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Home , Methazolamide

Table 7-1 Medications

Adverse Effects Comments, Including Time to Class/Compound Concentration Dosing Mechanism of Action IOP Reduction Ocular Systemic Peak Effect and Washout

Prostaglandin analogues 0.005% Once daily Increases 25%–32% Increased pigmentation of iris Flulike symptoms, joint/ ±IOP-lowering effect with uveoscleral and lashes, hypertrichosis, muscle pain, headache miotic outflow trichiasis, distichiasis, Peak: 10–14 hours primarily. blurred vision, keratitis, Washout: 4–6 weeks Also increases anterior uveitis, conjunctival Maximum IOP-lowering conventional hyperemia, exacerbation effect may take up to outflow. of herpes keratitis, CME, 6 weeks to occur -associated periorbitopathy 0.004% Once daily Same as above 25%–32% Same as above Same as above Same as above 0.03, 0.01% Once daily Same as above 27%–33% Same as above Same as above Same as above 0.0015% Once daily Increases 27%–31% Same as above Same as above Same as above uveoscleral outflow Latanoprostene 0.024% Once daily Increases 30%–32% Same as above, plus pain with Same as above Same as above bunod uveoscleral instillation outflow and may increase trabecular outflow facility b-Adrenergic antagonists (b-blockers) Nonselective maleate 0.25% and 0.50% Solutions: Decreases 20%–30% Blurring, irritation, corneal Bradycardia, heart block, May be less effective if solution or gel 1–2 times aqueous anesthesia, punctate keratitis, bronchospasm, lowered patient is taking systemic Also 0.1% gel daily production allergy; aggravation of blood pressure, decreased β-blockers; short-term Gels: once myasthenia gravis libido, CNS depression, escape, long-term drift; daily mood swings, reduced diabetic patients may exercise tolerance, experience reduced masked symptoms of glucose tolerance and hypoglycemia, exacerbation masking of hypoglycemic of myasthenia gravis signs/symptoms Peak: 2–3 hours Washout: 1 month Timolol hemihydrate 0.5% As above Same as above 20%–30% Same as above Same as above — 0.25, 0.5% As above Same as above 20%–30% Same as above Same as above Peak: 2–6 hours 0.3% 2 times daily Same as above 20%–30% Same as above Same as above Report of iritis Peak: 2 hours

(Continued) Adverse Effects Comments, Including Time to Class/Compound Concentration Dosing Mechanism of Action IOP Reduction Ocular Systemic Peak Effect and Washout

Carteolol 1.0% 1–2 times daily — — — Intrinsic sympathomimetic May have less effect on hydrochloride nocturnal pulse, blood pressure Peak: 4 hours Washout: 1 month Selective 0.25% 2 times daily Same as above 15%–20% Same as above Lower risk of pulmonary Peak: 2–3 hours complications Washout: 1 month a2-Adrenergic agonists Selective 0.5, 1.0% 2–3 times daily Decreases 20%–30% Irritation, ischemia, allergy, Hypotension, vasovagal Useful in pre- or postlaser hydrochloride aqueous eyelid retraction, conjunctival attack, dry mouth and nose, or cataract surgery production blanching, follicular fatigue Tachyphylaxis may limit conjunctivitis, pruritus, long-term use. dermatitis, ocular ache, Peak: <1–2 hours photopsia, miosis Washout: 7–14 days 0.2% 2–3 times daily Decreases 20%–30% Blurring, foreign-body Headache, fatigue, Highly selective for

tartrate 0.2% aqueous sensation, eyelid edema, hypotension, insomnia, α2-receptor production, dryness, less ocular depression, syncope, Brimonidine should not be increases sensitivity/allergy than with dizziness, anxiety, dry used in infants and young uveoscleral apraclonidine mouth children. outflow Peak: 2 hours Washout: 7–14 days Brimonidine tartrate 0.1% 2–3 times daily Same as above Same as above Same as above, except less Same as above, except less Same as above in Purite 0.1% allergy than with brimonidine fatigue and depression than 0.2% with brimonidine 0.2% Carbonic anhydrase inhibitors Oral 125 mg Seldom Decreases 15%–20% None Poor tolerance of carbonated May cause allergic reaction used for aqueous beverages, acidosis, in persons with sulfa IOP-lowering production depression, malaise, allergy therapy hirsutism, flatulence, Use with caution in patients paresthesias, numbness, susceptible to ketoacidosis 250 mg 2–4 times daily lethargy, blood dyscrasias, or hepatic insufficiency diarrhea, weight loss, Caution for using an oral 500 mg 2 times daily renal stones, loss of libido, CAI with other drugs that (sustained impotence, bone marrow cause potassium loss release) depression, hypokalemia, Peak: 3–6 hours (sustained cramps, anorexia, altered release) taste, increased serum 2–4 hours (oral) urate, enuresis Adverse Effects Comments, Including Time to Class/Compound Concentration Dosing Mechanism of Action IOP Reduction Ocular Systemic Peak Effect and Washout

