tolsura
Pharmaranks rates Tolsura 3.5/5 for recall safety — an independent score from its FDA recall history and its manufacturer's record. Tolsura (Itraconazole) is an azole antifungal used to treat Aspergillosis, Blastomycosis, Chronic Mucocutaneous Candidiasis, Oral Candidiasis.
Itraconazole · by Mayne Pharma
Based on 1 source · Recall-safety score from FDA recall history — this product's own recalls and its manufacturer's record. Not an efficacy or quality rating. methodology →
Key facts
- Active ingredient
- Itraconazole
- Drug class
- Azole Antifungal
- Form
- Capsule
- Strength
- Itraconazole 65MG
- Type
- Prescription (Rx)
- Brand or generic
- Brand-name
- Manufacturer
- Mayne Pharma
- Half-life
- Terminal (elimination) half-life is about 16 to 28 hours after a single dose, rising to roughly 34 to 42 hours with repeated (steady-state) dosing. (how long it stays in your system)
- What the pharmacy pays
- ~$0.84 per ml — not your price
- FDA application
- NDA208901
- FDA boxed warning
- Yes — see the boxed warning
What is Tolsura?
From the FDA label:TOLSURA (itraconazole capsules) is an azole antifungal drug for oral use. Itraconazole is an equal mixture of four diastereomers (two enantiomeric pairs), each possessing three chiral centers. It may be represented by the following structural formula and nomenclature: (±)-1-[( R *)- sec -butyl]-4-[ p -[4-[ p -[[(2 R *,4 S *)-2-(2,4-dichlorophenyl)-2-(1 H -1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-Δ 2 -1,2,4-triazolin-5-one mixture with (±)-1-[( R *)- sec -butyl]-4-[ p -[4-[ p -[[(2 S *,4 R *)-2-(2,4-dichlorophenyl)-2-(1 H -1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-Δ 2 -1,2,4-triazolin-5-one or (±)-1-[( RS )- sec -butyl]-4-[ p -[4-[ p -[[(2 R ,4 S )-2-(2,4-dichlorophenyl)-2-(1 H -1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-Δ 2 -1,2,4-triazolin-5-one. Itraconazole has a molecular formula of C 35 H 38 Cl 2 N 8 O 4 and a molecular weight of 705.64. It is a white to slightly yellowish powder. It is insoluble in water, very slightly soluble in alcohols, and freely soluble in dichloromethane. It has a pKa of 3.70 (based on extrapolation of values obtained from methanolic solutions) and a log (n-octanol/water) partition coefficient of 5.66 at pH 8.1. Each TOLSURA capsule contains 65 mg of itraconazole dispersed in a polymer matrix and encapsulated in a hard gelatin…
How to use
TOLSURA must be administered with food. TOLSURA capsules must be swallowed whole. Do not chew, crush or break TOLSURA capsules. Table 1 below describes the recommended dosage for TOLSURA. Table 1: Dosage and Administration of TOLSURA Indications Daily Dosing Treatment of Blastomycosis and Histoplasmosis Recommended dose 130 mg (2 × 65 mg capsules) once daily If no obvious improvement, or there is evidence of progressive fungal disease, the dose should be increased in 65 mg increments to a maximum of 260 mg/day (130 mg (2 × 65 mg capsules) twice daily). Doses above 130 mg/day should be given in two divided doses. Treatment of Aspergillosis Recommended dose 130 mg (2 × 65 mg capsules) once daily 260 mg/day (130 mg (2 × 65 mg capsules) twice daily) Treatment in Life-Threatening Situations Although clinical studies did not provide for a loading dose, it is recommended, based on pharmacokinetic data, that a loading dose should be used. A loading dose of 130 mg (2 × 65 mg capsules) three times daily (390 mg/day) is recommended to be given for the first 3 days, followed by the appropriate recommended dosing based on indication. Treatment should be continued for a minimum of three months and until clinical parameters and laboratory tests indicate that the active fungal infection has subsided. An inadequate period of treatment may lead to recurrence of active infection. Blastomycosis…
Side effects
