NULOESIDE/TIDE REVERSE TRANSRIPTASE INHIBITORS (N(t)RTIs) Abacavir AB (Ziagen) Emtricitabine FT (Emtriva) Lamivudine 3T (Epivir) Tenofovir disoproxil fumarate TDF (Viread) Zidovudine AZT, ZDV (Retrovir) N(t)RTI o-formulations Zidovudine/ Lamivudine AZT/3T (ombivir) Tablet: 300mg Generic tablet: 300mg Oral solution: 20mg/mL (brand and generic) apsules: 200mg Oral solution: 10mg/mL Tablets: 100mg, 150mg, 300mg Generic tablets: 100mg, 150mg, 300mg Oral solution: 5mg/mL, 10mg/mL Generic oral solution: 10 mg/ml Tablets: 150mg, 200mg, 250mg, 300mg Generic tablet: 300 mg Oral powder: 40mg/g apsule: 100mg Tablet: 300mg Oral syrup: 10mg/mL Generic capsule, tablet, oral syrup Injection solution: 10mg/mL Tablet: 300mg AZT/150mg 3T Generic tablets available 300mg BID 600mg QD 200mg QD (capsule) 240mg (24 ml) QD oral solution 150mg BID or 300mg QD 300mg QD 300mg BID 200mg TID One tablet (300/150) BID No renal adjustment required 5-6 200mg BID > 6 ontraindicated rl apsule Solution 30-49 200mg Q48h 120mg Q24h 15-29 200mg Q72h 80mg Q24h < 15 or HD 200mg Q96h 60mg Q24h 30-49 150mg QD 15-29 150mg x1, 100mg QD 5-14 150mg x1, 50mg QD < 5 or HD 50mg x1, 25mg QD No hepatic adjustment necessary 30-49 300mg Q48h 10-29 300mg Twice weekly HD 300mg Q7 days No hepatic adjustment necessary < 15 or HD 100mg TID or 300mg QD rl < 50mL/min: not recommended hepatotoxicity, mitochondrial toxicity, lactic acidosis N, V, HSR: fever, malaise, GI s/sx, R; do not re-challenge heck HLA-B*5701 to avoid hypersensitivity reaction HA, N, V HA, N, V N, V, flatulence, renal toxicity, bone mineral density Anemia, HA, N, V Minimal Minimal Minimal hepatotoxicity, mitochondrial toxicity, lactic acidosis See AZT & 3T Increases ddi AU: reduce ddi dose to 250mg QD if given with TDF. Minimal; avoid use with other bone marrow (BM) toxic medications. See AZT & 3T Abacavir / Lamivudine AB/3T (Epzicom) Tablet: 600mg AB/300mg 3T Generic tablets available One tablet (600/300) QD rl < 50mL/min: not recommended ontraindicated in mild-moderate hepatic impairment (PT B or ) See AB & 3T See AB & 3T
/ Emtricitabine TDF/FT (Truvada) Tenofovir AF/ Emtricitabine TAF/FT (Descovy) (TAF= tenofovir alafenamide) Tenofovir DF/Lamivudine TDF/FT (imduo or Temixys) Tablet: 300mg TDF/200mg FT, 150mg TDF/100mg FT, 200mg TDF/133mg FT, 250mg TDF/167mg FT Tablet: 25mg TAF/200mg FT Tablet: 300 mg 3T/300 mg TDF NON-NULOESIDE REVERSE TRANSRIPTASE INHIBITORS (NNRTIs) Adult Dosing Renal/Hepatic Dose Adjustments Adverse Reactions Potential for Interactions One tablet (300/200) QD One tablet (25/200) QD One tablet (300/300) QD 30-49 1 tab Q48h < 30 Not recommended o-formulation can be given if rl 30 ml/min. Not recommended if rl < 30 ml/min or on hemodialysis. No dose adjustment in hild-pugh A or B, No dosing data for hild-pugh rl < 50mL/min: not recommended ESRD on HD: not recommended See TDF & FT See TDF & FT N, LDL/total cholesterol Avoid strong inducers See TDF & 3T rash, hepatotoxicity See TDF & 3T Efavirenz EFV (Sustiva) apsules: 50mg, 200mg (brand and generic) Tablet: 600mg (brand and generic) 600mg QD Initially at HS and preferably on