brimonidine topical

Action and Spectrum

Actions and Spectrum: 

Actions: 

brimonidine acts as an alpha-2 adrenergic agonist, which stimulates alpha-2 adrenergic receptors in the body. Activation of these receptors leads to various physiological effects. 

brimonidine causes vasoconstriction, which is the narrowing of blood vessels. Constricting blood vessels helps reduce blood flow and decrease redness and inflammation. 

Spectrum: 

brimonidine gel has been specifically approved for treating facial redness associated with rosacea. Rosacea manifests as persistent facial redness, flushing, and visible blood vessels. brimonidine acts as a vasoconstrictor, reducing the dilation of blood vessels in the skin and improving the appearance of facial redness. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Flushing (10%) 

Erythema (8%) 

Increased intraocular pressure (4%) 

Headache (4%) 

Nasopharyngitis (5%) 

Skin-burning sensation (4%) 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

• Hypersensitivity 
• Cardiovascular disease 
• Hepatic impairment 
• Renal impairment 
• Concurrent use of MAO inhibitors 
• Ophthalmic condition 

Pregnancy / Lactation

Pregnancy consideration:  

Category C 

Breastfeeding warnings:  

No data is available regarding the excretion of the drug in breast milk.  

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

brimonidine is an alpha-2 adrenergic receptor agonist. It selectively activates alpha-2 adrenergic receptors, leading to various pharmacological effects. brimonidine causes vasoconstriction, which is the narrowing of blood vessels. Activation of alpha-2 adrenergic receptors on vascular smooth muscle cells leads to the constriction of blood vessels. This results in the reduction of blood flow. This vasoconstrictive effect helps reduce redness and inflammation.  

Pharmacodynamics: 

brimonidine acts on alpha-2 adrenergic receptors in the central nervous system, reducing sympathetic outflow. This modulation of the sympathetic nervous system contributes to the overall effects of brimonidine, including vasoconstriction and reduction of intraocular pressure. 

brimonidine topical gel has been used off-label to treat facial redness associated with rosacea. The vasoconstrictive effect of brimonidine helps reduce the dilation of blood vessels in the skin, reducing facial redness. 

Pharmacokinetics: 

Absorption 

when applied topically, brimonidine can be absorbed through the skin or ocular tissues. The extent of absorption depends on factors such as the formulation, concentration, and application site. Topical brimonidine eye drops are primarily absorbed through the cornea, while topical gel formulations are absorbed through the skin. 

Distribution 

After absorption, brimonidine is distributed within the body. The exact distribution pattern and extent of distribution need to be better characterized for topical formulations. However, systemic exposure to brimonidine is generally low with topical use, and significant systemic levels are not typically observed. 

Metabolism 

brimonidine undergoes hepatic metabolism via oxidation and conjugation processes. The specific enzymes involved in its metabolism have yet to be extensively studied. However, it is known that multiple pathways, including the cytochrome P450 system, metabolize brimonidine. 

Elimination and Excretion 

The primary route of eliminating brimonidine and its metabolites is renal excretion. The elimination half-life of brimonidine after topical application is relatively short. The exact elimination characteristics of topical brimonidine formulations have yet to be extensively studied. 

Adminstartion

Administration: 

Before application, clean & dry the affected area. Apply a bit of the cream or ointment as a fine layer to the affected area. Gently rub or spread the medication over the bruise. 

Wash your hands after the application of the medication. Follow the product labeling for specific instructions or as directed by your healthcare professional regarding the frequency of application and duration of use. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: brimonidine  

Pronounced: bri-MON-i-deen-TOP-i-kal 

Why do we use brimonidine? 

brimonidine gel has been approved for treating facial redness associated with rosacea. brimonidine acts by constricting the blood vessels in the skin, reducing facial redness, and improving the appearance of rosacea.