alpha 2 agonists Flashcards
List the alpha 2 agonists
Clonidine, Guanabenz, Guanfacine (also methyldopa is an alpha 2 agonist prodrug)
There are alpha 2 autoreceptors and alpha 2 heteroreceptors. What do the auto receptors do?
An autoreceptor is on the presynaptic neuron from which the neurotransmitter was released. It acts as a negative feedback receptor. When activated, alpha 2 auto receptors inhibit the release of NE from presynaptic neurons
There are alpha 2 auto and heteroreceptors. What do the heteroreceptors do?
Alpha 2 heteroreceptors are on non adrenergic neurons that are adjacent to the presynaptic neuron. They bind up the NE that was released from the presynaptic neuron so that it will not get in the way of that neuron’s native neurotransmitter
Alpha 2 heteroreceptor induces?
bradycardia, hypotension
What MUST alpha 2 agonists do in order to lower BP?
They MUST penetrate the BBB because alpha 2 agonists in the peripheral vasculature actually vasoconstrict the blood vessels. In the CNS, alpha 2 agonists decrease sympathetic tone and decrease BP
There are six clinical effects of alpha 2 agonsits. List them
- Lower BP
- No reflex tachycardia
- CO and RBF are unaffected
- Decrease plasma renin
- Regression of LVH
- Salt & Water retention
adverse effects of alpha 2 agonists?
somnolence, dry mouth
The prodrug methyldopa has a contraindication for anemic patients that are taking an iron compound. Why?
Iron chelates the alpha-methylnorepinephrine (active metabolite of methyldopa)
All these alpha 2 receptors that we’re talking about that lower BP when activated are located?
Vasomotor center of the medulla
Activation of alpha 2 in the peripheral vasculature would?
Vasoconstrict