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Pharmacology > Autonomic Nervous System > Flashcards

Autonomic Nervous System Flashcards

1
Q

sympathetic nerves originate from

A

thoracic and lumbar regions

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2
Q

parasympathetic nerves originate from

A

cranial and sacral regions

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3
Q

__________ nerves contain short preganglionic neurons and long postganglionic neruons

A

sympathetic

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4
Q

__________ nerves contain long preganglionic neurons and short postganglionic neurons

A

parasympathetic

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5
Q

sympathetic preganglionics are __________

A

cholinergic

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6
Q

sympathetic postganglionics are ___________

A

adrenergic

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7
Q

parasympathetic preganglionics are ___________

A

cholinergic

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8
Q

parasympathetic postganglionics are ___________

A

cholinergic

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9
Q

sympathetic postganglionic release

A

norepinephrine

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10
Q

sympathetic postganglionic stimulate

A

alpha and beta receptors

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11
Q

sympathetic postganglionic are metabolized by

A

MAO and COMT

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12
Q

parasympathetic postganglionic release

A

acetylcholine

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13
Q

parasympathetic postganglionic stimulate

A

muscarinic receptors

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14
Q

parasympathetic postganglionic are metabolized by

A

cholinesterase

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15
Q

What is a quarternary group?What is it’s significance?

A

1) When there are 4 C attached to a N

2) It has a charge and is therefore polar (i.e. does no go through lipids; cannot be transported into the CNS)

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16
Q

Benchmark parasympathetic responses

A

1) miosis
2) vasodilation of arterioles
3) negative chronotropic and negative ionotropic responses in heart
4) bronchoconstriction
5) SLUD (salivation, lacrimation, urination, diarrhea)

**this is all d/t muscarinic stimulation

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17
Q

Benchmark sympathetic responses

A

1) positive iontropic and positive chronotropic responses in heart (Beta 1 stim.)
2) bronchodilation (Beta 2 stim.)
3) relaxation of myometrium (Beta 2 stim.)
4) insulin release (Beta 2 stim.)
5) vasoconstriction of arterioles (Alpha 1 stim.)
6) mydriasis (Alpha 1 stim.)
7) NE release (Alpha 2 stim.)

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18
Q

Type(s) of parasympathomimetic drug(s)

A

muscarinic agonists

cholinesterase inhibitors

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19
Q

Type(s) of parasympatholytic drug(s)

A

muscarinic antagonists

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20
Q

Acetylcholine category

A

ANS - parasympathomimetic

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21
Q

Acetylcholine MOA

A

muscarinic and nicotinic agonist

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22
Q

Acetylcholine distinguishing characteristics

A

1) rapidly hydrolyzed by esterases b/c it has a ‘naked ester’
2) acts on both muscarinic and nicotinic receptors
3) quaternary ammonium group invokes polarity (can’t pass thru BBB)

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23
Q

Acetylcholine predictable characteristics

A

1) short half life (seconds)
2) diffuse activity (parasympathomimetic, sympathomimetic, and sk. mm.)
3) limited distribution
4) possible local opthalmic use, but other products better

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24
Q

Bethanechol (urecholine) category

A

ANS - parasympathomimetic

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25
Q

Bethanechol (urecholine) MOA

A

muscarinic agonist

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26
Q

Bethanechol (urecholine) distinguishing characteristics

A

1) not metabolized by esterase enzymes
2) quaternary ammonium compound
3) particular affinity for gut and bladder sm. mm.
4) oral route preferred

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27
Q

Bethanechol (urecholine) predictable characteristics

A

1) no CNS effect
2) half life allows distribution to areas of low blood flow
3) uses: gastroparesis (postoperative), urinary retention, xerostomia, ocular diagnostics
4) s/e: other parasympathomimetic effects esp. following parenteral Rx

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28
Q

Pilocarpine category

A

ANS - parasympathomimetic

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29
Q

Pilocarpine MOA

A

muscarinic receptor agonist

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30
Q

Pilocarpine distinguishing characteristics

A

1) plant origin (Pilocarpus jabarundi)
2) tertiary ammonium compound
3) preferential activity of sweat glands
4) resistance to esterases

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31
Q

Pilocarpine predictable characteristics

A

1) used as miotic and in tx of glaucoma
2) will cz accommodation
3) used to tx xerostomia
4) may cz CNS effects at high plasma levels
5) diaphoresis is common s/e
6) duration of action is up to 8 hr

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32
Q

Neostigmine category

A

ANS - parasympathomimetic

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33
Q

Neostigmine MOA

A

reversible cholinesterase inhibitor (i.e. it attaches to cholinesterases w/ a weak ionic bond)

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34
Q

Neostigmine distinctive characteristics

A

1) quaternary ammonium compound
2) contains ester group - slowly hydrolyzed (1-2 hr half life)
3) poorly absorbed following oral rx

