Indications for TOLSURA:
Blastomycosis. Histoplasmosis. Aspergillosis in patients who are intolerant of or refractory to amphotericin B.
Limitations of Use:
Not for treating onychomycosis. Not interchangeable or substitutable with other itraconazole products due to dosing differences.
Swallow whole. Take with food. Doses >130mg should be given in 2 divided doses. Blastomycosis, histoplasmosis: 130mg once daily, may increase by 65mg increments; max 260mg/day. Aspergillosis: 130mg once daily; max 260mg/day. Life-threatening conditions: give loading dose of 130mg three times daily for 1st 3 days, followed by the appropriate treatment dose; continue for at least 3 months until resolved.
Concomitant methadone, disopyramide, dofetilide, dronedarone, quinidine, isavuconazole, ergots, irinotecan, lurasidone, oral midazolam, pimozide, triazolam, felodipine, nisoldipine, ivabradine, ranolazine, eplerenone, naloxegol, lomitapide, lovastatin, simvastatin, avanafil, ticagrelor. Concomitant colchicine, fesoterodine, or solifenacin in renal/hepatic impairment. Concomitant eliglustat in poor or intermediate CYP2D6 metabolizers or those taking strong or moderate CYP2D6 inhibitors.
Congestive heart failure (CHF). Drug interactions.
CHF risk (eg, ischemic/valvular disease, COPD, renal failure, edema); monitor and reassess treatment if occurs. Monitor for signs/symptoms of liver dysfunction; discontinue and perform LFTs if develop. Discontinue if neuropathy, hearing loss or hypersensitivity occurs. Renal or hepatic impairment: monitor carefully. Elevated liver enzymes, active liver disease, previous hepatotoxicity: not recommended unless serious or life-threatening situation. Elderly. Pregnancy. Nursing mothers.
See Contraindications. Serious cardiac effects with pimozide, methadone, quinidine, others. Concomitant alfuzosin, silodosin, tamsulosin, fentanyl, apixaban, rivaroxaban, vorapaxar, antineoplastics (see full labeling), simeprevir, aliskiren, riociguat, sildenafil or tadalafil (for PAH), everolimus, sirolimus, IV temsirolimus, salmeterol, darifenacin, vardenafil, colchicine, conivaptan, tolvaptan, regorafenib, saccharomyces boulardii: not recommended during and 2 weeks after itraconazole. Avoid itraconazole for more than 2 weeks during bedaquiline therapy. Rifabutin, carbamazepine, lumacaftor/ivacaftor: avoid 2 weeks before, during, and 2 weeks after itraconazole. Avoid isoniazid, rifampicin, phenobarbital, phenytoin, efavirenz, nevirapine 2 weeks before and during itraconazole therapy. Potentiates alfentanil, buprenorphine, oxycodone, sufentanil, digoxin, clarithromycin, trimetrexate, cilostazol, dabigatran, warfarin, repaglinide, saxagliptin, praziquantel, eletriptan, certain antineoplastics (see full labeling), antipsychotics, anxiolytics, hypnotics, zopiclone, daclatasvir, indinavir, maraviroc, nadolol, diltiazem, other dihydropyridines, verapamil, bosentan, guanfacine, aprepitant, loperamide, budesonide, ciclesonide, dexamethasone, fluticasone, methylprednisolone, cyclosporine, tacrolimus, atorvastatin, venlafaxine, fesoterodine, solifenacin, dutasteride, oxybutynin, sildenafil, tadalafil, tolterodine, eliglustat, oral alitretinoin, cabergoline, cannabinoids, cinacalcet, ivacaftor; monitor, may need to reduce dose of these. Concomitant artemether-lumefantrine, quinine, cobicistat, elvitegravir (ritonavir-boosted), ritonavir, saquinavir (unboosted), tenofovir disoproxil fumarate, dienogest, ulipristal, netupitant; monitor for adverse events. Antagonizes meloxicam; increase dose if necessary. Potentiated by ciprofloxacin, erythromycin, clarithromycin, idelalisib, cobicistat, protease inhibitors, diltiazem, gastric acid suppressants (eg, antacids, H2 blockers, PPIs), other CYP3A4 inhibitors; monitor, may need to reduce itraconazole dose. Tinnitus or hearing impairment with quinidine. Increased risk of CHF with concomitant CCBs.
Nausea, rash, vomiting, edema, headache, diarrhea, fatigue, fever, pruritus, hypertension, abnormal hepatic function, abdominal pain, dizziness, hypokalemia, anorexia, malaise, decreased libido, somnolence, albuminuria, impotence; hepatotoxicity (may be serious), CHF, neuropathy, hearing loss, hypersensitivity.
Generic Drug Availability: