Drug Groups

approved

Description

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

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]

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