pharmacopeia
GET
/api/v1/drug/itraconazole

Boxed warning

Congestive Heart Failure, Cardiac Effects and Drug Interactions Congestive Heart Failure and Cardiac Effects: • Itraconazole capsules should not be administered for the treatment of onychomycosis in patients with evidence of ventricular dysfunction such as congestive heart failure (CHF) or a history of CHF. If signs or symptoms of congestive heart failure occur during administration of itraconazole capsules, discontinue administration. • When itraconazole was administered intravenously to dogs and healthy human volunteers, negative inotropic effects were seen. (See CONTRAINDICATIONS, WARNINGS, PRECAUTIONS: Drug Interactions, ADVERSE REACTIONS: Postmarketing Experience, and CLINICAL PHARMACOLOGY: Special Populations for more information.) Drug Interactions: • Coadministration of a number of CYP3A4 substrates are contraindicated with itraconazole capsules. Some examples of drugs that are contraindicated for coadministration with itraconazole capsules are: methadone, disopyramide, dofetilide, dronedarone, quinidine, isavuconazole, ergot alkaloids (such as dihydroergotamine, ergometrine (ergonovine), ergotamine, methylergometrine (methylergonovine)), irinotecan, lurasidone, oral midazolam, pimozide, triazolam, felodipine, nisoldipine, ivabradine, ranolazine, eplerenone, cisapride, naloxegol, lomitapide, lovastatin, simvastatin, avanafil, ticagrelor, finerenone, voclosporin.

2D structure
2-butan-2-yl-4-[4-[4-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one
SMILES CCC(C)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OC[C@H]5CO[C@](O5)(CN6C=NC=N6)C7=C(C=C(C=C7)Cl)Cl
InChIKey VHVPQPYKVGDNFY-ZPGVKDDISA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: 14-alpha Demethylase Inhibitors; Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 3A4 Inhibitors; Ergosterol Synthesis Inhibitors; P-Glycoprotein Inhibitors.

14-alpha DemethylaseBreast Cancer Resistance ProteinCytochrome P450 3A4Ergosterol SynthesisP-Glycoprotein

Indications

Sourced from openFDA
  • Itraconazole capsules are indicated for the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: 1. Blastomycosis, pulmonary and extrapulmonary 2.

Contraindications

Sourced from openFDA
  • Congestive Heart Failure: Itraconazole capsules should not be administered for the treatment of onychomycosis in patients with evidence of ventricular dysfunction such as congestive heart failure (CHF) or a history of CHF. (See BOXED WARNINGS, WARNINGS, PRECAUTIONS: Drug Interactions-Calcium Channel Blockers, ADVERSE REACTIONS: Postmarketing Experience, and CLINICAL PHARMACOLOGY: Special Populations.) Drug Interactions: Coadministration of a number of CYP3A4 substrates are contraindicated with itraconazole.contraindicated

Dosage & administration

Sourced from openFDA

Itraconazole capsules should be taken with a full meal to ensure maximal absorption. Itraconazole capsules must be swallowed whole. Itraconazole capsule is a different preparation than itraconazole Oral Solution and should not be used interchangeably. Treatment of Blastomycosis and Histoplasmosis: The recommended dose is 200 mg once daily (2 capsules). If there is no obvious improvement, or there is evidence of progressive fungal disease, the dose should be increased in 100-mg increments to a maximum of 400 mg daily. Doses above 200 mg/day should be given in two divided doses. Treatment of Aspergillosis: A daily dose of 200 to 400 mg is recommended. Treatment in Life-Threatening Situations: In life-threatening situations, a loading dose should be used. Although clinical studies did not provide for a loading dose, it is recommended, based on pharmacokinetic data, that a loading dose of 200 mg (2 capsules) three times daily (600 mg/day) be given for the first 3 days of treatment. 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. Itraconazole capsules and itraconazole Oral Solution should not be used interchangeably. Only the oral solution has been demonstrated effective for oral and/or esophageal candidiasis. Treatment of Onychomycosis: Toenails with or without fingernail involvement: The recommended dose is 200 mg (2 capsules) once daily for 12 consecutive weeks.

Warnings & precautions

Sourced from openFDA

Hepatic Effects: Itraconazole have been associated with rare 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, treatment should be discontinued and liver function testing performed. Continued itraconazole use or reinstitution of treatment with itraconazole is strongly discouraged unless there is a serious or life-threatening situation where the expected benefit exceeds the risk. (See PRECAUTIONS: Information for Patients and ADVERSE REACTIONS.) Cardiac Dysrhythmias: Life-threatening cardiac dysrhythmias and/or sudden death have occurred in patients using drugs such as cisapride, pimozide, methadone, or quinidine concomitantly with itraconazole and/or other CYP3A4 inhibitors. Concomitant administration of these drugs with itraconazole is contraindicated. (See BOXED WARNING, CONTRAINDICATIONS, and PRECAUTIONS: Drug Interactions.) Cardiac Disease: Itraconazole capsules should not be administered for the treatment of onychomycosis in patients with evidence of ventricular dysfunction such as congestive heart failure (CHF) or a history of CHF. Itraconazole capsules should not be used for other indications in patients with evidence of ventricular dysfunction unless the benefit clearly outweighs the risk.

