Pharmacology - Autonomic Drugs Part 1 Flashcards Preview

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Flashcards in Pharmacology - Autonomic Drugs Part 1 Deck (125):
1

From which regions of the central nervous system do parasympathetic nerves originate?

Cranial and sacral regions

2

From which regions of the central nervous system do sympathetic nerves originate?

Thoracic and lumbar regions

3

What types of nerves arise from the spinal cord and innervate skeletal muscle directly?

Somatic nerves

4

How many neurons are involved in parasympathetic transmission from the spinal cord to the target organ?

2

5

True or False? Craniosacral parasympathetic axons synapse on neurons in the peripheral ganglia.

True

6

What neurotransmitter mediates parasympathetic nervous system function?

Acetylcholine

7

What neurotransmitter receptor mediates parasympathetic nervous system function at the peripheral ganglia?

Nicotinic acetylcholine receptors

8

What neurotransmitter receptor mediates parasympathetic tone in the cardiac muscle?

Muscarinic acetylcholine receptors (specifically, M2)

9

What neurotransmitter receptor mediates parasympathetic tone in the smooth muscle?

Muscarinic acetylcholine receptors (specifically, M3)

10

What neurotransmitter receptor mediates parasympathetic tone in the glandular cells?

Muscarinic acetylcholine receptors (specifically, M1 and M3)

11

Somatic nerves that arise from the spine innervate skeletal muscle. What neurotransmitter receptor, which is located on skeletal muscle, receives this input?

Nicotinic acetylcholine receptors

12

How many neurons are involved in sympathetic transmission from the spinal cord to the target organ?

2

13

Where is the first synapse after the spinal cord in sympathetic innervation of an organ?

Preganglionic sympathetic axons synapse on neurons in the paravertebral ganglia

14

True or False? Preganglionic sympathetic axons synapse on neurons in the peripheral ganglia.

False; preganglionic sympathetic axons synapse on neurons in the paravertebral ganglia

15

At the paravertebral ganglia, the neurotransmitter _____ acts on _____ receptors to mediate sympathetic nervous system function.

Acetylcholine; nicotinic acetylcholine

16

What neurotransmitter mediates sympathetic nervous system function at the sweat glands?

Acetylcholine

17

What neurotransmitter receptor mediates sympathetic nervous system function at the sweat glands?

Muscarinic acetylcholine receptors

18

What neurotransmitter mediates sympathetic tone in the cardiac muscle, smooth muscle, and glandular cells?

Norepinephrine

19

What are four cell types in which α- and β-adrenergic receptors mediate sympathetic tone?

Cardiac muscle, smooth muscle, glandular cells, and terminal ends of neurons

20

What neurotransmitter mediates sympathetic tone in the renal vascular smooth muscle?

Dopamine

21

What neurotransmitter receptor mediates sympathetic tone in the renal vascular smooth muscle?

D1 receptors

22

What two substances are released into the blood from the adrenal medulla after the activation of the sympathetic nervous system?

Epinephrine and norepinephrine

23

How many synapses are involved in activation of the adrenal medulla?

One; the adrenal medulla releases epinephrine and norepinephrine into the blood

24

Are nicotinic acetylcholine receptors ligand-gated sodium-potassium channels or G-protein coupled receptors?

Nicotinic receptors are ligand gated sodium-potassium channels

25

Are muscarinic acetylcholine receptors ligand-gated sodium-potassium channels or G-protein-coupled receptors?

Muscarinic acetylcholine receptors are G-protein-coupled receptors that act through second messengers

26

To what class of G-proteins are α1-receptors linked?

q

27

To what class of G-proteins are α2-receptors linked?

i

28

To what class of G-proteins are β1-receptors linked?

s

29

To what class of G-proteins are β2-receptors linked?

s

30

To what class of G-proteins are M1-receptors linked?

q

31

To what class of G-proteins are M2-receptors linked?

i

32

To what class of G-proteins are M3-receptors linked?

q

33

To what class of G-proteins are D1-receptors linked?

s

34

To what class of G-proteins are D2-receptors linked?

i

35

To what class of G-proteins are H1-receptors linked?

q

36

To what class of G-proteins are H2-receptors linked?

s

37

To what class of G-proteins are V1-receptors linked?

q

38

To what class of G-proteins are V2-receptors linked?

s

39

What are the major effects of α1-receptor activation?

It increases vascular smooth muscle contraction, and increases pupillary dilator muscle contraction (mydriasis)

40

What are the major functions of α2-receptor activation?

It decreases sympathetic outflow and decreases insulin release

41

What are the major functions of β1-receptor activation?

It increases heart rate and contractility, increases renin release from the kidneys, and increases lipolysis of adipose tissue

42

What is the major function of β2-receptor activation on the body's vasculature?

Vasodilation

43

What is the major function of β2-receptor activation on the respiratory system?

Bronchodilation

44

What effect does β2-receptor activation have on glucagon release?

It increases glucagon release

45

Where are M1-receptors located?

The central nervous system

46

What effect does M2-receptor activation have on cardiac function?

