Ketorolac, sold under the brand names Toradol, Acular and Sprix, among others, is a nonsteroidal anti-inflammatory drug (NSAID) used for the short-term treatment of moderate to severe pain. Its use is generally limited to no more than five days because extended treatment increases the risk of serious adverse effects. It can be taken by mouth, by nose, by injection into a vein or muscle, and as eye drops. Effects begin within an hour and last for up to eight hours. Ketorolac also has antipyretic (fever-reducing) properties. Common side effects include sleepiness, dizziness, abdominal pain, swelling, and nausea. Serious side effects may include stomach bleeding, kidney failure, heart attacks, bronchospasm, heart failure, and anaphylaxis. Use is not recommended during the last part of pregnancy or during breastfeeding. Ketorolac works by blocking cyclooxygenase 1 and 2 (COX1 and COX2), thereby decreasing production of prostaglandins. Ketorolac was patented in 1976 and approved for medical use in 1989. It is available as a generic medication. In 2023, it was the 228th most commonly prescribed medication in the United States, with more than one million prescriptions. Due to a series of deaths due to gastrointestinal bleeding and kidney failure, ketorolac as a pain medication was removed from the German market in 1993. When ketorolac was introduced into Germany, it was often used as an opioid replacement in pain therapy because its side effects were perceived as much less severe, it did not produce any dependence, and a dose was effective for 7–8 hours, compared to morphine's 3–4 hours. As a very potent prostaglandin inhibitor, ketorolac diminishes the kidney's own defenses against vasoconstriction-related effects, e.g. during blood loss or high endogenous catecholamine levels.
Medical uses
Ketorolac is used for short-term management of moderate to severe pain. It is usually not prescribed for longer than five days, due to its potential to cause kidney damage. Ketorolac is effective when administered with paracetamol (acetaminophen) to control pain in newborns, because it does not depress respiration as opioids can do. Ketorolac is also an adjuvant to opioid medications and improves pain relief. It can also be used to treat dysmenorrhea as well as idiopathic pericarditis, where it reduces inflammation. For systemic use, ketorolac can be administered orally, under the tongue, by intramuscular injection, intravenously, and by nasal spray. Usually, it is initially administered by intramuscular injection or intravenously, with oral therapy used as a continuation after the initial IM or IV dose. Ketorolac is also used as an eye drop. It can be given during eye surgery to help with pain, and is effective in treating ocular itching. There is not enough evidence to decide if non-steroidal anti-inflammatory drugs can help in preventing cystoid macular edema. Ketorolac eye drops have also been used to manage pain from corneal abrasions. During treatment with ketorolac, clinicians monitor for the manifestation of adverse effects. Lab tests, such as liver function tests, bleeding time, BUN, serum creatinine and electrolyte levels are often used to identify potential complications.
Contraindications Ketorolac is contraindicated in those with hypersensitivity, allergies to the medication, cross-sensitivity to other NSAIDs, history of peptic ulcer disease, gastrointestinal bleeding, alcohol intolerance, renal impairment, cerebrovascular bleeding, nasal polyps, angioedema, and asthma, and before surgery. It is recommended that patients who have experienced cardiovascular disease, myocardial infarction, stroke, heart failure, coagulation disorders, renal impairment, and hepatic impairment be careful when taking ketorolac.
Adverse effects A common (>10%) side effect is drowsiness. Infrequent (<1%) side effects include paresthesia, prolonged bleeding time, injection site pain, purpura, sweating, abnormal thinking, increased production of tears, edema, pallor, dry mouth, abnormal taste, urinary frequency, increased liver enzymes, itching and others. Platelet function can be decreased by the use of ketorolac. Though uncommon, potentially fatal adverse effects include stroke, myocardial infarction, GI bleeding, Stevens–Johnson syndrome, toxic epidermal necrolysis and anaphylaxis. Ketorolac has been assessed to be a relatively higher-risk NSAID when compared to aceclofenac, celecoxib, and ibuprofen. Like all NSAIDs, ketorolac can cause premature constriction of the ductus arteriosus in the infant if taken by the mother during the third trimester of pregnancy. In October 2020, the U.S. Food and Drug Administration (FDA) required the prescribing information for all nonsteroidal anti-inflammatory medications to be updated to describe the risk of kidney problems in unborn babies that result in low amniotic fluid. They recommend avoiding NSAIDs in pregnant women at 20 weeks or later in pregnancy.
Interactions Ketorolac can interact with numerous other medications. Probenecid can increase the probability of having an adverse reaction 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 ticlopidine. Anticoagulants and thrombolytic medications also increase the likelihood of bleeding. Medications used to treat cancer can interact with ketorolac as can radiation therapy. The risk of toxicity to the kidneys increases when ketorolac is taken with cyclosporine. Ketorolac also interacts with some herbal supplements. For example, the use of Panax ginseng, clove, ginger, arnica, feverfew, dong quai, chamomile, and Ginkgo biloba increases the risk of bleeding.
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