Generic Brand Image

PIs

Atazanavir 300mg cap Reyataz

Darunavir 400mg tab Prezista

Indinavir 400mg cap Crixivan

Fosamprenavir 700mg tab Lexiva

Lopinavir/RTV 200/50mg tab Kaletra

Nelfinavir 625mg tab Viracept

Ritonavir 100mg tab Norvir

Saquinavir 500mg tab Invirase

Tipranavir 250mg cap Ap vus

C

ombi

naon

s

EFV+FTC+TDF 600/200/300mg Atripla

3TC+AZT 150/300mg Combivir

RPV+FTC+TDF 25/200/300mg Complera

ABC+3TC 600/300mg Epzicom

EVG+Cobi+FTC+TDF 150/150/200/300mg Stribild

ABC+3TC+AZT 300/150/300mg Trizivir

FTC+TDF 200/300mg Truvada

Generic Brand Image

N

RTIs

Abacavir 300mg tab Ziagen

Emtricitabine 200mg cap Emtriva

Didanosine 400mg cap Videx-EC

Lamivudine 300mg tab Epivir

Stavudine 40mg cap Zerit

Tenofovir 300mg tab Viread

Zidovudine 300mg tab Retrovir

NN

RTIs

Delavirdine 200mg tab Rescriptor

Efavirenz 600mg tab Su va

Etravirine 200mg tab Intelence

Nevirapine 200mg tab Viramune

Rilpivirine 25mg tab Edurant

Entr

y Maraviroc 300mg tab Selzentry

INT

Elvitegravir 150mg tab

Available as combo only (See Stribild)

Raltegravir 400mg tab Isentress

Pictures obtained from: Facts and Comparisons® eAnswers

HIV ANTIRETROVIRAL REFERENCE*

Updated 06/2014

Prepared by:Velliyur Viswesh, PharmD, BCPS

Carol Schneiderman, PharmD, BCACP, AAHIVP

Stephen Klotz, MD

* Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. Department of Health and Human Services. Updated March 27, 2012; Available at: http://www.aidsinfo.nih.gov/ContentFiles/AdultandAdolescentGL.pdf.

University Campus

Dolutegravir 50mg tab

Tivicay

Generic Brand Abbr. Dose and Pill Burden How to take Crush Tab?

Open Caps?

Oral soln/ powder? Class effects Common/serious side effects Other comments Renal/Hepatic Dose Adjustment

NR

TIs

Abacavir Ziagen ABC One 300mg tab BID OR Two 300mg tabs QD With/without food ND Yes

Lactic acidosis (esp. d4T, AZT, ddI), hepatomegaly w/ steatosis N/V (ddI, AZT > others)

Hypersensitivity reactions, ↑LDL, ↑TG, MI? HLA-B*5701 test prior to use Hepatic dose adjustment if Child-Pugh ≥ 5

Emtricitabine Emtriva FTC One 200mg cap QD With/without food ND Yes Minimal toxicity, skin discoloration, hyperpigmentation Indicated for HBV coinfection Dose adjustment if CrCl < 50

Didanosine Videx-EC ddI One 400mg cap QD (1) Take on empty stomach No Yes Pancreatitis, peripheral neuropathy, optic neuritis, DM,

portal HTN, SJS Contraindicated with allopurinol or ribavirin Dose adjustment if CrCl < 60

Lamivudine Epivir 3TC One 150mg tab BID OR One 300mg tab QD With/without food ND Yes Minimal toxicity, HA, nausea, diarrhea, pancreatitis Indicated for HBV coinfection and perinatal

use Dose adjustment if CrCl < 50

Stavudine Zerit d4T One 40mg cap BID (1) With/without food ND Yes Peripheral neuropathy, lipoatrophy, pancreatitis, progressive neuromuscular weakness (resembling GBS), DM, ↑LDL, ↑TG

Discontinue therapy if severe neuromuscular weakness arises (with or without lactic acidosis)

Dose adjustment if CrCl < 50

Tenofovir Viread TDF One 300mg tab QD With/without food Yes Yes Nephrotoxicity (Fanconi syndrome), ↓BMD, asthenia, HA, diarrhea Indicated for HBV coinfection Dose adjustment if CrCl < 50

Zidovudine Retrovir AZT, ZDV One 300mg tab BID With/without food ND ND Yes Bone marrow suppression, anemia, HA, nail

pigmentation, myopathy,↑LDL, ↑TG, DM, lipoatrophy Indicated for perinatal use Dose adjustment if CrCl < 15

NN

RTI

s

Delavirdine Rescriptor DLV Two 200mg tabs TID With/without food Yes No

Rash and SJS (NVP > DLV > ETR > EFV/ RPV), ↓BMD (with NRTI, PI coadmin), hepatic issues, many drug interactions

