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Tilidine (brand names Valoron, Valtran, Tilicomp, among others ) is a synthetic opioid analgesic. It mediates pain relieving, constipating, relaxing and euphoriant effects by agonizing µ-opioid receptors. As a pharmaceutical drug, tilidine is mainly used in some European countries such as Germany, Belgium, Luxembourg, Switzerland and also South Africa. As is the case with other opioids, it is also commonly used as a recreational drug in countries, where it is commonly prescribed and therefore available. 
After oral administration tilidine is rapidly absorbed, which results in an onset of action of 10-15 minutes and lasts for about 4-6 hours. The maximum effect is reached after about 25-50 minutes.  Oral tilidine has an analgesic potency of 0.2, which means that 100mg provide the same analgesia as 20mg of oral morphine. Parental administration is very uncommon, due to the high first-pass effect. 
Tilidine itself is only a weak µ-opioid agonist. Its pharmacological activity when administered is mediated by its active major metabolite nortilidine, which is further metabolised to the also active bisnortilidine. Tilidine is therefore a prodrug. The demethylation of tilidine to nortilidine and bisnortilidine occures in the liver and is catalysed by the Cytochrome P450 family of enzymes, mainly by CYP3A4 CYP2D6 and CYP2C19. 
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