ACUVAIL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ACUVAIL (ACUVAIL).
Ketorolac tromethamine, a nonsteroidal anti-inflammatory drug (NSAID), inhibits prostaglandin synthesis by blocking cyclooxygenase (COX-1 and COX-2) enzymes. This reduces ocular inflammation and pain.
| Metabolism | Primarily hepatic via conjugation with glucuronic acid; minor role of cytochrome P450 enzymes. Approximately 50% is excreted as parent drug and metabolites in urine. |
| Excretion | Primarily renal excretion of metabolites; less than 1% excreted unchanged. Biliary/fecal elimination accounts for <10%. |
| Half-life | Terminal elimination half-life is approximately 46 minutes in the aqueous humor following ocular administration in humans. |
| Protein binding | >99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Intravenous administration in animals suggests Vd ~0.15 L/kg, indicating limited distribution; clinically, it distributes into aqueous humor after topical dosing. |
| Bioavailability | Ocular bioavailability is dependent on formulation; systemic bioavailability after topical ocular administration is extremely low (<1%). |
| Onset of Action | Ocular: Clinical effect onset within 30 minutes after topical administration to the eye. |
| Duration of Action | Duration of action is approximately 4 to 6 hours for ocular inflammation and pain relief following a single dose. |
| Molecular Weight | 255.27 |
1 drop in the affected eye 4 times daily.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No adjustment required. Drug is minimally systemically absorbed. |
| Liver impairment | No adjustment required. Drug is minimally systemically absorbed. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established. |
| Geriatric use | No specific dosage adjustment is recommended; use same dose as younger adults. |
| 1st trimester | No adequate and well-controlled studies in pregnant women. Animal studies have shown adverse effects on fetal development at clinically relevant doses. Use only if potential benefit justifies potential risk to the fetus. |
| 2nd trimester | Same as T1. Nonsteroidal anti-inflammatory drugs (NSAIDs) may cause premature closure of the ductus arteriosus in the third trimester; consider this when using in the second trimester if near term. |
| 3rd trimester | Avoid in third trimester due to risk of premature closure of the fetal ductus arteriosus and oligohydramnios. NSAIDs are contraindicated. |
Clinical note
Comprehensive clinical and safety monograph for ACUVAIL (ACUVAIL).
| Placental transfer | Ketorolac has been shown to cross the placenta in animal studies. In humans, due to low systemic absorption from ophthalmic administration, placental transfer is expected to be low, but no specific human data are available. |
| Breastfeeding |
■ FDA Black Box Warning
No black box warning for ophthalmic use; however, systemic NSAIDs carry risk of serious cardiovascular and gastrointestinal events. Ophthalmic use rarely associated with corneal adverse events.
| Serious Effects |
Hypersensitivity to ketorolac or any component of the formulationActive bleeding or risk of bleeding, including hemophilia or other bleeding disordersPatients currently on anticoagulants (e.g., warfarin, heparin)Advanced renal disease or patients at risk for renal failure due to volume depletionNursing women (in some guidelines, especially if high doses used systemically; for ophthalmic use, caution advised)
| Precautions | Use with caution in patients with bleeding disorders or those on anticoagulants; may prolong bleeding time. Avoid in patients with known hypersensitivities to NSAIDs or aspirin. Can cause corneal keratopathy; discontinue if corneal epithelial breakdown occurs. |
| Food/Dietary | No specific food interactions; systemic absorption is minimal with ophthalmic use. Avoid concurrent use of other NSAID eye drops due to additive irritation. |
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| It is unknown if ketorolac (the active ingredient) is excreted in human milk after ophthalmic administration. However, systemic absorption is minimal. Caution is advised; consider the developmental and health benefits of breastfeeding along with the mother's clinical need for the drug. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Acuvail (ketorolac tromethamine ophthalmic solution) is classified as FDA Pregnancy Category C. Systemic exposure after ocular administration is minimal; however, NSAIDs may cause premature closure of the ductus arteriosus and oligohydramnios in the third trimester. Use during the first and second trimesters should be limited to cases where potential benefit outweighs risk; avoid during the third trimester due to risk of fetal harm. |
| Fetal Monitoring | Monitor for signs of systemic NSAID effects (e.g., gastrointestinal bleeding, renal impairment) if used frequently. In pregnant patients, monitor amniotic fluid volume and fetal ductus arteriosus if used beyond the first trimester. No specific monitoring is required for single-dose use. |
| Fertility Effects | NSAIDs may impair female fertility via reversible inhibition of ovulation. Ophthalmic ketorolac is unlikely to affect fertility due to minimal systemic absorption, but caution is advised in women attempting conception. |
| Clinical Pearls | Acuvail (ketorolac tromethamine ophthalmic solution 0.45%) is a nonsteroidal anti-inflammatory drug (NSAID) for ocular use. It is preserved with sodium chloride and not benzalkonium chloride, reducing corneal epithelial toxicity. Administer 1 drop twice daily for ocular pain and inflammation following cataract surgery. Use caution in patients with bleeding tendencies or those on anticoagulants due to risk of increased ocular bleeding. Monitor for corneal epithelial defects and keratitis, especially with prolonged use. |
| Patient Advice | Wash hands before each use; do not touch tip of bottle to eye or any surface to avoid contamination. · Remove contact lenses before instillation and wait at least 15 minutes before reinserting. · Contact your doctor if you experience eye pain, redness, vision changes, or if symptoms worsen. · Do not use this medication while wearing contact lenses unless directed by your doctor. · Store at room temperature, keep bottle tightly closed when not in use, and discard within 28 days of opening. |