Itraconazole


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Aspergillosis, Cryptococcosis, Histoplasmosis, Systemic candidiasis
Adult: When 1st-line systemic antifungal agents are ineffective or inappropriate: 200 mg bid via infusion over 1 hour for 2 days, then 200 mg once daily for up to 14 days.

Oral
Oropharyngeal candidiasis
Adult: As cap: 100 mg once daily for 15 days. Patients with AIDS or other immunocompromised (e.g. neutropenic) patients: 200 mg once daily for 15 days.

Oral
Systemic candidiasis
Adult: As cap: 100-200 mg once daily for 3 weeks to 7 months; increase to 200 mg bid in case of invasive or disseminated disease.

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
Cryptococcal meningitis
Adult: As cap: 200 mg bid for 2 months to 1 year.

Oral
Onychomycosis
Adult: For cases caused by dermatophytes and/or yeasts: As cap: 200 mg once daily for 3 months. As pulse treatment: 200 mg bid for 7 days, repeated once for fingernails or twice for toenails after drug-free intervals of 21 days.

Oral
Pityriasis versicolor
Adult: As cap: 100 mg bid or 200 mg once daily for 5-7 days.

Oral
Non-meningeal cryptococcosis
Adult: As cap: 200 mg once daily for 2 months to 1 year.

Oral
Vulvovaginal candidiasis
Adult: As cap: 200 mg bid for 1 day or 200 mg once daily for 3 days.

Oral
Histoplasmosis
Adult: As cap: 200 mg once daily; may increase in increments of 100 mg to a Max of 400 mg daily, if there is no obvious improvement, or there is evidence of progressive fungal disease. Doses above 200 mg daily should be given in two divided doses. Treatment duration: 8 months. Maintenance therapy in AIDS patients: 200 mg 1-2 times daily until immune recovery.

Oral
Aspergillosis
Adult: As cap: 200 mg once daily for 2-5 months; increase to 200 mg bid in case of invasive or disseminated disease.

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

Oral
Primary prophylaxis of infection in AIDS patients, Primary prophylaxis of infection in neutropenic patients, Secondary prophylaxis of infection in AIDS patients, Secondary prophylaxis of infection in neutropenic patients
Adult: As cap: 200 mg once daily; may increase to 200 mg bid if necessary.

Oral
Oesophageal candidiasis, Oral candidiasis
Adult: As oral solution: In HIV-positive or other immunocompromised patients: 200 mg daily in 1-2 divided doses for 1 week; may continue therapy for another 1 week if there is no response. For fluconazole-resistant cases: 100-200 mg bid for 2 weeks; may continue treatment for another 2 weeks if no response.

Oral
Prophylaxis of deep fungal infection
Adult: When standard therapy is inappropriate in patients with haematological malignancy or undergoing bone marrow transplant, and who are expected to become neutropenic: As oral solution: 5 mg/kg daily in 2 divided doses. Continue treatment until neutrophil count recovers (i.e. >1,000 cells/microliter).

