Ketoprofen 22071-15-4

Available forms

Ketoprofen is available as a 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 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 Ketodol, Fastum Gel, Lasonil,Orudis or Oki, in Poland, Serbia, Slovenia and Croatia as Knavon or Ketonal, in Mexico as Arthril, in Norway as Zon or Orudis, and in Venezuela as Ketoprofeno under an injectable solution of 100mg. 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.

Indication

Ketoprofen is generally prescribed for arthritis-related inflammatory pains or severe toothaches that result in the inflammation of the gums. Ketoprofen topical patches are being extensively used for treatment of musculoskeletal pain. The patches have been shown to provide rapid and sustained delivery to underlying tissues without significantly increasing levels of drug concentration in the blood when compared to the traditional oral administration. Ketoprofen undergoes metabolism in the liver via conjugation with glucoronic acid, CYP3A4 and CYP2C9 hydroxylation of the benzoyl ring, and reduction of its keto function. Ketoprofen is used for its antipyretic, analgesic, and anti-inflammatory properties by inhibiting cyclooxygenase-1 and -2 (COX-1 and COX-2) enzymes reversibly, which decreases production of pro-inflammatory prostaglandin precursors. 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 two other commonly used NSAIDs: flunixin and 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 1 mg/ lb, once per day, although this dosage may be lowered for ponies, who are most susceptible to NSAID side effects. It is also available as a capsule dosage form.

Ecological problems

Recent studies have found that Ketoprofen, like Diclofenac is a veterinary drug causing lethal effects in Asian vultures. Vultures feeding on the carcasses of recently-treated livestock suffer acute kidney failure within days of exposure. According to research,the vulture population has undergone a sharp decline Indian subcontinent, 95% decline in 2004, 99. 9% decline as of 2008 due to the use of Diclofenac in animals. The loss of vultures has had a social impact on the Indian Zoroastrian Parsi community, who traditionally use vultures to dispose of human corpses in Towers of Silence, but are now compelled to seek alternate methods of disposal.