Ketorolac Gel

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DRUGS
Ketorolac Gel

Ketorolac is a nonsteroidal anti-inflammatory drug, with analgesic properties. It is also used to relieve pain caused by ankle sprain. Ketorolac is indicated for short term management (up to 10 days) of moderate to severe pain. 

Introduction

Ketorolac is a non-steroidal anti-inflammatory drug, with analgesic properties. It is also used to relieve pain caused by ankle sprain. Ketorolac is indicated for short term management (up to 10 days) of moderate to severe pain.

Indications

  • Moderate to severe pain
  • Acute pain requiring opioid-level analgesia.

Pharamcological Action

Ketorolac inhibits prostaglandin synthesis by competitive blocking cyclooxygenase (COX) enzyme. Ketorolac reduces the prostaglandins synthesis, chemicals that cells of the immune system make that cause the redness, fever, swelling and pain of inflammation and also effective to reduce non-inflammatory pain.

Dosage

2% ketorolac gel should be used to reduce pain and swelling. Applied three or four times per day, however it may vary depending on the size of the affected area and response.

Pharmacokinetics

Ketorolac gel is rapidly absorbed. The skin permeation rate of ketorolac is 5.75±0.53. The plasma half-life of ketorolac is 6 hour. The protein binding of ketorolac is 99.2%. It can be used for short term pain management; an initial dose of ketorolac should be 30 or 60 mg. The terminal half life ranged from 6.6 to 9.7 hour. Topical route of administration may be a safe and effective alternative to the presently used oral routes.

Contraindications

  • Aspirin allergy
  • Peptic ulcer
  • As prophylactic analgesic before any major surgery. Treatment of Peri-operative pain in CABG (coronary artery bypass grafting ) setting
  • Advanced renal impairment
  • Hypovolemia
  • Cerebrovascular bleeding
  • Hemorrhagic diathesis
  • Concomitant probenecid, salicylates, pentoxifylline, other NSAIDs
  • Epidural or intrathecal inj. Labor & delivery

Drug Interactions

  • Aliskiren
  • ACE (angiotensin converting enzyme)  inhibitors (such as captopril, lisinopril)
  • Angiotensin II receptor blockers (such as valsartan, losartan)
  • Corticosteroids (such as prednisone)
  • Methotrexate
  • Probenecid
  • Cidofovir
  • Diuretics (such as furosemide)
  • Anti-platelet drugs such as clopidogrel and blood thinners such as dabigatran/enoxaparin/warfarin

Side effects

Common (affecting between 1- 10 to 1 in 100)

  • Abdominal pain & Dyspepsia
  • Nausea & Vomiting
  • Drowsiness

Uncommon (affecting 1-100 to 1 in 1000)

  • Edema
  • Pruritus
  • Skin Reactions
  • Headache

Very rare (affecting less than 1 in 10,000)

  • Anaphylaxis

Precautions

  • It may increase the risk of serious cardiovascular events, myocardial infarction and stroke.
  • Not to be used in children younger than 17 years old; safety and effectiveness in these children have not been confirmed.
  • Not be used by nursing mothers because it is excreted in breast milk.

Clinic Evidence

  • Ketorolac gel is effective in the reduction of inflammation and pain due to ankle sprain. Ketorolac gel was compared with etofenamate and placebo (ketorolac vehicle) in a 15-day study and ketorolac gel was significantly better than placebo in reducing the volume of the injured ankle based on the maximum, the area under the curve, and the day 15 percentage changes in ankle volume. Reductions in VAS (visual analogue scales) pain on movement were also greatest for the ketorolac group at all visits1

References

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