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Flashcards in Autonomic Drugs Deck (65):
1

acebutolol

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

2

atenolol

B-1 selective beta blocker

3

betaxolol

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

4

carvedilol

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

5

esmolol

B-1 selective beta blocker
short T1/2

6

labetalol

non-selective alpha and B blocker
use: HTN in pregnancy

7

metoprolol

B-1 selective beta blocker
lipid soluble

8

nadolol

non-selective beta blocker
long T1/2

9

nebivolol

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

10

pindolol

non-selective beta blocker: partial agonist
SE: tachycardia and HTN

11

propranolol

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

12

timolol

non-selective beta blocker
mod. lipid solubility

13

B-1

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

14

B-2

relaxes skeletal muscle vessels. glycogenolysis, glucagon release

15

alpha-1

vasoconstriction of skin and splanchnic vessels

16

NSAID effect on kidneys

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

17

isoproterenol

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

18

epinephrine

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

19

norepinephrine

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

20

Class II anti-arrhythmics

Beta blockers that also block fast Na channels

21

intrinsic sympathomimetic activity

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

22

inverse agonists

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

23

Use of B blockers

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

24

B blocker AE

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)

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