Brand name: Acular
Drug class: Nonsteroidal Anti-inflammatory Agents
- Nonsteroidal Anti-inflammatory Agents, Ophthalmic
- NSAIAs, EENT
- NSAIDs, EENT
ATC class: S01BC05
VA class: OP300
CAS number: 74103-07-4

Medically reviewed by Drugs.com on Dec 22, 2022. Written by ASHP.

Introduction

Prototypical NSAIA; a pyrrolizine carboxylic acid derivative.

Uses for Ketorolac (EENT)

Conjunctivitis

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

Postoperative Ocular Inflammation

Management of postoperative inflammation associated with cataract extraction.

Postoperative Ocular Pain

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

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

Cystoid Macular Edema

Treatment, with or without concomitant topical corticosteroid therapy, to prevent or relieve postoperative cystoid macular edema associated with cataract extraction^{† [off-label]}.

Has been used for the active treatment of chronic aphakic or pseudophakic cystoid macular edema^{† [off-label]}.

Inhibition of Intraoperative Miosis

Has been used prophylactically before ocular surgery to prevent or reduce intraoperative miosis^{† [off-label]}.

Ketorolac (EENT) Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the eye as an ophthalmic solution.

Avoid contamination of the solution container.

Do not administer while wearing contact lenses.

Preservative-free solution is for single use only in one or both eyes; use immediately after opening and discard any unused portion immediately after administration.

Has been safely administered with other ophthalmic medications (e.g., antibiotics, β-blockers, carbonic anhydrase inhibitors, cycloplegics, mydriatics).

Dosage

Available as ketorolac tromethamine; dosage expressed in terms of the salt.

Pediatric Patients

Conjunctivitis

Ophthalmic

Children ≥3 years of age: 1 drop (250 mg) of a 0.5% solution in the affected eye(s) 4 times daily.

Postoperative Ocular Inflammation

Ophthalmic

Children ≥3 years of age: 1 drop (250 mcg) of a 0.5% solution in the eye(s) undergoing surgery 4 times daily beginning 24 hours after surgery and typically continuing for 2 weeks after surgery.

Postoperative Ocular Pain

Ophthalmic

Children ≥3 years of age undergoing ocular incisional refractive surgery: 1 drop (250 mcg) of a 0.5% preservative-free solution 4 times daily in the eye(s) that underwent surgery as needed for up to 3 days after surgery.

Children ≥3 years of age undergoing corneal refractive surgery: 1 drop (200 mcg) of a 0.4% solution 4 times daily in the eye(s) that underwent surgery as needed for up to 4 days after surgery.

Adults

Conjunctivitis

Ophthalmic

1 drop (250 mg) of a 0.5% solution in the affected eye(s) 4 times daily.

Postoperative Ocular Inflammation

Ophthalmic

1 drop (250 mcg) of a 0.5% solution in the eye(s) undergoing surgery 4 times daily beginning 24 hours after surgery and typically continuing for 2 weeks after surgery.

Postoperative Ocular Pain

Ophthalmic

Patients undergoing ocular incisional refractive surgery: 1 drop (250 mcg) of a 0.5% preservative-free solution 4 times daily in the eye(s) that underwent surgery as needed for up to 3 days after surgery.

Patients undergoing corneal refractive surgery: 1 drop (200 mcg) of a 0.4% solution 4 times daily in the eye(s) that underwent surgery as needed for up to 4 days after surgery.

Cystoid Macular Edema

Postoperative Cystoid Macular Edema† [off-label]

Ophthalmic

1–2 drops (250–500 mcg) of a 0.5% solution in the eye(s) undergoing surgery every 6–8 hours beginning 24 hours prior to surgery and continuing for 3–4 weeks after surgery.

Chronic Aphakic or Pseudophakic Cystoid Macular Edema† [off-label]

Ophthalmic

1–2 drops (250–500 mcg) of a 0.5% solution in the affected eye(s) 4 times daily for 2–3 months.

Cautions for Ketorolac (EENT)

Contraindications

Known hypersensitivity to ketorolac tromethamine or any ingredient in the formulation.

Warnings/Precautions

Warnings

Hematologic Effects

May inhibit platelet aggregation and prolong bleeding time.

May increase bleeding (e.g., hyphemas) of ocular tissues in patients undergoing ocular surgery.

Use with caution in patients with underlying bleeding tendencies or in those receiving drugs known to prolong bleeding time.

Sensitivity Reactions

Cross-sensitivity

Possible cross-sensitivity with aspirin, phenylacetic acid derivatives, and other NSAIAs. Use with caution in patients with history of hypersensitivity to these drugs.

General Precautions

Wound Healing Complications

Possible slow or delayed wound healing; may be potentiated with concomitant adminsitration of topical NSAIAs or topical corticosteroids. (See Specific Drugs under Interactions.)

Ocular Effects

Use may result in keratitis. In susceptible patients, continued use may result in epithelial breakdown, corneal thinning, erosion, ulceration, or perforation, which may be sight-threatening.

If manifestations of corneal epithelial breakdown occur, discontinue immediately and closely monitor corneal health.

Increased risk of sight-threatening, adverse corneal effects in patients with complicated ocular surgeries, corneal denervation, corneal epithelial defects, diabetes mellitus, ocular surface diseases (e.g., dry eye syndrome), rheumatoid arthritis, or repeat ocular surgeries within a short period of time; use with caution in such patients.

Use >24 hours prior to surgery or >14 days postoperatively may precipitate or exacerbate adverse corneal effects.

Specific Populations

Pregnancy

Category C. Avoid use in the third trimester because of possible premature closure of the ductus arteriosus.

Lactation

Distributed into milk after systemic administration. Caution if used in nursing women.

Pediatric Use

Safety and efficacy not established in children <3 years of age.

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults.

Common Adverse Effects

Ocular stinging and burning.

Interactions for Ketorolac (EENT)

No formal drug interaction studies to date.

Specific Drugs

Ketorolac (EENT) Pharmacokinetics

Absorption

Bioavailability

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

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

Distribution

Extent

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

Ketorolac crosses the placenta and is distributed into milk following systemic administration.

Plasma Protein Binding

>99%.

Stability

Storage

Ophthalmic

0.4% Solution

15–25°C.

0.5% Solution

Light-resistant containers at 15–30°C.

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).

• Substantially reduces aqueous humor concentrations of these prostaglandins.

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

Advice to Patients

• Importance of learning and adhering to proper administration techniques to avoid contamination of the product.

• Importance of removing contact lenses before administration.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as concomitant illnesses.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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