Saquinavir mesylate

Saquinavir mesylate capsules and tablets and saquinavir soft gelatin capsules are not bioequivalent and cannot be used interchangeably. Use saquinavir mesylate only if it is combined with ritonavir, which significantly inhibits saquinavir s metabolism to... 

HIV infection Saquinavir mesylate in combination with ritonavir and other antiretroviral agents is indicated for the treatment of HIV infection. The twice-daily administration of saquinavir mesylate in combination with ritonavir is supported by safety data from the MaxCmin 1 study and pharmacokinetic data. The efficacy of saquinavir mesylate with ritonavir or saquinavir soft gelatin capsules (with or without ritonavir coadministration) has not been compared against the efficacy of antiretroviral regimens currently considered standard of care. 

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. 

Give ritonavir at the same time as saquinavir mesylate. 

Give saquinavir mesylate and ritonavir within 2 hours after a meal. 

Dose adjustment for combination therapy with saquinavir For serious toxicities that may be associated with saquinavir mesylate, the drug should be interrupted. Saquinavir mesylate at doses less than 1,000 mg with ritonavir 100 mg twice daily are not recommended since lower doses have not shown antiviral activity. For recipients of combination therapy with saquinavir mesylate and ritonavir, dose adjustments may be necessary. These adjustments should be based on the known toxicity profile of the individual agent and the pharmacokinetic interaction between saquinavir and the coadministered drug. Health care providers should refer the complete monographs for these drugs for comprehensive dose adjustment recommendations and drug-associated adverse reactions of nucleoside analogues. 

HIV-infected patients administered saquinavir mesylate (600 mg 3 times daily) had area under the curve (ADC) and maximum plasma concentration (Cmax) values approximately 2 to 2.5 times those observed in healthy... 

Saquinavir mesylate is contraindicated in patients with clinically significant hypersensitivity to saquinavir or to any of the components contained in the capsule. 

Saquinavir mesylate when administered with ritonavir is contraindicated in patients with severe hepatic impairment. 

Do not administer saquinavir mesylate concurrently with drugs listed in the Drug Interactions section. Inhibition of CYP3A4 by saquinavir could result in elevated plasma concentrations of these drugs, potentially causing serious or life-threatening reactions such as cardiac arrhythmias or prolonged sedation. 

Resistance/cross-resistance Varying degrees of cross-resistance among protease inhibitors have been observed. Continued administration of saquinavir mesylate therapy following loss of viral suppression may increase the likelihood of cross-resistance to other protease inhibitors. 

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. 

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. 

Invirase , saquinavir mesylate [package insert]. Nutley, NJ Roche Laboratories, Inc. (package insert revised 12/2003). 

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