The following clinically significant adverse reactions are described elsewhere in the labeling: Congestive Heart Failure [see Warnings and Precautions (5.1) ] Hepatotoxicity [see Warnings and Precautions (5.2) ] Cardiac Dysrhythmias [see Warnings and Precautions (5.3) ] Pseudoaldosteronism [see Warnings and Precautions (5.4) ] Peripheral Neuropathy [see Warnings and Precautions (5.6) ] Hearing Loss [see Warnings and Precautions (5.7) ] Hypersensitivity Reactions [see Warnings and Precautions (5.8) ] Most common adverse reactions (incidence ≥ 1%) are nausea, rash, vomiting, edema, headache, diarrhea, fatigue, fever, pruritus, hypertension, abnormal hepatic function, abdominal pain, dizziness, hypokalemia, anorexia, malaise, decreased libido, somnolence, albuminuria, impotence ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Mayne Pharma at 1-844-825-8500 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Adverse Reactions in the Treatment of Systemic Fungal Infections Safety data with itraconazole capsules were derived from 602 patients treated for systemic fungal disease…
FDA Boxed Warning (the FDA’s most serious warning)
Boxed (black-box) warning — from the FDA label
CONGESTIVE HEART FAILURE and DRUG INTERACTIONS WARNING: CONGESTIVE HEART FAILURE and DRUG INTERACTIONS See full prescribing information for complete boxed warning. Congestive Heart Failure TOLSURA can cause or exacerbate congestive heart failure (CHF). When itraconazole was administered intravenously to healthy human volunteers and dogs, negative inotropic effects were seen. If signs or symptoms of congestive heart failure occur or worsen during administration of TOLSURA, reassess the benefit-risk of continuing treatment. ( 5.1 , 6 ). Drug Interactions Co-administration of certain drugs that are metabolized by human CYP3A4 enzymes are contraindicated with TOLSURA because plasma concentrations of such drugs are increased. ( 4.1 , 5.5 , 7.1 ) Co-administration with colchicine, fesoterodine and solifenacin is contraindicated in subjects with varying degrees of renal or hepatic impairment. ( 4.1 , 7.1 ) Co-administration with eliglustat is contraindicated in poor or intermediate metabolizers of CYP2D6 and in subjects taking strong or moderate CYP2D6 inhibitors. ( 4.1 , 7.1 ) Increased plasma concentrations of some of these drugs can lead to QT prolongation and ventricular tachyarrhythmias including occurrences of torsades de pointes, a potentially fatal arrhythmia. ( 4.1 , 5.5 , 7.1 ) Congestive Heart Failure TOLSURA can cause or exacerbate congestive heart failure (CHF). When itraconazole was administered intravenously to healthy human volunteers and dogs, negative inotropic effects were seen. If signs or symptoms of congestive heart failure occur or worsen during administration of TOLSURA, reassess the benefit and risk of continuing treatment [ see Warnings and Precautions (5.1) and Adverse Reactions (6.1) ] . Drug Interactions Co-administration of certain drugs that are metabolized by human CYP3A4 enzymes are contraindicated with TOLSURA because plasma concentrations of such drugs are increased, which may also increase or prolong both the pharmacologic effects and/or adverse reactions to these drugs [see Contraindications (4.1) and Drug Interactions (7.1) ] Co-administration with colchicine, fesoterodine and solifenacin is contraindicated in subjects with varying degrees of renal or hepatic impairment, and Co-administration with eliglustat is contraindicated in subjects that are poor or intermediate metabolizers of CYP2D6 and in subjects taking strong or moderate CYP2D6 inhibitors. Increased plasma concentrations of some of these drugs caused by co-administration with TOLSURA can lead to QT prolongation and/or ventricular tachyarrhythmias, including occurrences of torsades de pointes , a potentially fatal arrhythmia [see Contraindications (4.1) , Warnings and Precautions (5.5) and Drug Interactions (7.1) ] .
