Names and pronunciation
(doe-loo-teg′ra-vir/ril-pi-vir′een) Juluca
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Drug reference
(doe-loo-teg′ra-vir/ril-pi-vir′een) Juluca
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Func. class.: Antiretroviral/antiviral
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Chem. class.: INST/NRTI
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ACTION: Rilpivirine is a nucleoside analog that inhibits HIV reverse transcriptase; dolutegravir inhibits the catalytic activ- ity of HIV integrase
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USES: HIV-1 infection in adults
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CONTRAINDICATIONS: Hypersensitivity Precautions: Alcoholism, autoim- mune disease, bone fractures, breast- feeding, children, depression, females, Graves disease, Guillain-Barré syn- drome, hepatic disease, hepatitis, hep- atitis B and HIV coinfection, hepatitis C and HIV coinfection, hepatomegaly, HIV resistance, hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, hypophosphatemia, immune reconsti- tution syndrome, lactic acidosis, obe- sity, osteomalacia, osteoporosis, preg- nancy, renal failure, renal impairment, serious rash, suicidal ideation, tors- ades de pointes
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Black Box Warning: Hepatitis B exac- erbation, hepatotoxicity Black Box Warning: Hepatotoxicity/ lactic acidosis: Monitor hepatitis B serol- ogy, LFTs, plasma hepatitis C RNA, lac- tic acidosis levels. If lab reports confirm these conditions, discontinue product. More common in females or those who are overweight. Avoid use in alcoholism • Patients coinfected with HBV and HIV who discontinue this product should have transaminase concentrations monitored q6wk for the first 3 mo, and q3-6 mo thereafter. • Resumption of anti–hepatitis B treat- ment may be required • Periodically monitor serum bilirubin (total and direct), serum creatinine, uri- nalysis, LFTs, amylase, lipase • Pregnancy: Obtain pregnancy testing prior to use; hepatitis B exacerbation: those with coexisting HBV and HIV infec- tions who discontinue this product may experience severe acute hepatitis B exac- erbation with some cases resulting in hepatic decompensation and hepatic failure Black Box Warning: Hepatotoxicity: to notify prescriber of dark urine, yellowing skin or eyes, clay-colored stools, anorex- ia, nausea, vomiting • Discuss with provider all Rx, OTC, herbs, and supplements taken, as there are many drug interactions • Immune reconstitution syndrome: Advise patients to inform their health care provider immediately of any signs and symptoms of infection, as inflammation from previous infection may occur • Instruct patients that if they miss a dose, to take it as soon as they remem- ber, not to double their next dose or take more than the prescribed dose
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SIDE EFFECTS CNS: Headache, abnormal dreams, depression, dizziness, insomnia, neu- ropathy, paresthesia, asthenia, fatigue, drowsiness GI: Nausea, vomiting, anorexia, diarrhea, abdominal pain, dyspepsia hepatomeg- aly with stenosis (may be fatal), hyper- bilirubinemia, hypercholesterolemia, pancreatitis GU: Glomerulonephritis membranous/ mesangial proliferative INTEG: Rash, skin discoloration MS: Arthralgia, myalgia, rhabdomyolysis RESP: Cough SYST: Change in body fat distribution, lactic acidosis
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INTERACTIONS Decreased levels, virologic resistance- CYP3A4 inhibitors (aldesleukin IL-2, amiodarone, aprepitant, atazanavir, basi liximab, boceprevir, bromocriptine, chloramphenicol, clarithromycin, coni vaptan, danazol, dalfopristin, darunavir, dasatinib, delavirdine, dilTIAZem, dronedarone, efavirenz, erythromycin, ethinyl estradiol, fluconazole, fluoxetine, fluvoxamine, fosamprenavir, fosaprepitant, imatinib, indinavir, isoniazid, itraconazole, ketoconazole, lanreotide, lapatinib, micon- azole, nefazodone, nelfinavir, nicardipine, octreotide, posaconazole, quinine, ranola- zine, rifAXIMin, tamoxifen, telaprevir, telithromycin, tipranavir, troleandomycin, verapamil, voriconazole, zafirlukast) Increased: metFORMIN Increased: dofetilide, coadministration is contraindicated Decrease: dolutegravir—carBAMaze- pine, rifAMPin, an additional dolutegra- vir 50-mg dose should be taken Decrease: dolutegravir—OXcarbazepine, phenytoin, phenobarbital, avoid coadministration Drug/Lab Test: Increase: AST/ALT, amylase, bilirubin, CK, glucose, lipase Decrease: neutrophils NURSING CONSIDERATIONS
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DOSAGE AND ROUTES Adults: PO 1 tablet 50 mg dolutegravir; 25 mg rilpivirine daily
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Available forms: Tablet 50 mg dolute- gravir, 25 mg rilpviirine
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Administer: • Give without regard to food • During coadministration with carBAMaz epine or rifAMPin, the dolutegravir dose needs to be increased to 50 mg bid; add 50 mg/day of dolutegravir (separated by 12 hr from dolutegravir; lamivudine) should be given • Avoid use in treatment-experienced patients and in patients with known sub- stitutions associated with resistance to dolutegravir or lamivudine • Do not use within 2 hr prior to or 6 hr after iron or calcium supplement • Do not use within 2 hr prior to or 6 D hr after antacids, laxatives, or other medicines that contain aluminum, magnesium, sucralfate, or buffered medicines • Admixtures are stable for at least 24 hr at room temperature under normal room fluorescent light in Baxter Viaflex PVC infusion containers
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Assess: • HIV infection: Assess symptoms of HIV, including opportunistic infections, prior to and during treatment, some may be life threatening; monitor plasma CD4+, CD8 cell counts, serum beta-2 microglobulin, serum antigen levels, treatment failures occur more often in those with baseline HIV-1 RNA concentrations <100,000 cop- ies/mL than in those <100,000 copies/mL; monitor blood glucose, CBC with differen- tial, serum cholesterol, lipid panel
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Evaluate: • Therapeutic response: improvement in CD4, HIV RNC counts, decreasing signs and symptoms of HIV
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Patient and caregiver information: • That hepatitis and HIV coinfected pa- tients should avoid consuming alcohol; offer vaccinations against hepatitis A/ hepatitis B as appropriate • That GI complaints resolve after 2-3 wk of treatment • To report suspected or planned preg- nancy, not to breastfeed. Instruct moth- ers with HIV-1 infection not to breastfeed because HIV-1 can be passed to the baby in the breast milk, inform patients that there is an antiretroviral pregnancy regis- try to monitor fetal outcomes • To take at the same time of day to maintain blood level; not to crush, break, or chew • That product controls the symptoms of HIV but does not cure, that patient is still able to infect others, that other prod- ucts may be necessary to prevent other infections • Lactic acidosis: to notify prescriber of fatigue, muscle aches/pains, abdominal pain, difficulty breathing, nausea, vomit- ing, change in heart rhythm
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PHARMACOKINETICS • Rilpivirine: Onset unknown, peak 4 hr, duration unknown, half-life 50 hr • Dolutegravir: 99% protein binding, metabolism occurs via UDP-glucuronos- yltransferase (UGT)1A1 (major) and by the hepatic isoenzyme CYP3A (minor), half-life 14 hr, 53% excreted unchanged in the feces, urine excretion 31%
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