Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Gel, External:
Mirvaso: 0.33% (30 g) [contains methylparaben, propylene glycol]
Pharmacology
Mechanism of Action
Relatively selective alpha2-receptor agonist that when applied topically may decrease erythema through direct vasoconstriction.
Pharmacokinetics/Pharmacodynamics
Metabolism
Hepatic
Excretion
Urine
Time to Peak
Maximum plasma concentrations observed after 15 days
Use: Labeled Indications
Rosacea: Topical treatment of persistent (nontransient) erythema of rosacea in adults 18 years and older.
Contraindications
Hypersensitivity to brimonidine or any component of the formulation.
Canadian labeling: Additional contraindications (not in the US labeling): Neonates and infants (<2 years)
Dosage and Administration
Dosing: Adult
Rosacea: Topical: Apply a pea-size amount once daily as a thin layer across the entire face covering the central forehead, each cheek, nose, and chin.
Dosing: Geriatric
Refer to adult dosing.
Administration
Topical: Apply smoothly and evenly as a thin layer across the entire face (central forehead, each cheek, nose, and chin) avoiding the eyes and lips. Wash hands immediately after applying. Do not apply to open wounds or irritated skin.
Storage
Store at 20°C to 25°C (68°F to 77°F), excursions permitted between 15°C and 30°C (59°F and 86°F).
Drug Interactions
Blood Pressure Lowering Agents: Brimonidine (Topical) may enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
CNS Depressants: Brimonidine (Topical) may enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Digoxin: Brimonidine (Topical) may enhance the bradycardic effect of Digoxin. Monitor therapy
Monoamine Oxidase Inhibitors: May enhance the adverse/toxic effect of Brimonidine (Topical). Monoamine Oxidase Inhibitors may increase the serum concentration of Brimonidine (Topical). Monitor therapy
Adverse Reactions
1% to 10%:
Cardiovascular: Flushing (3%)
Central nervous system: Burning sensation of skin (2%), localized warm feeling (1%), paresthesia (1%)
Dermatologic: Erythema (4%), acne vulgaris (1%), allergic contact dermatitis (1%; due to active ingredient [1 case] or preservative [1 case]), contact dermatitis (1%), dermatitis (1%), skin pain (1%)
Ophthalmic: Blurred vision (1%)
Respiratory: Nasal congestion (1%)
<1%, postmarketing, and/or case reports: Angioedema, bradycardia, dizziness, facial erythema, hypersensitivity reaction, hypotension (including orthostatic), pallor, pharyngeal edema, swelling of lips, swollen tongue, urticaria
Warnings/Precautions
Concerns related to adverse effects:
- Erythema: Effects of brimonidine gel may begin to diminish within hours of application; recurrent and sometimes worsening erythema (compared to baseline) has been observed at or outside of the treatment areas. Symptoms appear to resolve following discontinuation of therapy.
- Flushing: Intermittent flushing (increased frequency or new onset) occurring ~30 minutes to several hours after application has been observed; symptoms appear to resolve following discontinuation of therapy.
- Hypersensitivity: Allergic contact dermatitis has been reported; angioedema, throat tightening, tongue swelling, and urticaria may also occur. Discontinue use if significant hypersensitivity reactions occur.
- Pallor: Pallor or excessive whitening has been observed at or outside of the treatment areas.
- Systemic effects: Bradycardia, hypotension (including orthostatic hypotension), and dizziness have been reported; may require hospitalization. Systemic effects may be due to use in unapproved dosing and indications (eg, use after laser procedures).
Disease-related concerns:
- Cardiovascular disease: May lower blood pressure; use with caution in patients with orthostatic hypotension or with severe, unstable, or uncontrolled cardiovascular disease. May potentiate vascular insufficiency; use with caution in patients with cerebral or coronary insufficiency, scleroderma, thromboangiitis obliterans, and Raynaud phenomenon.
- Depression: Use with caution in patients with depression.
- Sjögren syndrome: Use with caution in patients with Sjögren syndrome.
Other warnings/precautions:
- Accidental ingestion: Serious adverse events (eg, respiratory distress with apneic episodes requiring intubation, sinus bradycardia, diaphoresis, lethargy, confusion and psychomotor hyperactivity) were reported in 2 children following accidental ingestion of brimonidine gel. Advise patients to store gel out of the reach of children.
- Appropriate use: For external use only; not for oral, ophthalmic, or intravaginal use; avoid contact with eyes and lips. Do not apply to open wounds or irritated skin.
Pregnancy
Pregnancy Risk Factor
B
Pregnancy Considerations
Adverse events were not observed in animal reproduction studies.
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience flushing, redness, pale skin, or burning. Have patient report immediately to prescriber severe skin irritation, dizziness, passing out, or slow heartbeat (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
