Chemistry:Tiletamine

From HandWiki

Tiletamine is a dissociative anesthetic and pharmacologically classified as an NMDA receptor antagonist.[1] It is an arylcyclohexylamine chemically related to ketamine.[2]

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.[3][4][5] It is sometimes used in combination with xylazine (Rompun) to chemically immobilize large mammals such as polar bears[6] and wood bison.[7] 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]

Use

Tiletamine is typically used in combination with the benzodiazepine zolazepam, as it often causes adverse reactions such as discomfort, muscle rigidity, and tremors when used alone.[8] In combination with zolazepam, tiletamine provides ~30 minutes of anaesthesia with a wide safety profile. In cats, zolazepam has a longer effect than tiletamine, whilst the inverse is true in dogs. This leads to cats having a smoother recovery from the drug combination than dogs, in general.[9]

Pharmacology

Tiletamine acts as an NMDA receptor antagonist at the PCP1 site, blocking the flow of ions.[10] 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.[11]

Society and culture

Recreational use of telazol has been documented.[12] Animal studies have also shown that tiletamine produces rewarding and reinforcing effects.[13] Products that combine Tiletamine and Zolazepam are classified as Schedule III controlled substances in the United States.[14] tiletamine is unscheduled in the US.[15]

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.[16]

See also

References

  1. ↑ "Paradoxical convulsant action of a novel non-competitive N-methyl-D-aspartate (NMDA) antagonist, tiletamine". Brain Research 461 (2): 343–348. October 1988. doi:10.1016/0006-8993(88)90265-X. PMID 2846121. 
  2. ↑ CID 26533 from PubChem
  3. ↑ 3.0 3.1 "Tiletamine". Drugs.com. https://www.drugs.com/international/tiletamine.html. 
  4. ↑ "Telazol--a review of its pharmacology and use in veterinary medicine". Journal of Veterinary Pharmacology and Therapeutics 16 (4): 383–418. December 1993. doi:10.1111/j.1365-2885.1993.tb00206.x. PMID 8126757. 
  5. ↑ "Tiletamine". Toxnet. U.S. National Library of Medicine. 21 January 2009. https://www.nlm.nih.gov/toxnet/index.html. 
  6. ↑ "Anesthesia of polar bears using xylazine-zolazepam-tiletamine or zolazepam-tiletamine". Journal of Wildlife Diseases 39 (3): 655–664. July 2003. doi:10.7589/0090-3558-39.3.655. PMID 14567228. 
  7. ↑ "Anesthesia of wood bison with medetomidine-zolazepam/tiletamine and xylazine-zolazepam/tiletamine combinations". The Canadian Veterinary Journal = la Revue Veterinaire Canadienne 41 (1): 49–53. January 2000. doi:10.4141/cjas61-007. PMID 10642872. 
  8. ↑ "A narrative review of the clinical applications of tiletamine-zolazepam in canine and feline anesthesia". Frontiers in Veterinary Science 13. 2026. doi:10.3389/fvets.2026.1807278. PMID 42382112. 
  9. ↑ Saunders Handbook of Veterinary Drugs (4th ed.). Elsevier. 2016. ISBN 978-0-323-24485-5. 
  10. ↑ "NMDA Receptor Antagonists: Emerging Insights into Molecular Mechanisms and Clinical Applications in Neurological Disorders". Pharmaceuticals (Basel, Switzerland) 17 (5): 639. May 2024. doi:10.3390/ph17050639. PMID 38794209. 
  11. ↑ "Comparison of the Psychopharmacological Effects of Tiletamine and Ketamine in Rodents". Neurotoxicity Research 32 (4): 544–554. November 2017. doi:10.1007/s12640-017-9759-0. PMID 28577066. 
  12. ↑ "Abuse of telazol: an animal tranquilizer". Journal of Toxicology. Clinical Toxicology 39 (4): 399–402. 2001. doi:10.1081/clt-100105161. PMID 11527235. 
  13. ↑ "Rewarding and reinforcing effects of the NMDA receptor antagonist-benzodiazepine combination, Zoletil®: difference between acute and repeated exposure". Behavioural Brain Research 233 (2): 434–442. August 2012. doi:10.1016/j.bbr.2012.05.038. PMID 22659394. 
  14. ↑ "Lists of: Scheduling Actions, Controlled Substances, Regulated Chemicals". Drug Enforcement Administration. http://www.deadiversion.usdoj.gov/schedules/orangebook/orangebook.pdf. 
  15. ↑ "Schedules of Controlled Substances: Placement of Preparations Which Contain Both Tiletamine and Zolazepam into Schedule III". Drug Enforcement Administration. January 21, 1987. http://isomerdesign.com/Cdsa/FR/52FR2221.pdf. 
  16. ↑ "Severe tremors induced by tiletamine e-cigarette and alcohol use: a case report". Frontiers in Psychiatry 16. 2025. doi:10.3389/fpsyt.2025.1537822. PMID 40248598. 

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