Warnings
Important safety information
Hepatotoxicity : Serious hepatotoxicity, including liver failure and death were reported with the use of itraconazole. Discontinue treatment if signs of liver dysfunction occur ( 5.2 ) Cardiac Dysrhythmias : Life-threatening cardiac dysrhythmias and/or sudden death have occurred in patients using certain drugs that are metabolized by human CYP450 enzymes concomitantly with oral itraconazole and/or other CYP3A4 inhibitors. ( 4 , 5.3 , 5.5 ) Pseudoaldosteronism : Manifested by the onset or worsening of hypertension, and abnormal laboratory findings. Monitor blood pressure and potassium levels and manage as necessary ( 5.4 ). Peripheral Neuropathy : This has been reported in patients on long-term therapy with itraconazole. Monitor and promptly evaluate neurologic symptoms. ( 5.6 ) Hearing Loss : Reversible or permanent has been reported in patients. Discontinue treatment if hearing loss occurs ( 5.7 ) 5.1 Congestive Heart Failure TOLSURA can cause or exacerbate congestive heart failure (CHF) [see Boxed Warning and Adverse Reactions (6.1) ]. For patients with evidence of ventricular dysfunction such as CHF, history or risk factors for CHF, physicians should carefully review the risks and benefits of TOLSURA therapy. These risk factors include cardiac disease such as ischemic and valvular disease; significant pulmonary disease such as chronic obstructive pulmonary disease; and renal failure and other edematous disorders. Inform such patients of the signs and symptoms of CHF and monitor carefully for signs and symptoms of CHF during treatment. If signs or symptoms of CHF appear or worsen during administration of TOLSURA, reassess the benefit-risk of continuing treatment. When itraconazole was administered intravenously to anesthetized dogs, a dose-related negative inotropic effect was demonstrated. In a healthy volunteer study of itraconazole intravenous infusion, transient, asymptomatic decreases in left ventricular ejection fraction were observed using gated SPECT imaging; these resolved before the next infusion, 12 hours later. Itraconazole has been associated with reports of CHF, peripheral edema, and pulmonary edema. In post-marketing experience, heart failure was more frequently reported in patients receiving higher total daily doses of itraconazole of 400 mg although there were also cases reported among those receiving lower total daily doses [see Adverse Reactions (6.2) ] . Calcium channel blockers can have negative inotropic effects which may be additive to those of itraconazole. In addition, itraconazole can inhibit the metabolism of calcium channel blockers. Therefore, when co-administering itraconazole and calcium channel blockers, monitor carefully for signs and symptoms of CHF during treatment due to an increased risk of CHF. Concomitant administration of TOLSURA and felodipine or nisoldipine is contraindicated [see Contraindications (4.1) , Drug Interactions (7.1) and Adverse Reactions (6.2) ] 5.2 Hepatotoxicity Itraconazole has been associated with cases of serious hepatotoxicity, including liver failure and death. Some of these cases had neither pre-existing liver disease nor a serious underlying medical condition, and some of these cases developed within the first week of treatment. If clinical signs or symptoms develop that are consistent with liver disease, discontinue treatment and perform testing for liver disease. Continued TOLSURA use or reinstitution of treatment with TOLSURA is strongly discouraged unless there is a serious or life-threatening situation where the expected benefit exceeds the risk [ see Adverse Reactions (6.1) ]. 5.3 Cardiac Dysrhythmias Life-threatening cardiac dysrhythmias and/or sudden death have occurred in patients using drugs such as, pimozide, methadone, or quinidine concomitantly with oral itraconazole and/or other CYP3A4 inhibitors. Concomitant administration of these drugs with TOLSURA is contraindicated [see Boxed Warning , Contraindications (4) and Drug Interactions (7) ]. 