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
Q

Tx of beta blocker overdose

A

glucagon or high dose insulin/glucose

can’t use B agonist because receptors are blocked

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26
Q

sotalol

A

B blocker and K blocker

SE: prolong QT, torsade de pointes, ventricular fibrillation

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27
Q

doxazosin

A

alpha-1 blocker

28
Q

terazosin

A

alpha-1 blocker

29
Q

prazosin

A

alpha-1 blocker

short T1/2

30
Q

phenoxybenzamine

A

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
Q

phentolamine

A

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
Q

yohimbine

A

alpha-2 blocker

Tx: erectile dysfunction

33
Q

subdivisions of alpha-1 receptors

A

b,d: vasculature

a: prostate

34
Q

alfuzosin

A

alpha-1a blokcer

Tx: BPH

35
Q

alpha-2

A

pre-synaptic

36
Q

alpha-2 agonist

A

reduce NE release
produces sedation
vagal stimulation: produce bradycardia, hypotension

37
Q

alpha blocker side effects

A
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
Q

Gi

A

MAD 2’s: M2, alpha-2, D2

inhibits AC-> decreases cAMP-> decreases PKA-> decreases Ca and myosin high chain kinase

39
Q

Gs

A

B1,2, D1, H2, V2

stimulates AC-> cAMP-> PKA-> Ca and myosin high chain kinase

40
Q

Gq

A

HAVe 1 M&M: H1, alpha-1, V1, M1, M3

PLC cleaves PIP2 into DAG (increases intracellular Ca) and IP3 (activates PKC)

41
Q

dopamine

A

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
Q

dobutamine

A

IV: short duration
B1> B2, alpha agonism
use: HF, stress tests
effect: increase CO, SV without changing HR

43
Q

phenylephrine

A

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
Q

ephedrine

A

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
Q

tyramine

A

release of pre-formed NT

46
Q

amphetamine

A

release of pre-formed NT

47
Q

MAOI

A

prevent breakdown of NT

48
Q

COMT inhibitors

A

prevent breakdown of NT

49
Q

reserpine

A

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
Q

M2

A

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
Q

M3

A

Gq (depolarization and excitation): synthesizes EDRF (endothelia derived relaxing factor, ex. NO) in endothelium of heart, brain, viscera
inhibits NE release

52
Q

atropine

A

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
Q

ACh

A

cholinergic agonist
vasodilation, decrease HR, AV conduction, cardiac contractility
reflex tachycardia
damaged endothelium: acts on underlying sm. muscle and will cause vasoconstriction

54
Q

mecamylamine

A

ganglionic blocker
no longer used to Tx HTN
Tx: Tourette’s, cocaine and nicotine addiction

55
Q

trimethophan

A

ganglionic blocker
Tx: emergency control of BP in patients with acute dissecting aortic aneurysm
AE: histamine release: asthma

56
Q

nicotinic receptors

A

2 molecules of ACh bind

ion channel

57
Q

ganglionic blockers

A

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
Q

hexmethonium

A

ganglionic blocker that blocks channel after it is open, shortening the duration of current

59
Q

methyldopa

A

IV
alpha-2 agonist prodrug-> alpha-methylnorepinephrine
Use: HTN in PREGNANCY
CI: dose adjustment in renal failure, chelated by iron, pheochromocytoma

60
Q

clonidine

A

IV, patch

alpha-2 agonist

61
Q

guanfacine

A

alpha-2 agonist

62
Q

alpha-2 auto receptors

A

Gi

limit NE release

63
Q

metyrosine

A

NE storage depletion: tyrosine hydroxylase inhibitor

Tx: pheochromocytoma

64
Q

alpha-2 agonists

A

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
Q

alpha-2 heteroreceptors

A

vagal activation (bradycardia, hypotension), analgesia, sedation, hypothermia, anesthetic-sparing effect