Ketoprofen
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Routes of administration | Oral, topical, intravenous (veterinary use) |
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Pharmacokinetic data | |
Protein binding | 99% |
Elimination half-life | 2-2.5 hours |
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ECHA InfoCard | 100.040.676 |
Chemical and physical data | |
Formula | C16H14O3 |
Molar mass | 254.281 g/mol g·mol−1 |
Ketoprofen, (RS)2-(3-benzoylphenyl)-propionic acid (chemical formula C16H14O3) is one of the propionic acid class of non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic effects. It acts by inhibiting the body's production of prostaglandin.
Ketoprofen was available over-the-counter in the United States in the form of 12.5 mg coated tablets (Orudis KT & Actron), but the product has been discontinued. It is available by prescription as 25, 50, 75, 100, 150, and 200 mg capsules.
Ketoprofen is available also as a 2,5% gel for topical application.
Brand names in the US are Orudis and Oruvail. It is available in the UK as Ketoflam and Oruvail, in Finland as Ketorin, Keto, Ketomex, and Orudis'; in France as Bi-Profénid, in Italy as Fastum Gel, Ketoprofene, Lasonil or Oki, in Poland as Ketonal, in Mexico as Arthril and Norway as Zon or Orudis.
In Lithuania, ketoprofen is called Ketoprofenum and/or Ketoprofenas. For topical application: the name brands are Fastum with 2.5% (gel) which is over the counter and Ketospray with 10% (liquid spray) which must be prescribed. In Switzerland, an innovative ketoprofen formulation based on Transfersome technology for direct application on the skin above the site to be treated has been approved.
In some countries, the optically pure (S)-enantiomer (dexketoprofen) is available; its trometamol salt is said to be particularly rapidly reabsorbed from the gastrointestinal tract, having a rapid onset of effects.
Ketoprofen is generally prescribed for arthritis-related inflammatory pains or severe toothaches that result in the inflammation of the gums.
Ketoprofen can also be used for treatment of some pain, especially nerve pain like post-herpetic neuralgia and referred pain for radiculopathy, in the form of a cream, ointment, liquid, spray, or gel which also contains ketamine and lidocaine, along with other agents which may be useful such as cyclobenzaprine, amitryptiline, acyclovir, gabapentin, orphenadrine and other drugs used as NSAIDs or adjuvant, atypical or potentiators for pain treatment. The results, of course, vary in each case, with varying degrees of the attenuation of the burning, tingling, and/or shooting component of the neuralgic pain being quite frequent along with a modest reduction in overall pain level in some cases. In severe cases and those involving multiple conditions in addition to the cause of the neuralgia, there is no substitute for comprehensive palliative therapy including systemic NSAIDs, opioids, muscle relaxants, intermittent corticosteroids and other agents if needed and adjuncts & potentiators to increase the power of the analgesics in addition to the topical preparation and physical and alternative modalities such as physiotherapy, acupuncture, biofeedback & related modalities, nutritional approaches and many others relevant to each case. Even the addition of the opioid tramadol to topical preparations is not known to be an adequate replacement for systemic opioids in cases where they can be useful and efficacious.
Use in horses and other animals
Ketoprofen (Ketofen) is a common NSAID, antipyretic, and analgesic used in horses and other equines. It is also used as a mild painkiller in smaller animals, generally following surgical procedures. It is most commonly used for muscoskeletal pain, joint problems, and soft tissue injury, as well as laminitis. It does not treat the underlying problem, nor does it speed the healing process. It is also used to control fevers and prevent endotoxemia. However, they may mask the symptoms of the underlying problem, and therefore make diagnosis more difficult for a veterinarian.
Side effects and precautions
Side effects are relatively uncommon if used as recommended, and less common than 2 other commonly used NSAIDs: flunixin or phenylbutazone. Side effects include gastrointestinal ulcers, drop in red blood cell count (a result of GI bleeding), and rarely kidney damage, protein loss, and bleeding disorders. It should therefore be used with caution in horses with liver or kidney disease, or gastrointestinal problems.
Additionally, it should not be used in horses allergic to aspirin.
Uses with other drugs
Ketoprofen should not be used in with other NSAIDs or corticosteroids, as this increases the risk of GI ulceration. It should also be used with caution with other anticoagulants. It is commonly used with omeprazole, sucralfate, and cimetidine to help protect the GI tract.
Administration
Ketoprofen is labeled to be administered intravenously only, and is recommended for a maximum of five days of use. Its analgesic and antipyretic effects begin to occur 1–2 hours following administration. The most common dosage is 10 mg/lb, once per day, although this dosage may be lowered for ponies, who are most susceptible to NSAID side effects.
References
- Kantor, T. G. Ketoprofen: a review of its pharmacologic and clinical properties. Pharmacotherapy. 1986 May-Jun;6(3):93-103.
- Forney, Barbara C, MS, VMD.Equine Medications, Revised Edition. Blood Horse Publications. Lexington, KY. Copyright 2007.
- ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.