empty stomach No hepatic adjustment; use with caution NS effects: dizziness, insomnia, vivid dreams Inducer, inhibitor, and substrate of liver enzymes Etravirine ETR (Intelence) Tablets: 25mg, 100mg, 200mg 200mg BID No renal dose adjustment A or B No data N ETR is a substrate and inducer of liver enzymes (3A4, 29, 219). Do not co-administer with TPV/r, FPV/r, ATV/r, non-rtv-boosted PIs, & other NNRTIs. Nevirapine NVP (Viramune) Tablet: 200mg (brand and generic) Extended release tablet: 100mg, 400mg (brand and generic) Oral suspension: 10mg/mL (brand and generic) 200mg QDx2wks; then 200mg BID rl 20 < 20 No data Dose ontraindicated in hild-pugh lass B or R, hepatotoxicity Both substrate and inducer of liver enzymes Rilpivirine RPV (Edurant) Tablet: 25mg 25mg QD Take with a normal to high calorie meal No hepatic dose adjustment required NS: depressive disorders, HA, insomnia; rash, increased cholesterol, hepatotoxicity Substrate of YP3A4; contraindicated with strong YP3A inducers. Also contraindicated with proton pump inhibitors. Give histamine receptor antagonists 12h before or 4h after RPV.
Doravirine DOR (Pifeltro) Tablet: 100 mg NRTI Pair plus NNRTI o-formulations Efavirenz/ Emtricitabine/ Tablet: 600mg EFV/200mg FT/300mg TDF EFV/FT/TDF (Atripla) Efavirenz/Lamivudine/ EFV/3T/TDF (Symfi) Tablet: 600mg EFV/300mg 3T/300mg TDF Also: 400mg EFV/300mg 3T/300mg TDF (Symfi Lo) 100 mg QD Preferably empty stomach Preferably empty stomach in renal impairment; no data for ESRD or in HD hild-pugh A or B Dose No data Not recommended if rl < 50mL/min Not recommended in hild-pugh lass B or Not recommended if rl < 50mL/min Not recommended in hild-pugh lass B or N, D, HA, dizziness Substrate of YP3A4; contraindicated with strong YP 3A4 inducers (e.g. rifampin, certain anticonvulsants) N, HA, D, NS effects See EFV, FT, TDF Possibly fewer NS effects with lower (i.e. 400mg) EFV dose in Symfi Lo See EFV, 3T, TDF Rilpivirine/ Emtricitabine/ RPV/FT/TDF (omplera) Rilpivirine/ Emtricitabine/ Tenofovir AF RPV/FT/TAF (Odefsey) Tablet: 25mg RPV/200mg FT/300mg TDF Tablet: 25mg RPV/200mg FT/25mg TAF Take with a full meal Take with a full meal Not recommended if rl < 50mL/min No adjustment recommended in mildmoderate hepatic impairment; no data in severe impairment Do not give co-formulation if rl < 30mL/min No dose adjustment in hild-pugh A or B, No dosing data for hild-pugh See RPV, FT, TDF See RPV, FT/TAF See RPV, FT, TDF See RPV, TAF/FT (TAF= tenofovir alafenamide) Doravirine/ Lamivudine/ (DOR/3T/TDF) (Delstrigo) Tablet: 100 mg DOR/300 mg 3T/300 mg TDF rl < 50 ml/min not recommended A or B No data See DOR, 3T, TDF See DOR, 3T, TDF INTEGRASE STRAND TRANSFER INHIBITORS (INSTI) Raltegravir RAL (Isentress, Isentress HD) Tablet: 400mg, 600 mg (HD) *hewable tablets: 25mg, 100mg *Powder for oral suspension: 100mg packets (*These formulations are NOT bioequivalent to 400mg tablet) 400mg BID 1200 mg (2 X 600 mg HD tabs) QD No hepatic dose recommendation; no data in severe impairment N, HA, increased creatine kinase Strong inducers of UGT 1A1 (e.g. rifampin) can decrease RAL concentrations.
