Prograf Injection

— THERAPEUTIC CATEGORIES —
  • Organ rejection prophylaxis
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Prograf Injection Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Tacrolimus 5mg/mL; soln for IV infusion after dilution; contains polyoxyl 60 hydrogenated castor oil.

    Pharmacological Class

    Immunosuppressant (calcineurin-inhibitor).

    See Also

    How Supplied

    Caps—100; Granules—50; Ampules—10

    Manufacturer

    Astellas Pharma US, Inc.

    Generic Availability

    YES

    Mechanism of Action

    Tacrolimus inhibits T-lymphocyte activation and proliferation. Experimental evidence suggests that tacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin inhibited.

    Prograf Injection Indications

    Indications

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

    Prograf Injection Dosage and Administration

    Adult

    Give at least 6hrs after transplantation if unable to tolerate oral caps. Heart: initially 0.01mg/kg/day. Liver or kidney: initially 0.03–0.05mg/kg/day. Lung: initially 0.01–0.03mg/kg/day. All: give by continuous IV infusion until oral caps 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. Post-op oliguria: give initial dose no sooner than 6hrs and within 48hrs of transplantation, but may be delayed until renal function recovers. See full labeling.

    Children

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

    Administration

    Give at least 6hrs after transplantation if unable to tolerate oral capsules. Administer as a continuous IV infusion. Conversion from IV to oral Prograf is recommended as soon as oral therapy can be tolerated. Avoid grapefruit or grapefruit juice in combination with Prograf. Do not use simultaneously with cyclosporine; discontinue Prograf or cyclosporine at least 24 hours before initiating the other. Do not mix or co-infuse with solutions with pH ≥9 (eg, ganciclovir, acyclovir).

    Nursing Considerations

    Give at least 6hrs after transplantation if unable to tolerate oral capsules. Administer as a continuous IV infusion. Conversion from IV to oral Prograf is recommended as soon as oral therapy can be tolerated. Avoid grapefruit or grapefruit juice in combination with Prograf. Do not use simultaneously with cyclosporine; discontinue Prograf or cyclosporine at least 24 hours before initiating the other.

    Prograf Injection Contraindications

    Not Applicable

    Prograf Injection Boxed Warnings

    Boxed Warning

    Malignancies. Serious infections.

    Prograf Injection Warnings/Precautions

    Warnings/Precautions

    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. Monitor Epstein-Barr virus serology, development of infections during therapy. 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 (esp. Hispanic and black patients); monitor blood glucose. Hepatic or renal impairment; monitor and consider dose reduction. Obtain tacrolimus whole blood concentrations, serum creatinine, serum 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. Risk for thrombotic microangiopathy (including hemolytic uremic syndrome and thrombotic thrombocytopenic purpura) esp. in those with severe infections, GVHD, HLA mismatch. Complete required immunizations prior to transplantation and treatment. IV: have epinephrine readily available. Elderly. Labor & delivery. Advise females and males of reproductive potential to use appropriate contraception prior to initiation. Pregnancy. Nursing mothers.

    Prograf Injection Pharmacokinetics

    Distribution

    Plasma protein bound: 99%.

    Metabolism

    Hepatic (CYP3A4). 

    Elimination

    Oral administration: fecal (92.6 ± 30.7%), renal (2.3 ± 1.1%). Half-life: 31.9 ± 10.5 hours (based on radioactivity); 48.4 ± 12.3 hours (based on tacrolimus concentrations).

    Prograf Injection Interactions

    Interactions

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

    Prograf Injection Adverse Reactions

    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, 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: anaphylaxis (monitor and discontinue if occurs).

    Prograf Injection Clinical Trials

    See Literature

    Prograf Injection Note

    Not Applicable

    Prograf Injection Patient Counseling

    See Literature

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