Chapter 7
GLAUCOMA
Pharmacology of Intraocular
Pressure-Lowering Drugs
Background Glaucoma describes a group of disorders with characteristic structural optic neuropathy (disc cupping) and associated visual field loss. Intraocular pressure (IOP) is often, but not always elevated.
Recognized types of glaucoma include:
■Primary open-angle glaucoma.
■Angle-closure glaucoma.
■Secondary glaucoma (due to uveitis, trauma, etc.).
■Congenital glaucoma.
Reducing IOP is often the most effective means of preserving the visual field.
IOP-lowering medications Prostaglandin agonists have superceded beta blockers as the first-choice therapy due to greater efficacy at lowering IOP and fewer side effects. If the firstchoice monotherapy alone is not effective or not tolerated, it is preferable to switch to another drug that can be initiated as monotherapy, such as a beta blocker.
Pilocarpine has been less prescribed in recent years because of the ocular side effects and the frequent daily dosage, but is still useful in primary angle closure with plateau iris configuration, in acute angle closure with pupillary block mechanism, and in aphakic glaucoma.
If monotherapy is well tolerated but insufficient to reach the target IOP, consider adding a second drug or using a combined drug preparation. The commonly prescribed combination drugs are:
■Timolol 0.5% and dorzolamide 2% (Cosopt) – this has additive effect with pilocarpine.
274 ■ Latanoprost 0.005% and timolol 0.5% (Xalacom).
Pharmacology of intraocular pressure-lowering drugs
Table 7.1: Common side effects
|
Category |
Generics |
Main |
Most common or severe side effects |
Contraindications (CI), |
|
|
|
|
mechanism |
|
precautions (P), and |
|
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|
|
|
|
|
|
|
of action |
|
theoretical risks (T) |
|
|
Prostaglandin |
Latanoprost |
Increased |
Increased skin and iris pigmentation, excessive lash |
T: risk of abortion (See p. 702). |
|
F2α analogues |
Travaprost |
uveoscleral |
growth, aphakic cystoid macular oedema. Rarely: |
|
|
|
|
Bimatoprost |
outflow |
reactivate herpes keratitis, uveitis. Latanoprost |
|
|
|
|
|
(IUSO) |
less likely to cause red eye than Bimatoprost or |
|
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|
Travaprost. |
|
|
|
Nonselective |
Timolol |
Reduced |
Bradycardia, arrhythmia, heart failure, |
CI: asthma, chronic obstructive |
|
β antagonists |
Levobunolol |
aqueous |
bronchospasm, syncope, nocturnal hypotension, |
airways disease (COAD), |
|
|
Carteolol |
production |
headache, depression. Mild corneal hypoaesthesia |
bradycardia, heart block, |
|
|
Metipranolol |
(RAP) |
with prolonged use. |
heart failure. Avoid in normal |
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pressure glaucoma. |
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T: patients on oral |
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hypotensives. |
|
Selective β1 |
Betaxolol |
RAP |
Similar to other β antagonists but theoretically |
P: asthma, COAD, bradycardia, |
|
antagonist |
|
|
fewer respiratory side effects. |
heart block, heart failure. |
|
Alpha2 agonists |
Brimonidine |
RAP & IUSO |
Allergy and red eye, taste disturbance. Respiratory |
CI: Oral monoamine oxidase |
|
|
Apraclonidine |
RAP |
failure and fatigue in children. Fatigue may also |
(MAO) inhibitor users and |
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|
|
occur in adults. |
children. |
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Table 7.1: Common side effects—cont’d
|
Category |
Generics |
Main |
Most common or severe side effects |
Contraindications (CI), |
|
|
|
|
mechanism |
|
precautions (P), and |
|
|
|
|
|
|
|
|
|
of action |
|
theoretical risks (T) |
|
|
Parasympathomimetics |
Pilocarpine |
Increased |
Miosis, pseudomyopia, brow ache, ciliary spasm. |
P: Urinary outflow obstruction, |
|
|
|
aqueous |
Rarely pupil block. Theoretical increased risk of |
asthma. |
|
|
|
outflow |
retinal detachment. |
T: Parkinsonism, peptic ulcers. |
|
Carbonic |
Brinzolamide |
RAP |
Blurred vision, aesthenia, paraesthesia, induced |
CI: sulphonamide allergy, |
|
anhydrase |
Dorzolamide |
|
myopia. |
severe renal impairment. |
|
inhibitors (CAI) |
|
|
|
P: corneal endothelial |
|
|
|
|
|
dysfunction. |
|
Oral CAI |
Acetazolamide |
RAP |
Paraesthesia, nausea, vomiting, diarrhoea, |
CI: suprarenal gland failure, |
|
|
|
|
depression, electrolyte imbalance. Rarely, blood |
electrolyte imbalance, severe |
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|
dyscrasias, metabolic acidosis, renal stones. |
liver disease. |
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P: reduce dose if renal failure |
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(liaise with renal physicians). |
|
Hyperosmotics |
Glycerol (1.0– |
RAP |
Hyperglycaemia (glycerol), pulmonary congestion, |
CI: diabetes. |
|
|
1.5 g/kg p.o.) |
|
electrolyte imbalance, dehydration, headache, |
P: renal failure, elderly patients |
|
|
Mannitol (1.0– |
|
chest pain (mannitol), disorientation, coma. |
with renal or cardiovascular |
|
|
1.5 g/kg i.v.) |
|
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disease. |
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GLAUCOMA 7 Chapter
A
B
Fig. 7.2: Gonioscopy showing a wide-open angle (A) and a closed angle (B). The corneal wedge is formed by the junction of the reflex from the corneoscleral junction (broad arrow) and the corneal endothelium (thin arrow). The apex of the wedge indicates the location of Schwalbe’s line. The trabecular meshwork is visible posterior to this in the top image. See also Fig. 7.13.