Names and pronunciation
Edurant
Source page 1158
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Individual generic drug information
Extracted information for rilpivirine only.
Edurant
Source page 1158
Func. class.: Antiretroviral
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Chem. class.: Nonnucleoside tran- scriptase inhibitors (NNTIs)
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ACTION: Inhibits HIV-1 reverse transcriptase; binds directly to a site on reverse transcriptase, causing disruption of the enzyme’s active site and blocking RNA- dependent and DNA-dependent DNA polymerase
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USES: HIV in combination with other antiretrovirals
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Extracted information for rilpivirine only.
CONTRAINDICATIONS: Hyper sensitivity Precautions: Pregnancy, breastfeeding, neonates, infants, children, adolescents <18 yr, immune reconstitution syn- drome, antimicrobial resistance, pancre- atitis, coinfection hepatitis B or C and HIV, hepatic disease, depression, suicidal ideation, QT prolongation, torsades de pointes, hyperlipidemia, hypertriglyceri- demia, hypercholesterolemia, immune reconstitution syndrome
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SIDE EFFECTS CNS: Depressed mood, dizziness, drows- iness, suicide attempts GI: Hepatotoxicity, nausea, vomiting, diarrhea INTEG: Drug reaction with eosinophilia and systemic symptoms (DRESS) MISC: Immune reconstitution syndrome
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INTERACTIONS Increase: rilpivirine effect—CYP3A4 inhibitors (delavirdine, efavirenz, daruna- vir, tipranavir, atazanavir, fosamprenavir, indinavir, nelfinavir, aldesleukin IL-2, amiodarone aprepitant, basiliximab, boceprevir, bromocriptine, chloram phenicol, clarithromycin, conivaptan, danazol, dalfopristin, dasatinib, diltia ZEM, dronedarone, erythromycin, ethinyl estradiol, fluconazole, FLUoxetine, fluvox- aMINE, fosaprepitant, imatinib, isoniazid, itraconazole, ketoconazole, lanreotide, lapatinib, miconazole, nefazodone, niCA- Rdipine, octreotide, posaconazole, qui- NINE, 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, pent- amidine; CYP3A4 inhibitors (amiodarone, clarithromycin, erythromycin, telithromy- cin, troleandomycin, arsenic trioxide); CYP3A4 substrates (methadone, pimo- zide, QUEtiapine, quiNIDine, risperiDONE, ziprasidone, lopinavir, saquinavir, flucon- azole, posaconazole, dasatinib, dronedar- one, lapatinib, octreotide, ranolazine, citalopram, abarelix, alfuzosin, amoxapine, apomorphine, artemether, lumefantrine, asenapine, ofloxacin, ciprofloxacin, clo- ZAPine, cyclobenzaprine, dolasetron, eriBULin, flecainide, gatifloxacin, gemiflo xacin, halogenated anesthetics, iloperidone, levoFLOXacin, maprotiline, mefloquine, moxifloxacin, nilotinib, norfloxacin, OLAN- Zapine, ondansetron, paliperidone, palo- nosetron, QUEtiapine) Increase: rilpivirine adverse reactions, fun- gal infections—fluconazole, voriconazole Decrease: rilpivirine effect, treatment failure—CYP3A4 inducers (phenytoin, fosphenytoin, barbiturates, OXcarbaze- pine, carBAMazepine, rifabutin, rifAMPin, rifapentine, dexamethasone), efavirenz, nevirapine, ritonavir; amino- glutethimide, bexarotene, bosentan, gris- eofulvin, metyraPONE, modafinil, flu- tamide, 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 hr before or 4 hr after rilpivirine Drug/Herb Decreased effect—St. John’s wort, do not use together Drug/Food Increase: adverse reactions—grapefruit juice
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Extracted information for rilpivirine only.
DOSAGE AND ROUTES Antiretroviral treatment-naive adults (HIV) in combination • Adult/child ≥12 yr and ≥35 kg: PO 25 mg/day with a meal; if used with rifabutin, increase rilpivirine dose to 50 mg/day
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Available forms: Tab 25 mg
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Administer: • Give with other antiretroviral agents; in antiretroviral treatment-naive adults, ril- pivirine is used as an alternative to efavi- renz in NNRTI-based treatment regimens; potential rilpivirine-based treatment regi- mens combine rilpivirine with either tenofovir plus emtricitabine or lamiVU- Dine; or abacavir plus emtricitabine or lamiVUDine; or zidovudine plus emtri citabine or lamiVUDine • Give with a meal • Store at room temperature away from heat and moisture
Source page 1158
Extracted information for rilpivirine only.
Assess: • HIV: Assess symptoms of HIV including opportunistic infections before and dur- ing treatment; some may be life-threaten- ing; monitor plasma HIV RNA, CD4+, CD8+ cell counts, serum β-2 microglob- ulin, serum ICD+24 antigen levels; treat- ment failures occur more frequently in those with baseline HIV-1 RNA concentra- R tions >100,000 copies/mL than in pa- tients with concentrations <100,000 cop- ies/mL; monitor serum cholesterol, lipid panel; assess for redistribution of body fat • Antiretroviral drug resistance testing before initiation of therapy in antiretrovi- ral treatment-naive patients • For adults and adolescents, initiation of antiretroviral therapy is recommended in any patient with a history of an AIDS-defin- ing infection; with a CD4 ≤500/mm3; who is pregnant; who has HIV-associated ne- phropathy; or who is being treated for hepatitis B (HBV) infection. Only delay treatment for resistance testing • Hepatic disease: monitor for elevated hepatic enzymes (>2.5 × ULN); grade 3 and 4 may be higher in patients coin- fected with hepatitis B or C • Suicidal thoughts/actions: assess for suicidal ideation often, report increase in depressive symptoms • DRESS: may occur in 2-8 wk, skin eruptions, eosinophilia, lymphadenopa- thy, fever, inflammation of internal or- gans; if these occur, stop product, report immediately; systemic steroids are usu- ally given • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; enroll preg- nant women taking this product in the Antiretroviral Pregnancy Registry, 1-800- 258-4263; do not breastfeed, excretion unknown
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That product is not a cure but controls symptoms; that continuing use is re- quired • That product must be taken in combi- nation with other prescribed products; that if dose is missed, not to take if next dose is within 12 hr • To discuss all products taken, includ- ing OTC, Rx, herbals, supplements, as there are many interactions • To report immediately mood changes and depression • To report hypersensitivity reactions • That dizziness may occur, not to drive until response is known • To immediately report if pregnancy is suspected; not to breastfeed
Source page 1160
Extracted information for rilpivirine only.
PHARMACOKINETICS: Protein binding (99.7%) to albumin; metabolism via oxidation CYP3A; 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)
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Filter the extracted dose blocks for this individual drug.
Antiretroviral treatment-naive adults (HIV) in combination
• Adult/child ≥12 yr and ≥35 kg: PO 25 mg/day with a meal; if used with rifabutin, increase rilpivirine dose to 50 mg/day
Candidate age grouping · source page 1158