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brimonidine (Alphagan P)

 

Classes: Antiglaucoma, Alpha Agonists

Dosing and uses of Alphagan (brimonidine)

 

Adult dosage forms and strengths

ophthalmic solution

  • 0.1%
  • 0.15%
  • 0.2%

 

Open-Angle Glaucoma or Ocular Hypertension

1 gtt in affected eye(s) q8hr

 

Optic Neuropathy (Orphan)

Treatment of anterior ischemic optic neuropathy

Orphan indication sponsor

  • Allergan, Inc; 2525 Dupont Drive, P.O. Box 19534; Irvine, CA 92713

 

Pediatric dosage forms and strengths

ophthalmic solution

  • 0.1%
  • 0.15%
  • 0.2%

 

Open-Angle Glaucoma or Ocular Hypertension

<2 years

  • Contraindicated

>2 years

  • 1 gtt in affected eye(s) q8hr

 

Alphagan (brimonidine) adverse (side) effects

Frequency not defined

Oral dryness

Conjunctival hyperemia

Allergic conjunctivitis

Eye pruritus

Rash

Photophobia

Headache

Fatigue

Dizziness

Dyspepsia

Blepharitis

Eye discharge

 

Postmarketing Reports

Skin and subcutaneous disorders: Pallor

Immune system disorders: Angioedema, hypersensitivity, lip swelling, swollen tongue, throat tightness, urticaria

Cardiovascular disorders: bradycardia, hypotension (including orthostatic hypotension)

 

Warnings

Contraindications

Hypersensitivity to product or components

Children <2 years

Concurrent MAO inhibitors

 

Cautions

Wait 15 min before inserting soft contact lenses

Use caution in severe cardiovascular disease, cerebral insufficiency, depression, hepatic impairment, orthostatic hypotension, renal impairment, thromboangiitis obliterans

May cause CNS depression, which may impair mental abilities

Children are at higher risk of adverse effects

Bradycardia, hypotension (including orthostatic hypotension) and dizziness reported

Avoid applying topical gel to skin or open wounds

Some patients have experienced erythema involving areas of face that were previously not affected by erythema and in areas (e.g., neck and chest) outside of treatment sites

Some patients have experienced increased frequency of flushing and/or increased depth of erythema with flushing; some patients reported new onset of flushing

Some patients have experienced pallor or excessive whitening at or outside application site following therapy

Allergic contact dermatitis was reported for topical geL

Adverse events reported for topical gel include angioedema, throat tightening, tongue swelling, and urticarial; institute appropriate therapy and discontinue therapy, if clinically significant hypersensitivity reaction occurs

 

Pregnancy and lactation

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.

 

Pharmacology of Alphagan (brimonidine)

Mechanism of action

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

 

Pharmacokinetics

Onset of action: 2hr (peak effect)

Half-Life: 2 hr

Peak plasma time: 0.5-2.5 hr

Metabolism: Liver

Excretion: urine (74%)