Itraconazole is an antifungal medication that is used in adults to treat infections caused by fungus. This includes infections in any part of the body including the lungs, mouth or throat, toenails, or fingernails.
The Tolsura brand of itraconazole is not for use in treating fungal infections of the fingernails or toenails. Avoid medication errors by using only the brand and strength your doctor prescribes.
Itraconazole may also be used for purposes not listed in this medication guide.
Warnings
You should not take itraconazole if you have ever had heart failure.
If you have liver or kidney disease, you should not take itraconazole with colchicine, fesoterodine, or solifenacin.
Itraconazole may harm an unborn baby. Avoid getting pregnant while taking itraconazole and for 2 months after your last dose.
Stop using itraconazole and call your doctor at once if you have signs of congestive heart failure: feeling tired or short of breath, cough with mucus, fast heartbeats, swelling, rapid weight gain, or sleep problems.
Life-threatening side effects may occur if you take itraconazole with certain other drugs. Tell your doctor about all your current medicines and any you start or stop using.
Before taking this medicine
You should not take this medicine if you are allergic to itraconazole or similar medicines such as fluconazole or ketoconazole, or if you have ever had congestive heart failure.
Life-threatening side effects may occur if you take itraconazole with certain other drugs. Your doctor may change your treatment plan if you have used other medicines in the past 2 weeks, especially:
avanafil;
cisapride;
eliglustat;
irinotecan;
isavuconazonium;
methadone;
naloxegol;
ranolazine;
ticagrelor;
lurasidone or pimozide (anti-psychotic medications);
dihydroergotamine, ergonovine, ergotamine, or methylergonovine (ergot medicines);
eplerenone, felodipine, ivabradine, or nisoldipine (heart or blood pressure medicines);
disopyramide, dofetilide, dronedarone, or quinidine (medicines for heart rhythm disorders); or
oral midazolam, or triazolam (Valium-like sedatives).
If you have liver or kidney disease, you should not take itraconazole with colchicine, fesoterodine, solifenacin, or telithromycin.
Itraconazole may harm an unborn baby. Use effective birth control to prevent pregnancy while you are using this medicine and for at least 2 months after your last dose. Tell your doctor if you become pregnant.
Tell your doctor if you have ever had:
heart problems;
cystic fibrosis or other lung problems;
liver or kidney disease; or
a weak immune system.
It may not be safe to breastfeed while using this medicine. Ask your doctor about any risk itraconazole Uses:
Aspergillosis (capsules):
Itraconazole is used to treat aspergillosis (whether pulmonary or extrapulmonary) if a patient is resistant or intolerant to Amphotericin B therapy.
According to the Infectious disease society of America amphotericin B formulations for invasive aspergillosis is recommended only when voriconazole is contraindicated or not tolerated.
Blastomycosis (capsules):
Itraconazole is also used to treat blastomycosis (both pulmonary and extrapulmonary) in patients who are immunocompromised as well as those who are immunocompetent.
Histoplasmosis (capsules):
Itraconazole is used in the treatment of histoplasmosis for chronic cavitary pulmonary and disseminated diseases except in meningeal histoplasmosis in both immunocompromised and immunocompetent patients.
Onychomycosis:
Capsules (100 mg [Sporanox]):
Itraconazole capsule is also used to treat onychomycosis of the toenail, and onychomycosis of the fingernail caused by dermatophytes (tinea unguium).
Tablets:
It is used to treat onychomycosis of the toenail caused by Trichophyton rubrum or Trichophyton mentagrophytes.
It is used to treat oropharyngeal and esophageal candidiasis.
Candidiasis, oral, and/or esophageal:
It is used to treat oral and/or esophageal candidiasis in immunocompromised and immunocompetent patients.
