B4-005 Autonomic Drugs Flashcards

1
Q

what adrenoreceptors:
* peripheral vasculature
* contraction of smooth muscle
* increase BP

A

alpha 1

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2
Q

what adrenoreceptor:
* presynaptic autoregulation of neurotransmitter release

A

alpha 2

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3
Q

what adrenoreceptor:
* approx equal affinity for Epi and NE

A

beta 1

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4
Q

what adrenoreceptor:
* higher affinity for Epi than NE

A

beta 2

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5
Q

densensitization of adrenoreceptors may limit

A

therapeutic response

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6
Q

denervation supersensitivity of adrenoreceptors may

A

exacerbate side effects

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7
Q

catecholamines

A
  • epinephrine
  • norepinephrine
  • isoproternol
  • dobutamine
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8
Q
  • very potent vasoconstrictor & cardiac stimulant
  • positive inotropic and chronotropic actions on heart
  • also activates beta2 receptors
A

epinephrine

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9
Q

similar potency at beta 1 receptors, but relatively little effect on beta 2

A

norepinephrine

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10
Q
  • compensatory vagal reflexes over come direct positive chronotropy
  • at high doses, may indirectly increase heart rate
A

norepinephrine

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11
Q
  • potent nonselective beta-receptor agonist
  • positive chronotropic and inotropic actions
  • decreases both diastolic and mean arterial pressure
A

isoproterenol

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12
Q
  • relatively beta 1 selective synthetic catecholamine
  • also activates alpha 1 receptors
A

dobutamine

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13
Q
  • prototypic alpha1 agonist
  • not a chatechol derivative
  • not inactivated by COMT
  • longer duration of action than catecholamines
  • mydriatic and decongestant
  • can raise blood pressure
A

phenylephrine

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14
Q

first orally active sympathomimetic drug

A

ephedrine

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15
Q
  • widely available OTC decongestant
  • also have indirect effects of releasing endogenous NE
A

psuedoephedrine

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16
Q
  • direct alpha 1 agonists
  • used as topical decongestants

2

A
  • oxymetazoline
  • xylometazoline
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17
Q
  • alpha 2 selective agonists
  • used (poorly) as antihypertensives
  • dimish SNS outflow

2

A
  • clonidine
  • methyldopa
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18
Q
  • beta 1 selective agonist
  • increases cardiac output with less reflex tachycardia
  • lack of beta 2 stimulated venous dilation
A

dobutamine

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19
Q
  • beta 2 selective agonists
  • treatment of asthma

2

A
  • albuterol
  • salmeterol
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20
Q
  • beta 2 selective agonist
  • treatment of premature labor
A

ritodrine

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21
Q
  • indirect sympathomimetics
  • marked stimulant effects on mood and alertness
  • depressant effect on appetite
A
  • amphetamine
  • methamphetamine
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22
Q
  • local anesthetic
  • sympathomimetic due to blockade of uptake 1
A

cocaine

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23
Q
  • releases stored catecholamines
  • found in high concentrations in fermented foods (cheese)
  • MOA inhibitors potentiate effects and can produce hypertension
A

tyramine

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24
Q
  • prototypic alpha antagonist
  • nonselective between alpha1 and alpha2
  • competitive blockade of receptors
  • reduces TPR, MAP
  • produces reflex tachycardia (SNA reflex)
A

phentolamine

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25
Q
  • irreversible-binds covalently to alpha receptors
  • postural hypotension and tachycardia limit use
A

phenoxybenzamine

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26
Q
  • alpha receptor antagonists
  • selective for alpha 1 receptors

