Generic Name and Formulations:
Everolimus 0.25mg, 0.5mg, 0.75mg; tabs.
Novartis Pharmaceuticals Corp
Indications for ZORTRESS:
Organ rejection prophylaxis in renal transplant patients with low-moderate immunologic risk, in combination with basiliximab induction and reduced doses of cyclosporine and corticosteroids. Organ rejection prophylaxis in liver transplant patients, in combination with reduced doses of tacrolimus and corticosteroids.
Limitations Of use:
High immunologic risk in renal transplant patients or prophylaxis in other organs: not established.
Swallow whole. ≥18yrs: Renal transplant: administer as soon as possible after transplantation. Initially 0.75mg every 12 hours (1.5mg/day) in combination with reduced dose cyclosporine. Initiate oral prednisone as soon as oral medication is tolerated. Liver transplant: administer no earlier than 30 days post transplant. Initially 1mg every 12 hours (2mg/day) in combination with reduced dose tacrolimus. Both: steroid doses may be further tapered on an individualized basis. May adjust dose at 4–5 day intervals to achieve everolimus trough concentration target range 3–8ng/mL. Hepatic impairment: Mild: reduce initial daily dose by ⅓; Moderate or severe: reduce initial daily dose by ½.
<18yrs: not established.
Malignancies. Serious infections. Kidney graft thrombosis. Nephrotoxicity. Mortality in heart transplantation.
Increased risk of infections and possible malignancies (eg, lymphoma, skin); kidney graft thrombosis; nephrotoxicity; and mortality in heart transplantation. Use in heart transplantation: not recommended. Avoid sun, UV light. Severe hepatic impairment or hereditary disorders (eg, galactose intolerance, Lapp lactase deficiency, glucose-galactose malabsorption): not recommended. Diabetes. Obtain everolimus, cyclosporine and tacrolimus whole blood concentrations periodically (see full labeling); and trough concentrations during dose adjustments. Monitor CBCs, renal function, urine protein, lipids, blood glucose; and for pneumonitis and serious (eg, bacterial, viral, fungal, protozoal) including opportunistic infections; polyoma virus infections (eg, BK virus-associated nephropathy, and JC virus-associated progressive multiple leukoencephalopathy). Antimicrobial prophylaxis for PCP and CMV recommended. Embryo-fetal toxicity. Pregnancy; avoid. Females of reproductive potential should use highly effective contraception during and up to 8 weeks after final dose. Nursing mothers: not recommended.
Avoid live vaccines, standard doses of cyclosporine. Increased risk of angioedema with ACE-inhibitors. Potentiated by CYP3A4 and/or P-glycoprotein inhibitors; avoid strong inhibitors (eg, ketoconazole, itraconazole, voriconazole, clarithromycin, telithromycin, ritonavir, boceprevir, telaprevir, grapefruit juice, digoxin); monitor and adjust dose with moderate inhibitors (eg, erythromycin, fluconazole, nicardipine, diltiazem, nelfinavir, indinavir, amprenavir), or CYP3A4 and P-glycoprotein substrate (eg, verapamil). Potentiates octreotide. Antagonized by CYP3A4 inducers (eg, carbamazepine, phenobarbital, phenytoin, efavirenz, nevirapine, St. John's Wort); avoid strong inducers (eg, rifampin, rifabutin). Avoid simvastatin, lovastatin; monitor if used with atorvastatin or pravastatin. Caution with other nephrotoxic drugs, CYP3A4 or CYP2D6 substrates with a narrow therapeutic index.
Peripheral edema, nausea, diarrhea, constipation, hypertension, headache, pyrexia, abdominal pain, leukopenia, anemia, infections (eg, UTI), hyperlipidemia, angioedema, malignancies (eg, lymphomas, skin), proteinuria, nephrotoxicity, kidney graft thrombosis, hepatic artery thrombosis, delayed wound healing/dehiscence, polyoma virus infections, interstitial lung disease/non-infectious pneumonitis (reduce or interrupt dose and/or manage with corticosteroids), thrombotic microangiopathy, thrombotic thrombocytopenic purpura, hemolytic uremic syndrome, new-onset diabetes post-transplant, male infertility.
Hepatic; 74% protein bound.
Fecal (primarily), renal.
Tabs—60 (10 x 6 blister strips)
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