HIV Antiretroviral (ARV) Medications (Bolded Medications Are on MMC

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HIV Antiretroviral (ARV) Medications (Bolded medications are on MMC Formulary) Individual Medications By Generic Name (Brand, Abbreviation) Combination Medications by Brand Name (Generic) Nucleos(t)ide Non-Nucleoside Pharmaco- Integrase Entry & Single Tablet Regimen Fixed Dose Reverse Reverse Protease Inhibitors kinetic Strand Transfer Attachment (complete regimen in one Combination Transcriptase Transcriptase (PIs) Enhancers Inhibitors Inhibitors tablet for most patients) (partial regimen) Inhibitors (NRTIs) Inhibitors (NNRTIs) “Boosters” (INSTIs) Atripla Abacavir Delavirdine Atazanavir Cobicistat Bictegravir Enfuvirtide Cimduo (Efavirenz/TDF/ (Ziagen, ABC) (Rescriptor, DLV) (Reyataz, ATV) (Tybost, c) (BIC) (Fuzeon, T20) (Lamivudine/TDF) Emtricitabine) Atazanavir/ Biktarvy Combivir Didanosine Doravirine Ritonavir Dolutegravir Ibalizumab-uiyk Cobicistat (Bictegravir/TAF/ (Lamivudine/ (Videx, ddl) (Pifeltro, DOR) (Norvir, r) (Tivicay, DTG) (Trogarzo, IBA) (Evotaz, ATV/c) Emtricitabine) Zidovudine) Maraviroc Complera Emtricitabine Efavirenz Darunavir Elvitegravir Descovy (Selzentry, (Rilpivirine/TDF/ (Emtriva, FTC) (Sustiva, EFV) (Prezista, DRV) (EVG) (TAF/Emtricitabine) MVC) Emtricitabine) Darunavir/ Raltegravir Lamivudine Etravirine Fostemsavir Delstrigo Epzicom Cobisistat (Isentress, (Epivir, 3TC) (Intelence, ETR) (Rukobia, FTR) (Doravirine/TDF/Lamivudine) (Abacavir/Lamivudine) (Prezcobix, DRV/c) RAL) Trizivir Stavudine Nevirapine Fosamprenavir Cabotegravir Dovato (Abacavir/Lamivudine/ (Viramune, NVP) (Lexiva, FPV) (Vocabria, CAB) (Dolutegravir/Lamivudine) (Zerit, d4T) Zidovudine) Tenofovir Genvoya Rilpivirine Indinavir Truvada alafenamide (Elvitegravir/Cobicistat/TAF/ (Edurant, RPV) (Crixivan, IDV) (TDF/Emtricitabine) (Vemlidy, TAF) Emtricitabine) Tenofovir Lopinavir/ Juluca disoproxil fumarate Ritonavir (Dolutegravir/Rilpivirine) (Viread, TDF) (Kaletra, LPV/r) Zidovudine Odefsey Nelfinavir (Retrovir, ZDV or (Rilpivirine/TAF/ (Viracept, NFV) AZT) Emtricitabine) Stribild Saquinavir (Elvitegravir/Cobicistat/ (Invirase, SQV) TDF/Emtricitabine) Tipranavir Symfi & Symfi Lo

(Aptivus, TPV) (Efavirenz/Lamivudine/TDF) Symtuza (Darunavir/Cobicistat/ All patients living with HIV should start treatment as soon as possible, if willing and able TAF/Emtricitabine)

Preferred treatment: 2 NRTIs + [1 INSTI* or 1 PI* or 1 NNRTI (INSTI > PI > NNRTI)] Cabenuva *A pharmacokinetic enhancer (“booster”) is generally used with the PIs and elvitegravir as a 4th medication (Cabotegravir/Rilpivirine intramuscular) Monitor CD4 count and viral load → Goals: CD4 >200 (14%) and undetectable viral load

Prophylaxis for low CD4 counts: <200: Bactrim DS or SS 1 tab PO daily – covers PJP and toxoplasmosis <50 and not receiving ARV treatment: Azithromycin 1200 mg PO once a week – covers MAC

