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Brimonidine Tartrate topical

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
Brands: Mirvaso

Introduction

Relatively selective α2-adrenergic agonist.1 2 5 6

Uses for Brimonidine Tartrate

Rosacea

Used topically for the treatment of persistent (nontransient) erythema associated with rosacea (acne rosacea).1 4

Effective in treating erythema, unlike other currently available medications for rosacea (e.g., azelaic acid, doxycycline, metronidazole).2 4 5 6

Does not affect the inflammatory lesions associated with rosacea.1 4

Brimonidine Tartrate Dosage and Administration

Administration

Topical Administration

Apply topically as a 0.33% gel.1

For external use only.1 Do not administer orally, vaginally, or topically to the eye.1

Apply smoothly and evenly as a thin layer across the entire face.1 Avoid contact with the eyes and lips; wash hands after application.1

Dosage

Available as brimonidine tartrate; dosage of gel expressed in terms of brimonidine.1

Adults

Rosacea
Topical

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.1

Cautions for Brimonidine Tartrate

Contraindications

  • No known contraindications.1

Warnings/Precautions

Sensitivity Reactions

Allergic Contact Dermatitis

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

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).1

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.1

Severe Cardiovascular Disease

α2-Adrenergic agonists, such as brimonidine, can lower BP.1 Use with caution in patients with cardiovascular disease that is severe, unstable, or uncontrolled.1

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.1 Both were discharged without sequelae after one night of hospitalization.1

Store out of reach of children.1

Erythema and Flushing

May cause erythema and flushing, sometimes requiring discontinuance.1 8 10 Effects may begin to diminish several hours after application of the gel.1 10

Severe, rebound erythema, sometimes accompanied by a severe burning sensation, has occurred 3–12 hours after application.8 9 10 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.8 9 However, returning erythema was worse in severity than at baseline in some patients.1 8 9 10

Intermittent flushing also reported with onset ranging from about 30 minutes to 3–4 hours after application.1

Erythema and flushing appear to resolve following discontinuance of the drug.1 9 10

Specific Populations

Pregnancy

Category B.1

Lactation

Distributed into milk in animals.1 Not known whether distributed into human milk.1 Discontinue nursing or the drug.1

Pediatric Use

Safety and efficacy not established.1

Accidental ingestion has caused serious adverse reactions in children; keep out of reach of children.1 (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.1

Common Adverse Effects

In short-term clinical trials, erythema,1 2 flushing,1 2 burning sensation of the skin.1

In a 12-month open-label trial, flushing,1 3 erythema,1 3 worsening of rosacea,1 3 nasopharyngitis,1 burning sensation of the skin,1 3 increased intraocular pressure,1 headache.1

Interactions for Brimonidine Tartrate

Specific Drugs

Drug

Interaction

Comments

Antihypertensive agents

Possible additive cardiovascular effects1

Use with caution1

β-Adrenergic blocking agents

Possible additive cardiovascular effects1

Use with caution1

Cardiac glycosides

Possible additive cardiovascular effects1

Use with caution1

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

Possible additive CNS depressant effects1

MAO inhibitors

Possible increased brimonidine exposure and increased adverse effects (e.g., hypotension)1

Use with caution1

Brimonidine Tartrate Pharmacokinetics

Absorption

Bioavailability

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).1 7

Mean peak plasma concentration and AUC were highest on day 15 in patients receiving brimonidine gel.1 7

Slightly lower systemic exposure observed on day 29, indicating no further drug accumulation.1 7

Onset

Maximal effects typically occur 3 hours after application.2

Duration

Maximal effects typically continue until about 6 hours after application.2

Total duration of effect >12 hours in majority of patients.2

Distribution

Extent

Distributed into milk in animals; not known whether distributed into human milk.1

Elimination

Metabolism

Extensively metabolized by the liver.1

Elimination Route

Excreted principally in urine as brimonidine and metabolites.1

Stability

Storage

Topical

Gel

20–25°C (may be exposed to 15–30°C).1

Actions

  • Relatively selective α2-adrenergic agonist.1 2 5 6

  • Topical application appears to reduce erythema through direct vasoconstriction.1 2 5 6

  • May act by targeting α-adrenergic receptors present in the smooth muscle sheath encasing the vessel wall of superficial cutaneous blood vessels.5

Advice to Patients

  • Patients should be given a copy of the patient information provided by the manufacturer.1

  • Importance of advising patients that brimonidine gel should only be used as directed by a clinician.1

  • Importance of advising patients that brimonidine gel is for external use only and that contact with the eyes and lips should be avoided; importance of not using the drug orally or intravaginally.1

  • Importance of advising patients not to apply to irritated skin or open wounds.1

  • Importance of washing hands immediately after applying brimonidine gel.1

  • Importance of advising patients of the possibility of erythema or flushing.1

  • Importance of advising patients to report adverse reactions to a clinician.1

  • Importance of advising patients to keep brimonidine gel out of the reach of children.1 (See Serious Adverse Reactions Following Ingestion under Cautions.)

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)

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.

Brimonidine Tartrate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Gel

0.33% (of brimonidine)

Mirvaso

Galderma

AHFS DI Essentials. © Copyright 2016, Selected Revisions December 10, 2015. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Galderma. Mirvaso (brimonidine) topical gel prescribing information. Fort Worth, TX; 2013 Aug.

2. Fowler J, Jackson M, Moore A et al. Efficacy and safety of once-daily topical brimonidine tartrate gel 0.5% for the treatment of moderate to severe facial erythema of rosacea: results of two randomized, double-blind, and vehicle-controlled pivotal studies. J Drugs Dermatol. 2013; 12:650-6. [PubMed 23839181]

3. Moore A, Kempers S, Murakawa G et al. Long-term safety and efficacy of once-daily topical brimonidine tartrate gel 0.5% for the treatment of moderate to severe facial erythema of rosacea: results of a 1-year open-label study. J Drugs Dermatol. 2014; 13:56-61. [PubMed 24385120]

4. Anon. Brimonidine gel (Mirvaso) for rosacea. Med Lett Drugs Ther. 2013; 55:82-3. [PubMed 24129112]

5. Del Rosso JQ. Management of facial erythema of rosacea: what is the role of topical α-adrenergic receptor agonist therapy?. J Am Acad Dermatol. 2013; 69(6 Suppl 1):S44-56. [PubMed 24229637]

6. Del Rosso JQ. Advances in understanding and managing rosacea: part 2: the central role, evaluation, and medical management of diffuse and persistent facial erythema of rosacea. J Clin Aesthet Dermatol. 2012; 5:26-36. [PubMed 22468177]

7. Benkali K, Leoni M, Rony F et al. Comparative pharmacokinetics and bioavailability of brimonidine following ocular and dermal administration of brimonidine tartrate ophthalmic solution and gel in patients with moderate-to-severe facial erythema associated with rosacea. Br J Dermatol. 2014; 171:162-9. [PubMed 24506775]

8. Routt ET, Levitt JO. Rebound erythema and burning sensation from a new topical brimonidine tartrate gel 0.33%. J Am Acad Dermatol. 2014; 70:e37-8. [PubMed 24438976]

9. Werner K, Kobayashi TT. Dermatitis medicamentosa: severe rebound erythema secondary to topical brimonidine in rosacea. Dermatol Online J. 2015; 21:. [PubMed 25780983]

10. Tanghetti EA, Jackson JM, Belasco KT et al. Optimizing the use of topical brimonidine in rosacea management: panel recommendations. J Drugs Dermatol. 2015; 14:33-40. [PubMed 25607906]

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