Oral
Blastomycosis
Adult: As cap: 100 mg once daily to 200 mg bid for 6 months.
Suy thận
Intravenous:
CrCl (mL/min) Dosage
<30 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.
Hướng dẫn pha thuốc
IV: Inject the entire volume (25 mL) of itraconazole concentrate into the provided 50 mL NaCl infusion bag over 60 seconds using the dedicated extension line with the 0.2 micrometer in-line filter. Withdraw the needle and gently mix the contents of the bag once the concentrate is completely transferred into the bag. The final concentration of the admixed solution is 3.33 mg itraconazole/mL.
Chống chỉ định
Hypersensitivity. Non-life-threatening indications (e.g. onychomycosis) in patients with evidence of ventricular dysfunction, such as CHF or a history of CHF. Severe renal impairment (IV). Pregnancy (for non-life-threatening cases). Concomitant use with methadone, levacetylmethadol, disopyramide, dofetilide, dronedarone, quinidine, astemizole, mizolastine, terfenadine, halofantrine, isavuconazole, ergot alkaloids (e.g. dihydroergotamine, ergometrine, ergotamine, methylergometrine), irinotecan, lurasidone, oral midazolam, pimozide, sertindole, triazolam, bepridil, felodipine, nisoldipine, lercanidipine, ivabradine, ranolazine, eplerenone, cisapride, domperidone, naloxegol, lomitapide, lovastatin, simvastatin, avanafil, ticagrelor; colchicine, fesoterodine, solifenacin, and telithromycin (in patients with varying degrees of renal or hepatic impairment). Coadministration with eliglustat (in poor or intermediate CYP2D6 metabolisers and those taking strong or moderate CYP2D6 inhibitors).
Thận trọng
Patient with risk factors for CHF (e.g. COPD, oedematous disorders, renal failure, ischaemic or valvular disease), hypersensitivity to other azole antifungals, cystic fibrosis; abnormal gastrointestinal motility, reduced gastric acidity such as achlorhydria (cap). Immunocompromised patients (e.g. neutropenic, AIDS, organ transplant patients). Oral preparations are not recommended for initiation of treatment in patients with immediately life-threatening systemic fungal infections due to pharmacokinetic properties. Oral solution and capsules are not interchangeable. Coadministration with Ca channel blockers or drugs that reduce gastric acidity. Renal and hepatic impairment. Pregnancy (for life-threatening indications); lactation.
Tác dụng không mong muốn
Significant: Transient or permanent hearing loss, peripheral neuropathy (prolonged use), peripheral or pulmonary oedema, hypersensitivity reactions.
Blood and lymphatic system disorders: Granulocytopenia, thrombocytopenia, leucopenia.
Cardiac disorders: Left ventricular failure, tachycardia.
Ear and labyrinth disorders: Tinnitus.
Eye disorders: Visual disturbance, diplopia, blurred vision.
Gastrointestinal disorders: Abdominal pain, nausea, vomiting, diarrhoea, dyspepsia, flatulence, constipation, dysgeusia.
General disorders and administration site conditions: Generalised oedema, face oedema, chest pain, fatigue, chills, pyrexia, pain; inj site inflammation (IV).
Hepatobiliary disorders: Hepatitis, jaundice.
Investigations: Increased ALT/AST, blood alkaline phosphatase, blood lactate dehydrogenase, blood urea, and gamma-glutamyltransferase; abnormal urine analysis.
Metabolism and nutrition disorders: Hyperglycaemia, hyperkalaemia, hypokalaemia, hypomagnesaemia, hyperbilirubinaemia, hypertriglyceridaemia.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia.
Nervous system disorders: Headache, dizziness, somnolence, tremor, paraesthesia.
Psychiatric disorders: Confusional state.
Renal and urinary disorders: Renal impairment, urinary incontinence, pollakiuria.
Reproductive system and breast disorders: Erectile dysfunction, menstrual disorder.
Respiratory, thoracic and mediastinal disorders: Dysphonia, cough, dyspnoea, sinusitis, rhinitis, upper respiratory tract infection.
Skin and subcutaneous tissue disorders: Erythematous rash, rash, hyperhidrosis, alopecia, urticaria, pruritus.
Vascular disorders: Hypertension, hypotension.
Potentially Fatal: CHF or exacerbation of CHF. Rarely, serious hepatotoxicity (including 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.
Chỉ số theo dõi
Monitor hepatic and renal functions, and serum trough concentrations for certain infections; signs and symptoms of CHF and liver toxicity during treatment.
Tương tác
Absorption of itraconazole capsules may be decreased by drugs that neutralise gastric acidity (e.g. Al hydroxide, H2-receptor antagonists, PPIs). Plasma concentrations may be decreased by rifampicin, rifabutin, isoniazid, carbamazepine, phenytoin, phenobarbital, nevirapine, efavirenz. Plasma concentrations may be increased by ciprofloxacin, clarithromycin, erythromycin, ritonavir-boosted darunavir, ritonavir-boosted fosamprenavir, indinavir, ritonavir, telaprevir, cobicistat. May increase the plasma concentrations of tamsulosin, certain opioid analgesics (e.g. alfentanil, sufentanil, buprenorphine, fentanyl, oxycodone), digoxin, certain anticoagulants (e.g. apixaban, rivaroxaban, cilostazol, coumarins, dabigatran), repaglinide, saxagliptin, praziquantel, certain antihistamines (e.g. bilastine, ebastine), certain antineoplastics (e.g. axitinib, docetaxel, dasatinib, vinca alkaloids, trabectedin, trastuzumab emtansine, olaparib, idelalisib, sonidegib, imatinib, panobinostat, busulfan), certain antipsychotics, anxiolytics and hypnotics (e.g. risperidone, alprazolam, buspirone, quetiapine, aripiprazole, haloperidol, midazolam IV), verapamil, nadolol, aliskiren, bosentan, riociguat, aprepitant, certain corticosteroids (e.g. budesonide, fluticasone, methylprednisolone, ciclesonide), salmeterol, certain immunosuppressants (e.g. ciclosporin, tacrolimus), certain urological drugs (e.g. tadalafil, sildenafil, darifenacin, tolterodine), cinacalcet, mozavaptan, tolvaptan, delamanid, artemether and lumefantrine, simeprevir, atorvastatin, alitretinoin. May decrease the plasma concentration of meloxicam.
Potentially Fatal: Increased risk of QT prolongation and ventricular tachyarrhythmia (including torsades de pointes) with disopyramide, dofetilide, dronedarone, quinidine, methadone, levacetylmethadol, astemizole, mizolastine, terfenadine, halofantrine, pimozide, sertindole, bepridil, cisapride, domperidone. Increases the plasma concentrations and the risk of serious adverse effects of isavuconazole, ergot alkaloids (e.g. dihydroergotamine, ergometrine, ergotamine, methylergometrine), irinotecan, lurasidone, oral midazolam, triazolam, felodipine, nisoldipine, lercanidipine, ivabradine, ranolazine, eplerenone, naloxegol, lomitapide, lovastatin, simvastatin, avanafil, ticagrelor; colchicine, fesoterodine, telithromycin and solifenacin (in patients with varying degrees of renal or hepatic impairment); eliglustat (in poor or intermediate CYP2D6 metabolisers and those taking strong or moderate CYP2D6 inhibitors).
Tương tác với thức ăn
Decreased plasma concentration with St. John’s wort. Serum levels may be altered by grapefruit or grapefruit juice. Cap: May enhance absorption with food and acidic beverages. Oral solution: Reduced rate and extent of absorption with food.
Tác dụng
Description: Itraconazole, a triazole derivative antifungal agent, inhibits the fungal CYP450 activity, resulting in decreased ergosterol biosynthesis (the principal sterol in the fungal cell membrane) thereby disrupting membrane synthesis by fungi.
Pharmacokinetics:
Absorption: Rapidly absorbed after oral administration. Enhanced absorption with food for cap, and without food for oral solution. Bioavailability: Approx 55% (oral). Time to peak plasma concentration: 2-5 hours (cap); 2.5 hours (oral solution).
Distribution: Widely distributed with highest concentrations in adipose, omentum, endometrium, cervical and vaginal mucus, skin, and nails, and small amounts into the CSF; also distributed into bronchial exudate and sputum. Enters breast milk (small amount). Volume of distribution: >700 L. Plasma protein binding: 99.8% (as itraconazole) and 99.6% (as hydroxy-itraconazole), mainly to albumin.
Metabolism: Extensively metabolised in the liver mainly via oxidation by CYP3A4 isoenzyme into >30 metabolites, including hydroxy-itraconazole (major metabolite).
Excretion: Mainly via faeces (54%; approx 3-18% as unchanged drug); urine (<1% active drug, 35% as inactive metabolites). Elimination half-life: Oral: 16-28 hours (single dose); 34-42 hours (multiple doses).
Đặc tính

