Rx information of PIs

Generic Name Indinavir Ritonavir Nelfinavir Form 200,333,400mg capsules 100mg capsules 600mg/7.5mL po solution 250mg tablets 50mg/g oral powder Dosing Recommendations 800mg q8h Separate dosing with ddI by 1 hour 600mg q12h Separate dosing with ddI by 2 hours   750mg tid or  1250mg bid Food Effect Levels decrease 77% Take 1 hour before or 2 hours after meals; may take with skim milk or low fat meal Levels increase 15% Take with food if possible; this may improve tolerability Levels increase 2-3 fold. Take with meal or snack Oral bioavailability 65% 65% 20-80% Serum half-life 1.5-2 hours 3-5 hours 3.5-5 hours Route of Metabolism P450 cytochrome 3A4 inhibitor (less than Ritonavir) P450 cytochrome 3A4>2D6 Potent 3A4 inhibitor   P450 cytochrome 3A4 inhibitor (less than Ritonavir) Storage Room temperature Refrigerate capsules. Oral solution should NOT be refrigerated Room temperature Adverse Effects Nephrolithiasis, GI intolerance, nausea, Lab: Increased indirect bilirubinemia (inconsequential) Misc.: Headache, asthenia, blurred vision, dizziness, rash, metallic taste, thrombocytopenia, alopecia. Hyperglycemia, Fat redistribution and lipid abnormalities, Possible increased bleeding episodes in patients with hemophilia. GI intolerance, nausea, vomiting, diarrhea, Paresthesias-circumoral and extremities. Hepatitis, Pancreatitis, Asthenia, Taste perversion, Lab.: Triglycerides increase> 200%, transaminase elevation, elevated CPK and uric acid Hyperglycemia, Fat redistribution and lipid abnormalities, Possible increased bleeding episodes in patients with hemophilia. Diarrhea, Hyperglycemia, Fat redistribution and lipid abnormalities, Possible increased bleeding episodes in patients with hemophilia *Dose escalation for Ritonavir: Day 1-2: 300mg bid; day 3-5; 400mg bid; day 6-13; 500mg bid; day 14, 600mg bid. Combination treatment regimen with Saquinavir (400mg po bid) plus Ritonavir (400mg po bid)

Source: Adapted from www.cdc.gov