Read Mosby's 2014 Nursing Drug Reference Online
Authors: Linda Skidmore-Roth
Canada only Side effects:
italics
= common;
bold
= life-threatening
Nurse Alert
Edurant
Func. class.:
Antiretroviral
Chem. class.:
Nonnucleoside transcriptase inhibitors (NNTIs)
Inhibits HIV-1 reverse transcriptase; unlike nucleoside reverse transcriptase inhibitors (NRTIs), it does not compete for binding nor does it require phosphorylation to be active. Binds directly to a site on reverse transcriptase causing disruption of the enzyme’s active site thereby blocking RNA-dependent and DNA-dependent DNA polymerase activities
HIV in combination with other antiretrovirals
Hypersensitivity
Precautions:
Pregnancy (B), breastfeeding, neonates, infants, children, adolescents <18 yr, immune reconstitution syndrome, antimicrobial resistance, pancreatitis, coinfection hepatitis B or C and HIV, hepatic disease, depression, suicidal ideation, QT prolongation, torsades de pointes, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, immune reconstitution syndrome
• Adults:
PO 25 mg/day with a meal
Available forms:
Tab 25 mg
•
Give in combination with other antiretroviral agents; in antiretroviral treatment–naive adults, rilpivirine is utilized as an alternative to efavirenz in NNRTI-based treatment regimens; potential rilpivirine-based treatment regimens combine rilpivirine with either tenofovir plus emtricitabine or lamiVUDine; or abacavir plus emtricitabine or lamiVUDine; or zidovudine plus emtricitabine or lamiVUDine
•
Give with a meal
CNS:
Depressed mood, dysphoria, major depression, mood alteration, negative thoughts,
suicide attempts,
fatigue, headache, dizziness, drowsiness
GI:
Nausea, vomiting, abdominal pain, diarrhea, cholecystitis, cholelithiasis, decreased appetite, elevated hepatic enzymes, hyperbilirubinemia, hypercholesterolemia
GU:
Glomerulonephritis membranous/glomerulonephritis mesangioproliferative
Protein binding (99.7%) to albumin; metabolism via oxidation CYP3A; terminal elimination half-life 50 hr, excretion feces (85%), 25% excreted unchanged; urine (6.1%); peak 4-5 hr; increased effect 40% (food), decreased effect 50% (high protein drink)
Increase:
rilpivirine effect—CYP3A4 inhibitors (delavirdine, efavirenz, darunavir, tipranavir, atazanavir, fosamprenavir, indinavir, nelfinavir, aldesleukin IL-2, amiodarone aprepitant, basiliximab, boceprevir, bromocriptine, chloramphenicol, clarithromycin, conivaptan danazol, dalfopristin, dasatinib, diltiazem, dronedarone, erythromycin, ethinyl estradiol, fluconazole, FLUoxetine, fluvoxaMINE, fosaprepitant, imatinib, isoniazid, itraconazole, ketoconazole, lanreotide, lapatinib, miconazole, nefazodone, niCARdipine, octreotide, posaconazole, quiNINE, ranolazine, rifaximin, tamoxifen, telaprevir, telithromycin, troleandomycin, verapamil, voriconazole, zafirlukast)
Increase:
QT prolongation—class IA/III antidysrhythmics, some phenothiazines, β-agonists, local anesthetics, tricyclics, chloroquine, droperidol, haloperidol, pentamidine; CYP3A4 inhibitors (amiodarone, clarithromycin, erythromycin, telithromycin, troleandomycin, arsenic trioxide, levomethadyl); CYP3A4 substrates (methadone, pimozide, QUEtiapine, quiNIDine, risperiDONE, ziprasidone, lopinavir, saquinavir, fluconazole, posaconazole, dasatinib, dronedarone, lapatinib, octreotide, ranolazine, citalopram, abarelix, alfuzosin, amoxapine, apomorphine, artemether, lumefantrine, asenapine, ofloxacin, ciprofloxacin, cloZAPine, cyclobenzaprine, dolasetron, eribulin, flecainide, gatifloxacin, gemifloxacin, halogenated anesthetics, iloperidone, levofloxacin, maprotiline, mefloquine, moxifloxacin, nilotinib, norfloxacin, OLANZapine, ondansetron, paliperidone, palonosetron, QUEtiapine)
Increase:
rilpivirine adverse reactions, fungal infections—fluconazole, voriconazole
Decrease:
