Itraconazole


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Cách dùng
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.
Tương kỵ
IV: Solutions other than the supplied 50 mL 0.9% NaCl inj.
Chống chỉ định
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.
Thận trọng
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.
Phản ứng phụ
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.
Thông tin tư vấn bệnh nhân
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.
Tương tác
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.
Tác dụng
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).
Đặc tính

Chemical Structure Image
Itraconazole

Source: National Center for Biotechnology Information. PubChem Database. Itraconazole, CID=3793, https://pubchem.ncbi.nlm.nih.gov/compound/Itraconazole (accessed on Jan. 21, 2020)

Bảo quản
Cap, tab: Store between 15-25°C. Protect from light and moisture. Oral solution, IV: Store below 25°C. Do not freeze.
Phân loại MIMS
Phân loại ATC
J02AC02 - itraconazole ; Belongs to the class of triazole derivatives. Used in the systemic treatment of mycotic infections.
References
Anon. Itraconazole. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 15/05/2019.

Anon. Itraconazole. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 15/05/2019.

Buckingham R (ed). Itraconazole. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/05/2019.

Itraconazole 10 mg/mL Concentrate and Solvent for Solution for Infusion (Neon Healthcare Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 15/05/2019.

Itraconazole 10 mg/mL Sugar Free Oral Solution (Syri limited t/a Thame Laboratories). MHRA. https://products.mhra.gov.uk/. Accessed 15/05/2019.

Joint Formulary Committee. Itraconazole. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/05/2019.

Onmel Tablet (Merz Pharmaceuticals, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 15/05/2019.

Sporanox Solution (Janssen Pharmaceuticals, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 15/05/2019.

Sporanox-Pulse (Janssen-Cilag Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 15/05/2019.

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