Trade Names:Acular- Solution 0.5%
Trade Names:Acular LS- Solution 0.4%
Trade Names:Acuvail- Solution 0.45%
Trade Names:Ketorolac Tromethamine- Tablets 10 mg- Injection 15 mg/mL- Injection 30 mg/mLApo-Ketorolac (Canada)Apo-Ketorolac Ophthalmic Solution (Canada)ratio-Ketorolac (Canada)Toradol (Canada)Toradol IM (Canada)
Decreases inflammation, pain, and fever through inhibition of prostaglandin synthesis.
Bioavailability is 100%. T max is approximately 44 min for oral single dose (10 mg), 33 min for IM, and 1.1 min for IV (15 mg). C max is approximately 0.87 mcg/mL for oral single dose (10 mg), 1.14 mcg/mL for IM, and 2.47 mcg/mL for IV (15 mg).
Ketorolac is 99% protein bound. Nevertheless, plasma concentrations as high as 10 mcg/mL will only occupy approximately 5% of the albumin binding sites. A decrease in serum albumin will lead to an increase in free drug concentrations. Vd is approximately 13 L.
Largely metabolized in the liver via hydroxylation and conjugation. Ketorolac is a racemic mixture of S- and R-enantiometric forms, with the S form having analgesic activity.
S-enantiomer is cleared 2 times faster than R-enantiomer. The t 1/ 2 of S-enantiomer is approximately 2.5 h and the half-life of R-enantiomer is approximately 5 h. 92% of dose excreted in the urine; 6% excreted in feces.
30 min for injection (IM).
2 to 3 h for injection (IM, PO).
4 to 6 h (IV, IM).
Ketorolac is contraindicated in patients with advanced renal impairment and in patients at risk for renal failure because of volume depletion. Adjust dose for patients with moderately elevated serum creatinine.Elderly
Adjust dosage for patients 65 yr of age and older.Patients weighing less than 50 kg
Short-term management of moderately severe, acute pain.IM, IV Children 2 yr of age and older
Moderately severe, acute pain.Ophthalmic forms Adults and children 3 yr of age and older Acular
Temporary relief of ocular itching caused by seasonal allergic conjunctivitis and treatment of postoperative inflammation in patients who have undergone cataract extraction.Acular LS
Reduction of ocular pain and burning/stinging following corneal refractive surgery.Adults Acuvail
Treatment of pain and inflammation following cataract surgery.
Patients in whom ketorolac, aspirin, or any NSAID have caused hypersensitivity or allergic-type or reactions; active peptic ulcer disease; recent GI bleeding or perforation; advanced renal impairment and in patients at risk for renal failure because of volume depletion; suspected or confirmed cerebrovascular bleeding; hemorrhagic diathesis, incomplete hemostasis, and those at high risk of bleeding; history of peptic ulcer disease or GI bleeding; as prophylactic analgesia before any major surgery and intraoperatively when hemostasis is critical; for intrathecal or epidural administration; labor and delivery; lactation; concomitant use with aspirin or other NSAIDs; concomitant use with probenecid.
IM Younger than 65 yr of age: 30 mg every 6 h. Do not exceed 120 mg/day. Older than 65 yr of age, renal impairment, or weight less than 50 kg (110 lbs): 15 mg every 6 h. Do not exceed 60 mg/day.Single DoseAdults
IM , IV Younger than 65 yr of age: 60 mg. Older than 65 yr of age, renal impairment, or weight less than 50 kg (110 lbs): 30 mg. IV Younger than 65 yr of age: 30 mg. Older than 65 yr of age, renal impairment, or weight less than 50 kg (110 lbs): 15 mg.Children 2 to 16 yr of age
IM 1 mg/kg up to 30 mg max. IV 0.5 mg/kg up to 15 mg max.Transition from IV or IM to OralAdults
Younger than 65 yr of age: 20 mg as a first oral dose for patients who received 60 mg IM single dose, 30 mg IV single dose, or 30 mg multiple dose IV/IM, followed by 10 mg every 4 to 6 h, not to exceed 40 mg per 24 h. Older than 65 yr of age, renal impairment, or weight less than 50 kg (110 lbs): 10 mg as a first oral dose for patients who received a 30 mg IM single dose, 15 mg IV single dose, or 15 mg multiple dose IV/IM, followed by 10 mg every 4 to 6 h, not to exceed 40 mg per 24 h.OphthalmicAdults and children 3 yr of age and older
Acular : 1 drop (0.25 mg) 4 times daily for relief of ocular itching caused by seasonal allergic conjunctivitis. For patients undergoing cataract extraction, 1 drop to affected eye(s) 4 times daily beginning 24 h after cataract surgery and continuing through the first 2 wk of the postoperative period. Acular LS : 1 drop 4 times daily in operated eye as needed for pain and burning/stinging for up to 4 days following corneal refractive surgery.Adults Acuvail
1 drop to affected eye twice daily beginning 1 day prior to cataract surgery, continued on the day of surgery and through the first 2 weeks of the post-operative period.
Store at 59° to 86°F. Protect from light.