It decreases heart rate and contractility

47

What are the effects of M3-receptor activation?

Increased exocrine gland secretions, gut peristalsis, bladder contraction, bronchoconstriction, miosis, and accommodation

48

What effect does D1-receptor activation have on renal vasculature?

It relaxes renal vascular smooth muscle

49

What are the effects of H1-receptor activation?

Pruritis, pain, nasal and bronchial mucus production, contraction of bronchioles

50

What is the effect of H2-receptor activation?

It increases gastric acid secretion

51

What effect does V1-receptor activation have on vascular smooth muscle?

It increases vascular smooth muscle contraction

52

The activation of what two types of G-protein-coupled receptors can increase vascular smooth muscle contraction? Which receptors mediate vascular relaxation?

α1- and V1-receptors increase contraction; relaxation is mediated by β2, and D1 (renal only)

53

What is the effect of V2-receptor activation? Where are they located?

It increases water permeability and reabsorption in the collecting tubules of the kidney

54

What five types of receptors are coupled with Gqproteins?

α1, M1, M3, H1, and V1

55

What five types of receptors are coupled with Gsproteins?

β1, β2, D1, H2, and V2

56

What three types of receptors are coupled with Giproteins?

a2, M2, and D2

57

What enzyme is activated directly downstream of Gq-coupled receptors?

Phospholipase C

58

What enzyme is activated directly downstream of Gs-coupled receptors?

Adenyl cyclase

59

What enzyme is inhibited directly downstream of Gi-coupled receptors?

Adenyl cyclase

60

Adenyl cyclase catalyzes the conversion of adenosine triphosphate into what molecule?

cAMP

61

What final effector enzyme is activated by receptors that are coupled with Gsproteins?

Protein kinase A

62

What final effector enzyme is inhibited by receptors that are coupled with Giproteins?

Protein kinase A

63

Phospholipase C catalyzes the cleavage of membrane lipids into what molecules?

Inositol trisphosphate3 and diacylglycerol

64

What is the effect of increased inositol triphosphate on the intracellular concentration of calcium?

It increases the intracellular calcium concentration

65

What enzyme is activated by diacylglycerol?

Protein kinase C

66

What pharmacologic agent blocks the uptake of choline into cholinergic nerve terminals?

Hemicholinium

67

What enzyme is responsible for the formation of acetylcholine? What are its two substrates?

Choline acetyltransferase; Acetyl-CoA and choline

68

What pharmacologic agent blocks the transport of acetylcholine into the presynaptic vesicles in nerve terminals?

Vesamicol

69

The entry of what ion into the nerve terminal induces the release of acetylcholine into the synaptic cleft?

Calcium

70

What toxin inhibits the calcium-induced release of acetylcholine from the cholinergic nerve terminals?

Botulinum

71

What enzyme breaks down acetylcholine in the synaptic cleft? What two products result from this reaction?

Acetylcholinesterase; choline and acetate

72

Tyrosine transporters are located in the nerve terminals of what type of cells?

Noradrenergic cells; tyrosine is the precursor of norepinephrine

73

Tyrosine is a precursor to the formation of which neurotransmitters? What is the order of their synthesis?

Tyrosine, DOPA, dopamine, norepinephrine, epinephrine

74

What pharmacologic agent blocks the conversion of tyrosine to DOPA?

Metyrosine

75

Tyrosine is converted into dopamine via what intermediate precursor?

DOPA; DOPA can be used as a pharmacologic agent to increase central nervous system dopamine

76

What pharmacologic agent blocks the transport of dopamine into the presynaptic vesicles in nerve terminals?

Reserpine

77

Dopamine is converted into norepinephrine in the ______ (cytoplasm/presynaptic vesicle).

Presynaptic vesicles

78

The entry of what ion into the nerve terminal induces the release of norepinephrine into the synaptic cleft?

Calcium

79

What pharmacologic agent inhibits the calcium-induced release of norepinephrine from the noradrenergic nerve terminals?

Guanethidine

80

What pharmacologic agent stimulates the release of norepinephrine from the noradrenergic nerve terminals?

Amphetamine

81

How is norepinephrine cleared form the synaptic cleft?

Diffusion, metabolism (monoamine oxidase A), and reuptake

82

What pharmacologic agents inhibit the reuptake of norepinephrine into the nerve terminals?

Cocaine, amphetamine, and tricyclic antidepressants

83

What three receptor types modulate the presynaptic release of norepinephrine from the noradrenergic nerve terminals?

M2-receptors, angiotensin II receptors, and α2-receptors

84

What effect does the activation of α2-receptors in presynaptic sympathetic nerve terminals have on norepinephrine release?

It inhibits norepinephrine release

85

What effect does the activation of angiotensin II receptors in presynaptic sympathetic nerve terminals have on norepinephrine release?

It stimulates norepinephrine release

86

What effect does the activation of M2-receptors in presynaptic sympathetic nerve terminals have on norepinephrine release?

It inhibits norepinephrine release

87

The norepinephrine-mediated activation of α2-receptors on presynaptic sympathetic nerve terminals is an example of a mechanism of what type of feedback?

