This drug may cause dizziness, visual disturbances and hearing loss, if affected, do not drive or operate machinery.
Monitor LFTs, renal function tests, serum trough concentrations for other infections. Assess for signs and symptoms of heart failure.
May decrease plasma concentrations with carbamazepine, phenobarbital, phenytoin isoniazid, rifabutin, rifampicin, nevirapine, efavirenz. May reduce absorption with antimuscarinics, antacids, PPIs, histamine H2-receptor antagonists. May increase plasma concentrations with indinavir, ritonavir, telaprevir, erythromycin, clarithromycin, ciprofloxacin. May reduce plasma concentration of meloxicam. May increase serum concentrations of digoxin, alfentanil, oxycodone, repaglinide, bilastine, alprazolam, midazolam (IV), buspirone, saquinavir, praziquantel, bosentan, aprepitant, reboxetine, fesoterodine, solifenacin, tamsulosin, tadalafil, sildenafil, cinacalcet, tolvaptan, antineoplastic agents (e.g. busulfan, docetaxel, trimetrexate, vinca alkaloids), immunosuppressants (e.g. ciclosporin, tacrolimus), corticosteroids (e.g. budesonide, dexamethasone, fluticasone), oral anticoagulants (e.g. apixaban, cilostazol, coumarins). May increase risk of respiratory depression with fentanyl. May enhance negative inotropic effects of verapamil. Potentially Fatal: May increase risk of QT prolongation and ventricular tachyarrhythmia (including torsades de pointes) with astemizole, bepridil, cisapride, disopyramide, dofetilide, dronedarone, felodipine, halofantrine, lercanidipine, levacetylmethadol, mizolastine, nisoldipine, pimozide, quinidine, sertindole, and terfenadine. May increase risk of ergotism with ergot alkaloids (e.g. dihydroergotamine, ergometrine). Increased risk of myopathy including rhabdomyolysis with HMG-CoA reductase inhibitors (e.g. simvastatin, lovastatin). May potentiate hypnotic and sedative effect of triazolam and oral midazolam. May increase plasma concentrations of lurasidone, irinotecan, eplerenone, ranolazine, and colchicine (patient with renal or hepatic impairment).
May increase absorption with food and acidic beverages. May decrease plasma concentrations with St. John’s wort. May alter serum levels with grapefruit or grapefruit juice.
Description: Itraconazole, a triazole derivative antifungal agent, inhibits the fungal CYP450 activity, thereby decreasing ergosterol biosynthesis and inhibiting fungal cell membrane formation. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Enhanced absorption with food (cap, tab); without food (oral solution). Bioavailability: Approx 55%, increases by 30% under fasted conditions (oral solution). Time to peak plasma concentration: 2-5 hours (cap, tab); 2.5 hours (oral solution). Distribution: Widely distributed into the organs, tissues, skin and nails; minimal concentration distributed in the CSF. Enters breast milk (small amounts). Volume of distribution: >700 L. Plasma protein binding: 99.8% mainly to albumin. Metabolism: Extensively metabolised in the liver via oxidation by CYP3A4 isoenzyme to hydroxy-itraconazole as its major active metabolite. May undergo saturable metabolism with multiple dosing. Excretion: Via urine (35% as inactive metabolites; <1% as active drug); faeces (54%, approx 3-18% as unchanged drug); stratum corneum and hair (small amounts). Elimination half-life: 16-28 hours (single dose); 34-42 hours (multiple doses).
Cap, tab: Store between 15-25°C. Protect from light and moisture. Oral solution, IV: Store below 25°C. Do not freeze.