Chromomycosis:
Itraconazole is also used in the treatment of chromomycosis in immunocompromised as well as immunocompetent patients
Dermatomycoses:
It is used to treat dermatomycoses due to tinea pedis, tinea cruris, tinea corporis, and of pityriasis versicolor in patients for whom oral therapy is appropriate
Onychomycosis:
Itraconazole is used to treat onychomycosis in immunocompromised and immunocompetent patients
Paracoccidioidomycosis:
Itraconazole is also used in the treatment of paracoccidioidomycosis in immunocompromised and immunocompetent patients
Sporotrichosis:
It is used to treat cutaneous and lymphatic sporotrichosis in immunocompromised and immunocompetent patients
Off Label Use of Itraconazole in Adults:
Candidiasis, vulvovaginal in HIV-infected patients
Coccidioidal meningitis in HIV-infected patients
Coccidioidal pneumonia in HIV-infected patients; Coccidioidomycosis (non-HIV infected)
Cryptococcosis in HIV-infected patients
Microsporidiosis, disseminated in HIV-infected patients
Penicilliosis in HIV-infected patients
Itraconazole Dose in Adults:
Note:
Formulations are not interchangeable.
Generally, the oral solution is the preferred formulation because of improved absorption.
Itraconazole Dose as an alternative agent in the treatment of Invasive Aspergillosis, (salvage therapy):
Oral solution:
200 mg twice daily;
duration of therapy is a minimum of 6 to 12 weeks, although the duration is highly dependent on the degree/duration of immunosuppression, disease site, and evidence of disease improvement.
Oral capsule (65 mg [Tolsura]):
130 mg once or twice daily;
for life-threatening infections, administer a loading dose of 130 mg 3 times daily for the first 3 days of therapy;
treatment should be continued for ≥3 months and until clinical and laboratory resolution.
Itraconazole Dose in the treatment of Blastomycosis:
Oral solution or capsule (100 mg [Sporanox]):
200 mg 3 times daily for 3 days, then 200 mg twice daily for 6 to 12 months;
in moderately severe to severe infection, therapy should be initiated with ~2 weeks of amphotericin B.
Oral capsule (65 mg [Tolsura]):
130 mg once daily;
if no improvement or if there is evidence of progressive fungal infection, increase dose in 65 mg increments to a maximum of 260 mg/day (doses >130 mg/day should be given in 2 divided doses).
For life-threatening infections, a loading dose of 130 mg 3 times daily for the first 3 days of therapy should be administered;
The treatment should be continued for ≥3 months and until clinical and laboratory resolution.
Itraconazole Dose in the treatment of Candidiasis: Oral:
Esophageal:
Oral solution:
Fluconazole-refractory disease:
200 mg once daily for 14 to 21 days.
HIV-infected patients:
200 mg once daily for 14 to 21 days.
US labeling:
Dosing in the prescribing information may not reflect current clinical practice.
Oral solution: 100 to 200 mg once daily
Canadian labeling:
Oral solution:
100 to 200 mg once daily for a minimum of 3 weeks; continue dosing for 2 weeks after resolution of symptoms
Oral capsule (100 mg [Sporanox]):
100 mg once daily for 4 weeks
Oropharyngeal:
Oral solution:
Fluconazole-refractory disease:
200 mg once daily for up to 28 days.
HIV-infected patients (alternative agent):
Oral solution: 200 mg once daily for 7 to 14 days.
US labeling:
Dosing in the prescribing information may not reflect current clinical practice.
Oral solution: 200 mg once daily;
in patients unresponsive or refractory to fluconazole: 100 mg twice daily
Canadian labeling:
Oral solution: 200 mg once daily or in divided doses daily for 1 to 2 weeks
Oral capsule (100 mg [Sporanox]): 100 mg once daily for 2 weeks
Itraconazole Dose in the treatment of Vulvovaginal (uncomplicated) in HIV-infected patients (alternative to preferred therapy) (off label):
Oral solution: 200 mg once daily for 3 to 7 days.
Itraconazole Dose in the treatment of Chromomycosis: Canadian labeling (not in US labeling):
Oral capsule (100 mg [Sporanox]): 200 mg once daily for 6 months
Itraconazole Dose in the treatment of Coccidioidomycosis, extrapulmonary (non-HIV infected) (off-label): Oral:
Soft tissue infection (not associated with bone infection):
200 mg twice daily for at least 6 to 12 months.
Bone and/or joint infection:
200 mg twice daily for 3 years to lifetime, depending on the severity and host immunocompetence.
Note: Amphotericin B may be used initially in severe cases and then switched to itraconazole.
Itraconazole Dose in the treatment of Coccidioidal pneumonia (off-label): Oral:
Non-HIV infected (symptomatic, chronic cavitary):
Oral: 200 mg twice daily for at least 12 months.
