Medication Summary
The goals of pharmacotherapy are to reduce morbidity (visual loss due to optic nerve damage). These are applied topically to the eye.
Prostaglandin Agonists
Class Summary
For reduction of IOP in patients intolerant to other IOP-lowering medications or who have failed to respond optimally to other IOP-lowering medications.
Latanoprost (Xalatan, Xelpros)
May increase the outflow of aqueous humor. Patients should be informed about possible cosmetic effects to the eye/eyelashes, especially if uniocular therapy is to be initiated.
Bimatoprost (Latisse, Lumigan)
This agent is a prostamide analogue with ocular hypotensive activity. It mimics the IOP-lowering activity of prostamides via the prostamide pathway. Bimatoprost ophthalmic solution is used to reduce IOP in open-angle glaucoma and ocular hypertension. Applied topically once a day prior to bed.
Travoprost ophthalmic (Travatan Z)
This agent is a prostaglandin F2-alpha analogue (FP). It is a selective FP prostanoid receptor agonist that is believed to reduce IOP by increasing uveoscleral outflow. Travoprost ophthalmic solution is used to treat open-angle glaucoma and ocular hypertension. Applied topically once a day prior to bed.
Tafluprost (Zioptan)
Tafluprost is a topical, preservative-free, ophthalmic prostaglandin analogue that is indicated for elevated IOP associated with open-angle glaucoma or ocular hypertension. The exact mechanism by which it reduces IOP is unknown, but it is thought to increase uveoscleral outflow. Applied topically once a day prior to bed.
Latanoprostene bunod ophthalmic (Vyzulta)
A 0.024% concentration of a prostamide analog used to lower intraocular (eye) pressure in patients with open-angle glaucoma or ocular hypertension.
Beta-Blockers, Ophthalmic
Class Summary
These agents decrease aqueous production, possibly by blocking adrenergic beta receptors present in the ciliary body. Unfortunately, the nonselective medications in this class also interact with the beta receptors in the heart and lungs, causing significant adverse effects.
Timolol ophthalmic (Timoptic, Timoptic XE, Betimol, Istalol)
Timolol may reduce elevated and normal IOP, with or without glaucoma, by reducing the production of aqueous humor. Timolol gel-forming solution (Timoptic XE) usually is administered at night, unless it is used concurrently with latanoprost therapy. Used as 0.25% or 0.5% solution and applied topically to the eye 1-2 times per day.
Levobunolol (Betagan)
Levobunolol is a nonselective beta adrenergic blocking agent that lowers IOP by reducing aqueous humor production and possibly increasing the outflow of aqueous humor.
Metipranolol
Metipranolol is a beta adrenergic blocker that has little or no intrinsic sympathomimetic effect and membrane-stabilizing activity. It also has little local anesthetic activity. The drug reduces IOP by reducing the production of aqueous humor.
Alpha Agonists, Ophthalmic
Class Summary
Alpha agonists work to both decrease production of fluid and increase drainage.
Brimonidine (Alphagan P)
Brimonidine is a relatively selective alpha2 adrenergic-receptor agonist that decreases IOP by dual mechanisms, reducing aqueous humor production and increasing uveoscleral outflow. Brimonidine has minimal effect on cardiovascular and pulmonary parameters. A moderate risk of allergic response to this drug exists. Caution should be used in individuals who have developed an allergy to Iopidine. IOP lowering of up to 27% has been reported. Applied topically 2-3 times a day.
Carbonic Anhydrase Inhibitors, Ophthalmic
Class Summary
By slowing the formation of bicarbonate ions, causing a reduction in sodium and fluid transport, these agents may inhibit carbonic anhydrase in the ciliary processes of the eye. This effect decreases aqueous humor secretion, reducing IOP. Carbonic anhydrase inhibitors typically have a weaker effect than beta blockers.
Dorzolamide (Trusopt)
Dorzolamide is a reversible carbonic anhydrase inhibitor that may decrease aqueous humor secretion, causing a decrease in IOP. Presumably, it slows bicarbonate ion formation, producing a subsequent reduction in sodium and fluid transport.