Negative feedback

88

Name four direct cholinergic agonists.

Bethanechol, carbachol, pilocarpine, methacholine

89

What is the clinical application of bethanechol?

Treatment of postoperative and neurogenic ileus and urinary retention (remember: Beth Anne, call (bethanechol) me if you want to activate your Bowels and Bladder)

90

What is the mechanism of action of bethanechol?

Bethanechol is a direct cholinergic agonist resistant to acetylcholinesterase that works on receptors in the bowel and bladder

91

What two direct agonist cholinomimetic drugs can be used to treat glaucoma?

Carbachol and pilocarpine

92

Carbachol and pilocarpine are effective for the treatment of open-angle glaucoma because they activate what muscle?

The ciliary muscle of the eye

93

What is a methacholine challenge test?

A test in which methacholine is inhaled to stimulate muscarinic receptors and induce bronchoconstriction to diagnose asthma

94

Pilocarpine is effective for the treatment of narrow-angle glaucoma because it activates what muscle?

The pupillary sphincter

95

True or False? Pilocarpine is susceptible to acetylcholinesterase.

False; pilocarpine is resistant to acetylcholinesterase

96

Name five indirect cholinergic agonists.

Neostigmine, pyridostigmine, edrophonium, physostigmine, echothiophate

97

What are the clinical indications for use of neostigmine?

The treatment of postoperative and neurogenic ileus

98

True or False? The treatment of myasthenia gravis is a clinical application of pyridostigmine.

True

99

Which anticholinesterase is used to diagnose myasthenia gravis? Why?

Edrophonium; the effects last for minutes and if weakness is transiently reversed it is diagnostic of myasthenia gravis

100

True or False? The treatment of glaucoma is a clinical application of physostigmine.

True (remember: "PHYS is for the EYES")

101

Which pharmacologic agent is used to treat atropine overdose?

Physostigmine, because it crosses the blood-brain barrier and is able to reverse central nervous system as well as peripheral nervous system effects

102

What is the clinical indication for use of echothiophate?

The treatment of glaucoma

103

Indirect cholinergic agonists increase endogenous acetylcholine by inhibiting what enzyme?

Acetylcholinesterase

104

Why is pyridostigmine used to treat myasthenia gravis?

It increases the amount of acetylcholine in the neuromuscular synapse, thereby increasing muscle strength

105

What effect does neostigmine have on the central nervous system?

None; it does not penetrate the blood-brain barrier (remember: NEO CNS = NO CNS)

106

What is the clinical application and mechanism of action of topical atropine, homatropine, and tropicamide?

These drugs antagonize muscarinic receptors in the eye to produce mydriasis and cycloplegia

107

What is the mechanism and clinical application for benztropine?

It is a muscarinic antagonist used to reduce symptoms of Parkinson's disease

108

What is the mechanism and clinical application for scopolamine?

It is a muscarinic antagonist used to treat motion sickness

109

What is the mechanism and clinical application for ipratropium?

It is a muscarinic antagonist used to treat asthma and chronic obstructive pulmonary disease (remember: I PRAY I can breathe soon!)

110

What is the mechanism and clinical application for methscopolamine?

It is a muscarinic antagonist used to treat peptic ulcers

111

What is the mechanism and clinical application for oxybutynin?

It is a muscarinic antagonist used to reduce urgency in mild cystitis and reduce bladder spasms

112

What is the mechanism and clinical application for glycopyrrolate?

It is a muscarinic antagonist used to reduce urgency in mild cystitis and reduce bladder spasms

113

What is the mechanism and clinical application for pirenzepine?

It is a muscarinic antagonist used to treat peptic ulcers

114

What is the mechanism and clinical application for propantheline?

It is a muscarinic antagonist used to treat peptic ulcers

115

Which muscarinic antagonist can be used to reduce urgency in patients with mild cystitis?

Oxybutynin (also glycopyrrolate)

116

Which muscarinic antagonist is most commonly used to treat motion sickness?

Scopolamine

117

Which muscarinic antagonist can be used to treat bladder spasms?

Oxybutynin (also glycopyrrolate)

118

You recently prescribed haloperidol to your patient to treat his schizophrenia, but he has since developed Parkinson's-like motor adverse effects. What drug could you add to his regimen to treat this?

Benztropine

119

Atropine is used for therapeutic effect in which four organ systems?

Eyes, gastrointestinal system, respiratory system, urinary system

120

What are the two effects of atropine on the eye?

Pupil dilation, cycloplegia

121

What is the effect of atropine on the airway mucosa?

It decreases secretions

122

What is the effect of atropine on the stomach?

It decreases acid secretion

123

What is the effect of atropine on gastrointestinal motility?

It decreases motility

124

What is the effect of atropine on the bladder in a patient with cystitis?

It decreases urgency

125

A patient affected by botulinum toxin will be affected at which neurotransmitter/receptor group(s)?

Botulinum toxin affects all neurotransmitter/receptor groups that have acetylcholine as the neurotransmitter

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