Autonomic pharm II Flashcards

1
Q

What are the receptors on the ciliary muscle of the eye? What happens when each is activated?

A
M3 = contraction (parasymp)
B2 = Relaxation (symp)
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2
Q

What are the receptors on the ciliary body of the eye? What happens when they are activated?

A

B1, B2

Increased aqueous humor production

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3
Q

Stimulation of the M receptors on the sphincter muscle and ciliary muscle causes what?

A

Miosis and spasm of accomodation

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4
Q

Activation of what receptors on the pupillary radial muscle causes mydriasis?

A

A1

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5
Q

What are the receptors on blood vessels that cause vasorelaxation? MOA?

A

M3–ACh allows Ca to flow into cells, leading to NO production

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6
Q

What is the MOA of NO?

A

Stimulation of guanylyl cyclase to make cGMP, inhibiting enzymes

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7
Q

When the endothelium of a blood vessel is damaged what happens to lose its ability to relax?

A

Fails to produce NO

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8
Q

How does the neuromuscular plate function?

A

ACh depolarizes the muscle membrane, allowing Na to produce EPSP

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9
Q

What leads to the stopping of signal for the neuromuscular junction?

A

AChesterases

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10
Q

What happens to nicotinic receptors on excessive activation?

A

desensitization

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11
Q

True or false: all autonomic ganglia have nicotinic receptors?

A

True

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12
Q

If all autonomic ganglia have nicotinic receptors, how does the ANS produce para and symp results?

A

Depends on the balance between symp and para innervation at a given tissue

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13
Q

Blood vessels are solely innervated by which division of the ANS?

A

Symp (leads to vasoconstriction)

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14
Q

The GI tract is solely innervated by which division of the ANS?

A

Para

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15
Q

What is the type of nicotinic receptor on the adrenal medulla? What is the response it elicits?

A

Nn, secretion of E and NE

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16
Q

What is the type of nicotinic receptor on autonomic ganglia? What is the response it elicits?

A

Nn–stimulation

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17
Q

What is the type of nicotinic receptor on the neuromuscular junction? What is the response it elicits?

A

Nm

muscle action

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18
Q

What are cholinomimetic drugs?

A

Drugs that work on choline receptors

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19
Q

What are the direct acting cholinomimetic drugs?

A

Cholinoceptor agonists (activate Muscarinic or nicotinic receptors)

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20
Q

What are the indirect acting cholinomimetic drugs?

A

inhibit acetylcholine esterase

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21
Q

NO synthase produces NO from what chemical?

A

R

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22
Q

Increasing [Ca] in vascular smooth muscle results in what?

A

Constriction

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23
Q

M3 activation in sphincters results in what? What is the one exception to this?

A

Relaxation

Lower esophageal sphincter will constrict

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24
Q

M3 activation in glands results in what?

A

Secretion

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25
Q

M3 activation on the bladder results in what?

A

Relaxation

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26
Q

M3 activation on the bronchioles results in what?

A

Contraction/bronchospasm

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27
Q

M2 activation on the SA node results in what?

A

decreased HR

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28
Q

M2 activation on the AV node results in what?

A

Decreased conduction velocity

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29
Q

M3 activation in the stomach results in what?

A

motility/cramps

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30
Q

M3 activation in the intestines results in what?

A

Contraction= diarrhea

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31
Q

M3 activation on blood vessels results in what?

A

Vasodilation

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32
Q

Why must drugs that act on nicotinic receptors be used carefully?

A

Because every presynaptic nerve uses nicotinic receptors

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33
Q

What are the two types of direct acting cholinoceptor agonists?

A

Muscarinic

Nicotinic

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34
Q

What are the two types of indirect acting cholinoceptor stimulants?

A

Reversible

Irreversible

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35
Q

Muscarinic or nicotinic direct acting cholinoceptor stimulant: ACh?

A

Muscarinic

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36
Q

Muscarinic or nicotinic direct acting cholinoceptor stimulant: muscarinic?

A

Muscarinic

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37
Q

Muscarinic or nicotinic direct acting cholinoceptor stimulant: methacholine?

A

Muscarinic

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38
Q

Muscarinic or nicotinic direct acting cholinoceptor stimulant: nicotine?

A

Nicotinic

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39
Q

Muscarinic or nicotinic direct acting cholinoceptor stimulant: succinylcholine?

A

Nicotinic

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40
Q

Muscarinic or nicotinic direct acting cholinoceptor stimulant: bethanechol?

A

Muscarinic

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41
Q

Muscarinic or nicotinic direct acting cholinoceptor stimulant: carbachol?

A

Muscarinic

42
Q

Reversible or irreversible indirect acting cholinoceptor: edrophonium

A

Reversible

43
Q

Reversible or irreversible indirect acting cholinoceptor: neostigamine

A

reversible

44
Q

Reversible or irreversible indirect acting cholinoceptor:physostigmine

A

Reversible

45
Q

Reversible or irreversible indirect acting cholinoceptor: echothiophate

A

Irreversible

46
Q

Reversible or irreversible indirect acting cholinoceptor: malathion

A

Irreversible

47
Q

Reversible or irreversible indirect acting cholinoceptor: parathion

A

Irreversible

48
Q

Reversible or irreversible indirect acting cholinoceptor: denepezil

A

Reversible

49
Q

Reversible or irreversible indirect acting cholinoceptor: sarin

A

Irreversible

50
Q

All of the choline esters are what type of molecule?

A

Cationic quaternary ammonium (insoluble in lipids)

51
Q

Why are direct acting cholinoceptor agonists poorly absorbed in the GI tract and CNS?

