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Oxymetazoline

AFRIN

Pronunciation: ox-i-me-TAZ-oe-leen

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

What it isAlpha-1 and alpha-2 agonist causing local vasoconstriction; nasal congestion and rosacea erythema.

Why this oneThe same rapid topical vasoconstriction also makes it useful for epistaxis without systemic decongestant exposure.

What limits itContinuous nasal use beyond three days can cause severe rebound congestion and escalating spray dependence.

Oxymetazoline molecular structure (skeletal formula)
Molecular structure: Oxymetazoline

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Nasal congestionAdults & children ≥6 yr (with supervision)2-3 sprays each nostril q10-12h PRN2 doses per 24 h

Renal Undefined

Hepatic Undefined

Do not exceed 2 doses in any 24-hour period

Instructions

Available strengths

Pregnancy Undefined

Lactation Undefined

Cost

Oxymetazoline (AFRIN)
Strength#/mogeneric $/unitCostPlus
0.05 g/100 mLsprayper unitnot offered
NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Oxymetazoline is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2021

NO BOXED WARNINGS

Principal riskRebound congestion after three days

Classes and tags

Clinical profile

Therapeutic safety burden0 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk0 / 4

Legacy pregnancy categoryC

Defining liabilityLocal irritation, sensitization or administration-site injury; negligible systemic toxicity at usual use.

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