Acular

Name: Acular

Ketorolac Ophthalmic Interactions

While using this medication, do not wear any contact lens that has not been approved by your doctor.

Do not use any other eye medications unless your doctor has prescribed them.

Tell your doctor about all other medications you use, especially a blood thinner such as warfarin (Coumadin).

This list is not complete and there may be other drugs that can interact with ketorolac ophthalmic. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.

What is Acular (ketorolac ophthalmic)?

Ketorolac is a nonsteroidal anti-inflammatory drug (NSAID) that works by reducing hormones that cause inflammation and pain in the body.

Ketorolac ophthalmic (for the eye) is used to relieve eye itching caused by seasonal allergies.

Ketorolac ophthalmic is also used to reduce swelling, pain, and burning or stinging after cataract surgery or corneal refractive surgery.

Ketorolac ophthalmic may also be used for purposes not listed in this medication guide.

What happens if I overdose?

An overdose of ketorolac ophthalmic is not expected to be dangerous. Seek emergency medical attention or call the Poison Help line at 1-800-222-1222 if anyone has accidentally swallowed the medication.

What should I avoid while using Acular (ketorolac ophthalmic)?

While using this medication, do not wear any contact lens that has not been approved by your doctor.

Do not use other eye medications unless your doctor tells you to.

Dosage Forms and Strengths

10 mL size bottle filled with 5 mL of ketorolac tromethamine ophthalmic solution, 0.5% (5 mg/mL)

Acular Description

Acular® (ketorolac tromethamine ophthalmic solution) 0.5% is a member of the pyrrolo-pyrrole group of nonsteroidal anti-inflammatory drugs (NSAIDs) for ophthalmic use. Its chemical name is (±)-5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid, compound with 2-amino-2-(hydroxymethyl)-1,3-propanediol (1:1) and it has the following structure:

Acular® ophthalmic solution is supplied as a sterile isotonic aqueous 0.5% solution, with a pH of 7.4. Acular® ophthalmic solution contains a racemic mixture of R-(+) and S-(-)- ketorolac tromethamine. Ketorolac tromethamine may exist in three crystal forms. All forms are equally soluble in water. The pKa of ketorolac is 3.5. This white to off-white crystalline substance discolors on prolonged exposure to light. The molecular weight of ketorolac tromethamine is 376.41. The osmolality of Acular® ophthalmic solution is 290 mOsmol/kg.

Each mL of Acular® ophthalmic solution contains: Active: ketorolac tromethamine 0.5%. Preservative: benzalkonium chloride 0.01%. Inactives: edetate disodium 0.1%; octoxynol 40; purified water; sodium chloride; hydrochloric acid and/or sodium hydroxide to adjust pH.

Acular - Clinical Pharmacology

Mechanism of Action

Ketorolac tromethamine is a nonsteroidal anti-inflammatory drug which, when administered systemically, has demonstrated analgesic, anti-inflammatory, and anti-pyretic activity. The mechanism of its action is thought to be due to its ability to inhibit prostaglandin biosynthesis.

Pharmacokinetics

Two drops of 0.5% ketorolac tromethamine ophthalmic solution instilled into the eyes of patients 12 hours and 1 hour prior to cataract extraction achieved a mean ketorolac concentration of 95 ng/mL in the aqueous humor of 8 of 9 eyes tested (range 40 to 170 ng/mL).

One drop of 0.5% ketorolac tromethamine ophthalmic solution was instilled into 1 eye and 1 drop of vehicle into the other eye TID in 26 healthy subjects. Five (5) of 26 subjects had detectable concentrations of ketorolac in their plasma (range 11 to 23 ng/mL) at Day 10 during topical ocular treatment. The range of concentrations following TID dosing of 0.5% ketorolac tromethamine ophthalmic solution are approximately 4 to 8% of the steady state mean minimum plasma concentration observed following four times daily oral administration of 10 mg ketorolac in humans (290 ± 70 ng/mL).

Clinical Studies

Two controlled clinical studies showed that ketorolac tromethamine ophthalmic solution was significantly more effective than its vehicle in relieving ocular itching caused by seasonal allergic conjunctivitis.

Two controlled clinical studies showed that patients treated for two weeks with ketorolac tromethamine ophthalmic solution were less likely to have measurable signs of inflammation (cell and flare) than patients treated with its vehicle.

Results from clinical studies indicate that ketorolac tromethamine has no significant effect upon intraocular pressure; however, changes in intraocular pressure may occur following cataract surgery.

In Summary

Common side effects of Acular include: burning sensation of eyes and stinging of eyes. See below for a comprehensive list of adverse effects.

For Healthcare Professionals

Applies to ketorolac ophthalmic: ophthalmic solution

General

The most frequently reported side effects were transient stinging and burning on instillation.[Ref]

Ocular

Common (1% to 10%): Intraocular pressure increased, conjunctival hyperemia, conjunctival hemorrhage, corneal edema, ocular pain, tearing, vision blurred, corneal infiltrates, ocular edema, iritis, ocular inflammation, ocular irritation, superficial keratitis, superficial ocular infection, conjunctivitis, ocular pruritus, keratic precipitates, retinal hemorrhage, cystoid macular edema, eye trauma, ptosis, blepharitis, photophobia, corneal lesion, glaucoma
Uncommon (0.1% to 1%): Ulcerative keratitis, eye dryness, epiphora, corneal ulcer
Postmarketing reports: Corneal erosion, corneal perforation, corneal thinning, corneal melt, epithelial breakdown[Ref]

Local

Very common (10% or more): Transient stinging (up to 40%), burning (up to 40%)
Common (1% to 10%): Local allergic reaction[Ref]

Nervous system

Common (1% to 10%): Headache[Ref]

Respiratory

Postmarketing reports: Bronchospasm, asthma exacerbated[Ref]

Hypersensitivity

Common (1% to 10%): Hypersensitivity reaction[Ref]

Some side effects of Acular may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

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