↑transaminases, N/V, HA Separate from antacids by 1hr, contraindicated w/ alprazolam, midazolam No adjustment

Efavirenz Sustiva EFV One 600mg tab QHS Take on empty stomach No Yes -

200mg Yes (2) Somnolence, insomnia, depression, psychosis, ↑LDL, ↑TG, abnormal dreams, lipodystrophy, ↑transaminases Contraindicated with pregnancy Limited data with hepatic

impairment (use with caution)

Etravirine Intelence ETR One 200mg tab BID Following a meal Yes No Hypersensitivity reactions with hepatic failure, N/V Rash and SJS has been reported No adjustment

Nevirapine Viramune NVP One 200mg tab BID (3) With/without food No Yes Rash/SJS, symptomatic hepatitis incl. fatal hepatic necrosis reported

Contraindicated if pre-NVP CD4 > 400 in men and > 250 in women

Contraindicated if Child-Pugh class B/C, dose after dialysis

Rilpivirine Edurant RPV One 25mg tab QD Take with meals (high fat) ND No Depression, insomnia, HA, ↑transaminases, ↑LDL,

↑TG Contraindicated with PPIs or CYP3A inducers (carbamazepine, phenytoin, rifampin)

Renal: No adjustment Hepatic: No data

PIs

Atazanavir Reyataz ATV Two 200mg caps QD OR One 300mg caps QD + One RTV 100mg tab QD (4)

Take with meals Yes No

Lipodystrophy, ↑glucose (except ATV/r), ↑LDL, ↑TG, diarrhea, N/V, ↑bleeding, hepatotoxicity, use with caution w/ statins due to increased risk of rhabdo (simvastatin contraindicated), many drug interactions, MI?

Less GI intolerance and effect on TGs than other PIs, ↑Tbili, PR prolongation, skin rash, nephrolithiasis, SJS

PPIs contraindicated in ARV-experienced patients. Adjustments needed with PPIs, H2RA, and antacids

Not recommended with severe hepatic insuff. or with dialysis in ARV-experienced patients

Darunavir Prezista DRV Two 400mg tabs QD + One RTV 100mg tab QD (5) Take with meals Yes No Less GI intolerance and effects on TGs than

other PIs, HA, skin rash, SJS Caution w/ sulfa allergy Do not use with severe hepatic impairment

Indinavir Crixivan IDV Two 400mg caps BID + Two RTV 100mg tabs BID With/without food ND No Nephrolithiasis, ↑Tbili, HA, blurred vision, dizziness,

thrombocytopenia, alopecia, hemolytic anemia Should be taken 1hr before or 2hrs after meals if administered without RTV-boosting

Mild/moderate hepatic impairment: Use 600mg Q8h without RTV

Fosamprenavir Lexiva FPV Two 700mg tabs BID OR Two 700mg tabs QD + 1-2 RTV 100mg tabs QD (6)

With food if RTV boosted ND Yes Diarrhea, HA, skin rash, nephrolithiasis, SJS (Caution w/ sulfa allergy? Possible based on

molecular structure but has not been reported) Hepatic dose adjustment if Child-Pugh ≥ 5

Lopinavir/ ritonavir Kaletra LPV/r Two 200/50mg tabs BID OR

Four 200/50mg tabs QD (7) With/without food Yes Yes PR prolongation, pancreatitis, GI intolerance, asthenia, QT prolongation/torsades reported, SJS Indicated for perinatal use (BID dosing only) Use caution in hepatic impairment.

Avoid QD dosing in HD

Nelfinavir Viracept NFV Two 625mg tabs BID OR Three 250mg tabs TID Take with meals Yes Yes Diarrhea common Not recommended as part of an initial ARV

regimen. Not recommended if Child-Pugh class B/C

Ritonavir Norvir RTV Only used as PI-booster, refer to other PIs for dosing Take with meals Yes No Yes GI intolerance, paresthesias, hepatitis,

asthenia, altered taste Use is contraindicated with flecainide and propafenone Limited data

Saquinavir Invirase SQV Two 500mg tabs BID + One RTV 100mg tab BID Take with meals ND No QT/PR prolongation, GI intolerance, asthenia,

torsades reported Contraindicated w/ prolonged QT (>450msec) or drugs that prolong QT, AV block

Use w/ caution in hepatic impairment. Do not use if severe.

Tipranavir Aptivus TPV Two 250mg tabs BID + Two RTV 100mg tabs BID Take with meals ND Yes Intracranial hemorrhages reported, higher frequency of

hepatitis than other PIs. Caution w/ sulfa allergy, use capsules within 60 days of opening bottle, refrigerate caps.

