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41 Cards in this Set

  • Front
  • Back
Alpha 2 Agonists
Brimonidine
Aproclonidine (aka Iopidine)
Aproclonidine (Iopidine) profile
-hardly used for POAG bc of allergy

-Tachyphylaxis (rapid development of tolerance)
Aproclonidine MoA
- decrease AH production at the ciliary body

- late increase in uveoscleral outflow
Aproclonidine ocular SE
- conjunctival blanching
- lid retraction
- mydriasis
Aproclonidine systemic SE
- dry mouth and nose
- taste abnormality
Aproclonidine Contraindications
- Cardiovascular disease
- MAOIs
- NSAIDs
Aproclonidine use other than for APOAG
- used after surgery to control IOP spikes
Brimonidine (Alphagan) Characteristics
- more selective
- more lipid soluble
- penetrates the CNS better
- high melanin binding
- neuroprotective (?)
Brimonidine MoA
- same as aproclonidine

- decrease AH production at the ciliary body

- late increase in uveoscleral outflow
Brimonidine ocular SE
- conj blanching
- eyelid retraction
- miosis
Brimonidine systemic SE
- Dry mouth / nose
- dermatitis
Beta blockers include:
- timolol
- betaxolol
- levobunolol
- metipranolol
- carteolol
Timolol characteristics
- non selective B antagonist
- MSA ?
- No hypotensive effect @ night
- Long acting
- well tolerated
- contralateral effect
Timolol MoA
- decrease AH production by blocking beta adrenergic sites
Timolol ocular SE
- stinging
- punctate keratitis (maybe from preservatives?)
- decreased corneal sensitivity
- dry eyes
- decrease ONH perfusion
Timolol systemic SE
- respiratory distress
- asthma
- cardiovascular
- masked hypoglycemia
- altered plasma lipids (decrease in HDL)
Timolol Contraindications
- bronchial asthma
- labile diabetes
- thyroid disease
- cardiovascular disease?
Timolol Drug Interactions
- Systemic beta blockers
- Ca2+ channel blockers
- beta agonists
- NSAIDs
Betaxolol Ocular SE
- stinging
- punctate keratitis (maybe from preservatives?)
- decreased corneal sensitivity
- dry eyes
- decrease ONH perfusion
Levobunolol Ocular SE
- stinging
- punctate keratitis (maybe from preservatives?)
- decreased corneal sensitivity
- dry eyes
- decrease ONH perfusion
Metipranolol Ocular SE
- stinging
- punctate keratitis (maybe from preservatives?)
- decreased corneal sensitivity
- dry eyes
- decrease ONH perfusion
Betaxolol Characteristics
- selective beta 1 antagonist (cardioselective)
- MSA ?
- Inactive metabolite (only one of bb)
- neuroprotective
- better for pts with asthma
Betaxolol MoA
- decrease AH production by blocking beta adrenergic sites
Betaxolol Systemic SE
- respiratory distress
- asthma
- cardiovascular
- masked hypoglycemia
- altered plasma lipids (decrease in HLD)
Betaxolol Contraindications
- bronchial asthma
- labile diabetics
- thyroid disease
- cardiovascular disease ?
Betaxolol drug interactions
- systemic beta blockers
- Ca2+ channel blockers
- heart meds
- beta agonists
- NSAIDs
Levobunolol Ocular SE
- stinging
- punctate keratitis (maybe from preservatives?)
- decreased corneal sensitivity
- dry eyes
- decrease ONH perfusion
Levobunolol Systemic SE
- respiratory distress
- asthma
- cardiovascular
- masked hypoglycemia
- altered plasma lipids (decrease in HDL)
Levobunolol Drug Interactions
same as timolol, metipranolol, and betaxolol
Metipranolol characteristics
- non-selective B antagonist
- active metabolite
- long acting
Levobunolol characteristics
- non selective bb
- active metabolite
- MSA ?
- long acting
carteolol characteristics
- non selective bb
- active metabolite
- ISA
- MSA ?
Carbonic Anhydrase Inhibitors (CAIs) include
- acetazolamide
- methazolamide
- dichlorphenamide
- dorzolamide
- brinzolamide
Acetazolamide Characteristics
- Potent inhibitor CAII
- Not metabolized
- Highly protein bound
- Alkalizes urine
- hypotensive effect parallels plasma levels
- hastens excretion of acidic drugs (increases its own secretion)
- effective day and night
All CAIs MoA
↓ Aqeous inflow (↓ edema) by inhibiting carbonic anhydrase (conversion of CO2 + H2O → H2CO3)
All CAIs ocular SE
- High intolerance (30-80%)
- Numbness, tingling
- Metallic taste (also with topical CAIs)
- Symptom complex
- Transient myopia
- Side effects are rare with topical CAIs but could include corneal edema
All CAIs contraindications
- Allergies to sulfonamides
-Renal, liver disease
- COPDs (asthma)
- Hemoglobinopathies + hyphema
- Pregnancy
All CAIs drug interactions
- K+ depleting diuretics
- Digitalis
- Amphetamines
- TCAs
- quinidine
- Aspirin
Acetazolamide Special uses
- IV acetazolamide in AACG in combo with timolol
- macular edema with RPE dysfunction (chronic uveitis, CME)
Methazolamide Characteristics
- more potent
- Higher lipid solubility
- Mostly inactivated by metabolism
- Less binding to plasma protein
- Less effect on acid-base balance
- longer action due to reabsorption
- one of the best tolerated
- preferred for those with COPD and predisposition to renal calculi (kidney stones)
Dorzolamide & Brinzolamide characteristics
- Very potent inhibitor CA II
- Enhanced corneal/scleral penetration