Itraconazole (Page 4 of 8)

Drug Interactions:

Effect of Itraconazole Capsules on Other Drugs

Itraconazole and its major metabolite, hydroxy-itraconazole, are potent CYP3A4 inhibitors. Itraconazole is an inhibitor of the drug transporters P-glycoprotein and breast cancer resistance protein (BCRP). Consequently, itraconazole has the potential to interact with many concomitant drugs resulting in either increased or sometimes decreased concentrations of the concomitant drugs. Increased concentrations may increase the risk of adverse reactions associated with the concomitant drug which can be severe or life-threatening in some cases (e.g., QT prolongation, Torsade de Pointes , respiratory depression, hepatic adverse reactions, hypersensitivity reactions, myelosuppression, hypotension, seizures, angioedema, atrial fibrillation, bradycardia, priapism). Reduced concentrations of concomitant drugs may reduce their efficacy. Table 1 lists examples of drugs that may have their concentrations affected by itraconazole, but is not a comprehensive list. Refer to the approved product labeling to become familiar with the interaction pathways, risk potential, and specific actions to be taken with regards to each concomitant drug prior to initiating therapy with itraconazole.

Although many of the clinical drug interactions in Table 1 are based on information with a similar azole antifungal, ketoconazole, these interactions are expected to occur with itraconazole.

