January 10, 2011

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents Page 41 

Appendix B, Table 2. Characteristics of Non-Nucleoside Reverse Transcriptase Inhibitors 

 (NNRTIs) (Updated January 10, 2011)

Generic Name 

(abbreviation)/ 

Trade Name

Formulations

Dosing Recommendations

(For dosage adjustment in 

renal or hepatic 

insufficiency, see 

Appendix B, Table 7.)

Elimination Serum 

Half-life

Adverse Events

(Also see Table 13) 

Delavirdine

(DLV)/

Rescriptor

100-, 200-mg 

tablets

400 mg TID (Four 100-mg 

tablets can be dispersed in 

>3 oz. of water to produce a 

slurry; 200-mg tablets 

should be taken as intact 

tablets.)

Take without regard to 

meals

Separate dose from antacids 

by 1 hour

CYP3A4 substrate and 

inhibitor; 51% excreted 

in urine (<5% 

unchanged) and 44% in 

feces

5.8 hrs • Rash*

• Increased transaminase levels

• Nausea, headache

Efavirenz 

(EFV)/

Sustiva

Also available 

as:

• 50-, 200-mg 

capsules

• 600-mg 

tablets

600 mg once daily at or 

before bedtime

Take on an empty stomach 

to reduce side effects

Metabolized by CYPs 

2B6 and 3A4

CYP3A4 mixed inducer/ 

inhibitor (more an 

inducer than an inhibitor)

40–55 hrs • Rash*

• Neuropsychiatric symptoms†

• Increased transaminase levels

• Hyperlipidemia

• False-positive results reported with some 

cannabinoid and benzodiazepine screening 

assays

• Teratogenic in nonhuman primates and 

potentially teratogenic in humans

Atripla

EFV 

with FTC + 

TDF

Atripla

EFV 600 mg + 

FTC 200 mg + 

TDF 300 mg

Atripla

1 tablet once daily at or 

before bedtime 

Etravirine 

(ETR)/ 

Intelence

• 100-mg 

tablets

• 200-mg 

tablets

200 mg BID

Take following a meal

CYP3A4, 2C9, and 2C19 

substrate

3A4 inducer; 2C9 and 

2C19 inhibitor

41 +/– 20 hrs • Rash, including Stevens-Johnson syndrome*

• Hypersensitivity reactions (HSRs) have been 

reported, characterized by rash, 

constitutional findings, and sometimes organ 

dysfunction, including hepatic failure

• Nausea

Nevirapine

(NVP)/

Viramune

• 200-mg 

tablets

• 50-mg/5-mL 

oral 

suspension

200 mg once daily for 14 

days (lead-in period); 

thereafter, 200 mg BID

Take without regard to 

meals

Repeat lead-in period if 

therapy is discontinued for 

>7 days

In patients who develop 

mild to moderate rash 

without constitutional 

symptoms, continue lead-in 

period until rash resolves 

but no longer than 28 days 

total.

CYP450 substrate, 

inducer of 3A4 and 2B6; 

80% excreted in urine 

(glucuronidated 

metabolites, <5% 

unchanged); 10% in feces

25–30 hrs • Rash, including Stevens-Johnson syndrome*

• Symptomatic hepatitis, including fatal 

hepatic necrosis, has been reported‡

* During clinical trials, NNRTI was discontinued because of rash among 7% of NVP-treated, 4.3% of DLV-treated, 1.7% of EFV-treated, and 2% of ETR-treated 

patients. Rare cases of Stevens-Johnson syndrome have been reported with all NNRTIs; the highest incidence was seen with NVP.

† Adverse events can include dizziness, somnolence, insomnia, abnormal dreams, confusion, abnormal thinking, impaired concentration, amnesia, agitation, 

depersonalization, hallucinations, and euphoria. Approximately 50% of patients receiving EFV may experience any of these symptoms. Symptoms usually 

subside spontaneously after 2–4 weeks, but may necessitate discontinuation of EFV in a small percentage of patients.

