Glaucoma Drugs

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THE

SECTION SUBJECT TOPIC

Eye Disorders Glaucoma Introduction

MERCK MANUALS

FOR HEALTHCARE ONLINE MEDICAL LIBRARY PROFESSIONALS

DRUGS USED TO TREAT GLAUCOMA Drug/Dose/ Frequency Mechanism of Action on Eye

Type Miotics, direct-acting (cholinergic agonists; topical)

Comments Less effective as monotherapy than β-blockers Possible need for higher strengths in patients with darker-pigmented pupils; hinder dark adaptation Shorter acting, reversible inhibition Very long acting; irreversible inhibition; can cause cataracts and retinal detachment; should be avoided in angle-closure glaucoma because of the extreme miosis; hinder dark adaptation Systemic effects (eg, sweating, headache, tremor, excess saliva production, diarrhea, abdominal cramps, nausea) more likely than with direct-acting miotics May still be excellent choices in pseudophakic patients

Carbachol 1 drop Cause miosis, bid–tid increase aquePilocarpine 1 drop ous outflow bid–qid

Miotics, indirect- Demecarium acting 1 drop (cholinesterase once/day–bid* inhibitors; Echothiophate topical) iodide 1 drop once/day–bid* Isoflurophate 1 drop once/day–bid* Neostigmine 1 drop once/day–bid† Physostigmine 1 drop once/day–bid† Carbonic anhydrase inhibitors (oral or IV)

Cause miosis, increase aqueous outflow

Acetazolamide Decrease aqueous Used as adjunctive therapy 125–250 mg po production Cause fatigue, altered taste, qid (or 500 mg anorexia, depression, paresthepo bid using sias, electrolyte abnormalities, extended-release kidney stones, blood dyscrasias capsules) or 500 Possibly nausea, diarrhea, weight mg IV single loss dose (adult) Methazolamide 25–50 mg po bid–tid Brinzolamide 1 drop bid–qid Dorzolamide 1 drop bid–tid Low risk of systemic effects, but may cause bad taste in mouth

Carbonic anhydrase inhibitors (topical)

Nonselective Dipivefrin 1 drop Cause mydriasis, Often combined with a miotic adrenergic agobid increase aque(dipivefrin, a prodrug, is metabnists (topical) ous outflow and olized to epinephrine) Epinephrine decrease aque- Less reliable than selective 1 drop bid ous production adrenergic agents and higher incidence of allergic and toxic reactions (eg, hypertension, tachycardia) Apraclonidine α2-Selective 1 drop bid–tid adrenergic agonists (topical) Brimonidine 1 drop bid–tid‡ Decrease aqueous With apraclonidine, high rate production; may of allergic reactions and increase tachyphylaxis; less common uveoscleral with brimonidine, which may aqueous outcause dry mouth flow; may cause Systemic effects (eg, hypertenmydriasis sion, tachycardia) less common than with nonselective agonists

THE

SECTION SUBJECT TOPIC

Eye Disorders Glaucoma Introduction

MERCK MANUALS

FOR HEALTHCARE ONLINE MEDICAL LIBRARY PROFESSIONALS

DRUGS USED TO TREAT GLAUCOMA—Continued Drug/Dose/ Frequency Timolol 1 drop once/day–bid Betaxolol 1 drop once/day–bid§ Carteolol 1 drop once/day–bid Levobetaxolol 1 drop bid Levobunolol 1 drop once/day–bid Metipranolol 1 drop once/day–bid Mechanism of Action on Eye

Type β-Blockers (topical)

Comments

Decrease aqueous Systemic adverse effects production; do (eg, bronchospasm, depression, not affect pupil fatigue, confusion, erectile size dysfunction, hair loss, bradycardia) May develop insidiously and be attributed by patients to aging or other processes

Prostaglandin Bimatoprost Increase uveoscle- Increased pigmentation of the iris analogs (topical) 1 drop at bedral outflow and skin; possible worsening of time rather than alter- uveitis ing conventional Elongated and thickened eyeLatanoprost (trabeculo1 drop at lashes; muscle, joint, and back canalicular) bedtime pain; skin rash aqueous outflow Travoprost 1 drop at bedtime Unoprostone 1 drop at bedtime Osmotic diuretics Glycerin Cause increased Used for acute angle closure (oral, IV) 1–1.5 g/kg body serum osmoHave adverse systemic effects weight po larity, which draws fluid from May repeat eye 8–12 h later Mannitol 0.5–2.0 g/kg body weight IV over 30–45 min May repeat 8–12 h later
* † ‡ §

Irreversible; may be cataractogenic; increased risk of retinal detachment. Reversible. More α2-selective than apraclonidine. β1-selective.

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