Prograf: Advanced Immunosuppression for Transplant Success
Prograf
| Product dosage: 0.5mg | |||
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| 360 | $2.00
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| Product dosage: 1mg | |||
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Synonyms | |||
Prograf (tacrolimus) is a cornerstone calcineurin inhibitor immunosuppressant, meticulously engineered to prevent organ rejection in transplant recipients. Its potent mechanism selectively inhibits T-lymphocyte activation, providing a critical foundation for long-term graft survival. This macrolide immunosuppressant is indicated for the prophylaxis of organ rejection in patients receiving allogeneic liver, kidney, or heart transplants, often as part of a comprehensive immunosuppressive regimen. Clinical evidence supports its efficacy in maintaining immunosuppression while allowing for tailored therapeutic drug monitoring to optimize individual patient outcomes.
Features
- Active pharmaceutical ingredient: Tacrolimus
- Available formulations: Immediate-release capsules (0.5 mg, 1 mg, 5 mg), prolonged-release capsules, injection for intravenous use
- Mechanism: Calcineurin inhibition, preventing interleukin-2 transcription and T-cell proliferation
- High potency: 10-100 times more potent than cyclosporine in vitro
- Narrow therapeutic index requiring therapeutic drug monitoring
- Bioavailability: Approximately 17-22% (varies with formulation and patient factors)
- Protein binding: Extensive binding to albumin and alpha-1-acid glycoprotein
- Metabolism: Primarily hepatic via CYP3A4/5 enzyme system
- Half-life: Approximately 12 hours in healthy volunteers (prolonged in hepatic impairment)
Benefits
- Significantly reduces acute rejection rates in solid organ transplantation
- Enables corticosteroid-sparing regimens, reducing steroid-related complications
- Provides flexible dosing options with multiple formulations for individualized therapy
- Established therapeutic drug monitoring protocols for precision dosing
- Demonstrated long-term graft survival benefits in clinical studies
- May improve cosmetic outcomes compared to other immunosuppressants (reduced hirsutism and gingival hyperplasia)
Common use
Prograf is primarily utilized as a maintenance immunosuppressive agent following solid organ transplantation. It is typically initiated immediately post-transplantation, often in combination with other immunosuppressants such as mycophenolate mofetil and corticosteroids. The medication is commonly used in adult and pediatric patients receiving liver, kidney, or heart transplants, with dosing carefully adjusted based on therapeutic drug monitoring results. Some transplant centers also employ Prograf in combination regimens for intestinal, lung, and pancreas transplantation, though these are considered off-label uses.
Dosage and direction
Initial dosing: Liver transplantation: 0.10-0.15 mg/kg/day in two divided doses; Kidney transplantation: 0.15-0.20 mg/kg/day in two divided doses; Heart transplantation: 0.075-0.15 mg/kg/day in two divided doses. Administer consistently with regard to meals, preferably on an empty stomach.
Therapeutic monitoring: Maintain whole blood trough concentrations typically between 5-20 ng/mL during early post-transplant period, with target ranges decreasing over time. Specific target ranges vary by transplant type, time since transplantation, and institutional protocols.
Dose adjustments: Required based on clinical response, toxicity, and concomitant medications that affect CYP3A4 metabolism. Reduce dosage in hepatic impairment. Pediatric patients may require higher doses per body weight compared to adults.
Precautions
- Requires careful therapeutic drug monitoring due to narrow therapeutic index
- Increased susceptibility to infections and possible development of lymphoma and other malignancies
- Monitor renal function regularly; nephrotoxicity may occur
- Hyperkalemia and hypomagnesemia may develop; monitor electrolytes
- Glucose metabolism abnormalities, including new-onset diabetes, may occur
- Neurotoxic effects including tremor, headache, and seizures have been reported
- Hypertension may develop and require antihypertensive therapy
- 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
- Hypersensitivity to polyoxyl 60 hydrogenated castor oil (injection formulation only)
- Concurrent use with cyclosporine (increased nephrotoxicity risk)
- Avoid concomitant use with strong CYP3A4 inhibitors unless benefits outweigh risks
Possible side effect
Very common (>10%): Tremor, headache, hypertension, diarrhea, nausea, renal impairment, hyperglycemia, hypomagnesemia, hyperkalemia
Common (1-10%): Insomnia, paresthesia, seizures, leukopenia, anemia, vomiting, abdominal pain, rash, pruritus, alopecia
Uncommon (0.1-1%): Pancreatitis, hepatic dysfunction, thrombocytopenia, hearing loss, photosensitivity
Rare (<0.1%): Toxic epidermal necrolysis, Stevens-Johnson syndrome, hemolytic uremic syndrome, posterior reversible encephalopathy syndrome (PRES)
Drug interaction
Strong CYP3A4 inhibitors: Ketoconazole, itraconazole, voriconazole, clarithromycin, erythromycin - significantly increase tacrolimus levels (dose reduction required)
Strong CYP3A4 inducers: Rifampin, rifabutin, carbamazepine, phenytoin, St. John’s wort - significantly decrease tacrolimus levels (dose increase may be needed)
Nephrotoxic agents: Aminoglycosides, amphotericin B, NSAIDs - increased risk of nephrotoxicity
Potassium-sparing diuretics, ACE inhibitors: Increased risk of hyperkalemia
Vaccines: Diminished immune response to vaccines; avoid live vaccines
Missed dose
If a dose is missed, administer as soon as remembered on the same day. If remembered near the time of the next scheduled dose, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed dose. Consistent timing of administration is critical for maintaining therapeutic drug levels. Contact your transplant team for specific guidance regarding missed doses, particularly in the early post-transplant period.
Overdose
Symptoms may include tremor, headache, nausea, vomiting, infection, nephrotoxicity, hyperglycemia, and neurotoxicity (including seizures and encephalopathy). Management includes immediate discontinuation of Prograf and supportive care. Hemodialysis is not effective due to extensive protein binding. Charcoal hemoperfusion may be considered in severe cases. Maintain adequate renal function and monitor tacrolimus levels frequently until they return to therapeutic range.
Storage
Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F). Keep in original container, tightly closed. Protect from moisture and light. Do not freeze. Keep out of reach of children. Do not use beyond the expiration date printed on the packaging. Capsules should be kept in the blister pack until immediately before use.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Prograf should be used only under the supervision of a qualified healthcare professional experienced in immunosuppressive therapy. Dosage must be individualized based on therapeutic drug monitoring and clinical response. Patients should not adjust their dosage without consulting their transplant team. The full prescribing information should be consulted before initiating therapy.
Reviews
“After my kidney transplant, Prograf has been instrumental in maintaining stable graft function for over seven years. The therapeutic drug monitoring provides reassurance that my levels remain appropriate.” - Renal transplant recipient
“As a transplant hepatologist, I appreciate Prograf’s predictable pharmacokinetics and the ability to fine-tune dosing based on trough levels. It remains a cornerstone of our immunosuppressive protocols.” - Transplant specialist
“The transition from twice-daily to once-daily prolonged-release formulation significantly improved medication adherence for our pediatric liver transplant patients without compromising efficacy.” - Pediatric transplant coordinator
“While effective, the required frequent monitoring and potential metabolic side effects necessitate careful patient education and multidisciplinary management.” - Transplant pharmacist