HIV-infected patients (focal pneumonia):
200 mg twice daily.
Itraconazole Dose in the treatment of Coccidioidal meningitis (off-label):
Non-HIV infected:
Oral: 200 mg 2 to 4 times daily; close monitoring required to assure adequate absorption.
Treatment: 200 mg 3 times daily for 3 days, then 200 mg twice daily, followed by chronic suppressive therapy
Chronic suppressive therapy:
200 mg twice daily continued indefinitely, even with an increase in CD4 count on ART
Itraconazole Dose as an alternative agent in the treatment of Cryptococcosis in HIV-infected patients (off-label use): Oral:
Treatment, consolidation therapy:
200 mg twice daily for ≥8 weeks.
Histoplasmosis:
Treatment:
Oral solution or capsule (100 mg [Sporanox]):
200 mg 3 times daily for 3 days, then 200 mg twice daily (or once daily in mild-moderate disease) for 6 to 12 weeks in mild to moderate disease or ≥12 months in progressive disseminated or chronic cavitary pulmonary histoplasmosis;
in moderately severe to severe infection, therapy should be initiated with ~2 weeks of a lipid formation of amphotericin B.
Oral capsule (65 mg [Tolsura]):
130 mg once daily;
if no improvement or if there is evidence of progressive fungal infection, increase dose in 65 mg increments to a maximum of 260 mg/day (doses >130 mg/day should be given in 2 divided doses).
For life threatening infections, administer a loading dose of 130 mg 3 times daily for the first 3 days of therapy;
treatment should be continued for ≥3 months and until clinical and laboratory resolution.
HIV-infected patients (oral solution or capsule [100 mg (Sporanox)]):
Mild disseminated disease:
Induction and maintenance therapy:
200 mg 3 times daily for 3 days, then 200 mg twice daily for ≥12 months (HHS [OI adult 2017])
Moderate to severe disseminated disease:
Maintenance therapy (following at least 2 weeks of induction therapy with an appropriate agent):
200 mg 3 times daily for 3 days, then 200 mg twice daily for ≥12 months (HHS [OI adult 2017])
Itraconazole Dose in the treatment of Meningitis:
Maintenance therapy (following 4 to 6 weeks of induction therapy with an appropriate agent):
200 mg 2 to 3 times daily for ≥12 months and until resolution of abnormal CSF findings.
Prophylaxis (off-label):
Oral solution or capsule (100 mg [Sporanox]):
Primary prophylaxis in HIV-infected patients:
200 mg once daily;
primary prophylaxis is indicated when CD4 count <150 cells/mm and at increased risk of exposure.
Long-term suppression therapy (secondary prophylaxis) in HIV-infected patients:
200 mg once daily; long-term suppressive therapy is indicated in patients who relapse despite appropriate therapy or in patients with CNS or severe disseminated infection.
Itraconazole Dose in the treatment of Microsporidiosis, disseminated (caused by Trachipleistophora or Anncaliia) in HIV infected patients (off-label):
Oral: 400 mg once daily in combination with albendazole.
Itraconazole Dose in the treatment of Onychomycosis (fingernail involvement only):
Oral capsule (100 mg [Sporanox]):
200 mg twice daily for 1 week; repeat 1-week course after 3-week off-time
Itraconazole ( Dose in the treatment of Onychomycosis (toenails due to Trichophyton rubrum or T. mentagrophytes):
Oral tablet: 200 mg once daily for 12 consecutive weeks.
Itraconazole ( Dose in the treatment of Onychomycosis (toenails with or without fingernail involvement):
Oral capsule (100 mg [Sporanox]):
200 mg once daily for 12 consecutive weeks
Canadian labeling (not in US labeling):
Oral capsule (100 mg [Sporanox]):
“Pulse-dosing”: 200 mg twice daily for 1 week;
repeat 1-week course twice with 3-week off-time between each course
Itraconazole Dose in the treatment of Paracoccidioidomycosis:
Canadian labeling (not in US labeling):
Oral capsule (100 mg [Sporanox]): 100 mg once daily for 6 months
Itraconazole Dose in the treatment of Penicilliosis in HIV-infected patients:
Primary prophylaxis:
200 mg once daily for patients with a CD4 count <100 cells/mm³ who spend extensive time in northern Thailand, Vietnam, and Southern China, especially rural areas
Treatment:
200 mg twice daily for 8 weeks (mild disease) or 10 weeks (severe infections), then continue with maintenance therapy. In severely ill patients, initiate therapy with 2 weeks of liposomal amphotericin B.
