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.
NSAIDs are not recommended for use with other NSAIDs because of the potential for additive side effects.
The protein-binding effect of most non-aspirin NSAIDs is inhibited by the presence of aspirin in the blood.
As with other NSAIDs, the mechanism of the drug is associated with the chiral S form. Conversion of the R enantiomer into the S enantiomer has been shown to occur in the metabolism of ibuprofen; it is unknown whether it occurs in the metabolism of ketorolac.
|Ketorolac adverse effects|
|General||Edema. Less frequently, hypersensitivity reactions (such as anaphylaxis, bronchospasm, laryngeal edema, tongue edema, hypotension), flushing, weight gain, or fever. Very infrequently, asthenia.|
|Cardiovascular||Hypertension. Less frequently, palpitation, pallor, or fainting (syncope).|
|Dermatologic||Rash or pruritus. Less frequently, Lyell's syndrome, Stevens-Johnson syndrome, musculo-papular rash, exfoliative dermatitis, or urticaria.|
|Gastrointestinal||Nausea, dyspepsia, gastrointestinal pain, constipation, diarrhea, flatulence, gastrointestinal fullness, vomiting or stomatitis. Less frequently, peptic ulceration, gastrointestinal hemorrhage, gastrointestinal perforation, melena, rectal bleeding, gastritis, eructation, anorexia, or increased appetite. Very infrequently, pancreatitis.|
|Hemic and lymphatic||Purpura. Less frequently, postoperative wound hemorrhage, thrombocytopenia, epistaxis, or anemia. Very infrequently, leukopenia or eosinophilia.|
|Neurological||Drowsiness, dizziness, headache, sweating, injection site pain. Less frequently convulsions, vertigo, tremors, abnormal dreams, hallucinations, or euphoria. Very infrequently, paresthesia, depression, insomnia, inability to concentrate, nervousness, excessive thirst, dry mouth, abnormal thinking, hyperkinesis, or stupor.|
|Respiratory||Less frequently, dyspnea, asthma and pulmonary edema. Very infrequently, rhinitis or cough.|
|Urogenital||Less frequently, acute renal failure. Very infrequently polyuria or increased urinary frequency.|
It should be noted that when administered intravenously through the same IV catheter as morphine, the two drugs have been known to sometimes combine to form a precipitate in the IV, which may block the line. Line flushing with a syringe of saline solution can push the blockage through.
Ketorolac is not recommended for long-term chronic pain patients.
However, ketorolac has been co-administered with meperidine and morphine without apparent adverse effects on patients.
Injected dosages are 15, 30 and 60 mg; US price for 10 vials of 30 mg each is around US$45, making the Intramuscular preparation considerably more expensive per dose. One 60-mg dose would require the administration by injection of two vials, at about $9 per dose. Australian pricing for 5 vials is around AU$58, or about $23 per dose. Ketorolac is not available on the Pharmaceutical Benefits Scheme.
In the United States, United Kingdom, Canada, and Australia this drug cannot be sold over-the-counter and must be administered only with a prescription. It is commonly available over-the-counter in Mexico and other areas of Latin America, at the pharmacist's discretion.
Apotex, a Canadian manufacturer, offers generic Ketorolac tromethamine 0.5% ophthalmic solution under the name "Apo-Ketorolac" in Canada and some other countries. Syntex and Allergan sued Apotex for patent infringement of US Patent No. 5,110,493, over the generic ketorolac tomethamine product. In May, 2005, the United States Court of Appeals for the Federal Circuit handed Apotex a victory, ruling that a lower court upholding the Syntex patent misapplied the rules for judging whether an invention was obvious. Allergan had claimed that the patent is valid until 2009.