‡ Symptomatic, sometimes serious, and even fatal hepatic events (accompanied by rash in approximately 50% of cases) occur at significantly higher frequency in 

ARV-naïve female patients with pre-NVP CD4 counts >250 cells/mm3 or in ARV-naïve male patients with pre-NVP CD4 counts >400 cells/mm3

. NVP should 

not be initiated in these patients unless the benefit clearly outweighs the risk. This toxicity has not been observed when NVP is given as single doses to mothers or 

infants for prevention of mother-to-child transmission of HIV.
January 10, 2011

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents Page 42 

Appendix B, Table 3. Characteristics of Protease Inhibitors (PIs) (Updated January 10, 2011)

Page 1of 3

Generic Name 

(abbreviation)/ 

Trade Name

Formulations

Dosing Recommendations

(For dosage adjustment 

in hepatic insufficiency, 

see Appendix B, Table 7)

Elimination Serum 

Half-life Storage Adverse Events

(Also see Table 13)

Atazanavir 

(ATV)/

Reyataz

100-, 150-, 

200-, 300-mg 

capsules

ARV-naïve patients:

400 mg once daily or (ATV 

300 mg + RTV 100 mg) 

once daily

With TDF or for ARVexperienced patients:

(ATV 300 mg + RTV 100 

mg) once daily

With EFV in ARV-naïve 

patients:

(ATV 400 mg + RTV 100 

mg) once daily

(For dosing 

recommendations with H2

antagonists and proton 

pump inhibitor (PPIs), 

refer to Table 16a)

Take with food

CYP3A4 

inhibitor and 

substrate

Dosage 

adjustment in 

hepatic 

insufficiency 

recommended 

(See Appendix

B, Table 7.)

7 hrs Room 

temperature

(up to 25oC or 

77oF)

• Indirect hyperbilirubinemia

• PR interval prolongation: First degree 

symptomatic atrioventricular (AV) block 

reported. Use with caution in patients with 

underlying conduction defects or on concomitant 

medications that can cause PR prolongation.

• Hyperglycemia

• Fat maldistribution

• Possible increased bleeding episodes in patients 

with hemophilia

• Nephrolithiasis

• Skin rash (20%)

• Serum transaminase elevations

• Hyperlipidemia (especially with RTV boosting)

Darunavir 

(DRV)/

Prezista

75-, 150-, 300-, 

400-, 600-mg 

tablets

ARV-naïve patients or 

ARV-experienced patients 

with no DRV mutations:

(DRV 800 mg + RTV 100 

mg) once daily

ARV-experienced patients

with at least one DRV 

mutation:

(DRV 600 mg + RTV 100 

mg) BID

Unboosted DRV is not

recommended

Take with food

CYP3A4 

inhibitor and 

substrate

15 hrs 

(when 

combined 

with 

RTV)

Room 

temperature

(up to 25oC or 

77oF)

• Skin rash (10%): DRV has a sulfonamide moiety; 

Stevens-Johnson syndrome and erythrema 

multiforme have been reported.

• Hepatotoxicity

• Diarrhea, nausea

• Headache

• Hyperlipidemia

• Serum transaminase elevation

• Hyperglycemia

• Fat maldistribution

• Possible increased bleeding episodes in patients 

with hemophilia

Fosamprenavir 

(FPV)/

Lexiva (a prodrug 

of amprenavir 

[APV])

• 700-mg 

tablet

• 50-mg/mL 

oral 

suspension

ARV-naïve patients:

• FPV 1,400 mg BID or

• (FPV 1,400 mg + RTV 

100–200 mg) once daily 

or

• (FPV 700 mg + RTV 100 

mg) BID

PI-experienced patients 

(once-daily dosing not

recommended):

•(FPV 700 mg + RTV 100 

mg) BID

With EFV:

• (FPV 700 mg + RTV 100 

mg) BID or

• (FPV 1,400 mg + RTV 

300 mg) once daily

Tablet: Take without 

regard to meals (if not 

boosted with RTV tablet)

Suspension: Take without 

food

FPV w/RTV tablet: Take 

with meals

APV is a 

CYP3A4 

substrate, 

inhibitor, and 

inducer

Dosage 

adjustment in 

hepatic 

insufficiency 

recommended 

(See Appendix

B, Table 7.)

