ACULAR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ACULAR (ACULAR).
Nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, which decreases inflammation, pain, and fever.
| Metabolism | Hepatic metabolism primarily via cytochrome P450 2C9 (CYP2C9). |
| Excretion | Renal: ~80% as unchanged drug and glucuronide conjugates; biliary/fecal: ~20% |
| Half-life | Terminal half-life: 1.8 hours (ketorolac tromethamine); clinical context: short half-life supports dosing every 6 hours for acute pain, but prolonged in elderly or renal impairment (↑ to 5-6 hours, thus dose reduction required). |
| Protein binding | 99% bound; primary binding protein: albumin. |
| Volume of Distribution | 0.11-0.25 L/kg; clinical meaning: low Vd indicates primarily confined to extracellular compartment (plasma and interstitial fluid), minimal tissue penetration. |
| Bioavailability | Ophthalmic: ~2% systemic absorption after topical instillation (due to corneal permeability and nasolacrimal drainage); oral formulation not used for Acular (ophthalmic only). |
| Onset of Action | Ophthalmic: ~1 hour after topical administration; peak effect at 2-3 hours for reduction of ocular inflammation. |
| Duration of Action | Ophthalmic: 4-6 hours for anti-inflammatory effect; clinical note: used preoperatively and postoperatively, often QID dosing. |
One drop of 0.5% ophthalmic solution into 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. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established; use not recommended. |
| Geriatric use | No specific dosage adjustment required; use same dosing as for younger adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ACULAR (ACULAR).
| Breastfeeding | Ketorolac is excreted in human milk at low levels. The M/P ratio is not well defined. Due to potential adverse effects in nursing infants, caution is advised. Use only if clearly indicated and consider alternative agents. |
| Teratogenic Risk | Pregnancy Category C. No adequate studies in pregnant women. Ketorolac tromethamine, like other NSAIDs, may cause premature closure of the ductus arteriosus and fetal renal impairment in the third trimester. First and second trimester use should be avoided unless clearly needed. The potential benefits should be weighed against the risks. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Hypersensitivity to ketorolac tromethamine or any component of the formulation","History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs","Active epithelial herpes simplex keratitis","Late pregnancy (third trimester) due to risk of premature closure of ductus arteriosus"]
| Precautions | ["May increase bleeding time due to inhibition of platelet aggregation; use with caution in patients with known bleeding tendencies or those receiving other medications that may prolong bleeding time.","May cause corneal effects including keratitis and corneal thinning; discontinue if corneal epithelial breakdown occurs.","Use with caution in patients with prior sensitivity to aspirin, phenylacetic acid derivatives, or other NSAIDs.","May delay wound healing or exacerbate infections; avoid use in patients with active epithelial herpes simplex keratitis."] |
| Food/Dietary | No known food interactions. Avoid alcohol if concomitant oral NSAIDs are used due to increased risk of gastrointestinal bleeding, but this is not specific to ophthalmic use. |
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| Fetal Monitoring |
| Monitor fetal heart rate and uterine activity if used near term. In chronic use, monitor amniotic fluid index and ductus arteriosus patency via ultrasound. Maternal monitoring includes renal function, platelet count, and signs of bleeding. |
| Fertility Effects | NSAIDs may impair female fertility by affecting ovulation via inhibition of prostaglandin synthesis. This effect is reversible upon discontinuation. Ketorolac use should be avoided in women attempting conception. |
| Clinical Pearls | ACULAR (ketorolac tromethamine ophthalmic solution) is a nonsteroidal anti-inflammatory drug (NSAID) used for ocular inflammation. Avoid concomitant use with other NSAIDs or corticosteroids due to increased risk of corneal adverse events. Use with caution in patients with bleeding disorders or those on anticoagulants, as it may increase bleeding tendency. Monitor for corneal toxicity, especially in patients with compromised corneal integrity. Ensure proper storage at room temperature and discard if solution changes color or becomes cloudy. |
| Patient Advice | Do not touch the dropper tip to any surface to avoid contamination. · Remove contact lenses before instillation and wait at least 15 minutes before reinserting. · Apply pressure to the inner corner of the eye (nasolacrimal occlusion) for 1 minute after instillation to reduce systemic absorption. · Do not use while wearing soft contact lenses, as the preservative may be absorbed. · Report any signs of corneal problems such as pain, redness, or vision changes immediately. · Use exactly as prescribed and do not share the medication with others. |