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Posaconazole

NOXAFIL

What it isTriazole antifungal; prophylaxis in neutropenia and mucormycosis.

Why this oneThe broadest azole spectrum, covering Mucorales, which voriconazole does not.

What limits itA strong CYP3A4 inhibitor. The delayed-release tablet absorbs far better than the suspension and they are not interchangeable.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Prophylaxis of invasive Aspergillus and Candida infectionsAdults300 mg BID ×1 day (load)300 mg QD300 mg QD
Prophylaxis of invasive Aspergillus and Candida infectionsPeds 13 to <18 yr, >40 kg300 mg BID ×1 day (load)300 mg QD300 mg QD

Renal No dosage adjustment; monitor closely for breakthrough fungal infections in severe renal impairment

Hepatic Undefined

Not substitutable with the oral suspension / PowderMix formulations

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy May cause fetal harm based on animal data (skeletal malformations)

Lactation No human data; present in rat milk

NO BOXED WARNINGS

Principal riskA strong CYP3A4 inhibitor; formulations are not interchangeable

Cost, est. cash$10–$300/month

Generic entry2019

Classes and tags

Clinical profile

Therapeutic safety burden3 / 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 liabilityHepatotoxicity and clinically important CYP/QT interactions; organ toxicity varies markedly by agent.

Mechanism of action: Posaconazole ballicule

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

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