Montefiore Formulary ARVs 1. Drug Interactions Adult Dose & Food Renal Dosing based on Crushable and/or Drug 2. Adverse Events Considerations CrCl (mL/min) Liquid Available? 3. Clinical Pearls Nucleos(t)ide Reverse Transcriptase Inhibitors (NRTIs) Class Adverse Events: lactic acidosis, hepatic steatosis, pancreatitis, myopathy, peripheral neuropathy, lipoatrophy (ddl, d4T, ZDV >> ABC, FTC, 3TC, TAF, TDF) 1. No significant drug interactions

Yes, mix with water 2. Possible increased risk of MI, hepatotoxicity (Child-Pugh A: use 600 mg q24h Abacavir or food 200 mg q12h, avoid use if severe hepatic impairment) or None (Ziagen, ABC) or use oral soln 20 3. Must be HLA-B*5701 negative to initiate. Rare but severe, 300 mg q12h mg/ml possibly fatal hypersensitivity (nausea, vomiting, diarrhea, fever, rash, malaise, myalgia), rechallenge is NOT recommended 30-49: 200 mg q48h (cap) 120 mg q24h (oral soln) 1. Do not take with 3TC Capsule: 200 mg Yes, open up caps 15-29: 200 mg q72h (cap) 2. Hyperpigmentation of palms and soles, generally mild. Emtricitabine q24h and mix with water 80 mg q24h (oral soln) 3. Cross resistance with 3TC especially if M184V mutation present. (Emtriva, FTC) Oral soln: 240 mg or use oral soln 10 Active against Hepatitis B virus (HBV) – avoid abrupt q24h < 15: 200 mg q96h (cap) mg/ml 60 mg q24h (oral soln) discontinuation due to risk of severe HBV exacerbation HD: 200mg q24h (cap or soln) 30-49: 150 mg q24h 1. Do not take with FTC 2. Cross resistance with FTC especially if M184V mutation present. 300 mg q24h 15-29: 150 mg q24h x 1, Yes, mix with water Lamivudine Active against HBV – avoid abrupt discontinuation due to risk of or then 100 mg q24h or use oral soln 10 (Epivir, 3TC) severe HBV exacerbation 150 mg q12h mg/ml <15 or HD: 100 mg q24h 3. To avoid using the liquid formulation since tablet can be crushed 1. Avoid adefovir, carbamazepine, fosphenytoin, phenytoin, oxcarbazepine, phenobarbital, rifampin/rifamycins, TDF Tenofovir alafenamide < 15 and not on HD: avoid use No data, but bitter, 2. Minimal renal and bone toxicities compared to TDF 25 mg q24h (Vemlidy, TAF) HD: 25 mg q24h burnt taste 3. TAF is under investigation for pre-exposure prophylaxis (PrEP). Active against HBV – avoid abrupt discontinuation due to risk of severe HBV exacerbation Yes for tabs only, 1. Avoid adefovir, TAF and other nephrotoxic agents Tenofovir disoproxil 30-49: 300 mg q48h mix with water. Do 2. Nephrotoxicity and decreased bone density with chronic use. fumarate 300 mg q24h 10-29: 300 mg q72-96h not mix powder 3. TDF is associated with lower lipid levels than ABC or TAF. (Viread, TDF) HD: 300 mg once weekly formulation with Active against HBV – avoid abrupt discontinuation due to risk of water. severe HBV exacerbation Yes, mix with water 1. Monitor for hematologic toxicities with methadone, atovaquone, Zidovudine or food ribavirin (Retrovir, ZDV or 300 mg q12h < 15 or HD: 300 mg q24h or use oral soln 10 2. Anemia and neutropenia (but not thrombocytopenia), malaise AZT) mg/ml 3. IV formulation is only for intrapartum or postpartum prophylaxis

interruption > 7 days: 1. Use of rifampin is contraindicated. Dose adjustment with Nevirapine 200 mg q24h x 14 Yes, or use rifabutin is unnecessary but use with caution (Viramune, NVP) days, then 200 mg oral soln 10 mg/ml 2. Severe rash and hepatotoxicity, especially in first 18 weeks q12h 3. Do not initiate if pre-treatment CD4 > 250 in women or > 400 in Chronic: 200 mg q12h men due to increased hepatotoxicity 1. Needs acidic environment for absorption – avoid PPIs, use H RAs and antacids with caution. Rifampin is contraindicated. Yes, crush and mix 2 Rilpivirine 25 mg q24h With rifabutin, increase RPV to 50 mg q24h with semisolid food (Edurant, RPV) Take with food 2. Depression, suicidal ideation, hyperlipidemia or liquid 3. Do not initiate if pre-treatment CD4 <200 and/or HIV RNA >100,000

