Indications for: INVIRASE
HIV-1 infection, in combination with ritonavir and other antiretroviral agents.
Take within 2hrs 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. Switching from another regimen: see full labeling.
≤16yrs: not recommended.
Congenital long QT syndrome (see full labeling). Refractory hypokalemia or hypomagnesemia. Complete AV block without implanted pacemakers, or those who are at high risk. Severe hepatic impairment. Use in combination with drugs that both increase saquinavir plasma concentrations and prolong the QT interval. Concomitant alfuzosin, amiodarone, bepridil, dofetilide, flecainide, lidocaine (systemic), propafenone, quinidine, trazodone, clarithromycin, erythromycin, halofantrine, pentamidine, rifampin, lurasidone, clozapine, haloperidol, pimozide, sertindole, ziprasidone, phenothiazines, chlorpromazine, mesoridazine, thioridazine, ergots, atazanavir, lovastatin, simvastatin, tacrolimus, rilpivirine (concomitant use and switching to Invirase/ritonavir without ≥2 weeks washout period), sildenafil (as Revatio for PAH), triazolam, oral midazolam, dasatinib, sunatinib, disopyramide, quinine.
Increased risk of cardiac conduction abnormalities in patients with ischemic heart or underlying structural heart disease, pre-existing conduction abnormalities, cardiomyopathies. Monitor ECG in those with CHF, bradyarrhythmias, hepatic impairment, and electrolyte abnormalities. Discontinue if significant arrhythmias, QT/PR prolongation occurs. Correct hypokalemia or hypomagnesemia before starting and monitor during therapy. Galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption: not recommended. Underlying hepatitis B or C, cirrhosis, chronic alcoholism. Hepatic impairment. Severe renal impairment or ESRD. Hemophilia (monitor for spontaneous bleeding). Diabetes. Monitor cholesterol, triglycerides, and for hyperglycemia. Elderly. Pregnancy. Nursing mothers: not recommended.
HIV-1 protease inhibitor.
See Contraindications. Concomitant cobicistat, delavirdine, efavirenz, nevirapine, indinavir, nelfinavir, ibutilide, sotalol, fusidic acid, dapsone, tipranavir/ritonavir, salmeterol, St. John's wort, garlic capsules, ketoconazole >200mg/day, carbamazepine, phenobarbital, phenytoin, colchicine (in renal/hepatic impairment): not recommended. Potentiates atorvastatin (max 20mg/day), maraviroc (max 150mg twice daily), colchicine (see full labeling), quetiapine (reduce dose to ⅙), benzodiazepines, IV midazolam, calcium channel blockers, bosentan (see full labeling), sildenafil, vardenafil, tadalafil (reduce dose of these), fentanyl, alfentanil; monitor. Antagonizes methadone (may need to increase dose), oral contraceptives (consider alternative or additional contraceptive). Antagonized by CYP3A-inducing corticosteroids (eg, systemic dexamethasone or others): consider alternatives. Monitor warfarin, TCAs, digoxin, cyclosporine, rapamycin. Caution with lopinavir/ritonavir, nefazodone, itraconazole, quinupristin/dalfopristin, omeprazole, IV vincamine; monitor for toxicity. Concomitant rifabutin: reduce rifabutin dose by ≥75%; monitor. See full labeling.
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.