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itraconazole (Rx)Brand and Other Names:Sporanox, Sporanox Oral Solution, more...Onmel

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 100mg

oral solution

  • 10mg/mL

tablet

  • 200mg
more...

Life-Threatening Infections

200 mg PO q8hr initially for 3-4 days, then 200-400 mg/day for at least 3 months

Blastomycosis

Immunocompromised and non-immunocompromised patients: 200 mg PO q8hr for 3 days, then 200 mg PO q12hr for 6-12 months; initiate therapy with aproximately 2 weeks of amphotericin B if infection is moderately severe to severe

Aspergillosis

Immunocompromised and non-immunocompromised patients: 200-400 mg/day PO; may be used in combination with corticosteroids

Life-threatening infection: Administer a loading dose of 200 mg PO TID for first 3 days of therapy; continue treatment for at least 3 months and until clinical and laboratory evidence suggest that infection has resolved; current dose on candidiasis is for esophageal candidiasis

Histoplasmosis

Immunocompromised and non-immunocompromised patients: 200 mg/day PO; may be increased by 100 mg/day increments; not to exceed 400 mg/day

Onychomycosis in Non-immunocompromised Patients

Fingernails: 2 treatment pulses, each consisting of 200 mg q12hr for 1 week

Toenails, with or without fingernail involvement: 200 mg/day PO for 12 weeks

Oral Candidiasis

Oral solution: 100-200 mg/day for at least 3 weeks; continued for 2 weeks after symptom resolution

Refractory to fluconazole: 100 mg PO q12hr for 2-4 weeks

Swish in mouth 10 mL at a time for several seconds, then swallow; take without food if possible

Oropharyngeal candidiasis in patients unresponsive to fluconazole: 200 mg PO qDay for 1-2 weeks

Otomycosis (Orphan)

Suspension: Topical treatment of fungal otitis externa (otomycosis)

Orphan indication sponsor

  • Fairfield Clinical Trials, LLC; 200 Steep Hill Road; Weston, CT 06883

Dosage Forms & Strengths

capsule

  • 100mg

oral solution

  • 10mg/mL
more...

Systemic Fungal Infections (Off-label)

<3 years: Safety and efficacy not established 

≥3 years: 3-5 mg/kg/day PO initially (limited data)

Candidiasis (Off-label)

HIV exposed or positive

Infants and children

  • Oropharyngeal: 2.5 mg/kg/dose oral solution BID; not to exceed 200 mg/day for 7-14 days; 400 mg qDay if fluconazole refractory
  • Esophageal: 5 mg/kg/day oral solution qDay or divided BID for 14-21 days

Adolescents

  • Oropharyngeal: 200 mg oral solution qDay for 7-14 days
  • Esophageal: 200 mg oral solution qDay for 14-21 days

Histoplasmosis (Off-label)

HIV exposed or positive

Infants and children

  • Mild disseminated disease: 2-5 mg/kg/dose TID for 3 days; followed by twice daily for 12 months; not to exceed 200 mg/dose
  • Relapse prevention: Oral solution: 5 mg/kg/dose BID; not to exceed 400 mg/day

Adolescents

  • 200 mg PO TID for 3 days; then 200 mg BID for at least 12 months
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Interactions

Interaction Checker

itraconazole and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Nausea (11%)

            1-10%

            Rash (9%)

            Vomiting (5%)

            Edema (4%)

            Headache (4%)

            Abnormal liver function test results (3%)

            Diarrhea (3%)

            Fever (3%)

            Hypertension (3%)

            Pruritus (3%)

            Fatigue (2-3%)

            Abdominal pain (2%)

            Dizziness (2%)

            Hypertriglyceridemia (2%)

            Hypokalemia (2%)

            Albuminuria (1%)

            Anorexia (1%)

            Decreased libido (1%)

            Hepatitis (1%)

            Malaise (1%)

            Postmarketing Reports

            Blood and Lymphatic System Disorders: Leukopenia, neutropenia, thrombocytopenia

            Immune System Disorders: Anaphylaxis; anaphylactic, anaphylactoid and allergic reactions; serum sickness; angioneurotic edema

            Nervous System Disorders: Peripheral neuropathy, paresthesia, hypoesthesia, tremor

            Eye Disorders: Visual disturbances, including vision blurred and diplopia

            Ear and Labyrinth Disorders: Transient or permanent hearing loss

            Cardiac Disorders: Congestive heart failure

            Respiratory, Thoracic and Mediastinal Disorders: Pulmonary edema, dyspnea

            Gastrointestinal Disorders: Pancreatitis, dysgeusia

            Hepatobiliary Disorders: Serious hepatotoxicity (including some cases of fatal acute liver failure), hepatitis

            Skin and Subcutaneous Tissue Disorders: Toxic epidermal necrolysis, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis, erythema multiforme, exfoliative dermatitis, leukocytoclastic vasculitis, alopecia, photosensitivity, urticaria

            Musculoskeletal and Connective Tissue Disorders: Arthralgia

            Renal and Urinary Disorders: Urinary incontinence, pollakiuria

            Reproductive System and Breast Disorders: Erectile dysfunction

            General Disorders and Administration Site: Peripheral edema

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            Warnings

            Black Box Warnings

            Congestive heart failure

            • Do not use for the treatment of onychomycosis in patients with ventricular dysfunction (eg, history of CHF)
            • If signs or symptoms of CHF occur during itraconazole therapy, discontinue administration

