Action and Spectrum

Actions and Spectrum 

Prostaglandins, which have a role in inflammation and pain, are produced when ketorolac is used. It relieves pain by preventing the activity of the cyclooxygenase (COX) enzymes, notably COX-1 and COX-2, which reduce the formation of prostaglandins.  

ketorolac is frequently used to treat moderate to severe post-operative pain, including that associated with orthopaedic, dental, and gynaecological procedures.

Drug Interaction

Adverse Reaction

Frequency defined  

<1% 

Anaphylaxis 

Cholestatic jaundice 

Depression  

Urinary frequency 

Stomatitis 

Urinary retention 

Euphoria  

Pallor 

Rectal bleeding 

Melena  

Vasodilation 

Nervousness 

Peptic ulcer 

Rash 

Insomnia 

Laryngeal/lingual edema 

Increased liver function test values 

Hypotension 

Dysgeusia 

Difficulty in concentration 

Blurred vision  

Liver failure 

Oliguria  

Hemolytic-uremic syndrome 

Abnormal thinking 

Hyponatremia 

Bronchospasm 

Hepatitis 

Hyperkalemia 

1-10% 

Diarrhea (3-9%) 

Pruritus (3-9%)  

Edema (1-3%)  

Hypertension (4%) 

Constipation (<3%)  

Purpura (<3%) 

Drowsiness (6%) 

Increased serum creatinine (2%) 

Dizziness (3-9%) 

Increased blood urea nitrogen (BUN) (3%) 

>10%  

Dyspepsia (12-13%) 

Nausea (12-13%) 

Somnolence (3-14%) 

GI pain (12-13%) 

Headache (17%) 

Black Box Warning

Black Box Warning 

The risk of major cardiovascular thrombotic events, such as heart attack and stroke, may rise after taking ketorolac. ketorolac use is associated with an increased risk of gastrointestinal bleeding, ulceration, and perforation, which can be fatal. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Individuals with a known reactivity or allergy to ketorolac or other NSAIDs should not take it. 
• Patients who have a history of asthma, bronchospasm, or allergic responses brought on by NSAIDs should not take ketorolac because it could bring on or exacerbate these symptoms. 
• People with active or recent gastrointestinal bleeding or perforation, as well as those who have a history of peptic ulcer disease or gastrointestinal bleeding, should not take ketorolac. 

Caution: 

• Patients with renal impairment should use ketorolac with caution since it can worsen kidney function and raise the risk of acute renal failure.  
• ketorolac may result in peripheral edema and fluid retention. Patients who have a history of heart failure, high blood pressure, or illnesses that can cause fluid retention should use it with caution. 
• ketorolac may slow bleeding and prevent platelet aggregation. In patients with coagulation abnormalities and bleeding tendencies, caution is suggested when using ketorolac. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: C and D (in third trimester) 

Lactation: Excretion into human milk known with multiple doses and avoid its use.  

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

A non-steroidal anti-inflammatory medication (NSAID) with analgesic, anti-inflammatory, and antipyretic effects is ketorolac. By preventing the production of prostaglandins, which are chemical mediators involved in pain, inflammation, and fever, it has an anti-inflammatory effect. ketorolac’s analgesic and anti-inflammatory actions are brought about through COX-1 inhibition. 

Pharmacodynamics 

ketorolac inhibits COX-2, which reduces the generation of prostaglandins that promote inflammation.The ability of ketorolac to prevent prostaglandin formation also applies to controlling body temperature. The production of COX-2-mediated prostaglandins is a key factor in the development of fever. ketorolac can aid in bringing down a fever-related rise in body temperature by lowering prostaglandin levels.  

Pharmacokinetics 

Absorption   

ketorolac is well absorbed following oral administration.  

Intravenous administration of ketorolac provides immediate and complete bioavailability. 

Distribution 

ketorolac distributes widely throughout the body and has a moderate volume of distribution. 

Metabolism 

The significant hepatic metabolism of ketorolac occurs mainly by glucuronidation and, to a lesser extent, hydroxylation. 

Elimination and excretion 

The kidneys are primarily responsible for eliminating ketorolac and its metabolites. Less than 1% of the dosage is eliminated unaltered, leaving about 92% of it in the urine. 

Adminstartion

Administration 

The oral tablets are swallowed whole with a glass of water. 

Intramuscular injections of ketorolac are typically administered in the upper outer quadrant of the gluteal region. 

Intravenous ketorolac is administered as a slow injection, usually over a period of 15 seconds to 1 minute. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: ketorolac 

Why do we use ketorolac? 

Following surgical treatments, ketorolac is frequently used to relieve discomfort. During the healing process, it can help with pain relief, inflammatory reduction, and general comfort.  

ketorolac is useful for treating the acute pain brought on by musculoskeletal problems such sprains, strains, and sports injuries. It can offer comfort by easing discomfort and inflammation in afflicted tissues.  

ketorolac can be used to treat the severe discomfort linked to renal colic, which is brought on by kidney stones passing through the kidneys.