Table 1 Drug Interactions with Itraconazole that Affect Concomitant Drug Concentrations
Concomitant Drug Within Class Prevention or Management
Drug Interactions with Itraconazole that Increase Concomitant Drug Concentrations and May Increase Risk of Adverse Reactions Associated with the Concomitant Drug
Alpha Blockers
Alfuzosin Silodosin Tamsulosin Not recommended during and 2 weeks after itraconazole treatment.
Analgesics
Methadone Contraindicated during and 2 weeks after itraconazole treatment.
Fentanyl Not recommended during and 2 weeks after itraconazole treatment.
Alfentanil Buprenorphine (IV and sublingual) Oxycodone a Sufentanil Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Antiarrhythmics
Disopyramide Dofetilide Dronedarone Quinidine a Contraindicated during and 2 weeks after itraconazole treatment.
Digoxin a Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Antibacterials
Bedaquiline b Concomitant itraconazole not recommended for more than 2 weeks at any time during bedaquiline treatment.
Rifabutin Not recommended 2 weeks before, during, and 2 weeks after itraconazole treatment. See also Table 2.
Clarithromycin Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. See also Table 2.
Trimetrexate Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Anticoagulants and Antiplatelets
Ticagrelor Contraindicated during and 2 weeks after itraconazole treatment.
Apixaban Rivaroxaban Vorapaxar Not recommended during and 2 weeks after itraconazole treatment.
Cilostazol Dabigatran Warfarin Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Anticonvulsants
Carbamazepine Not recommended 2 weeks before, during, and 2 weeks after itraconazole treatment. See also Table 2.
Antidiabetic Drugs
Repaglinide a Saxagliptin Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Antihelminthics, Antifungals and Antiprotozoals
Isavuconazonium Contraindicated during and 2 weeks after itraconazole treatment.
Praziquantel Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Artemether-lumefantrine Quinine a Monitor for adverse reactions.
Antimigraine Drugs
Ergot alkaloids (e.g., dihydroergotamine, ergotamine) Contraindicated during and 2 weeks after itraconazole treatment.
Eletriptan Monitor for adverse reactions. Concomitant drug dose reduction may be necessary
Antineoplastics
Irinotecan Contraindicated during and 2 weeks after itraconazole treatment.
Axitinib Bosutinib Cabazitaxel Cabozantinib Ceritinib Cobimetinib a Crizotinib Dabrafenib Dasatinib Docetaxel Ibrutinib Lapatinib Nilotinib Olaparib a Pazopanib Sunitinib Trabectedin Trastuzumab- emtansine Vinca alkaloids Not recommended during and 2 weeks after itraconazole treatment.
Bortezomib Brentuximab- vedotin Busulfan a Erlotinib Gefitinib a Idelalisib Imatinib Ixabepilone Nintedanib Panobinostat Ponatinib Ruxolitinib Sonidegib Vandetanib a Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. For idelalisib, see also Table 2.
Antipsychotics, Anxiolytics and Hypnotics
Alprazolam a Aripiprazole a Buspirone a Cariprazine Diazepam a Haloperidol a Midazolam (IV) a Quetiapine Ramelteon Risperidone a Suvorexant Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Zopiclone a Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Lurasidone Midazolam (oral) a Pimozide Triazolam a Contraindicated during and 2 weeks after itraconazole treatment.
Antivirals
Simeprevir Not recommended during and 2 weeks after itraconazole treatment.
Daclatasvir Indinavir a Maraviroc Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. For indinavir, see also Table 2.
Cobicistat Elvitegravir (ritonavir-boosted) Ombitasvir/Paritaprevir/Ritonavir with or without Dasabuvir Ritonavir Saquinavir (unboosted) a Monitor for adverse reactions. See also Table 2.
Elbasvir/grazoprevir Glecaprevir/pibrentasvir Tenofovir disoproxil fumarate Not recommended during and 2 weeks after itraconazole treatment. Monitor for adverse reactions. Monitor for adverse reactions.
Beta Blockers
Nadolol a Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Calcium Channel Blockers
Felodipine a Nisoldipine Contraindicated during and 2 weeks after itraconazole treatment.
Diltiazem Other dihydropyridines Verapamil Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. For diltiazem, see also Table 2.
Cardiovascular Drugs, Miscellaneous
Ivabradine Ranolazine Contraindicated during and 2 weeks after itraconazole treatment.
Aliskiren a Riociguat Sildenafil (for pulmonary hypertension) Tadalafil (for pulmonary hypertension) Not recommended during and 2 weeks after itraconazole treatment. For sildenafil and tadalafil, see also Urologic Drugs below.
Bosentan Guanfacine Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Contraceptives*
Dienogest Ulipristal Monitor for adverse reactions.
Diuretics
Eplerenone Contraindicated during and 2 weeks after itraconazole treatment.
Gastrointestinal Drugs
Cisapride Naloxegol Contraindicated during and 2 weeks after itraconazole treatment.
Aprepitant Loperamide a Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Netupitant Monitor for adverse reactions.
Immunosuppressants
Everolimus Sirolimus Temsirolimus (IV) Not recommended during and 2 weeks after itraconazole treatment.
Budesonide (inhalation) a Budesonide (non-inhalation) Ciclesonide (inhalation) Cyclosporine (IV) a Cyclosporine (non-IV) Dexamethasone a Fluticasone (inhalation) a Fluticasone (nasal) Methylprednisolone a Tacrolimus (IV) a Tacrolimus (oral) Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Lipid-Lowering Drugs
Lomitapide Lovastatin a Simvastatin a Contraindicated during and 2 weeks after itraconazole treatment.
Atorvastatin a Monitor for drug adverse reactions. Concomitant drug dose reduction may be necessary
Respiratory Drugs
Salmeterol Not recommended during and 2 weeks after itraconazole treatment.
SSRIs, Tricyclics and Related Antidepressants
Venlafaxine Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Urologic Drugs
Avanafil Contraindicated during and 2 weeks after itraconazole treatment.
Fesoterodine Patients with moderate to severe renal or hepatic impairment: Contraindicated during and 2 weeks after itraconazole treatment. Other patients: Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Solifenacin Patients with severe renal or moderate to severe hepatic impairment: Contraindicated during and 2 weeks after itraconazole treatment. Other patients: Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Darifenacin Vardenafil Not recommended during and 2 weeks after itraconazole treatment.
Dutasteride Oxybutynin a Sildenafil (for erectile dysfunction) Tadalafil (for erectile dysfunction and benign prostatic hyperplasia) Tolterodine Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. For sildenafil and tadalafil, see also Cardiovascular Drugs above.
Miscellaneous Drugs and Other Substances
Colchicine Patients with renal or hepatic impairment: Contraindicated during and 2 weeks after itraconazole treatment. Other patients: Not recommended during and 2 weeks after itraconazole treatment.
Eliglustat CYP2D6 EMs c taking a strong or moderate CYP2D6 inhibitor, CYP2D6 IMs c , or CYP2D6 PMs c : Contraindicated during and 2 weeks after itraconazole treatment. CYP2D6 EMs c not taking a strong or moderate CYP2D6 inhibitor : Monitor for adverse reactions. Eliglustat dose reduction may be necessary.
Lumacaftor/Ivacaftor Not recommended 2 weeks before, during, and 2 weeks after itraconazole treatment.
Alitretinoin (oral) Cabergoline Cannabinoids Galantamine Cinacalcet Ivacaftor Monitor for adverse reactions. Concomitant drug dose reduction may be necessary.
Vasopressin Receptor Antagonists
Conivaptan Tolvaptan Not recommended during and 2 weeks after itraconazole treatment.
Drug Interactions with Itraconazole that Decrease Concomitant Drug Concentrations and May Reduce Efficacy of the Concomitant Drug
Antineoplastics
Regorafenib Not recommended during and 2 weeks after itraconazole treatment.
Gastrointestinal Drugs
Saccharomyces boulardii Not recommended during and 2 weeks after itraconazole treatment.
Nonsteroidal Anti-Inflammatory Drugs
Meloxicam a Concomitant drug dose increase may be necessary.

