metadata toggle
Pharmacological particulars
Pharmacotherapeutic group: Medication for the nervous system, other general anaesthetics, combinations.
ATCvet-code: QN01AX99
Pharmacodynamic properties
Tiletamine is a compound belonging to the family of phencyclidines and is pharmacologically similar to ketamine. It antagonises NMDA-type receptors (N-methyl-D-aspartate) of the excitatory neurotransmitter, glutamic acid. It generates a so-called dissociative anaesthesia because it depresses certain cerebral regions such as the thalamus and the cortex whilst other regions, in particular the limbic system, remain active.
Zolazepam is a benzodiazepine and pharmacologically similar to diazepam. It has a sedative, anxiolytic and muscle-relaxing action.
Associations in proportions of 1/1 of two compounds with complementary actions enable the following effects:
- fast catalepsy, without agitation, followed by relaxation of the muscle,
- moderate superficial, immediate and visceral analgesia,
- surgical anaesthesia with muscle relaxation, preservation of laryngeal, pharyngeal and palpebral reflexes, without bulbar depression.
Pharmacokinetic particulars
After intramuscular administration of 10 mg of tiletamine per kg and 10 mg of zolazepam per kg, the peak plasma concentrations of tiletamine and zolazepam (Cmax) are reached within 30 minutes in dogs and cats, indicating fast absorption.The terminal half-life of tiletamine (T1/2) is 2.5 hours in cats. It is shorter in dogs (1.2 to 1.3 hour).The terminal half-life of zolazepam is longer in cats (4.5hours) than in dogs (< 1 hour).Both active substances are extensively metabolised. Less than 4% of the dose is found in a non-metabolised form in urine and less than 0.3% in faeces.