rilpivirine effect, treatment failure—CYP3A4 inducers (phenytoin, fosphenytoin, barbiturates, OXcarbazepine, carBAMazepine, rifabutin, rifampin, rifapentine, dexamethasone), efavirenz, nevirapine, ritonavir; aminoglutethimide, bexarotene, bosentan, griseofulvin, metyrapone, modafinil, flutamide, nafcillin, pioglitazone, primidone, topiramate); proton pump inhibitors (PPIs)
Decrease:
rilpivirine effect, treatment failure—H2 receptor antagonists (cimetidine, famotidine, nizatidine, ranitidine), give 12 hr before or 4 hr after rilpivirine
Decrease:
rilpivirine effect—antacids, use >2 hrs before, or 4 hr after rilpivirine
Increase:
adverse reactions—grapefruit juice
•
HIV:
Assess symptoms of HIV including opportunistic infections before and during treatment, some may be life- threatening; monitor plasma HIV RNA, CD4+, CD8 + cell counts, serum β-2 microglobulin, serum ICD+24 antigen levels; treatment failures occur more frequently in those with baseline HIV-1 RNA concentrations >100,000 copies/ml than in patients with concentrations <100,000 copies/ml; monitor serum cholesterol, lipid panel
•
Antiretroviral drug resistance testing is recommended before initiation of therapy in antiretroviral treatment–naive patients
•
For adults and adolescents, initiation of antiretroviral therapy is recommended in any patient with a history of an AIDS-defining infection; with a CD4 ≤500/mm
3
; who is pregnant; who has HIV-associated nephropathy; or who is being treated for hepatitis B (HBV) infection
Suicidal thoughts/behaviors:
Assess frequently for suicidal ideation, report any increase in depressive symptoms
•
Hepatic disease: monitor for elevated hepatic enzymes (>2.5 × ULN); grade 3 and 4 may be higher in patients co-infected with hepatitis B or C
•
Storage at room temperature away from heat and moisture
•
That product is not a cure but controls symptoms
•
That product must be taken in combination with other prescribed products
Canada only Side effects:
italics
= common;
bold
= life-threatening
Nurse Alert
(rill′you-zole)
Rilutek
Func. class.:
ALS agent
Chem. class.:
Benzathiazole
May act by modulating the release of glutamate and inactivating voltage-dependent sodium channels
Amyotropic lateral sclerosis (ALS)
Hypersensitivity
Precautions:
Pregnancy (C), breastfeeding, children, geriatric patients, neutropenia, renal/hepatic disease, cigarette smoking, febrile illness, pneumonia
• Adult:
PO
50 mg q12hr, take 1 hr before or 2 hr after meals
Available forms:
Tabs 50 mg
•
1 hr before or 2 hr after meals; high-fat meal decreases absorption
CNS:
Hypertonia, depression, dizziness, insomnia, somnolence, vertigo, paresthesia
CV:
Hypertension, tachycardia, phlebitis, palpitation, postural hypertension
GI:
Nausea, vomiting, dyspepsia, anorexia, diarrhea, flatulence, stomatitis, dry mouth, increased LFTs, jaundice, abdominal pain
GU:
UTI, dysuria
HEMA:
Neutropenia
INTEG:
Pruritus, eczema, alopecia,
exfoliative dermatitis
MS:
Arthralgia
RESP:
Decreased lung function, rhinitis, increased cough, pneumonia
Well absorbed; extensively metabolized by liver; excretion in urine, feces
Increase:
elimination of riluzole—cigarette smoking, rifampin, omeprazole, charcoal-broiled food
Increase:
hepatic injury—allopurinol, methyldopa, sulfaSALAzine, leflunomide, methotrexate, tacrine
Increase:
LFTs—barbiturates, carBAMazepine
Decrease:
elimination of riluzole—caffeine, theophylline, amitriptyline, quinolones
Decrease:
absorption—high-fat meal
•
Clinical improvement of neurologic function
•
Hepatic studies: AST, ALT, bilirubin, GGT at baseline, monthly × 3 mo, then q3mo; monitor LFTs
•
Neutropenia <500/mm
•
Therapeutic response: improvement in neurologic status
•
To report febrile illness, signs of infection, cardiac/respiratory changes, which may indicate neutropenia
•
About the reason for the product, expected results