Adrenergic Antagonists- T2 Flashcards
alpha adrenergic receptor antagonists may be classified as
reversible competitive antagonists and irreversible competitive alpha-adrenergic antagonists
phentolamine is a
non-selective (both alpha 1 and 2) reversible competitive alpha-adrenergic receptor antagonists.
prazosin, doxazosin, and terazosin are
alpha1 selective reversible competitive alpha-adrenergic receptor antagonists
tamsulosin and silodosin (rapaflo) are
alpha1A/D selective reversible competitive alpha-adrenergic receptor antagonists
phenoxybenzamine is
a irreversible competitive non selective alpha adrenergic antagonist
4 piperazinyl quinazolines
prazosin, terazosin, doxazosin, alfuzosin
3 indoles
yohimbine, indoramin, silodosin
alpha1 and 2 adrenoceptors are responsible for the
maintenance of TPR and maintain pressure.
in many patients with essential HTN, TPR may be abnormally elevated due to
increased alpha-adrenergic receptor stimulation.
the 6 alpha-adrenergic receptor subtypes
1a, 1b, 1d, 2a, 2b, 2c
agents that antagonize both alpha1 and 2 tend to be
less efficacious in lowering BP than alpha1 selective
blockade of alpha2 adrenoceptors will cause
enhanced release of NE at the sympathetic neurons leading to excess adrenoceptor stimulation.
alpha2 blockage causes veno___ which leads to__
venodilation leading to a reduction in preload and then reduces SV.
why would we want to give a selective alpha antagonist opposed to non selective
giving a selective reduces the peripheral resistance, if it doesn’t have selectivity, we won’t have effects that come from antagonizing a specific alpha receptor.
prazosin and htn tx
a alpha1 selective antagonist that is prone to hepatic metabolism, has the shortest half life and primarily eliminated in the bile. if the patient has renal impairment you would want to use this.
doxazosin and terazosin in htn tx.
alpha1 selective antagonists have more renal eliminated of the parent compound and longer half life of elimination, would want to use these if the pt had liver failure.
antagonism of alpha1 adrenoceptors result in
dilation of arteries, arterioles, and veins.
arteriolar dilation results in
decreased after load (decreased TPR)
afterload is
the pressure that the heart has to work against.
venous dilation causes
decreased preload