Chronic maintenance (secondary prophylaxis):
200 mg once daily until CD4 count >100 cells/mm³ for ≥6 months in response to ART
Itraconazole Dose in the treatment of Pityriasis versicolor:
Canadian labeling (not in US labeling):
Oral capsule (100 mg [Sporanox]):
100 mg twice daily or 200 mg once daily for 5 to 7 days
Itraconazole Dose in the treatment of Sporotrichosis: Oral:
Cutaneous:
Canadian labeling (not in US labeling): Oral capsule (100 mg [Sporanox]):
100 to 200 mg once daily for 3 to 6 months (localized lesions);
200 mg twice daily for 3 to 6 months (extensive lesions)
Lymphocutaneous:
200 mg daily for 3 to 6 months.
Canadian labeling (not in US labeling): Oral capsule (100 mg [Sporanox]):
100 to 200 mg once daily for 3 to 6 months (localized lesions);
200 mg twice daily for 3 to 6 months (extensive lesions)
Osteoarticular and pulmonary:
200 mg twice daily for ≥1 years (may use amphotericin B initially for stabilization).
Itraconazole Dose in the treatment of Tinea corporis or tinea cruris:
Canadian labeling (not in US labeling):
Oral capsule (100 mg [Sporanox]):
100 mg once daily for 14 consecutive days or 200 mg once daily for 7 consecutive days.
Note: Equivalency between regimens not established.
Itraconazole Dose in the treatment of Tinea pedis:
Canadian labeling (not in US labeling):
Oral capsule (100 mg [Sporanox]):
100 mg once daily for 28 consecutive days or 200 mg twice daily for 7 consecutive days.
Note: Equivalency between regimens not established.
Patients with chronic resistant infection may benefit from lower doses and extended treatment time (100 mg once daily for 28 days).
Itraconazole Dose in Children:
Note:
Formulations are not interchangeable.
Generally, the oral solution is the preferred formulation because of improved absorption.
Oral absorption varies between patients and as a result, monitoring of serum concentrations is suggested to ensure adequate and nontoxic levels are achieved.
Onmel (tablets) has been discontinued in the US for >1 year.
Itraconazole General dosing, susceptible infection: Limited data available:
Infants, Children, and Adolescents:
Oral: 5 mg/kg/dose every 12 hours for treatment;
The usual maximum daily dose: 200 mg/day;
some infections may require up to 400 mg/day.
Itraconazole Dose in the treatment of Blastomycosis, non-CNS infections:
Infants, Children, and Adolescents:
Oral solution: 5 mg/kg/dose twice daily;
The maximum dose: 200 mg/dose;
duration determined by severity and response;
The usual duration for mild to moderate disease is 6 to 12 months;
for moderately severe to severe disease a total duration of 12 months including 1 to 2 weeks of amphotericin B.
Itraconazole Dose in the treatment of Candidiasis (HIV-exposed/-positive patients):
Oropharyngeal, treatment:
Infants and Children: Fluconazole-refractory: Oral solution:
2.5 mg/kg/dose twice daily for 7 to 14 days;
maximum daily dose range: 200 to 400 mg/day
Adolescents: Oral solution:
200 mg once daily for 7 to 14 days
Esophageal, treatment:
Infants and Children:
Fluconazole-refractory: Oral solution:
2.5 mg/kg/dose twice daily for at least 21 days and at least 2 weeks following resolution of symptoms.
