Tilidine

**Semantic type:** Pharmacologic Substance

**Definition:** A synthetic opioid and a prodrug form of nortilidine, that can be used to treat moderate to severe acute and chronic pain. Upon administration, tilidine is metabolized to its active metabolite nortilidine, which crosses the blood-brain barrier (BBB), and binds to and activates the mu-opioid receptor. This induces anti-nociception responses mediated through inhibiting the release of various neurotransmitters such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin, and somatostatin.

**Synonyms:** - TILIDINE