Alpha blockers Flashcards
Alpha 2A locations:
medulla (presynpactic)
Alpha 2A stimulation results in:
decreased sympathetic outflow
Alpha 2B locations:
vascular smooth muscle
Alpha 2B stimulation results in:
vasoconstriction
Mechanism of action of Clonidine
ALPHA 2 AGONIST
activation of central presynaptic alpha 2A receptors –> suppression of central symp. outflow
suppression of peripheral presynaptic alpha 2 receptors –> inhibition of NE, ATP, NPY release
Effects of Clonidine?
CNS - decreases BP (HR, SV decrease and relaxation of capacitance vessels)
Renal - decreases renin (alpha 2 stimulation)
Eyes - decreases IOP
Abrupt discontinuation of clonidine after high dosage prolonged use can result in
hypertensive crisis
Major therapeutic use of clonidine?
Minor?
Major: hypertension
Minor: decrease diarrhea in diabetics with autonomic neuropathy;
treatment of withdrawal of opiate addicts (their bp may increase);
menopausal hot flashes
MoA of methyldopa?
ALPHA 2 AGONIST
a-methylnorepinephrine (metabolite) stimulates alpha 2 receptors in brainstem
Effects of methyldopa?
CVS - decreases PVR. (little change in CO and HR)
renal system - decreases renin secretion (alpha 2)
Most common side effect of methyldopa?
sedation.
Also, dry mouth.
Which adrenergic drug causes a positive Coombs test?
methyldopa
Which alpha 2 agonist is used to decrease IOP?
apraclonidine
brimonidine
Which alpha 2 agonist is used as a muscle relaxant for treatment of spasticity?
Tizanidine
Which alpha 2 agonist is used as an anti-MI drug
Mivazerol
Which alpha 2 agonist is used to treat HTN AND ADHD in 16-17 year olds
Guanfacine
Result of alpha 1 blockage:
Beta 2 unopposed - vasodilation and decrease of PVR and BP
Result of alpha 2 blockage
presynaptic –> inhibition of inhibition of NE –> INCREASES NE –> B1 in heart and JG cells stimulated –> INCREASED HR and renin release