brimonidine (Rx, OTC)

Frequency Not Defined

Oral dryness

Conjunctival hyperemia

Allergic conjunctivitis

Eye pruritus

Rash

Photophobia

Headache

Fatigue

Dizziness

Dyspepsia

Blepharitis

Eye discharge

Contraindications

Hypersensitivity to product or components

Children <2 years (0.1-0.15% ophthalmic solution)

Cautions

Remove contact lenses before instilling eye drops; wait 15 min before reinserting contact lenses

If >1 ophthalmic product is being administered, wait 5 minutes between instilling eye drops

May potentiate syndromes associated with vascular insufficiency; caution with depression, cerebral or coronary insufficiency, Raynaud phenomenon, orthostatic hypotension, or thromboangiitis obliterans

Although brimonidine ophthalmic had minimal effect on the blood pressure of patients in clinical studies, caution with severe cardiovascular disease

Bacterial keratitis associated with the use of multiple-dose containers of topical ophthalmic products; instruct patients on how to avoid contamination

Drug interaction overview

• Because brimonidine ophthalmic may reduce blood pressure, caution in using drugs such as antihypertensives and/or cardiac glycosides with advised
• Although specific drug interaction studies have not been conducted with brimonidine ophthalmic, the possibility of an additive or potentiating effect with CNS depressants (alcohol, barbiturates, opiates, sedatives, or anesthetics) should be considered
• Tricyclic antidepressants (TCAs) have been reported to blunt the hypotensive effect of systemic clonidine; unknown whether the concurrent use TCAs with brimonidine ophthalmic can interfere with IOP lowering effect
• MAOIs may theoretically interfere with the metabolism of brimonidine and potentially result in increased systemic effects (eg, hypotension); advise caution to patients taking MAO inhibitors

Pregnancy Category: B

Lactation: It is not known whether this drug is excreted in milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Open-Angle Glaucoma or Ocular Hypertension

• Alpha-2 adrenergic receptor agonist; decreases aqueous humor secretion, increases uveoscleral outflow

Ocular Redness

• Dilutes alpha-2 receptor agonist; rapidly eliminates redness along the bulbar conjunctival microvasculature

Pharmacokinetics

Onset of action: 2hr (peak effect)

Half-Life: 2 hr

Peak plasma time: 0.5-2.5 hr

Metabolism: Liver

Excretion: urine (74%)