Names and pronunciation
(el-vye-teg′gra-veer/koe-bik′-i-stat/ em-tra-sye′tah-ben/ten-oh-foh′veer) Stribild Genvoya
PDF page 457
Loading InternPractice…
Drug reference
(el-vye-teg′gra-veer/koe-bik′-i-stat/ em-tra-sye′tah-ben/ten-oh-foh′veer) Stribild Genvoya
PDF page 457
Func. class.: Antiretrovirals
PDF page 457
ACTION: Elvitegravir: Inhibits the activity of HIV integrase, which is one of three HIV-encoded enzymes required for viral replication. Cobicistat: An inhibitor of CYP3A enzymes Emtricitabine: A synthetic nucleoside analog of cytidine, inhibits the activity of HIV-1 reverse transcriptase (RT) by com- peting with the natural substrate into viral DNA, resulting in chain termination Tenofovir disoproxil fumarate: Inhib- its viral reverse transcriptase.
PDF page 457
USES: HIV in treatment-naive patients
PDF page 457
CONTRAINDICATIONS: Hyper- sensitivity, CCr <50 mL/min, severe hepatic disease PRECAUTIONS Pregnancy, obesity, osteoporosis, renal disease, Hispanic patients immune reconstitution syndrome
PDF page 457
Black Box Warning: Hepatitis B/HIV combination, hepatitis B exacerbation Black Box Warning: Hepatotoxicity: do not use in risk factors such as alcoholism; discontinue if hepatotoxicity occurs • Carefully evaluate drug interactions before starting therapy • Hepatitis B and HIV coinfection (unlabeled); perform HBV screening in any patient who has HIV; avoid single- drug treatments in HBV • Pregnancy/breastfeeding: use if clearly needed; register pregnant women in the Antiretroviral Pregnancy Registry at 800-258-4263; to reduce the risk of post- natal transmission, HIV-infected mothers are advised to avoid breastfeeding Black Box Warning: Hepatotoxicity: to notify prescriber of dark urine, yellowing of skin/eyes, clay-colored stools, ano- rexia, nausea, vomiting product • To report planned or suspected preg- nancy; not to breastfeed while taking
PDF pages 457, 458, 459
SIDE EFFECTS GI: Abdominal pain, diarrhea, dyspepsia, flatulence, hepatic decompensation, hepatic failure, hepatitis B exacerbation, hepatomegaly, nausea, vomiting, weight gain, pancreatitis, increased LFTs CNS: Anxiety, depression, dizziness, fatigue, headache, insomnia, paresthesias, periph- eral neuropathy, suicidal ideation, fever INTEG: Angioedema, rash, pruritis, skin discoloration/hyperpigmentation MS: Arthralgia, back pain, bone frac- tures, bone pain, myalgia, myopathy, rhabdomyolysis RESP: Cough, dyspnea, pharyngitis, rhi- nitis, sinusitis GU: Glycosuria, hematuria, proteinuria, renal failure, Fanconi syndrome META: Hyperamylasemia, hyperbilirubine- mia, hypercholesterolemia, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypo- glycemia, hypokalemia, hypophosphatemia HEMA: Neutropenia MISC: Infection, lactic acidosis, myas- thenia, steatosis
PDF page 457
DOSAGE AND ROUTES Stribild • Adult/child ≥12 yr, ≥35 kg, CCr ≥70 mL/min: PO 1 tablet daily with food Renal dose • Adult: PO do not use in CCr <50 mL/min Genvoya • Adult/child .512 yr, .535 kg: PO 1 tablet daily with food
PDF page 457
Available forms: Stribid: Tablet 150 mg: elvitegravir-150 mg cobicistat-200 mg emtricitabine-300 mg tenofovir diso- proxil ; Genvoya: tablet 150 mg elvite- gravir, 150 mg cobicistat, 200 mg emtric- itabine, 10 mg tenofovir alafenamide Administer • Administer tablet with food • Don’t use with other antiretrovirals E
PDF page 457
Assess: • HIV: monitor for infections and improvement in symptoms of HIV • Renal/hepatic function tests: AST, ALT, bilirubin, amylase, lipase, triglycerides periodically during treatment • Lactic acidosis, severe hepatomegaly with steatosis: if lab reports confirm these condi- tions, discontinue treatment; may be fatal; more common in females or those who are overweight; monitor lactic acid levels, LFTs
