Tilidine

Tilidine is a synthetic opioid painkiller, used mainly in Germany, Switzerland, South Africa and Belgium for treatment of moderate to severe pain, both acute and chronic. Its effectiveness in treating pain has been compared to that of morphine, and it has been used off-label for the treatment of neuropathic pain. It is also used in some cases for the treatment of pulmonary edema. Tilidine is marketed under several brand names, such as Valoron and Valtran.

Etymology

The term "Tilidine" is derived from the German "Tilidin", which is the INN and generic name of the drug in Germany and other countries. The exact etymology of the word is not known.

Pharmacology

Tilidine is a prodrug, which means it is metabolized in the liver into its active form, nortilidine, by the enzyme CYP2C19. Nortilidine is about 20 times more potent than tilidine, and it is nortilidine that provides the analgesic effect. Tilidine itself has very little analgesic effect.

Tilidine works by binding to the mu-opioid receptor, which is the same receptor that drugs like morphine and heroin bind to. This binding causes a decrease in the perception of pain.

Side Effects

Like all opioids, tilidine has a number of side effects. The most common side effects are nausea, dizziness, and dry mouth. More serious side effects can include respiratory depression, which can be life-threatening.

Legal Status

In the United States, tilidine is a Schedule I controlled substance, which means it has a high potential for abuse and no accepted medical use. In Germany, it is a prescription medicine, and it is also controlled under the Betäubungsmittelgesetz (Narcotics Act).

See Also

• Opioid
• Pain management
• Prodrug

References

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  Chemical structure of Tilidine

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  3D model of Tilidine

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  Tilidine retard tablets

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  Synthesis pathway of Tilidine