A

insoluble in lipids

52
Q

Addition of what functional group to methacholine and bethanechol increases their half life?

A

methyl

53
Q

carbachol and bethanechol are not susceptible to which enzyme?

A

Cholinesterase

54
Q

What are the two choline esters that are not susceptible to acetylcholine esterase?

A

Carbachol

Bethanechol

55
Q

Methacholine has more muscarinic, or nicotinic action?

A

Muscarinic

56
Q

Bethanechol has more muscarinic or nicotinic action?

A

muscarinic

57
Q

What are the effects of choline esters on the cardiovascular system?

A

Hypotension

Bradycardia

58
Q

What are the effects of choline esters on the GI system? (3)

A
  • Increased tone and contractility of gut
  • Increased acid secretion
  • n/v/d
59
Q

What are the effects of choline esters on the GU system?

A

Involuntary urination

60
Q

What are the effects of choline esters on the eyes?

A

Miosis

Contraction of ciliary muscle for near vision

61
Q

What are the effects of choline esters on the respiratory system?

A

bronchoconstriction

62
Q

What are the effects of choline esters on glands?

A

Increased secretions

63
Q

What are homeostatic reflexes?

A

reflexes that respond to a stimulus to maintain homeostasis

64
Q

Why does ACh have limited clinical use?

A

Fast degradation

65
Q

What are the nicotinic effects of ACh?

A

not commonly seen since does not penetrate fat

66
Q

How does ACh cause vasodilation?

A

Acts on M3 receptors to produce NO

67
Q

What is the clinical use of methacholine?

A

Diagnosis of bronchiolar hypersensitivity via M3 receptors

68
Q

What is the use of carbachol? MOA?

A

Activates both nicotinic and muscarinic cholinoceptors,

Open canal of schlemm to decrease intraocular pressure

69
Q

What is the effect of high doses of carbachol?

A

cardiac arrest

70
Q

What are the clinical uses of Bethanechol? What receptor does it act on?

A

Acts on M3 to increase detrusor tone, and increase gastric motility

(gastric atony
Gastric emptying, urinary retention)

71
Q

Muscarine is found in what?

A

Mushrooms

72
Q

What is the MOA of muscarine?

A

Directly activates all Muscarininc, ACh receptors with x100 potency

73
Q

What are the symptoms of muscarine ingestion?

A

Increase secretions
Abdominal pain, n/v/d
Cardiac arrest

74
Q

What is the MOA of pilocarpine?

A

Direct agonist of M3

75
Q

What is pilocarpine used for in the eye? MOA?

A

Contraction of the iris sphincter muscle and ciliary muscles

Relieves glaucoma

76
Q

What is pilocarpine used for when not used in the eye?

A

Tests autonomic state

77
Q

Why should you not use choline agonists when there are peptic ulcers, GI tract disorders, or asthma?

A

Causes increased HCl secretion, and bronchoconstriction

78
Q

What are the three major drugs that have antimuscarinic properties?

A

Quinidine
Procainamide
TCA

79
Q

What are the two direct acting nicotinic drugs?

A

Nicotine

Succinylcholine

80
Q

Nicotine acts on what receptors? What does this cause?

A

Nm–skeletal muscle contractions

Nn–lots o stuff

81
Q

What is the effect of nicotine when it activates Nn receptors on the: heart?

A

Increases HR

82
Q

What is the effect of nicotine when it activates Nn receptors on the: vasculature?

A

Peripheral vasoconstriction

83
Q

What is the effect of nicotine when it activates Nn receptors on the: GI tract?

A

Increased gut motility

84
Q

What is the effect of nicotine when it activates Nn receptors on the: Carotid bodies?

A

Increased respiratory rate

85
Q

What is the effect of nicotine when it activates Nn receptors on the: medullary emetic chemoreceptors?

A

N/v

86
Q

What is the effect of nicotine on the hypothalamus?

A

Increases cortisol, causing pleasant feeling

87
Q

What is the MOA of indirect acting cholinomimetics?

A

Inhibit AchE

88
Q

Is edrophonium short or long lasting?

A

Short

89
Q

What are the clinical use of edrophonium?

A

Dx myasthenia gravis by blocking AchE

90
Q

What is the MOA of myasthenia gravis?

A

Autoimmune attack against the nicotinic receptor

91
Q

What are the two drugs used to treat myasthenia gravis?

A

Neostigmine

Pyridostigmine

92
Q

What is the antidote for atropine overdose?

A

Physostigmine

93
Q

Neostigmine is contraindicated with what condition?

A

Bladder obstruction

94
Q

How do anti-AchE drugs work to treat glaucoma?

A

open canal of schlemm

95
Q

What are the two cholinesterase inhibitors used in treating alzheimer’s? MOA?

A

Tacrine

Dopenezil

96
Q

What is the neurotransmitter that is decreased in alzheimer’s?

A

Dopamine

97
Q

What are the symptoms of cholinesterase inhibitor intoxication?

A

DUMBBELSS

98
Q

What are the components of the DUMBBELSS mnemonic for cholinesterase intoxication?

A
Diarrhea
Uncontrolled urination
Miosis of eye
Bronchiolar constriction
Bradycardia
Excitation of nervous system
Lacrimation
Sweating
Salivation
99
Q

What is the drug used to treat cholinesterase intoxication? MOA?

A

Atropine

Muscarinic receptor antagonist

100
Q

What is the MOA of pralidoxim (2-PAM)?

A

Dephosphorylates the AChE