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Tilidine
Tilidine is a synthetic opioid analgesic used mainly for the treatment of moderate to severe pain, both acute and chronic. It is considered a low-to-medium-potency opioid relative to morphine. In some countries it is formulated in a fixed combination with naloxone, intended to lower abuse liability by antagonizing the opioid if the preparation is injected, though the effectiveness of this approach has been questioned. It is also used in the treatment of restless legs syndrome.
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
With slow-release tablets there is a risk of overdose due to delayed release of the active ingredient. The perceived effect is extremely different depending on the person and tolerance. In combination preparations with naloxone, the desired psychoactive effect of the tilidine is cancelled out from approx. 300-400 mg by the naloxone contained. First-time users should take low doses, as the risk of respiratory arrest is increased. Start with a low dose and wait for the effect and tolerance before adding more; do not exceed the maximum daily dose. Do not rely on dosage information from regular opioid users, whose doses are much higher due to habituation or dependence and can be fatal for new users. After a period of abstinence, take a much lower dose. Considered a low-to-medium-potency opioid, tilidine has an oral potency of about 0.2, that is, 100mg orally is equianalgesic to approximately 20mg morphine sulfate orally. Tilidine is subject to a pronounced first-pass effect and is converted to the more active metabolite nortilidine via CYP3A4 and CYP2C19; inhibition of these enzymes can alter efficacy and tolerability. The elimination half-life for nortilidine is 3-5 hours and is prolonged in liver impairment.
Duration
Subjective Effects
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Tilidine produces an opioid experience centred on pain relief, with euphoria and anxiety relief emerging at higher doses. The perceived effect varies greatly between individuals and with tolerance. In combination preparations containing naloxone, the psychoactive effect is cancelled out above roughly 300-400 mg, and injecting such preparations instead precipitates withdrawal.
Physical
Drowsiness, tiredness, and dizziness are common, alongside nausea and vomiting. Excessive sweating, tremor, and a drop in blood pressure may also occur.
Cognitive
The headspace is described as euphoric, anxiety-relieved, and disinhibited; at higher doses this disinhibition can shade into aggression, loss of control, and increased risk-taking. Confusion and nervousness are also reported.
Emotional
Multisensory
Pharmacology
Pharmacodynamics
Tilidine is itself only a weak opioid and functions primarily as a prodrug, acting through its active metabolite nortilidine, which binds opioid receptors in the central and peripheral nervous systems to suppress the perception and transmission of pain. Analgesic activity resides in the (1S,2R)-isomer, dextilidine. It is considered a low-to-medium-potency opioid, with an oral potency of roughly 0.2 relative to morphine, such that 100 mg orally is approximately equianalgesic to 20 mg of oral morphine sulfate. In some markets tilidine is formulated with the opioid receptor antagonist naloxone, at a ratio intended not to impair the analgesic effect when taken orally but to antagonize tilidine's effects if the preparation is injected; the effectiveness of this approach has been called into question.
Pharmacokinetics
Tilidine is rapidly absorbed after oral administration and undergoes a pronounced first-pass effect, being rapidly metabolized in the liver and gut to its more active metabolite nortilidine and subsequently to bisnortilidine. Conversion to nortilidine involves CYP3A4 and CYP2C19, so inhibition of these enzymes can alter the efficacy and tolerability profile of the drug. Around 90% of tilidine is metabolized and eliminated renally, with the remainder appearing in the feces. In hepatic insufficiency, peak nortilidine plasma concentrations are lower and the half-life is prolonged, and in severe impairment the formation of active nortilidine may be too low to produce adequate analgesia; naloxone in combination preparations may also be inactivated insufficiently, further antagonizing nortilidine's effect. The reverse ester of tilidine is also a prodrug.
Interactions
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Harm Potential
History & Culture
Tilidine has been marketed under the brand name Valoron and other names, and has seen medical use mainly in Belgium, Bulgaria, Germany, Albania, Luxembourg, and South Africa. In Germany it is sold in a fixed combination with naloxone as Valoron N and its generics, an arrangement intended to reduce…
Legality
Article Status
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Recent changes7 human edits · latest
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24 January 2026
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
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