Lecture 9 Flashcards
Define the term sedation:
a level of central nervous system depression that facilitates clinical activity
Explain the mechanism of action of benzodiazepines:
They act as GABA agonists depressing central nervous system depression. They cause the inside of the neutron to become more negatively charged than the outside making them harder to active and thus has made it become inhibited
What is an example of a benzodiazepine?
diazepam, midazolam
Explain the mechanism of action of neuroleptics:
Neuroleptics are dopamine antagonists. Dopamine is used for brain reward pathways including motivation, purposefulnes and movements. The neuroleptics are also antagonists at other receptors e.g. alpha-1 adrenergic receptors.
Explain the mechanism of action of opioids
The opioids work on opioid receptors. u(mu ) and k(kappa) primarily. The central effects include central nervous system depression that causes sedation. The peripheral effects include actions on Ca and K channels to decrease the ascending pain pathways.
What is the effect of alpha-2-agonists?
The alpha-2-agonists are sedative by decreasing the central concentrations of NAdr. The a2 agonists bind to the a2 receptor and induces the auto-regulatory inhibitory feedback mechanism to decrease the release of NAdr. The major central effects of NAdr include altertness, arousal and pain perceptions the a2 agonist ultimately leads to sedation and analgesia.
What are some examples of alpha-2 agonists?
Medetomidine and dexmedetomidine: small animals
Detomidine and xylazine: horses
Xylazine: ruminants
What are the CVS effects of Benzodiazepines?
Virtually none
What are the CVS effects of Opiods?
minimal - well suited for pain relief during shock
What are the CVS effects of neuroleptics?
vasodilation through effects on alpha1-receptors causing hypotension
What are the CVS effects of alpha-2-agonists?
- peripherally mediated (alpha-2 receptors in blood vessels) strong short lived vasoconstriction
- IV infusion causes increased blood pressure
- IV bolus causes increased and then decreased BP
- Bradycardia
Name a benzodiazepine antagonist and common on the necessity of having one:
Flumazenil - almost never needed due to the safety of this class of drug
Name an opioid antagonist:
Naloxone- antagonist at all opioid receptor types
Name an alpha-2 antagonist:
Atipamezole (medetomidine and dexmedetomidine) is highly effective and rapidly acting
Yohimbine (for xylazine) less effective
Name a neuroleptic antagonist:
No reversal agent available