Products
Tilidine is commercially available as an oral solution (Valoron). It has been approved in many countries since 1975. In Germany, tilidine fix is combined with the opioid antagonist naloxone to prevent abuse (Valoron N).
Structure and properties
Tilidine (C17H23NO2, Mr = 273.4 g/mol) is present in drugs as tilidine hydrochloride hemihydrate, a racemate and white crystalline powder that is readily soluble in water. It is a prodrug and is converted in the organism to the active ingredient nortilidine.
Effects
Tilidine (ATC N02AX01) has analgesic and psychotropic properties. The effects are due to binding to μ-opioid receptors.
Indications
For the treatment of moderate to severe acute and persistent pain.
Abuse
Like all opioids, tilidine can be abused as a relaxant and psychoactive intoxicant.
Dosage
According to the prescribing information. The drops are taken four times daily with some liquid (Germany: up to six times daily).
Contraindications
- Hypersensitivity
- Opioid addiction
- Acute porphyria
- Respiratory depression
- Intestinal obstruction
- Acute abdomen
- Traumatic brain injury
- Increased intracranial pressure
- Concurrent treatment with MAO inhibitors.
For complete precautions, see the drug label.
Interactions
Drug-drug interactions are possible with central depressant drugs, alcohol, and MAO inhibitors. Tilidine is biotransformed by CYP3A4 and CYP2C19 to its active metabolite nortilidine. Corresponding interactions are observed.
Adverse effects
The most common potential adverse effects include dizziness, lightheadedness, drowsiness, fatigue, nausea, vomiting, constipation, abdominal pain, sweating, and respiratory depression at high doses.