Montefiore Formulary ARVs 1. Drug Interactions Adult Dose & Food Renal Dosing based on Crushable and/or Drug 2. Adverse Events Considerations CrCl (mL/min) Liquid Available? 3. Clinical Pearls Protease Inhibitors (PIs) Class Drug Interactions: Significant risk of drug interactions including azole antifungals, antiarrhythmics, anticoagulants, anticonvulsants, HCV drugs, methadone, midazolam, rifampin/rifamycins (rifampin is contraindicated with all PIs, use rifabutin 150mg daily instead), QTc prolonging agents, sildenafil, statins, inhaled and oral steroids (e.g. fluticasone) Class Adverse Events: Significant metabolic changes; hyperlipidemia, hyperglycemia, lipodystrophy, hepatotoxicity, GI intolerance (ATV, DRV < Other PIs) Class Resistance Characteristics: high barrier to resistance 300 mg q24h 1. Acidic environment needed for absorption – avoid PPIs, give (400 mg q24h if HD & treatment-naïve only: 2 hrs before or 10 hrs after H RAs, use antacids with caution Atazanavir Yes, open caps and 2 given unboosted or if 300 mg plus 100 mg ritonavir 2. Hyperbilirubinemia, cholelithiasis, nephrolithiasis (Reyataz, ATV) mix with food pregnant) once daily- 3. Least CVD risk of the PIs. Usually boosted with concurrent Take with food ritonavir or cobicistat Atazanavir/Cobicistat 1 tablet q24h < 70: do not initiate as part of No See atazanavir and cobicistat notes (Evotaz, ATV/c) Take with food TDF-based regimen 1. See class drug interactions 800 mg q24h Yes, mix with water Darunavir 2. See class adverse events or 600 mg q12h None or use oral soln (Prezista, DRV) 3. Contains sulfonamide moiety, caution with sulfa allergy. Always Take with food 100mg/ml boosted with concurrent ritonavir or cobicistat Darunavir/Cobicistat 1 tablet q24h < 70: do not initiate as part of Yes See darunavir and cobicistat notes (Prezcobix, DRV/c) Take with food TDF-based regimen 2 tablets q12h 1. See class drug interactions and ritonavir notes; see package insert Lopinavir/Ritonavir or 4 tablets q24h Yes, use oral soln for dose if taking with carbamazepine, efavirenz, or phenytoin None (Kaletra, LPV/r) Take oral soln with 400/100mg/5ml 2. Diarrhea, possible increased risk of MI food 3. Oral solution is 42% ethanol per volume Pharmacokinetic Enhancers (“Boosters”) Class Drug Interactions: Many: azole antifungals, antiarrhythmics, anticoagulants, anticonvulsants, HCV drugs, methadone, midazolam, rifampin/rifamycins, QTc prolonging agents, sildenafil, statins, inhaled and oral steroids (e.g. fluticasone)

< 70: do not initiate as part of 1. See class drug interactions Cobicistat 2. Increase in SCr (typically <0.2 mg/dL) due to decreased 150 mg q24h TDF-based regimen No (Tybost, c) creatinine secretion (no impact on GFR) < 50: discontinue use 3. Always use in combination with ATV, DRV or EVG 1. See class drug interactions 2. Hepatotoxicity, taste perversion with horrible-tasting oral Ritonavir 100-200 mg q12h or None No, use oral soln solution (chocolate milk, peanut butter, sweet liquids can help) (Norvir, r) q24h 3. Always use in combination with PIs. Oral solution is 43% ethanol per volume, 27% propylene glycol per volume

