Tiletamine
Also called Telazol
Part of the metabolic pathway of Tiletamine. See the timeline on the metabolic highway.
Dosage
Intramuscular
Oral
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Oral Light: 10-25mg Common: 25-50mg Strong: 50-100mg+ | Intramuscular Light: 2.5-5mg Common: 5-10mg Strong: 10-20mg+ TS
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Duration
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Mixing
Acute combinations: what happens when these are taken close together. Entries backed by a medical journal or agency are listed first.
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Risks and toxicity
Testing
Effects
Overview
A relatively rare dissociative anesthetic, pharmacologically classified as an NMDA receptor antagonist. It is related to other anesthetics in this family such as Ketamine and phencyclidine. Has been used to cut Ketamine, in which case it may cause additional nausea. In Veterinary practice it is mixed with Zolazolam, a potent anaesthetic at a 1:1 ratio. TS
Tiletamine is a dissociative anesthetic and pharmacologically classified as an NMDA receptor antagonist. It is an arylcyclohexylamine chemically related to ketamine.[1]
It is used in veterinary medicine in the combination product Telazol (tiletamine/zolazepam, 50 mg/ml of each in 5 ml vial) as an injectable anesthetic for use in cats and dogs. It is sometimes used in combination with xylazine (Rompun) to chemically immobilize large mammals such as polar bears and wood bison. Telazol is the only commercially available tiletamine product in the United States. It is contraindicated in patients of an ASA score of III or greater and in animals with CNS signs, hyperthyroidism, cardiac disease, pancreatic or renal disease, pregnancy, glaucoma, or penetrating eye injuries.[3–7] WP
History
Legal status
Society and culture
Recreational use of telazol has been documented. Animal studies have also shown that tiletamine produces rewarding and reinforcing effects. Products that combine Tiletamine and Zolazepam are classified as Schedule III controlled substances in the United States. tiletamine is unscheduled in the US.[8–11] WP
The use of pure tiletamine outside of the veterinary mixes has been documented being smoked in e-cigarettes, with both abuse and withdrawal causing severe limb tremors.[12] WP
Pharmacology
Pharmacology
Tiletamine acts as an NMDA receptor antagonist at the PCP₁ site, blocking the flow of ions. It acts at this site with a Kᵢ of 55-83 nM, suggesting that it is 6-8x more potent than ketamine there. Compared to other NMDA receptor antagonists such as dizocilpine, PCP, and ketamine, tiletamine does not significantly impact the release or metabolism of dopamine.[13]
Chemistry
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References
- Journal / agency Klockgether T, Turski L, Schwarz M, Sontag KH, Lehmann J. Paradoxical convulsant action of a novel non-competitive N-methyl-D-aspartate (NMDA) antagonist, tiletamine. Brain Research. October 1988. doi:10.1016/0006-8993(88)90265-X · PMID 2846121
- Other PubChem 26533
- Other Tiletamine
- Journal / agency Lin HC, Thurmon JC, Benson GJ, Tranquilli WJ. Telazol--a review of its pharmacology and use in veterinary medicine. Journal of Veterinary Pharmacology and Therapeutics. December 1993. doi:10.1111/j.1365-2885.1993.tb00206.x · PMID 8126757
- Journal / agency Tiletamine. 21 January 2009
- Journal / agency Cattet MR, Caulkett NA, Lunn NJ. Anesthesia of polar bears using xylazine-zolazepam-tiletamine or zolazepam-tiletamine. Journal of Wildlife Diseases. July 2003. doi:10.7589/0090-3558-39.3.655 · PMID 14567228
- Journal / agency Caulkett NA, Cattet MR, Cantwell S, Cool N, Olsen W. Anesthesia of wood bison with medetomidine-zolazepam/tiletamine and xylazine-zolazepam/tiletamine combinations. The Canadian Veterinary Journal = la Revue Veterinaire Canadienne. January 2000. doi:10.4141/cjas61-007 · PMID 10642872 · PMC1476335
- Journal / agency Quail MT, Weimersheimer P, Woolf AD, Magnani B. Abuse of telazol: an animal tranquilizer. Journal of Toxicology. Clinical Toxicology. 2001. doi:10.1081/clt-100105161 · PMID 11527235
- Journal / agency de la Peña JB, Lee HC, de la Peña IC, Woo TS, Yoon SY, Lee HL, Han JS, Lee JI, Cho YJ, Shin CY, Cheong JH. Rewarding and reinforcing effects of the NMDA receptor antagonist-benzodiazepine combination, Zoletil®: difference between acute and repeated exposure. Behavioural Brain Research. August 2012. doi:10.1016/j.bbr.2012.05.038 · PMID 22659394
- Other Lists of: Scheduling Actions, Controlled Substances, Regulated Chemicals
- Harm reduction site Schedules of Controlled Substances: Placement of Preparations Which Contain Both Tiletamine and Zolazepam into Schedule III. January 21, 1987
- Journal / agency Zhou B, Yang S, Zhou X, Chen Q, Tu E, Zhang B, Shi L, Zhou X. Severe tremors induced by tiletamine e-cigarette and alcohol use: a case report. Frontiers in Psychiatry. 2025. doi:10.3389/fpsyt.2025.1537822 · PMID 40248598 · PMC12004490
- Journal / agency Egunlusi AO, Joubert J. NMDA Receptor Antagonists: Emerging Insights into Molecular Mechanisms and Clinical Applications in Neurological Disorders. Pharmaceuticals. May 2024. doi:10.3390/ph17050639 · PMID 38794209 · PMC11124131
- Journal / agency Popik P, Hołuj M, Kos T, Nowak G, Librowski T, Sałat K. Comparison of the Psychopharmacological Effects of Tiletamine and Ketamine in Rodents. Neurotoxicity Research. November 2017. doi:10.1007/s12640-017-9759-0 · PMID 28577066 · PMC5602060
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