Medical Treatment of Glaucoma Fritz Allen ,MD Visionary Ophthalmology September 7 th 2014 Medical Management of Glaucoma Beta-adrenergic Antagonists (Beta Blockers) Parasympathomimetic Agents Carbonic Anhydrase Inhibitors (CAI) Adrenergic Agonists Prostaglandin Analogues Combined Medications Hyperosmotic Agents A 64-year-old male with POAG is taking timolol, dorzolamide, brimonidine, and latanoprost OU. He must begin phenelzine, a systemic monoamine oxidase (MAO) inhibitor. Which one of the following should
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Medical Treatment of
Glaucoma Fritz Allen ,MD
Visionary Ophthalmology
September 7th 2014
Medical Management of
Glaucoma Beta-adrenergic Antagonists (Beta
Blockers)
Parasympathomimetic Agents
Carbonic Anhydrase Inhibitors (CAI)
Adrenergic Agonists
Prostaglandin Analogues
Combined Medications
Hyperosmotic Agents
A 64-year-old male with POAG is taking
timolol, dorzolamide, brimonidine, and
latanoprost OU. He must begin phenelzine, a
systemic monoamine oxidase (MAO)
inhibitor. Which one of the following should
be discontinued?
• Latanoprost
• Brimonidine
• Dorzolamide
• Timolol
Which of the following glaucoma
medications is contraindicated for use in
children younger than age 2?
• Timolol
• Levobunolol
• Brimonidine
• Dorzolamide
Adrenergic Agonists Indications
Non-selective agonists (epinephrine,
dipivefrin)
Selective adrenergic agonists
(apraclonidine, brimonidine) IOP lowering
OAG / ocular hypertension
Prophylaxis against post-op pressure
spikes
Prior to and immediately after
laser treatment (laser
trabeculoplasty, laser PI, Nd:YAG
capsulotomy)
Cataract surgery
Acute ACG Miosis after refractive surgery (off-label
use)
Adrenergic Agonists Contraindications and precautions
Non-selective Narrow AC angles- may precipitate
pupillary block
Blepharoptosis surgery- stimulates
Müller’s muscle, inadequate correction
Retrobulbar anesthesia
Local – risk of vasospasm &
occlusion of ophthalmic or central
retinal artery
Systemic – tachyarrhythmias, death Aphakia- CME risk (13-30%)
Adrenergic Agonists Selective
Proven sensitivity to these agents
Concomitant use of monoamine oxidase
inhibitors (MAOI)
Infants and children < 2 years: brimonidine
is an absolute contraindication due to apnea,
bradycardia, dyspnea
Pediatric (ages 2-7) usage reports:
convulsions, cyanosis, hypoventilation,
lethargy; brimonidine is relatively
contraindicated
Precaution in patients with severe
cardiovascular disease
Precaution in patients with depression,
cerebral or coronary insufficiency,
Raynaud’s phenomenon, orthostatic
hypotension
Pregnancy: category B drug- use only if
potential benefits justify potential risk
Adrenergic Agonists Method of action
Non-selective-mixed α and ß adrenergic
agonist; effect varies over time, initially
raising IOP slightly, followed by reduction
lasting 12-24 hours
Selective-alpha adrenergic receptor agonist;
reduction of aqueous humor production is
primary mechanism of action Fluorophotometric studies suggest that
Brimonidine tartrate also increases
uveoscleral outflow
Controversial neuroprotective effect:
prevent demise of retinal ganglion cells due
to trauma or toxins
Adrenergic Agonists Complications of therapy
Non-selective Local - conj injection, follicular
conjunctivitis, burning, stinging, mydriasis,
blurry vision, headache
Cardiovascular - tachycardia, arrhythmias,
hypertension
Selective Local - hyperemia, follicular conjunctivitis,
conjunctival blanching
Systemic - dry mouth, fatigue, anxiety,
respiratory depression in neonates
Adrenergic Agonists Contraindications and precautions
Non-selective Narrow AC angles- may precipitate
pupillary block
Blepharoptosis surgery- stimulates
Müller’s muscle, inadequate correction
Retrobulbar anesthesia
Local – risk of vasospasm &
occlusion of ophthalmic or central
retinal artery
Systemic – tachyarrhythmias, death Aphakia- CME risk (13-30%)
Adrenergic Agonists Selective
Proven sensitivity to these agents
Concomitant use of monoamine oxidase
inhibitors (MAOI)
Infants and children < 2 years: brimonidine
is an absolute contraindication due to apnea,
bradycardia, dyspnea
Pediatric (ages 2-7) usage reports:
convulsions, cyanosis, hypoventilation,
lethargy; brimonidine is relatively
contraindicated
Precaution in patients with severe
cardiovascular disease
Precaution in patients with depression,
cerebral or coronary insufficiency,
Raynaud’s phenomenon, orthostatic
hypotension
Pregnancy: category B drug- use only if
potential benefits justify potential risk
Adrenergic Agonists Method of action
Non-selective-mixed α and ß adrenergic
agonist; effect varies over time, initially
raising IOP slightly, followed by reduction
lasting 12-24 hours
Selective-alpha adrenergic receptor agonist;
reduction of aqueous humor production is
primary mechanism of action Fluorophotometric studies suggest that
Brimonidine tartrate also increases
uveoscleral outflow
Controversial neuroprotective effect:
prevent demise of retinal ganglion cells due
to trauma or toxins
Adrenergic Agonists Complications of therapy
Non-selective Local - conj injection, follicular
conjunctivitis, burning, stinging, mydriasis,
blurry vision, headache
Cardiovascular - tachycardia, arrhythmias,
hypertension
Selective Local - hyperemia, follicular conjunctivitis,
conjunctival blanching
Systemic - dry mouth, fatigue, anxiety,
respiratory depression in neonates
Adrenergic Agonists -
Allergy
Adrenergic Agonists -
Allergy
Adrenergic Agonists -
Allergy A 64-year-old male with POAG is taking
timolol, dorzolamide, brimonidine, and
latanoprost OU. He must begin phenelzine, a
systemic monoamine oxidase (MAO)
inhibitor. Which one of the following should
be discontinued?