Chemical Structure Image
Itraconazole

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 55283, Itraconazole. https://pubchem.ncbi.nlm.nih.gov/compound/Itraconazole. Accessed Apr. 26, 2022.

Bảo quản
Cap: Store between 15-25°C. Protect from light and moisture. Oral solution: Store at or below 25°C. Do not freeze. Solution for infusion: Store below 25°C. Do not freeze. Protect from light.
Phân loại MIMS
Thuốc kháng nấm
Phân loại ATC
J02AC02 - itraconazole ; Belongs to the class of triazole and tetrazole derivatives. Used in the systemic treatment of mycotic infections.
Tài liệu tham khảo
Anon. Itraconazole. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 28/02/2022.

Anon. Itraconazole. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 28/02/2022.

Buckingham R (ed). Itraconazole. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/02/2022.

Itraconazole 10 mg/mL Concentrate and Solvent for Solution for Infusion (Neon Healthcare Ltd). MHRA. https://products.mhra.gov.uk. Accessed 28/02/2022.

Itraconazole 10 mg/mL Oral Solution (Focus Pharmaceuticals Ltd). MHRA. https://products.mhra.gov.uk. Accessed 28/02/2022.

Itraconazole 100 mg Capsules, Hard (Accord Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 28/02/2022.

Janssen-Cilag (New Zealand) Ltd. Sporanox 10 mg/mL Oral Solution data sheet 7 February 2022. Medsafe. http://www.medsafe.govt.nz. Accessed 28/02/2022.

Joint Formulary Committee. Itraconazole. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/02/2022.

Sporanox Capsule (Janssen Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 28/02/2022.

Sporanox Capsule 100 mg (Johnson & Johnson Sdn Bhd). MIMS Malaysia. http://www.mims.com/malaysia. Accessed 28/02/2022.

Sporanox Oral Solution (Johnson & Johnson Sdn Bhd). MIMS Malaysia. http://www.mims.com/malaysia. Accessed 28/02/2022.

Sporanox Solution (Janssen Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 28/02/2022.

Sporanox-Pulse (Janssen-Cilag Ltd). MHRA. https://products.mhra.gov.uk. Accessed 28/02/2022.

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