Zolazepam
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Collated from TripSit, Pharmacology, DailyMed. Where sources differ (e.g. dosing), Compare shows them side by side.
A substance that is structurally related to benzodiazepines. Is only used in Veterinary medicine. It is usually used in tandem with either the potent NMDA antagonist Tiletamine (at a 1:1 ratio) or with the α2 adrenergic receptor agonist Xylazine. Is roughly around four times the potency of Diazepam. Yet is water soluable.TS
Insufflated
Route dataTripSit
| Threshold | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| — | 1–3 mg | 3–6 mg | 6–12 mg | —+ |
Intramuscular
Route dataTripSit
| Threshold | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| — | 1–3 mg | 3–5 mg | 5–10 mg | —+ |
Oral
Route dataTripSit
| Threshold | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| — | 2.5–5 mg | 5–10 mg | 10–20 mg | —+ |
Mechanism of actionDM
Tzed (tiletamine and zolazepam for injection) is a rapid-acting anesthetic combination of tiletamine hydrochloride and zolazepam hydrochloride. Tiletamine hydrochloride is a dissociative anesthetic agent whose pharmacologic action is characterized by profound analgesia, normal pharyngeal-laryngeal reflexes and cataleptoid anesthesia. The anesthetic state produced does not fit into the conventional classification of stages of anesthesia, but instead Tzed produces a state of unconsciousness which has been termed "dissociative" anesthesia in that it appears to selectively interrupt association pathways to the brain before producing somesthetic sensory blockade.
Cranial nerve and spinal reflexes remain active; however, these reflexes must not be confused with inadequate anesthesia. Analgesia results from apparent selective interruption of sensory inputs to the brain and usually persists after the anesthetic effect has subsided.
Protective reflexes, such as coughing and swallowing, are maintained under tiletamine anesthesia. Other reflexes, e.g., corneal, pedal, are maintained during tiletamine anesthesia, and should not be used as criteria for judging depth of anesthesia. The eyes normally remain open with the pupil dilated. It is suggested that a bland ophthalmic ointment be applied to the cornea if anesthesia is to be prolonged.
Used alone, tiletamine hydrochloride does not provide adequate muscle relaxation for abdominal surgical procedures. When combined with zolazepam hydrochloride, good muscle relaxation is generally attained during the phase of deep surgical anesthesia.
Pharmacokinetics
AbsorptionDM
The pharmacokinetics of tiletamine and zolazepam injectable solution was evaluated in 12 healthy adult Beagle dogs, following a single intravenous (IV) administration of 2.2 mg/kg bodyweight, which is equivalent to 1.1 mg/kg for both tiletamine hydrochloride and zolazepam hydrochloride. After administration of 2.2 mg/kg tiletamine and zolazepam IV, the initial mean concentration of tiletamine (C0) was 1018 ng/mL, the systemic clearance (CL) was 6223 mL/kg/h, the area under the curve to the last measured concentration (AUC 0-last) was 178 ng*hr/mL, and steady state volume of distribution (Vss) was 3250 mL/kg. The mean elimination half-life of tiletamine was 0.87 hours. For zolazepam, the mean C0 was 2594 ng/mL, CL was 1993 mL/kg/h and Vss was 604 mL/kg. The mean elimination half-life of zolazepam was 0.41 hours. The mean C0 and AUC0-t(last) were approximately 2.5 and 3 times, respectively, greater for zolazepam than for tiletamine. However, the mean half-life (T1/2) of tiletamine was approximately 2.5 times longer than for zolazepam, resulting in quantifiable plasma concentrations up to 2 hours longer.
Pretreatment with an alpha2-agonist or phenothiazine followed by inhalant isoflurane has been shown to increase in the initial concentration of both tiletamine and zolazepam.
Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.