5.4 Pseudoaldosteronism Pseudoaldosteronism, manifested by the onset of hypertension or worsening of hypertension, and abnormal laboratory findings (hypokalemia, low serum renin and aldosterone, and elevate 11-deoxycortisol), has been reported with itraconazole use in the postmarketing setting. Monitor blood pressure and potassium levels and manage as necessary. Management of pseudoaldosteronism may include discontinuation of TOLSURA, substitution with an appropriate antifungal drug that is not associated with pseudoaldosteronism, or use of aldosterone receptor antagonists. 5.5 Drug Interaction Potential Itraconazole has a potential for clinically important drug interactions [see Drug Interactions (7.1 , 7.2) ] . Co-administration of specific drugs with TOLSURA may result in changes in the efficacy of itraconazole and/or the co-administered drug, life-threatening effects and/or sudden death. [see Boxed Warning , Contraindications (4.1) and Drug Interactions (7.1 , 7.2) ]. 5.6 Peripheral Neuropathy Cases of peripheral neuropathy have been reported in patients on long-term therapy with itraconazole. Monitor for and promptly evaluate neurologic symptoms. If neuropathy attributable to TOLSURA occurs, discontinue treatment. 5.7 Hearing Loss Reversible or permanent hearing loss has been reported in patients receiving treatment with itraconazole. Several of these reports included concurrent administration of quinidine which is contraindicated [see Boxed Warning , Contraindications (4.2) and Drug Interactions (7) ] . The hearing loss usually resolves when treatment is stopped but can persist in some patients. 5.8 Hypersensitivity Reactions TOLSURA is contraindicated in patients with a known hypersensitivity to itraconazole [see Contraindications (4.2) ]. Hypersensitivity reactions have been reported with the use of itraconazole [see Adverse Reactions (6.2) ] . Due to the limited information regarding cross-hypersensitivity between itraconazole and other azole antifungal drugs, careful enquiry about previous hypersensitivity to other azole antifungal drugs should be made when prescribing TOLSURA. If hypersensitivity reactions to TOLSURA occurs, discontinue the drug and institute appropriate therapy.
Who should not take Tolsura
Co-administration with certain drugs that either affect metabolism of itraconazole or whose metabolism is affected by itraconazole. ( 4.1 ) Hypersensitivity to itraconazole ( 4.2 ) 4.1 Drug Interactions Co-administration of certain drugs that are metabolized by human CYP3A4 substrates are contraindicated with TOLSURA because plasma concentrations of such drugs are increased, which may also increase or prolong both the pharmacologic effects and/or adverse reactions to these drugs [see Warnings and Precaution (5.5) and Drug Interactions (7.1) ] . Co-administration with colchicine, fesoterodine and solifenacin is contraindicated in subjects with varying degrees of renal or hepatic impairment. Co-administration with eliglustat is contraindicated in subjects that are poor or intermediate metabolizers of CYP2D6 and in subjects taking strong or moderate CYP2D6 inhibitors [see Drug Interactions (7.1) ] . Increased plasma concentrations of some of these drugs due to co-administration of TOLSURA can lead to QT prolongation and ventricular tachyarrhythmias including occurrences of torsade de pointes , a potentially fatal arrhythmia [ see Drug Interactions (7.1) ] . 4.2 Hypersensitivity TOLSURA is contraindicated in patients with known hypersensitivity to itraconazole. There is limited information regarding cross-hypersensitivity between itraconazole and other azole antifungal agents [see Warnings and Precautions (5.8) ] .
Overdose — what happens if you take too much
Itraconazole is not removed by dialysis. In the event of accidental overdosage, supportive measures should be employed. Activated charcoal may be given if considered appropriate.
U.S. Poison Control: call or text 1-800-222-1222 (free, 24/7). In an emergency call 911. From the FDA label; not medical advice.
