Common brands: Tilidin, Valoron
Tilidine 200mg/16mg Stada is a synthetically produced active substance that belongs to the group of opioids. It has a pain-relieving effect. Doctors use it primarily when milder painkillers are not enough. To prevent misuse in the case of opioid dependence and side effects, tilidine is usually combined with its counterpart naloxone.
How tilidine works
Opioids such as tilidine achieve their analgesic effect by activating opioid receptors in the human body. The body’s own, but not structurally related, endorphins (endogenous painkillers) also bind to the same receptors. By activating the opioid receptors, tilidine indirectly inhibits the pain-mediating neuronal systems in the body.
The time to onset of action depends on the dosage form used (drops or tablets). In the body, tilidine is converted in the liver into the actual active substance nortilidine. The average duration of action is approximately three to five hours.
The active ingredient tilidine is used to relieve moderate to severe pain. Physicians prescribe the drug primarily when non-opioid analgesics (e.g., ibuprofen, diclofenac, paracetamol, metamizole) do not provide sufficient relief.
The active ingredient is available for use in drop or tablet form. To prevent misuse, tilidine is combined with naloxone in Germany. At very high doses or when the drug is injected, naloxone inhibits the effect of tilidine. Opiate or opioid addicts develop withdrawal symptoms as a result.
Tilidine was developed as a synthetic drug in the early 1970s. In the beginning, drops were marketed because tilidine dosing is easier with drops.
Because this substance, like any opioid, can cause dependence, a few years later the drug began to be discontinued in drug-dependent patients. Abuse is prevented by adding the antagonist naloxone. However, deaths have also occurred in opioid severely addicted patients, as severe withdrawal symptoms can result from naloxone.