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Brimonidine (Topical) (Monograph)

Brand name: Mirvaso
Drug class: Skin and Mucous Membrane Agents, Miscellaneous
Chemical name: 5-Bromo-6-(2-imidazolidinylideneamino) quinoxaline L-tartrate
Molecular formula: C11H10BrN5 • C4H6O6
CAS number: 70359-46-5


Relatively selective α2-adrenergic agonist.

Uses for Brimonidine (Topical)


Used topically for the treatment of persistent (nontransient) erythema associated with rosacea (acne rosacea).

Effective in treating erythema, unlike other currently available medications for rosacea (e.g., azelaic acid, doxycycline, metronidazole).

Does not affect the inflammatory lesions associated with rosacea.

Brimonidine (Topical) Dosage and Administration


Topical Administration

Apply topically as a 0.33% gel.

For external use only. Do not administer orally, vaginally, or topically to the eye.

Apply smoothly and evenly as a thin layer across the entire face. Avoid contact with the eyes and lips; wash hands after application.


Available as brimonidine tartrate; dosage of gel expressed in terms of brimonidine.



Apply a pea-sized amount to each of the 5 areas of the face (central forehead, chin, nose, and each cheek, for a total of 5 pea-sized amounts) once daily.

Cautions for Brimonidine (Topical)



Sensitivity Reactions

Allergic Contact Dermatitis

Allergic contact dermatitis reported in about 1% of individuals in clinical trials.

Two of these individuals underwent patch testing; one was sensitive to brimonidine, and the other was sensitive to phenoxyethanol (a preservative contained in brimonidine gel).

Potentiation of Vascular Insufficiency

Use with caution in patients with depression, cerebral or coronary insufficiency, Raynaud's phenomenon, orthostatic hypotension, thromboangiitis obliterans, scleroderma, or Sjögren's syndrome.

Severe Cardiovascular Disease

α2-Adrenergic agonists, such as brimonidine, can lower BP. Use with caution in patients with cardiovascular disease that is severe, unstable, or uncontrolled.

Serious Adverse Reactions Following Ingestion

Serious adverse reactions requiring hospitalization (e.g., lethargy, respiratory distress with apneic episodes requiring intubation, sinus bradycardia, confusion, psychomotor hyperactivity, diaphoresis) reported in at least 2 young children following accidental ingestion. Both were discharged without sequelae after one night of hospitalization.

Store out of reach of children.

Erythema and Flushing

May cause erythema and flushing, sometimes requiring discontinuance. Effects may begin to diminish several hours after application of the gel.

Severe, rebound erythema, sometimes accompanied by a severe burning sensation, has occurred 3–12 hours after application. In some cases, erythema returned 3–6 hours after application; in others, erythema returned as drug effects waned (10–12 hours after application) and was similar to baseline. However, returning erythema was worse in severity than at baseline in some patients.

Intermittent flushing also reported with onset ranging from about 30 minutes to 3–4 hours after application.

Erythema and flushing appear to resolve following discontinuance of the drug.

Specific Populations


Category B.


Distributed into milk in animals. Not known whether distributed into human milk. Discontinue nursing or the drug.

Pediatric Use

Safety and efficacy not established.

Accidental ingestion has caused serious adverse reactions in children; keep out of reach of children. (See Serious Adverse Reactions Following Ingestion under Cautions.)

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.

Common Adverse Effects

In short-term clinical trials, erythema, flushing, burning sensation of the skin.

In a 12-month open-label trial, flushing, erythema, worsening of rosacea, nasopharyngitis, burning sensation of the skin, increased intraocular pressure, headache.

Drug Interactions

Specific Drugs




Antihypertensive agents

Possible additive cardiovascular effects

Use with caution

β-Adrenergic blocking agents

Possible additive cardiovascular effects

Use with caution

Cardiac glycosides

Possible additive cardiovascular effects

Use with caution

CNS depressants (e.g., alcohol, general anesthetics, barbiturates, opiates, sedatives)

Possible additive CNS depressant effects

MAO inhibitors

Possible increased brimonidine exposure and increased adverse effects (e.g., hypotension)

Use with caution

Brimonidine (Topical) Pharmacokinetics



Following administration of brimonidine tartrate gel (1 g to the entire face) once daily for 29 days in patients with erythema associated with rosacea, peak plasma concentration and AUC were 40 and 20%, respectively, those observed following administration of brimonidine tartrate 0.2% ophthalmic solution (1 drop in each eye every 8 hours for 24 hours).

Mean peak plasma concentration and AUC were highest on day 15 in patients receiving brimonidine gel.

Slightly lower systemic exposure observed on day 29, indicating no further drug accumulation.


Maximal effects typically occur 3 hours after application.


Maximal effects typically continue until about 6 hours after application.

Total duration of effect >12 hours in majority of patients.



Distributed into milk in animals; not known whether distributed into human milk.



Extensively metabolized by the liver.

Elimination Route

Excreted principally in urine as brimonidine and metabolites.





20–25°C (may be exposed to 15–30°C).


Advice to Patients


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.

Brimonidine Tartrate


Dosage Forms


Brand Names




0.33% (of brimonidine)



AHFS DI Essentials™. © Copyright 2024, Selected Revisions December 10, 2015. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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