Brimonidine

Products

Brimonidine is commercially available in the form of eye drops (Alphagan, generic). It is also available in combination with timolol (Combigan, generic) and has been approved in many countries since 1998. The active ingredient is also used for the external treatment of rosacea, see under the article Brimonidine gel. Finally, brimonidine is also combined fixed with brinzolamide, see under brinzolamide brimonidine (Simbrinza).

Structure and properties

Brimonidine (C11H10BrN5, Mr = 292.1 g/mol) is present in drugs as brimonidine tartrate, a white to yellow powder that is soluble in water. It has a similar structure to clonidine and apraclonidine.

Effects

Brimonidine (ATC S01EA05) is a selective α2-adrenoceptor agonist. It is sympathomimetic and lowers intraocular pressure.

Indications

For the treatment of elevated intraocular pressure.

Dosage

According to the drug label. The usual dose is 1 drop per affected eye twice daily at approximately 12-hour intervals. See also under Administering eye drops. It is recommended that fingertip pressure be applied to the corner of the eye for 1 minute to decrease systemic absorption and the risk for adverse effects.

Contraindications

  • Hypersensitivity
  • Children under 2 years
  • Treatment with MAO inhibitors and drugs that affect noradrenergic neurotransmission.

For complete precautions, see the drug label.

Interactions

Central depressant medications and alcohol may potentially increase adverse effects.

Adverse effects

Despite local application to the eye, systemic adverse effects affecting the whole organism are also possible. The most common adverse effects include local irritation of the eye, headache, dry mouth, drowsiness, dry mouth, and fatigue. Dizziness, taste disturbances, respiratory and and digestive problems are also common. Other possible side effects include: Depression, dry nose, palpable heartbeats, arrhythmias, hypersensitivity reactions, high or low blood pressure, and sleep disturbances.