Ketorolac information from DrugsUpdate
P - Contraindicated in pregnancy
L - Contraindicated in lactation
Ketorolac or ketorolac tromethamine (marketed under the trademarks Toradol and Acular in the US, where generics have also been approved, and various other brand names around the world) is a non-steroidal anti-inflammatory drug (NSAID) in the family of heterocyclic acetic acid derivatives, often used as an analgesic, antipyretic (fever reducer), and anti-inflammatory. Ketorolac acts by inhibiting the bodily synthesis of prostaglandins. Ketorolac in its oral (tablet or capsule) and intramuscular (injected) preparations is a racemic mixture of both (S)-(−)-ketorolac, the active isomer, and (R)-(+)-ketorolac. An ophthalmic (i.e., eye-drop) solution of ketorolac is available and is used to treat eye pain and to relieve the itchiness and burning of seasonal allergies.
Pharmacodynamics
Ketorolac tromethamine is a non-steroidal anti-inflammatory drug (NSAID) that exhibits analgesic activity in animal models. The mechanism of action of Ketorolac, like that of other NSAIDs, is not completely understood but may be related to prostaglandin synthetase inhibition. The biological activity of Ketorolac tromethamine is associated with the S-form. Ketorolac tromethamine possesses no sedative or anxiolytic properties.
The peak analgesic effect of Ketorolac tromethamine occurs within 2 to 3 hours and is not statistically significantly different over the recommended dosage range of Ketorolac tromethamine. The greatest difference between large and small doses of Ketorolac tromethamine is in the duration of analgesia.
Pharmacokinetics
Ketorolac inhibits prostaglandin synthesis by decreasing the activity of the cyclooxygenase enzyme.
Onset
30-60 minutes (oral); 10 minutes (IM).
Duration
6-8 hours (oral/IM).
Absorption
Well absorbed (oral/IM); peak plasma concentrations after 30-60 minutes.
Distribution
Protein-binding: 99%. Crosses the placenta; enters breast milk; poorly penetrates into CSF.
Metabolism
Hepatic via glucuronic acid conjugation.
Excretion
Via urine (90%, as unchanged drug and metabolites); via faeces (remaining dose). Terminal elimination half-life: 4-6 hours; 6-7 hours (elderly); 9-10 hours (renal impairment).
Ketorolac Indications / Ketorolac Uses
Information Not Available
Ketorolac Adverse Reactions / Ketorolac Side Effects
GI ulcer, bleeding and perforation, drowsiness, rash, bronchospasm, hypotension, psychosis, dry mouth, fever, bradycardia, chest pain, dizziness, headache, sweating, oedema, pallor, liver function changes. Transient stinging and local irritation (ophthalmic).
Potentially Fatal: Anaphylaxis. Severe skin reactions. MI, stroke, GI bleeding.
Precautions
Ketorolac tromethamine cannot be expected to substitute for corticosteroids or to treat corticosteroid insufficiency. Abrupt discontinuation of corticosteroids may lead to disease exacerbation. Patients on prolonged corticosteroid therapy should have their therapy tapered slowly if a decision is made to discontinue corticosteroids.
The pharmacological activity of Ketorolac tromethamine in reducing inflammation may diminish the utility of this diagnostic sign in detecting complications of presumed noninfectious, painful conditions.
Overdosage
Symptoms: Abdominal pain, nausea, vomiting, hyperventilation, peptic ulceration, erosive gastritis and renal dysfunction. Management: Supportive and symptomatic.
Special Precautions
Elderly, patients weighing <50 kg, hepatic dysfunction, heart failure, predisposition to reduced blood volume or renal blood flow. Mild renal impairment; monitor renal function closely.
Other Drug Interactions
May reduce effects of antihypertensives (e.g. ACE inhibitors or angiotensin II receptor antagonists). Increased risk of renal toxicity with ACE inhibitors, diuretics. Increased adverse effects with aspirin or other NSAIDs. Hallucinations may occur when used with fluoxetine, thiothixene, alprazolam.
Potentially Fatal: Increased risk of GI bleeding with warfarin. May increase toxicity of methotrexate and lithium. Increased plasma concentrations with probenecid.