Serum aminoglycoside levels may be increased.Anticoagulants
May increase risk of gastric erosion and bleeding.Aspirin, NSAIDs
Risk of inducing serious NSAID-related side effects. Concomitant use is contraindicated.Furosemide
IM/IV may reduce the diuretic response about 20%.Lithium
Serum lithium levels may be increased.Methotrexate
May increase methotrexate levels.Probenecid
May increase ketorolac plasma levels. Concomitant use is contraindicated.SSRIs (fluoxetine, paroxetine)
Risk of GI adverse reactions may be increased.
Drug may prolong bleeding time.
Edema (4%); hypertension (greater than 1%); flushing, hypotension (postmarketing).
Headache (17%); dizziness (7%); drowsiness (6%); sweating (greater than 1%); aseptic meningitis, convulsions, psychosis (postmarketing).
Pruritus, rash (greater than 1%); exfoliative dermatitis, Lyell syndrome, maculopapular rash, Stevens-Johnson syndrome, urticaria (postmarketing).
Stomatitis (greater than 1%).Ophthalmic
Burning/stinging (40%); corneal edema, iritis, ocular inflammation/irritation, superficial keratitis, superficial ocular infections (1% to 10%); conjunctival hyperemia and/or hemorrhage, increased intraocular pressure, ocular pain, tearing/vision blurred (1% to 6%); corneal erosion, corneal perforation, corneal thinning, epithelial breakdown (postmarketing).
GI pain (13%); dyspepsia, nausea (12%); diarrhea (7%); constipation, flatulence, GI fullness, vomiting (greater than 1%); acute pancreatitis, esophagitis; GI hemorrhage/perforation, hematemesis, melena, peptic ulceration (postmarketing).
Acute renal failure, hemolytic uremic syndrome, interstitial nephritis (postmarketing).
Leukopenia, postoperative wound hemorrhage, thrombocytopenia (postmarketing).
Abnormal LFTs, cholestatic jaundice, hepatitis, liver failure (postmarketing).
Hyperkalemia, hyponatremia (postmarketing).
Asthma, bronchospasm (postmarketing).
Injection site pain, purpura (greater than 1%); anaphylaxis/anaphylactoid reaction, angioedema, flank pain, laryngeal edema, myalgia, tongue edema (postmarketing).Ophthalmic
Allergic reactions (1% to 10%).
Limit therapy to 5 days. Oral therapy is indicated only as continuation therapy to IV/IM, and the combined use is not to exceed 5 days because of the increased risk of serious adverse reactions.GI effects
Peptic ulcers, GI bleeding, and/or perforation can occur. Contraindicated in patients with active or history of these states.Renal effects
Contraindicated in patients with advanced renal impairment or at risk of renal failure caused by volume depletion.
Bleeding risk is caused by platelet inhibition. Contraindicated as preoperative analgesic or as intra-operative analgesic when hemostasis is critical or in patients at high risk of bleeding. Intrathecal/epidural administration is contraindicated because of alcohol content.
Category C . Avoid use in late pregnancy because it may cause premature closure of the ductus arteriosus.
Excreted in breast milk. Contraindicated.
Safety and efficacy not established in patients younger than 2 yr of age.Ophthalmic
Safety and efficacy not established in patients younger than 3 yr of age ( Acular and Acular LS ). Safety and efficacy not established ( Acuvail ).
Increased risk of adverse reactions.
Hypersensitivity may occur; use drug with caution in aspirin-sensitive individuals because of possible cross-sensitivity.
Assess function before and during therapy because NSAID metabolites are eliminated renally. Dosage adjustments may be necessary.
May lead to liver enzyme elevations.
May occur without known hypersensitivity to aspirin, ketorolac, or other NSAIDs, or in patients with a history of angioedema, bronchospastic activity, and nasal polyps.
Fluid retention and edema have been reported with ketorolac. Use cautiously in patients with cardiac decompensation, hypertension, or other similar conditions.
Not intended for long-term use. Limit to short-term therapy (no longer than 5 days).
All topical NSAIDs and corticosteroids may slow or delay healing. Thus, concomitant use of ketorolac and corticosteroids may increase the risk of healing problems.
Use cautiously in patients with coagulation disorders.
Use of topical NSAIDs may result in keratitis. Continued use may result in epithelial breakdown, corneal thinning, corneal erosion, corneal ulceration, or corneal perforation. These reaction may be sight-threatening. Patients with complicated ocular surgeries, corneal denervation, corneal epithelial defects, diabetes mellitus, ocular surface diseases, rheumatoid arthritis, or repeat ocular surgeries within a short period of time may be at increased risk for corneal adverse reactions. Topical use of NSAIDs more than 24 h prior to surgery or for use beyond 14 days postsurgery may increase risk for occurrence and severity of corneal adverse reaction.
Abdominal pain, anaphylactoid reaction, drowsiness, lethargy, vomiting, nausea, renal dysfunction, erosive gastritis, hyperventilation, peptic ulcers, GI bleeding (hypertension, acute renal failure, respiratory depression, coma [rare]).
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