3

A
  • prazosin
  • terazosin
  • doxazosin
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27
Q
  • alpha2 selective antagonist
  • no established clinical role
A

yohimbine

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28
Q
  • block effects of catecholamines at beta receptors
  • varied affinity for beta1 vs. beta2 receptors
  • selectivity has important clinical implications
  • non are absolutel specific for beta1 receptors
A

beta receptor antagonists

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29
Q
  • lower blood pressure in patients with hypertension
  • negative inotropic and chronotropic effects
  • reduce oxygen demand of myocardium
A

beta receptor antagonists

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30
Q

clinically useful for:
* hypertension
* ischemic heart disease
* cardiac arrhythmias
* glaucoma
* hyperthyroidism

A

beta blockers

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31
Q
  • prototypical beta-blocking drug
  • nonselective
A

propranolol

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32
Q

beta-1 selective beta blockers

2

A

metoprolol
atenolol

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33
Q

beta blockers with a very long duration of action

2

A

nadolol and timolol

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34
Q
  • reversible alpha1 antagonist
  • also nonselective beta antagonist
  • hypotension with less tachycardia than alpha blockers
A

labetalol

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35
Q
  • beta blocker
  • selective for beta2 receptors
  • no obvious clinical application
A

butoxamine

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36
Q

name the adrenoreceptor:

sympathetic activity contracts the radial muscle of the iris

A

a1

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37
Q

name the adrenoreceptor:

parasympathetic activity contracts the circular muscle of the iris

A

M3

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38
Q

name the adrenoreceptor:

sympathetic activity relaxes ciliary muscle of eye

A

beta

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39
Q

name the adrenoreceptor:

parasympathetic activity contracts the ciliary muscle of eye

A

M3

40
Q

name the adrenoreceptor:

sympathetic activity accelerates SA node

A

b1/b2

41
Q

name the adrenoreceptor:

parasympathetic activity decelerats SA node

A

M2

42
Q

name the adrenoreceptor:

sympathetic activity accelerates ectopic pacemakers

A

b1/b2

43
Q

name the adrenoreceptor:

sympathetic activity increases contractility of the heat

A

b1/b2

44
Q

name the adrenoreceptor:

parasympathetic activity decreases contractility of the heart

A

M2

45
Q

name the adrenoreceptor:

sympathetic activity contracts blood vessels of skin and splanchnic vessels

A

alpha

46
Q

name the adrenoreceptor:

sympathetic activity relaxes blood vessels in skeletal muscles

A

b2, M3

47
Q

name the adrenoreceptor:

sympathetic activity contracts blood vessels in skeletal muscles

A

a

48
Q

name the adrenoreceptor:

parasympathetic activity releases EDRF in blood vessels of endothelium

A

m3

49
Q

name the adrenoreceptor:

sympathetic activity relaxes bronchiolar smooth muscle

A

b2

50
Q

name the adrenoreceptor:

parasympathetic activity contracts bronchiolar smooth muscle

A

m3

51
Q

name the adrenoreceptor:

sympathetic activity relaxes walls of smooth muscle in GI tract

A

a2, b2

52
Q

name the adrenoreceptor:

sympathetic activity contracts sphincters of GI tract

A

a1

53
Q

name the adrenoreceptor:

parasympathetic activity contracts walls of smooth muscle in GI tract

A

m3

54
Q

name the adrenoreceptor:

parasympathetic activity relaxes spinchters in GI tract

A

m3

55
Q

parasympathetic activity increases secretion in GI tract

A

m3

56
Q

name the adrenoreceptor:

parasympathetic activity activates mesenteric plexus in GI tract

A

m1

57
Q

name the adrenoreceptor:

sympathetic activity relaxes bladder wall

A

b2

58
Q

name the adrenoreceptor:

parasympathetic activity contracts badder wall

A

m3

59
Q

name the adrenoreceptor:

sympathetic activity contracts spinchters in GU tract

A

a1

60
Q

name the adrenoreceptor:

parasympathetic activity relaxes spinchters in GU tract

A

m3

61
Q

name the adrenoreceptor:

sympathetic activity relaxes uterus

A

b2

62
Q

name the adrenoreceptor:

sympathetic activity contracts uterus

A

a

63
Q

name the adrenoreceptor:

