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Indications

High Alert

Afinitor:

Zortress:

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

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.

Metab: hyperlipidemia, hypertriglyceridemia.

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), (ZORTRESS)LYMPHOMA/SKIN CANCER .

Interactions

Drug-Drug:

Drug-Natural Products:

Drug-Food:

Availability

(Generic available)

Route/Dosage

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

US Brand Names

Afinitor, Afinitor Disperz, Zortress

Action

Therapeutic Effects:

Classifications

Therapeutic Classification: antineoplastics, Immunosuppressant agents

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics

Absorption: Well absorbed following oral administration.

Distribution: 20% confined to plasma.

Metabolism/Excretion: Mostly metabolized by liver via the CYP3A4 isoenzyme; metabolites are mostly excreted in feces (80%) and urine (5%).

Half-life: 30 hr.

Time/Action Profile

(plasma concentrations)

ROUTEONSETPEAKDURATION
POunknown1–2 hr24 hr

Patient/Family Teaching

Pronunciation

e-ver-OH-li-mus