Acetazolamide 500 mg Usually every Same as above Same as above Same as above Same as above Same as above (parenteral) 5–10 mg/kg 6–8 hours Methazolamide 25, 50 mg 2–3 times daily Same as above Same as above Same as above Same as above Same as above Topical 2% 2–3 times daily Same as above 15%–20% Induced myopia, blurred Less likely to induce Peak: 2–3 hours vision, stinging, keratitis, systemic effects of CAI, but Washout: 48 hours punctate keratopathy, may occur; bitter taste conjunctivitis, dermatitis 1% 2–3 times daily Same as above Same as above Same as above, except less Same as above Same as above stinging when compared with dorzolamide Parasympathomimetic agents (miotics) Cholinergic agonist (direct acting) HCl 0.5, 1.0, 2.0, 3.0, 2–4 times daily Increases 15%–25% Posterior synechiae, keratitis, Increased salivation, Exacerbation of cataract 4.0, 6.0% trabecular , brow ache, cataract increased secretion effect; more effective in outflow growth, angle-closure (gastric), abdominal cramps lighter irides 1 potential, myopia, retinal Peak: 1 /2 –2 hours tear/detachment, dermatitis, Washout: 48 hours change in retinal sensitivity, color vision changes, epiphora Anticholinesterase agent (indirect acting) iodide 0.125% 1–2 times daily Same as above 15%–25% Intense miosis, iris pigment Same as pilocarpine; more Increased inflammation cyst, myopia, cataract, gastrointestinal difficulties with ocular surgery; retinal detachment, angle may be helpful in closure, punctal stenosis, aphakia, anesthesia risks pseudopemphigoid, epiphora (prolonged recovery); useful in eyelid-lash lice, cataract surgery postoperatively Rho kinase inhibitors 0.02% Once daily Increases 18%–23% Conjunctival hyperemia, None — (nighttime) trabecular conjunctival hemorrhage, outflow facility; cornea verticillata, pruritus, reduces increased lacrimation, episcleral blurred vision venous pressure

(Continued) Adverse Effects Comments, Including Time to Class/Compound Concentration Dosing Mechanism of Action IOP Reduction Ocular Systemic Peak Effect and Washout

Fixed combinations Timolol/ 0.5%/1% 2 times daily Reduces aqueous 25%–30% Same as those of nonselective Same as those of — brinzolamide secretion β-adrenergic antagonist, nonselective β-adrenergic topical CAI antagonist, topical CAI Timolol/dorzolamide 0.5%/2% 2 times daily Decreases 25%–30% Same as those of nonselective Same as those of Peak: 2–3 hours aqueous β-blocker, topical CAI nonselective β-blocker, Washout: 1 month production topical CAI Timolol/latanoprost 0.5%/0.005% Once daily Same as Greater than Same as those of nonselective Same as those of Not currently available in (nighttime) nonselective monotherapy β-blocker and latanoprost nonselective β-blocker and the United States β-blocker and with each latanoprost latanoprost individually Timolol/travoprost 0.5%/0.004% Once daily Same as Same as above Same as those of nonselective Same as nonselective Same as above (nighttime) nonselective β-blocker and travoprost β-blocker and travoprost β-blocker and travoprost Timolol/bimatoprost 0.5%/0.03% Once daily Same as Same as above Same as those of nonselective Same as nonselective Same as above (nighttime) nonselective β-blocker and bimatoprost β-blocker and bimatoprost β-blocker and bimatoprost Timolol/brimonidine 0.5%/0.2% 2 times daily Same as Same as above Same as those of nonselective Same as those of — tartrate nonselective β-blocker and α-agonist nonselective β-blocker and β-blocker and α-agonist α-agonist Brimonidine/ 0.2%/1% 2–3 times daily Decreases 26%–36% Same as those of the Same as those of the — brinzolamide aqueous individual components individual components production; may increase uveoscleral outflow Hyperosmotic agents Mannitol (parenteral) 20% 0.5–2.0 g/kg Creates osmotic — IOP rebound, increased Urinary retention, headache, Contraindicated in patients body weight gradient; aqueous flare congestive heart failure, in renal failure or on dehydrates diabetic complications, dialysis; caution in heart vitreous nausea, vomiting, diarrhea, failure; useful in acute electrolyte disturbance, increased IOP confusion, backache, myocardial infarction Glycerol (oral) 50% 1–1.5 g/kg Same as above — Similar to above Similar to above; can cause Similar to above; may problems in diabetic precipitate diabetic patients ketoacidosis