loss
- Tinnitus
Drug interaction
Tacrolimus is extensively metabolized by CYP3A4 and is a substrate for P-glycoprotein, resulting in numerous clinically significant interactions:
Strong inhibitors of CYP3A4 (increase tacrolimus levels):
- Ketoconazole, itraconazole, voriconazole, posaconazole
- Clarithromycin, erythromycin
- Diltiazem, verapamil
- Grapefruit juice
- Cyclosporine
Strong inducers of CYP3A4 (decrease tacrolimus levels):
- Rifampin, rifabutin
- Carbamazepine, phenobarbital, phenytoin
- St. John’s Wort
Other significant interactions:
- NSAIDs: Increased nephrotoxicity risk
- Potassium-sparing diuretics: Increased hyperkalemia risk
- Vaccines: Diminished immune response
- Other nephrotoxic drugs: Additive renal impairment
Missed dose
If a dose is missed, take it as soon as remembered unless it is nearly time for the next dose. Do not double the dose to make up for a missed dose. Resume the regular dosing schedule. Patients should maintain accurate dosing records and contact their transplant team if multiple doses are missed, as this may require additional monitoring or dosage adjustment.
Overdose
Symptoms of overdose are primarily extensions of pharmacological effects and may include:
- Severe renal impairment
- Tremor, headache, mental status changes
- Hyperkalemia
- QT prolongation
- Seizures
Management involves immediate discontinuation of tacrolimus and supportive care. General supportive measures and symptomatic treatment should be implemented. Hemodialysis is not effective due to high protein binding and extensive erythrocyte distribution. Charcoal hemoperfusion may be considered in severe cases.
Storage
- Store at 25°C (77°F); excursions permitted to 15–30°C (59–86°F)
- Keep in original container with lid tightly closed
- Protect from moisture and light
- Do not freeze
- Keep out of reach of children
- Do not use after expiration date
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made by qualified healthcare professionals based on individual patient characteristics. Dosage and administration must be determined by a physician experienced in immunosuppressive therapy. Regular monitoring of tacrolimus blood concentrations, renal function, electrolytes, and other parameters is essential. Patients should not adjust or discontinue medication without consulting their healthcare provider.
Reviews
“After my kidney transplant 5 years ago, Prograf has been essential to maintaining my graft function. The therapeutic drug monitoring allows my team to fine-tune the dosage, and while I experienced some tremor initially, it subsided with dosage adjustment.” — Renal transplant recipient, 47
“As a transplant coordinator, I’ve observed consistent outcomes with tacrolimus-based regimens. The ability to monitor levels precisely helps us balance efficacy and toxicity, particularly important in our pediatric transplant population.” — Transplant coordinator, 12 years experience
“The transition from cyclosporine to tacrolimus in our liver transplant program has resulted in improved rejection rates and better long-term outcomes. The side effect profile, while significant, is generally manageable with careful monitoring.” — Transplant hepatologist, academic medical center