Tilidine
Also called Tilidate, Tilidin, Valoron, Valtran, trans-Tilidine, IDS-NT-003, Dextilidine
Part of the metabolic pathway of Tilidine. See the timeline on the metabolic highway.
Enzymes that break it down: CYP3A4 and CYP2C19. Wikipedia’s drug infobox says: “Metabolized by the liver, mostly via the enzymes CYP3A4 and CYP2C19” (revision 1365331528).
Dosage
Oral
TripSit dose text
TripSit's factsheet also states its doses as text.
Tilidine dose Oral Light: 25-50mg Common: 50-100mg Strong: 100-200mg. TS
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Duration
TripSit factsheet
Mixing
For best safety practice, don't mix this drug with other depressants.
Why: respiratory depression. PsychonautWiki says:
- “Respiratory depression (also known as hypoventilation) can be described as a reduced urge to breathe that can be fatal depending on its intensity.” (PsychonautWiki, Respiratory depression, revision 150612)
- “... otherwise safe dosages of these compounds can become fatal when combined with even small amounts of other classes of depressant. For example, benzodiazepines combined with opioids are an extremely common cause of fatal respiratory depression. It is therefore strongly discouraged to combine these depressants at any dosage range.” (PsychonautWiki, Respiratory depression, revision 150612)
- “The most common cause of substance-related deaths is the combination of depressants (such as opiates, benzodiazepines, or alcohol) with other depressants.” (PsychonautWiki, Responsible drug use, revision 168206)
- “This combination potentiates the muscle relaxation, amnesia, sedation, and respiratory depression caused by one another. At higher doses, it can lead to a sudden, unexpected loss of consciousness along with a dangerous amount of depressed respiration.” (PsychonautWiki, dangerous interactions table, "Depressants" row, revision 156847)
Quotes from PsychonautWiki, CC BY-SA 4.0.
Acute combinations: what happens when these are taken close together. Entries backed by a medical journal or agency are listed first.
Backed by medical journals
TripSit combination chart
TripSit rates each pairing. Only pairings with a number carry a citation from TripSit. See the whole chart; TripSit's own notes are on combo.tripsit.me.
Risks and toxicity
TripSit factsheet
- Avoid
- All other CNS depressants. TS
Testing
Effects
Overview
Synthetic opioid, used mainly for treatment of moderate to severe pain. In some countries it's mixed with Naloxone to lower the abuse liability. Though in some only Tilidine. Roughly 0.2 - 1 on the potency scale to Morphine. (So 20mg's of Morphine to 100mg's Tilidine) TS
Tilidine, sold under the brand-name Valoron among others, is a synthetic opioid analgesic, used mainly in Belgium, Bulgaria, Germany, Albania, Luxembourg, and South Africa for the treatment of moderate to severe pain, both acute and chronic. Its onset of pain relief after oral administration is about 10-15 minutes and peak relief from pain occurs about 25-50 minutes after administration.[1]
History
Legal status
Pharmacology
Pharmacology
Considered a low-to-medium-potency opioid, tilidine has the oral potency of about 0.2, that is, a dose of 100mg p.o. is equianalgesic to approximately 20mg morphine sulfate orally. It is administered orally (by mouth), rectally (by a suppository), or by injection (SC, IM, or slowly IV).[4] WP
Tilidine itself is only a weak opioid, but is rapidly metabolized in the liver and gut to its active metabolite nortilidine and then to bisnortilidine. It is the (1S,2R)-isomer (dextilidine) that is responsible for its analgesic activity. Nortilidine binds to opiate receptors in the central and peripheral nervous systems and suppresses pain perception and transmission.[5–8] WP
To purportedly counteract the abuse potential, tilidine is used in combination with the opioid receptor antagonist naloxone. The mixing ratio with naloxone is chosen so that the analgesic effect of tilidine is not impaired. WP
Pharmacokinetics
Tilidine is rapidly-absorbed after oral administration and is subject to a pronounced first-pass effect. WP
The conversion of tilidine into the more active metabolite nortilidine occurs with the participation of CYP3A4 and CYP2C19. The inhibition of these enzymes can thus alter the efficacy and tolerability profile of tilidine. The analgesic effect occurs after 10-15 minutes. After oral administration of 100mg tilidine plus 8mg naloxone, the maximum effect is reached in about 25-50 minutes. The duration of action is given as 4-6 hours. WP
The elimination half-life for nortilidine is 3-5 hours. Tilidine is metabolized to 90% and eliminated renally. The rest appears in the feces. WP
Depending on the extent of the impairment, the maximum concentration of nortilidine in plasma is lower in insufficient liver function than in healthy individuals and the half-life is prolonged. In case of severe hepatic insufficiency the therapy is questionable. In these cases, it is possible that the formation of active nortilidine may be so low that the analgesic effect is insufficient. In addition, in the combination preparations with naloxone, the inactivation of the same can only be insufficient. The consequent antagonism of nortilidine’s effect can lead to a further loss of activity.[9] WP
Chemistry
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References
- Other Tilidine Hydrochloride. 13 December 2013
- Other Tilidine
- Other Tilidin N Sandoz® DP Lösung zum Einnehmen. December 2012
- Other Waldvogel HH. Analgetika, Antinozizeptiva, Adjuvanzien: Handbuch für die Schmerzpraxis. 2001
- Other Buschmann, H. Analgesics: From Chemistry and Pharmacology to Clinical Application. 2002
- Journal / agency Schulz R, Bläsig J, Wüster M, Herz A. The opiate-like action of tilidine is mediated by metabolites. Naunyn-Schmiedeberg's Archives of Pharmacology. September 1978. doi:10.1007/bf00495543 · PMID 212687
- Other dextilidine - C17H23NO2 - ChemSpider
- Journal / agency Satzinger G. Drug discovery and commercial exploitation. Drug News & Perspectives. May 2001. doi:10.1358/dnp.2001.14.4.858403 · PMID 12819791
- Other Tilidin
Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), TripSit factsheets, PubChem (public domain). Each value links to the exact revision it came from.