Prograf: Advanced Immunosuppression for Transplant Success

Prograf

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Product dosage: 0.5mg
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Product dosage: 1mg
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Synonyms Protopic

Prograf (tacrolimus) is a cornerstone immunosuppressive agent indicated for the prophylaxis of organ rejection in patients receiving allogeneic liver, kidney, or heart transplants. It is a calcineurin inhibitor that acts by selectively inhibiting T-lymphocyte activation, a critical pathway in the immune response against foreign tissue. This medication is integral to modern transplant protocols, offering a potent mechanism to help ensure graft survival and long-term patient outcomes. Its use requires meticulous therapeutic drug monitoring and management by a specialized transplant team to balance efficacy with the risk of adverse effects.

Features

• Active Pharmaceutical Ingredient: Tacrolimus.
• Mechanism of Action: Calcineurin inhibitor; suppresses T-cell activation and proliferation.
• Available Formulations: Immediate-release capsules (0.5 mg, 1 mg, 5 mg), prolonged-release capsules, and injection for intravenous infusion.
• Bioavailability: Exhibits variable oral bioavailability (approximately 17-22% for immediate-release), significantly influenced by food and other factors.
• Metabolism: Primarily hepatically metabolized via the CYP3A4 enzyme system.
• Half-life: Mean elimination half-life is approximately 12 hours in healthy subjects, with considerable inter-patient variability.
• Therapeutic Monitoring: Requires frequent monitoring of trough blood concentrations (Cmin) to individualize dosing and maintain therapeutic window.

Benefits

• Potent Rejection Prophylaxis: Provides highly effective suppression of the cellular immune response, significantly reducing the incidence of acute organ rejection episodes.
• Improved Long-Term Graft Survival: Contributes to enhanced one-year and five-year graft survival rates when used as part of a multi-drug immunosuppressive regimen.
• Corticosteroid-Sparing Potential: May allow for reduced corticosteroid dosing or earlier corticosteroid withdrawal, mitigating the long-term adverse effects associated with chronic steroid use.
• Flexible Dosing Protocols: Availability of immediate and prolonged-release formulations allows for tailored dosing schedules to improve adherence and therapeutic management.
• Established Clinical Profile: Backed by decades of extensive clinical research and real-world experience in solid organ transplantation.

Common use

Prograf is primarily used for the prophylaxis of organ rejection in patients receiving allogeneic transplants. Its most common applications include:

• Primary immunosuppression following liver transplantation.
• Primary immunosuppression following kidney transplantation.
• Primary immunosuppression following heart transplantation. It is typically initiated post-operatively and used concomitantly with other immunosuppressive agents, such as corticosteroids and sometimes an antiproliferative agent (e.g., mycophenolate mofetil), as part of a multi-drug regimen. In some cases, it may also be used in rescue therapy for the treatment of acute rejection episodes that are refractory to other treatment.

Dosage and direction

Administration must be under the direct supervision of a physician experienced in immunosuppressive therapy and management of transplant patients.

• Oral Administration (Capsules): Usually administered twice daily (approximately every 12 hours). Dosing is highly individualized based on patient status, organ transplanted, and target trough blood concentrations.
• Initial Dosing: For adult liver transplant patients, initial oral doses are often in the range of 0.10 - 0.15 mg/kg/day in two divided doses. Dosing for kidney and heart transplant patients may differ.
• Intravenous Administration: Reserved for patients unable to take oral medication. The intravenous dose is typically one-fifth of the recommended oral dose and administered as a continuous 24-hour infusion.
• Consistent Timing: Must be taken consistently in relation to food. Administration on an empty stomach or consistently with food is required to minimize variability in absorption; taking it with food decreases bioavailability.
• Therapeutic Drug Monitoring (TDM): Dosage adjustments are guided by frequent monitoring of tacrolimus trough whole-blood concentrations. The target therapeutic range is specific to the transplanted organ, time post-transplant, institutional protocol, and concomitant therapy.
• Prolonged-Release Formulation: If prescribed, is taken once daily in the morning.

Precautions

• Nephrotoxicity: Prograf can cause dose-dependent and concentration-dependent renal impairment. Renal function (serum creatinine, BUN, estimated GFR) must be monitored closely.
• Neurotoxicity: Potentially severe neurotoxic events, including tremor, headache, altered mental status, seizures, and posterior reversible encephalopathy syndrome (PRES), have been reported. Risk is increased with higher trough concentrations.
• Infections: Due to immunosuppression, patients are at increased risk for developing bacterial, viral, fungal, and protozoal infections, including opportunistic infections and reactivation of latent infections (e.g., BK virus, CMV, EBV).
• Malignancies: Immunosuppressed patients are at an increased risk for developing malignancies, particularly skin cancers and lymphoma. Regular skin examinations are recommended.
• Hyperglycemia / New-Onset Diabetes: May cause insulin-dependent, non-insulin-dependent, and insulin-requiring post-transplant diabetes mellitus. Blood glucose should be monitored regularly.
• Hyperkalemia: Can frequently cause elevated serum potassium levels, which may require treatment. Concomitant use of other drugs that cause hyperkalemia (e.g., potassium-sparing diuretics, ACE inhibitors) increases risk.
• Hypertension: Commonly causes or exacerbates hypertension, requiring antihypertensive therapy.
• Pregnancy: Tacrolimus crosses the placenta. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Pregnancy should be reported immediately.

