A pyrrolo-pyrrole non-steroidal anti-inflammatory agent with antipyretic and analgesic properties; similar in actions to ibuprofen but substantially more potent and capable of relieving severe pain. Often used by injection.
(05 Mar 2000)
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Ketorolac
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| Systematic (IUPAC) name | |
| (±)-5-benzoyl-2,3-dihydro- 1H-pyrrolizine-1-carboxylic acid, 2-amino-2-(hydroxymethyl)-1,3-propanediol |
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| Identifiers | |
| CAS number | |
| ATC code | M01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C15H13NO3 |
| Mol. mass | 376.4 g/mol |
| Pharmacokinetic data | |
| Bioavailability |
100% (All routes) |
| Metabolism | Hepatic |
| Half life | 3.5-9.2 hrs, young adults; 4.7-8.6 hrs, elderly (mean age 72) |
| Excretion | Renal Biliary:6.1% (mean) |
| Therapeutic considerations | |
| Pregnancy cat. |
C(AU) C(US) |
| Legal status |
℞ Prescription only |
| Routes | oral, I.M., I.V. |
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
Ketorolac, like other 2-arylpropionate derivatives (including Ketoprofen
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
The primary mechanism of action responsible for ketorolac's anti-inflammatory, antipyretic and analgesic effects is the inhibition of prostaglandin synthesis by competitive blocking of the enzyme cyclooxygenase (COX). Like most NSAIDs, ketorolac is a non-selective COX inhibitor.
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 is indicated for short-term management of pain (up to five days maximum).
Ketorolac is contraindicated in patients with a previously demonstrated hypersensitivity to ketorolac, and in patients with the complete or partial syndrome of nasal polyps, angioEdema
Similar to other NSAIDs. See inset "Ketorolac adverse effects."
| Ketorolac adverse effects | |
|---|---|
| Body system | Effects |
| General | Edema. Less frequently, hypersensitivity reactions (such as anaphylaxis, bronchospasm, laryngeal edema, tongue edema, hypotension), flushing, weight gain, or fever. Very infrequently, asthenia. |
| Cardio |
Hypertension |
| Dermatologic | Rash or pruritus. Less frequently, Lyell's syndrome, Stevens-Johnson syndrome |
| Gastrointestinal | Nausea |
| Hemic and lymphatic | Purpura |
| Neuro |
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. |
The most serious risks associated with ketorolac are, as with other NSAIDs, gastrointestinal ulcers, bleeding and perforation; renal (kidney) events ranging from interstitial nephritis to complete kidney failure; hemorrhage, and hypersensitivity reactions.
As with other NSAIDs, fluid and solute retention and edema have been reported with ketorolac. Ketorolac also elevates liver protein levels.
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 pre-operative analgesia or co-administration with anesthesia because it inhibits platelet aggregation and thus may be associated with an increased risk of bleeding.
Ketorolac is not recommended for obstetric analgesia because it has not been adequately tested for obstetrical administration and has demonstrable fetal toxicity in laboratory animals.
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.
Oral dosage is 10 mg; United States price for 20 tablets hovers around US$28. Australian pricing for 20 tablets is around AU$44.[1] It is considerably less expensive in Mexico (where it is called ketorolaco, and marketed under various brand names, such as Glicima, from Atlantis Pharma, and Supradol, from Laboratorios Liamont), costing approximately US$10 for 20 tablets.
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[1], or about $23 per dose. Ketorolac is not available on the Pharmaceutical Benefits Scheme.[2]
In the United States,[3] United Kingdom,[4] Canada,[5] and Australia[6] 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.
The Syntex company, of Palo Alto, California developed the ophthalmic solution Acular, and holds the registered trademark on that name, as well as on the Toradol. The actual product using this brand name is manufactured and distributed by Allergan under license from Syntex.[7]
Apotex, a Canadian manufacturer, offers generic Ketorolac tromethamine as a 0.5% ophthalmic solution and as 10mg tablets under the name "Apo-Ketorolac"[8], 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.[9]
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