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Pharmacology > Autonomics > Flashcards

Autonomics Flashcards

1
Q

Mecamylamine mechanism

A

non-competitive antagonist of the nicotinic ganglionic receptors

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2
Q

Botulinum toxin type A mechanism

A

Inactivates SNAP25 inhibiting exocytosis

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3
Q

Muscarine mechanism

A

Muscarinic receptor agonist found in mushrooms

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4
Q

Atropine mechanism

A

Competitive antagonist for muscarinic receptors found in nightshade and jimson weed

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5
Q

Nicotine mechanism

A

Nicotinic receptor agonist

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6
Q

d-Turbocurare mechanism

A

Competitive antagonist for nicotinic receptors at NMJ

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7
Q

non-competitive antagonist of the nicotinic ganglionic receptors

A

Mecamylamine

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8
Q

Inactivates SNAP25 inhibiting exocytosis

A

Botulinum toxin type A

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9
Q

Muscarinic receptor agonist found in mushrooms

A

Muscarine

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10
Q

Competitive antagonist for muscarinic receptors found in nightshade and jimson weed

A

Atropine

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11
Q

Nicotinic receptor agonist

A

Nicotine

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12
Q

Competitive antagonist for nicotinic receptors at NMJ

A

d-Turbocurare

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13
Q

Preganglionic fibers exit from thoracic and lumbar regions of spinal chord

A

Sympathetic

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14
Q

Preganglionic fibers exit from cranial and sacral regions of CNS

A

Parasympathetic

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15
Q

Ganglia within CNS

A

Somatic

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16
Q

One efferent, myelinated nerve fiber from ganglia

A

Somatic

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17
Q

Denervation produces muscle atrophy

A

Somatic

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18
Q

Ganglia outside CNS

A

Autonomic

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19
Q

Two efferent non-myelinated nerve fibers

A

Autonomic

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20
Q

Two neurotransmitters of the autonomic nervous system

A

Norepinephrine and acetylcholine

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21
Q

Denervation revelats intrinsic tone

A

Autonomic

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22
Q

What is the primary site of drug action in the ANS

A

postganglionic nerves

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23
Q

What is the primary site of ANS integration into the CNS

A

hypothalmus

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24
Q

What is the CNS site of integration of cardiovascular reflexes and blood pressure control

A

medulla oblongata

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25
Q

ANS division with Discrete innervation

A

Parasympathetic

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26
Q

ANS division with diffuse innervation

A

Sympathetic

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27
Q

ANS division distributed to all tissues

A

Sympathetic

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28
Q

ANS division with chain ganglia

A

Sympathetic

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29
Q

ANS division with long pre-ganglionic fiber

A

Parasympathetic

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30
Q

The adrenal medulla is part of which ANS division

A

Sympathetic

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31
Q

What ANS division innervates the sweat glands? Which type of receptors are found there?

A

Sympathetic, Muscarinic

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32
Q

Name the receptor subtypes in the SA node of the heart which ANS division they belong to and the responses they illicit

A

M2, parasympathetic, decrease heart rate

B1, sympathetic, increase heart rate

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33
Q

Name the receptor subtypes in the AV node of the heart which ANS division they belong to and the responses they illicit

A

M2, parasympathetic, decrease conduction velocity

B1, sympathetic, conduction velocity

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34
Q

What is the SA node of the heart

A

the sinoatrial node is the impulse-generating (pacemaker) tissue located in the right atrium of the heart, and thus the generator of normal sinus rhythm.

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35
Q

What is the AV node of the heart

A

The atrioventricular node controls conduction velocity

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36
Q

Name the receptor subtypes in the atria and ventricles of the heart which ANS division they belong to and the respones they illicit

A

M2, parasympathetic, decrease contractility

B1, sympathetic, increase contractility

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37
Q

Name the receptor subtypes in the blood vessels, which ANS division they belong to and the responses they illicit

A

Innervated by sympathetic only
Skeletal muscle-Alpha1 (Constriction), Beta2 (Dilation),
but contains M3 which constricts VSM, but causes NO release from endothelium resulting in dilation of VSM.

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38
Q

What occurs when MAP drops?

A

baroreceptors inactivate and there is increased sympathetic outflow

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39
Q

What occurs when MAP rises

A

baroreceptors activate increasing parasympathetic outflow.

