| Item |
Information |
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Drug Groups
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approved |
|
Description
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A pyrrolizine carboxylic acid derivative structurally related to indomethacin. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed) |
| Indication |
For the short-term (~5 days) management of moderately severe acute pain that requires analgesia at the opioid level, usually in a postoperative setting. |
| Pharmacology |
Ketorolac, an antiinflammatory agent with analgesic and antipyretic properties, is used to treat osteoarthritis and control acute pain. It is a peripherally acting analgesic. The biological activity of ketorolac tromethamine is associated with the S-form. Ketorolac tromethamine possesses no sedative or anxiolytic properties. |
| Toxicity |
LD50 = 189 mg/kg (rat, oral). |
| Affected Organisms |
| • |
Humans and other mammals |
|
| Biotransformation |
Primarily hepatic. Less than 50% of a dose is metabolized. The major metabolites are a glucuronide conjugate, which may also be formed in the kidney, and p-hydroxy ketorolac. Neither metabolite has significant analgesic activity. |
| Absorption |
Rapidly and completely absorbed after oral administration |
| Half Life |
2.5 hours for the S-enantiomer compared with 5 hours for the R-enantiomer |
| Protein Binding |
99% |
| Elimination |
The principal route of elimination of ketorolac and its metabolites is renal. Approximately 6% of a dose is excreted in the feces. |
| Distribution |
* 0.26 ± 0.08 L/kg [children 4 to 8 years old] |
| Clearance |
* 0.042 +/- 0.01 L/hr/kg [Pediatric Patients]
* 0.02 L/h/kg [Normal Subjects IM]
* 0.03 L/h/kg [Normal Subjects oral]
* 0.02 L/h/kg [Healthy Elderly Subjects IM]
* 0.02 L/h/kg [Healthy Elderly Subjects oral]
* 0.03 L/h/kg [Patients with Hepatic Dysfunction IM]
* 0.03 L/h/kg [Patients with Hepatic Dysfunction oral]
* 0.02 L/h/kg [Patients with Renal Impairment IM]
* 0.02 L/h/kg [Patients with Renal Impairment oral]
* 0.02 L/h/kg [Renal Dialysis Patients IM] |
| External Links |
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