Prograf (Tacrolimus) – Comprehensive Product Description
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What is Prograf used for?
Prograf (Tacrolimus) is an immunosuppressive medication used to prevent organ rejection in patients undergoing liver, kidney, or heart transplantation. It works by suppressing the immune system to prevent it from attacking the newly transplanted organ.

Product Name:
Prograf

Generic Name:
Tacrolimus

Other Popular and Common Names:
FK-506

Tacrolimus Capsules

Tacrolimus Extended-Release (Envarsus XR, Astagraf XL – brand alternatives)

Immunosuppressive Tacrolimus

Drug Classification:
Therapeutic Class: Immunosuppressants

Pharmacologic Class: Calcineurin Inhibitors

Form: Oral Capsules (available in 0.5 mg, 1 mg, 5 mg), IV injection

Prescription Status: Prescription-only

Active Ingredient:
Tacrolimus (USP)

Mode of Action:
Tacrolimus acts by inhibiting calcineurin, an enzyme crucial for the activation of T-cells in the immune system. By blocking T-lymphocyte activation, tacrolimus significantly reduces immune response and prevents organ transplant rejection. The drug selectively suppresses interleukin-2 (IL-2) transcription, a key cytokine involved in T-cell proliferation.

Indications and Approved Uses:
Prograf is indicated for the prophylaxis of organ rejection in patients receiving:

Liver transplants

Kidney transplants

Heart transplants

It is also sometimes used off-label in:

Severe atopic dermatitis (topical forms)

Certain autoimmune disorders

Dosage and Administration:
Initial Adult Dosing (Liver Transplant, Oral):
0.10–0.15 mg/kg/day, administered in two divided doses (every 12 hours)

Initiate dosing within 12–24 hours post-transplantation

Titrate based on blood trough levels (target 5–15 ng/mL depending on organ type and time since transplant)

IV Form (when oral is not feasible):
Administer as continuous infusion at 0.01–0.05 mg/kg/day

Switch to oral as soon as possible

Dosage Adjustments:
Modify based on trough levels, renal function, hepatic function, and clinical signs of rejection or toxicity

Always monitor whole blood tacrolimus levels during treatment. Do not interchange extended-release and immediate-release forms without medical supervision.

Prescribing Guidelines:
Therapeutic Drug Monitoring (TDM) is essential

Use the lowest effective dose

Not interchangeable with other tacrolimus products (e.g., Astagraf XL, Envarsus XR) without clinical guidance

Not approved for pediatric transplant use unless supervised by a transplant specialist

Safety Information:
Contraindications:
Known hypersensitivity to tacrolimus or any of its excipients

Coadministration with cyclosporine is contraindicated

Monitoring Requirements:
Blood levels of tacrolimus

Serum creatinine (renal function)

Liver enzymes

Blood pressure

Electrolytes, especially potassium and magnesium

Glucose levels (risk of post-transplant diabetes)

Side Effects:
Common:
Hypertension

Hyperglycemia and new-onset diabetes after transplantation (NODAT)

Nephrotoxicity

Tremor, headache

Gastrointestinal disturbances (nausea, diarrhea)

Serious:
Increased risk of infections and lymphoproliferative disorders (PTLD)

Nephrotoxicity leading to renal impairment

Neurotoxicity (seizures, confusion, encephalopathy)

QT prolongation

Rare hypersensitivity reactions

Warnings and Precautions:
Increased susceptibility to infections and malignancies

Monitor renal and hepatic function regularly

May cause electrolyte disturbances (hyperkalemia, hypomagnesemia)

Risk of neurotoxicity especially at high blood concentrations

Avoid grapefruit or grapefruit juice (inhibits CYP3A4 and increases drug levels)

Use caution in patients with pre-existing cardiac arrhythmias

Drug Interactions:
Tacrolimus is metabolized by CYP3A4 and CYP3A5 enzymes. Significant interactions include:

CYP3A4 Inhibitors (↑ Tacrolimus levels):
Ketoconazole, Fluconazole, Itraconazole

Clarithromycin, Erythromycin

Protease inhibitors (ritonavir, saquinavir)

Calcium channel blockers (diltiazem, verapamil)

Grapefruit juice

CYP3A4 Inducers (↓ Tacrolimus levels):
Rifampin, Rifabutin

Phenytoin, Carbamazepine

St. John’s Wort

Other Notable Interactions:
NSAIDs: Increased nephrotoxicity risk

Sirolimus: Increased risk of thrombocytopenia and nephrotoxicity

Live vaccines: Avoid during treatment due to immunosuppression

Frequently Asked Questions – Prograf (Tacrolimus)
Q1: How long do I need to take Prograf after my transplant?
A1: Prograf is typically taken lifelong to prevent rejection unless your doctor adjusts or stops therapy based on your progress.

Q2: Can I switch between generic tacrolimus and brand-name Prograf?
A2: Only under close medical supervision. Even minor changes in formulation can affect blood levels and graft survival.

Q3: Is it safe to take Prograf with my other medications?
A3: Many medications interact with Prograf. Always consult your transplant physician before starting or stopping any drugs.

Q4: What should I avoid while taking tacrolimus?
A4: Avoid grapefruit, herbal supplements (especially St. John’s Wort), live vaccines, and over-the-counter NSAIDs.

Q5: How is tacrolimus monitored in the body?
A5: Through trough blood level testing, usually measured before the morning dose.