Oxymetazoline (Topical) (Monograph)

Brand name: Rhofade
Drug class: Skin and Mucous Membrane Agents, Miscellaneous
Chemical name: Phenol, 3-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-6-(1,1-dimethylethyl)-2,4-dimethyl-, monohydrochloride
Molecular formula: C₁₆H₂₄N₂O•HCl
CAS number: 2315-02-8

Medically reviewed by Drugs.com on May 11, 2023. Written by ASHP.

Introduction

Vasoconstrictor; an imidazoline-derivative sympathomimetic amine.

Uses for Oxymetazoline (Topical)

Rosacea

Used topically for the treatment of persistent (nontransient) facial erythema associated with rosacea (acne rosacea).

Oxymetazoline (Topical) Dosage and Administration

Administration

Topical Administration

Apply topically as a 1% cream; available in a tube or pump bottle.

For external use only. Do not administer orally, ophthalmically, or vaginally.

Prime pump bottle prior to initial use by actuating until cream appears, followed by 3 additional pumps; discard cream from priming actuations. Necessary only to prime the pump prior to first dose.

Apply smoothly and evenly as a thin layer across the entire face. Avoid contact with the eyes and lips; wash hands immediately after application.

Dosage

Available as oxymetazoline hydrochloride; dosage expressed in terms of the salt. Each gram of cream contains 10 mg (1%) of oxymetazoline hydrochloride equivalent to 8.8 mg (0.88%) of oxymetazoline free base.

Adults

Rosacea

Topical

Apply a pea-sized amount once daily to the 5 facial areas (forehead, chin, nose, and each cheek).

Cautions for Oxymetazoline (Topical)

Contraindications

• Manufacturer states none known.

Warnings/Precautions

Cardiovascular Effects

α₁-Adrenergic agonists (e.g., oxymetazoline) can affect BP. Use with caution in patients with severe, unstable, or uncontrolled cardiovascular disease; orthostatic hypotension; and/or uncontrolled hypertension/hypotension. Advise patients with cardiovascular disease, orthostatic hypotension, and/or uncontrolled hypertension/hypotension to obtain immediate medical care if their condition worsens.

Potentiation of Vascular Insufficiency

Use with caution in patients with cerebral or coronary insufficiency, Raynaud's phenomenon, thromboangiitis obliterans, scleroderma, or Sjögren's syndrome. Advise patients to obtain immediate medical care if signs and/or symptoms of potentiation of vascular insufficiency develop.

Angle-Closure Glaucoma

Possible increased risk of angle-closure glaucoma in patients with narrow-angle glaucoma. Advise patients to obtain immediate medical care if signs and/or symptoms of acute angle-closure glaucoma develop.

Serious Adverse Reactions Following Ingestion

Serious adverse reactions requiring hospitalization (e.g., nausea, vomiting, lethargy, tachycardia, decreased respiration, bradycardia, hypotension, hypertension, sedation, somnolence, mydriasis, stupor, hypothermia, drooling, coma) reported in children following accidental ingestion of oxymetazoline nasal solutions.

Store oxymetazoline cream out of reach of children.

Specific Populations

Pregnancy

No adequate or well-controlled studies of topical oxymetazoline in pregnant women. No adequate data regarding topical use of the drug in pregnant women.

No evidence of developmental abnormalities in animal studies with oral oxymetazoline.

Lactation

Distributed into milk in rats. Not known whether distributed into human milk. Effects of drug on nursing infants or human milk production unknown.

Consider benefits of breast-feeding and importance of the drug to the woman; also consider potential adverse effects on the breast-fed child from the drug or underlying maternal condition.

Pediatric Use

Safety and efficacy not established in children <18 years of age.

Accidental ingestion of oxymetazoline nasal solution has caused serious adverse reactions in children. (See Serious Adverse Reactions Following Ingestion under Cautions.)

Geriatric Use

No overall differences in safety and efficacy observed in patients ≥65 years of age compared with younger patients. Clinical studies of oxymetazoline did not include sufficient numbers of patients ≥65 years of age to determine whether they respond differently than younger adults.

Common Adverse Effects

Dermatitis, pruritus, erythema, and pain at application site; worsening inflammatory lesions of rosacea.

Drug Interactions

Does not inhibit CYP isoenzymes 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A4/5 in vitro. Not an inducer of CYP isoenzymes 1A2, 2B6, or 3A4 in vitro.

Specific Drugs

Oxymetazoline (Topical) Pharmacokinetics

Absorption

Bioavailability

Following topical administration of oxymetazoline hydrochloride cream (approximately 0.3 g to the entire face) in patients with erythema associated with rosacea, plasma concentrations of drug are measurable.

Distribution

Extent

Distributed into milk in rats; not known whether distributed into human milk.

Plasma Protein Binding

56.7–57.5%.

Elimination

Metabolism

Minimally metabolized by hepatic microsomal enzymes in vitro.

Elimination Route

Excretion not determined in humans.

Stability

Storage

Topical

Cream

20–25°C (may be exposed to 15–30°C).

Actions

• Imidazoline derivative sympathomimetic amine that acts as a vasoconstrictor.

• Highly selective α_1A-adrenergic agonist and partially selective α_2A-adrenergic agonist.

• Topical application appears to reduce erythema through direct vasoconstriction.

• May act by targeting α-adrenergic receptors present in the smooth muscle sheath encasing the vessel wall of superficial cutaneous blood vessels.

Advice to Patients

• Importance of giving patients a copy of the patient information provided by the manufacturer.

• Importance of advising patients to use oxymetazoline cream only as directed by a clinician.

• Importance of advising patients that the cream is for external use only and to avoid contact with the eyes and lips. Importance of not using the drug orally, ophthalmically, or intravaginally.

• Importance of advising patients using the pump bottle to prime the pump before initial use and to discard the cream resulting from the priming actuations.

• Importance of advising patients not to apply the cream to irritated skin or open wounds.

• Importance of washing hands immediately after application.

• Importance of advising patients to report adverse reactions to a clinician.

• Importance of advising patients to keep the cream out of the reach of children. (See Serious Adverse Reactions Following Ingestion under Cautions.)

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses, including glaucoma and cardiovascular disease.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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