Adolescents: Oral solution:
200 mg once daily for 14 to 21 days
Vulvovaginal, uncomplicated:
Adolescents: Oral solution:
200 mg once daily for 3 to 7 days
Secondary prophylaxis:
Infants and Children: Oral solution:
2.5 mg/kg/dose twice daily
Itraconazole Dose in the treatment of Coccidioidomycosis:
Treatment:
Bone and/or joint infection:
Infants and Children: Independent of HIV status: Oral solution:
Itraconazole Dose in the treatment of Cryptococcal meningitis (HIV-exposed/-positive):
Consolidation treatment:
Infants and Children: Oral solution (preferred):
Initial load: 2.5 to 5 mg/kg/dose 3 times daily for 3 days;
maximum dose: 200 mg/dose
Maintenance dose:
5 to 10 mg/kg/day divided once or twice daily for a minimum of 8 weeks;
maximum daily dose: 400 mg/day
Adolescents: Oral:
200 mg twice daily for a minimum of 8 weeks
Secondary prophylaxis/Relapse prevention:
Infants and Children: Oral solution:
5 mg/kg/dose once daily;
maximum daily dose: 200 mg/day
Itraconazole Dose in the treatment of Histoplasmosis: Limited data available:
Treatment:
Pulmonary, acute primary disease:
HIV-exposed/-positive:
Infants and Children: Oral solution (preferred):
Initial load: 2 to 5 mg/kg/dose 3 times daily for 3 days;
maximum dose: 200 mg/dose
Maintenance dose:
2 to 5 mg/kg/dose twice daily for 12 months;
maximum dose: 200 mg/dose.
Treatment duration of 12 weeks may be adequate in children with functional cellular immunity (CD4 percentage >20% or if age ≥6 years, CD4 cell count >300 cells/mm³) if clinically improved and urine antigen concentrations decreased.
Non-HIV-exposed/-positive:
Infants, Children, and Adolescents:
Oral solution (preferred):
2.5 to 5 mg/kg/dose twice daily for 6 to 12 weeks;
maximum dose: 200 mg/dose.
Disseminated disease, mild to moderate:
HIV-exposed/-positive:
Infants and Children: Oral solution (preferred):
Initial load:
2 to 5 mg/kg/dose 3 times daily for 3 days;
maximum dose: 200 mg/dose
Maintenance dose:
2 to 5 mg/kg/dose twice daily for 12 months;
maximum dose: 200 mg/dose
Adolescents: Oral solution (preferred):
Initial load: 200 mg 3 times daily for 3 days
Maintenance dose: 200 mg twice daily for at least 12 months
Non-HIV-exposed/-positive:
Infants, Children, and Adolescents:
Oral solution (preferred): 2.5 to 5 mg/kg/dose twice daily for 3 to 12 months.
Disseminated disease, moderately severe to severe:
Consolidation treatment following appropriate induction treatment:
HIV-exposed/positive:
Infants and Children: Oral solution:
Initial load: 2 to 5 mg/kg/dose 3 times daily for 3 days; maximum dose: 200 mg/dose
Maintenance dose: 2 to 5 mg/kg/dose twice daily for 12 months; maximum dose: 200 mg/dose
Adolescents: Oral solution (preferred):
Initial load: 200 mg 3 times daily for 3 days
Maintenance dose: 200 mg twice daily for ≥12 months
Non-HIV-exposed/positive, step-down:
Infants, Children, and Adolescents:
Oral solution (preferred): 2.5 to 5 mg/kg/dose twice daily for 3 to 12 months based on the severity of disease;
Oral solution: 5 to 10 mg/kg/dose once daily; maximum dose: 200 mg/dose.
Adolescents:
Oral: 200 mg once daily.
Non-HIV-exposed/positive:
Infants, Children, and Adolescents:
Oral: 5 mg/kg/dose once daily;
maximum dose: 200 mg/dose.
Itraconazole Dose in the treatment of Microsporidiosis, a disseminated disease caused by Trachipleistophora or Anncaliia, treatment (HIV-exposed/-positive):
Adolescents:
Oral: 400 mg once daily in conjunction with albendazole.
