Medznat

Ketorolac injection is used for short-term relief of moderate to severe pain. It is generally used before or after medical procedures or after surgery.

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Introduction

Ketorolac injection is used for short-term relief of moderate to severe pain. It is generally used before or after medical procedures or after surgery.

Indications

Moderate to severe pain
Acute pain requiring opioid-level analgesia

Pharmachologic action

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

Dosage

IV: 30 mg as single dose or 30 mg every 6hour; not to exceed 120 mg/day

Pharmacokinetics

Ketorolac is rapidly absorbed and mean peak plasma concentration of 2.4μg/ml at an average of 5.4 minutes after dosing. More than 99% of the ketorolac in plasma is protein-bound over a wide concentration range. The terminal plasma elimination half-life was 5.1 hours, average volume of distribution 0.15 l/kg, and total plasma clearance 0.35ml/min/kg. The primary route of excretion of ketorolac and its metabolites is renal: 91.4% (mean) of a given dose being found in the urine and 6.1% (mean) in the faeces.

Contraindications

History or active Gastrointestinal diseases such as bleeding, ulceration or perforation
In patients who have previously shown hypersensitivity reactions (e.g. asthma, rhinitis, angioedema or urticaria) in response to non-steroidal anti-inflammatory drugs
In patients with suspected or confirmed cerebrovascular bleeding, hemorrhage or incomplete haemostasis and coagulation disorders.
Syndrome of nasal polyps, angioedema or bronchospasm
Concurrent treatment with aspirin or other NSAIDs including cyclooxygenase 2 specific inhibitors.
Probenecid or lithium salts
Moderate or severe renal impairment (serum creatinine> 160 micromol/l)
Asthma
Severe heart failure, hepatic failure and renal failure
Anti-coagulants including warfarin and low dose heparin (2500 - 5000 units twelve hourly)
During pregnancy, labour, delivery or lactation
Children under 16 years of age
For neuraxial (epidural or intrathecal) administration due to its alcohol content

Drug interaction

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 between 1-100 to 1 in 1000)

Edema
Hypertension
Pruritus
Skin Reactions
Headache

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

Peptic Ulcer
Gastro intestinal bleed/perforation
Renal or Liver Failure
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.

Clinical evidence

Ketorolac is nonsteroidal anti- inflammatory drugs (NSAID) that have the potential to replace opioids in the treatment of severe pain. Ketorolac trometamol if given intravenously is effective in the management of surgical pain and pain related to cancer and has fewer side-effects in comparison to morphine. The administration time of Ketorolac is much shorter than other drugs. Intravenous ketorolac can be used for severe pain in isolated limb injuries¹.
Continuous intravenous administration of Ketorolac reduces pain and morphine consumption after total hip or knee arthroplasty. Less sedation and reduced requirement of antiemetic is seen in the patients receiving Ketorolac².a