Classes
DEA Class; Rx
Common Brand Names; Invirase
- HIV, Protease Inhibitors
Description
Protease inhibitor (PI)
Used to treat HIV-1 infections in combination with ritonavir and other antiretroviral agents
Only use when ‘boosted’ with ritonavir; PR and QT prolongation (including TdP) reported
Indications
Indicated for the treatment of human immunodeficiency virus (HIV) infection in combination with other antiretroviral agents.
Contraindications
Hypersensitivity (eg, anaphylactic reaction, Stevens-Johnson syndrome)
An ECG should be performed prior to initiation of treatment; patients with a QT interval = 450 msec should not initiate therapy
Treatment-naïve patients initiating therapy should receive a reduced starting dose of saquinavir 500-mg twice daily with ritonavir 100-mg twice daily for the first 7 days of treatment followed by saquinavir/ritonavir 1000/100 mg twice daily due to potential for an increased risk of PR and QT interval prolongation with the standard 1000/100-mg twice daily dose
QT and PR interval prolonation and torsades de pointes have been reported rarely; do not use saquinavir/ritonavir with congenital or documented acquired QT prolongation (≥450 msec), refractory hypokalemia or magnesemia, and in combination with drugs that prolong QT interval
Complete atrioventricular (AV) block without implanted pacemakers or high risk of complete AV block
Severe hepatic impairment
Coadministration of saquinavir/ritonavir with rifampin due to the risk of severe hepatotoxicity
Adverse Effects
- Rash
- Hyperglycemia
- Diarrhea
- Abdominal discomfort
- Nausea
- Abdominal pain
- Buccal mucosa ulceration
- Paresthesia
- Weakness
- Increased CPK
- Headache
- Confusion
- Seizures
- Ataxia
- Pain
- Stevens-Johnson syndrome
- Hypoglycemia
- Hyper- & hypokalemia
- Low serum amylase
- AML
- Hemolytic anemia
- Thrombocytopenia
- Jaundice
- Ascites
Warnings
Hyperlipidemia may occur
Take within 2 hr after meal; absorption increased with high-fat meal
Must be used in combination with ritonavir (ie, boosted therapy) to achieve necessary levels for effectiveness
Autoimmune disorders (eg, Graves disease, polymyositis, Guillain-Barré syndrome) reported in the setting of immune reconstitution; however, time to onset is variable, and can occur many months after treatment initiation
Risk of QT and PR prolongation that might lead to Torsades de Pointes (particularly if used with ritonavir); discontinue therapy if significant arrhythmias, QT or PR prolongation occurs; perform ECG prior to initiation of treatment; patients with a baseline QT interval < 450 msec, an on-treatment ECG is recommended after approximately 10 days of therapy; patients with a QT interval prolongation over pre-treatment by > 20 msec should discontinue saquinavir/ritonavir therapy
May develop new onset or exacerbations of diabetes mellitus, hyperglycemia, elevated cholesterol and/or triglyceride concentrations, redistribution/accumulation of body fat, and immune reconstitution syndrome; monitor cholesterol and triglycerides prior to therapy and periodically thereafter
Pregnancy and Lactation
Prospective pregnancy data from the APR are not sufficient to adequately assess a drug-associated risk of birth defects or fetal outcomes; limited number of reports on use of drug during pregnancy has been submitted to the APR and number of exposures to drug is insufficient to make a risk assessment compared to a reference population
There are no data available regarding presence of drug in human milk, effects on breastfed infant, or on milk production
Maximum Dosage
NOTE: The following maximum dosage limits apply for typical saquinavir use; maximum dosage limits may be altered based on certain individual patient circumstances, such as in the case of specific drug interactions.
2,000 mg/day PO.
2,000 mg/day PO.
17 years: 2,000 mg/day PO.
13 to 16 years: Safety and efficacy have not been established; however, doses up to 100 mg/kg/day PO or 1,500 mg/m2/day (Max: 1,600 mg) have been studied.
7 years and older: Safety and efficacy have not been established; however, doses up to 100 mg/kg/day PO or 1,500 mg/m2/day (Max: 1,600 mg) have been studied.
2 years to 6 years: Safety and efficacy have not been established; however, doses up to 100 mg/kg/day PO have been studied.
Younger than 2 years: Safety and efficacy have not been established.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
How supplied
Saquinavir mesylate
tablet
- 500mg