Itraconazole (Sporanox) Dose in the treatment of Penicilliosis (HIV-exposed/-positive):
Adolescents:
Primary prophylaxis:
Oral: 200 mg once daily for patients with a CD4 count <100 cells/mm³ who spend extensive time in northern Thailand, Vietnam, and Southern China, especially rural areas
Acute infection (severely ill), treatment:
Oral: 200 mg twice daily for 10 weeks;
initiate after completion of 2 weeks induction therapy with amphotericin B
Itraconazole Dose in the treatment of Sporotrichosis:
Infants, Children, and Adolescents:
Lymphocutaneous or localized cutaneous: Oral solution (preferred):
3 to 5 mg/kg/dose twice daily; continue 2 to 4 weeks after all lesions have resolved,
usual total duration: 3 to 6 months;
maximum dose: 200 mg/dose
Step down therapy, visceral or disseminated (after initial treatment and clinical response with amphotericin B): Oral:
3 to 5 mg/kg/dose twice daily;
continue for at least 12 months;
maximum dose: 200 mg/dose
Itraconazole Dose in the treatment of Tinea capitis, Microsporum canis and trichophyton sp: Limited data available:
Infants, Children, and Adolescents:
Oral: 5 mg/kg/dose once daily;
maximum dose: 100 mg/dose;
duration of therapy depends on the organism:
Microsporum sp: 4 to 8 weeks;
trichophyton sp:
2 to 3 weeks;
up to 12 weeks of treatment may be required.
Alternatively, a pulse regimen may be used: 1 week treatment pulses with at least 2 weeks off between pulses
Dosing: Renal Impairment:
Pediatric Nondialyzable.
The manufacturer’s labeling states to use with caution in patients with renal impairment;
dosage adjustment may be needed.
Limited data suggest that no dosage adjustments are required in renal impairment; in adults, wide variations observed in plasma concentrations versus time profiles in patients with uremia or receiving hemodialysis or continuous ambulatory peritoneal dialysis.
Itraconazole Pregnancy Risk Category: C
Postmarketing surveillance has revealed multiple congenital anomalies (eg, skeletal and genitourinary tract malformations, cardiovascular malformations, chromosomal malformations and multiple malformations). However, no causal relationship has been established.
Itraconazole should not be used during pregnancy to treat onychomycosis
Itraconazole should not be used during the first trimester, despite its widespread approval to treat various systemic fungal infections.
It is not recommended for females who are planning to have a baby. Effective contraception should also be used during treatment and for at least 2 months afterward, according to the manufacturer.
The second or third day after menses, therapy should be initiated.
Itraconazole use during breastfeeding:
Breast milk contains Itraconazole.
According to the manufacturer the decision to continue breastfeeding while on therapy should be made based on the risks to infants and the benefits to the mother.
To reduce the risk of HIV transmission, HIV-infected women should stop breastfeeding.
Itraconazole Dose in Kidney Disease:
A wide variation is observed in those receiving hemodialysis or continuous ambulatory peritoneal dialysis.
Limited data suggest that no dosage adjustments are required in renal impairment.
The manufacturer’s labeling states to use with caution in patients with renal impairment; dosage adjustment may be needed.
Hemodialysis: Nondialyzable
Itraconazole Dose in Liver disease:
Manufacturer’s labeling provided no dosage adjustment, however, should be used with caution and monitor closely for signs/symptoms of toxicity.
Common Side Effects of Itraconazole :
Gastrointestinal:
Diarrhea
Nausea
Less Common Side Effects of Itraconazole :
Cardiovascular:
Edema
Chest Pain
Hypertension,
Central Nervous System:
Headache
Dizziness
Anxiety
Depression
Fatigue
Pain
Malaise
Abnormal Dreams
Dermatologic:
Skin Rash
Pruritus
Diaphoresis
Endocrine & Metabolic:
Hypertriglyceridemia
Hypokalemia
Gastrointestinal:
Vomiting
Abdominal Pain
Dyspepsia
Flatulence
Gastrointestinal Disease
Gingivitis
Aphthous Stomatitis
Constipation
Gastritis
Gastroenteritis
Increased Appetite
Genitourinary:
Cystitis
Urinary Tract Infection
Hepatic:
Abnormal Hepatic Function Tests
Increased Liver Enzymes
Infection:
Herpes Zoster
Neuromuscular & Skeletal:
Bursitis
Myalgia
Tremor
Respiratory:
Rhinitis
Upper Respiratory Tract Infection
Sinusitis
Cough
Dyspnea
Pneumonia
Pharyngitis
Miscellaneous:
Fever
Contraindication to Itraconazole :
Hypersensitivity to itraconazole and any component of the formulation
Concurrent administration
avanafil,
cisapride,
disopyramide,
dofetilide,
dronedarone,
eplerenone,
ergot derivatives,
Fetodipine
irinotecan,
isavuconazole,
ivabradine,
Lomotapide
lovastatin,
lurasidone,
Methadone
midazolam (oral),
naloxegol,
nisoldipine,
pimozide,
quinidine,
ranolazine,
simvastatin,
ticagrelor, or
triazolam;
concurrent administration with colchicine, fesoterodine, or solifenacin in patients with varying degrees of renal or hepatic impairment;
Patients who are intermediate or poor metabolizers or patients taking strong or moderate CYP2D6 inhibitors may co-administer eliglustat with them.