Interactions
Itraconazole is mainly metabolized through CYP3A4. Other drugs that either share this metabolic pathway or modify CYP3A4 activity may influence the pharmacokinetics of itraconazole. ( 4 , 5 , 7.1 , 7.2 ) 7.1 Effect of TOLSURA 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 4 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 4 are based on information with a similar azole antifungal, ketoconazole, these interactions are expected to occur with itraconazole. Table 4: Drug Interactions with TOLSURA that Affect Concomitant Drug Concentrations Concomitant Drug Within Class Prevention or Management Drug Interactions with TOLSURA 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 TOLSURA treatment. Analgesics Methadone Contraindicated during and 2 weeks after TOLSURA treatment. Fentanyl Not recommended during and 2 weeks after TOLSURA treatment. Alfentanil Buprenorphine (IV and sublingual) Oxycodone Based on clinical drug interaction information with itraconazole. Sufentanil Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. Antiarrhythmics Disopyramide Dofetilide Dronedarone Quinidine Contraindicated during and 2 weeks after TOLSURA treatment. Digoxin Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. Antibacterials Bedaquiline Based on 400 mg Bedaquiline once daily for 2 weeks. Concomitant TOLSURA not recommended for more than 2 weeks at any time during bedaquiline treatment. Rifabutin Not recommended 2 weeks before, during, and 2 weeks after TOLSURA treatment. See also Table 5 . Clarithromycin Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. See also Table 5 . Trimetrexate Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. Anticoagulants and Antiplatelets Ticagrelor Contraindicated during and 2 weeks after TOLSURA treatment. Apixaban Rivaroxaban Vorapaxar Not recommended during and 2 weeks after TOLSURA 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 TOLSURA treatment. See also Table 5 . Antidiabetic Drugs Repaglinide Saxagliptin Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. Antihelminthics, Antifungals and Antiprotozoals Isavuconazonium Contraindicated during and 2 weeks after TOLSURA treatment. Praziquantel Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. Artemether-lumefantrine Quinine Monitor for adverse reactions. Antimigraine Drugs Ergot alkaloids (e.g., dihydroergotamine, ergotamine) Contraindicated during and 2 weeks after TOLSURA treatment. Eletriptan Monitor for adverse reactions. Concomitant drug dose reduction may be necessary Antineoplastics Irinotecan Contraindicated during and 2 weeks after TOLSURA treatment. Axitinib Bosutinib Cabazitaxel Cabozantinib Ceritinib Cobimetinib Crizotinib Dabrafenib Dasatinib Docetaxel Ibrutinib Lapatinib Nilotinib Olaparib Pazopanib Sunitinib Trabectedin Trastuzumab-emtansine Vinca alkaloids Not recommended during and 2 weeks after TOLSURA treatment. Bortezomib Brentuximab-vedotin Busulfan Erlotinib Gefitinib Idelalisib Imatinib Ixabepilone Nintedanib Panobinostat Ponatinib Ruxolitinib Sonidegib Vandetanib Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. For Idelalisib, see also Table 5 . Antipsychotics, Anxiolytics and Hypnotics Alprazolam Aripiprazole Buspirone Diazepam Haloperidol Midazolam (IV) Quetiapine Ramelteon Risperidone Suvorexant Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. Zopiclone Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. Lurasidone Midazolam (oral) Pimozide Triazolam Contraindicated during and 2 weeks after TOLSURA treatment. Antivirals Simeprevir Not recommended during and 2 weeks after TOLSURA treatment. Daclatasvir Indinavir Maraviroc Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. For indinavir, see also Table 5 . Cobicistat Elvitegravir (ritonavir-boosted) Ritonavir Saquinavir (unboosted) Monitor for adverse reactions. See also Table 5 . Tenofovir disoproxil fumarate Monitor for adverse reactions. Beta Blockers Nadolol Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. Calcium Channel Blockers Felodipine Nisoldipine Contraindicated during and 2 weeks after TOLSURA treatment. Diltiazem Other dihydropyridines Verapamil Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. For diltiazem, see also Table 5 . Cardiovascular Drugs, Miscellaneous Ivabradine Ranolazine Contraindicated during and 2 weeks after TOLSURA treatment. Aliskiren Riociguat Sildenafil (for pulmonary hypertension) Tadalafil (for pulmonary hypertension) Not recommended during and 2 weeks after TOLSURA 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 TOLSURA treatment. Gastrointestinal Drugs Naloxegol Contraindicated during and 2 weeks after TOLSURA treatment. Aprepitant Loperamide 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 