Page 233 - HIV/AIDS Guidelines

Appendix B, Table 3. Characteristics of Protease Inhibitors (PIs) (Last updated October 14, 2011; last
reviewed March 27, 2012) (page 3 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.)
Lopinavir + Tablets: LPV/r 400 mg/100 mg BID CYP3A4 inhibitor 5–6 hrs Oral tablet is • GI intolerance, nausea, vomiting,
Ritonavir (LPV 200 mg + or and substrate stable at diarrhea
(LPV/r)/ RTV 50 mg) or room • Pancreatitis
Kaletra (LPV 100 mg + LPV/r 800 mg/200 mg once temperature.
RTV 25 mg) daily • Asthenia
Oral solution
Oral solution: Once-daily dosing is not is stable at • Hyperlipidemia (especially
Each 5 mL recommended for patients 2°–8°C hypertriglyceridemia)
contains with ≥3 LPV-associated (36°–46°F) • Serum transaminase elevation
(LPV 400 mg + mutations, pregnant women, until date on
RTV 100 mg) or patients receiving EFV, label and is • Hyperglycemia
NVP, FPV, NFV, stable for up
Oral solution carbamazepine, phenytoin, • Insulin resistance/diabetes
contains 42% or phenobarbital. to 2 months mellitus
alcohol when stored • Fat maldistribution
With EFV or NVP (PI-naive at room
or PI-experienced patients): temperature • Possible increased bleeding
LPV/r 500-mg/125-mg (up to 25ºC episodes in patients with
tablets BID (Use a or 77ºF). hemophilia
combination of two • PR interval prolongation
LPV/r 200-mg/50-mg tablets
+ one LPV/r 100-mg/25-mg • QT interval prolongation and
tablet to make a total dose of torsades de pointes have been
LPV/r 500 mg/125 mg.) reported; however, causality could
not be established.
or
LPV/r 533-mg/133-mg oral
solution BID
Tablet: Take without regard
to meals
Oral solution: Take with food

Nelfinavir (NFV)/ • 250-, 625-mg 1250 mg BID or CYP2C19 and 3A4 3.5–5 hrs Room • Diarrhea
Viracept tablets 750 mg TID substrate— temperature • Hyperlipidemia
metabolized to (15º–30ºC/
• 50-mg/g oral Dissolve tablets in a small • Hyperglycemia
powder amount of water, mix active M8 59º–86ºF)
admixture well, and metabolite; • Fat maldistribution
consume immediately. CYP 3A4 inhibitor
• Possible increased bleeding
Take with food episodes in patients with
hemophilia
• Serum transaminase elevation

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents O-8

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