brimonidine/brinzolamide (Simbrinza)

Introduction

brimonidine 0.2%, brinzolamide 1%

Indications

• open-angle glaucoma

Contraindications

• sulfonamide hypersensitivity
• severe renal impairment
• severe cardiovascular disease
• severe liver failure
• angle-closure glaucoma

Dosage

• 1 drop in each eye BID-TID

Ophthalmic: 8 mL

* shake well before using

Store at 2-25 C (36-77 F)

Adverse effects

• >10% (brimonidine)
  • xerostomia
  • ocular hyperemia
  • burning & stinging
  • headache
  • blurring
  • foreign body sensation
  • fatigue/drowsiness
  • conjunctival follicles
  • ocular allergic reactions
  • ocular pruritus (10-30%)
• 1-10% (brimonidine)
  • corneal staining/erosion
  • photophobia
  • eyelid erythema
  • ocular ache/pain
  • ocular dryness
  • tearing
  • upper respiratory symptoms
  • eyelid edema
  • conjunctival edema]
  • dizziness
  • blepharitis
  • ocular irritation
  • gastrointestinal symptoms
  • asthenia
  • conjunctival blanching
  • abnormal vision
  • muscular pain
  • lid crusting
  • conjunctival hemorrhage
  • dysgeusia
  • insomnia (<3%)
  • conjunctival discharge
  • depression
  • hypertension
  • anxiety
  • palpitations/arrhythmias
  • nasal dryness
  • syncope
• 1-10% (brinzolamide)
  • blurred vision
  • dysgeusia
  • blepharitis
  • dermatitis
  • xerophthalmia
  • foreign body sensation eye
  • headache
  • hperemia
  • ocular discharge
  • ocular discomfort
  • ocular keratitis
  • ocular pain
  • ocular pruritus
  • rhinitis
• <1% (brinzolamide)
  • allergic reactions
  • alopecia
  • chest pain
  • conjunctivitis
  • diarrhea
  • diplopia
  • dizziness
  • xerostomia
  • dyspnea
  • dyspepsia
  • eye fatigue
  • hypertonia
  • keratoconjunctivitis
  • keratopathy
  • kidney pain
  • eyelid margin crusting or sticky sensation
  • nausea
  • pharyngitis
  • tearing
  • urticaria
• not common (3-5%)*
  • blurred vision
  • eye irritation
  • dysgeusia
  • xerostomia
  • eye allergy
• uncommon
  • brimonidine may reduce blood pressure
  • corneal edema in susceptible patients (carbonic anhydrase)

* treatment discontinuation due to adverse reactions 11%

Drug interactions

• MAO inhibitors
  • may inhibit metabolism of brimonidine
• oral carbonic anhydrase inhibitors
• CNS depressants
  • Simbrinza may potentiate effects of CNS depressants
• antihypertensive agents
  • brimonidine may reduce blood pressure
• cardiac glycosides
• tricyclic antidepressants
  • unknown whether may blunt centrally-acting brimonidine
• high-dose salicylates
  • electrolyte imbalances have occurred in combination of oral carbonic anhydrase inhibitors

Mechanism of action

• combination carbonic anhydrase inhibitor & alpha-2 adrenergic agonist
• both agents reduce aqueous humor production

More general terms

• pharmacologic combination

Components

• brimonidine (Alphagan)
• brinzolamide (Azopt)