TOLSURA treatment. Budesonide (inhalation) Budesonide (noninhalation) Ciclesonide (inhalation) Cyclosporine (IV) Cyclosporine (non-IV) Dexamethasone Fluticasone (inhalation) Fluticasone (nasal) Methylprednisolone Tacrolimus (IV) Tacrolimus (oral) Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. Lipid-Lowering Drugs Lomitapide Lovastatin Simvastatin Contraindicated during and 2 weeks after TOLSURA treatment. Atorvastatin Monitor for drug adverse reactions. Concomitant drug dose reduction may be necessary . Respiratory Drugs Salmeterol Not recommended during and 2 weeks after TOLSURA 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 TOLSURA treatment. Fesoterodine Patients with moderate to severe renal or hepatic impairment : Contraindicated during and 2 weeks after TOLSURA 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 TOLSURA treatment. Other patients : Monitor for adverse reactions. Concomitant drug dose reduction may be necessary. Darifenacin Vardenafil Not recommended during and 2 weeks after TOLSURA treatment. Dutasteride Oxybutynin 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 TOLSURA treatment. Other patients : Not recommended during and 2 weeks after TOLSURA treatment. Eliglustat CYP2D6 EMs EMs: extensive metabolizers; IMs: intermediate metabolizers, PMs: poor metabolizers. taking a strong or moderate CYP2D6 inhibitor, CYP2D6 IMs , or CYP2D6 PMs : Contraindicated during and 2 weeks after TOLSURA treatment. CYP2D6 EMs 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 TOLSURA treatment. Alitretinoin (oral) Cabergoline Cannabinoids 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 TOLSURA treatment. Drug Interactions with TOLSURA that Decrease Concomitant Drug Concentrations and May Reduce Efficacy of the Concomitant Drug Antineoplastics Regorafenib Not recommended during and 2 weeks after TOLSURA treatment. Gastrointestinal Drugs Saccharomyces boulardii Not recommended during and 2 weeks after TOLSURA treatment. Nonsteroidal Anti-Inflammatory Drugs Meloxicam Concomitant drug dose increase may be necessary. 7.2 Effect of Other Drugs on TOLSURA 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 TOLSURA resulting in either increased or sometimes decreased concentrations of TOLSURA. Increased concentrations may increase the risk of adverse reactions associated with TOLSURA. Decreased concentrations may reduce TOLSURA efficacy. Table 4 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 TOLSURA. Although many of the clinical drug interactions in Table 5 are based on information with a similar azole antifungal, ketoconazole, these interactions are expected to occur with TOLSURA. Table 5: Drug Interactions with Other Drugs that Affect TOLSURA Concentrations Concomitant Drug Within Class Prevention or Management Drug Interactions with Other Drugs that Increase TOLSURA Concentrations and May Increase Risk of Adverse Reactions Associated with TOLSURA Antibacterials Ciprofloxacin Based on clinical drug interaction information with itraconazole. Erythromycin Clarithromycin Monitor for adverse reactions. TOLSURA dose reduction may be necessary. Antineoplastics Idelalisib Monitor for adverse reactions. TOLSURA dose reduction may be necessary. See also Table 4 . Antivirals Cobicistat Darunavir (ritonavir-boosted) Elvitegravir (ritonavir-boosted) Fosamprenavir (ritonavir-boosted) Indinavir Ritonavir Saquinavir Monitor for adverse reactions. TOLSURA dose reduction may be necessary. For, cobicistat, elvitegravir, indinavir, ritonavir, and saquinavir, see also Table 4 . Calcium Channel Blockers Diltiazem Monitor for adverse reactions. TOLSURA dose reduction may be necessary. See also Table 4 . 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 (e.g., omeprazole). Co-administration of these drugs, including omeprazole, with TOLSURA increases the systemic exposure to itraconazole. Monitor for adverse reactions. TOLSURA dose reduction may be necessary [see Clinical Pharmacology (12.3) ]. Drug Interactions with Other Drugs that Decrease TOLSURA Concentrations and May Reduce Efficacy of TOLSURA Antibacterials Isoniazid Rifampicin Not recommended 2 weeks before and during TOLSURA treatment. Rifabutin Not recommended 2 weeks before, during, and 2 weeks after TOLSURA treatment. See also Table 4 . Anticonvulsants Phenobarbital Phenytoin Not recommended 2 weeks before and during TOLSURA treatment. Carbamazepine Not recommended 2 weeks before, during, and 2 weeks after TOLSURA treatment. See also Table 4 . Antivirals Efavirenz Nevirapine Not recommended 2 weeks before and during TOLSURA treatment. Miscellaneous Drugs and Other Substances Lumacaftor/Ivacaftor Not recommended 2 weeks before, during, and 2 weeks after TOLSURA treatment.
