ACULAR LS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ACULAR LS (ACULAR LS).
Selective COX-2 inhibitor; inhibits prostaglandin synthesis, reducing ocular inflammation and pain.
| Metabolism | Primarily hepatic via CYP2C9; undergoes glucuronidation and oxidation to inactive metabolites. |
| Excretion | Renal excretion of metabolites and unchanged drug accounts for approximately 26% of the dose. Fecal excretion accounts for approximately 74% of the dose, primarily as metabolites. |
| Half-life | The terminal elimination half-life is approximately 1.8 hours (range 1.2–2.5 hours) following topical ocular administration. This short half-life is consistent with rapid clearance from the systemic circulation. |
| Protein binding | Ketorolac is highly protein bound, approximately 99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | The volume of distribution is approximately 0.12 L/kg, indicating distribution primarily into extracellular fluid with limited tissue penetration. |
| Bioavailability | Ophthalmic bioavailability is approximately 2% of the administered dose due to extensive nasolacrimal drainage and systemic absorption. Oral bioavailability of ketorolac is approximately 80-100%, but this route is not used for ophthalmic formulations. |
| Onset of Action | Following topical ocular administration, the onset of anti-inflammatory activity occurs within 30 minutes, as measured by reduction in ocular inflammation markers. |
| Duration of Action | The duration of anti-inflammatory effect is approximately 6 hours after a single topical dose, supporting four times daily dosing for sustained efficacy. |
1 drop in the affected eye(s) four times daily
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for renal impairment |
| Liver impairment | No dosage adjustment required for hepatic impairment but use with caution in severe hepatic disease due to potential for increased systemic exposure |
| Pediatric use | Safety and efficacy in pediatric patients below 2 years of age have not been established; for children 2 years and older, same as adult dosing |
| Geriatric use | No specific dose adjustment recommended; use with caution due to increased incidence of age-related ocular conditions |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ACULAR LS (ACULAR LS).
| Breastfeeding | It is not known whether ketorolac is excreted in human milk after ophthalmic administration. Systemic levels are low, and following oral administration, ketorolac is excreted in breast milk at low concentrations (M/P ratio approximately 0.37). Due to the potential for adverse effects on the nursing infant, caution should be exercised. The low systemic absorption likely poses minimal risk. |
| Teratogenic Risk | Ketorolac tromethamine, the active ingredient in ACULAR LS, is a nonsteroidal anti-inflammatory drug (NSAID). In animal reproduction studies, administration of ketorolac during organogenesis resulted in increased embryofetal mortality, delayed ossification, and increased incidence of skeletal abnormalities at doses less than the maximum recommended human ophthalmic dose. However, systemic exposure following ocular administration is very low. NSAIDs are generally avoided during pregnancy, especially in the third trimester, due to the risk of premature closure of the ductus arteriosus and oligohydramnios. The risk is considered low for ophthalmic use but should be used only if clearly needed. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to ketorolac tromethamine or any component of the formulation","Patients with active peptic ulcer disease, recent GI bleeding, or perforation","Patients with advanced renal disease or at risk for renal failure","Patients with known history of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs"]
| Precautions | ["Increased risk of bleeding and bleeding-related adverse events due to platelet inhibition","May prolong bleeding time","Cross-sensitivity with aspirin and other NSAIDs","Caution in patients with prior history of corneal epithelial defects or ocular surgery","Not for intraocular injection"] |
| Food/Dietary | No known food interactions for ophthalmic ketorolac. However, maintain good hydration and nutrition to support corneal healing. |
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| Fetal Monitoring | No specific monitoring is typically required for ophthalmic ketorolac use in pregnancy. However, if used systemically or for prolonged periods, monitor for maternal renal function, gastrointestinal bleeding, and fetal ultrasound for oligohydramnios or ductus arteriosus constriction, especially in the third trimester. Given ophthalmic route, monitoring is not routinely indicated. |
| Fertility Effects | Ketorolac and other NSAIDs may impair female fertility by inhibiting prostaglandin synthesis, which can affect ovulation. Reversible delay in ovulation has been reported with systemic NSAIDs. The effect of ophthalmic ketorolac on fertility is unknown but likely negligible due to minimal systemic exposure. |
| Clinical Pearls | ACULAR LS (ketorolac tromethamine ophthalmic solution 0.4%) is a nonsteroidal anti-inflammatory drug (NSAID) indicated for the reduction of ocular pain and photophobia following corneal refractive surgery. Use with caution in patients with known bleeding tendencies or those on anticoagulants due to increased risk of ocular bleeding. Avoid concurrent use with other NSAIDs or steroids to minimize corneal adverse effects. Monitor for corneal epithelial breakdown or delayed healing. |
| Patient Advice | Do not touch the dropper tip to any surface to avoid contamination. · Remove contact lenses before instillation and wait at least 10 minutes before reinserting. · Use only in the affected eye(s) as prescribed; do not use for longer than directed. · Temporary stinging or burning may occur upon instillation. · Report any persistent pain, redness, or visual changes to your doctor immediately. · Avoid driving or operating machinery if vision is blurred after use. |