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Drugs acting on eye
The eye is a complex sensory organ responsible for sight. Injury
or disease to the ocular system can result in vision loss. A variety of ophthalmic preparations (topical, parenteral, and oral) are available for both therapeutic and diagnostic use. Medications play a key role in the management of chronic dry- eye, diabetic retinopathy, glaucoma, infection, inflammation, and macular degeneration For the treatment of glaucoma Prostaglandin Analogs attenuate intraocular pressure (IOP) by improving the outflow of aqueous humor. Prostaglandin analogs exhibit agonistic activity on FP prostanoid receptors, which promotes uveoscleral outflow. Medications within this class include latanoprost, travoprost, bimatoprost, tafluprost, and unoprostone isopropyl α-Adrenoreceptor Agonists can be applied topically to decrease production of aqueous humor. Ophthalmic α2 agonists include brimonidine and apraclonidine. By activating α2 receptors in the ciliary epithelium, adenylyl cyclase becomes inhibited and cyclic adenosine monophosphate (cAMP) is no longer formed. This hinders ion transport and, thus, fluid production. Over time, these medications appear to improve fluid outflow as well. β-Adrenoreceptor Antagonists administered topically can reduce IOP by decreasing aqueous humor production. Beta-blockers antagonize the effects of sympathetic neurotransmitters by inhibiting β1 and β2 receptors; however their mechanistic action in glaucoma is unclear. Examples include timolol, betaxolol, carteolol, and levobunolol.
Carbonic Anhydrase Inhibitors (CAIs) work by decreasing
production of aqueous humor. Carbonic anhydrase is an enzyme that catalyzes the formation of bicarbonate from carbon dioxide and water (and vice-versa), with the most active isoform being carbonic anhydrase II. Inhibition of this isoenzyme within the ciliary epithelium slows the formation of bicarbonate ions; decreasing the extracellular transport of water necessary for aqueous humor production. Dorzolamide and brinzolamide are topical medications within this class Acetazolamide is administered orally and has a higher rate of IOP reduction when compared to topical CAIs Parasympathomimetic Agents are topical cholinergic agonists that reduce IOP by improving fluid outflow through the trabecular meshwork. Activation of muscarinic (M3) receptors allows for contraction of ciliary muscle fibers, which expands the pores of the trabecular meshwork to enhance outflow. Ophthalmic agents within this class include carbachol and pilocarpine.