How long does Itraconazole stay in your body?
The elimination half-life of itraconazole is Terminal (elimination) half-life is about 16 to 28 hours after a single dose, rising to roughly 34 to 42 hours with repeated (steady-state) dosing. — the time it takes the body to clear about half of it. As a rule of thumb, a medicine is mostly gone after roughly 4 to 5 half-lives, though this varies from person to person with age and kidney or liver function. The label reports the terminal half-life explicitly (not a distribution phase). Itraconazole has an ACTIVE metabolite, hydroxy-itraconazole, whose in-vitro antifungal activity is comparable to the parent and whose trough plasma concentrations are about twice those of itraconazole, so effective antifungal exposure persists beyond the parent's half-life. Populations: in cirrhotic (hepatic impairment) subjects the elimination half-life roughly doubled to about 37 hours (vs ~16 hours in healthy subjects after a single 100 mg capsule). In renal impairment, the mean terminal half-life was similar to healthy subjects (range of means ~42-49 hours vs 48 hours after a single IV dose), though overall AUC exposure fell ~30-40% in moderate-to-severe impairment; dialysis has no effect on itraconazole or hydroxy-itraconazole half-life. The label does not give a separate geriatric half-life. Note also non-linear pharmacokinetics: itraconazole accumulates with multiple dosing (clearance saturates), which is why the half-life lengthens at steady state.
This is general information, not medical advice. It doesn’t tell you when a drug test would read negative (tests detect substances for different, often longer, windows) or when it’s safe to take another dose — ask your pharmacist or prescriber. Source: Itraconazole capsules — FDA label (DailyMed), Clinical Pharmacology, Pharmacokinetics and Metabolism.
Drug class
How this class works, per Antifungal Ergosterol Synthesis Inhibitors — StatPearls, NCBI Bookshelf (NIH).
May treat (source: NIH RxClass)
- aspergillosis
- blastomycosis
- chronic mucocutaneous candidiasis
- oral candidiasis
- vulvovaginal candidiasis
- coccidioidomycosis
See how Tolsura ranks — best-rated azole antifungal for:
Dosage forms
Capsule
The forms currently marketed in the U.S., per the FDA National Drug Code Directory.
Ways to save
Ask for the generic
Same active ingredient, far cheaper. Is there a generic? →
Request a 90-day supply
Bulk fills usually lower the per-dose price vs monthly refills.
Use copay cards
Manufacturer copay cards & patient-assistance programs — especially for brand drugs.
Compare alternatives
A same-class option may cost less. See alternatives →
Frequently asked questions
- What does Tolsura treat?
- Tolsura (Itraconazole) may be used to treat aspergillosis, blastomycosis, chronic mucocutaneous candidiasis, oral candidiasis, vulvovaginal candidiasis, coccidioidomycosis, based on NIH RxClass drug-classification data (conditions a drug may treat — not a verbatim copy of the FDA-approved label). This is general reference, not medical advice.
- How does Tolsura work?
- Tolsura is a azole antifungal. Azole antifungals block a fungal enzyme (lanosterol 14-alpha-demethylase) that the fungus needs to make ergosterol, a key building block of its cell membrane. Without enough ergosterol the membrane becomes leaky and unstable, which stops the fungus from growing and can cause it to break apart and die.
