Invirase 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. 

Fig. 18.7. Oral bioavailability of saquinavir with and without CFJ [42], Saquinavir (600 mg three capsules of Invirase, 200 mg each tablet) was administered to eight healthy male subjects (average body weight 76 kg) before and after consumption of two glasses (200 mL each) of CFJ at 15 and 45 min before drug administration. QMPRPIus was used to estimate human effective permeability (0.93 X 10-4 cm s 1), pure aqueous water...

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

Invirase Saquinavir mesylate 1,000 mg twice daily (5 x 200 mg capsules or 2 x 500 mg tablets) in combination with ritonavir 100 mg twice daily. 

Similar labeling language also in the labeling of INVIRASE (Roche Laboratories) (saquinavir mesylate) capsules, December 2003 KALETRA (Abbott) (lopinavir/ritonavir) capsules, (lopinavir/ritonavir) oral solution, February 2004 and LEXIVA (GlaxoSmithKline) (fosamprenavir calcium) tablets. May 2004. 

In its original formulation as a hard gel capsule (saguinavir-H Invirase), oral saquinavir is pooriy bioavailable (only about 4% after food). However, reformulation of saquinavir-H for once-daily dosing in combination with low-dose ritonavir has both improved antiviral efficacy and decreased gastrointestinal adverse effects. 

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. 

SAQUINAVIR (INVIRASE HARD CAPSULES) GRAPEFRUIT JUICE Possibly t efficacy Possibly t bioavailability 1 presystemic metabolism. Constituents of grapefruit irreversibly inhibit intestinal cytochrome CYP3A4. Transport via P-gp and MRP-2 efflux pumps is also inhibited No dose adjustment is advised. Oral bioavailability is very low and is enhanced beneficially with grapefruit juice or grapefruit. Soft gel capsules have greater bioavailability so may interact to a lesser degree... 

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

Saquinavir/Invirase (SQV) 200 mg capsules 1,000 mg b.i.d. with lOOmg bid of ritonavir invirase alone is not recommended GI intolerance, increased transaminases, metabolic complications 4.0... 

Invirase Hard Capsules (Saquinavir mesilate), Roche Products Ltd. UK Summary of product characteristics, May 2007,... 

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