Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
ACULAR LS vs SUMATRIPTAN
Clinician-reviewed, head-to-head comparison of mechanism, dosing, pharmacokinetics, and safety profiles.
Last clinically reviewed: July 2026 · OpiCalc Medical Review Team
Selective COX-2 inhibitor; inhibits prostaglandin synthesis, reducing ocular inflammation and pain.
Selective 5-HT1B/1D receptor agonist; causes vasoconstriction of cranial arteries and inhibits trigeminal nerve transmission.
FDA: Treatment of postoperative inflammation in patients who have undergone cataract surgery,Off-label: Relief of ocular pain, photophobia, and inflammation associated with corneal abrasion or refractive surgery
Acute treatment of migraine with or without aura,Acute treatment of cluster headache episodes
1 drop in the affected eye(s) four times daily
Sumatriptan is available as oral tablets (25 mg, 50 mg, 100 mg), subcutaneous injection (6 mg/0.5 m L), and nasal spray (5 mg, 20 mg). For acute migraine: oral: 50-100 mg at onset, may repeat after 2 hours (max 200 mg/day). Subcutaneous: 6 mg at onset, may repeat after 1 hour (max 12 mg/24h). Nasal spray: 20 mg in one nostril at onset, may repeat after 2 hours (max 40 mg/day).
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.
2.5 hours (range 1–4 h); clinically relevant for redosing interval of ≥2 h.
Primarily hepatic via CYP2C9; undergoes glucuronidation and oxidation to inactive metabolites.
Primarily via monoamine oxidase A (MAO-A); minor via cytochrome P450 (CYP) enzymes.
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.
60% renal (as indole acetic acid metabolite), 40% fecal; <3% unchanged in urine.
Ketorolac is highly protein bound, approximately 99% bound to plasma proteins, primarily albumin.
14–21%, primarily to albumin and alpha-1-acid glycoprotein.
The volume of distribution is approximately 0.12 L/kg, indicating distribution primarily into extracellular fluid with limited tissue penetration.
2.0–3.3 L/kg; indicates extensive tissue distribution.
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.
Oral: 15% (due to first-pass metabolism); subcutaneous: 97%; intranasal: 17% (with variability).
No dosage adjustment required for renal impairment
No specific dose adjustment is recommended for renal impairment. However, sumatriptan and its metabolites are excreted renally, and caution is advised in severe renal impairment (Cr Cl <15 m L/min). No specific GFR-based guidelines are established.
No dosage adjustment required for hepatic impairment but use with caution in severe hepatic disease due to potential for increased systemic exposure
Contraindicated in severe hepatic impairment (Child-Pugh C). For mild to moderate hepatic impairment (Child-Pugh A or B): oral maximum dose is 50 mg; nasal spray: 5 mg single dose; subcutaneous: no specific adjustment, but caution advised due to reduced clearance.
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
Not approved for pediatric use <18 years. However, off-label: adolescent (12-17 years): oral 25-100 mg at onset, may repeat after 2 hours (max 200 mg/day). Subcutaneous: 3-6 mg at onset (based on weight, e.g., 0.06 mg/kg). Nasal spray: 5-20 mg at onset.
No specific dose adjustment recommended; use with caution due to increased incidence of age-related ocular conditions
Limited data in elderly. Start with the lowest effective dose (e.g., oral 25 mg, subcutaneous 3 mg, nasal spray 5 mg). Caution due to potential for cardiovascular risk, hypertension, and reduced hepatic/renal function. Avoid in patients with uncontrolled hypertension or ischemic heart disease.
None
Not recommended for use in patients with risk factors for coronary artery disease (e.g., hypertension, diabetes, smoking) unless a cardiovascular evaluation confirms absence of coronary artery disease.
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
Risk of myocardial ischemia, infarction, and Prinzmetal's angina,Life-threatening serotonin syndrome with concomitant serotonergic drugs,Elevations in blood pressure,Increased risk of cerebrovascular events,Overuse headache with frequent use
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
Ischemic heart disease,History of myocardial infarction,Uncontrolled hypertension,Hemiplegic or basilar migraine,Concomitant use of MAO-A inhibitors or within 2 weeks of discontinuation,Severe hepatic impairment,Hypersensitivity to sumatriptan
No known food interactions for ophthalmic ketorolac. However, maintain good hydration and nutrition to support corneal healing.
No significant food interactions. Avoid alcohol during migraine attacks as it can worsen headaches. May be taken with or without food.
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 Pregnancy Category C. In first trimester, no increased risk of major congenital malformations from available data; however, animal studies show embryo lethality and increased malformations at high doses. Second and third trimester risks include potential for uterine hypertonus and fetal hypoxia during maternal use for migraine attacks; avoid during third trimester due to risk of premature uterine contractions.
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.
Sumatriptan is excreted into human breast milk with a relative infant dose of 3.5% of maternal weight-adjusted dose (M/P ratio approximately 0.6-4.3). Clinical studies show no adverse effects in breastfed infants; however, wait at least 12 hours after injection or 24 hours after oral dose to breastfeed to minimize exposure.
