Ketoconazole

NIZORAL

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Pronunciation: kee-toe-KON-na-zoel

Ketoconazole ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Ketoconazole ballicule

Ketoconazole NIZORAL mascot mnemonic cartoon — Visual mnemonic: Ketoconazole mascot
**“Key to cone (Nice oral)”**

What it isImidazole antifungal enzyme inhibitor; fungal infections, with systemic use now restricted.

Why this oneIts steroid-synthesis blockade makes oral ketoconazole useful for lowering cortisol in Cushing syndrome.

What limits itSystemic use can cause severe hepatotoxicity and QT prolongation; potent CYP3A4 inhibition drives major interactions.

Ketoconazole molecular structure (skeletal formula) — Molecular structure: Ketoconazole

FDA-approved for

fungal infections (1981)
Cushing syndrome (off-label)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Hepatotoxicity (some fatal); not for onychomycosis or skin/Candida infections—use only when other antifungals unavailable/not tolerated; QT prolongation with certain coadministered drugs

FDA dosing	Population	Start	Target	Max
Systemic fungal infection	adult	200 mg QD		400 mg QD
Systemic fungal infection	children >2 yr	3.3-6.6 mg/kg QD

Renal Undefined

Hepatic Undefined

Instructions

Document infection (lab and clinical) before starting
Usual duration for systemic infection is 6 months; continue until active infection subsides
Not studied in children under 2 yr

Available strengths

tab 200 mg
cream 2 %
shampoo 1, 2 %
sol 0.01 g/mL
susp 20 mg/mL
foam 2 %
soap 1 g/100 g

Cautions

Hepatotoxicity, including fatalities—monitor liver function
QT prolongation/torsades with coadministered drugs
Anaphylaxis/anaphylactoid reactions
Adrenal insufficiency at higher doses (cortisol suppression)

Adverse reactions

Nausea, vomiting, abdominal pain
Hepatitis, jaundice, abnormal hepatic function
Rash, pruritus, urticaria
Headache, dizziness
Gynecomastia

Pregnancy Undefined

Lactation Undefined

Cost

Ketoconazole (NIZORAL)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $	CostPlus
200 mg	tab	30 qd	$19.37/mo	offered
2 %	cream	per unit		not offered
1 %	shampoo	per unit		not offered
2 %	shampoo	per unit		not offered

Generic entry1986

⚠ BOXED WARNINGS

Hepatotoxicity
QT prolongation and drug interactions

Classes and tags

Clinical profile

Therapeutic safety burden4 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades2 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilitySevere hepatotoxicity, adrenal suppression and strong CYP3A inhibition restrict systemic use.

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Memory aids: interaction avatars

CYP3A4 inhibitor (strong)

P-gp inhibitor (strong)

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