            Contraindicated drug interactions

            • Itraconazole is potent CYP4503A4 inhibitor
            • Coadministration of the following drugs are contraindicated with itraconazole: methadone, disopyramide, dofetilide, dronedarone, quinidine, ergot alkaloids (eg, dihydroergotamine, ergonovine, ergotamine, methylergonovine), irinotecan, lurasidone, oral midazolam, pimozide, triazolam, felodipine, nisoldipine, ranolazine, eplerenone, cisapride, lovastatin, simvastatin, ticagrelor, and, in patients with varying degrees of renal or hepatic impairment, colchicine, fesoterodine, telithromycin, and solifenacin
            • Coadministration with itraconazole can cause elevated plasma concentrations of these drugs and may increase or prolong both the pharmacologic effects and/or adverse reactions to these drugs (eg, increased plasma concentrations of some of these drugs can lead to QT prolongation and ventricular tachyarrhythmias including occurrences of torsades de pointes)

            Contraindications

            Onychomycosis treatment in pregnancy or contemplated pregnancy

            Hypersensitivity

            Contraindicated with certain CYP3A4 substrate drugs (see Black Box Warnings)

            Renal or hepatic impairment

            Treatment of onychomycosis in women who are pregnant or plan to become pregnant

            Ventricular dysfunction (eg, current or previous CHF), except for treatment of life-threatening or other serious infections

            Cautions

            Discontinue if liver disease develops, and perform liver function tests; readministration discouraged

            Prolongs QT interval; caution with concurrent QT-prolonging drugs or congenital long QT (see Black Box Warnings for drugs contraindicated for use with itraconazole)

            Not for the treatment of other indications in patients with evidence of ventricular dysfunction unless benefit clearly outweighs risks; practitioners should carefully review risks and benefits; 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 patients of signs and symptoms of CHF, and treat with caution; monitor for signs and symptoms of CHF during treatment; if signs or symptoms of CHF appear during therapy, discontinue treatment

            Oral capsule and oral solution are not bioequivalent; do not use interchangeably

            Parenteral form is incompatible with most aqueous solutions; use dedicated line, and do not mix with other drugs in any way

            If neuropathy occurs that may be attributable to itraconazole, discontinue treatment

            If cystic fibrosis patient does not respond to itraconazole, consider switching to alternative therapy; large differences in itraconazole pharmacokinetic parameters observed in cystic fibrosis patients

            Transient or permanent hearing loss reported in patients receiving treatment with itraconazole; several reports included concurrent administration of quinidine, which is contraindicated; the hearing loss usually resolves when treatment is stopped, but can persist in some patients

            May cause CNS depression, which may impair physical or mental abilities; caution when operating heavy machinery or performing tasks that require mental alertness

            Rare cases of serious hepatotoxicity reported in patients without preexisting liver disease or risk factors; use caution in patients with preexisting hepatic impairment; monitor liver function closely and adjust dose as necessary; not recommended for use in patients with elevated liver enzymes, active liver disease, or prior hepatotoxic reactions to other drugs unless the expected benefit exceeds the risk of hepatotoxicity

            Use with caution in patients with renal impairment; not studied

            Absorption of itraconazole capsules is reduced when gastric acidity reduced; administer capsules with acidic beverage in patients with reduced gastric acidity and do not administer concomitantly with acid suppressive therapy; monitor for response

            Only oral solution shown to be effective in oral/esophageal candidiasis; oral solution not recommended in patients at immediate risk for systemic candidiasis

            Itraconazole should not be used to treat voriconazole-refractory aspergillosis; both agents may share resistance mechanisms

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Drug enters breast milk; weigh risk against benefit

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
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            Pharmacology

            Mechanism of Action

            Triazole antifungal agent; inhibits cytochrome P450-dependent synthesis of ergosterol, which in turn inhibits cell-membrane formation

            Absorption

            Peak plasma time: Oral solution with fasting, 2.2 hr; capsule with food, 5 hr

            Peak plasma concentration: Oral solution with fasting, 544 ng/mL; capsule with food, 302 ng/mL

            Distribution

            Protein bound: 99.8%

            Vd: 796 L or 10 L/kg

            Metabolism

            Metabolized by hepatic enzyme CYP3A4

            Enzymes inhibited: CYP3A4

            Elimination

            Half-life: 64±32 hr

            Excretion: Urine, feces

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            Administration

            Oral Administration

            Capsule: Take with food if possible

            Oral solution: Swish in mouth 10 mL at a time for several seconds, then swallow; take without food if possible 

            IV Preparation

            Precise dilution (3.33 mg/mL) is required to maintain stability and avoid precipitate formation

            Dilute with NS only; do not use dextrose or lactated Ringer solution

            Add 25 mL (1 ampule = 250 mg) to 50 mL NS

            Mix and withdraw 15 mL of solution before infusing

            IV Administration

            Using flow-control device, infuse 60 mL of diluted solution (200 mg itraconazole; pH 4.8) over 60 minutes, using extension line and infusion set provided

            After administration, flush infusion set with 15-20 mL NS over 30 seconds to 15 minutes via 2-way stopcock; do not use bacteriostatic NS

            Discard entire infusion set

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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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