Dolutegravir DTG (Tivicay) Tablet: 10mg, 25mg, 50mg 50mg QD (TN or TE but INSTI-naïve) 50mg BID (INSTIexperienced or with certain UGT1A/YP3A inducers) NRTI pair + INTEGRASE STRAND TRANSFER INHIBITORS (INSTI) o-formulations Elvitegravir (EVG)/ cobicistat/tdf/ft (Stribild) Elvitegravir (EVG)/ cobicistat/taf/ft (Genvoya) (TAF= tenofovir alafenamide) Dolutegravir (DTG)/AB/3T (Triumeq) Tablet: 150mg EVG/150mg cobicistat/ 200mg FT/300mg TDF Tablet: 150mg EVG/150mg cobicistat/ 200mg FT/10mg TAF Tablet: 50mg DTG/600mg AB/300mg 3T Take with food Take with food ; caution for INSTI-experienced pts with severe renal impairment No dose adjustment for mild or moderate hepatic impairment; PK unknown for severe hepatic impairment rl 70 Dose < 70 Initial use not recommended < 50 ontinued use not recommended HD Not recommended -------------------------------------------------------- A or B Not recommended an be given in patients with rl < 15mL/min who are on hemodialysis (administer after dialysis completed on HD days). Do not give co-formulation if rl 15-30mL/min. Do not give co-formulation if rl < 15mL/min and NOT on dialysis. No dose adjustment in hild-pugh A or B Not recommended in hild-pugh DTG/AB/3T NOT recommended if rl < 50 ml/min because 3T renal dosing is not possible with co-formulation. DTG/AB/3T NOT recommended in hild- Pugh A or higher. AB dose-reduced if hild- Pugh A. HA, insomnia, increased LFTs N, HA, increased creatine kinase, renal toxicity N, D, HA See DTG, AB. 3T Must establish HLA -B*5701 status of pt (to screen for AB hypersensitivity) Strong inducers of UGT1A or YP3A can decrease DTG levels; metformin; divalent/polyvalent cations; see package insert for dose adjustments or contraindicated combinations. Strong 3A4 inducers can decrease EVG obi is a YP3A inhibitor, which EVG exposure; may exposure to other YP3A substrates ontraindicated with rifampin, lovastatin, simvastatin, sildenafil dosed as Revatio for PAH Strong 3A4 inducers can decrease EVG obi is a YP3A inhibitor, which EVG exposure; may exposure to other YP3A substrates ontraindicated with rifampin, lovastatin, simvastatin, sildenafil dosed as Revatio for PAH Strong inducers of UGT1A or YP3A can decrease DTG levels; metformin; divalent/polyvalent cations; see package insert for dose adjustments or contraindicated combinations. Bictegravir (BI)/TAF/FT (Biktarvy) Tablet: 50mg BI/200mg FT/25mg TAF Do not give co-formulation if rl < 30mL/min Not recommended in hild-pugh D, N, HA Strong inducers of UGT1A or YP3A can decrease BI levels; metformin; divalent/polyvalent cations; see package insert for dose adjustments or contraindicated combinations.