Contraindications

Prograf is contraindicated in patients with:

• A known hypersensitivity to tacrolimus or any component of the formulation.
• A known hypersensitivity to other macrolides (due to structural similarities).
• Concomitant use with cyclosporine. Prograf should not be administered simultaneously with cyclosporine; cyclosporine should be discontinued at least 24 hours before initiating Prograf.

Possible side effect

A very common (>1/10) and common (≥1/100 to <1/10) side effects include:

• Infections and Infestations: Bacterial, viral, fungal, and opportunistic infections.
• Metabolism and Nutrition: New-onset diabetes mellitus, hyperkalemia, hypomagnesemia, hyperuricemia, hyperlipidemia, acidosis.
• Nervous System: Tremor, headache, insomnia, paresthesia, dizziness, seizures, encephalopathy.
• Gastrointestinal: Diarrhea, nausea, vomiting, abdominal pain, constipation.
• Renal and Urinary: Renal impairment, increased blood creatinine.
• Cardiac: Hypertension.
• Psychiatric: Anxiety, confusion.
• Vascular: Hemorrhage, thrombosis.
• Skin and Subcutaneous Tissue: Pruritus, rash, alopecia. Less common but serious side effects include severe neurotoxicity (e.g., PRES), severe nephrotoxicity, cardiomyopathy, and pure red cell aplasia.

Drug interaction

Prograf is a substrate of CYP3A4 and P-glycoprotein. Concomitant use with drugs that affect these pathways can significantly alter its blood concentrations.

• Strong Inhibitors of CYP3A4 (Increase Tacrolimus Levels):
  • Macrolide antibiotics: Clarithromycin, erythromycin.
  • Antifungals: Ketoconazole, itraconazole, voriconazole, fluconazole, posaconazole.
  • Protease Inhibitors: Ritonavir, nelfinavir.
  • Others: Nefazodone, telaprevir, cobicistat, diltiazem, verapamil, nicardipine, grapefruit juice.
• Strong Inducers of CYP3A4 (Decrease Tacrolimus Levels):
  • Anticonvulsants: Phenytoin, phenobarbital, carbamazepine.
  • Antimycobacterials: Rifampin, rifabutin.
  • Herbal Preparations: St. John’s Wort (Hypericum perforatum).
• Nephrotoxic Drugs (Additive Toxicity): Concomitant use with other nephrotoxic agents (e.g., aminoglycosides, amphotericin B, cisplatin, NSAIDs, ganciclovir) may increase the risk of renal dysfunction.
• Potassium-Sparing Agents: Concomitant use with potassium-sparing diuretics, ACE inhibitors, ARBs, or potassium supplements can increase the risk of severe hyperkalemia.

Missed dose

• If a dose is missed, it should be taken as soon as it is remembered on the same day.
• If it is close to the time for the next scheduled dose, the missed dose should be skipped. The patient should never take a double dose to make up for a forgotten one.
• The patient should inform their transplant coordinator or physician about the missed dose, as it may be necessary to check a trough level.
• Maintaining a strict, consistent dosing schedule is critical for stable drug levels and efficacy.

Overdose

• Signs and Symptoms: Overdose is expected to produce exaggerated adverse effects, particularly severe nephrotoxicity, neurotoxicity (tremor, headache, altered mental status, seizures), hyperkalemia, and gastrointestinal symptoms.
• Management: There is no specific antidote. Management consists of immediate general supportive measures and symptomatic treatment.
• Decontamination: Gastric lavage may be considered soon after ingestion. Activated charcoal may be effective if given promptly.
• Monitoring: Frequent monitoring of tacrolimus blood levels, electrolytes, renal function, and neurological status is essential.
• Treatment: Since tacrolimus is highly protein-bound and has a large volume of distribution, dialysis is not effective in enhancing elimination.

Storage

• Store at room temperature between 20°C to 25°C (68°F to 77°F). Excursions are permitted between 15°C and 30°C (59°F and 86°F).
• Keep the capsules in their original blister packaging or bottle to protect from light and moisture.
• Keep out of reach of children and pets.
• Do not use after the expiration date printed on the packaging.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician, transplant team, or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has been compiled from various reputable sources but may not be comprehensive or reflect the most recent medical developments. Dosing and administration must be determined solely by a qualified healthcare professional.

Reviews

• Clinical Consensus: Prograf is widely regarded by the global transplant community as a gold-standard immunosuppressant. Its potent efficacy in preventing acute rejection is well-documented in countless clinical trials and decades of post-marketing surveillance.
• Transplant Team Perspective: Specialists value its potency and the ability to monitor levels precisely, but emphasize the demanding requirement for vigilant therapeutic drug monitoring and management of its significant side-effect profile. It is a powerful tool that requires expert handling.
• Patient Feedback: Patient experiences are highly variable and deeply personal. Many express immense gratitude for the role Prograf has played in saving their lives and preserving their graft function. Commonly cited challenges include managing the strict dosing schedule, coping with side effects like tremors and headaches, and the constant vigilance required for blood tests and potential interactions. The trade-off between side effects and graft survival is a constant theme in patient discussions.
• Overall: Prograf receives high marks for its proven efficacy and critical role in transplant medicine. Its reviews are tempered by the acknowledgment of its narrow therapeutic index and complex management requirements, underscoring that its success is dependent on a dedicated partnership between the patient and a highly specialized medical team.