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Pharmacologic classification: kinase inhibitor
Therapeutic classification: antineoplastic
Pregnancy risk category: D
AVAILABLE FORMS
Tablets: 5 mg, 10 mg
INDICATIONS AND DOSAGES
Advanced renal cell carcinoma after treatment with sunitinib or sorafenib fails—
Adults: 10 mg P.O. daily.
CONTRAINDICATIONS AND CAUTIONS
Contraindicated in patients hypersensitive to the drug, its components, or other rapamycin derivatives.
Avoid use in patients with severe hepatic impairment or severe infections.
INTERACTIONS
Drug-drug.
CYP3A4 strong or moderate inhibitors, P-glycoprotein inhibitors (amprenavir, aprepitant, atazanavir, clarithromycin, delavirdine, diltiazem, erythromycin, fluconazole, fosamprenavir, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, verapamil, voriconazole: May increase everolimus level. Avoid using together.
CYP3A4 strong inducers (carbamazepine, dexamethasone, phenobarbital, phenytoin, rifabutin, rifampin): May decrease everolimus level. Avoid using together; if unable, increase dose of everolimus at 5 mg-increments up 20 mg daily.
Drug-herb.
St. John's wort: May alter drug level. Discourage use together.
Drug-food.
Grapefruit, grapefruit juice: May increase drug level. Discourage use together.
ADVERSE REACTIONS
CNS: asthenia, dizziness, dysgeusia, fever, headache, insomnia, paresthesia.
CV: chest pain, heart failure, hypertension, tachycardia.
EENT: conjunctivitis, eyelid edema, mucosal inflammation, nasopharyngitis, pharyngolaryngeal pain, rhinorrhea, sinusitis.
GI: abdominal pain, anorexia, diarrhea, dry mouth, dysphagia, hemorrhoids, nausea, stomatitis, vomiting.
GU: renal failure, UTI.
Hematologic: hemorrhage.
Metabolic: exacerbation of diabetes mellitus, weight loss.
Musculoskeletal: extremity pain, jaw pain.
Respiratory: bronchitis, cough, dyspnea, epistaxis, pleural effusion, pneumonia, pneumonitis.
Skin: acneiform dermatitis, dry skin, erythema, hand-foot syndrome, nail disorder, pruritus, onychoclasis, rash, skin lesion.
Other: chills, fatigue, peripheral edema.
Reactions may be common, uncommon, life-threatening,
or COMMON AND LIFE-THREATENING.
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everolimus