Antiretroviral Agents in HIV-1

Antiretroviral Agents in HIV

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Elimination CYP3A4 inhibitor and substrate Serum/ Half-life Storage 5-6 hrs Oral tablet is stable at room temperature. Oral solution is stable at 2º-8ºC until date on label and is stable when stored at room temperature (up to 25ºC or 77ºF) for 2 months. Adverse Events ▶ GI intolerance, nausea, vomiting, diarrhea ▶ Asthenia ▶ Hyperlipidemia (especially hypertriglyceridemia) ▶ Elevated serum transaminases ▶ Hyperglycemia ▶ Fat maldistribution ▶ Possible increased bleeding episodes in pts with hemophilia ▶ PR interval prolongation ▶ QT interval prolongation and torsade de pointes have been reported; however, causality could not be established. CYP2C19 and 3A4 substrate— metabolized to active M8 metabolite; CYP 3A4 inhibitor CYP3A4 >2D6 substrate; potent 3A4, 2D6 inhibitor 3.5-5 hrs Room temperature (15º-30ºC/ 59º-86ºF) 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). CYP3A4 inhibitor and substrate 1-2 hrs Room temperature (15º-30ºC/ 59º-86ºF) ▶ Diarrhea ▶ Hyperlipidemia ▶ Hyperglycemia ▶ Fat maldistribution ▶ Possible increased bleeding episodes in pts with hemophilia ▶ Serum transaminase elevation ▶ GI intolerance, nausea, vomiting, diarrhea ▶ Paresthesias—circumoral and extremities ▶ Hyperlipidemia (especially hypertriglyceridemia) ▶ Hepatitis ▶ Asthenia ▶ Taste perversion ▶ Hyperglycemia ▶ Fat maldistribution ▶ Possible increased bleeding episodes in pts with hemophilia ▶ GI intolerance, nausea, and diarrhea ▶ Headache ▶ Elevated transaminase enzymes ▶ Hyperlipidemia ▶ Hyperglycemia ▶ Fat maldistribution ▶ Possible increased bleeding episodes in pts with hemophilia Continued on next page. ▶ 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 full guideline for details) 17

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