Acular eent

Name: Acular eent

Introduction

Prototypical NSAIA; a pyrrolizine carboxylic acid derivative.1 2 3 4 14 21 22 25 26 27 28

Uses for Acular

Conjunctivitis

Temporary relief of ocular itching due to seasonal allergic (hay fever, pollinosis) conjunctivitis.1 141 142 143

Postoperative Ocular Inflammation

Management of postoperative inflammation associated with cataract extraction.1 11 17 18 19 61 85 110 147

Postoperative Ocular Pain

Reduction of ocular pain and burning/stinging following corneal refractive surgery and photorefractive keratectomy (PRK).155 156

Ketorolac tromethamine 0.5% preservative-free ophthalmic solution is used for the reduction of ocular pain and photophobia following incisional refractive surgery.154

Cystoid Macular Edema

Treatment, with or without concomitant topical corticosteroid therapy, to prevent or relieve postoperative cystoid macular edema associated with cataract extraction†.61

Has been used for the active treatment of chronic aphakic or pseudophakic cystoid macular edema†.14 20 23

Inhibition of Intraoperative Miosis

Has been used prophylactically before ocular surgery to prevent or reduce intraoperative miosis†.53 81 106 107 108 110 137 139

Acular Pharmacokinetics

Absorption

Bioavailability

Extent of ocular and systemic absorption not fully elucidated;1 however, limited concentrations are achieved systemically following topical application to the eye relative to usual oral or parenteral doses.1 14 16 18

Following topical application to the eye, plasma ketorolac concentrations were detectable (range: 10.7–22.5 ng/mL) in about 20% of patients.1 154 155

Distribution

Extent

Distribution into human ocular tissues and fluids not fully characterized to date.1 14 78

Ketorolac crosses the placenta21 28 46 47 78 and is distributed into milk following systemic administration.2 14 21 22 48 78

Plasma Protein Binding

>99%.2 14 28 45 49 78

Stability

Storage

Ophthalmic

0.4% Solution

15–25°C.155

0.5% Solution

Light-resistant containers at 15–30°C.1 154

Actions

  • Inhibits synthesis of certain ocular prostaglandins (e.g., PGE2) in iris, ciliary body, and conjunctiva by inhibiting cyclooxygenase-1 (COX-1) and -2 (COX-2).1 2 4 6 10 21 28 40 62 66 68 69 70 71 72 73 77 80 81 110 154 155

  • Substantially reduces aqueous humor concentrations of these prostaglandins.1 80 81 110 121 122 123 126 128

  • Does not appear to inhibit lipoxygenase;21 81 does not inhibit aspects of inflammation mediated by leukotrienes.81 119 137

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