Organ rejection prophylaxis:

Indications for: ENVARSUS XR

Organ rejection prophylaxis in de novo kidney transplant patients or in stable kidney transplant patients converted from tacrolimus immediate-release formulations, in combination with other immunosuppressants.

Adult Dosage:

Swallow whole. Take once daily in the morning, preferably on an empty stomach. De novo: initially 0.14mg/kg/day. Titrate dose based on tolerability and to achieve target whole blood trough concentration ranges. During Month 1: 6–11ng/mL; >Month 1: 4–11ng/mL. Converting from tacrolimus immediate-release: give 80% of total daily dose of the immediate-release product; monitor and titrate dose to achieve ranges 4–11ng/mL. Hepatic impairment: severe (Child-Pugh ≥10): use lower initial dose; moderate: monitor. Black patients may require higher doses. See full labeling.

Children Dosage:

Not established.

Boxed Warning:

Malignancies. Serious infections.

ENVARSUS XR Warnings/Precautions:

Not interchangeable or substitutable with other tacrolimus products. Increased risk of lymphomas and other malignancies (eg, skin). Avoid sun, UV light. Epstein Barr Virus seronegative; monitor. Increased risk of infections (eg, bacterial, viral, fungal, protozoal), opportunistic infections including polyoma virus, JC virus-associated progressive multifocal leukoencephalopathy, cytomegalovirus; monitor. New-onset diabetes: monitor blood glucose levels esp. in Black and Hispanic patients. Monitor for neurotoxicity; consider dose reduction or discontinuation if occurs. Renal impairment; monitor and consider dose reduction. Obtain tacrolimus whole blood concentrations (see full labeling), serum creatinine, and serum potassium periodically. Avoid in congenital long QT syndrome. CHF, bradyarrhythmias, concomitant antiarrhythmic drugs, or electrolyte disturbances: consider obtaining ECGs and monitor electrolytes periodically. Elderly. Labor & delivery. Advise females of reproductive potential and male patients to use appropriate contraception prior to initiation. Pregnancy: monitor. Nursing mothers.

ENVARSUS XR Classification:

Immunosuppressant (calcineurin-inhibitor).

ENVARSUS XR Interactions:

Concomitant live vaccines: not recommended. Avoid grapefruit/grapefruit juice, alcohol. Concomitant mycophenolic acid (MPA) products; monitor and reduce MPA dose as needed. Concomitant strong CYP3A inhibitors (eg, protease inhibitors, azole antifungals, clarithromycin, troleandomycin, chloramphenicol, nefazodone, cobicistat) or inducers (eg, antimycobacterials, anticonvulsants, St. John's wort): adjust dosing regimen, closely monitor tacrolimus blood concentrations and for QT prolongation. Concomitant voriconazole, posaconazole: give ⅓ of original dose. Concomitant mild or moderate CYP3A inhibitors (eg, erythromycin, calcium channel blockers, amiodarone, danazol, ethinyl estradiol, cimetidine, lansoprazole, omeprazole, azole antifungals, imatinib, nilotinib, letermovir) or inducers (eg, methylprednisolone, prednisone), magnesium and aluminum hydroxide antacids, metoclopramide: monitor and adjust dose as needed. Concomitant potassium-sparing diuretics, ACEIs, ARBs may increase risk of hyperkalemia; monitor. Additive nephrotoxicity with CYP3A inhibitors, aminoglycosides, ganciclovir, amphotericin B, cisplatin, nucleotide reverse transcriptase inhibitors, protease inhibitors. Concomitant with direct acting antivirals; monitor closely.

Adverse Reactions:

Diarrhea, anemia, UTI, hypertension, tremor, constipation, diabetes mellitus, peripheral edema, hyperkalemia, headache, increased creatinine; infections, malignancies (lymphomas, skin), post-transplant lymphoproliferative disorder, nephrotoxicity or neurotoxicity (esp. in high doses), posterior reversible encephalopathy syndrome, QT prolongation, pure red cell aplasia (consider discontinuation).

Generic Drug Availability:


How Supplied:

Ext-rel tabs—30, 100