Treatment of onychomycosis or other non-life-threatening indications in patients with evidences of ventricular dysfunction (e.g. congestive heart disease (CHF)) or a history CHF.
Treatment of onychomycosis for pregnant women or those who are contemplating becoming pregnant
Canadian labeling: Additional contraindications not in US labeling
Concurrent administration with
domperidone,
Eletriptan, and
fesoterodine in patients with moderate to severe renal or hepatic impairment, or solifenacin in patients with severe renal impairment or moderate to severe hepatic impairment (capsule, oral solution);
Concurrent administration of the following drugs (none are available in Canada).
Astemizole,
bepridil,
Halofantrine
Invabradine
lercanidipine,
levacetylmethadol
mizolastine,
Telithromycin is used in patients with severe renal impairment or hepatic impairment.
sertindole
Terfenadine (capsules, orally solution);
Treatment of dermatomycosis in pregnant women (capsule), including tinea cruris (tinea pedis), tinea corporis (tinea corporis), pityriasis vericolor).
Warnings and precautions
CNS depression:
CNS depression can result. Patients who are required to drive, operate heavy machinery, or perform other activities that require mental alertness must be aware of this.
Hearing loss:
As reported, it can result in permanent or transient hearing loss.
Quinidine, a contraindicated medication, was used in multiple of these cases concurrently.
Most patients experience hearing loss within a few days of stopping therapy. However, some patients may have persistent hearing problems.
Heart failure: [US Boxed Warning]:
Itraconazole may cause or exacerbate heart failure (HF) in patients already suffering from it.
Inotropic effects can be caused by intravenous administration.
It is best to avoid heart disease in patients at high risk (edematous disorders or COPD), and those with a history of valvular disease.
These patients should be made aware of the symptoms and treatment options for HF.
If you notice HF symptoms or signs, discontinue treatment.
Post-marketing data showed that HF was more common in patients who received a daily total dose of 400mg, but there were cases among patients who took lower daily doses.
Itraconazole, according to the American Heart Association (magnitude : major), may cause underlying myocardial dysfunction (magnitude : major). This should be avoided if you are treating serious fungal infections (AHA [Page 2016,]).
Hepatotoxicity:
Rare cases of severe hepatotoxicity (including death and liver failure) have been reported. Some cases occurred within the first week of treatment.
If you notice signs or symptoms of hepatotoxicity, discontinue treatment.
Hypersensitivity
Reports of hypersensitivity reactions have been made. If you experience one, stop using the medication and get supportive care.
Patients with a history or hypersensitivity to other Azoles should be cautious.
Neuropathy:
Patients on long-term itraconazole have been known to develop peripheral neuropathy.
If you notice any signs or symptoms of neuropathy, discontinue treatment immediately.
Cystic Fibrosis:
Cystic Fibrosis patients who received the oral solution showed large differences in their pharmacokinetic parameters. Alternative therapies should be considered if they do not respond to therapy.
Hepatic impairment
Patients with hepatic impairment should be cautious; closely monitor liver function.
Patients with liver disease or elevated liver enzymes are not recommended.
Onychomycosis: [US Boxed Warning]:
Patients with heart failure (HF), ventricular dysfunction (HF) or a history are not recommended for onychomycosis treatment.
This patient population has seen cases of HF, peripheral and pulmonary embolisms.
Before treating onychomycosis, the manufacturer suggests that nail specimens be tested for diagnosis.
Renal impairment
Patients with impaired renal function should be cautious. There is limited information available. Dosage adjustment may be necessary.
Monitoring parameters:
Liver function in patients with preexisting hepatic dysfunction, and in all patients as clinically indicated;
renal function;
signs/symptoms of HF
For invasive aspergillosis (treatment or prolonged prophylaxis), guidelines recommend monitoring serum trough concentrations.
