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Viral infections
Only 4 drugs may be compared at once

Generic Name and Formulations:

Saquinavir (as mesylate) 500mg.


Genentech, Inc.

Select therapeutic use:

Indications for INVIRASE TABLETS:

HIV-1 infection, in combination with ritonavir and other antiretroviral agents.


Take within 2 hours after a meal. ≥16yrs: saquinavir 1g twice daily + ritonavir 100mg twice daily (taken at same time). Treatment-naive or switching from a delavirdine- or rilpivirine-containing regimen: initially saquinavir 500mg twice daily + ritonavir 100mg twice daily for 7 days, then increase to saquinavir 1g twice daily + ritonavir 100mg twice daily.


<16yrs: not recommended.


Congenital long QT syndrome. Refractory hypokalemia or hypomagnesemia. Complete AV block without implanted pacemakers, or those who are at high risk. Severe hepatic impairment (with ritonavir). Use in combination with drugs that both increase saquinavir plasma concentrations and prolong the QT interval. Concomitant alfuzosin, amiodarone, atazanavir, bepridil, chlorpromazine, cisapride, clarithromycin, clozapine, dapsone, disopyramide, dofetilide, ergots, erythromycin, flecainide, halofantrine, haloperidol, lidocaine, lovastatin, lurasidone, mesoridazine, oral midazolam, pentamidine, phenothiazines, pimozide, propafenone, quinidine, quinine, rifampin, sildenafil (Revatio; when used to treat PAH), sertindole, simvastatin, tacrolimus, thioridazine, trazodone, triazolam, ziprasidone.


Not bioequivalent to soft gel form of saquinavir; do not interchange. Increased risk of cardiac conduction abnormalities in patients with ischemic heart or underlying structural heart disease, pre-existing conduction abnormalities, cardiomyopathies. PR/QT interval prolongation: see full labeling. Monitor ECG in those with CHF, bradyarrhythmias, hepatic impairment, and electrolyte abnormalities. Correct hypokalemia or hypomagnesemia before starting and monitor during therapy. Underlying hepatitis B or C, cirrhosis, chronic alcoholism. Hepatic impairment. Severe renal impairment or ESRD. Hemophilia (monitor for spontaneous bleeding). Diabetes. Monitor clinical chemistry, triglycerides, and for hyperglycemia. Elderly. Pregnancy (Cat.B). Nursing mothers: not recommended.


See Contraindications. Concomitant cobicistat, delavirdine, efavirenz, nevirapine, indinavir, nelfinavir, ibutilide, sotalol, fusidic acid, dexamethasone, tipranavir/ritonavir, fluticasone, salmeterol, St. John's wort, garlic capsules, ketoconazole or itraconazole >200mg/day: not recommended. Limit dose of atorvastatin to 20mg/day. Plasma levels reduced by other CYP3A4 inducers (eg, carbamazepine, phenobarbital, phenytoin): not recommended. Plasma levels increased by ritonavir, nefazodone. Antagonizes oral contraceptives; consider alternative or additional contraceptive. Potentiates CYP3A4 substrates (eg, calcium channel blockers, warfarin, cyclosporine, rapamycin, sildenafil, vardenafil, tadalafil), quetiapine, benzodiazepines, fentanyl, maraviroc, bosentan, colchicine; monitor their effects; may need reduced doses. Caution with lopinavir/ritonavir, methadone, IV vincamine, digoxin, quinupristin/dalfopristin, tricyclics, omeprazole, others (see full labeling). Concomitant rifabutin: reduce rifabutin dose by at least 75%; monitor.

See Also:


Pharmacological Class:

HIV-1 protease inhibitor.

Adverse Reactions:

Nausea, diarrhea, vomiting, fatigue, abdominal pain, pneumonia, lipodystrophy; hyperglycemia, hyperlipidemia, fat redistribution, immune reconstitution syndrome, hepatotoxicity; rare: 2nd or 3rd-degree AV block, QT prolongation, torsades de pointes.


Register pregnant patients exposed to saquinavir by calling (800) 258-4263. See Norvir entry in this section for more information on ritonavir.

How Supplied:

Caps—270; Tabs—120