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Ketorolac (Toradol)


  • Generic name: Ketorolac Tromethamine
  • Trade names: Toradol, Acular, Sprix (Intranasal)
  • Pharmacologic category: Nonsteroidal Anti-inflammatory Drug
  • FDA approved: December 20, 1991
  • Habit forming? No
  • Pregnancy risk factor: C
Medical uses

Ketorolac is a quite potent non-steroidal anti-inflammatory drug which is licensed for short term use in the management of moderate to severe postoperative pain. It is one of the newest NSAIDs.

Ketorolac analgesic potency resembles that of the centrally acting analgesics, with 15 to 30 mg of ketorolac producing analgesia equivalent to a 12-mg dose of morphine. It is an accepted alternative to narcotic analgesics.

Pharmacological characteristics
  • Onset of action: Intramuscular ~10 minutes, maximum effect within 2 hours.
    Oral ~30-60 minutes. Peak analgesia after Intramuscular injection lags behind peak plasma levels by 45 to 90 minutes.
  • Duration of action: 6-8 hours
  • Metabolism: Hepatic
  • Elimination half-life: 2-6 hours; prolonged 30% to 50% in elderly; up to 19 hours in renal impairment
  • Excretion: Urine (92%, 61% as unchanged drug)
Benefits
  • Injectable formulation. Available in injectable form which can be used in situations where oral NSAIDs are excluded (eg. acute post-operative pain).
  • Less nausea and sedation than narcotic analgesics.
Risks & Disadvantages
  • Expensive. One of the most expensive NSAIDs.
  • Weak anti-inflammatory action. In comparison to the other NSAIDs, ketorolac has poor anti-inflammatory activity.
  • Severe gastrointestinal complications. Ketorolac is reported to have the highest rate of serious gastrointestinal complications of all non-steroidal anti-inflammatory drugs. Ketorolac can cause peptic ulcers, gastrointestinal bleeding and perforation of the stomach or intestines, which can be fatal. Results of a case control study2 comparing the GI toxicity of different NSAIDs suggest that ketorolac was approximately five times more likely to cause upper GI bleeding than other NSAIDs.
  • Ketorolac may cause kidney failure.
Unlabeled uses
  • Severe migraine headache
  • Pain after surgery in children
Mode of action

Ketorolac is a pyrrolizine carboxylic acid derivative. It has analgesic, antipyretic and anti-inflammatory activity. The primary mechanism of action is the inhibition of prostaglandin synthesis by competitive blocking of the enzyme cyclooxygenase (COX).

References
  • 1. U.S. FDA. Ketorolac (Toradol) Prescribing Information.
  • 2. Garcia Rodriguez LA, Cattaruzzi C, Troncon M, Agostinis L. Risk of hospitalization for upper gastrointestinal tract bleeding associated with ketorolac, other anti-inflammatory drugs, calcium antagonists, and other antihypertensive drugs. Arch Intern Med. 1998;158(1):33-9.

Last modified: October, 2013

Toradol

toradol

  • Initially ketorolac was introduced in 1990 as a peripheral analgesic for short-term use and for the relief of ocular itching caused by seasonal allergic conjunctivitis.
  • Ketorolac is a potent analgesic, and its use carries many risks.

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