Tiletamine

Tiletamine is a dissociative anesthetic and pharmacologically classified as an NMDA receptor antagonist.[1] It is related chemically to ketamine.[2] Tiletamine hydrochloride exists as odorless white crystals.

Tiletamine
(S)-tiletamine
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration		IV, IM, SC, Other
ATC code
  • none
Legal status
Legal status
Pharmacokinetic data
MetabolismLiver
ExcretionKidneys
Identifiers
  • 2-Ethylamino-2-(2-thienyl)cyclohexanone
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard100.034.559
Chemical and physical data
FormulaC12H17NOS
Molar mass223.33 g·mol−1
3D model (JSmol)
  • O=C2C(c1sccc1)(NCC)CCCC2
  • InChI=1S/C12H17NOS/c1-2-13-12(11-7-5-9-15-11)8-4-3-6-10(12)14/h5,7,9,13H,2-4,6,8H2,1H3 checkY
  • Key:QAXBVGVYDCAVLV-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

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]

Society and Culture

Recreational use of telazol has been documented.[8] Animal studies have also shown that tiletamine produces rewarding and reinforcing effects.[9] Products that combine Tiletamine and Zolazepam are classified as Schedule III controlled substances in the United States.[10] Otherwise, as noted by the DEA, tiletamine is unscheduled: “…[R]ules applicable to the scheduling of tiletamine and zolazepam as individual entities are not warranted [or in effect] at this time. Neither tiletamine nor zolazepam, as discrete substances, is perceived to pose a significant threat to the health and general welfare at this time…”[11]

References
  1. Klockgether T, Turski L, Schwarz M, Sontag KH, Lehmann J (October 1988). "Paradoxical convulsant action of a novel non-competitive N-methyl-D-aspartate (NMDA) antagonist, tiletamine". Brain Research. 461 (2): 343–348. doi:10.1016/0006-8993(88)90265-X. PMID 2846121. S2CID 41671395.
  2. CID 26533 from PubChem
  3. "Tiletamine". Drugs.com. Retrieved 5 January 2012.
  4. Lin HC, Thurmon JC, Benson GJ, Tranquilli WJ (December 1993). "Telazol--a review of its pharmacology and use in veterinary medicine". Journal of Veterinary Pharmacology and Therapeutics. 16 (4): 383–418. doi:10.1111/j.1365-2885.1993.tb00206.x. PMID 8126757.
  5. "Tiletamine". Toxnet. U.S. National Library of Medicine. 21 January 2009.
  6. Cattet MR, Caulkett NA, Lunn NJ (July 2003). "Anesthesia of polar bears using xylazine-zolazepam-tiletamine or zolazepam-tiletamine". Journal of Wildlife Diseases. 39 (3): 655–664. doi:10.7589/0090-3558-39.3.655. PMID 14567228.
  7. Caulkett NA, Cattet MR, Cantwell S, Cool N, Olsen W (January 2000). "Anesthesia of wood bison with medetomidine-zolazepam/tiletamine and xylazine-zolazepam/tiletamine combinations". The Canadian Veterinary Journal. 41 (1): 49–53. doi:10.4141/cjas61-007. PMC 1476335. PMID 10642872.
  8. Quail MT, Weimersheimer P, Woolf AD, Magnani B (2001). "Abuse of telazol: an animal tranquilizer". Journal of Toxicology. Clinical Toxicology. 39 (4): 399–402. doi:10.1081/clt-100105161. PMID 11527235. S2CID 21280839.
  9. de la Peña JB, Lee HC, de la Peña IC, Woo TS, Yoon SY, Lee HL, et al. (August 2012). "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. doi:10.1016/j.bbr.2012.05.038. PMID 22659394. S2CID 25425333.
  10. "Lists of: Scheduling Actions, Controlled Substances, Regulated Chemicals" (PDF). Drug Enforcement Administration. Retrieved 5 January 2012.
  11. "Schedules of Controlled Substances: Placement of Preparations Which Contain Both Tiletamine and Zolazepam into Schedule III" (PDF). Isomer Design. Drug Enforcement Administration. January 21, 1987. Archived (PDF) from the original on March 3, 2022. Retrieved January 16, 2023.
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