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Overview
| Generic Names: | Ketoralac; Ketorolac Tromethamine; Ketorolaco [Spanish]; Ketorolacum [Latin] |
|---|---|
| Trade Names: | Acular; Acular LS; Acular Preservative Free; Toradol |
| PharmGKB Accession Id: | PA450150 |
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) (source: Drug Bank)
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. (source: Drug Bank)
ATC Therapeutic Categories
- M01AB:Acetic acid derivatives and related substances
- S01BC:Antiinflammatory agents, non-steroids
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Ketorolac is a nonsteroidal anti-inflammatory drug (NSAID) chemically related to indomethacin and tolmetin. Ketorolac tromethamine is a racemic mixture of []S and [+]R-enantiomeric forms, with the S-form having analgesic activity. Its antiinflammatory effects are believed to be due to inhibition of both cylooxygenase-1 (COX-1) and cylooxygenase-2 (COX-2) which leads to the inhibition of prostaglandin synthesis leading to decreased formation of precursors of prostaglandins and thromboxanes from arachidonic acid. The resultant reduction in prostaglandin synthesis and activity may be at least partially responsible for many of the adverse, as well as the therapeutic, effects of these medications. Analgesia is probably produced via a peripheral action in which blockade of pain impulse generation results from decreased prostaglandin activity. However, inhibition of the synthesis or actions of other substances that sensitize pain receptors to mechanical or chemical stimulation may also contribute to the analgesic effect. In terms of the ophthalmic applications of ketorolac - ocular administration of ketorolac reduces prostaglandin E2 levels in aqueous humor, secondary to inhibition of prostaglandin biosynthesis.
(source:
Drug Bank)
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. (source: Drug Bank)
Food Interactions
Take with food to reduce GI irritation (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
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. (source: Drug Bank)
Protein Binding
99% (source: Drug Bank)
Absorption
Rapidly and completely absorbed after oral administration (source: Drug Bank)
Toxicity
LD<sub>50</sub> = 189 mg/kg (rat, oral). (source: Drug Bank)
Isomeric SMILES Code:
c1ccc(cc1)C(=O)c2ccc3n2CCC3C(=O)O (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
|
PDE4D |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| PTGS1 |
|
(source: Drug Bank) |
| PTGS2 |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| acenocoumarol |
|
The NSAID increases the anticoagulant effect (source: Drug Bank) |
| alendronate |
|
Increased risk of gasrtic toxicity (source: Drug Bank) |
| aspirin |
|
ASA increases toxicity of ketorolac (source: Drug Bank) |
| dicumarol |
|
The NSAID increases the anticoagulant effect (source: Drug Bank) |
| lithium |
|
The NSAID increases serum levels of lithium (source: Drug Bank) |
| methotrexate |
|
The NSAID increases the effect and toxicity of methotrexate (source: Drug Bank) |
| probenecid |
|
Probenecid increases toxicity of ketorolac (source: Drug Bank) |
| warfarin |
|
The NSAID increases the anticoagulant effect (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Pain |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