parasympathetic activity contracts uterus

A

m3

64
Q

name the adrenoreceptor:

sympathetic activity causes ejaculation

A

a

65
Q

name the adrenoreceptor:

parasympathetic activity causes erection

A

M

66
Q

name the adrenoreceptor:

sympathetic activity contracts pliomotor smooth muscle

A

a

67
Q

name the adrenoreceptor:

sympathetic activity increases thermoregulatory sweat glands

A

M

68
Q

name the adrenoreceptor:

sympathetic activity increases apocrine sweat glands

A

a

69
Q

name the adrenoreceptor:

sympathetic activity increases gluconeogenesis

A

b2 and a

70
Q

name the adrenoreceptor:

sympathetic activity increases glycogenolysis

A

b2 and a

71
Q

name the adrenoreceptor:

sympathetic activity stimultes lypolysis

A

b3

72
Q

name the adrenoreceptor:

sympathetic activity stimulates renin release

A

b1

73
Q

name the adrenoreceptor:

parasympathetic activity decreases NE release

A

M

74
Q

name the adrenoreceptor:

sympathetic activity decreases ACh release

A

a

75
Q

cholinomimetic agents mimic

A

acetylcholine

76
Q

cholinoceptor-activating and cholinoesterase-inhibiting drugs are classified by

A

receptor action
* muscarinic
* nicotinic
mechanism of action
* direct
* indirect

77
Q

directly bind and activate muscarinic or nicotinic receptors

A

direct acting

78
Q

directly bind and activate muscarinic or nicotinic receptors

A

direct acting

cholinomimetic agents

79
Q
  • reduce hydrolysis of acetylcholine
  • increase endogenous acetylcholine concentration at synapse
  • excess acetylcholine increases responses
  • drugs act primarily where acetylcholine is physiologically released
A

indirect acting agents

ihibit acetylcholinesterase

80
Q

ACh effects are terminated by

A

acetylcholinesterase

indirect agents inhibit this

81
Q

3 chemical groups that cholinesterase inhibitors fall into

A
  1. simple alcohols
  2. carbamic acid esters
  3. organic derivatives of phosphoric acid (organophosphates)
82
Q
  • simple alcohol
  • colinesterase inhibitor
A

edrophonium

83
Q

quaternary carbamic acid ester

A

neostigmine

84
Q

tertiary carbamic acid ester

A

physostigmine

85
Q

organophosphates

A

soman
sarin
malathion

86
Q

used as insecticide

A

malathion

87
Q

direct affect is to slow heart rate

A

muscarinic agonists

88
Q
  • autonomic ganglia are major site of action
  • simultaneous SNS and PSN discharge
  • predominant tone predicts effects
A

nicotinic agonists

SNS-vasculature
PNS-most other tissues

88
Q
  • autonomic ganglia are major site of action
  • simultaneous SNS and PSN discharge
  • predominant tone predicts effects
A

nicotinic agonists

SNS-vasculature
PNS-most other tissues

89
Q
  • antimuscarinic drugs
  • tertiary compounds used for their effects in eye or CNS
A
  • atropine
  • scopolamine
90
Q
  • antimuscarinic drugs
  • quaternary amines selectively produce peripheral effects
A

ipratropium

91
Q
  • prototypic antimuscarinic drug
  • causes reversible blockade
  • not selective between subtypes
A

atropine

92
Q

neuronal nicotinic receptor antagionists

3

A
  • hexamethonium
  • trimethapan
  • mecamylamine
93
Q
  • block actions of ACh and other agonists at nicotinic receptors
  • receptors located in both PNS and SNS autonomic ganglia
  • non-selectivity produces limited side effects
  • synthetic amines
A

neuronal nicotinic receptor antagonists

94
Q
  • first ANS ganglion blocking drugs
  • short duration of action
  • mangement of hypertension
A

tetraethylammonium (TEA)