NNRTI + INSTI o-formulation Dolutegravir (DTG)/Rilpivirine (RPV) (Juluca) PROTEASE INHIBITORS (PIs) Atazanavir ATV (Reyataz) ATV/c (Evotaz) (c=cobicistat) Tablet: 50mg DTG/25 mg RPV apsules: 150mg, 200mg, 300mg (brand and generic) *Pediatric Powder: 50mg packets (*apsules and pediatric powder are NOT interchangeable) Evotaz tablet: 300mg co-formulated with cobicistat 150mg With a meal TN: 400mg QD TN or TE: 300mg QD + [RTV 100mg QD or cobi 150mg QD] or ATV/cobi one tab QD TN with EFV: 400mg + RTV 100mg No renal dose adjustment for mild-moderate renal dysfunction. Monitor for increased adverse effects if severe impairment (rl < 30) or ESRD. See DTG, RPV See DTG and RPV No dose adjustment in mild or moderate hepatic impairment; PK unknown in severe hepatic impairment hepatotoxicity, lipodystrophy, dyslipidemias, insulin resistance/ hyperglycemia No HD HD (TN) HD (TE) ATV 300mg + RTV 100mg Not recommended ---------------------------------------------------------- B 300mg QD (no RTV) Not recommended bilirubin, EKG changes (rare), kidney stones Substrate and inhibitor of liver enzymes. Boost with RTV when given with TDF. Refer to package insert when given with H-2 blockers or PPIs. Darunavir DRV (Prezista) DRV/c (Prezcobix) (c=cobicistat) DRV/c/TAF/FT (Symtuza) Lopinavir/ ritonavir LPV/r (Kaletra) Ritonavir RTV (Norvir) Tablets: 75mg, 150mg, 400mg, 600mg, 800mg Oral suspension: 100mg/mL Prezcobix tablet: 800mg co-formulated with cobicistat 150mg Symtuza tablet: 800 mg/150mg cobicistat/200mg FT/10 mg TAF Tablets: 100mg/25mg, 200mg/50mg LPV/r Oral solution (brand and generic): 80mg LPV-20mg RTV/mL apsule: 100mg (soft gelatin) Tablet: 100mg Oral solution: 80mg/mL TN or TE with no DRV mutations: 800mg + [RTV 100mg QD or cobi 150 mg QD] or DRV/cobi one tab QD TE w/ 1 DRV mutations: 600mg + RTV 100mg BID Two tablets (200/50 per tablet) BID Four tablets QD (not recommended if 3 LPV mutations) Given 100-200mg QD-BID to boost PIs ; DRV/cobi + TDF should not be administered if rl < 70 ml/min No hepatic dose recommendation; not recommended in severe hepatic impairment No hepatic dose recommendation; use with caution Follow recommendations for primary PI for hepatic dose adjustment R, N, D, HA Inhibitor of YP3A D, N, GGT D, N, V Substrate & inhibitor of liver enzymes; contains RTV (potent enzyme inhibitor) Refer to package insert for concomitant dosing with EFV, NVP, FPV, NFV. Significant drug interactions Inhibitor of YP3A and 2D6 Inducer p-glycoprotein
OTHERS (Fusion Inhibitors, R5 o-receptor Antagonists, Post-attachment Inhibitors) Maraviroc MV (Selzentry) Tablets: 150mg, 300mg Oral solution: 20mg/mL MV+strong YP3A inhibitor (except TPV): 150mg BID MV+YP3A inducer only: 600mg BID MV+NRTIs, TPV, NVP: 300mg BID When co-administered with potent inducers or inhibitors, MV NOT recommended when rl < 30mL/min or in pts on HD. See package insert for specifics. No hepatic dose recommendation R, cough, fever, musculoskeletal symptoms, hepatotoxicity MV is a substrate of liver enzymes. YP3A inhibitors (w/ or w/o inducers), PIs (except TPV/r) and DLV can increase MV YP3A inducers (w/o inhibitors) can decrease MV Ibaluzimab-uiyk (Trogarzo) Injection: 200 mg/1.33ml single-use vials; must be diluted in 0.9% sodium chloride 2000 mg IV infusion loading dose followed by 800 mg IV infusion q2 weeks No formal studies in pts with renal or hepatic insufficiency; renal impairment is not expected to affect drug PK D, N, R, dizziness No drug-drug interactions conducted; none expected based on drug mechanism of action