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Organ rejection prophylaxis
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Drug Name:


Generic Name and Formulations:
Tacrolimus 5mg/mL; soln for IV infusion after dilution; contains polyoxyl 60 hydrogenated castor oil.

Astellas Pharma US, Inc.

Therapeutic Use:

Indications for PROGRAF INJECTION:

Organ rejection prophylaxis in patients with allogeneic kidney, liver, and heart transplants, in combination with other immunosuppressants.


Give at least 6hrs after transplantation if unable to tolerate oral capsules. Heart: initially 0.01mg/kg/day. Liver or kidney: initially 0.03–0.05mg/kg/day. All: give by continuous IV infusion until capsules can be tolerated. Monitor at least the first 30mins of infusion and at frequent intervals thereafter. Concomitant corticosteroid is recommended early post-transplantation. Renal or hepatic impairment: use lowest effective dose (see full labeling). Post-op oliguria: may delay therapy until renal function recovers.


Give at least 6hrs after transplantation if unable to tolerate oral capsules. Liver: initially 0.03–0.05mg/kg/day by continuous IV infusion until capsules can be tolerated. Monitor at least the first 30mins of infusion and at frequent intervals thereafter.

Boxed Warning:

Malignancies. Serious infections.


Increased risk of lymphomas and other malignancies (eg, skin) due to immunosuppression. Avoid sun, UV light. Increased risk of infections (eg, bacterial, viral, fungal, protozoal), including opportunistic infections. Oral forms are not interchangeable with other tacrolimus ext-rel products. Only physicians experienced in immunosuppressive therapy should prescribe Prograf. Risk of new onset diabetes after transplant. Hepatic or renal impairment; monitor and consider dose reduction. Obtain tacrolimus whole blood concentrations, serum creatinine, potassium, and fasting glucose periodically. Monitor and control BP. Avoid in congenital long QT syndrome. CHF, bradyarrhythmias, concomitant antiarrhythmic drugs, or electrolyte disturbances; consider obtaining ECGs and monitor electrolytes periodically. Discontinue or reduce dose if myocardial hypertrophy occurs. Pregnancy, labor & delivery, nursing mothers: see full labeling.

See Also:


Pharmacological Class:

Immunosuppressant (calcineurin-inhibitor).


Concomitant sirolimus (in liver/heart transplant), live vaccines: not recommended. Concomitant strong CYP3A4 inhibitors/inducers or substrates: must adjust dosing regimen, closely monitor tacrolimus blood concentrations and for QT prolongation. Avoid grapefruit or grapefruit juice. Caution with potassium-sparing diuretics, ACEIs, ARBs during therapy. Additive nephrotoxicity with cyclosporine (discontinue at least 24hrs prior to initiating the other drug), aminoglycosides, ganciclovir, amphotericin B, cisplatin, NRTIs, protease inhibitors. May be potentiated by calcium channel blockers (eg, diltiazem, nifedipine), antifungals (eg, fluconazole, ketoconazole, voriconazole, posaconazole, itraconazole), macrolides (eg, troleandomycin, clarithromycin, erythromycin), metoclopramide, lansoprazole, omeprazole, chloramphenicol, cimetidine, cyclosporine, danazol, ethinyl estradiol, amiodarone, schisandra sphenanthera extract, protease inhibitors (eg, nelfinavir, telaprevir, boceprevir, ritonavir), nefazodone, magnesium-aluminum-hydroxide. May be antagonized by carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, St. Johns Wort, methylprednisolone, prednisone. Caution with mycophenolic acid; reduce dose of these as needed.

Adverse Reactions:

Tremor, headache, constipation, diarrhea, nausea, abdominal pain, insomnia, hypertension, renal dysfunction, fever, serious viral infections (eg, CMV, PML, PVAN), leukopenia, anemia, bronchitis, pericardial effusion, UTI, paresthesia, peripheral edema, hypophosphatemia, hyperkalemia, hypomagnesemia, hyperlipidemia, hyperglycemia; nephrotoxicity or neurotoxicity (esp. in high doses), diabetes mellitus, posterior reversible encephalopathy syndrome (consider reduced dose or discontinue), malignancies (eg, lymphomas, skin), post-transplant lymphoproliferative disorder, myocardial hypertrophy, pure red cell aplasia, Torsade de Pointes; IV: anaphylactic reactions (monitor).


Hepatic (CYP3A4); 99% protein bound.


Fecal (primary), renal.

Generic Availability:


How Supplied:

Caps—100; Ampules—10

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