7.7 hrs 

(APV)

Room 

temperature

(up to 25oC or 

77oF)

• Skin rash (12%–19%) – FPV has a sulfonamide 

moiety

• Diarrhea, nausea, vomiting

• Headache

• Hyperlipidemia

• Serum transaminase elevation

• Hyperglycemia

• Fat maldistribution

• Possible increased bleeding episodes in patients 

with hemophilia

• Nephrolithiasis
January 10, 2011

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents Page 43 

Generic Name 

(abbreviation)/ 

Trade Name

Formulations

Dosing Recommendations

(For dosage adjustment 

in hepatic insufficiency, 

see Appendix B, Table 7)

Elimination Serum 

Half-life Storage Adverse Events

(Also see Table 13)

Indinavir

(IDV)/

Crixivan

100-, 200-, 

400-mg 

capsules

800 mg every 8 hrs

Take 1 hour before or 2 

hours after meals; may take 

with skim milk or low-fat 

meal

With RTV:

(IDV 800 mg + RTV 100–

200 mg) BID

Take without regard to 

meals

CYP3A4 

inhibitor and 

substrate

Dosage 

adjustment in 

hepatic 

insufficiency 

recommended 

(See Appendix

B, Table 7.)

1.5–2 hrs Room

temperature 

(15o–30oC/ 

59o–86oF)

Protect from 

moisture

• Nephrolithiasis

• GI intolerance, nausea

• Hepatitis

• Indirect hyperbilirubinemia

• Hyperlipidemia

• Headache, asthenia, blurred vision, dizziness, 

rash, metallic taste, thrombocytopenia, alopecia, 

and hemolytic anemia

• Hyperglycemia

• Fat maldistribution 

• Possible increased bleeding episodes in patients 

with hemophilia

Lopinavir + 

Ritonavir 

(LPV/r)/

Kaletra

Tablets:

(LPV 200 mg + 

RTV 50 mg) or

(LPV 100 mg + 

RTV 25 mg)

Oral solution: 

Each 5 mL 

contains (LPV 

400 mg + RTV 

100 mg)

Oral solution 

contains 42% 

alcohol

LPV/r 400-mg/100-mg 

BID

or

LPV/r 800-mg/200-mg 

once daily

Once-daily dosing is not 

recommended for patients 

with >3 LPV-associated 

mutations, pregnant 

women, or patients 

receiving EFV, NVP, FPV, 

NFV, carbamazepine, 

phenytoin, or 

phenobarbital.

With EFV or NVP (PInaïve or PI-experienced 

patients):

LPV/r 500-mg/125-mg 

tablets BID (Use a 

combination of two LPV/r 

200-mg/50-mg tablets + 

one LPV/r 100-mg/25-mg 

tablet to make a total dose 

of LPV/r 500 mg/125 mg.)

or

LPV/r 533-mg/133-mg oral 

solution BID

Tablet: Take without 

regard to meals

Oral solution: Take with 

food

CYP3A4 

inhibitor and 

substrate

5–6 hrs Oral tablet is 

stable at room 

temperature.

Oral solution 

is stable at 

2°–8°C (36°–

46°F) until 

date on label 

and is stable 

when stored 

at room 

temperature 

(up to 25oC or 

77oF) for 2 

months.

• GI intolerance, nausea, vomiting, diarrhea

• Pancreatitis

• Asthenia

• Hyperlipidemia (especially hypertriglyceridemia)

• Serum transaminase elevation

• Hyperglycemia

• Insulin resistance/diabetes mellitus

• Fat maldistribution

• Possible increased bleeding episodes in patients 

with hemophilia

• PR interval prolongation

• QT interval prolongation and torsades de pointes 

have been reported; however, causality could not 

be established.

Nelfinavir (NFV)/

Viracept

• 250-, 625-

mg tablets

• 50-mg/g 

oral powder

1,250 mg BID or

750 mg TID

May dissolve tablets in a 

small amount of water; 

once dissolved, patients 

should mix the cloudy 

liquid well and consume it 

immediately.

Take with food

CYP2C19 and 

3A4

substrate—

metabolized to 

active M8 

metabolite;

CYP 3A4 

inhibitor

3.5–5 hrs Room 

temperature 

(15o–30oC/ 

59o–86oF)

• Diarrhea

• Hyperlipidemia

• Hyperglycemia

• Fat maldistribution

• Possible increased bleeding episodes in patients 

with hemophilia

• Serum transaminase elevation

Appendix B, Table 3. Characteristics of Protease Inhibitors (PIs)

Page 2 of 3