Consider monitoring serum trough concentrations for other infections; itraconazole has a variable pharmacokinetic profile and high concentrations may increase the risk of adverse events.
How to administer Itraconazole ?
Oral: Formulations are not interchangeable; generally, the oral solution is the preferred formulation because of improved absorption.
Administer capsule and tablet with a full meal.
The oral solution should be taken on an empty stomach; when treating oropharyngeal and esophageal candidiasis, the solution should be swished vigorously in the mouth (10 mL at a time), then swallowed. Swallow capsule whole; do not crush, chew, or break.
Mechanism of action of Itraconazole :
It inhibits cytochrome P450 activity and decreases ergosterol synthesis (principal sterol found in fungal cell membranes).
Absorption
Capsule: 100mg Sporanox capsule (Sporanox), requires gastric acidity (absorption increases when taken with food).
Tolsura 65 mg capsule (Tolsura 65 mg capsule), has a higher absorption when taken empty stomach. However, Tolsura (2×65 mg capsule) when combined with food can result in exposures similar those experienced when Sporanox (2×100 mg capsule) is taken with food.
Oral solution: Absorption increased when empty stomach.
Tablet: Prefers gastric acidity. Absorption is increased when taken with food.
Distribution:
Plasma concentrations are lower than plasma concentrations because they are highly lipophilic.
Concentrations of the highest amount are found in adipose and skin/nails, omentum and endometrium, cervical mucus, vaginal mucus and cervical mucus.
The concentrations of aqueous fluids, such as CSF and urine, are negligible. They can be distributed into bronchial exudate or sputum.
Protein binding, plasma:
99.8%; metabolite hydroxy-itraconazole: 99.6%
Metabolism:
Extensively hepatic via CYP3A4 into >30 metabolites including hydroxy-itraconazole (major metabolite); appears to have in vitro antifungal activity.
The main metabolic pathway is oxidation; may undergo saturation metabolism with multiple dosing.
Bioavailability:
Variable, ~55% increases by 30% under fasted conditions (oral solution);
Note: The oral solution has a higher degree of bioavailability (149% ± 68%) relative to oral capsules; should not be interchanged
Half-life elimination:
Children (6 months to 12 years):
Oral solution: ~36 hours;
Metabolite hydroxy-itraconazole: ~18 hours
Adults: Oral:
Single-dose: 16 to 28 hours,
Multiple doses: 34 to 42 hours;
Cirrhosis (single dose): 37 hours (range: 20 to 54 hours)
Time to peak, plasma:
Capsules/tablets: 2 to 5 hours;
Oral solution: 2.5 hours
Excretion:
Urine (<1% active drug, 35% as inactive metabolites);
feces (54%; ~3% to 18% as unchanged drug)
What happens if I miss a dose?
Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.
What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.
What should I avoid while taking itraconazole?
Avoid driving or hazardous activity until you know how itraconazole will affect you. Your reactions could be impaired.
Avoid taking antacids within 1 hour before or 2 hours after you take itraconazole. Some antacids can make it harder for your body to absorb itraconazole.
International Brand Names of Itraconazole:
Onmel
Sporanox
Sporanox Pulsepak
Tolsura
JAMP Itraconazole
MINT-Itraconazole
Sporanox
Arozole
Canadiol
Candistat
Canditral
Chme
Cladosol
Conazole
Funginox
Fungizol
Funit
Hantrazol
Hitrazole
Icomein
Icon
Iconal
Ikonaz
Inox
Isox
Itcozol
Itol
Itra
Itrabloxus
Itrac
Itracap
Itracon
Itrafung
Itragen
Itramed
Itranax
Itranol
Itranols
Itranox
Itrapex
Itrasix
Itrason
Itraspor
Itrazol
Itrazole
Itrizole
Itzol
Konitra
Lozanoc
Micogal
Micoral
Mycotrazol
Newtrazole
Norspor
Nufatrac
Omicral
Orugal
Orungal
Orzol
Quali-Itrazole
Rixtal
Sempera
Sinozol
Spazol
Sponex
Sporacid
Sporagal
Sporal
Sporanox
Sporanox IV
Sporavast
Spornar
Spyrocon
Trachon
Tracon
Tracor
Unitrac
Vanoran
join with us to know more drugs like this- whatsapp grp1
