Ketorolac
Nonsteroidal anti-inflammatory drug (NSAID; analgesic) / From Wikipedia, the free encyclopedia
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Ketorolac, sold under the brand name Toradol among others, is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain.[2][3] Specifically it is recommended for moderate to severe pain.[4] Recommended duration of treatment is less than six days,[3] and in Switzerland not more than two days.[5] It is used by mouth, by nose, by injection into a vein or muscle, and as eye drops.[3][4] Effects begin within an hour and last for up to eight hours.[3]
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Trade names | Toradol, Acular, Sprix, others |
Other names | Ketorolac tromethamine |
AHFS/Drugs.com | Monograph |
MedlinePlus | a693001 |
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Routes of administration | By mouth, under the tongue, intramuscular, intravenous, eye drops, nasal spray |
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Bioavailability | 80–100% (oral) 100% IV/IM |
Metabolism | Liver |
Elimination half-life | 3.5 h to 9.2 h, young adults; 4.7 h to 8.6 h, elderly (mean age 72) |
Excretion | Kidney: 91.4% (mean) Biliary: 6.1% (mean) |
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ECHA InfoCard | 100.110.314 |
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Formula | C15H13NO3 |
Molar mass | 255.273 g·mol−1 |
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Chirality | Racemic mixture |
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Common side effects include sleepiness, dizziness, abdominal pain, swelling, and nausea.[3] Serious side effects may include stomach bleeding, kidney failure, heart attacks, bronchospasm, heart failure, and anaphylaxis.[3] Use is not recommended during the last part of pregnancy or during breastfeeding.[3] Ketorolac works by blocking cyclooxygenase 1 and 2 (COX1 and COX2), thereby decreasing production of prostaglandins.[3][6]
Ketorolac was patented in 1976 and approved for medical use in 1989.[7][3] It is available as a generic medication.[4] In 2021, it was the 210th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[8][9]
Due to a series of deaths due to gastrointestinal bleeding and kidney failure, ketorolac as a pain medication was removed from the German market in 1993.[10] When ketorolac was introduced into Germany, it was often mis-used as an opioid replacement in pain therapy because its side effects were perceived as much less severe, it did not produce any dependence, and a dose was effective for 7–8 hours compared to morphine with 3–4 hours. As a very potent prostaglandin inhibitor, ketorolac diminishes the kidney's own defenses against vasoconstriction-related effects, e.g. during blood loss or high endogenous catecholamine levels.[11]