*CYP3A4 inhibitors (including itraconazole) may increase systemic contraceptive hormone concentrations.

a Based on clinical drug interaction information with itraconazole.

b Based on 400 mg bedaquiline once daily for 2 weeks.

c EMs: extensive metabolizers; IMs: intermediate metabolizers, PMs: poor metabolizers

Effect of Other Drugs on Itraconazole

Itraconazole is mainly metabolized through CYP3A4. Other substances that either share this metabolic pathway or modify CYP3A4 activity may influence the pharmacokinetics of itraconazole. Some concomitant drugs have the potential to interact with itraconazole resulting in either increased or sometimes decreased concentrations of itraconazole. Increased concentrations may increase the risk of adverse reactions associated with itraconazole. Decreased concentrations may reduce itraconazole efficacy.

Table 2 lists examples of drugs that may affect itraconazole concentrations, but is not a comprehensive list. Refer to the approved product labeling to become familiar with the interaction pathways, risk potential and specific actions to be taken with regards to each concomitant drug prior to initiating therapy with itraconazole.

Although many of the clinical drug interactions in Table 2 are based on information with a similar azole antifungal, ketoconazole, these interactions are expected to occur with itraconazole.

Table 2. Drug Interactions with Other Drugs that Affect Itraconazole Concentrations
Concomitant Drug Within Class Prevention or Management
Drug Interactions with Other Drugs that Increase Itraconazole Concentrations and May Increase Risk of Adverse Reactions Associated with Itraconazole
Antibacterials
Ciprofloxacin a Erythromycin a Clarithromycin a Monitor for adverse reactions. Itraconazole dose reduction may be necessary.
Antineoplastics
Idelalisib Monitor for adverse reactions. Itraconazole dose reduction may be necessary. See also Table 1.
Antivirals
Cobicistat Darunavir (ritonavir-boosted) Elvitegravir (ritonavir-boosted) Fosamprenavir (ritonavir-boosted) Indinavir a Ombitasvir/ Paritaprevir/ Ritonavir with or without Dasabuvir Ritonavir Saquinavir Monitor for adverse reactions. Itraconazole dose reduction may be necessary. For, cobicistat, elvitegravir, indinavir, ombitasvir/ paritaprevir/ ritonavir with or without dasabuvir, ritonavir, and saquinavir, see also Table 1.
Calcium Channel Blockers
Diltiazem Monitor for adverse reactions. Itraconazole dose reduction may be necessary. See also Table 1.
Drug Interactions with Other Drugs that Decrease itraconazole Concentrations and May Reduce Efficacy of itraconazole
Antibacterials
Isoniazid Rifampicin a Not recommended 2 weeks before and during itraconazole treatment.
Rifabutin a Not recommended 2 weeks before, during, and 2 weeks after itraconazole treatment. See also Table 1.
Anticonvulsants
Phenobarbital Phenytoin a Not recommended 2 weeks before and during itraconazole treatment.
Carbamazepine Not recommended 2 weeks before, during, and 2 weeks after itraconazole treatment. See also Table 1.
Antivirals
Efavirenz a Nevirapine a Not recommended 2 weeks before and during itraconazole treatment.
Gastrointestinal Drugs
Drugs that reduce gastric acidity e.g. acid neutralizing medicines such as aluminum hydroxide, or acid secretion suppressors such as H 2 -receptor antagonists and proton pump inhibitors. Use with caution. Administer acid neutralizing medicines at least 2 hours before or 2 hours after the intake of itraconazole capsules
Miscellaneous Drugs and Other Substances
Lumacaftor/Ivacaftor Not recommended 2 weeks before, during, and 2 weeks after itraconazole treatment.

a Based on clinical drug interaction information with itraconazole.

Pediatric Population

Interaction studies have only been performed in adults.

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