Generic
Itraconazole
56 brands available in the market
At a glance
Itraconazole is an antifungal medication used for the treatment of fungal infections of the mouth, throat, vagina, skin, and nails.
Description
Itraconazole is a triazole antifungal drug that inhibits Cytochrome P-450 dependent enzymes resulting in impairment of ergosterol biosynthesis, a major component of the cell membrane of yeast and fungal cells. It is used for oropharyngeal candidiasis, vulvovaginal candidiasis, pityriasis versicolor, tinea pedis, tinea cruris, tinea corporis, tinea manuum, onychomycosis, histoplasmosis, systemic candidiasis, aspergillosis, and cryptococcosis.
Indications
- Oropharyngeal candidiasis
- Vulvovaginal candidiasis
- Pityriasis versicolor
- Tinea pedis, tinea cruris, tinea corporis, tinea manuum
- Onychomycosis (fungal nail infections)
- Histoplasmosis
- Systemic candidiasis
- Aspergillosis
- Cryptococcosis
Therapeutic class
Drugs for subcutaneous and mycoses
Pharmacological class
Triazole Antifungal
Pharmacology
Itraconazole inhibits Cytochrome P-450 dependent enzymes resulting in impairment of ergosterol biosynthesis, a major component of the cell membrane of yeast and fungal cells. Being integral to proper functioning of the cell membrane, inhibition of ergosterol synthesis leads to abnormalities in permeability, membrane bound enzyme activity, and coordination of chitin synthesis, leading to inhibition of growth, abnormal cell wall formation and accumulation of intracellular lipids and membranous vesicles.
Mechanism of action
Inhibits Cytochrome P-450 enzymes to disrupt ergosterol synthesis and fungal cell membrane function, killing the fungus.
Dosage
Adult Dose (Oral):
- Vulvovaginal candidiasis: 200 mg twice daily × 1 day
- Pityriasis versicolor: 200 mg once daily × 7 days
- Tinea corporis/cruris: 100 mg once daily × 15 days or 200 mg once daily × 7 days
- Tinea pedis/manuum: 100 mg once daily × 30 days
- Oropharyngeal candidiasis: 100 mg once daily × 15 days
- Onychomycosis: 200 mg once daily × 3 months or pulse therapy: 200 mg twice daily × 7 days, 21 days off, repeat
- Systemic fungal infections: 100-200 mg once daily; invasive/disseminated: 200 mg twice daily
Child Dose (Oral):
- 10 mg/kg/day (max 200 mg/day) q12h; 5 mg/kg/day q24h for chronic mucocutaneous Candida
- <3 years: Safety and efficacy not established
Administration
Take with food; swallow whole tablet/capsule; do not chew, crush or break; take antacids 2 hours before or after taking Itraconazole.
Missed dose
If you miss a dose, take it as soon as possible; if it is almost time for your next dose, skip the missed dose and go back to regular schedule; do not double the dose.
Side effects
Common Side Effects:
- Nausea
- Abdominal pain
- Dyspepsia
- Constipation
- Headache
- Dizziness
- Raised liver enzymes
- Menstrual disorders
Others: Allergic reactions (pruritus, rash, urticaria, angioedema), hepatitis and cholestatic jaundice, peripheral neuropathy, Stevens-Johnson syndrome, hypokalemia, edema, hair loss (with prolonged use)
Precautions & warnings
Precautions:
- Itraconazole may affect your ability to drive (dizziness, blurred/double vision, hearing loss)
- Absorption is impaired when gastric acidity is reduced; take antacids 2 hours after Itraconazole
- Take after a full meal
- Monitor liver function regularly (treatment >1 month)
- Inform doctor if signs of jaundice (yellowing of eyes or skin, dark urine, stomach pain)
- Contraindicated in pregnancy and lactation
Contraindications
Contraindications:
- Hypersensitivity to azole antifungals
- Pregnancy and lactation
- Hepatic disease
- Severe liver disease
- Patients taking rifampin
Drug interactions
Drug Interactions:
- Do not use with terfenadine, astemizole, cisapride, HMG-CoA reductase inhibitors (simvastatin), oral midazolam or triazolam
- Significant interactions with rifampin, phenytoin, phenobarbital, digoxin, calcium channel blockers
- Antacids, PPIs, H2 receptor antagonists reduce absorption
- Strong CYP3A4 inhibitors (azole antifungals, macrolides, HIV protease inhibitors) increase plasma concentration
Food interactions
Food Interactions: Caution is advised when consuming alcohol with Itraconazole; consult your doctor.
Use in pregnancy
Use in Pregnancy: May be unsafe; animal studies have shown harmful effects; contraindicated in pregnancy.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; limited data suggests drug may pass into breastmilk and harm baby; not recommended during breastfeeding.
Pediatric use
Safety and efficacy not established in children under 3 years; dose for children over 3 years provided above.
Geriatric use
No specific dosage adjustment needed for elderly; however caution advised.
Renal / hepatic impairment
Renal Impairment: Limited information available; caution required; IV contraindicated with CrCl <30 mL/min.
Hepatic Impairment: Caution in liver disease; contraindicated in severe hepatic disease; inform doctor if signs of jaundice.
Overdose effects
Overdose: No experience of overdosage; if accidental overdose occurs, gastric lavage and symptomatic treatment; no specific antidote.
Storage conditions
Store below 25°C, in a cool & dry place; keep away from light; keep out of reach of children.
Chemical structure
Itraconazole