- How is Tolsura rated?
- pharmaranks gives Tolsura a composite score of 3.5 out of 5, currently based on 1 weighted source (FDA regulatory recall-safety data weighted highest). See our methodology at /how-we-rate.
- How much does Tolsura cost?
- Nobody can tell you what you will pay — your price is set by your insurer's formulary, your deductible and the pharmacy's markup, and none of those are published. What IS published is what the pharmacy paid to acquire it: about $0.84 per ml, per the CMS NADAC survey. Treat that as the floor, not the quote — ask the pharmacist for the cash price as well as your copay, because for cheap generics the cash price often wins. Pharmacies pay less for a same-class option, Clotrimazole — about $0.21 on the same basis.
- Is there a coupon or discount for Tolsura?
- pharmaranks is an independent ratings site, not a pharmacy — we don't issue coupons or sell Tolsura. To pay less, ask your prescriber or pharmacist whether a generic equivalent exists, check the manufacturer's copay/savings card and patient-assistance program, and compare a pharmacy discount card against your insurance copay. Prices vary by pharmacy, insurance, and location, so always confirm at the counter. This is general reference, not medical or financial advice.
- Who makes Tolsura?
- Tolsura is marketed by Mayne Pharma. You can see Mayne Pharma's full profile, rating, and other products on pharmaranks.
- Is Tolsura a brand-name or generic drug?
- Tolsura is a brand-name product with the active ingredient Itraconazole.
- Is Tolsura available over the counter?
- No. Tolsura is a prescription (Rx) medication in the US — you need a prescription from a licensed clinician (in person or via telehealth); it isn't sold over the counter. For some conditions there are OTC alternatives — ask your pharmacist.
- What forms does Tolsura come in?
- Tolsura is currently marketed as capsule, per the FDA's National Drug Code Directory.
- What class of drug is Tolsura?
- Tolsura is classified as azole antifungal, per the FDA's Established Pharmacologic Class.
- Is Tolsura FDA-registered?
- Tolsura is on record with the U.S. FDA under application number NDA208901. You can verify this on its official FDA label.
- Has Tolsura been recalled by the FDA?
- Tolsura has no FDA recalls recorded under its own application in the openFDA enforcement database. Its recall-safety score reflects its manufacturer's overall recall record. This is general reference, not medical advice — check the FDA recall database for the latest alerts.
- Is Tolsura safe?
- There's no single safe-or-not verdict. pharmaranks gives Tolsura a recall-safety score of 70/100, based on its FDA recall history (no recalls under its own FDA application) — not an efficacy or side-effect rating. Review its FDA-label side effects and warnings before use, and always consult a licensed professional.
- What are the side effects of Tolsura?
- Tolsura's side effects are taken directly from its FDA label. From the label: The following clinically significant adverse reactions are described elsewhere in the labeling: Congestive Heart Failure [see Warnings and Precautions (5.1) ] Hepatotoxicity [see Warnings and Precautions (5.2) ] Cardiac Dysrhythmias [see Warnings and Precautions (5.3) ] Pseudoaldosteronism [see Warn… Both common and serious reactions are documented in full on this page. This is general reference from the FDA, not medical advice — always consult a professional.
Clinical content sourced from the FDA label via openFDA (U.S. FDA). View the FDA label on DailyMed → Provided for general reference only — not medical advice. Always consult a licensed professional and the current prescribing information.
Reviews
No reviews yet. Be the first to write one.
People also viewed
voriconazole
Voriconazole
clotrimazole
Clotrimazole
ketoconazole
Ketoconazole
monistat 3
Miconazole Nitrate
monistat 3 combination pack
Miconazole Nitrate
monistat 3 combination pack (prefilled)
Miconazole Nitrate
Compare Tolsura head-to-head
More azole antifungal drugs
Browse medications A–Z
Research products from A to Z, compare independent ratings, and find alternatives.
tolsura
70/100