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40
Q

What are the three tissues where sympathetic innervation is dominant

A

arterioles, veins, and sweat glands

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41
Q

What is the enzyme that synthesizes acetylcholine

A

Choline acetyl-transferase (CAT)

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42
Q

What two molecules are combined to create acetylcholine

A

Acetyl CoA and choline

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43
Q

What is the rate limiting step of acetylcholine synthesis

A

Transport of choline into nerve terminal by active transport

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44
Q

What are therapeutic uses of botulinum toxin type A

A

1) IM for muscle spasms/dystonias
2) Cosmetic
3) Intradermal for axillary hyperhidrosis (sweating)
4) Overactive bladder

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45
Q

Name the two enzymes that degrade acetylcholine

A

Acetylcholinesterase (AChE) and Butyrylcholinesterase

46
Q

Name in order the intermediates in epinephrine synthesis

A

Tyrosine, Dopa, Dopamine, Norepinephrine

47
Q

What is reserpine’s MOA

A

irreversibly blocks VMAT-2 which depletes catecholamines from nerve terminals

48
Q

Therapeutic use of reserpine

A

anti-hypertensive agent and antipsychotic

49
Q

Side effects of reserpine

A

sedation, unopposed cholinergic effects (cramping, diarrhea), depression

50
Q

Tyramine’s MOA

A

displaces NE from vesicles leading to increased cytosolic concentrations and reversal of NE transporter actions

51
Q

Where is tyramine found

A

In the diet. Aged cheeses, beer, wine, soy sauce, smoked meats, etc.

52
Q

In what patients is tyramine a concern

A

Those taking MAOIs, since tyramine is normally degraded by MAO in the GI tract

53
Q

Methyldopa’s MOA

A

prodrug that is converted to methyl-NE and is an alpha-2 selective adrenergic receptor agonist. Since it does not stimulate the other receptors it is called a false transmitter. alpha-2 stimulation reduces sympathetic outflow from the CNS

54
Q

Clinical use of methyldopa

A

oral antihypertensive agent that can be used safely during pregnancy

55
Q

Side effects of methyldopa

A

sedation, dry mouth, parkinsonism and hyperlactinemia

56
Q

Where are alpha-1 receptors and what response do they mediate

A

smooth muscle contraction

57
Q

Where are alpha-2 receptors and what response do they mediate

A

Inhibitory response on nerves including presynaptic autoreceptors

58
Q

Where are Beta-1 receptors and what response do they mediate

A

excitation of the heart, contraction of the kidney

59
Q

Where are Beta-2 receptors and what response do they mediate

A

relaxation of the lung, skeletal muscle, vasculature, uterus.

60
Q

What are two mechanisms of NE signal termination

A

neuronal re-uptake via NET

Extraneuronal uptake by ENT

61
Q

Cocaine’s MOA

A

Inhibits NE reuptake, causes excess NE in the synapse

62
Q

Name the two enzymes that metabolize catecholamines

A

MAO-mitochondrial, catechol-O-methyltransferase (COMT)- cytosolic (liver, kidney)

63
Q

Only clinical use for acetylcholine

A

Wide angle glaucoma, contraction of the ciliary muscle opens trabelcular meshwork and increases outflow of aqueous humor

64
Q

Do synthetic choline esters or cholinomimetic alkaloids penetrate the BBB

A

cholinomimetic alkaloids penetrate the BBB

65
Q

bethanechol info

A

Synthetic choline ester
Prolonged effects, resistant to hydrolysis by cholinesterases
postop, postpartum urinary retention
GERD gastric atony

66
Q

pilocarpine info

A

cholinomimetic alkaloid
Partial agonist of all muscarinic subtypes
Topical for wide-angle glaucoma
xerostomia (dry mouth)

67
Q

cevimeline info

A

Cholinomimetic alkaloid
selective M3 agonist
Dry mouth for Sjogren’s syndrome
Longer duration, fewer side effects than pilocarpine

68
Q

Toxicity of muscarinic agonists

A

Sweating, hypotension, cramps, diarrhea

69
Q

Contraindication of muscarinic agonists

A

hyperthyroidism (reflex tachycardia), asthma, peptic ulcer

70
Q

Antidotes for muscarinic agonists

A

atropine and/or epinephrine

71
Q

Atropine pharmokinetics

A

readily crosses BBB

72
Q

What is the therapeutic indication for atropine?

A

Peptic ulcers

73
Q

Name two reasons atropine is not a good drug for treating peptic ulcers

A
  1. Toxicities at low doses (reduced secretions, mydriasis, cycloplegia, tachycardia, constipation, retention), therapeutic effect at high doses (10mg)
  2. Only partially reduces gastric acid secretion
74
Q

What is the effect of atropine on the CNS

A

mild excitation at low doses, toxic doses produce hallucinations and delirium resembling psychosis
(not present with scopolamine)

75
Q

What are the ocular effects of atropine

A

mydriasis and photophobia, cycloplegia (paralysis of near vision)

