Read Mosby's 2014 Nursing Drug Reference Online
Authors: Linda Skidmore-Roth
Canada only Side effects:
italics
= common;
bold
= life-threatening
Nurse Alert
(re′goe-raf′e-nib)
Stivarga
Func. class.:
Antineoplastic biologic-response modifier; multikinase inhibitor
Chem. class.:
Signal transduction inhibitor (STI)
Inhibits tyrosine kinase in patients with colorectal cancer
Metastatic colorectal cancer in those who have received fluoropyrimidine, oxaliplatin, irinotecan-based chemotherapy, an anti-VEGF therapy; and an anti-EGFR therapy if
KRAS
wild type
Pregnancy (D)
Precautions:
Breastfeeding, children, geriatric patients, cardiac/renal/hepatic/dental disease, fistula, GI bleeding or perforation, bone marrow suppression, infection, wound dehiscence, thrombocytopenia, neutropenia, immunosuppression
Black Box Warning:
Hepatic disease
• Adult:
PO
160 mg/day with a low-fat breakfast × 21 days of a 28-day cycle, cycles may be repeated
Available forms:
Tabs 40 mg
•
Store at 77°F (25°C)
•
Give at the same time each day with a low-fat breakfast that contains less than 30% fat such as 2 slices of white toast with 1 TBSP of low-fat margarine and 1 TBSP of jelly, and 8 oz of skim milk; or 1 cup of cereal, 8 oz of skim milk, 1 slice of toast with jam, apple juice, and 1 cup of coffee or tea
•
Swallow tablets whole
•
If a dose is missed, take as soon as possible that day; do not take 2 doses on the same day
Reduce to 120 mg (grade 2 palmar–plantar erythrodysesthesia); hold if grade 2 toxicity does not improve in ≤7 days or recurs; hold for ≥7 days in grade 3 toxicity; reduce to 80 mg for recurrent grade 2 toxicity; discontinue if 80 mg is not tolerated
Hold in grade 2 hypertension
Hold until toxicity resolves in grade 3 or 4 toxicity; consider the risk/benefits of continuing therapy in grade 4 toxicity, reduce dosage to 120 mg; if grade 3 or 4 toxicity recurs, hold until toxicity resolves, then reduce to 80 mg; discontinue in those who do not tolerate 80-mg dose
Baseline mild (Child-Pugh class A) or moderate (Child-Pugh class B): no change; baseline severe hepatic impairment (Child-Pugh class C): use not recommended; AST/ALT elevations during therapy: For grade 3 AST/AST level elevations, hold dose; if therapy is continued, reduce to 120 mg after levels recover; discontinue in those with AST/ALT > 20× ULN; AST/ ALT > 3× ULN and bilirubin >2× ULN; recurrence of AST/ALT >5× ULN despite a reduction to 120 mg
CNS:
Headache, tremor
CV:
Hypertensive crisis, MI
EENT:
Blurred vision, conjunctivitis
GI:
Hepatotoxicity, GI hemorrhage,
diarrhea,
GI perforation, xerostomia
HEMA:
Neutropenia, thrombocytopenia, bleeding
INTEG:
Rash, alopecia
META:
Hypokalemia
MISC:
Fatigue, decreased weight, hand–foot syndrome, hypothyroidism
Protein binding 99%, metabolized by CYP3A4, UGT1A0, half-life 14-58 hr
Increase:
regorafenib concentrations—CYP3A4 inhibitors (ketoconazole, itraconazole, erythromycin, clarithromycin)
Increase:
plasma concentrations of simvastatin, calcium-channel blockers, ergots
Increase:
plasma concentration of warfarin; avoid use with warfarin; use low-molecular-weight anticoagulants instead
Decrease:
regorafenib concentrations—CYP3A4 inducers (dexamethasone, phenytoin, carBAMazepine, rifampin, PHENobarbital)
Increase:
regorafenib effect—grapefruit juice; avoid use while taking product
Decrease:
imatinib concentration—St. John’s wort
Black Box Warning:
Hepatic disease: fatal hepatotoxicity can occur; obtain LFTs baseline and at least every 2 wk × 2 mo, then monthly
From GI, respiratory, GU tracts; permanently discontinue in those with severe bleeding
More common in those previously treated; reddening swelling, numbness, desquamation on palms, soles
Discontinue if this occurs, assess for pain in epigastric area, dyspepsia, flatulence, fever, chills
Hypertension usually occurs in the first cycle in those with preexisting hypertension, do not start treatment until B/P is controlled; monitor B/P every wk × 6 wk, then at start of each cycle or more often if needed, temporarily or permanently discontinue for severe uncontrolled hypertension
•
Therapeutic response: decrease in spread or size of tumor
•
To report adverse reactions immediately: bleeding, rash
•
About reason for treatment, expected results
•
That effect on male fertility is unknown