Read Mosby's 2014 Nursing Drug Reference Online
Authors: Linda Skidmore-Roth
Mosby's 2014 Nursing Drug Reference (416 page)
Zelboraf
Func. class.:
Biologic response modifiers; signal transduction inhibitors (STIs)
Inhibitor of some mutated forms of BRAF serine threonine kinase, thereby blocking cellular proliferation in melanoma cells with the mutation; inhibits other kinases including CRAF, ARAF, wild-type BRAF, SRMA, ACK1, MAP4H5, and FGR; potent adenosine triphosphate-competitice inhibitor of RAFs, with a modest preference for mutant BRAF and CRAF compared with wild-type BRAF
Unresectable or metastatic malignant melanoma with V600E mutation of the BRAF gene
Precautions:
Pregnancy (D), breastfeeding, children, infants, neonates, hepatic disease, QT prolongation, secondary malignancy, torsades de pointes, hypokalemia, hypomagnesia, sunlight exposure
Calculator
• Adult:
PO
960 mg (4 tabs) bid about q12hr
Grade 1 or tolerable grade 2 adverse events:
no dosage change;
intolerable grade 2 or grade 3 adverse events (1st episode):
interrupt treatment until toxicity resolves to grade ≤1, when resuming, reduce dosage to 720 mg (3 tabs) bid;
intolerable grade 2 or grade 3 adverse events (2nd episode):
interrupt treatment until toxicity resolves to grade ≤1, when resuming, reduce dose to 480 mg (2 tabs) bid;
intolerable grade 2 or grade 3 adverse events (3rd episode)
discontinue treatment permanently;
grade 4 adverse events (1st episode):
discontinue permanently or interrupt until toxicity resolves to grade ≤1, when resuming, reduce dose to 480 mg (2 tabs) bid;
grade 4 adverse events (2nd episode):
discontinue permanently
Available forms:
Tabs 240 mg
•
Continue until disease progresses or unacceptable toxicity occurs
•
Missed doses can be taken up to 4 hr before the next dose is due, take about 12 hr apart, take without regard to meals
•
Swallow whole with a full glass of water, do not crush or chew
CNS:
Fatigue, fever, asthenia, headache, dizziness, peripheral neuropathy, muscle paralysis
CV:
QT prolongation, atrial fibrillation,
peripheral edema, hypotension
EENT:
Uveitis, blurred vision, iritis, photophobia
GI:
Nausea, diarrhea, vomiting, constipation, dysgeusia, decreased appetite, weight loss
INTEG:
Alopecia, pruritus, hyperkeratosis, maculopapular rash, actinic keratosis, xerosis/dry skin, papular rash, palmar-plantar erythrodysesthesia (hand and foot syndrome), photosensitivity
MS:
Arthralgia, myalgias, extremity pain, musculoskeletal pain, back pain, arthritis
RESP:
Cough
SYST:
Secondary malignancy, anaphylaxis
>99% protein binding (albumin and alpha-1 acid glycoprotein) an inhibitor of CYP1A2, 2A6, 2C9, 2C19, 2D6, 3A4/5 CYP1A2 inhibitor, a weak CYP2D6 inhibitor, and a CYP3A4 inducer; elimination 94% in feces, 1% in urine, half-life 57 hr
Increase:
vemurafenib effect—CYP3A4/CYP1A2 inhibitors (enoxacin, cimetidine, delavirdine, indinavir, isoniazid, itracon
azole, dalfopristin, quinupristin, tipranavir)
Increase:
QT prolongation, torsades de pointes—arsenic trioxide, certain phenothiazines (chlorproMAZINE, mesoridazine, thioridazine), grepafloxacin, levomethadyl, pentamidine, probucol, sparfloxacin, troleandomycin, class IA antiarrhythmics (disopyramide, procainamide, quiNIDine), class III antiarrhythmics (amiodarone, dofetilide, ibutilide, sotalol), clarithromycin, ziprasidone, pimozide, haloperidol, halofantrine, quiNIDine, chloroquine, dronedarone, droperidol, erythromycin, methadone, posaconazole, propafenone, saquinavir, abarelix, amoxapine, apomorphine, asenapine, β-agonists, ofloxacin, eribulin, ezogabine, flecainide, gatifloxacin, gemifloxacin, halogenated anesthetics, iloperidone, levofloxacin, local anesthetics, magnesium sulfate, potassium sulfate, sodium, maprotiline, moxifloxacin, nilotinib, norfloxacin, ciprofloxacin, OLANZapine, paliperidone, some phenothiazines (fluPHENAZine, perphenazine, prochlorperazine, trifluoperazine), telavancin, tetrabenazine, tricyclic antidepressants, venlafaxine, vorinostat, citalopram, alfuzosin, cloZAPine, cyclobenzaprine, dolasetron, palonosetron, QUEtiapine, rilpivirine, SUNItinib, tacrolimus, vardenafil, indacaterol, dasatinib, fluconazole, lapatinib, lopinavir/ritonavir, mefloquine, octreotide, ondansetron, ranolazine, risperiDONE, telithromycin, vemurafenib
Decrease:
vemurafenib effect—CYP3A4 inducers (rifampin, barbiturates, carBAMazepine, phenytoin, erythromycin, ketoconazole, fluvoxaMINE, alcohol, etravirine, ritonavir, bexarotene, rifabutin, OXcarbazepine, nevirapine, modafinil, metyrapone)
Increase:
serum creatinine, LFTs, alkaline phosphatase, bilirubin
•
Hepatic Disease:
Liver function test (LFT) abnormalities, altered bilirubin levels, may occur; monitor LFTs and bilirubin levels before treatment, then monthly; more frequent testing is needed in those with grade 2 or greater toxicities; laboratory alterations should be managed with dose reduction, treatment interruption, or discontinuation
QT prolongation
: has been reported with the use of this product; therefore, should be avoided in patients with QT prolongation; monitor ECG and electrolytes in those with congestive heart failure, bradycardia, electrolyte imbalance (hypokalemia, hypomagnesemia), or those who are taking concomitant medications known to prolong the QT interval; treatment interruption, dosage adjustment, treatment discontinuation may be needed in those who develop QT prolongation
Pregnancy/breastfeeding:
Identify if pregnancy is planned or suspected, pregnancy category D, avoid breastfeeding
•
Serum electrolytes
•
Storage at room temperature, in original container
•
Decreased spread of malignancy
•
Teach patient missed doses can be taken up to 4 hr before the next dose is due to maintain the twice-daily regimen
Teach patient to use reliable contraception; both women and men of childbearing age should use adequate contraceptive methods during therapy and for at least 90 days after completing treatment, pregnancy category D
Canada only Side effects:
italics
= common;
bold
= life-threatening Nurse Alert
(ven-la-fax′een)
Effexor
, Effexor XR
Func. class.:
Antidepressant—SNRI
Chem. class.:
SNRI