CV: MYOCARDIAL INFARCTION/ISCHEMIA (PANCREATIC CANCER PATIENTS).
Derm: rash, BULLOUS AND EXFOLIATIVE SKIN DISORDERS, dry skin, pruritus.
EENT: ↓ tear production, abnormal eyelash growth, conjunctivitis, corneal perforation, corneal ulceration, keratitis.
GI: diarrhea, hepatotoxicity, ↑ liver enzymes, abdominal pain, anorexia, GI PERFORATION, nausea, stomatitis, vomiting.
GU: RENAL FAILURE.
Hemat: microangiopathic hemolytic anemia with thrombocytopenia (pancreatic cancer patients).
Neuro: CEREBROVASCULAR ACCIDENT (PANCREATIC CANCER PATIENTS), fatigue.
Resp: dyspnea, cough, INTERSTITIAL LUNG DISEASE.
Non–Small-Cell Lung Cancer
- PO (Adults): 150 mg once daily; Concurrent use of strong CYP3A4 inhibitor or concurrent use of CYP3A4 and CYP1A2 inhibitor (e.g., ciprofloxacin): Consider ↓ dose in 50-mg increments (avoid concomitant use, if possible); Concurrent use of strong CYP3A4 inducer: consider ↑ dose by 50 mg every 2 wk (max dose = 450 mg/day) (avoid concomitant use, if possible); Concurrent cigarette smoking or concurrent use of moderate CYP1A2 inducer: ↑ dose by 50 mg every 2 wk (max dose = 300 mg/day); immediately ↓ dose to recommended initial dose for indication upon smoking cessation.
Pancreatic Cancer
- PO (Adults): 100 mg once daily. Concurrent use of strong CYP3A4 inhibitor or concurrent use of CYP3A4 and CYP1A2 inhibitor (e.g., ciprofloxacin): Consider ↓ dose in 50-mg increments (avoid concomitant use, if possible); Concurrent use of strong CYP3A4 inducer: consider ↑ dose by 50 mg every 2 wk (max dose = 450 mg/day) (avoid concomitant use, if possible); Concurrent cigarette smoking or concurrent use of moderate CYP1A2 inducer: ↑ dose by 50 mg every 2 wk (max dose = 300 mg/day); immediately ↓ dose to recommended initial dose for indication upon smoking cessation.
Therapeutic Classification: antineoplastics
Pharmacologic Classification: enzyme inhibitors
Absorption: 60% absorbed; bioavailability ↑ to 100% with food.
Distribution: Unknown.
Protein Binding: 93% protein bound.
Metabolism/Excretion: Mostly metabolized by the liver, primarily by the CYP3A4 isoenzyme. 83% excreted in feces (<1% as unchanged drug) and 8% excreted in urine (<1% as unchanged drug).
Half-life: 36 hr.