Other Interactions
Information Not Available
Dosage
Oral
Moderate to severe pain
Adult: 10 mg every 4-6 hours. Max: 40 mg/day. Max duration: 7 days.
Elderly: 10 mg every 6-8 hours. Max duration: 7 days.
Renal impairment: Contraindicated in moderate to severe impairment.
Parenteral
Moderate to severe pain
Adult: 60 mg as a single dose via IM injection or 30 mg as a single IV dose. Alternatively, 30 mg every 6 hours via IM or IV admin up to a max of 120 mg daily. Halve the doses in patients weighing <50 kg. Max duration: 2 days; patient should be transferred to oral therapy as soon as possible.
Elderly: 30 mg as a single dose via IM inj or 15 mg as a single IV dose. Alternatively, 15 mg every 6 hours via IM or IV admin up to a max of 60 mg daily.
Renal impairment: 30 mg as a single dose via IM injection or 15 mg as a single IV dose. Alternatively, 15 mg every 6 hours via IM or IV admin up to a max of 60 mg daily. Contraindicated in moderate to severe impairment.
Ophthalmic
Ocular itching associated with seasonal allergic conjunctivitis
Adult: As trometamol: Instil 1 drop of a 0.5% solution into the affected eye(s) 4 times daily.
Renal impairment: Contraindicated in moderate to severe impairment.
Ophthalmic
Prophylaxis and reduction of postoperative ocular inflammation
Adult: As trometamol: Instil 1 drop of a 0.5% solution into the appropriate eye(s) 4 times daily starting 24 hours after surgery. Continue for 2 weeks
Renal impairment: Contraindicated in moderate to severe impairment.
Ophthalmic
Cystoid macular oedema
Adult: As trometamol: Instil 1-2 drops of a 0.5% solution into the appropriate eye(s) every 6-8 hours starting 24 hours before surgery and continue for 3-4 weeks after surgery.
Renal impairment: Contraindicated in moderate to severe impairment.
Ophthalmic
Pain and photophobia after incisional refractive surgery
Adult: As trometamol: Instil 1 drop of a 0.5% solution 4 times daily into the operated eye for up to 3 days after surgery.
Renal impairment: Contraindicated in moderate to severe impairment.
Incompatibility
Y-site incompatibility: Fenoldopam, azithromycin. Syringe incompatibility: Promethazine, hydroxyzine, nalbuphine, haloperidol, prochorperazine edisylate, triethylperazine. Admixture incompatibility: Promethazine, morphine, hydroxyzine, meperidine.
Food(before/after)
Information Not Available
List of Contraindications
Ketorolac and Pregnancy
Contraindicated in pregnancy
Ketorolac and Lactation
Contraindicated in lactation
Ketorolac and Children
Ketorolac tromethamine tablets are not indicated for use in pediatric patients. The safety and effectiveness of Ketorolac tromethamine tablets in pediatric patients below the age of 17 have not been established.
Ketorolac and Geriatic
Because Ketorolac tromethamine may be cleared more slowly by the elderly who are also more sensitive to the dose related adverse effects of NSAIDs, extreme caution, reduced dosage and careful clinical monitoring must be used when treating the elderly with Ketorolac tromethamine.
Ketorolac and Other Contraindications
Hypersensitivity to aspirin or other NSAIDs, asthma. Hypovolaemia or dehydration. Do not give postoperatively to patients with high risk of haemorrhage. History of peptic ulcer or coagulation disorders. Nasal polyps, angioedema, bronchospasm. Labour. Moderate to severe renal impairment. GI bleeding, cerebrovascular bleeding. As prophylactic analgesic before surgery. Pregnancy, lactation.
Storage
Ophthalmic
Store at 15-25°C (59-77°F).
Oral
Store at 15-30°C (59-86°F).
Parenteral
Store at 15-30°C (59-86°F). Protect from light.
Lab interference
Ophthalmic
Store at 15-25°C (59-77°F).
Oral
Store at 15-30°C (59-86°F).
Parenteral
Store at 15-30°C (59-86°F). Protect from light.
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