Montefiore Formulary ARVs 1. Drug Interactions Adult Dose & Food Renal Dosing based on Crushable and/or Drug 2. Adverse Events Considerations CrCl (mL/min) Liquid Available? 3. Clinical Pearls Integrase Strand Transfer Inhibitors (INSTIs) Class Drug Interactions: cation-containing antacids or laxatives, iron or calcium containing oral supplements, buffered medications, carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin/rifamycins Class Adverse Events: insomnia, increase in SCr (usually <0.2 mg/dL) from decreasing creatinine secretion (no impact on GFR), depression, weight gain 1. With rifampin, increase DTG to 50 mg q12h (no adjustment 50 mg q24h needed with rifabutin or weekly rifapentine). Maximum dose of Dolutegravir (50 mg q12h in Yes, mix with water None metformin is 850 mg BID when given with DTG. (Tivicay, DTG) INSTI- experienced or food 2. Potential teratogenicity (neural tube defects) patients) 3. High genetic barrier to resistance IR tab: 400 mg q12h 1. With rifampin, increase RAL to 800 mg q12h (no RAL dose or 1200 mg q24h adjustment needed with rifabutin) Raltegravir HD: no adjustment, on dialysis Yes, mix with water 2. Myopathy, rhabdomyolysis (Isentress, RAL) days give after HD or use chewable tab Chew tab: 300 mg 3. Bioavailability is not equivalent among IR tablet and chewable q12h tablet, therefore, dosage formulations are NOT interchangeable Note: Bictegravir and elvitegravir are INSTIs that are only available as part of combination medications. They do not have individualized dosing, safety, or efficacy data as they were studied and approved only as part of combination medications. Entry Inhibitors & Others

1. Standard dose is 300 mg PO q12h. Use 150 mg q12h if taking < 30 and strong CYP3A4 with strong CYP3A inhibitors (e.g. itraconazole, clarithromycin, inhibitors or inducers: avoid Drug interactions most PIs). Use 600 mg q12h if taking with strong CYP3A4 Maraviroc use determine dose Yes, mix with water inducers (without a strong CYP3A4 inhibitor) (e.g. efavirenz, (Selzentry, MVC) 150-600 mg q12h < 30 with other medications etravirine, rifampin, carbamazepine, and phenytoin) and postural hypotension: 150 2. Rash, hepatotoxicity, CNS disturbances, postural hypotension mg q12h 3. Requires positive tropism test for CCR5 virus before use

Montefiore Formulary ARVs Refer to individual medication details. See below for select: Adult Dose & Food Renal Dosing based on Crushable and/or 1. Drug Interactions Drug Considerations CrCl (mL/min) Liquid Available? 2. Adverse Events 3. Clinical Pearls Combination Medications-Single Tablet Regimen 1 tablet q24h at < 50: Give EFV, TDF, FTC Atripla bedtime No, separate out separately. Please see renal 1. Avoid in patients with psychiatric comorbidities (see EFV). (EFV/TDF/FTC) Take on empty components dosing for TDF and FTC stomach Biktarvy 1 tablet q24h < 30: avoid use No data 1. Avoid all rifamycins (BIC/TAF/FTC) 1. Avoid in patients with psychiatric comorbidities (see RPV). < 50: Give RPV, TDF, FTC 2. Needs acidic environment for absorption – avoid PPIs, use Complera 1 tablet q24h No, separate out separately. Please see renal H2RAs and antacids with caution. (RPV/TDF/FTC) Take with food components dosing for TDF and FTC 3. Do not initiate if pre-treatment CD4 <200 and/or HIV RNA >100,000 < 30: not recommended Genvoya 1 tablet q24h HD: no adjustment, on dialysis No 1. Contains cobicistat, so many drug interactions (EVG/c/TAF/FTC) days give after HD < 30: Give RPV, TAF, FTC 1. Avoid in patients with psychiatric comorbidities (see RPV). separately. Please see renal 2. Needs acidic environment for absorption – avoid PPIs, use Odefsey No, separate out 1 tablet q24h dosing for TAF and FTC H2RAs and antacids with caution. (RPV/TAF/FTC) components HD: no adjustment, on dialysis 3. Do not initiate if pre-treatment CD4 <200 and/or HIV RNA days give after HD >100,000 Stribild < 70: do not initiate Yes, mix with water 1 tablet q24h 1. Contains cobicistat, so many drug interactions (EVG/c/TDF/FTC) < 50: discontinue use or food < 30: Give DTG, ABC, 3TC Triumeq Yes, mix with water 1. Must be HLA*B-5701 negative to initiate 1 tablet q24h separately. Please see renal (DTG/ABC/3TC) or food dosing for 3TC Combination Medication-Fixed Dose Combination < 30: Give TAF and FTC separately. Please see renal No data, only Descovy 1. TAF is approved by FDA for HIV PrEP in MSM and 1 tablet q24h dosing for TAF and FTC anecdotal (TAF/FTC) transgender women. HD: no adjustment, on dialysis experience days give after HD 30-49: 1 tablet q48h Truvada < 30: Give TDF and FTC 1. Preferred regimen for HIV PrEP: CrCl > 60 ml/min: no dosage 1 tablet q24h Yes, mix with water (TDF/FTC) separately. Please see renal adjustment needed, CrCl <60 ml/min: not recommended. dosing for TDF and FTC