Systemic absorption can affect carbonic anhydrase in the kidney, reducing hydrogen ion secretion at the renal tubule and increasing renal excretion of sodium, potassium bicarbonate, and water. Dorzolamide is less stinging on instillation secondary to buffered pH. Applied 2-3 times per day.
Brinzolamide (Azopt)
Brinzolamide catalyzes a reversible reaction involving hydration of carbon dioxide and dehydration of carbonic acid. It may be used concomitantly with other topical ophthalmic drug products to lower IOP. If more than 1 topical ophthalmic drug is being used, administer them at least 10 minutes apart. Applied 2-3 times per day.
Methazolamide (Neptazane)
Methazolamide reduces aqueous humor formation by inhibiting the enzyme carbonic anhydrase, which results in decreased IOP. Oral carbonic anhydrase inhibitors have significant adverse effects, including tiredness, malaise, and anorexia. Because of an increased incidence of adverse effects, it is rarely indicated for the treatment of ocular hypertension.
Antiglaucoma Fixed Combination Formulations, Ophthalmic
Class Summary
Combination solution may further decrease aqueous humor secretion compared to each solution used as monotherapy, while improving compliance. These agents have been approved by the FDA for children aged 2 years or older.
Brinzolamide/brimonidine (Simbrinza)
This combination product contains the carbonic anhydrase inhibitor brinzolamide and the alpha2 adrenergic receptor agonist brimonidine. It is indicated for reduction of elevated intraocular pressure in patients with primary open-angle glaucoma.
Timolol/brimonidine (Combigan)
Brimonidine is a selective alpha2 adrenergic receptor agonist and timolol is a nonselective beta-adrenergic receptor inhibitor. Each of these agents decrease elevated IOP, whether or not associated with glaucoma.
Timolol/dorzolamide (Cosopt)
Dorzolamide is a carbonic anhydrase inhibitor that decreases aqueous humor secretion, causing a decrease in IOP. This agent presumably slows bicarbonate ion formation with subsequent reduction in sodium and fluid transport. Timolol is a nonselective beta-adrenergic receptor blocker that decreases IOP by decreasing aqueous humor secretion.
Carbonic Anhydrase Inhibitors, Systemic
Class Summary
By slowing the formation of bicarbonate ions, causing a reduction in sodium and fluid transport, these agents may inhibit carbonic anhydrase in the ciliary processes of the eye. This effect decreases aqueous humor secretion, reducing IOP. Carbonic anhydrase inhibitors typically have a weaker effect than beta blockers.
Acetazolamide (Diamox Sequels)
Acetazolamide is primarily used for the treatment of refractory POAG and secondary glaucomas. Oral carbonic anhydrase inhibitors have significant adverse effects, including tiredness, malaise, and anorexia. Because of an increased incidence of adverse effects, it is rarely indicated for the treatment of ocular hypertension.
Methazolamide (Neptazane)
Methazolamide reduces aqueous humor formation by inhibiting the enzyme carbonic anhydrase, which results in decreased IOP. Oral carbonic anhydrase inhibitors have significant adverse effects, including tiredness, malaise, and anorexia. Because of an increased incidence of adverse effects, it is rarely indicated for the treatment of ocular hypertension.
Rho Kinase Inhibitor, Ophthalmic
Class Summary
Agents in this class may reduce intraocular pressure by increasing the outflow of aqueous humor through the trabecular meshwork route.
Netarsudil ophthalmic (Rhopressa)
Netarsudil ophthalmic solution 0.02% is a newly approved (2018) rho kinase inhibitor indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. It has not been evaluated for the treatment of juvenile glaucoma.
Latanoprost/netarsudil ophthalmic (Rocklatan)
Newly approved (2019) combination of a rho kinase inhibitor plus an ophthalmic prostaglandin analogue. It is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. It has not been evaluated for the treatment of juvenile glaucoma.
