Congenital long QT syndrome. 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, cisapride, dofetilide, ergots, flecainide, lidocaine, oral midazolam, pimozide, propafenone, quinidine, rifampin, sildenafil (Revatio; when used to treat PAH), lovastatin, simvastatin, trazodone, triazolam.
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, CHF, bradyarrhythmias. Monitor ECG at baseline and during treatment. If QT interval >450msec, do not give ritonavir-boosted saquinavir. If QT interval <450msec, do on-treatment ECG after 3 to 4 days therapy; if QT interval >480msec or prolongation over pre-treatment by >20msec, discontinue therapy. Correct and monitor electrolyte imbalances before and during therapy. Underlying hepatitis B or C, cirrhosis, chronic alcoholism. Hepatic impairment. Severe renal impairment. Hemophilia (monitor for spontaneous bleeding). Diabetes. Monitor clinical chemistry, triglycerides, and for hyperglycemia. Elderly. Pregnancy (Cat.B). Nursing mothers: not recommended.
See Contraindications. Concomitant tipranavir/ritonavir, fluticasone, salmeterol, St. John's wort, garlic capsules: not recommended. Limit dose of atorvastatin to 20mg daily. Plasma levels reduced by efavirenz, nevirapine, rifabutin, other CYP3A4 inducers (eg, carbamazepine, phenobarbital, phenytoin, dexamethasone). Plasma levels increased by clarithromycin (see literature), atazanavir, indinavir, lopinavir/ritonavir, ritonavir, delavirdine. Antagonizes methadone, oral contraceptives. Potentiates CYP3A4 substrates (eg, calcium channel blockers, warfarin, cyclosporine, tacrolimus, rapamycin, sildenafil, vardenafil, tadalafil), maraviroc, bosentan, colchicine, ketoconazole, itraconazole; monitor their effects; may need reduced doses. Caution with digoxin, ibutilide, sotalol, tricyclics, benzodiazepines, neuroleptics (eg, clozapine, haloperidol, thioridazine), omeprazole, erythromycin, halofantrine, pentamidine, others (see literature).
GI disturbances, fatigue, abdominal pain, headache, paresthesia, weakness, lab abnormalities, depression, hyperglycemia, diabetes, hyperlipidemia, fat redistribution, immune reconstitution syndrome, hepatotoxicity, rash, pruritus; 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.