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tilidine + naloxone
- Development stage
- Unknown
- Lead developer
- Hebei Aoxing Pharmaceutical Group
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Tilidine + naloxone is a fixed-dose combination analgesic used for the management of moderate to severe pain. Tilidine is a synthetic opioid prodrug that undergoes rapid first-pass metabolism in the liver to form nortilidine, a potent agonist at the mu-opioid receptor responsible for the drug's analgesic effects. Naloxone, an opioid antagonist, is included in the formulation to deter intravenous abuse. When administered orally, naloxone undergoes extensive first-pass metabolism and remains largely inactive, allowing the analgesic effect of tilidine to predominate. However, if the drug is administered parenterally, naloxone becomes systemically available and antagonizes the effects of nortilidine, potentially precipitating withdrawal symptoms in opioid-dependent individuals. This combination is widely used in Germany and other European markets, and is also produced by regional manufacturers such as Hebei Aoxing Group Pharmaceutical in China.
- Brand names
- Tilidin-NaloxonTiliduraTilinovoTiligen
- Other names
- tilidine hydrochloride + naloxone hydrochloride
02
Targets
KOR (Kappa opioid receptor)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)
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