Fortovase capsules

Fortovase should be used for the initiation of saquinavir therapy (see Administration and Dosage) because Fortovase capsules provide greater bioavailability and efficacy than Invirase. For patients taking Invirase capsules with a viral load below the limit of quantification, a switch to Fortovase is recommended to maintain a virologic response. For patients taking Invirase capsules who have not had an adequate response or are failing therapy, if saquinavir resistance is clinically suspected, then do not use Fortovase. If resistance to saquinavir is not clinically suspected, consider a switch to Fortovase. 

Saquinavir soft gelatin capsules Fortovase) and saquinavir mesylate capsules Invirase) are not bioequivalent and cannot be used interchangeably. 

Fortovase Six 200 mg capsules 3 times daily taken with a meal or up to 2 hours after a meal. When used in combination with nucleoside analogs, do not reduce the dosage of saquinavir, as this will lead to greater than dose-proportional decreases in saquinavir plasma levels. 

Saquinavir is a potent inhibitor of HIV-1 and HIV-2 protease. Fortovase, a soft gel preparation of saquinavir, has largely replaced saquinavir mesylate capsules (Jnvirase) because it has improved bioavailability. Saquinavir is usually well tolerated and most frequently produces mild gastrointestinal side effects. 

Hugen PW, Burger DM, Koopmans PP, et al. Saquinavir soft-gel capsules (Fortovase) give lower exposure than expected, even after a high-fat breakfast. Pharm World Sci 2002 24(3) 83-86. 

Oral (Invirase) 200 mg hard gel capsules, 500 mg tablets Oral (Fortovase) 200 mg soft gel capsules Stavudine... 

In its original formulation as a hard gel capsule (saquinavir-H Invirase), oral saquinavir was poorly bioavailable (about 4% in the fed state). It was therefore largely replaced in clinical use by a soft gel capsule formulation (saquinavir-S Fortovase), in which absorption was increased approximately threefold. However, reformulation of saquinavir-H for once-daily dosing in combination with low-dose ritonavir (see Ritonavir) has both improved antiviral efficacy and decreased the gastrointestinal side effects typically associated with saquinavir-S. Moreover, coadministration of saquinavir-H with ritonavir results in blood levels of saquinavir similar to those associated with saquinavir-S, thus capitalizing on the pharmacokinetic interaction of the two agents. 

Both formulations of saquinavir should be taken within 2 hours after a fatty meal for enhanced absorption. Saquinavir has a large volume of distribution but is 98% protein-bound penetration into the cerebrospinal fluid is negligible. The elimination half-life is 12 hours. Excretion is primarily in the feces. Reported adverse effects include gastrointestinal discomfort (nausea, diarrhea, abdominal discomfort, dyspepsia these are more common with Fortovase) and rhinitis. Although refrigeration is recommended for storage, the capsules are stable at room temperature for up to 3 months. 

Saquinavir (SQV) Invirase Fortovase Invirase 200 mg capsule, 500 mg tablet Fortovase 200 mg capsule Itraconazole, ketoconazole, fluconazole, voriconazole, erythromycins. 

Saquuiavh/Fortovase (.SQV-sgc) 200mg soft gel capsules 1200mg t.i.d. GI hitolerance, hicreased dansami-nases, metabohc complications 4.0... 

Saquinavir/Fortovase (SQV-sgc) 200 mg soft gel capsules 1200 mg t.i.d. Gl intolerance, increased transaminases, metabolic comphcations 4.0... 

Ritonavir, an HIV protease inhibitor with peptidelike structure, has an intrinsic water solubility of l.Opg/ml. Norvir is a thermodynamically stable solution formulation containing 100 mg of ritonavir dissolved in a mixture of oleic acid, Cremophor EL, ethanol, and the antioxidant butylated hydroxytoluene (BHT), and filled into soft gelatin capsules. However, Norvir is being replaced by Kaletra oral solution and soft gelatin capsule, which is a combination of 133.3 mg of lopinavir and 33.3 mg ritonavir dissolved in a mixture of oleic acid, polyoxyl 35 castor oil (Cremophor EL), and propylene glycol. The water-insoluble HIV protease inhibitor, saquinavir, is solubilized by a mixture of Vitamin E and medium-chain mono- and diglycerides in 200 mg Fortovase soft gelatin capsules. 

Fortovase 1200 mg three times/day Saquinavir three 200 mg capsules given three times daily within 2 hours after a full meal do not give less than 600 mg/day (does not produce antiviral activity). Recommended daily doses of ddC or AZT ddC 0.75 mg three times daily ... 

The concurrent use of saquinavir soft capsules (Fortovase) [no longer available] 1.2 g three times daily and erythromycin 250 mg four times daily doubled the AUC and maximum serum levels of saquinavir in HIV-infected subjects. The manufacturer notes that there are no data on the interaction using ritonavir-boosted saquinavir hard capsules or tablets In-virase). ... 

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