what are the 4 classes of sympathoplegic agents for HTN?
- Beta-Blockers
- Alpha-1 Blockers
- Alpha-2 Agonists
- Adrenergic blocking agents
ACE-I’s are eliminated where, except for which one is hepatically eliminated
all renally eliminated
except fosinopril has some hepatic elimination
nitric oxide has what effect on PVR
decreases PVR
nitric oxide is a vasodilator
what catecholamine receptors are found on the presynaptic cell?
alpha2
what receptors are on post synaptic vascular smooth muscle cells
alpha1 receptors
what receptors are responsible for chronotropic action
beta1
what receptor activation increases liver’s release of renin
beta 1
what are beta blockers effect on chronotropic and inotropic effects?
decrease both
chronotropic effects refers to what specifically?
heart reate
inotropic effects refer to what specifically
stroke volume
list the adverse effects of beta blockers
HBBEEF hypoglycemia bradycardia exacerbate heart failure bronchoconstriction (B2 rec) depression ED fatigue
how do BB’s worsen HF?
by decreasing CO
which BB’s are B1 selective
NEVER BE BAMA Nebivolol Bisoprolol Betaxolol Acebutolol Metroprolol Atenolol
why should BB’s not be stopped abruptly
receptor upregulation leads to rebound hypertension
who should use BB’s with caution
CHAD
COPD
Heart Failure
Asthma
Diabetes
what was the 1st BB?
propranolol
what drugs can interact with metoprolol
SSRI’s
Bupropion
H2-antagonists
what is metoprolol’s extended release form
metoprolol succinate
what is metoprolol’s immediate release form
metoprolol tartrate
what type of metabolism does metoprolol go through?
hepatic metabolism
CYP2D6
how is atenolol primarily excreted
unchanged in urine
what 2 nonselective BB’s are excreted in urine unchanged
nadolol and carteolol
name 2 cardioselective BB’s other than metoprolol metabolized by CYP2D6
betaxolol and bisoprolol
name 2 cardioslective BB’s dosed once daily due to long half life
betaxolol and bisoprolol
name 3 partial agonist BB’s?
pindolol
acebutolol
penbutolol
define B-receptor partial agonist
binds to B receptor but produces little effect,
very little side effects
intrinsic sympathomoimetic activity
name a cardioselective partial agonist BB
acebutolol
what are the 2 inactive isomers of labetalol
SS and RS are inactive
what is the potent alpha-blocker isomer of labetalol
SR = potent alpha
what is the potent non-selective beta blocking isomer of latetalol
RR
list the 4 isomers mixed in laetalol
SS = inactive RS = inactive SR = potent alpha blocker RR = poten non-selective B-blocker
what are the two ismomers mixed for Carvedilol and there effects
S(-) = nonselective B-blocker and alpha-blocker R(+) = alpha-blocker
how is carvedilol metabolized?
hepatic metabolism
2C9 and 2D6
what 2 isomers are mixed racemically for Nebivolol and there effects
D- = beta1 selective L- = increased NO production
what is the half life of Nebbivolol
10 hours
what are 3 racemically mixed vasodilating BBs
- labetolol
- carvedilol
- nebivolol
name a cardioselective, rapidly metabolized BB
esmolol
what is esmolol’s half life?
how is it metsabolized
9-10 minutes
RBC esteraces
how is esmolol administered?
for what?
continuous IV infusion
intraoperative HTN or HTN emergency with tachycardia
BB’s are used concomitantly with HTN and what other diseases?
Supraventricular tachycardia
heart failure
angina pectoris
previous MI