Pre-Exposure Prophylaxis (PrEP) Post-Exposure Prophylaxis (PEP)

All patients must be tested and documented as HIV negative first Preferred regimen: Truvada 1 tablet PO daily PLUS Preferred regimen: Truvada (TDF/Emtricitabine) 1 tablet PO once daily Alternative regimen: Descovy (TAF/Emtricitabine) 1 tablet PO once daily • Preferred, except if potential for or early pregnancy (see important pregnancy warning below): Dolutegravir 50 mg tablet 1 tablet PO daily Provide a maximum of 90 tablets per refill (or per provider’s assessment) OR To encourage timely follow-up at least every 3 months • Alternative: Raltegravir 400mg tablet PO q12h, or non-formulary Raltegravir XR (Isentress HD) 1200 mg PO once daily Monitoring: • Signs and symptoms of acute HIV infection Pregnancy Warning – Dolutegravir is contraindicated in women of childbearing • Side effects, adherence, acquisition risk behaviors potential under any of the following circumstances: 1) attempting to conceive; 2) not on effective contraception; or 3) pregnant and under 14 weeks since their last • Repeat pregnancy testing if at risk menstrual period. • Consider STI and hepatitis C testing if symptomatic or high risk • CrCl (<60 mL/min: use is not preferred for this indication) Renal adjustment for Truvada: • Need for continued use of PrEP CrCl >50 mL/min: 1 tablet daily CrCl 30-49 mL/min: 1 tablet q48h PrEP can take 1-3 weeks to achieve sufficient protective levels against HIV, Preventing HIV Perinatal Transmission Important OnlineCrCl HIV< 30 TreatmentmL/min: use and is not Management preferred References

Viralplease suppression discuss detailsof mother with during HIV carepregnancy provider. is critical Total duration: 28 days Intrapartum prophylaxis: Pregnant Women 1. US Department of Health and Human Services AIDSinfo Guidelines Zidovudine - given if HIV RNA >1,000 copies/mL or unknown at delivery • Begin 3 hours before scheduled delivery 2. The University of Liverpool HIV Drug Interactions Checker • Load with 2 mg/kg IV over 1 hour, then 1 mg/kg/hr until delivery complete 3. POZ HIV Drug Chart Postpartum prophylaxis: Neonates Updated annually, colored pictures of all available HIV medications Zidovudine – given to all HIV exposed neonates based on gestational age. Start as soon as possible and continue for 4-6 weeks per OB/GYN and neonatology 4. American Association for the Study of Liver Diseases Practice Guidelines • ≥ 35 weeks: 4 mg/kg/dose PO or 3 mg/kg/dose IV q12h Guidelines and considerations for co-infections and drug interactions in the setting of HIV and HBV, HCV, and liver transplantation • ≥ 30 to <35 weeks: 2 mg/kg/dose PO or 1.5 mg/kg/dose IV q12h o Increase to 3 mg/kg/dose PO or 2.3 mg/kg/dose IV q12h at age 15 days 5. CDC STD Treatment Guidelines

• < 30 weeks: 2 mg/kg/dose PO or 1.5 mg/ kg/dose IV q12h o Increase to 3 mg/kg/dose PO or 2.3 mg/kg/dose IV q12h at age 28 days 6. Stanford University HIV Drug Resistance Database

Nevirapine – only given if the mother was indicated to receive intrapartum zidovudine as 7. Toronto General Hospital Oral Antiretroviral Administration: Information on described above Crushing and Liquid Formulations • 3 doses in total, based on birth weight – ≤ 2 kg: 8 mg or > 2 kg: 12 mg st o 1 dose: within 48 hours after birth, but ideally as soon as possible Prepared by Yi Guo, PharmD, BCIDP; Hongkai (Jack) Bao, PharmD, BCIDP nd st o 2 dose: 48 hours after 1 dose o 3rd dose: 96 hours after 2nd dose June 2021