Tiletamine

Tiletamine is a dissociative anesthetic and pharmacologically classified as an NMDA receptor antagonist. It is related chemically to ketamine. Tiletamine hydrochloride exists as odourless white crystals.

Pharmacology

Tiletamine is a non-competitive NMDA receptor antagonist. Non-competitive here refers to the drug binding to a site other than the active site, which changes the shape and function of the receptor. The NMDA receptor is a glutamate receptor and ion channel protein found in nerve cells. It is activated when glutamate and glycine (or D-serine) bind to it, and when activated it allows positively charged ions to flow through the cell membrane. The NMDA receptor is very important for controlling synaptic plasticity and memory function.

Veterinary use

Tiletamine 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 tranquilize large mammals such as polar bears and wood bison. Tiletamine products are classified as Schedule III controlled substances in the United States.

Side effects

Tiletamine has similar side effects to other NMDA receptor antagonists. In humans, health effects include visual disturbances, confusion, euphoria, depersonalization, excitation, and potentially serious changes in heart function and respiration.

See also

• Veterinary medicine
• Anesthesia
• NMDA receptor antagonist

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