Dosing & Uses
Dosage Forms & Strengths
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
Rosacea
Indicated for the topical treatment of persistent facial erythema associated with rosacea in adults
Apply topically qDay; use a pea-sized amount of cream in a thin layer to cover the entire face (forehead, nose, each cheek, and chin), avoiding the eyes and lips
Wash hands immediately after application
<18 years: Safety and efficacy not established
Dosage Forms & Strengths
topical cream 1% (available in a tube or pump bottle)
Rosacea
Indicated for the topical treatment of persistent facial erythema associated with rosacea in adults
Apply topically qDay; use a pea-sized amount of cream in a thin layer to cover the entire face (forehead, nose, each cheek, and chin) avoiding the eyes and lips
Wash hands immediately after application
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (0)
Serious - Use Alternative (0)
Monitor Closely (31)
- alfuzosin
oxymetazoline topical increases and alfuzosin decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- atenolol
oxymetazoline topical increases and atenolol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- betaxolol
oxymetazoline topical increases and betaxolol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- bisoprolol
oxymetazoline topical increases and bisoprolol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- carvedilol
oxymetazoline topical increases and carvedilol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- digoxin
oxymetazoline topical decreases effects of digoxin by pharmacodynamic synergism. Use Caution/Monitor. Digoxin reduces catecholamine reuptake at nerve terminals, rendering blood vessels more sensitive to endogenous or exogenous catecholamines.
- doxazosin
oxymetazoline topical increases and doxazosin decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- droxidopa
oxymetazoline topical and droxidopa both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- ephedrine
oxymetazoline topical and ephedrine both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- epinephrine
oxymetazoline topical and epinephrine both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- esmolol
oxymetazoline topical increases and esmolol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- isocarboxazid
oxymetazoline topical and isocarboxazid both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- labetalol
oxymetazoline topical increases and labetalol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- metoprolol
oxymetazoline topical increases and metoprolol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- midodrine
oxymetazoline topical and midodrine both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- nadolol
oxymetazoline topical increases and nadolol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- nebivolol
oxymetazoline topical increases and nebivolol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- norepinephrine
oxymetazoline topical and norepinephrine both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- penbutolol
oxymetazoline topical increases and penbutolol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- phenelzine
oxymetazoline topical and phenelzine both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- phenoxybenzamine
oxymetazoline topical increases and phenoxybenzamine decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- phentolamine
oxymetazoline topical increases and phentolamine decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- phenylephrine
oxymetazoline topical and phenylephrine both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- prazosin
oxymetazoline topical increases and prazosin decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- propranolol
oxymetazoline topical increases and propranolol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- silodosin
oxymetazoline topical increases and silodosin decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- sotalol
oxymetazoline topical increases and sotalol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- tamsulosin
oxymetazoline topical increases and tamsulosin decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- terazosin
oxymetazoline topical increases and terazosin decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- timolol
oxymetazoline topical increases and timolol decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- tranylcypromine
oxymetazoline topical and tranylcypromine both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
Minor (0)
Adverse Effects
1-10%
Application-site dermatitis (2%)
Worsening inflammatory lesions of rosacea (1%)
Application-site pruritus (1%)
Application-site erythema (1%)
Application-site pain (1%)
Warnings
Contraindications
None
Cautions
Alpha-adrenergic agonists may increase blood pressure; use caution with severe, unstable, or uncontrolled cardiovascular disease, orthostatic hypotension, or uncontrolled hypertension or hypotension; advise patients to seek immediate medical care if their condition worsens
Caution with cerebral or coronary insufficiency, Raynaud phenomenon, thromboangiitis obliterans, scleroderma, or SjÖgren syndrome; advise patients to seek immediate medical care if signs and symptoms of vascular insufficiency develop
May increase risk of angle-closure glaucoma in patients with narrow-angle glaucoma; advise patients to seek immediate medical care if signs and symptoms of acute angle-closure glaucoma develop
Drug interaction overview
- Antihypertensives or cardiac glycosides: Alpha-adrenergic agonists, as a class, may increase blood pressure; caution with coadministration of beta-blockers, antihypertensives, and/or cardiac glycosides
- Monoamine oxidase (MAO) inhibitors: Caution is advised if coadministered with MAO inhibitors, which can affect the metabolism and uptake of circulating amines
- Other alpha1 adrenergic receptor agonists: Use caution in patients receiving alpha1 adrenergic receptor antagonists (eg, treatment of cardiovascular disease, benign prostatic hypertrophy, or Raynaud disease)
Pregnancy
Pregnancy
No available data on oxymetazoline topical use in pregnant women to inform a drug-associated risk for major birth defects and miscarriage
Data describing intranasal decongestant use in pregnant women identified a potential association between second-trimester exposure to oxymetazoline (with no decongestant exposure in the first trimester) and renal collecting system anomalies
Lactation
Unknown if distributed in human breast milk
Oxymetazoline was detected in the milk of lactating rats
Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Alpha1A-adrenoceptor agonist; elicits vasoconstriction of the cutaneous microvasculature
Absorption
Peak plasma concentration: 60.5 pg/mL (first dose); 66.4 pg/mL (28-days)
AUC: 895 pg·hr/mL (first dose); 1050 pg·hr/mL (28-days)
Distribution
Protein bound: ~57%
Metabolism
Minimally metabolized (~4%)
Elimination
Not characterized in humans
Administration
Topical Preparation
Tubes do not require priming
Pumps
- Pumps require priming before initial use and discard product from the first 3 pumps with the pump in the upright position; repeatedly depress the actuator until cream is dispensed and then pump 3 times
- Discard the cream from priming actuations
- It is only necessary to prime the pump before the first dose
Topical Administration
Use a pea-sized amount of cream once daily in a thin layer to cover the entire face (forehead, nose, each cheek, and chin)
Avoid contact with the eyes and lips
Wash hands immediately after application For topical use only; not for oral, ophthalmic, or intravaginal use
Do not to apply to irritated skin or open wounds
Storage
Store at controlled room temperature (20-25°C [68-77°F]); excursions permitted to 15-30°C (59-86°F)
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Formulary
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