Ketoprofen

Products

Ketoprofen is commercially available as a gel (Fastum). It has been approved in many countries since 1992 and in the EU since 1978. The -enantiomer dexketoprofen is available as tablets and as a solution for injection (Ketesse). This article refers to external use. After the safety of topical ketoprofen was questioned in France in 2009 due to adverse skin reactions, the European Medicines Agency (EMA) reviewed the approval and published its findings in July 2010. The EMA concluded that the benefits continued to outweigh the risks of the drug, but that precautions needed to be taken to prevent skin reactions (see below).

Structure and properties

Ketoprofen (C16H14O3, Mr = 254.3) is a white crystalline powder that is practically insoluble in water. Structurally, it is a substituted benzophenone. Local adverse effects are also attributed to this structural element. Ketoprofen was developed as an analog of ibuprofen and is present as a racemate. The -enantiomer dexketoprofen is approved for oral and parenteral therapy, unlike the racemate, which is used only locally.

Effects

Ketoprofen (ATC M01AE03, M02AA10) has analgesic and anti-inflammatory properties when applied topically. The effect is due to inhibition of cyclooxygenase and inhibition of the synthesis of prostaglandins.

Indications

For local treatment of pain and inflammation, for example, bruises, strains, and arthritis.

Dosage

The gel is lightly rubbed 1-2 times a day. Wash hands well after application.

Contraindications

  • Hypersensitivity to ketoprofen or other NSAIDs.
  • Do not apply to mucous membranes, open wounds and pre-damaged skin.

Sensitization may occur with long-term treatment. Patients must be made aware that the treated skin must be protected from the sun, as phototoxic and photoallergic reactions may occur. The skin should be protected from the sun for up to two weeks after treatment. Full precautions can be found in the drug label.

Interactions

The SmPC draws attention to a possible interaction with vitamin K antagonists, as both agents may affect blood clotting. Combination with the UV filter octocrylene, which is present in some sunscreens, should be avoided because skin reactions may occur.

Adverse effects

It is known that ketoprofen can cause local skin reactions such as phototoxic and photoallergic reactions, as well as hypersensitivity reactions. Therefore, the treated skin should be protected from sun or UV radiation. If such reactions occur, the drug must be discontinued. Long-term use should be reviewed because it promotes sensitization.