Page 234 - HIV/AIDS Guidelines

Appendix B, Table 3. Characteristics of Protease Inhibitors (PIs) (Last updated October 14, 2011; last
reviewed March 27, 2012) (page 4 of 5)

Dosing
Generic Name Recommendations
Serum/
(abbreviation)/ Formulations (For dosage adjustment Elimination Half-life Storage Adverse Events
Trade Name in renal or hepatic (Also see Table 13)
insufficiency, see
Appendix B, Table 7.)

Ritonavir (RTV)/ • 100-mg soft As pharmacokinetic booster CYP3A4 >2D6 3–5 hrs Refrigerate • GI intolerance, nausea,
Norvir gel capsule for other PIs: substrate; capsules. vomiting, diarrhea
100–400 mg per day in 1–2 potent 3A4, 2D6
• 100-mg tablet Capsules can be • Paresthesias (circumoral and
divided doses (refer to other inhibitor
• 80-mg/mL oral PIs for specific dosing left at room extremities)
solution recommendations) temperature (up • Hyperlipidemia (especially
to 25ºC or 77ºF)
Oral solution Tablet: Take with food for up to 30 days. hypertriglyceridemia)
contains 43% • Hepatitis
alcohol. Capsule and oral solution: Tablets do not
To improve tolerability, take require • Asthenia
with food if possible. refrigeration.
• Taste perversion
Oral solution • Hyperglycemia
should not be
refrigerated; • Fat maldistribution
store at room • Possible increased bleeding
temperature 20º– episodes in patients with
25ºC (68º–77ºF). hemophilia

Saquinavir • 500-mg tablet (SQV 1000 mg + CYP3A4 1–2 hrs Room • GI intolerance, nausea, and
(SQV)/ RTV 100 mg) BID inhibitor and temperature diarrhea
• 200-mg hard
Invirase substrate (15º–30ºC/ 59º–
gel capsule Unboosted SQV is not • Headache
86ºF)
recommended.
• Serum transaminase elevation
Take with meals or within 2
• Hyperlipidemia
hours after a meal.
• 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).

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents O-9

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