Page 231 - HIV/AIDS Guidelines

Appendix B, Table 3. Characteristics of Protease Inhibitors (PIs) (Last updated October 14, 2011; last
reviewed March 27, 2012) (page 1 of 5)

Dosing
Recommendations
Generic Name Serum/ Adverse Events
(abbreviation)/ Formulations (For dosage adjustment Elimination Half-life Storage (Also see Table 13)
in renal or hepatic
Trade Name
insufficiency, see
Appendix B, Table 7.)
Atazanavir 100-, 150-, ARV-naive patients: CYP3A4 inhibitor 7 hrs Room • Indirect hyperbilirubinemia
(ATV)/ 200-, 300-mg 400 mg once daily or and substrate temperature • PR interval prolongation: First
Reyataz capsules (ATV 300 mg + RTV 100 mg) Dosage (up to 25ºC degree symptomatic AV block
once daily or 77ºF)
adjustment in reported. Use with caution in
With TDF or in ARV- patients with patients with underlying
experienced patients: hepatic conduction defects or on
(ATV 300 mg + RTV 100 mg) insufficiency concomitant medications that can
once daily recommended cause PR prolongation.
(See Appendix B, • Hyperglycemia
With EFV in ARV-naive
patients: Table 7.) • Fat maldistribution
(ATV 400 mg + RTV 100 mg) • Possible increased bleeding
once daily
episodes in patients with
(For recommendations on hemophilia
dosing with H2 antagonists • Nephrolithiasis
and PPIs, refer to Table 16a.)
• Skin rash (20%)
Take with food
• Serum transaminase elevations
• Hyperlipidemia (especially with
RTV boosting)
Darunavir 75-, 150-, 300-, ARV-naive patients or ARV- CYP3A4 inhibitor 15 hrs Room • Skin rash (10%): DRV has a
(DRV)/ 400-, 600-mg experienced patients with no and substrate (when temperature sulfonamide moiety; Stevens-
Prezista tablets DRV mutations: combined (up to 25ºC Johnson syndrome and erythrema
(DRV 800 mg + RTV with RTV) or 77ºF) multiforme have been reported.
100 mg) once daily • Hepatotoxicity
ARV-experienced patients • Diarrhea, nausea
with at least one DRV • Headache
mutation:
(DRV 600 mg + • Hyperlipidemia
RTV 100 mg) BID • Serum transaminase elevation
Unboosted DRV is not • Hyperglycemia
recommended
• Fat maldistribution
Take with food
• Possible increased bleeding
episodes in patients with
hemophilia

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents O-6

Downloaded from http://aidsinfo.nih.gov/guidelines on 12/8/2012 EST.