Itraconazole

SPORANOX

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What it isTriazole antifungal; onychomycosis, histoplasmosis and blastomycosis.

Why this oneIt covers the endemic dimorphic fungi that fluconazole does not.

What limits itNegative inotropy, so it is contraindicated in heart failure. A strong CYP3A4 inhibitor; capsules need acid and food, the solution does not.

FDA-approved for

fungal infections (1992)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Negative inotropy/CHF — do not use for onychomycosis in ventricular dysfunction or CHF. Numerous CYP3A4-substrate drugs are contraindicated (risk of QT prolongation and torsade de pointes).

FDA dosing	Population	Start	Target	Max
Blastomycosis / Histoplasmosis	Adult	200 mg QD	200 mg QD	400 mg/day (doses >200 mg/day split BID)
Aspergillosis	Adult	200 mg/day	200-400 mg/day	400 mg/day
Life-threatening infection (loading)	Adult	200 mg TID (600 mg/day) x3 days	then usual maintenance
Onychomycosis — toenail	Adult	200 mg QD	200 mg QD x12 weeks
Onychomycosis — fingernail (pulse)	Adult	200 mg BID x1 week	200 mg BID x1 week per pulse

Renal Limited data; use with caution.

Hepatic Limited data; use with caution.

Fingernail onychomycosis: two 1-week pulses separated by a 3-week interval without drug.

Instructions

Take with a full meal to ensure maximal absorption
Swallow capsules whole
Capsules and oral solution are not interchangeable (only the solution is effective for oral/esophageal candidiasis)

Contraindications

Onychomycosis in patients with ventricular dysfunction or CHF / history of CHF
Onychomycosis in pregnant patients or women contemplating pregnancy

Cautions

Rare serious hepatotoxicity, including liver failure and death — monitor LFTs
Negative inotropic effect / risk of congestive heart failure
Many contraindicated CYP3A4-substrate co-medications (QT prolongation, torsade de pointes)

Adverse reactions

Nausea, vomiting, diarrhea
Rash, pruritus
Headache, dizziness
Edema, fatigue
Abnormal hepatic function
Hypertension, hypokalemia

Pregnancy Contraindicated for onychomycosis in pregnancy or women contemplating pregnancy.

Lactation Undefined

⚠ BOXED WARNINGS

Negative inotropy and heart failure
Drug interactions from CYP3A4 inhibition

Cost, est. cash$10–$300/month

Generic entry2004

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityHeart-failure risk, hepatotoxicity and strong CYP3A inhibition.

Mechanism of action: Itraconazole ballicule

Itraconazole ballicule: receptor binding, kinetics and half-life diagram

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Memory aids: mascots and interaction avatars

Itraconazole SPORANOX mascot mnemonic cartoon — **“Spore-knocking Eye tracker”**
Strong CYP3A4 inHibitor

CYP3A4 inhibitor (strong)

Open Itraconazole in the interactive console ↗