76
Q

What are the cardiovascular effects of atropine

A

Heart:
transient slowing due to blockade of M1 autoreceptors
tachycardia from blocking parasympathetic impulses
Circulation:
no effect at normal dose, flushing reaction by unknown mechanism

77
Q

What are the respiratory effects of atropine

A

decrease bronchial secretions, relaxes bronchial smooth muscle

78
Q

What are the GI effects of atropine

A

inhibits salvation, reduces motility and tone, partial reduction in gastric acid secretion

79
Q

What are the 4 therapeutic uses of atropine

A
  1. preoperative medication to reduce secretion
  2. Bradycardia and AV block cardiac resuscitation
  3. Mydriasis and cycloplegia (long duration)
  4. Acetylcholinesterase inhibitor poisoning
80
Q

Adverse effects of atropine

A

dry mouth, blurred vision, photophobia, tachycardia, GI distress (constipation), hot and dry skin

81
Q

Contraindications for atropine

A

prostatic hypertrophy (trouble urinating), narrow-angle glaucoma

82
Q

Atropine antidote

A

physostigmine, anti-cholinsterase

83
Q

Drug interactions with atropine

A

drugs with anti-cholinergic side effects: antihistamines, phenothiazines, tricyclic antidepressants

84
Q

Scopoamine info

A

muscarinic antagonist
better CNS penetration than atropine
sedative
can produce euphoria
suppresses emesis due to effect on vestibular apparatus
prophylatic patch for motion sickness and recovery from anesthesia

85
Q

Ipratropium bromide info

A

muscarinic antagonist

quaternary amine-does not cross membranes

86
Q

Tropicamide

A

muscarinic antagonist
For diagnosis and surgery of ophthalmic disorders
mydriatic, cycloplegic
shorter duration (6 hrs) than atropine (7-12 d)
blurred vision and photophobia are side effects

87
Q

Tolterodine

A

muscarinic antagonist for treatment of overactive bladder (urge incontinence)
unclear mechanism, only 30% effective
CNS-related anti-cholinergic effects, especially in elderly

88
Q

Neostigmine

A

Anticholinesterase, only one that also acts as an angonist at NMJ nicotinic receptors. Therapeutically used for myasthenia gravis. Reversal of d-Turbocurarine poisoning. Post operative urinary retention.

89
Q

Physostigmine

A

Anticholinesterase. Blood-brain permeable, mostly used for atropine poisoning.

90
Q

Donepezil

A

Anticholinesterase. CNS selective, used to ameliorate Alzheimer’s symptoms.

91
Q

Malathion

A

Irreversible cholinesterase inhibitor. Nerve gas. Antidotes Atropine and Pralidoxime

92
Q

Pralidoxime

A

reactivates AChE at NMJ, but must be done before aging occurs.

93
Q

Features of catecholamine sympathomimetics

A

Not orally effective, short duration of action, does not cross BBB.

94
Q

Features of non-catecholamine sympathomimetics

A

do not contain catechol functional group. orally effective, long duration of action, CNS effects

95
Q

effects of alpha-1 activation

A

Vasoconstriction- homeostasis, decongestant, prolong anesthetics, blood pressure elevation
Mydriasis without cycloplegia (phenylephrine)

96
Q

Effects of alpha-2 activation

A

CNS- reduces CNS sympathetic outflow

Glaucoma- reduces intaocular pressure reduction of aqueous humor from cilliary body. (clonidine)

97
Q

Effects of beta-1 activation

A

Increase cardiac output, treatment of shock (dobutamine)

98
Q

Effects of beta-2 activation

A

Asthma and COPD, delay preterm labor (tertbutaline)

99
Q

epinephrine receptor

A

all adrenergic receptors agonist

100
Q

norepinephrine receptor

A

Alpa-1, Alpha-2, Beta-1 agonist

101
Q

Isoproterenol receptor

A

Beta-2, Beta-2 agonist

102
Q

Dopamine receptor

A

D1, B1, A1 agonist

103
Q

Dobutamine receptor

A

B1 agonist

104
Q

Phenylephrine receptor

A

A1 agonist

105
Q

clonidine receptor

A

A2 agonist

106
Q

terbutaline receptor

A

B2 agonist

107
Q

Effect of alpha-1 blockade

A

reduced blood pressure, BPH, coldness of extremities

108
Q

Beta-1 blockade

A

reduce blood presure, angia pectoris and MI, CHF and cardiac arrhythmias, decrase intaocular pressure, stage fright, migrane.

109
Q

prazosin receptor

A

Alpha-1 antagonist

110
Q

tamsulosin receptor

A

Alph-1a antagonist, used for BPH

111
Q

Propranolol receptor

A

Beta-1,2 antagonist

112
Q

Metapropol receptor

A

Beta-1 antagonist

Pharmacology (35 decks)

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