No dosing adjustments are necessary for ophthalmic use during pregnancy due to negligible systemic absorption. Standard dosing (1 drop in the affected eye(s) four times daily) is recommended. Systemic NSAIDs may require dose adjustment due to increased volume of distribution and renal changes, but this does not apply to topical ocular ketorolac.
No specific dose adjustments required for pregnancy based on pharmacokinetic changes; however, lower starting doses may be considered due to increased sensitivity to vascular effects. Avoid use in preeclampsia or uncontrolled hypertension.
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.
Sumatriptan is a 5-HT1B/1D receptor agonist used for acute migraine. It is available in oral, nasal, subcutaneous, and rectal formulations. Onset of action is fastest with subcutaneous injection (10-15 minutes). Avoid use within 24 hours of other triptans or ergot alkaloids. Contraindicated in patients with ischemic heart disease, cerebrovascular disease, uncontrolled hypertension, or hemiplegic/basilar migraine. Monitor for serotonin syndrome when combined with SSRIs/SNRIs.
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.
Take sumatriptan at the first sign of migraine headache for best results.,Do not exceed the recommended dose: maximum 100 mg orally or 20 mg intranasally per single dose, with a maximum of 200 mg daily for oral formulations.,Seek emergency medical attention if you experience chest pain, shortness of breath, irregular heartbeat, or signs of stroke.,Avoid driving or operating machinery until you know how sumatriptan affects you, as it may cause dizziness or drowsiness.,Inform your doctor if you have heart disease, high blood pressure, or are pregnant or breastfeeding.
No interactions on record
"Concurrent use of sumatriptan, a serotonin 5-HT1B/1D receptor agonist, and rasagiline, a selective monoamine oxidase B (MAO-B) inhibitor, can lead to serotonin syndrome due to excessive serotonergic activity in the central nervous system. Rasagiline inhibits the metabolism of serotonin, while sumatriptan indirectly increases serotonin release; their combination may result in life-threatening neuromuscular excitation, autonomic instability, and altered mental status. Symptoms may include hyperthermia, rigidity, myoclonus, and rapid fluctuations in vital signs, requiring immediate medical intervention."
"Sumatriptan, a 5-HT1B/1D receptor agonist used for migraine, and sulpiride, a dopamine D2 receptor antagonist with atypical antipsychotic properties, may exhibit additive or synergistic effects on the central nervous system. This combination can potentially increase the risk of serotonin syndrome (due to sumatriptan's serotonergic activity) and may also lead to enhanced extrapyramidal symptoms or neuroleptic malignant syndrome via combined dopaminergic antagonism. Clinical outcomes may include hyperthermia, rigidity, altered mental status, and autonomic instability."
"The combination of sumatriptan (a 5-HT1B/1D receptor agonist) and paroxetine (a selective serotonin reuptake inhibitor) increases the risk of serotonin syndrome, a potentially life-threatening condition characterized by neuromuscular excitation, autonomic instability, and altered mental status. This interaction is due to additive serotonergic effects, as both drugs enhance serotonin activity in the central nervous system. Clinical outcomes range from mild symptoms (tremor, hyperreflexia, diaphoresis) to severe manifestations (hyperthermia, rigidity, seizures) and require immediate medical attention."
Explore head-to-head clinical comparisons of other medications in the same therapeutic classes.
Common clinical questions about ACULAR LS vs SUMATRIPTAN, answered by our medical review team.
ACULAR LS is a NSAID Ophthalmic that works by Selective COX-2 inhibitor; inhibits prostaglandin synthesis, reducing ocular inflammation and pain.. SUMATRIPTAN is a 5-HT1 Agonist that works by Selective 5-HT1B/1D receptor agonist; causes vasoconstriction of cranial arteries and inhibits trigeminal nerve transmission.. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between ACULAR LS and SUMATRIPTAN depend on the specific clinical indication. These are agents from distinct pharmacological classes and are not directly interchangeable by dose. A physician or clinical pharmacist should guide any therapeutic switching decisions.
The standard adult dose of ACULAR LS is: 1 drop in the affected eye(s) four times daily. The standard adult dose of SUMATRIPTAN is: Sumatriptan is available as oral tablets (25 mg, 50 mg, 100 mg), subcutaneous injection (6 mg/0.5 m L), and nasal spray (5 mg, 20 mg). For acute migraine: oral: 50-100 mg at onset, may repeat after 2 hours (max 200 mg/day). Subcutaneous: 6 mg at onset, may repeat after 1 hour (max 12 mg/24h). Nasal spray: 20 mg in one nostril at onset, may repeat after 2 hours (max 40 mg/day).. Dosing should always be individualized based on indication, renal and hepatic function, age, and other patient factors.
No direct drug-drug interaction has been formally documented between ACULAR LS and SUMATRIPTAN in current clinical databases. However, individual patient risk factors including other medications, organ function, and comorbidities should always be evaluated by a qualified healthcare provider.
The maternal-fetal safety profiles differ. ACULAR LS is classified as Category C. Ketorolac tromethamine, the active ingredient in ACULAR LS, is a nonsteroidal anti-inflammatory drug (NSAID). In animal reproduction studies, administration of ketorolac during org. SUMATRIPTAN is classified as Category D/X. FDA Pregnancy Category C. In first trimester, no increased risk of major congenital malformations from available data; however, animal studies show embryo lethality and increased m. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.