Adverse reactions

Sourced from openFDA

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. Itraconazole has been associated with rare 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. If clinical signs or symptoms develop that are consistent with liver disease, treatment should be discontinued and liver function testing performed. The risks and benefits of itraconazole use should be reassessed. (See WARNINGS: Hepatic Effects and PRECAUTIONS: Hepatotoxicity and Information for Patients.) Adverse Events in the Treatment of Systemic Fungal Infections Adverse event data were derived from 602 patients treated for systemic fungal disease in U.S. clinical trials who were immunocompromised or receiving multiple concomitant medications. Treatment was discontinued in 10.5% of patients due to adverse events. The median duration before discontinuation of therapy was 81 days (range: 2 to 776 days). The table lists adverse events reported by at least 1% of patients.

Use in specific populations

Sourced from openFDA

Pregnancy: Teratogenic Effects: Itraconazole was found to cause a dose-related increase in maternal toxicity, embryotoxicity, and teratogenicity in rats at dosage levels of approximately 40 to 160 mg/kg/day (1 to 4 times the MRHD based on body surface area comparisons), and in mice at dosage levels of approximately 80 mg/kg/day (1 time the MRHD based on body surface area comparisons). Itraconazole has been shown to cross the placenta in a rat model. In rats, the teratogenicity consisted of major skeletal defects; in mice, it consisted of encephaloceles and/or macroglossia. There are no studies in pregnant women. Itraconazole should be used for the treatment of systemic fungal infections in pregnancy only if the benefit outweighs the potential risk. Itraconazole should not be administered for the treatment of onychomycosis to pregnant patients or to women contemplating pregnancy. Itraconazole should not be administered to women of childbearing potential for the treatment of onychomycosis unless they are using effective measures to prevent pregnancy and they begin therapy on the second or third day following the onset of menses. Highly effective contraception should be continued throughout itraconazole therapy and for 2 months following the end of treatment. During postmarketing experience, cases of congenital abnormalities have been reported.

Overdosage

Sourced from openFDA

Itraconazole is not removed by dialysis. In the event of accidental overdosage, supportive measures should be employed. Contact a certified poison control center for the most up to date information on the management of itraconazole capsules overdosage (1-800-222-1222 or www.poison.org). In general, adverse events reported with overdose have been consistent with adverse drug reactions already listed in this package insert for itraconazole. (See ADVERSE REACTIONS.)

Approval history

Sourced from openFDA
  • Sep 11, 1992NDANDA020083Janssen Pharms
  • Oct 30, 2015ANDAANDA205573Amneal Pharms
  • Sep 26, 2016ANDAANDA205080Amneal Pharms
  • Dec 13, 2016ANDAANDA206741Alembic
  • Dec 13, 2016ANDAANDA205724Rising
  • Jun 12, 2017ANDAANDA208591Alkem Labs Ltd
  • Aug 24, 2018ANDAANDA209460Torrent
  • Dec 11, 2018NDANDA208901Mayne Pharma

FDA shortages

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Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

  • Sporanox, Capsule, 100 mg (NDC 10147-1700-3)To be discontinued
    Sponsor: Janssen Pharmaceuticals
    Updated
  • Sporanox, Capsule, 100 mg (NDC 50458-290-01)To be discontinued
    Sponsor: Janssen Pharmaceuticals
    Updated
  • Sporanox, Capsule, 100 mg (NDC 50458-290-04)To be discontinued
    Sponsor: Janssen Pharmaceuticals
    Updated

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
11,463 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Interaction1,14310.0%
  2. 2Drug Ineffective1,1149.7%
  3. 3Off Label Use6205.4%
  4. 4Pyrexia5835.1%
  5. 5Dyspnoea4834.2%
  6. 6Pneumonia4694.1%
  7. 7Nausea4554.0%
  8. 8Diarrhoea3973.5%
  9. 9Condition Aggravated3933.4%
  10. 10Febrile Neutropenia3703.2%
  11. 11Fatigue3352.9%
  12. 12Rash3072.7%
  13. 13Anaemia3022.6%
  14. 14Neutropenia2982.6%
  15. 15Cough2912.5%

Literature

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Recent PubMed references pinned to Itraconazole as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 490 ClinicalTrials.gov registrations naming Itraconazole as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Itraconazole work?
Mechanism-of-action classes: 14-alpha Demethylase Inhibitors; Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 3A4 Inhibitors; Ergosterol Synthesis Inhibitors; P-Glycoprotein Inhibitors.
What is Itraconazole used for?
According to FDA labeling, Itraconazole carries indications including: Itraconazole capsules are indicated for the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: 1. Blastomycosis, pulmonary and extrapulmonary 2.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Itraconazole?
Itraconazole is classified as Triazole and tetrazole derivatives, Azole Antifungal, 14-alpha Demethylase Inhibitors, Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 3A4 Inhibitors, Ergosterol Synthesis Inhibitors, P-Glycoprotein Inhibitors, Decreased Cell Wall Integrity.
What are the brand names for Itraconazole?
Itraconazole is marketed under brand names including Sporanox, Tolsura.
What are the contraindications for Itraconazole?
Itraconazole labeling lists contraindications including: Congestive Heart Failure: Itraconazole capsules should not be administered for the treatment of onychomycosis in patients with evidence of ventricular dysfunction such as congestive heart failure (CHF) or a history of CHF. (See BOXED WARNINGS, WARNINGS, PRECAUTIONS: Drug Interactions-Calcium Channel Blockers, ADVERSE REACTIONS: Postmarketing Experience, and CLINICAL PHARMACOLOGY: Special Populations.) Drug Interactions: Coadministration of a number of CYP3A4 substrates are contraindicated with itraconazole.. Always consult the full prescribing information and a clinician.
Note. Data for itraconazole is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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