Oxymetazoline

DEA Class;  Rx

Common Brand Names;

Ophthalmic: Upneeq

Intranasal OTC: Afrin, Duramist Plus, Dristan 12 Hr, Cheracol Nasal, Duration, Genasal, QlearQuil 12 Hour Nasal Decongestant Moisturizing Spray, Sinarest 12 Hour, Vicks Sinex 12 Hour

Topical: Rhofade

  • Alpha Agonists, Ophthalmic
  • Decongestants, Intranasal
  • Alpha Agonists, Topical

Intravenous catecholamine
Used for restoration of blood pressure in patients with acute hypotensive states
Potent alpha-adrenergic receptor agonist with modest beta-agonist activity

Indicated for acquired blepharoptosis in adults

Indicated for temporary relief of nasal congestion

Indicated for the topical treatment of persistent facial erythema associated with rosacea in adults

Hypersensitivity

  • Punctate keratitis (1-5%)
  • Conjunctival hyperemia (1-5%)
  • Dry eye (1-5%)
  • Blurred vision (1-5%)
  • Instillation site pain (1-5%)
  • Eye irritation (1-5%)
  • Headache (1-5%)
Intranasal OTC
  • Insomnia
  • Headache
  • Burning
  • Stinging
  • Dryness
  • Sneezing
  • Rebound congestion

Topical

  • Application-site dermatitis (2%)
  • Worsening inflammatory lesions of rosacea (1%)
  • Application-site pruritus (1%)
  • Application-site erythema (1%)
  • Application-site pain (1%)

Alpha-adrenergic agonists may impact blood pressure; caution with severe or unstable cardiovascular disease, orthostatic hypotension, and uncontrolled hypertension or hypotension

Caution with cerebral insufficiency, coronary insufficiency, or Sjögren syndrome

May increase risk of angle-closure glaucoma in patients with untreated narrow-angle glaucoma

Advise patients to seek medical care if signs and symptoms of cardiovascular disease, vascular insufficiency, or acute angle-closure glaucoma develop

Ptosis may be associated with neurologic or orbital diseases such as stroke and/or cerebral aneurysm, Horner syndrome, myasthenia gravis, external ophthalmoplegia, orbital infection and orbital masses; give consideration to these conditions in the presence of ptosis with decreased levator muscle function and/or other neurologic signs

Ophthalmic

Data are not available regarding use during pregnancy to inform a drug-associated risk for major birth defects and miscarriage

Data are unavailable to assess effects on breastmilk quantity or production, or to establish the level of oxymetazoline present in human breastmilk

Intranasal OTC

Pregnancy category: C

Lactation: Not known if excreted in breast milk

Topical

No available data on oxymetazoline topical use in pregnant women to inform a drug-associated risk for major birth defects and miscarriage

Unknown if distributed in human breast milk

Adults

8 drops/eye/day of the 0.025% ophthalmic solution; 1 drop/eye/day of the 0.1% ophthalmic solution; 6 sprays/nostril/day of the nasal spray; 1 topical application/day of the cream.

Geriatric

8 drops/eye/day of the 0.025% ophthalmic solution; 1 drop/eye/day of the 0.1% ophthalmic solution; 6 sprays/nostril/day of the nasal spray; 1 topical application/day of the cream.

Adolescents

8 drops/eye/day of the 0.025% ophthalmic solution; 6 sprays/nostril/day of the nasal spray; safety and efficacy have not been established for the 0.1% ophthalmic solution or the topical cream.

Children

6 to 12 years: 8 drops/eye/day of the 0.025% ophthalmic solution; 6 sprays/nostril/day of the nasal spray; safety and efficacy have not been established for the 0.1% ophthalmic solution or the topical cream.
1 to 5 years: Safety and efficacy have not been established.

Infants

Safety and efficacy have not been established.

Neonates

Safety and efficacy have not been established.

Norepinephrine bitartrate 

ophthalmic solution

  • 0.1% (as HCl salt [0.09% as base])

Intranasal solution

  • 0.05%

topical cream

  • 1% (available in a tube or pump bottle)
  • Each gram of cream contains 10 mg (1%) oxymetazoline hydrochloride, which is equivalent to 8.8 mg (0.88%) of oxymetazoline free base

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