5. Anti-Glaucoma Agents
D.J. Rhee et al., Ophthalmologic Drug Guide, 2nd ed., DOI 10.1007/978-1-4419-7621-5_5,
Springer ScienceþBusiness Media, LLC 2011
A. ALPHA AGONISTSS (WHITE TOP – IOPIDINE; PURPLE TOP – ALPHAGAN)
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Mechanism of Action: Activation of alpha-2 receptors in ciliary body inhibits aqueous secretion. Brimonidine also reported to
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increase uveoscleral outflow |
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Side Effects: |
Local irritation, allergy, mydriasis, dry mouth, dry eye, hypotension, lethargy |
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Contraindications: |
MAO inhibitor use |
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Drug |
Trade |
Concentration |
Usual Dose |
Notes |
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apraclonidine |
Iopidine |
Soln, 0.5% |
TID |
for short term use |
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Soln, 1% |
single dose |
for prophylaxis of post-laser IOP spike |
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brimonidine |
Alphagan-P |
Soln, 0.1% or 0.15% |
TID/BID |
highly selective alpha-2 agonist |
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may cause apnea in children |
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(generic) |
Soln, 0.15% or 0.2% |
TID/BID |
highly selective alpha-2 agonist |
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may cause apnea in children |
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Combigan |
Soln, 0.2% |
BID |
Combigan is a combination agent with timolol – see |
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combination agents listed below
SFor listing of preservatives of anti-glaucoma medications, refer to Appendix 5
B. BETA BLOCKERSS (0.25% – LIGHT BLUE TOP, 0.5% – YELLOW TOP)
Mechanism of action: Beta blockade in ciliary body reduces intraocular pressure by decreasing aqueous humor production Side Effects: Local: Blurred vision, corneal anesthesia, superficial punctate keratitis
Systemic: Bradycardia/heart block, bronchospasm, fatigue, mood change, impotence, decreases sensitivity to hypoglycemic symptoms in insulin dependent diabetics, worsening of myasthenia gravis
Contraindications: Asthma, severe COPD, bradycardia, heart block, CHF, myasthenia gravis
Drug |
Trade |
Concentration |
Usual Dose |
Notes |
betaxolol |
Betoptic S |
Soln, 0.25% |
BID |
relatively cardioselective |
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Betoptic |
Soln, 0.5% |
BID |
relatively cardioselective |
carteolol |
Carteolol HCl |
Soln, 1% |
BID |
non-selective, has intrinsic |
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sympathomimetic activity |
levobetaxolol |
Betaxon |
Soln, 0.5% |
BID |
relatively cardioselective |
levobunolol |
AKBETA, Betagan, |
Soln, 0.25, 0.5% |
QD-BID |
non-selective (long half life) |
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Levobunolol HCl |
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metipranolol |
Optipranolol |
Soln, 0.3% |
BID |
non-selective (WHITE top) |
timolol |
Betimol |
Soln, 0.25, 0.5% |
BID |
non-selective |
hemihydrate |
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timolol |
Timoptic |
Soln, 0.25, 0.5% |
BID |
non-selective |
maleate |
Timoptic XE |
Soln, 0.25, 0.5% |
QD |
non-selective, gel-forming solution |
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Timolol GFS |
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Istalol |
Soln, 0.5% |
QD |
non-selective |
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Cosopt |
see notes |
see notes |
Cosopt is a combination agent with dorzolamide – |
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see combination agents listed below |
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SFor listing of preservatives of anti-glaucoma medications, refer to Appendix 5
Anti-Glaucoma Agents 55
C. CARBONIC ANHYDRASE INHIBITORSS (ORANGE TOP) 56
Mechanism of Action: Inhibition of carbonic anhydrase decreases aqueous production in ciliary body; when given parentally, will also dehydrate the vitreous
Side Effects: Local (with topical therapy): bitter taste
Systemic (with topical therapy): diuresis, fatigue, GI upset, Stevens-Johnson syndrome, theoretical risk of aplastic anemia
(with systemic therapy): hypokalemic/acidosis, renal stones, paresthesias, nausea, cramps, diarrhea, malaise, lethargy, depression, impotence, unpleasant taste, aplastic anemia, Stevens-Johnson syndrome
Contraindications: sulfa allergy, hyponatremia/kalemia, recent renal stones, thiazide diuretics, digitalis use
Drug |
Trade |
Concentration |
Usual Dose |
Notes |
acetazolamide |
Diamox |
125, 250 mg tabs |
QD-QID |
onset within 2 hrs, lasts 4–6 hrs |
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Diamox Sequels |
500 mg caps |
QD-BID |
lasts 12–24 hrs |
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500 mg IV |
one dose |
immediate onset, duration 4 hrs for temporary IOP |
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5–10 mg/kg/dose |
PO TID-QID |
control in Infantile Glaucoma; definitive treatment is |
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surgical. For preparation instructions see Appendix 2. |
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Also see subject index for further discussion. |
brinzolamide |
Azopt |
Soln, 1% |
BID-TID |
TID for single therapy |
dorzolamide |
Trusopt |
Soln, 2% |
BID-TID |
TID for single therapy |
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BID when used in combination with beta blockers |
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Cosopt |
see notes |
see notes |
Cosopt is a combination agent with timolol maleate – |
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see combination agents listed below |
methazolamide |
Neptazane, MZM, |
25, 50 mg tabs |
BID-QID |
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Glauctabs |
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SFor listing of preservatives of anti-glaucoma medications, refer to Appendix 5