Selecting a Treatment Regimen
Table 5C. Characteristics of Protease Inhibitors (PIs) Drug
Formulation
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
Dosing Recommendations
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 (PI-naïve or PI- experienced pts): 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
Nelfinavir (NFV) Viracept®
250, 625 mg tablets 50 mg/g oral powder
1,250 mg bid or 750 mg tid Take with food
Ritonavir (RTV) Norvir®
100 mg tablets 100 mg capsules 80 mg/mL oral solution
As pharmacokinetic booster for other PIs: 100-400 mg per day in 1-2 divided doses (refer to other PIs for specific dosing recommendations) (not FDA- approved)
Tablet: Take with food Capsule and oral solution: Take with food, if possible, to improve tolerability
Saquinavir (SQV) Invirase® a
500 mg tablets or 200 mg hard gel capsules
(SQV 1,000 mg + RTV 100 mg) bid Unboosted SQV is NOT recommended Take within 2 hours after a meal
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a Risk of cardiac arrhythmia when combined with ritornavir.