alpha adrenergic agonists
Topical management of persistent (nontransient) facial erythema due to rosacea.
Acts as a selective alpha-2 adrenergic agonist, causes direct vasoconstriction.
Decreased erythema in rosacea.
Absorption: Some absorption follows topical use.
Metabolism and Excretion: Extensively metabolized by the liver; drug and metabolites are excreted in urine.
TIME/ACTION PROFILE (decreased erythema)
|top||within 3 hr||3–6 hr||at least 12 hr|
- Lactation: Discontinue breastfeeding or drug.
Use Cautiously in:
- Cerebral/coronary insufficiency;
- Reynaud's phenomenon;
- Severe/unstable/uncontrolled cardiovascular disease;
- Orthostatic hypotension;
- Thromboangiitis obliterans;
- Sjögren's syndrome;
- Vascular insufficiency (may potentiate)
- OB: Use only if potential benefit justifies potential fetal risk
- Pedi: Safe and effective use in children has not been established; inadvertent ingestion has caused serious adverse effects.
Adverse Reactions/Side Effects
CV: bradycardia, hypotension
Derm: flushing, contact dermatitis, erythema, pallor, skin burning sensation
Neuro: dizziness, headache
Misc: HYPERSENSITIVITY REACTIONS(including angioedema, anaphylaxis, and urticaria)
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- Due to possible ↓ in BP, use cautiously with antihypertensives, beta-adrenergic blockers, digoxin.
- May ↑ risk of sedation with alcohol, anti-anxiety agents, barbiturates and opioids sedative/hypnotics.
- Concurrent use with MAO inhibitors may ↑ risk of systemic side effects, including hypotension, undertake concurrent use with caution.
Topical (Adults >18 yr): Apply pea-sized amount to each of five areas on the face (forehead, chin, nose and each cheek) once daily.
Topical gel: 0.33%
- Assess face for erythema of rosacea periodically during therapy.
Apply a pea-size amount to central forehead, chin, nose, and each cheek. Spread smoothly and evenly as a thin layer across entire face, avoiding eyes and lips. Do not apply to irritated skin or open wounds. Wash hands after application.
- Not for oral, ophthalmic, or intravaginal use.
- Instruct patient in correct application of brimonidine. Caution patient not to use more gel than prescribed. Advise patient to read Patient Information Leaflet prior to therapy and with each Rx refill in case of changes.
- Inform patient that erythema or flushing may occur; usually diminishes 30 min to several hrs after application; resolves after discontinuation.
- Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
- Advise female patients to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Decreased facial erythema of rosacea.