Tiletamine

Tiletamine
Systematic (IUPAC) name
2-ethylamino-2-(2-thienyl) cyclohexanone
Clinical data
AHFS/Drugs.com International Drug Names
Routes of
administration		 IV, IM, SC, Other
Legal status
Legal status
Pharmacokinetic data
Metabolism Liver
Excretion Kidneys
Identifiers
CAS Number 14176-50-2 N
ATC code none
PubChem CID 26533
ChemSpider 24714 YesY
UNII 2YFC543249 YesY
KEGG D08596 YesY
Chemical data
Formula C12H17NOS
Molar mass 223.34 g/mol
 NYesY (what is this?)  (verify)

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 odourless white crystals.

It is used in veterinary medicine in the compound 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 tranquilize 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]

Abuse of Telazol has been documented.[8] Animal studies have also shown that tiletamine produces rewarding and reinforcing effects.[9] Tiletamine products are classified as Schedule III controlled substances in the United States.[10]

See also

References

  1. ↑ Klockgether, Thomas; Turski, Lechoslaw; Schwarz, Michael; Sontag, Karl-Heinz; Lehmann, John (1 October 1988). "Paradoxical convulsant action of a novel non-competitiveN-methyl-d-aspartate (NMDA) antagonist, tiletamine". Brain Research 461 (2): 343–348. doi:10.1016/0006-8993(88)90265-X. PMID 2846121.
  2. ↑ NIH Pubchem entry for Tiletamine
  3. 1 2 "Tiletamine entry at Drugs.com". Retrieved 5 January 2012.
  4. ↑ Lin HC, Thurmon JC, Benson GJ, Tranquilli WJ. Telazol: a review of its pharmacology and use in veterinary medicine. J Vet Pharmacol Ther. 1993 Dec;16(4):383-418. Review. PMID 8126757
  5. ↑ NIH Tiletamine entry in Toxnet Page last reviewed 1/21/2009
  6. ↑ Cattet, M.R.; Caulkett, N.A.; Lunn, N.J. (July 2003). "Anesthesia of polar bears using xylazine-zolazepam-tiletamine or zolazepam-tiletamine.". Journal of wildlife diseases 39 (3): 655–64. doi:10.7589/0090-3558-39.3.655. PMID 14567228.
  7. ↑ Caulkett, N.A.; Cattet, M.R.; 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/La revue veterinaire canadienne 41 (1): 49–53. 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.
  9. ↑ 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 (2012). "Rewarding and reinforcing effects of the NMDA receptor antagonist-benzodiazepine combination, Zoletil®: difference between acute and repeated exposure". Behavioural Brain Research 233 (2): 434–42. doi:10.1016/j.bbr.2012.05.038. PMID 22659394.
  10. ↑ "Lists of: Scheduling Actions, Controlled Substances, Regulated Chemicals" (PDF). Drug Enforcement Administration. Retrieved 5 January 2012.

External links


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