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SS- Cardio > Autonomic Drugs > Flashcards

Autonomic Drugs Flashcards

1
Q

acebutolol

A

B-1 selective beta blocker: partial agonist
membrane stabilizing: block fast Na channels
SE: tachycardia and HTN

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2
Q

atenolol

A

B-1 selective beta blocker

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3
Q

betaxolol

A

B-1 selective beta blocker
Ca block
mod. long T1/2
lipid soluble

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4
Q

carvedilol

A

non-selective alpha and B blocker
Ca block, antioxidant
lipid soluble
membrane stabilizing: block fast Na channel

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5
Q

esmolol

A

B-1 selective beta blocker

short T1/2

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6
Q

labetalol

A

non-selective alpha and B blocker

use: HTN in pregnancy

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7
Q

metoprolol

A

B-1 selective beta blocker

lipid soluble

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8
Q

nadolol

A

non-selective beta blocker

long T1/2

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9
Q

nebivolol

A

B-1 blocker + B3 stimulation leading to NO synthase
antioxidant
long T1/2

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10
Q

pindolol

A

non-selective beta blocker: partial agonist

SE: tachycardia and HTN

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11
Q

propranolol

A

non-selective beta blocker
highly lipid soluble
membrane stabilizing: block fast Na channels
SE: seizure and coma

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12
Q

timolol

A

non-selective beta blocker

mod. lipid solubility

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13
Q

B-1

A

accelerates SA node, ectopic pacemakers
increases heart contractility and rate
release of renin from juxtaglomerular cells: angiotensin to angiotensin I and II (potent vasoconstrictor)

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14
Q

B-2

A

relaxes skeletal muscle vessels. glycogenolysis, glucagon release

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15
Q

alpha-1

A

vasoconstriction of skin and splanchnic vessels

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16
Q

NSAID effect on kidneys

A

inhibit PGs and AE on renal perfusion by preventing vasoconstrictor actions instigated through renin release

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17
Q

isoproterenol

A 
parenteral or aerosol
non-selective beta agonist
use: AV/heart block, bradycardia
effect: increase CO, decrease diastolic
AE: palpitations, tachycardia, headache, flushing
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18
Q

epinephrine

A

IV, inhale, IM, SC
alpha-1,2 and beta-1,2 agonist
low dose: B, widened pulse pressure
high does: alpha, no widened pulse pressure
use: anaphylaxis, cardiac arrest, hypotension, with local anesthetic
AE: angina, ventricular arrhythmia
CI: nonspecific beta blockers (fatal HTN and cerebral hemorrhage)
effects: increase systolic pressure, decrease diastolic pressure (B2), increase HR (accelerated depol), CO, SV; renin release, decrease renal blood flow

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19
Q

norepinephrine

A

IV
alpha-1,2 and beta-1 agonist
low dose: cardiac stimulant
high dose: vasoconstrictor
use: hypotension (but with decreased renal perfusion)
effects: decrease CO, increase BP, SV, coronary BF, MAP
AE: necrosis, decreased blood flow to organs, HTN
use: increase BP, arrhythmia

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20
Q

Class II anti-arrhythmics

A

Beta blockers that also block fast Na channels

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21
Q

intrinsic sympathomimetic activity

A

partial agonist B blockers
can prevent profound bradycardia or neg. entropy in a resting heart
DON’T use in secondary prevent MI

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22
Q

inverse agonists

A

bind to inactive from of receptor and shift the conformational equilibrium in to the inactive state
in systems not constitutively active behave like competitive antagonists

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23
Q

Use of B blockers

A

HTN (block renin and inhibition of presynaptic B receptors)
ischemic heart disease
atrial flutter and fibrillation arrhythmias (increase AV node refractory period)
CHF
Non-cardiac: tremor, thyrotoxicosis, anxiety, migraine prophylaxis, esophageal varicies prophylaxis (nonspecific), glaucoma

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24
Q

B blocker AE

A

taper to discontinue to avoid rebound effect
bradycardia, bradyarrhythmia, hypotension, hypoglycemia
bronchospasm and dyslipidemia (increase TG and decrease HDL)- less likely with B-1 selective or partial agonist
CNS depression and vivid dreams (lipophilic)
CI: CV or pulmonary disease patient at increased risk of lethal outcome, diabetics (mask tachycardia that is a sign for insulin-induced hypoglycemia)

