Ketoprofen

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Oruvail Gel

Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID). As such, it possesses analgesic, antipyretic and anti-inflammatory properties. Ketoprofen was first synthesised in 1967, although it was not introduced into clinical practice until 1973. It is available as Oruvail Gel, a clear, transparent gel that contains 2.5% w/w ketoprofen B.P. and is used to provide short-term local relief in instances of mild to moderate pain.

Ketoprofen is a phenyl propionic acid derivative with the chemical name 2-(3-benzoylphenyl)-propionic acid. It works by inhibiting the production of the enzyme cyclo-oxygenase in the body. Cyclo-oxygenase (COX) controls how much of the chemicals known as prostaglandins are produced by the body's immune system. Prostaglandins are released in order to alert the body to the presence of damage caused by injury or disease. The reduction in the amount of prostaglandin biosynthesised correspondingly lowers the amount of pain and inflammation experienced by the patient. Ketoprofen in gel form reduces the concentration of prostaglandins and other related compounds in the localised tissue. Ketoprofen is a potent inhibitor of prostaglandin synthetase but, because the gel is only applied at the location of the pain, its effects are not systemic. The bioavailability of ketoprofen in gel form is equivalent to about 5% of that taken orally.

Studies have shown that the gel achieves significant pain relief when applied topically to an area of the skin. In this way, the ketoprofen is able to treat affected tissue through direct diffusion. This is particularly useful in instances of pain being the result of active or passive movement or additional pressure on the joint. Ketoprofen relieves musculoskeletal pain and inflammation in muscles and joints, including arthritis pain, osteoarthritis, stiffness of the joints, soft tissue rheumatism, tendonitis, bursitis, backache, gout, and sports injuries such as musculotendinous contusions, bruising, sprains, and strains.

When applied as a gel to a painful skin area, ketoprofen is slowly absorbed by the body. Pain relief occurs within 30 minutes of applying ketoprofen gel. Applying it externally in the form of a topical gel reduces the potential for side effects related to the stomach and GI upsets. This is because, while skin concentrations are high, plasma levels are lower than if the ketoprofen was taken orally. Peak plasma concentrations are achieved in 30 minutes to two hours. Ketoprofen gel produces plasma levels that are about 60% lower than those experienced after a single oral dose of ketoprofen.

Ketoprofen is metabolised by the liver and excreted by the kidneys and, as such, it is dialyzable. The main metabolite of ketoprofen is the pharmacologically inactive glucuronide conjugate. Ketoprofen is non-habit forming and there is only a minimal chance of its accumulation by the body. The normal half-life for ketoprofen after oral administration is one to two hours, although this may be extended if used by geriatric patients or patients with liver complications. For ketoprofen gel, the half-life is greatly extended, due to its absorption across a cutaneous surface.

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