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35
Q

Neostigmine predictable characteristics

A

1) elevates Ach levels
2) cz both muscarinic and nicotinic stimulation
3) numerous peripheral s/e but not CNS
4) uses: miosis and glaucoma (local admin.), myasthenia gravis, antidote to some drugs (atropine), atonic gut and bladder

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36
Q

Malathione category

A

ANS - parasympathomimetic

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37
Q

Malathione MOA

A

irreversible cholinesterase inhibitor (binds to cholinesterase with a covalent bond)

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38
Q

Malathione distinguishing characteristics

A

1) tertiary ammonium compound
2) binds covalently to esterase enzymes
3) not hydrolyzed by esterase enzymes
4) rapidly absorbed thru multiple routes

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39
Q

Malathione characteristics

A

1) cz SLUD and other ANS activities
2) cz CNS disturbances
3) no therapeutic use
4) used as insecticide
5) similar agents used as chemical weapons
6) atropine is antidote plus supportive therapy

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40
Q

Atropine category

A

ANS - parasympatholytic

41
Q

Atropine MOA

A

muscarinic receptor antagonist

42
Q

Atropine distinguishing characteristics

A

1) Tertiary ammonium compound
2) Ester group required for activity
3) resistance to hydrolysis by esterases
4) metabolized in liver with half life of about 4 hr

43
Q

Atropine predictable characteristics

A

1) CNS toxicity esp. in children (even after ophthalmic rx)
2) inhibit SLUD and other parasympathetic activities
3) used in ophthalmology - mydriasis and cycloplegia
4) used as antidote to parasympathomimetics
5) used to tx diarrhea
6) once used to tx asthma, but now better drugs available

44
Q

Ipratropium (Atrovent) category

A

parasympatholytic

45
Q

Ipratropium (Atrovent) MOA

A

muscarinic antagonist

46
Q

Ipratropium (Atrovent) distinguishing characteristics

A

1) quaternary ammonium compound
2) minimal inhibition of mucociliary clearance
3) one of MC rx drugs

47
Q

Ipratropium (Atrovent) predictable characteristics

A

1) no CNS effects
2) bronchodilation - used to tx asthma and COPD
3) limited mucous accumulation

48
Q

Scopolamine category

A

ANS - parasympatholytic

49
Q

Scopolamine MOA

A

muscarinic receptor antagonist

50
Q

Scopolamine distinguishing characterics

A

1) from plant source - Hyocyamus niger
2) Greater CNS distribution than atropine
3) other characteristic similar to atropine

51
Q

Scopolamine predictable characteristics

A

1) greater CNS s/e and abuse potential than atropine
2) used less frequently than atropine
3) used to tx motion sickness

52
Q

Type(s) of sympathomimetic drug(s)

A
  • alpha agonists (alpha 1 and alpha 2 )
  • beta agonists (beta 1 and beta 2)
  • alpha and beta agonist
  • monamine oxidase inhibitors
53
Q

Type(s) of sympatholytic drug(s)

A
  • adrenergic antagonists (alpha antagonists, beta 1 and 2 antagonists, beta 1 antagonist)
  • adrenergic depletor (reserpine)
54
Q

Epinephrine category

A

ANS - sympathomimetic

55
Q

Epinephrine MOA

A

stimulate alpha and beta receptors (G protein which facilitate second messengers)

56
Q

Epinephrine distinguishing characteristics

A

1) metabolized in gut, blood and multiple tissues

2) more beta and less alpha activity than NE

57
Q

Epinephrine predictable characteristics

A

1) ineffective orally
2) very short half-life (minutes)
3) cardiac emergencies
4) bronchospasm - drug of choice for anaphylaxis
5) adjunct to local anesthesia
6) s/e: tachycardia, increased force of contraction, BP disturbance (usu. HTN)

58
Q

Is Epinephrine a good drugs for asthma?

A

NO

although it bronchodilates, it also vasoconstricts so it increases BP and strain on ht.; epi is too broad in its action to be used for asthma tx

59
Q

Phenylephrine (Neosynephrine) category

A

ANS - sympathomimetic

60
Q

Phenylephrine (Neosynephrine) MOA

A

alpha 1 receptor agonist

61
Q

Phenylephrine (Neosynephrine) distinguishing characteristics

A

1) effective orally

2) limited access to CNS

62
Q

Phenylephrine (Neosynephrine) predictable characteristics

A

1) nasal decongestant
2) mydriatic
3) s/e: rebound congestion, increased peripheral resistance (don’t use in HTN pt.), reflex bradycardia (d/t carotid reflex)

63
Q

Clonidine (Catapres) category

A

ANS - sympathomimetic ?

