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.
Interaction studies have only been performed in adults.
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