Ketorolac

Ketorolac
ATC Code M01AB15, S01BC05
Formula C15H13NO3
Molar Mass (g·mol−1) 255,27
Physical State solid
Density (g·cm−3) 1,33
Melting Point (°C) 160,5
Boiling Point (°C) 493,2
PKS Value 3,49
CAS Number 74103-06-3
PUB Number 3826
Drugbank ID DB00465
Solubility soluble in water

Basics

Ketorolac is a non-steroidal anti-inflammatory drug (NSAID) and is commercially available as an oral tablet, injectable solution, nasal spray, and ophthalmic solution. Its analgesic properties make it a useful pain management agent in many areas, including postoperative pain, rheumatoid arthritis, osteoarthritis, menstrual cramps, headaches, spinal and soft tissue pain, and ankylosing spondylitis. Ketorolac similar efficacy to standard doses as some opioids (for example, morphine), making it a very effective agent with no potential for dependence.

Ketorolac was patented in 1976 and approved for medical use in 1989.

Pharmacology

Pharmacodynamics and mechanism of action

Ketorolac is a non-selective NSAID and acts by inhibiting the two enzymes COX-1 and COX-2, which are normally responsible for the conversion of arachidonic acid to prostaglandins. The COX-1 enzyme is constitutively active and is found in platelets, gastric mucosa, and vascular endothelium. The COX-2 enzyme mediates inflammation, pain, and fever.

Therefore, inhibition of the COX-1 enzyme is associated with an increased risk of bleeding and gastric ulcers, whereas the desired anti-inflammatory and analgesic properties are associated with inhibition of the COX-2 enzyme. Therefore, despite its efficacy in pain management, ketorolac should not be used long-term because it increases the risk of serious adverse effects such as gastrointestinal bleeding, peptic ulceration, and perforation.

Pharmacokinetics

Ketorolac is rapidly and completely absorbed after oral administration, with bioavailability after oral administration of approximately 80%. Maximum plasma concentratione is reached 20-60 minutes after administration. Over 99% of the dose is bound to plasma proteins in the blood. Ketorolac is metabolized by hydroxylation or conjugation in the liver. The enzymes involved mainly include CYP2C8 and CYP2C9. Ketorolac is excreted primarily through the kidneys, with approximately 92% of the dose excreted through the kidneys. The remainder is excreted in the stool.

Drug Interactions

Probenecid may increase the likelihood of adverse reactions when taken with ketorolac. The risk of gastrointestinal effects is increased if potassium supplements, aspirin, other NSAIDs, corticosteroids, or alcohol are taken at the same time. The risk of bleeding increases with concomitant use of clopidogrel, cefoperazone, valproic acid, cefotetan, eptifibatide, tirofiban, and ticlopidine. Anticoagulants and thrombolytic medications also increase the likelihood of bleeding.

Toxicity

Side effects

Possible side effects are:

  • Drowsiness
  • Paresthesias
  • Prolonged bleeding time
  • Pain at the injection site
  • Purpura
  • Sweating
  • Increased tear production
  • Edema
  • Pallor
  • Dry mouth
  • Abnormal taste
  • Urinary frequency
  • Elevated liver enzymes
  • Itching

Contraindications and precautions

Ketorolac is contraindicated in patients with active ulcer disease, in patients with recent gastrointestinal bleeding or perforation, and in patients with history of peptic ulcer disease or gastrointestinal bleeding. Ketorolac should not be given if there is a known allergy to the active ingredient.

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

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