Contents

Search

brimonidine (Alphagan)

Tradename: Alphagan. Indications: - open-angle glaucoma, increased intraocular pressure - rosacea [4] Contraindications: patients receiving MAO inhibitors Caution: 1) patients with cardiovascular disease 2) depression 3) cerebrovascular disease 4) coronary artery disease 5) Raynaud's phenomenon 6) orthostatic hypotension 7) thromboangiitis obliterans 8) hepatic impairment 9) renal insufficiency Dosage: 1) 1 drop OU TID 2) allow at least 15 minutes after instilling brimonidine before placing soft contact lenses; benzalkonium chloride, a preservative may be absorbed by soft contact lenses 0.1%, 0.15%, 0.2% 5 mL, 10 mL, 15 mL Pharmacokinetics: 1) onset of action: 1-4 hours 2) duration of action: 12 hours 3) loss of effect may occur; routine monitoring of intraocular pressure required 4) peak serum levels 1-4 hours after ocular administration, with elimination 1/2life of 3 hours 5) metabolized in liver; metabolites excreted in the urine Adverse effects: 1) common (> 10%) - headache, fatigue*, drowsiness*, xerostomia, orthostatic hypotension*, ocular hyperemia, burning & stinging, blurring, foreign body sensation, conjunctival follicles, ocular allergic reactions, ocular pruritus 2) less common (1-10%) - dizziness, corneal staining, corneal erosion, photophobia, eyelid erythema, ocular pain, ocular dryness, ocular irritation, conjunctival edema, conjunctival blanching, conjunctival hemorrhage, conjunctival discharge, tearing, blepharitis, eyelid edema, abnormal vision, lid crusting, dysgeusia, upper respiratory tract symptoms, ocular dryness, dizziness, gastrointestinal symptoms, asthenia, muscular pain, insomnia, depression, hypertension, anxiety , palpitations. arrhythmias, nasal dryness, syncope 3) uncommon (< 1%) 1) allergic response 2) central nervous system (CNS) effect * closely monitor patients with fatigue or drowsiness * according to ref [5] timolol causes more orthostatic hypotension than brimonidine Drug interactions: 1) avoid use with monoamine oxidase (MAO) inhibitors 2) use caution with: a) CNS depressants b) beta-adrenergic receptor antagonists (beta blockers) 1] ocular 2] systemic c) antihypertensive agents d) digitalis e) tricyclic antidepressants (TCA) Mechanism of action: - alpha-2 adrenergic receptor agonist

Interactions

drug adverse effects (more general classes)

General

alpha-2 adrenergic receptor agonist

Properties

AGONIST-FOR: alpha-2 adrenergic receptor MISC-INFO: pregnancy-category B safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. PDR 56th ed 2002
  4. Deprecated Reference
  5. NEJM Knowledge+ Ophthalmology
  6. Department of Veterans Affairs, VA National Formulary

Component-of

brimonidine/brinzolamide (Simbrinza) brimonidine/timolol