PDF page 458
Evaluate: • Therapeutic response: decreased signs, symptoms of HIV; decreased viral load, increased CD4 counts
PDF page 458
CLINICAL CONSIDERATIONS
PDF page 458
Patient and caregiver information: • That GI complaints resolve after 3-4 wk of treatment • That product must be taken at same time of day to maintain blood level; solution and capsule are not interchange- able; that if dose is missed, to take as soon as remembered; not to double doses; not to share with others • That product will control symptoms but is not a cure for HIV; patient still infectious, may pass HIV virus on to others; that other prod- ucts may be necessary to prevent other infec- tions; to practice safe sex and use a condom; not to share needles or donate blood • That changes in body fat distribution may occur • Lactic acidosis: to notify prescriber immediately if fatigue, muscle aches/pains, abdominal pain, difficulty breathing, nausea, vomiting, change in heart rhythm occur
PDF pages 458, 459
PHARMACOKINETICS Elvitegravir: Onset unknown, peak 4 hr, duration unknown, half-life 13 hr Cobicistat: Onset unknown, peak 3 hr, duration unknown, half-life 4 hr Emtricitabine: Onset unknown, peak 3 hr, duration unknown, half-life 10 hr Tenofovir disoproxil fumarate: Onset unknown, peak 2 hr, duration unknown, half-life 12-18 hr Interactions Decrease: elvitegravir levels—antacids Increase: alfa1 adrenoreceptor antago- nists (alfuzosin) Decrease: elvitegravir, cobicistat levels with analeptics (modafinil) Increase: antiarrhythmic levels (amiod- arone, bepridil, digoxin, disopyramide, fle- cainide, systemiclidocaine, propafenone, quiNIDine) Increase: antibacterials (clarithromycin, telithromycin), cobicistat Increase or Decrease: anticoagulants (warfarin) levels possible Increase: anticonvulsants (carBAMzepine, OXcarbazepine, phenobarbital, phenytoin, clomazepam, ethosuximide), cobicistat, tenofovir, alafenamide Increase: Antidepressants (SSRI parox- etine, tricyclic antidepressants [TCAs], amatriptyline, desipramine, imipramine, nortriptyline, buPROPion; traZODone) Increase: antifungals (itraconazole, keto- conazole, voriconazole Increase: antigout (colchicine) Decrease: elvitegrvir, cobicistat, tenofo- vir, alafenamide Increase: rifabutim with antimicrobac- terial (rifabutim, rifAMPin, rifapentine) Increase: levels of antipsychotic (quetiapine) Increase: levels of benzodiazepine (diaze- PAM, lorazePAM, midazolam, triazolam) Increase: levels of beta-blockers (meto- prolol, timolol) Increase: levels of calcium channel block- ers (amLODIPine, dilTIAZem, felodipine, nicardipine, nifedipine, verapamil) Decrease: levels of elvitegravir, cobicistat with corticosteroids (dexamethasome) Increase: levels of corticosteroids (beta- methasone, budesonide, dexamethasone, fluticasone, mometasone, triamcinolone) Increase: levels of endothelin receptor antagonists (bosentan) Increase: levels of ergot derivatives (dihydroergotamine, ergonovine, ergota- mine, methylergonovine) Increase: levels of GI motility agents (cisapride) Increase: levels of HCV antivirals (teno- fovir, elbasvir, grazoprevir, alafenamide) Increase: levels of HMG-CoA reduc- tase inhibitors Increase: drospirenone, norgesimate Decrease: ethinyl estradiol Increase: levels of immunosuppres- sants, tenofovir alafenamide
PDF pages 457, 458
• Adult/child ≥12 yr, ≥35 kg, CCr ≥70 mL/min: PO 1 tablet daily with food Renal dose
PDF page 457
• Adult/child .512 yr, .535 kg: PO 1 tablet daily with food
PDF page 457