axitinib
Brand: Inlyta
(none listed)
Pharmacological Action
Inhibits receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)- 1, VEGFR- 2, and VEGFR- 3; inhibits tumor growth and phosphorylation of VEGFR- 2 and VEGF- mediated endothelial cell proliferation
Therapeutic outcome: Decreased spread of malignancy
Uses
Treatment of advanced renal cell cancer after failure of one prior systemic therapy
Contraindications
Pregnancy (D), breastfeeding
Precautions: Risk for or history of thromboembolic disease, recent bleeding, untreated brain metastasis, recent GI bleeding, GI perforation, fistula, surgery, moderate hepatic disease, uncontrolled hypertension, hyper/hypothyroidism, proteinuria, infertility, end- stage renal disease (CrCl < 15 ml/min ); not intended for use in adolescents, children, infants, neonates
Dosage & Routes
Adult: PO 5 mg bid (at 12 hr intervals), may increase to 7 mg bid and then to 10 mg bid in those not receiving antihypertensives who tolerate the lower dosage for at least 2 consecutive wk with no more than grade 2 adverse reactions. Reduce to 3 mg bid if a dose reduction is needed; if further reduction is necessary, reduce to 2 mg bid Adult receiving a strong CYP 3 A4/5 inhibitor: Reduce dose by 1/2, adjust as needed
Available forms: Tab 1, 5 mg
Implementation Give with or without food; swallow tablet whole with a glass of water If patient vomits or misses a dose, an additional dose should not be taken; the next dose should be taken at the usual time Store at room temperature
Adverse Effects
CNS: Dizziness, headache, reversible posterior leukoencephalopathy syndrome (RPLS), fatigue
CV: Hypertension, arterial thromboembolic events (ATE), venous thromboembolic events (VTE)
ENDO: Hypothyroidism, hyperthyroidism
GI: Lower GI bleeding/perforation/fistula. abdominal pain, constipation, diarrhea, dysgeusia, dyspepsia, dysphonia, hemorrhoids, nausea, mucosal inflammation, stomatitis, vomiting, increased ALT/AST
GU: Proteinuria
HEMA: Bleeding intracranial bleeding, anemia, polycythemia, decreased/increased hemoglobin, lymphopenia thrombocytopenia, neutropenia
INTEG: Palmar-plantar erythrodysesthesia (hand and foot syndrome) rash, dry skin, pruritus, alopecia, erythema
MISC: Weight loss dehydration metabolic and electrolyte laboratory abnormalities included
MS: Asthenia, arthralgia, musculoskeletal pain, myalgia
RESP: Cough, dyspnea
Pharmacokinetics
Absorption: Unknown
Distribution: Protein binding > 99%
Metabolism: Liver
Excretion: Unknown
Half-life: 2.5-6.1 hr
Pharmacodynamics
Onset: Unknown
Peak: Unknown
Duration: Unknown
Interactions
Individual drugs CYP3 A4/5 inhibitor, strong, moderate (ketoconazole, boceprevir, chloramphenicol, conivaptan, delavirdine, fosamprenavir, imatinib, indinavir, isoniazid, itraconazole, dalfopristin; quinupristin, posaconazole, ritonavir, telithromycin, tipranavir [boosted with ritonavir], darunavir [boosted with ritonavir], aldesleukin, IL- 2, amiodarone, aprepitant, fosaprepitant atazanavir, bromocriptine, clarithromycin, crizotinib, danazol, diltiazem, dronedarone, erythromycin, fluvoxaMINE, lanreotide, lapatinib, miconazole, mifepristone, nefazodone, nelfinavir, niCARdipine, octreotide, pantoprazole, saquinavir, tamoxifen, verapamil, voriconazole, grapefruit juice): increased axitinib effect CYP3 A4/5 inducers, strong/moderate (rifampin, carBAMazepine, dexamethasone, phenytoin, PHENobarbital, rifabutin, rifapentine, St. John's wort, ethanol, bexarotene, bosentan, efavirenz, etravirine, griseofulvin, metyrapone, modafinil, nafcillin, nevirapine, OXcarbazepine, vemurafenib, pioglitazone, topiramate): decreased effect of axitinib CYP3 A4/5 inhibitor and inducers (quiNINE): increased or decreased axitinib effect
Drug/lab test
Increase: creatinine, lipase, amylase, sodium, potassium, glucose
Decrease: bicarbonate, calcium, albumin, glucose, phosphate, sodium Increase or decrease: sodium, glucose
Drug/herb St. John's wort: decreased effect of axitinib
Nursing Considerations
Assessment
Bleeding: monitor for GI bleeding or perforation; temporarily discontinue therapy at a patient develops any bleeding that requires treatment
Surgery: discontinue \geq 24 hr before surgery, may be resumed after adequate wound healing Hepatic/renal disease: dosage should be reduced in patients with moderate (Child-Pugh Class B) hepatic disease, monitor liver function tests (ALT, AST, bilirubin) before and periodically during therapy; monitor Cr before and during treatment
Hypertension: B/P should be well controlled before starting treatment; monitor patients for hypertension and administer antihypertensive therapy as needed before and during therapy; dose should be reduced for persistent hypertension; therapy should be discontinued if B/P remains elevated after a dosage reduction or if there is evidence of hypertensive crisis; after discontinuation monitor B/P for hypotension in those receiving antihypertensives
Hyper/hypothyroidism: monitor thyroid function tests before and periodically during therapy; thyroid disease should be treated with thyroid medications Monitor for proteinuria before and periodically during therapy; product may need to be decreased or discontinued if moderate to severe proteinuria occurs
Pregnancy/breastfeeding: pregnancy category D; determine if the patient is pregnant or breastfeeding before using this product; may also cause infertility
Patient/family education Instruct patient to use contraception during treatment (pregnancy category D) or to avoid use of this product; to notify prescriber if pregnancy is planned or suspected, not to breastfeed Instruct patient to notify prescriber of bleeding that is severe or that requires treatment Teach patient that product will be discontinued \geq 24 hr before surgery; may be resumed after adequate wound healing Teach patient that laboratory testing will be required before and periodically during product use Teach patient how to monitor B/P and that B/P products should be continued as directed by prescriber
Evaluation
Positive therapeutic outcome: Decreased spread of malignancy
Reference
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