Itraconazole


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Oesophageal candidiasis; Oral candidiasis As oral solution: 200 mg daily, preferably in 2 divided doses or as a single daily dose for 1-2 weeks. For fluconazole-resistant infection: 100-200 mg bid for 2-4 weeks. Prophylaxis of fungal infections in immunocompromised patients As oral solution: 5 mg/kg daily in 2 divided doses. Oropharyngeal candidiasis As cap: 100 mg once daily for 15 days. In patient with AIDS or neutropenia: 200 mg once daily for 15 days. Vulvovaginal candidiasis As cap: 200 mg bid for 1 day. Pityriasis versicolor As cap: 200 mg once daily for 7 days. Tinea corporis; Tinea cruris As cap: 100 mg once daily for 15 days or 200 mg once daily for 7 days. Tinea manuum; Tinea pedis As cap: 100 mg once daily for 30 days. As pulse treatment: 200 mg bid for 7 days. Nail fungal infections As cap: 200 mg once daily for 90 days. As pulse treatment: 200 mg bid for 7 days, repeated once for fingernails and twice for toenails after drug-free intervals of 21 days. Systemic fungal infections As cap: 100-200 mg once daily, may increase to 200 mg bid for invasive or disseminated infections. In life-threatening infections: As cap: Loading dose: 200 mg tid for 3 days. Prophylaxis of infections in neutropenic or AIDS patients As cap: 200 mg daily, may increase to 200 mg bid if necessary. IV Systemic fungal infections 200 mg via infusion over 1 hour bid for 2 days, then 200 mg via infusion over 1 hour once daily thereafter to complete the 14 days treatment.
Dosage Details
Intravenous
Systemic fungal infections
Adult: 200 mg via infusion over 1 hour bid for 2 days, followed by 200 mg via infusion over 1 hour once daily thereafter to complete the 14 days treatment.

Oral
Prophylaxis of fungal infections in immunocompromised patients
Adult: As oral solution: 5 mg/kg daily in 2 divided doses.

Oral
Nail fungal infections
Adult: As cap: 200 mg once daily for 90 days. As pulse treatment: 200 mg bid for 7 days, repeated once for fingernails and twice for toenails after drug-free intervals of 21 days.

Oral
Pityriasis versicolor
Adult: As cap: 200 mg once daily for 7 days.

Oral
Primary or secondary prophylaxis of infections in neutropenic or AIDS patients
Adult: As cap: 200 mg daily, may increase to 200 mg bid if necessary.

Oral
Tinea corporis, Tinea cruris
Adult: As cap: 100 mg once daily for 15 days or 200 mg once daily for 7 days.

Oral
Oropharyngeal candidiasis
Adult: As cap: 100 mg once daily for 15 days. In patient with AIDS or neutropenia: 200 mg once daily for 15 days.

Oral
Systemic fungal infections
Adult: As cap: 100-200 mg once daily, may increase to 200 mg bid for invasive or disseminated infections. In life-threatening infections: As cap: Loading dose: 200 mg tid for 3 days.

Oral
Oesophageal candidiasis, Oral candidiasis
Adult: As oral solution: 200 mg daily, preferably in 2 divided doses or as a single daily dose for 1-2 weeks. Patient with fluconazole-resistant infection: 100-200 mg bid for 2-4 weeks.

Oral
Tinea manuum, Tinea pedis
Adult: As cap: 100 mg once daily for 30 days. As pulse treatment: 200 mg bid for 7 days.

Oral
Vulvovaginal candidiasis
Adult: As cap: 200 mg bid for 1 day.
Renal Impairment
Intravenous:
CrCl <30 mL/min: Contraindicated.
Administration
Oral Soln: Should be taken on an empty stomach. Refrain from eating for at least 1 hr after intake.
Cap: Should be taken with food. Take immediately after a full meal.
Incompatibility
IV: Solutions other than the supplied 50 mL 0.9% NaCl inj.
Contraindications
Hypersensitivity. Non-life-threatening indications in patients with ventricular dysfunction (e.g. CHF, history of CHF). Severe renal impairment (IV). Pregnancy (non-life-threatening infection). Coadministration with astemizole, bepridil, cisapride, disopyramide, dofetilide, dronedarone, eplerenone, ergot alkaloids, felodipine, halofantrine, irinotecan, ivabradine, lercanidipine, levacetylmethadol, lovastatin, lurasidone, methadone, midazolam (oral), misolaztine, nisoldipine, pimozide, quinidine, ranolazine, sertindole, simvastatin, terfenadine, or triazolam; colchicine in patients with varying degrees of renal or hepatic impairment.
Special Precautions
Patients with risk factors for CHF (e.g. ischaemic or valvular disease, oedematous disorders, renal failure, COPD), reduced gastric acidity (e.g. achlorhydria), immediate life-threatening systemic fungal infections, cystic fibrosis, or immunocompromised patients (e.g. neutropenic, AIDS, organ transplant patients). Coadministration with Ca channel blockers or drugs that reduce gastric acidity. Renal and hepatic impairment. Elderly. Pregnancy (life-threatening infection) and lactation.
Adverse Reactions
Significant: Heart failure, pulmonary oedema, neuropathy, transient or permanent hearing loss, transient asymptomatic decrease of LVEF, hepatotoxicity, hypersensitivity reactions.
Blood and lymphatic system disorders: Granulocytopenia, leukopenia, thrombocytopenia.
Cardiac disorders: Chest pain, tachycardia.
Ear and labyrinth disorders: Tinnitus.
Eye disorders: Visual disturbance, blurred vision, diplopia.
Gastrointestinal disorders: Nausea, abdominal pain, vomiting, diarrhoea, dyspepsia, constipation.
General disorders and administration site conditions: Oedema, fatigue, pyrexia.
Hepatobiliary disorders: Jaundice, hepatitis, hyperbilirubinaemia.
Immune system disorders: Urticaria.
Investigations: Elevated liver enzymes, increased serum creatine phosphokinase.
Metabolism and nutrition disorders: Hypokalaemia, hypertriglyceridaemia.
Musculoskeletal and connective tissue disorders: Myalgia, arthralgia.
Nervous system disorders: Headache, dizziness, paraesthesia, dysgeusia.
Renal and urinary disorders: Pollakiuria, urinary incontinence.
Reproductive system and breast disorders: Menstrual disorder, erectile dysfunction.
Respiratory, thoracic and mediastinal disorders: Dyspnoea, cough, sinusitis, rhinitis.
Skin and subcutaneous tissue disorders: Rash, pruritus, photosensitivity, alopecia.
Vascular disorders: Hypertension, hypotension.
Potentially Fatal: Rarely, acute liver failure.
Patient Counseling Information
This drug may cause dizziness, visual disturbances and hearing loss, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor LFTs, renal function tests, serum trough concentrations for other infections. Assess for signs and symptoms of heart failure.
Drug Interactions
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).
Food Interaction
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.
Action
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).
Chemical Structure

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Storage
Cap, tab: Store between 15-25°C. Protect from light and moisture. Oral solution, IV: Store below 25°C. Do not freeze.
MIMS Class
ATC Classification
J02AC02 - itraconazole ; Belongs to the class of triazole derivatives. Used in the systemic treatment of mycotic infections.
Disclaimer: This information is independently developed by MIMS based on Itraconazole from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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