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
January 10, 2011

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents Page 44 

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)

Ritonavir (RTV)/

Norvir

• 100-mg soft 

gel capsules

• 100-mg 

tablets

• 80-mg/mL 

oral solution

Oral solution 

contains 43% 

alcohol

As pharmacokinetic 

booster for other PIs: 

100–400 mg per day in 1–2 

divided doses (refer to 

other PIs for specific 

dosing recommendations)

Tablet: Take with food

Capsule and oral solution: 

Take with food, if possible, 

to improve tolerability.

CYP3A4 >2D6 

substrate;

potent 3A4, 

2D6 inhibitor

3–5 hrs Refrigerate 

capsules.

Capsules can 

be left at 

room 

temperature 

(up to 25oC or 

77oF) for up 

to 30 days.

Tablets do not 

require 

refrigeration.

Oral solution 

should not be 

refrigerated; 

store at room 

temperature 

20o–25oC 

(68o–77oF).

• GI intolerance, nausea, vomiting, diarrhea

• Paresthesias—circumoral and extremities

• Hyperlipidemia (especially hypertriglyceridemia)

• Hepatitis

• Asthenia

• Taste perversion

• Hyperglycemia

• Fat maldistribution

• Possible increased bleeding episodes in patients 

with hemophilia

Saquinavir 

tablets and hard 

gel capsules

(SQV)/

Invirase 

• 500-mg 

tablets 

• 200-mg 

hard gel 

capsules

(SQV 1,000 mg + RTV 

100 mg) BID

Unboosted SQV is not

recommended.

Take with meals or within 

2 hours after a meal

CYP3A4 

inhibitor and 

substrate

1–2 hrs Room 

temperature 

(15o–30oC/ 

59o–86oF)

• GI intolerance, nausea, and diarrhea

• Headache

• Serum transaminase elevation

• Hyperlipidemia

• Hyperglycemia

• Fat maldistribution

• Possible increased bleeding episodes in patients 

with hemophilia

• PR interval prolongation

• QT interval prolongation, torsades de pointes 

have been reported. Patients with pre-SQV QT 

interval >450 msec should not receive SQV (See 

Table 5b.).

Tipranavir 

(TPV)/

Aptivus

• 250-mg 

capsules 

• 100-mg/mL 

oral solution

(TPV 500 mg + RTV 200 

mg) BID

Unboosted TPV is not

recommended.

TPV taken with RTV 

tablets: Take with meals

TPV taken with RTV 

capsules or solution: Take 

without regard to meals

Cytochrome 

P450 3A4 

inducer and 

substrate

Net effect 

when combined 

with RTV 

(CYP 3A4, 

2D6 inhibitor)

6 hrs 

after 

single 

dose of 

TPV/r

Refrigerate 

capsules.

Capsules can 

be stored at 

room 

temperature 

(25oC or 

77oF) for up 

to 60 days.

Oral solution 

should not be 

refrigerated or 

frozen and 

should be 

used within 

60 days after 

opening the 

bottle.

• Hepatotoxicity: Clinical hepatitis (including 

hepatic decompensation and hepatitis-associated 

fatalities) has been reported; monitor closely, 

especially in patients with underlying liver 

diseases.

• Skin rash (3%–21%): TPV has a sulfonamide 

moiety; use with caution in patients with known 

sulfonamide allergy.

• Rare cases of fatal and nonfatal intracranial 

hemorrhages have been reported. Risks include 

brain lesion, head trauma, recent neurosurgery, 

coagulopathy, hypertension, alcoholism,, use of 

anti-coagulant or anti-platelet agents including 

vitamin E.

• Hyperlipidemia

• Hyperglycemia

• Fat maldistribution

• Possible increased bleeding episodes in patients 

with hemophilia

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

Page 3 of 3