Sedatives Flashcards
What are the 2 mechanisms of action of sedatives?
Antagonise excitatory neurotransmitters
Potentiate inhibitory neurotransmitters
Name the 4 groups of sedatives and give examples of drugs from each class
Phenothiazines - ACP
Alpha 2 agonists - Medetomidine, Dexmedatomidine, Xylazine
Benzodiazepines - Diazdepam, Midazolam
Butyrophenones - Azaperone, Hypnorm
Describe the mechanism of action of ACP
Non-selective dopamine antagonist causing tranquilisation/sedation and anti-emesis
no analgesia
Describe the pharmacokinetics of ACP
Solution for injection IM, IV, SC Oral paste in horses Duration of action - 4hrs Hepatic metabolism Potentiates opioids, injectable and inhaled anaesthetics
What are the effects of ACP?
CV - vasodilation (due to alpha 1 antagonist), hypotension, variable effect on HR, antiarrhythmic (increases the threshold for adrenaline induced arrhythmias)
RESP - min direct effect
GIT - decreases smooth muscle activity, antisialogogue
Hypothermia, priapism, decreased PCV
What are the clinical indications for using ACP?
Premed, sedation, motion sickness
What are the contraindications for using ACP?
Hypovolaemia , breeding bulls/stallions, giant breeds have an increased sensitivity to lower doses
Describe the mechanism of action of the alpha 2 agonists
Agonise alpha 2 adrenergic receptors.
CNS - presynaptic - reduce noradrenaline release
Peripheral - act on pre and postsynaptic receptors
Describe the pharmacokinetics of alpha 2s
IM, IV, SC, epidural, transmucosal
High first pass metabolism with oral admin
Can give antagonists to reverse action
Marked anaesthetic sparing effect
What are the effects of the alpha 2s?
CNS - sedation is mild-profound, analgesia has a shorter duration than sedation, muscle relaxation
CVS - peripheral vasoconstriction, increased blood pressure, arrthymias (sinus and AV block)
RESP -mild-mod depression, arterial hypoxaemia in ruminants
GIT - v+, decreased motility
Endocrine - inhibits ADH and insulin release
Uterine contraction
What are the clinical indications for using alpha 2s?
Premed, sedation, analgesia, offset ketamine hypertonicity
What are the contradindications associated with using alpha 2s?
Reserved for use in young, healthy patients, cases with CV dysfunction
Describe the differences between different alpha 2 drugs
Duration: xylazine
What are the differences between detomidine and medetomidine
Medetomidine is a racemic mixture
May delay hepatic metabolism of other drugs
May decrease activity of dexmedetomidine
May contribute to undesirable cardiac effects
Dex is more potent
Describe the mechanism of action of benzodiazepines
Potentiates activity of inhibitory NT GABA