Adrenergic Antagonists Flashcards
Reversible Alpha Receptor Antagonists
compete w.agonists and endogenous catecholamines
blocks receptor and can dissociated if agonist is present in high amounts
duration depends on drugs affinity for receptor and the drugs 1/2 life
irreversible Alpha Receptors
covalent bonds (permanently block) longer 1/2 life duration of action dependent in synthesis of new receptors
Alpha Antagonists on CV system
block alpha 1 vasoconstriction=vasodilation=drop in BP
reflex tachycardia develops in response to maintain CO
Other Effects of Alpha 1 antagonists
block mydriasis (get miosis=constriction) block nasal vasoconstriction=congestion block urinary retantion=facilitates urination
Phenoxybenzamine (Dibenzyline)
alpha antagonist
irreversibly blocks alpha 1
causes vasodilation
also blocks presynaptic alpha 2 receptors
tx Pheochromocytoma
excessive catecholamine release (oversecretion of NE and Epi)
Phentolamine (OraVerse)
alpha antagonist
Reversibley blocks Alpha 1 and presynaptic alpha 2
a1 block=decrease BP
A2 block=increase cardiac stimulation
tx pheochromocytoma
Prazosin (Minipress)
alpha 1 antagonist
tx HTN
Terazosin (Hytrin)
alpha 1 antagonist
used to tx HTN
Doxazosin (Cardura)
alpha 1 antagonist
used to tx HTN
Tamsulosin (Flomax)
alpha 1 agonist
tx HTN and relax smooth muscle of prostate to tx BPH=allows urination
Beta Receptor Antagonists
bind reversibly
drugs differ in affinity and selectivity for blocking Beta 1 and Beta 2 receptors
selectivity decreases with higher dose
Beta antagonists on cardiovascular system
“beta blockers”
tx HTN in pt that also has angina, CHF, MI
reduces cardiac work loads (-inotropic and - chronotropic)
slows AV node and decreases HR
Beta Blockers and BP
block Beta 2 receptors=Bp decreases
enhanced by agents that also bock alpha 1 receptos–>labetolol`
Beta Blocker use in Angina
imprives balance between oxygen supply and demand.
Block adrenergic=reduction in cardiac work load
Contraindication of Beta blocker use in Pt’s with asthma and COPD
B blcokers are not selective, so beta blcokers can worsen asthma and COPD because b2 antagonists can cause bronchoconstriction