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Chapter 19
Indirect-Acting Antiadrenergic Drugs
7
Medical
Graduate
09/11/2014

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Term
-What are the indirect-acting antiadrenergic agents?

-What are the 2 types?
Definition
-drugs that prevent the activation of peripheral adrenergic receptors, but by mechanisms that do NOT involve direct interaction with peripheral receptors

-adrenergic neuron-blocking agents (decrease NE release)
-centrally acting a2 agonists (reduce impulses along sympathetic nerves)
Term
-What are centrally acting a2 agonists?
-How do they work? and what are the effects similar to?
-Whats the primary use?

ex?
Definition
-Type of indrect-acting antiadrenergic agent
-Reduce firing of sympathetic neurons, similar effects to those of the direct-acting adrenergic receptor blockers
-HTN

-clonodine, guanfacine, methyldopa
Term
Clonidine: mechanism of antihypertensive action?

-pharm effects?

-therapeutic uses?

-adverse effects?

-pregnancy?
Definition
-selective activation of a2 receptors in CNS
-reduces sympathetic outflow to blood vessels and heart

-bradcardia and decrease CO, minimal ortho hypotension

-uses: hypertension and SEVERE PAIN

-adverse: drowsiness, dry mouth, REBOUND HTN...must withdraw slowly over 2-4 days!!

-contraindicated
Term
Guanfacine?

indication?
Definition
-similar to clonidine (centrally active a2 agonist, reducing impulses along nerves)

-HTN, ADHD
Term
Methyldopa: MOA?
-pharm effects?


indications?

Adverse effects?

pregnancy?
Definition
-not really a centrally active a2 agonist (reducing impulses along nerves) but can be taken up into the brainstem and converted into a2 agonist
*this will result in blockage of NE release

-lowers BP by ACTING AT SITES WITHIN CNS

-vasodilation, not cardiosuppression
-lowers bp in supine and standing subjects

-for HTN


-adverse: positive coombs' test and hemolytic anemia
-hepatotoxicity
-xerostomia, sexual dysfunction, OH, and CNS effects

-CLASS B in preg! tradition DOC for htn women in pregnancy
Term
Adrenergic Neuron-blocking agents: MOA?

ex?
Definition
-type of indirect acting antiadrenergic agent
-act presynaptically to reduce the release of NE from sympathetic neurons

-Reserpine (only agent)
Term
Reserpine: MOA?

-what does it resemble?

-What an it deplete?

-pharm effects? (including CNS)

-adverse effects?

-therapeutic uses?
Definition
-adrenergic neuron-blocking agent
-depletion of NE from postganglionic sympathetic neurons
-First it displaces NE from neuron exposing it to MOA enzyme for rapid destruction
-secondly it suppresses the syntheses of NE (bc it blocks uptake of dopamine)

-beta blockade

-depletion of transmitters (serotonin, catecholamines)

-slows HR and reduces CO, decreases alpha activation which causes vasodilation...=decrease in BP
-CNS-sedation and state of indifference


-principle: HTN (but not a preferred drug), psychotic states (not preferred)

-DEPRESSION, bradycardia, OH, nasal congestion, GI problems
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