• Latanoprost
• Brimonidine
• Dorzolamide
• Timolol
Which of the following glaucoma
medications is contraindicated for use in
children younger than age 2?
• Timolol
• Levobunolol
• Brimonidine
• Dorzolamide
A 52-year-old woman with ocular
hypertension is started on a monocular trial
with a glaucoma medication. Which
glaucoma medication is most likely to
produce a decrease in IOP in the contralateral
(untreated) eye?
• Dorzolamide
• Latanoprost
• Timolol
• Brimonidine
Which class of glaucoma
medications should be avoided in
myasthenia gravis? • Miotics
• Prostaglandin analogues
• Beta blockers
• Topical CAIs
Beta-adrenergic
Antagonists (Beta
Blockers) Agents
Non-selective Timolol maleate (Timoptic)
Timolol hemihydrate (Betimol)
Levobunolol HCL (Betagan)
Carteolol HCL (Ocupress)
Metipranolol HCL (Optipranolol)
Selective Betaxolol (Betoptic-S)
Beta-adrenergic
Antagonists (Beta
Blockers) Indications
First line and adjunctive therapy to lower
IOP All types of glaucoma
Before or after laser surgery
After cataract surgery
Contraindications Proven sensitivity to agents
Reactive airway disease Bronchospasm
COPD
Greater than first degree heart block
Beta-adrenergic
Antagonists (Beta
Blockers) Relative contraindications
Congestive heart failure
Bradycardia
Method of action
1- and 2- receptors are on the ciliary
processes. Receptor blockade reduces
aqueous humor production via direct action Direct effect on non-pigmented ciliary
epithelium to decrease secretion via
inhibition of cyclic adenosine
monophosphate
Decreases local capillary perfusion to
reduce ultrafiltration
Beta-adrenergic
Antagonists (Beta
Blockers) Administration
Good corneal penetration
Peak aqueous concentration within 1-2
hours of topical dose. IOP effect peaks at 2
hours and lasts at least 24 hours Short-term escape
Dramatic reduction in IOP after
initial use followed by small
pressure rise that plateaus within
few days
May be due to increase in
receptors during first few days
Wait approximately 1 month to
evaluate response Long-term drift / tachyphylaxis
Approximately 3 months after
initiating therapy, some patients
have a mild decrease in IOP
response
Some will regain responsiveness
after a
drug holiday
Beta-adrenergic
Antagonists (Beta
Blockers) Efficacy
Non-selective 1- and 2- antagonists:
20-30% IOP reduction
1- selective antagonist: 14-17% IOP
reduction
Decreased efficacy possible when used
concomitantly with oral beta-blockers
Systemic absorption may result in IOP
lowering in contralateral eye
Beta-adrenergic
Antagonists (Beta
Blockers) Complications
Ocular toxicity Burning, hyperemia
Corneal anesthesia, punctate keratopathy,
erosions, toxic keratopathy
Periocular contact dermatitis
Dry eye
Cardiovascular 1 blockade slows pulse and decreases
cardiac contractility
May cause syncope, bradycardia,
arrhythmias, heart failure, decreased
exercise tolerance
Beta-adrenergic
Antagonists (Beta
Blockers) Respiratory
2 blockade produces contraction of
bronchial smooth muscle
May cause bronchospasm and airway
obstruction, especially in asthmatics
May cause dyspnea and apneic spells
especially in young children
Central nervous system Depression, anxiety, confusion,