Ketorolac , sold under the brand name Toradol among others, is a nonsteroidal anti-inflammatory drug (NSAID) in the heterocyclic acetic acid derivative family, used as an analgesic. This is considered the first generation of NSAIDs.
Ketorolac acts by inhibiting prostaglandin synthesis. Ketorolac in oral preparations (tablets or capsules) and intramuscular (injected) is a racemic mixture of both ( S ) - (-) - ketorolac, active isomers, and ( R ) - () - ketorolak.
Ketorolac was developed in 1989 by Syntex Corp (now part of Roche). It was approved for medical use in the United States in 1989. Eyed-eye formulations were approved by the FDA in 1992. The intranasal formulation was approved by the FDA in 2010 for short-term management of moderate to moderate severe pain requiring opioid-level analgesia. By 2015, the cost for typical treatment programs in the United States is less than US $ 25.
Video Ketorolac
Medical use
Ketorolac is used for short-term management of moderate to severe pain. Usually not prescribed for more than five days. Ketorolac is effective when administered with paracetamol to control pain in neonates because it does not suppress respiration as opioids do. Ketorolak is also an adjuvant for opioid drugs 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 that lasts no longer than five days, and can be administered orally, with intramuscular, intravenous, and nasal sprays. The initial discharges are given by intramuscular or intravenous injection. Oral therapy is only used as a continuation of an intramuscular or intravenous starting point.
Ketorolac is used during eye surgery to maintain midriasis, or 'relaxation' of the iris muscles that will allow the surgeon to perform cataract surgery. Ketorolak effective in treating itchy eyes. Ketorolac eye formulation is associated with a decreased development of macular edema after cataract surgery and is more effective on its own than as a combination of opioid/ketoroline treatment. Ketorolak has also been used to manage the pain of corneal blisters.
During treatment with ketorolak, doctors monitor the manifestations of side effects and side effects. Laboratory tests, such as liver function tests, bleeding time, BUN, serum creatinine and electrolyte levels are often used and help identify potential complications.
Maps Ketorolac
Contraindications
Ketorolac is contraindicated in those with hypersensitivity, drug allergies, cross-sensitivity to other NSAIDs, before surgery, history of peptic ulcer disease, gastrointestinal bleeding, alcohol intolerance, renal impairment, cerebrovascular hemorrhage, nasal polyps, angioedema, and asthma. Recommendations exist to be careful using ketorolac to those who have had cardiovascular disease, myocardial infarction, stroke, heart failure, coagulation disorders, renal impairment, and liver disorders.
Adverse effects
Although rare, potentially fatal side effects are stroke, myocardial infarction, GI bleeding, Stevens-Johnson syndrome, toxic epidermal necrolysis and anaphylaxis. Less serious and more common (& gt; 10%) side effects are drowsiness. Rare side effects (& lt; 1%) are paresthesia, prolonged bleeding time, injection site pain, purpura, sweating, abnormal thoughts, increased tear production, edema, pale, dry mouth, abnormal taste, urinary frequency, increased enzyme liver, itching and others. Ketorolac can cause premature constriction of the ductus arteriosis in infants during the third trimester of pregnancy. Decreased platelet function associated with the use of ketorolak.
The practice of limiting treatment with ketorolac is due to its potential to cause kidney damage.
Interactions
Ketorolak can interact with other drugs. Probenecid may increase the likelihood of having adverse reactions or experiencing adverse effects when taken with ketorolac. Pentoxifylline may increase the risk of bleeding. When aspirin is taken together with ketorolac, its effectiveness decreases. The GI effects are problematic additives and become more likely if potassium supplements, aspirin, other NSAIDs, corticosteroids, or alcohol are taken at the same time. The effectiveness of antihypertensives and diuretics can be decreased. The use of ketorolac can increase serum lithium levels to the point of toxicity. Toxicity to methotrexate is more likely if ketorolak is taken at the same time. The risk of bleeding increases with clopidogrel, cefoperazone, valproic acid, cefotetan, eptifibatide, tirofiban, and copidine. Anticoagulant drugs and thrombolytics also increase the likelihood of bleeding. Drugs used to treat cancer can interact with ketorolac along with radiation therapy. Risk of toxicity in the kidney increases when ketorolak is taken with cyclosporine.
The interaction with ketorolak occurs with some herbal supplements. Panax ginseng , cloves, ginger, arnica, feverfew, dong quai, chamomile, and Ginkgo biloba , increases the risk of bleeding.
Action mechanism
The main mechanism of action responsible for anti-inflammatory, antipyretic and analgesic effects of ketorolac is inhibition of prostaglandin synthesis by competitive blocking of cyclooxygenase (COX) enzymes. Ketorolak is a non-selective COX inhibitor. Ketorolac has been assessed as a relatively higher risk of NSAIDs when compared with aceclofenac, celecoxib, and ibuprofen.
History
In the US, ketorolac is the only widely available intravenous NSAID for many years; IV forms of paracetemol, which are not NSAIDs, were available in Europe in 2009 and later in the US.
The Syntex company, Palo Alto, California developed the Acular eye solution around 2006.
In 2007, there were concerns about the high incidence of reported adverse events. This results in maximum dosage restriction and duration of use. In the UK, treatment begins only in hospitals, although this is not designed to exclude its use in pre-hospital care and mountain rescue arrangements. Dose guidelines were published at the time.
Concerns over the high incidence of reported adverse events with ketorolac trometamol caused withdrawal (irrespective of eye formulation) in some countries, while in other doses were allowed and the duration of maximum treatment was reduced. From 1990 to 1993, 97 reactions with fatal results were reported worldwide.
References
Bibliography
- drug information AHFS . Bethesda, MD: American Society of Health-System Pharmacists. 2011. ISBN: 9781585282609.
- Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition . Jones & amp; Bartlett Learning. p.Ã, 9. ISBNÃ, 9781284057560.
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Handley, Dean A.; Cervoni, Peter; McCray, John E.; McCullough, John R. (1998). "Preclinical enantioselective pharmacology of (R) - and (S) - ketorolac". J Clin Pharmacol . 38 (2 Suppl): 25S-35S. doi: 10.1002/j.1552-4604.1998.tb04414.x. ISSNÃ, 0091-2700. PMID 9549656. - Henry, Norma (2016). RN pharmacology for nursing: review module . Overland Park, KS: Institute for Technology Assessment. ISBN: 9781565335738.
- Kizior, Robert (2017). Saunders 2017 nursing guidebook . St. Louis, MO: Elsevier. ISBN: 9780323442916.
External links
- cme.medscape.com on nose ketorolak, accessed March 30, 2017
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