Adult Dosing
Treatment of HIV-1 infection
- 1000 mg PO bid with ritonavir 100 mg PO bid
- 1000 mg PO bid with lopinavir/ritonavir 400/100 mg PO bid
Notes:- Must be used in combination with ritonavir, because it significantly inhibits saquinavir's metabolism to provide increased plasma saquinavir levels
- Saquinavir and ritonavir should be taken together within 2 hours after a meal
Pediatric Dosing
- Safety and effectiveness in pediatric patients <16 years of age have not been established
Treatment of HIV-1 infection
>16 years
- 1000 mg PO bid with ritonavir 100 mg PO bid
- 1000 mg PO bid with lopinavir/ritonavir 400/100 mg PO bid
Notes:- Must be used in combination with ritonavir, because it significantly inhibits saquinavir's metabolism to provide increased plasma saquinavir levels
- Saquinavir and ritonavir should be taken together within 2 hours after a meal
[Outline]
See Supplemental Patient Information
- Serious or severe toxicity may occur with saquinavir therapy; discontinue saquinavir until the etiology of the event is identified or the toxicity resolves
- Concomitant administration of saquinavir/ritonavir with drugs that are metabolized by CYP3A is contraindicated, as it can cause severe life-threatening adverse events or significant drug interactions
- Saquinavir/ritonavir prolongs the PR interval in a dose-dependent manner. Patients with underlying structural heart disease, preexisting conduction system abnormalities, cardiomyopathies and ischemic heart disease may be at increased risk for developing cardiac conduction abnormalities. ECG monitoring is recommended in these patients
- Contraindicated in patients with long QT syndrome, as it causes dose-dependent QT prolongation. Monitor ECG during therapy in patients with CHF, bradyarrhythmias, hepatic impairment and electrolyte abnormalities
- Hypokalemia or hypomagnesemia should be corrected prior to initiating saquinavir therapy and should be monitored periodically during therapy. Avoid using in combination with drugs that increase saquinavir plasma concentrations and prolong QT interval
- Co-administration of saquinavir/ritonavir with other drugs that prolong PR interval, including calcium channel blockers, beta-adrenergic blockers, digoxin and atazanavir should be undertaken with caution, particularly with those drugs metabolized by CYP3A
- New onset diabetes mellitus, exacerbation of preexisting diabetes mellitus and hyperglycemia have been reported in HIV-1infected patients on protease-inhibitor therapy; diabetic ketoacidosis has occurred in rare cases. Initiation and dose adjustments of insulin or oral hypoglycemic agents may be required for the treatment of these events. Persistent hyperglycemia has been reported in some cases after discontinuation of protease-inhibitor therapy
- Worsening liver disease has been reported in patients with underlying hepatitis B or C, cirrhosis, chronic alcoholism and/or other underlying liver abnormalities
- Increase in cholesterol and/or triglyceride levels have occurred in certain patients taking saquinavir/ritonavir; a marked increase in triglyceride level increases the risk of pancreatitis. Monitor cholesterol and triglyceride levels prior to initiating combination therapy and periodically thereafter
- Redistribution/accumulation of body fat including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and cushingoid appearance have occurred in patients receiving antiretroviral therapy
- Immune reconstitution syndrome may develop in patients treated with combination antiretroviral therapy. During the initial phase of combination therapy, patients may develop an inflammatory response to indolent or residual opportunistic infections, which may require further evaluation and treatment
- Autoimmune disorders (eg, Graves' disease, polymyositis, and Guillain-Barre syndrome) in the setting of immune reconstitution have been reported
- Continuation of therapy following loss of viral suppression may increase the likelihood of cross resistance to other protease inhibitors
Cautions: Use cautiously in
- Severe renal impairment
- Mild-moderate hepatic impairment
- Hemophilia
Supplemental Patient Information
- Inform patients that saquinavir is not a cure for HIV-1 infection and that they may continue to acquire illnesses associated with advanced HIV-1 infection, including opportunistic infections
- Advise patients that saquinavir must be used in combination with ritonavir; instruct patients to take the combination drugs within 2 hours after a full meal
Pregnancy Category:B
Breastfeeding: HIV-infected mothers should generally not breastfeed their infants in the United States and other developed countries. In countries where no acceptable, feasible, sustainable and safe replacement feeding is available, exclusive breastfeeding for 6 months is recommended for HIV-infected mothers to reduce the risk of HIV transmission from the mother to the infant compared with mixed feeding. In these settings, abrupt weaning at 4 months does not reduce the risk of HIV transmission or produce an overall health benefit compared to continued breastfeeding, and increases the risk of infant death in HIV-infected infants. Extended antiretroviral prophylaxis in breastfed infants with antiretroviral drugs reduces the rate of HIV transmission during breastfeeding by about half, but the optimal regimen and duration of prophylaxis has not yet been defined. An alternate drug may be preferred especially while nursing a newborn or preterm infant as there is little published experience with saquinavir during breastfeeding. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 14 January 2011). The Centers for Disease Control and Prevention recommend HIV-infected mothers not to breastfeed their infants to avoid risking postnatal transmission of HIV. It is unknown whether saquinavir is excreted in human milk. Manufacturer advises to instruct infected mothers not to breast-feed during therapy because of the potential for HIV-1 transmission and the potential of serious adverse reactions in nursing infants.
