Ketorolac, sold under the brand name Toradol among others, is a nonsteroidal anti-inflammatory drug (NSAID) in the family of heterocyclic acetic acid derivatives, used as an analgesic. It is considered a first-generation NSAID.
Ketorolac acts by inhibiting the bodily synthesis of prostaglandins. Ketorolac in its oral (tablet or capsule) and intramuscular (injected) preparations is a racemic mixture of both (S)-(-)-ketorolac, the active isomer, and (R)-(+)-ketorolac.
Ketorolac was developed in 1989 by Syntex Corp. (now part of Roche). It was approved for medical use in the United States in 1989. The eye-drop formulation was approved by the FDA in 1992. An intranasal formulation was approved by the FDA in 2010 for short-term management of moderate to moderately severe pain requiring analgesia at the opioid level. As of 2015, the cost for a typical course of medication in the United States is less than US$25.
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Medical uses
Ketorolac is used for short-term management of moderate to severe pain. It is usually not prescribed for longer than five days. Ketorolac is effective when administered with acetaminophen to control pain in neonates because it does not depress respiration as do opioids. Ketorolac is also an adjuvant to opioid medications and improves pain relief. It is also used to treat dysmenorrhea. Ketorolac is used to treat idiopathic pericarditis, where it reduces inflammation.
Ketorolac is used for short-term pain control not lasting longer than five days, and can be administered orally, by intramuscular injection, intravenously, and by nasal spray. Ketorolac is initially administered by intramuscular injection or intravenously. Oral therapy is only used as a continuation from the intramuscular or intravenous starting point.
Ketorolac is used during eye surgery to maintain mydriasis, or the 'relaxing' of the iris muscles that will allow surgeons to perform cataract surgery. Ketorolac is effective in treating ocular itching. The ketorolac ophthalmic formulation is associated with a decreased development of macular edema after cataract surgery and is more effective alone rather than as an opioid/keterolac combination treatment. Ketorolac has also been used to manage pain from corneal abrasions.
During treatment with ketorolac, clinicians monitor for the manifestation of adverse effects and side effects. Lab tests, such as liver function tests, bleeding time, BUN, serum creatinine and electrolyte levels are often used and help to identify potential complications.
Contraindications
Ketorolac is contraindicated in those with hypersensitivity, allergies to the medication, cross-sensitivity to other NSAIDs, prior to surgery, history of peptic ulcer disease, gastrointestinal bleeding, alcohol intolerance, renal impairment, cerebrovascular bleeding, nasal polyps, angioedema, and asthma.
Recommendations exist for cautious use of ketorolac in those who have experienced cardiovascular disease, myocardial infarction, stroke, heart failure, coagulation disorders, renal impairment, and hepatic impairment.
Adverse effects
Though uncommon, potentially fatal adverse effects are stroke, myocardial infarction, GI bleeding, Stevens-Johnson Syndrome, Toxic epidermal necrolysis and anaphylaxis. A less serious and more common (>10%) side effect is drowsiness. Infrequent (<1%) side effects are paresthesia, prolonged bleeding time, injection site pain, purpura, sweating, abnormal thinking, increased tearing (eyes), edema, pallor, dry mouth, abnormal taste, urinary frequency increased liver enzymes, itching and others. Ketorolac can cause premature constriction of the ductus arteriosis in an infant during the third trimester of pregnancy. Platelet function is decreased related to the use of ketorolac.
The practice of restricting treatment with ketorolac is due to its potential to cause kidney damage.
Interactions
Ketorolac can interact with other medications. Probenecid can increase the probability of having an adverse reaction or experiencing a side effect when taken with ketorolac. Pentoxifylline can increase the risk of bleeding. When aspirin is taken at the same time as ketorolac, the effectiveness is decreased. Problematic GI effects are additive and become more likely if potassium supplements, aspirin, other NSAIDS, corticosteroids, or alcohol is taken at the same time. The effectiveness of antihypertensives and diuretics can be lowered. The use of ketorolac can increase serum lithium levels to the point of toxicity. Toxicity to methotrexate is more likely if ketorolac is taken at the same time. The risk of bleeding increases with the concurrent medications clopidogrel, cefoperazone, valproic acid, cefotetan, eptifibatide, tirofiban, and copidine. Anticoagulants and thrombolytic medications also increase the likelihood of bleeding. Medications used to treat cancer can interact with ketorolac along with radiation therapy. The risk of toxicity to the kidneys increases when ketorolac is taken with cyclosporine.
Interactions with ketorolac exist with some herbal supplements. Panax ginseng, clove, ginger, arnica, feverfew, dong quai, chamomile, and Ginkgo biloba, increases the risk of bleeding.
Mechanism of action
The primary mechanism of action responsible for ketorolac's anti-inflammatory, antipyretic and analgesic effects is the inhibition of prostaglandin synthesis by competitive blocking of the enzyme cyclooxygenase (COX). Ketorolac is a non-selective COX inhibitor. Ketorolac has been assessed to be a relatively higher risk NSAID when compared to aceclofenac, celecoxib, and ibuprofen.
History
In the US, ketorolac was the only widely available intravenous NSAID for many years; an IV form of paracetemol became available in Europe in 2009 and then in the US.
The Syntex company, of Palo Alto, California developed the ophthalmic solution Acular around 2006.
In 2007 there were concerns about the high incidence of reported side effects. This led to restriction in its dosage and maximum duration of use. In the UK, treatment was initiated only in a hospital. Dosing guidelines were published at this time.
Concerns over the high incidence of reported side effects with ketorolac trometamol led to its withdrawal (apart from the ophthalmic formulation) in several countries, while in others its permitted dosage and maximum duration of treatment have been reduced. From 1990 to 1993, 97 reactions with a fatal outcome were reported worldwide.
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