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Oxymetazoline Hydrochloride

Class: Skin and Mucous Membrane Agents, Miscellaneous
Chemical Name: 6-tert-butyl-3-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2,4-dimethylphenol;hydrochloride
Molecular Formula: C16H25ClN2O
CAS Number: 1491-59-4
Brands: Rhofade

Introduction

Oxymetazoline hydrochloride, an alpha1A adrenoceptor agonist, is a vasoconstrictor.1

Uses for Oxymetazoline Hydrochloride

Oxymetazoline hydrochloride has the following uses:

Oxymetazoline hydrochloride is an alpha1A adrenoceptor agonist indicated for the topical treatment of persistent facial erythema associated with rosacea in adults.1

Oxymetazoline Hydrochloride Dosage and Administration

General

Oxymetazoline hydrochloride is available in the following dosage form(s) and strength(s):

Cream, 1%. Each gram of cream contains 10 mg (1%) oxymetazoline hydrochloride, equivalent to 8.8 mg (0.88%) of oxymetazoline free base.1

Dosage

It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

  • Not for oral, ophthalmic, or intravaginal use.1

  • Prime pump bottle before initial use and discard product from first three pumps.1

  • Apply a pea-sized amount once daily in a thin layer to cover the entire face (forehead, nose, each cheek, and chin) avoiding the eyes and lips.1

  • Wash hands after application.1

Cautions for Oxymetazoline Hydrochloride

Contraindications

  • None.1

Warnings/Precautions

Potential Impacts on Cardiovascular Disease

Alpha-adrenergic agonists may impact blood pressure. Oxymetazoline hydrochloride topical cream should be used with caution in patients with severe or unstable or uncontrolled cardiovascular disease, orthostatic hypotension, and uncontrolled hypertension or hypotension. Advise patients with cardiovascular disease, orthostatic hypotension, and/or uncontrolled hypertension/hypotension to seek immediate medical care if their condition worsens. 1

Potentiation of Vascular Insufficiency

Oxymetazoline hydrochloride topical cream should be used with caution in patients with cerebral or coronary insufficiency, Raynaud's phenomenon, thromboangiitis obliterans, scleroderma, or Sjögren's syndrome. Advise patients to seek immediate medical care if signs and symptoms of potentiation of vascular insufficiency develop. 1

Risk of Angle Closure Glaucoma

Oxymetazoline hydrochloride topical cream may increase the 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. 1

Specific Populations

Pregnancy

There are no available data on the use of oxymetazoline hydrochloride topical cream in pregnant women to inform a drug-associated risk for major birth defects and miscarriage. A literature article describing use of intranasal oxymetazoline as a decongestant 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. In animal reproduction studies, there were no adverse developmental effects observed after oral administration of oxymetazoline hydrochloride in pregnant rats and rabbits at systemic exposures up to 3 and 73 times, respectively, the exposure associated with the maximum recommended human dose (MRHD). The estimated background risks of major birth defects and miscarriage for the indicated population are unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. 1

Following repeated use of oxymetazoline hydrochloride solution nasal spray for the treatment of nasal congestion at a dose 5 times higher than recommended, one case of fetal distress was reported in a 41-week pregnant patient. The fetal distress resolved hours later, prior to the delivery of the healthy infant. The anticipated exposures for the case are 8- to 18-fold higher than plasma exposures after topical administration of oxymetazoline hydrochloride cream. 1

No adequate and well-controlled trials of oxymetazoline hydrochloride topical cream have been conducted in pregnant women. Across all clinical trials of oxymetazoline hydrochloride topical cream, two pregnancies were reported. One pregnancy resulted in the delivery of a healthy child. One pregnancy resulted in a spontaneous abortion, which was considered to be unrelated to the trial medication. A literature article summarizing the results of exploratory analyses of use of intranasal oxymetazoline as a decongestant during pregnancy identified a potential association between second-trimester exposure to oxymetazoline hydrochloride solution (with no decongestant exposure in the first trimester) and renal collecting system anomalies. 1

Effects on embryo-fetal development were evaluated in rats and rabbits following oral administration of oxymetazoline hydrochloride during the period of organogenesis. Oxymetazoline hydrochloride did not cause adverse effects to the fetus at oral doses up to 0.2 mg/kg/day in pregnant rats during the period of organogenesis (3 times the MRHD on an AUC comparison basis). Oxymetazoline hydrochloride did not cause adverse effects to the fetus at oral doses up to 1 mg/kg/day in pregnant rabbits during the period of organogenesis (73 times the MRHD on an AUC comparison basis). Maternal toxicity, such as decreased maternal body weight, was produced at the high dose of 1 mg/kg/day in pregnant rabbits and was associated with findings of delayed skeletal ossification. In a rat perinatal and postnatal development study, oxymetazoline hydrochloride was orally administered to pregnant rats once daily from gestation day 6 through lactation day 20. Maternal toxicity was produced at the high dose of 0.2 mg/kg/day (3 times the MRHD on an AUC comparison basis) in pregnant rats and was associated with an increase in pup mortality and reduced pup body weights. Delayed sexual maturation was noted at 0.1 and 0.2 mg/kg/day (2 times the MRHD and 3 times the MRHD on an AUC comparison basis, respectively). Oxymetazoline hydrochloride did not have any adverse effects on fetal development at a dose of 0.05 mg/kg/day (one-half of the MRHD on an AUC comparison basis).1

Lactation

No clinical data are available to assess the effects of oxymetazoline on the quantity or rate of breastmilk production, or to establish the level of oxymetazoline present in human breastmilk post-dose. Oxymetazoline was detected in the milk of lactating rats. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for oxymetazoline hydrochloride topical cream and any potential adverse effects on the breast-fed child from oxymetazoline hydrochloride or from the underlying maternal condition. 1

Pediatric Use

Safety and effectiveness of oxymetazoline hydrochloride topical cream have not been established in pediatric patients below the age of 18 years. 1

Geriatric Use

One hundred and ninety-three subjects aged 65 years and older received treatment with oxymetazoline hydrochloride topical cream (n = 135) or vehicle (n = 58) in clinical trials. No overall differences in safety or effectiveness were observed between subjects ≥ 65 years of age and younger subjects, based on available data. Clinical studies of oxymetazoline hydrochloride topical cream did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. 1

Common Adverse Effects

Most common adverse reactions (incidence ≥ 1%) are application site dermatitis, worsening inflammatory lesions of rosacea, application site pruritus, application site erythema, and application site pain.1

Drug Interactions

Specific Drugs

It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:

Please see product labeling for drug interaction information.

Actions

Mechanism of Action

Oxymetazoline is an alpha1A adrenoceptor agonist. Oxymetazoline acts as a vasoconstrictor. 1

Advice to Patients

Patient Counseling Information

Advise the patient and/or caregiver to read the FDA-approved patient labeling. 1

Important Administration Instructions

Oxymetazoline hydrochloride cream is for topical use only. 1

Oxymetazoline hydrochloride cream pumps require priming before initial use and discard product from the first three pumps. 1

Do not to apply oxymetazoline hydrochloride topical cream to irritated skin or open wounds. 1

Avoid contact with the eyes and lips. 1

Wash hands immediately after application. 1

Keep oxymetazoline hydrochloride topical cream out of reach of children. 1

Additional Information

AHFS First Release. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.

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.

Oxymetazoline Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Cream

10 mg /1 g

Rhofade

Allergan

AHFS Drug Information. © Copyright 2017, Selected Revisions March 8, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Allergan. RHOFADE (Oxymetazoline Hydrochloride) TOPICAL prescribing information. 2017 Jan.

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