Therapeutic Classification: antineoplastics, Immunosuppressant agents
Pharmacologic Classification: kinase inhibitors
High Alert
Absorption: Well absorbed following oral administration.
Distribution: 20% confined to plasma.
Half-Life: 30 hr.
Contraindicated in:
Heart transplantation (Zortress) (↑ risk of mortality)
;Use Cautiously in:
CV: peripheral edema
Derm: delayed wound healing, dry skin, pruritus, rash
Endo: hyperglycemia
GI: anorexia, constipation, diarrhea, mouth ulcers, mucositis, nausea, stomatitis, vomiting, HEPATIC ARTERY THROMBOSIS
GU: ↓fertility, acute renal failure, amenorrhea, KIDNEY ARTERIAL/VENOUS THROMBOSIS (ZORTRESS), menstrual irregularities, proteinuria
Hemat: anemia, leukopenia, thrombocytopenia, HEMOLYTIC UREMIC SYNDROME, THROMBOTIC MICROANGIOPATHY, THROMBOTIC THROMBOCYTOPENIC PURPURA
MS: extremity pain
Neuro: fatigue, weakness, dysgeusia, headache
Resp: cough, dyspnea, pulmonary embolism, INTERSTITIAL LUNG DISEASE, PULMONARY HYPERTENSION
Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA), INFECTION (INCLUDING ACTIVATION OF LATENT VIRAL INFECTIONS SUCH AS BK VIRUS-ASSOCIATED NEPHROPATHY), LYMPHOMA/SKIN CANCER (ZORTRESS)
Drug-drug:
↑risk of nephrotoxicity with aminoglycosides, amphotericin B, cisplatin, or cyclosporine
.Drug-Natural Products:
Drug-Food:
Advanced Renal Cell Carcinoma, Advanced Progressive Neuroendocrine Tumors, Advanced Neuroendocrine Tumors, Advanced Hormone Receptor-Positive, HER2-Negative Breast Cancer, and Renal Angiomyolipoma With Tuberous Sclerosis Complex (Afinitor)
Hepatic Impairment
Subependymal Giant Cell Astrocytoma With Tuberous Sclerosis Complex (Afinitor)
Hepatic Impairment
Tuberous Sclerosis Complex-Associated Partial-Onset Seizures (Afinitor)
Hepatic Impairment
Kidney Transplantation (Zortress)
Hepatic Impairment
Liver Transplantation (Zortress)
Hepatic Impairment
Assess for signs and symptoms of systemic fungal infections (fever, malaise, weight loss, sweats, cough, dyspnea, pulmonary infiltrates, serious systemic illness with or without concurrent shock). Withhold therapy until infection has been diagnosed and adequately treated.
Lab Test Considerations:
Zortress (Kidney Transplantation)Both cyclosporine doses and the target range for whole blood trough concentrations should be ↓ when given in a regimen with Zortress in order to minimize the risk of nephrotoxicity. The recommended cyclosporine therapeutic ranges when administered with Zortress are 100200 ng/mL through Month 1 post-transplant, 75150 ng/mL at Months 2 and 3 post-transplant, 50100 ng/mL at Month 4 post-transplant, and 2550 ng/mL from Month 6 through Month 12 post-transplant. Cyclosporine, USP Modified is to be administered as oral capsules twice daily unless cyclosporine oral solution or IV administration of cyclosporine cannot be avoided. Cyclosporine, USP Modified should be initiated as soon as possible and no later than 48 hr after reperfusion of the graft and dose adjusted to target concentrations from Day 5 onward. If impairment of renal function is progressive, the treatment regimen should be adjusted. In renal transplant patients, the cyclosporine dose should be based on cyclosporine whole blood trough concentrations. Prior to dose ↓ of cyclosporine, steady-state everolimus whole blood trough concentration should be ≥3 ng/mL. Everolimus concentrations may ↓ if cyclosporine exposure is ↓.
Zortress: Antimicrobial prophylaxis for Pneumocystis jirovecipneumonia and prophylaxis for cytomegalovirus is recommended in transplant recipients.
NDC Code