Pharm Flashcards
What are the 3 principal alpha-blocker used to treat essential hypertension?
doxazosin, terazosin, prazosin
What 2 alpha blockers act on both alpha 1 and 2 receptors and therefore have limited use?
phenoxybenzamine, phentolamine
Where are alpha receptors located anatomically?
primarily blood vessels. Also skeletal muscles
Where are beta receptors located anatomically?
primarily the heart. Also beta-2 are found in skeletal muscle.
What is the difference in location of alpha1 and alpha2 receptors?
Alpha 2: presynaptically–> activation causes increase release of norepinephrine leading to tachycardia.
Alpha 1: downstream signaling at effector organ. Smooth muscle contraction
What are the subtypes of alpha-1 receptors and what is the significance of this?
a: found in prostate
b and d found in vasculature
What are the 2 main side effects associated with alpha blockers?
first dose orthostatic hypotension and sinus-tach, syncope, vertigo
First dose orthostatic hypotension associated with alpha blockers is most prominent with ____.
prazosin
Why do alpha blockers cause tachycardia?
Blocking alpha-2 presynaptic receptors augments release of NE causing tachycardia.
____ is a non-competitive, covalent, alpha1 and 2 antagonist.
Phenoxybenzamine
Indications for phenoxybenzamine
sympathetic excess due to pheochromocytoma, raynaud’s, frostbite, acrocyanosis
Adverse effects of phenoxybenzamine
sinus-tach, nasal congestion, drowsiness, fatigue, weakness, malaise, confusion, headache, xerostomia, ejaculation dysfunction
_____ is a short-acting, competitive antagonist at alpha 1 and 2 receptors.
phentolamine
Indications of phentolamine
pheochromocytoma, hypertensive emergency
Adverse effects of phentolamine
postural hypotension, reflex tachycardia–> arrhythmias
Describe the dose effect when taking phentolamine
Smaller doses alpha 2 predominates–> increase BP
Larger doses alpha 1 predominates causing peripheral vasodilation and decrease BP
How do alpha blockers affect NE treatment?
Decrease BP caused by NE because they block vascoconstriction.
How to alpha blockers effect EP Rx?
Decrease BP caused by EP resulting in hypotension. This is because EP also acts to beta receptors in muscles which vasodilate.
Describe the affinity of terazosin, doxazosin, prazosin?
alpha 1»_space;»» alpha 2
Describe the affinity of phenoxybenzamine.
alpha 1 > alpha 2