(actually reduces NE released b/c it’s an alpha 2 receptor agonist…so although it’s stimulating adrenergic receptors, it’s actually causing more of a parasympathetic response)

64
Q

Clonidine (Catapres) MOA

A

alpha 2 receptor agonist

65
Q

Clonidine (Catapres) distinguishing characteristics

A

1) effective orally
2) crosses BBB
3) prefers alpha receptors in brainstem
4) long half-life and duration of action
5) Diminish d/c from medular vasomotor center

66
Q

Clonidine (Catapres) predictable characteristics

A

1) antihypertensive

2) s/e: dry mouth, sedation, sexual dysfn

67
Q

Isoproterenol (Isuprel) category

A

ANS - sympathomimetic

68
Q

Isoproterenol (Isuprel) MOA

A

beta 1 and 2 receptor agonist

more selective than EPI b/c it stimulates beta but not alpha receptors

69
Q

Isoproterenol (Isuprel) distinguishing characteristics

A

1) metabolized by COMT
2) short duration of action
3) both beta 1 and beta 2

70
Q

Isoproterenol (Isuprel) predictable characteristics

A

1) cardiac arrest
2) actions include tachycardia and bronchodilation
3) replaced often by more selective beta agonists - it was used to tx asthma d/t bronchodilation, but it also cz tachycardia and in asthma there is already a strain on the heart

71
Q

Albuterol (Ventolin) category

A

ANS - sympathomimetic

72
Q

Albuterol (Ventolin) MOA

A

Beta 2 receptor agonist

thus we can get bronchodilation w/out tachycardia

73
Q

Albuterol (Ventolin) distinguishing characteristics

A

1) effective orally or by inhalation
2) limited cardiovascular effects
3) duration of action several hours

74
Q

Albuterol (Ventolin) predictable characteristics

A

1) bronchodilator

2) s/e: weak and occasional tachycardia, vasodilation

75
Q

Amphetamine category

A

ANS sympathomimetic

76
Q

Amphetamine MOA

A

stimulates release of NE and dopamine

77
Q

Amphetamine distinguishing characteristics

A

1) enters CNS

2) inhibits MAO

78
Q

Amphetamine predictable characteristics

A

1) alpha and beta stimulation by NE (vasoconstriction, cardiac stimulation, incr. BP, mydriasis)
2) CNS stimulation (euphoria, insomnia, anxiety, loss of appetite, hyperthermia)
3) tx: narcolepsy, obesity, ADHD
4) high abuse potential makes it scheduled substance

79
Q

Phenelzine (Nardil) category

A

ANS - sympathomimetic

80
Q

Phenelzine (Nardil) MOA

A

monoamine oxidase inhibitor

MAO is the main enzyme responsible for breaking down catecholamines - Epi, NE, dopamine

81
Q

Phenelzine (Nardil) distinguishing characteristics

A

1) readily absorbed
2) crosses BBB
3) increases synaptic catecholamine levels

82
Q

Phenelzine (Nardil) predictable characteristics

A

1) antidepressant

2) s/e: sympathomimetic actions

83
Q

Types of sympatholytics

**not on exam

A

1) adrenergic antagonists (alpha antagonist, beta 1 and 2 antagonist, beta 1 antagonist)
2) adrenergic depletor

84
Q

Prazocin (Minipress) category

**not on exam

A

ANS - sympatholytic

85
Q

Prazocin (Minipress) MOA

**not on exam

A

alpha 1 receptor antagonist

86
Q

Prazocin (Minipress) distinguishing characteristics

**not on exam

A

1) effective orally
2) highly protein bound (5% free)
3) reflex tachycardia

87
Q

Prazocin (Minipress) predicted characteristics

**not on exam

A

1) tx HTN

2) s/e: hypotension, syncope

88
Q

Propranolol (Inderal) category

**not on exam

A

ANS - sympatholytic

89
Q

Propranolol (Inderal) MOA

**not on exam

A

Beta 1 and 2 receptor antagonist

90
Q

Propranolol (Inderal) distinguishing characteristics

**not on exam

A

1) very lipid soluble
2) significant 1st pass metabolism
3) highly variable plasma levels
4) multiple uses (not all very predictable)

91
Q

Propranolol (Inderal) predictable characteristics

**not on exam

A

1) use: antihypertensive, anti-angina, anti-arrythmic

2) s/e: place asthma pt. at risk, place diabetics at risk

92
Q

Metoprolol (Lopressor) category

**not on exam

A

ANS - sympatholytic

93
Q

Metoprolol (Lopressor) MOA

**not on exam

A

Beta 1 receptor antagonist

94
Q

Metoprolol (Lopressor) predictable characteristics

**not on exam

A

1) antihypertensive w/out risk to asthmatics and diabetics

95
Q

Reserpine category

**not on exam

A

ANS - sympatholytic

96
Q

Reserpine MOA

**not on exam

A

promotes release of NE and reduces reuptake resulting in depletion of NE stores

97
Q

Reserpine distinguishing characteristics

**not on exam

A

1) derived from plant
2) transitory sympathomimetic followed by prolonged sympatholytic effect
3) antiquated for therapeutic use, extensive research use

98
Q

Reserpine predictable characteristics

**not on exam

A

1) antihypertensive

2) s/e: prolonged paralysis of sympathetic nervous system

Pharmacology (14 decks)

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