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25
Tx of beta blocker overdose
glucagon or high dose insulin/glucose | can't use B agonist because receptors are blocked
26
sotalol
B blocker and K blocker | SE: prolong QT, torsade de pointes, ventricular fibrillation
27
doxazosin
alpha-1 blocker
28
terazosin
alpha-1 blocker
29
prazosin
alpha-1 blocker | short T1/2
30
phenoxybenzamine
alpha-1>2 blocker Tx: pheochromacytoma, Raynaud's, frostbite, acrocyanosis duration: days (covalently binds) minor actions in blocking serotonin, histamine, ACh SE: sinus tach, nasal congestion
31
phentolamine
alpha-1,2 blocker Tx; pheochromocytoma, hypertensive emergency SE: orthostatic hypotension, sinus tach leading to arrhythmias low dose: cardio-stimulation and BP increases high doses: decreased BP NOT used routinely for HTN
32
yohimbine
alpha-2 blocker | Tx: erectile dysfunction
33
subdivisions of alpha-1 receptors
b,d: vasculature | a: prostate
34
alfuzosin
alpha-1a blokcer | Tx: BPH
35
alpha-2
pre-synaptic
36
alpha-2 agonist
reduce NE release produces sedation vagal stimulation: produce bradycardia, hypotension
37
alpha blocker side effects
``` SE: orthostatic hypotension first dose, syncope, vertigo sinus tachycardia (angina, palpitations; more likely in non-specific alpha blockers due to augmentation of NE release through alpha-2) ```
38
Gi
MAD 2's: M2, alpha-2, D2 | inhibits AC-> decreases cAMP-> decreases PKA-> decreases Ca and myosin high chain kinase
39
Gs
B1,2, D1, H2, V2 | stimulates AC-> cAMP-> PKA-> Ca and myosin high chain kinase
40
Gq
HAVe 1 M&M: H1, alpha-1, V1, M1, M3 | PLC cleaves PIP2 into DAG (increases intracellular Ca) and IP3 (activates PKC)
41
dopamine
IV: short duration D1,2 > B > alpha agonism, causes NE release from terminals low dose: D1,2 intermediate dose: B, increase CO high dose: alpha, increase BP use: unstable bradycardia, HF, shock effect: D1: vasodilation of kidney, improves GFR
42
dobutamine
IV: short duration B1> B2, alpha agonism use: HF, stress tests effect: increase CO, SV without changing HR
43
phenylephrine
SC, IM, IV alpha agonist use: hypotension effect: increase BP (reflex decrease HR and CO) AE: angina, anxiety, hallucinations, HTN, dixxc, insomnia, pallor, restless
44
ephedrine
oral release NE and alpha/beta agonist use: hypotension of anesthesia, narcolepsy, nasal congestion, asthma, bronchospasm effect: increased HR, CO; variable increase BP BAN on herbal products, use to make meth
45
tyramine
release of pre-formed NT
46
amphetamine
release of pre-formed NT
47
MAOI
prevent breakdown of NT
48
COMT inhibitors
prevent breakdown of NT
49
reserpine
NE storage depletion: inhibits VMAT and prevents NE from being packaged in vesicles days to weeks to make new vesicles effects on drugs: direct acting: response not reduced, may increase (up regulate receptors) indirect acting: abolishes response mixed acting: blunted effects AE: CNS toxicity (sedation, inability to concentrate, depression) CI: PUD or ulcerative colitis, teratogen, avoid breastfeeding
50
M2
decelerates SA and AV (no effect on ventricular), decreases contractility Gi: activation of inward K channel (hyper polarize) and inhibition of L-Ca channel inhibits NE release autoreceptor: auto inhibition
51
M3
Gq (depolarization and excitation): synthesizes EDRF (endothelia derived relaxing factor, ex. NO) in endothelium of heart, brain, viscera inhibits NE release
52
atropine
cholinergic antagonist low dose: slow heart (block M1 auto receptors) high dose: increase HR (M2 receptor) effects: diminishes heart slowing and bradycardia; increase AV node conduction (for AV block, and severe sinus/nodal bradcardia) use: inhibit overactivity of vagal heart tone and abolish para sympathomimetic drugs SE: inhibition sweating, flushing
53
ACh
cholinergic agonist vasodilation, decrease HR, AV conduction, cardiac contractility reflex tachycardia damaged endothelium: acts on underlying sm. muscle and will cause vasoconstriction
54
mecamylamine
ganglionic blocker no longer used to Tx HTN Tx: Tourette's, cocaine and nicotine addiction
55
trimethophan
ganglionic blocker Tx: emergency control of BP in patients with acute dissecting aortic aneurysm AE: histamine release: asthma
56
nicotinic receptors
2 molecules of ACh bind | ion channel
57
ganglionic blockers
nACh receptor blockers; act on postganglionic neurons: open Na/K channels (depoloraize) vasodilation, of arterioles and veins, increase HR use: intraoperative and malignant HTN emergency, control arteriolar bed bleeding in surgery AE: postural hypotension, tachycardia, arrhythmia, blurry/dbl. vision, dry mouth, constipation, ileus, N/V, urinary retention, impotence, drowsiness, seizure, hallucinations, tremor, confusion, NMJ block
58
hexmethonium
ganglionic blocker that blocks channel after it is open, shortening the duration of current
59
methyldopa
IV alpha-2 agonist prodrug-> alpha-methylnorepinephrine Use: HTN in PREGNANCY CI: dose adjustment in renal failure, chelated by iron, pheochromocytoma
60
clonidine
IV, patch | alpha-2 agonist
61
guanfacine
alpha-2 agonist
62
alpha-2 auto receptors
Gi | limit NE release
63
metyrosine
NE storage depletion: tyrosine hydroxylase inhibitor | Tx: pheochromocytoma
64
alpha-2 agonists
effects of agonists: local effect: vasoconstriction systemic effect: sympatholytic: decrease BP via vasomotor center, decrease renin NO reflex tachycardia-> can block reflex of vasodilating drugs NO effect on glucose or lung pure autonomic failure: increase BP (no central effect) other: sedation, analgesia, anxiolysis terminate further NE release long term use: tolerance due to receptor down regulation SE: drowsiness, xerotomia (dry mouth)
65
alpha-2 heteroreceptors
vagal activation (bradycardia, hypotension), analgesia, sedation, hypothermia, anesthetic-sparing effect

SS- Cardio (16 decks)

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