Drug information of Itraconazole

Mechanism of effect

Itraconazole inhibits the cytochrome P450-dependent synthesis of ergosterol, which is a vital component of fungal cell membranes.

Pharmacodynamic

Itraconazole is an azole antifungal agent. Itraconazole is an imidazole/triazole type antifungal agent. Itraconazole is a highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethylation via the inhibition of the enzyme cytochrome P450 14α-demethylase.

Pharmacokinetics

Itraconazole is rapidly absorbed after oral administration. Peak plasma concentrations of Itraconazole are reached within 2 to 5 hours following an oral capsule dose. The oral bioavailability of Itraconazole is maximal when Itraconazole Capsules are taken immediately after a full meal. Most of the Itraconazole in plasma is bound to protein (99.8%), with albumin being the main binding component . Itraconazole is extensively metabolized by the liver . Itraconazole is excreted mainly as inactive metabolites in urine (35%) and in feces (54%). As re-distribution of Itraconazole from keratinous tissues appears to be negligible, elimination of Itraconazole from these tissues is related to epidermal regeneration.

Drug indications

fungal infections

Dosage

Usual Adult Dose for Systemic Fungal Infection
Empirical therapy: 200 mg orally twice a day
Usual Adult Dose for Fungal Infection Prophylaxis
Antifungal prophylaxis for patients with chemotherapy-induced neutropenia: 200 mg orally twice a day
Usual Pediatric Dose for Oral Thrush
Oropharyngeal candidiasis in patients 5 years or older: 2.5 mg/kg orally twice a day

Drug contraindications

hypersensitivity to drug or its components. , congestive heart failure

Side effects

nausea , Headache , abdominal pain , dizziness , vomiting , fatigue , Hepatic dysfunction , rash , Diarrhea , pruritus , Hypertension , edema , fever , impotence , anorexia , somnolence , malaise , Hypokalemia , decreased libido

Interactions

Aluminium MGS , Amlodipine/Atorvastatine , Aprepitant , Erlotinib , Esomeprazole , Everolimus , Oxybutynin , Ipratropium bromide , Erythromycin , Irinotecan , Ciprofloxacin , Cisapride , Midazolam , Clarithromycin , Colchicine , Ifosfamide , Imatinib , Bromocriptine , Budesonide , Buspirone , Pantoprazole , pimecrolimus , Tadalafil , Tamsulosin , Trazodone , Topotecan , Daunorubicin , Deflazacort , Dexamethasone , Domperidone , Zolpidem , Zonisamide , Sunitinib , Sodium bicarbonate , Sildenafil , Cilostazol , Cyclosporine , Fluticasone propinate , Flurazepam , Lansoprazole , Lapatinib , Loratadin , Lovastatin , Methylergonovin , Methylprednisolone , Nilotinib , Nimodipine , Vardenafil , Venlafaxine , Vinblastin , Vincristin , Vinorelbine , Carbamazepine , Solifenacin , Enzalutamide , Disulfiram , Bisoprolol , eplerenone , fentanyl , Ranolazine , astemizole , propoxyphene , Axitinib , Almotriptan , ritonavir , nelfinavir , eletriptan , Apixaban , Ivabradine , Mifepristone , Afatinib , Droperidol , sparfloxacin , Indinavir , Procainamide , Mefloquine , Indapamide , Dofetilide , Ticagrelor , brigatinib , Abiraterone , Budesonide , nasal Mometasone , Dutasteride , Copanlisib , Tipranavir , Simeprevir , lumacaftor and Ivacaftor , Dabrafenib , Acalabrutinib , Cabazitaxel , Maraviroc , Halofantrine , Darifenacin , Mibefradil , Nicardipine , Nisoldipine , Terfenadine , Fesoterodine , Alfuzosin , Aliskiren , Ergoloid Mesylate , Erdafitinib , Palbociclib , Pimavanserin , Tasimelteon , Betrixaban , Dexlansoprazole , trabectedine , elagolix , Sonidegib , Flibanserin , Crizotinib , Avanafil , Edoxaban , Entrectinib , Methscopolamine , Levomilnacipran , Temsirolimus , ELBASVIR/GRAZOPREVIR , Larotrectinib , gilteritinib , glasdegib , Abemaciclib , Eliglustat , Ruxolitinib , tolvaptan , Bepridil , bazedoxifene/conjugated estrogens , Gefitinib , Dasatinib , Remdesivir , Cannabidiol , talazoparib , vemurafenib , vorapaxar , Macitentan , voxelotor , Avapritinib , Fidaxomicin , Capmatinib

Alerts

1- If clinical signs or symptoms develop that are consistent with liver disease, treatment should be discontinued and liver function testing performed.
2- Because hypochlorhydria has been reported in HIV-infected individuals, the absorption of Itraconazole in these patients may be decreased.

Points of recommendation

1-Itraconazole Capsules should be administered after a full meal.
2- Advise patients to discontinue therapy and inform their physicians if any hearing loss symptoms occur.
3- Instruct patients that dizziness or blurred/double vision can sometimes occur with Itraconazole. Advise patients that if they experience these events, they should not drive or use machines.

Pregnancy level

C

Related drugs

Voriconazole , Ketoconazole , miconazol