Names and pronunciation
(bik-teg′-ra-veer/em-try-sye′tah- been/ten-of′oh-veer al′e′fen′ a-mide) Biktarvy
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Drug reference
(bik-teg′-ra-veer/em-try-sye′tah- been/ten-of′oh-veer al′e′fen′ a-mide) Biktarvy
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Func. class.: HIV antivirals
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Chem. class.: Integrase strand transfer inhibitor (INSTI); nucleoside and nucleotide reverse transcriptase inhibitor (NRTI) combinations
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ACTION: A 3-drug combination of bictegravir (BIC), an HIV-1 integrase strand transfer inhibitor (INSTI), and emtricitabine (FTC) and tenofovir alafen- amide (TAF), both HIV-1 nucleoside analog reverse transcriptase inhibitors (NRTIs)
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USES: Complete regimen for the treat- ment of HIV-1 infection in adults who have no antiretroviral treatment history or to replace the current antiretroviral regi- men in those who are virologically sup- pressed (HIV-1 RNA <50 copies per mL)
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CONTRAINDICATIONS: Do not use with dofetilide, rifAMPin; hypersen sitivity Precautions: Alcoholism, breastfeed- ing, Graves’ disease, pregnancy, hepatic impairment, HIV resistance, immune reconstitution syndrome, infection resis- tance, osteoporosis, renal impairment, lactic acidosis/severe hepatomegaly with steatosis, suicidal ideation
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Black Box Warning: Hepatitis B and HIV coinfection, hepatitis B exacerbation Black Box Warning: Exacerbations of HBV in coinfection with HBV: monitor for several months after treatment especially in hepatotoxicity • Pregnancy/breastfeeding: for preg- nant women, therapy should begin im- mediately after HIV diagnosis. Therapy may be initiated before drug resistance testing results are available; modify based on the assay • Depression and suicidal ideation: al- though rare, has occurred in those with depression before treatment • Immune reconstitution syndrome: that patients may develop an inflamma- tory response to opportunistic infections (such as Mycobacterium avium infection, cytomegalovirus, Pneumocystis jirovecii pneumonia [PCP], or TB), autoimmune disorders (Graves’ disease, polymyositis, and Guillain-Barré syndrome); response B may occur during or many months after starting treatment
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SIDE EFFECTS CNS: Fatigue, abnormal dreams, head- ache, depression, suicidal ideation GI: Nausea, vomiting, diarrhea, steatosis, hepatomegaly, exacerbation of HBV infection HEMA: Immune reconstitution syndrome MISC: Lactic acidosis, rash
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INTERACTIONS • Do not use with other antiretrovirals for HIV, rifAMPin Increase: effect of metFORMIN Increase: effect of this HIV combination product—OCT2 and MATE1 (dofeti- lide); CYP3A4 inhibitors, UGT1A1 inhibitors Decrease: concentration of this HIV combination product—carBAMazepine, OXcarbazepine, phenobarbital, phenyt- oin; use alternative anticonvulsants Decrease: concentration of this HIV combination product—products that in- hibit P-gp and BCRP Drug/Herb Avoid use with St. John’s wort
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DOSAGE AND ROUTES • Adult: 1 tablet daily
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Available forms: Tablets 50 mg bicte- gravir, 200 mg emtricitabine, 25 mg te- nofovir alafenamide
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Administer: • With or without food • Do not use 2 hr before or after dairy products or antacids that contain alumi- num, magnesium, or calcium
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Assess: • HIV: symptoms and change in severity; opportunistic infections may occur with HIV; assess for these infections through- out therapy • Osteoporosis and bone mineral loss: assess those who have had prior frac- tures, osteoporosis, or mineral bone loss • Hepatitis B infection: before use, test for hepatitis B virus infection; monitor hepatitis B serology, plasma hepatitis C RNA • Lab testing: before use and periodi- cally during treatment, assess serum cre- atinine, estimated CCr, urine glucose, urine protein, serum phosphorus in those with chronic kidney disease • Monitor blood glucose, CBC with dif- ferential, CD4+ T-cell count, LFTs, plasma HIV RNA, pregnancy testing (if applicable), serum bilirubin (total and direct), serum cholesterol, BUN, serum lipid profile, urinalysis
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Evaluate: • Therapeutic response: improving signs and symptoms of HIV, improving CD4+ counts, plasma HIV RNA with only mod- erate side effects TEACH PATIENT/FAMILY • To take as directed, not to skip or double doses; if missed, to take when remembered; not to share with others • That product is not a cure; that pa- tient is still infective and may transmit infection to others via sexual contact, blood transfusions, or sharing nee- dles; to practice safe sex, as using a condom will prevent transmission from person to person; not to donate blood • That lab testing will be required peri- odically during treatment • Lactic acidosis/hepatomegaly with stenosis: to report immediately nausea, vomiting, abdominal pain, severe weakness • To inform all health care providers of OTC, Rx, herbal products, supplements taken; not to start or stop without con- sent of prescriber; to avoid St. John’s wort • Not to use antacids, dairy products 2 hr before or after this product • Pregnancy/breastfeeding: to notify health care provider if pregnancy is planned or suspected; if pregnant, to enroll in the Antiretroviral Pregnancy Registry (800-258-4263); to avoid breastfeeding
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CLINICAL CONSIDERATIONS
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PHARMACOKINETICS Bictegravir: Protein binding >99%, elim- ination via metabolism, mediated by CYP3A and UGT1A1 enzymes; excreted in feces (60.3%), urine (35%), half-life 17.3 hr Emtricitabine: Protein binding <4%, ex- creted in urine (70%), feces (13.7%), half-life 10 hr Tenofovir AF: Protein binding 80%, elim- ination via metabolism (more than 80% of dose), excreted in feces (31.7%), elimination of metabolite via kidneys (70%-80%) by a combination of glo- merular filtration and active tubular se- cretion, half-life 0.51 hr; metabolite half-life of 150-180 hr
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• Adult: 1 tablet daily
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