Contraindicated if Child-Pugh class B/C

INT-

inh

Elvitegravir - EVG Available as combo only (See Stribild) Take with meals ND No

Nausea, diarrhea, headache, ↑transaminases, rash Metabolized by CYP3A4, always check for

potential drug interactions No data (FTC/TDF components of Stribild require dose adjustments)

Raltegravir Isentress RAL One 400mg tab BID With/without food Yes No Lipodystrophy, ↑CPK, muscle weakness, rhabdomyolysis, nausea, HA, diarrhea, pyrexia

Use two 400mg tabs BID when used in combination with rifampin

No data in severe hepatic impairment

(1) Dosing varies if patient is < 60kg (or when ddI is administered with TDF)

Entr

y-in

h Enfuvirtide Fuzeon T20 90mg SubQ BID

Injection site reactions (100% incidence), increased risk of bacterial pneumonia, hypersensitivity reactions

Store at room temp. Reconstituted solution should be refrigerated and used w/in 24hrs.

Limited data but no dosage adjustment required

Maraviroc Selzentry MVC One 300mg tab BID. Dose depends on other medications taken (8)

With/without food ND No Rash, abdominal pain, cough, dizziness, pyrexia, musculoskeletal symptoms, URIs, hepatotoxicity, orthostatic hypotension

CCR5-tropism test must be performed prior to use

Dose adjustment if CrCl < 30 Use with caution in moderate-severe hepatic impairment

Com

bos

Atripla Efavirenz 600mg + Emtricitabine 200mg + Tenofovir 300mg One tablet QD, take on an empty stomach, preferably at bedtime, DO NOT crush tablets (not bioequivalent) Combivir Lamivudine 150mg + Zidovudine 300mg One tablet BID, take with or without food Complera Rilpivirine 25mg + Emtricitabine 200mg + Tenofovir 300mg One tablet QD, take with food (preferably high fat), DO NOT crush tablets (rilpivirine insoluble in water) Epzicom Abacavir 600mg + Lamivudine 300mg One tablet QD, take with or without food Stribild Elvitegravir 150mg + Cobicistat 150mg + Emtricitabine 200mg + Tenofovir 300mg One tablet QD, take with food Trizivir Abacavir 300mg + Lamivudine 150mg + Zidovudine 300mg One tablet BID, take with or without food Truvada Emtricitabine 200mg + Tenofovir 300mg One tablet QD, take with or without food, tablets may be crushed

(2) Liquid formulation available through Pediatric Oral Liquid Expanded Access Program for HIV-infected children and adolescents ages 3-16 years (call 1-877-372-7097) (3) Therapy should be initiated with 200mg QD for 14 days (lead-in period) to observe for rash, lead-in period may be continued (not > 28days) until resolution of mild-moderate rash without constitutional symptoms. Repeat lead-in period if therapy discontinued for > 7days, (4) Use RTV-boosted regimen for patients that are treatment-experienced or on TDF. In combination with EFV in ARV-naive patients, use two 200mg caps QD + one RTV 100mg tab QD. Medication adjustments necessary when used with H2RA, PPIs, and antacids (5) Once-daily dosing may be used in both treatment naïve and experienced patients but if at least one DRV mutation is present or suspected, use twice daily dosing of one 600mg tab BID + one RTV 100mg tab BID (6) For PI-experienced patients, use one 700mg tab BID + one RTV 100mg tab BID. In combination with EFV, use dosing as with PI-experienced or use two 700mg tabs QD + three RTV 100mg tabs QD (7) Once daily dosing not recommended for patients with ≥ 3 LPV-associated mutations, pregnant women, or patients on EFV, NVP, FPV, NFV, carbamazepine, phenytoin or phenobarbital. When admi nistered with EFV or NVP, use two 200/50mg tabs and one 100/25mg tab (total 500/125mg) BID (8) Use one 150mg tab BID when given with CYP3A inhibitors (PIs excluding TPV/r, DLV, azoles, clarithromycin, nefazodone). Use two 300mg tabs BID when given with CYP3A inducers (EFV, ETR, rifampin, carbamazepine, phenobarbi tal, phenytoin). Abbreviations: BMD- bone mineral density, DM- diabetes, ESRD- end-stage renal disease, GBS- Guillan-Barre syndrome, GI- gastrointestinal, H2RA- histamine2 receptor antagonist, HA- headache, HD- hemodialysis, HBV- hepatitis B virus, MI- myocardial infarction, ND- no data available, N/V- nausea/vomiting, Rhabdo – rhabdomyolysis, SJS- Steven's Johnson syndrome, Tbili- total bilirubin, TG- triglycerides, URI- upper respiratory infection

Dolutegravir Tivicay DTG One 50mg tab daily With/without food ND No HA, hyperglycemia, increase lipase, Increase LFT’sincrease CPK

INT-inh but coadministered with efavirennz, fosamprenavir/ ritonavir, rifampin then dose at 50mg bid

Limited data, no dosage recommendations. Severe hepatic impairment not recommended