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Pharm > Cholinoceptor blocking drugs > Flashcards

Cholinoceptor blocking drugs Flashcards

1
Q

What type of drug is atropine? (What receptor does it work on?)

A

Muscarinic antagonist

M

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2
Q

What type of drug is ipratropium? (What receptor does it work on?)

A

Muscarinic antagonist

M

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3
Q

What type of drug is benztropine? (What receptor does it work on?)

A

Muscarinic antagonist

M

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4
Q

What type of drug is hexamethonium? (What receptor does it work on?)

A

Nicotinic antagonist

Nn, Nm

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5
Q

What type of drug is mecamylamine? (What receptor does it work on?)

A

Nicotinic antagonist

Nn, Nm

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6
Q

What type of drug is d-tubocuraine? (What receptor does it work on?)

A

Non-depolarizing neuromuscular blocker

Nm

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7
Q

What type of drug is succinylcholine? (What receptor does it work on?)

A

Depolarizing neuromuscular blocker

Nm

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8
Q

True or false: atropine blocks only M1 type of muscarinic receptors

A

False–all muscarinic

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9
Q

What are the pharmacological effects of atropine on secretions?

A

decreased secretions

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10
Q

What are the pharmacological effects of atropine on the heart?

A

Tachycardia

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11
Q

What are the pharmacological effects of atropine on bod heat?

A

Hyperthermia

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12
Q

What are the pharmacological effects of atropine on the urinary tract?

A

Retention and constipation

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13
Q

What are the pharmacological effects of atropine on the CNS?

A

Behavioral excitation and hallucinations

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14
Q

True or false: atropine does not affect blood pressure when given alone

A

True

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15
Q

Atropine is used in the treatment of what?

A

Peripheral vasodilation caused by choline esters or AChE inhibitors

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16
Q

Acute intoxication of physostigmine is treated with what?

A

Atropine

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17
Q

Why is atropine given for pericardiocentesis?

A

Prevents vagal reaction in some procedures

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18
Q

What are the effects of ipratropium (atrovent) on the lungs? What receptors are used here?

A

Decreases bronchoconstriction
Decreases bronchial secretions
M3

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19
Q

What are the clinical uses for ipratropium (atrovent)?

A

COPD flares

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20
Q

What is the primary site of action for benztropine (cogentin)?

A

Muscarinic receptors in the brain

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21
Q

What is the effect of benztropine (cogentin)?

A

Reestablishes dopaminergic cholinergic balance

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22
Q

What is the clinical use of benztropine?

A

Parkinson’s disease

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23
Q

What are the two ganglionic blocking agents discussed in class?

A

hexamethonium

Mecamylamine

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24
Q

What is the effect of hexamethonium/mecamylamine on arterioles?

A

vasodilation/hypotension

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25
Q

What is the effect of hexamethonium/mecamylamine on veins?

A

Dilation, decreased CO

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26
Q

What is the effect of hexamethonium/mecamylamine on the heart?

A

tachycardia

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27
Q

What is the effect of hexamethonium/mecamylamine on iris?

A

Mydriasis

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28
Q

What is the effect of hexamethonium/mecamylamine on ciliary muscle?

A

cycloplegia

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29
Q

What is the effect of hexamethonium/mecamylamine on the GI tract?

A

Decreased tone, and motility

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30
Q

What is the effect of hexamethonium/mecamylamine on the bladder?

A

urinary retention

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31
Q

What is the effect of hexamethonium/mecamylamine on salivary glands?

A

Xerostomia

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32
Q

What is the effect of hexamethonium/mecamylamine on sweat glands?

A

Anhidrosis

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33
Q

How do depolarizing neuromuscular blocking agents like succinylcholine cause paralysis?

A

Overload the receptors by keeping channel open

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34
Q

How do non-depolarizing neuromuscular blocking agents like D-tubocurarine cause paralysis?

A

Block Nm receptors

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35
Q

All of the neuromuscular blocking drugs resemble what chemical?

A

Ach

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36
Q

Do neuromuscular blocking drugs cross the cell membrane?

A

No–ionized

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37
Q

What are the neuromuscular blocking drugs used for?

A

Facilitate tracheal intubation

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38
Q

Why don’t the neuromuscular blocking drugs act on the CNS?

A

Have a quaternary N+

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39
Q

What is the MOA of d-tubocurarine (small doses and large)?

A

Prevents opening of nicotinic channel

small doses compete with Ach, large doses enter channel pore

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40
Q

What is phase 1 of the MOA of succinylcholine?

A

Binds to Nm, keeps channel open

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41
Q

What is phase 2 of the MOA of succinylcholine?

A

end plate is repolarized, but desensitized

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42
Q

What is the clinical use of succinylcholine?

A

Decreases neuromuscular transmission during anesthesia

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43
Q

What is the last muscle to be affected by succinylcholine?

A

diaphragm

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44
Q

What are the side effects of neuromuscular blockers?

A

Hypotension

Hyperkalemia

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45
Q

Hyper or hypokalemia with succinylcholine?

A

Hyperkalemia

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46
Q

What causes the hyperkalemia seen with succinylcholine?

A

Massive muscle contraction

47
Q

What is the order of response to succinylcholine (which types are affected first/last)?

A

Larger muscles paralyzed first

48
Q

How does tubocurarine produce hypotension?

A

Massive histamine release

49
Q

What is the effect on the eye with succinylcholine?

A

Increased intraocular pressure

50
Q

Why is muscle pain a side effect of succinylcholine use?

A

Large muscular contractions

51
Q

What is the pathway of catecholamine synthesis? (5)

A 
Y
Dopa
Dopamine
Norepi
Epi
52
Q

In most sympathetic postganglionic pathways, what is the final product/neurotransmitter?

A

norepinephrine

53
Q

What happens to norepinephrine in the adrenal medulla?

A

Converted to epinephrine

54
Q

What is the rate limiting step in catecholamine synthesis?

A

Y to dopa by tyrosine hydroxylase

55
Q

What is the drug that can interfere with catecholamine synthesis?

A

Metyrosine

56
Q

People who eat fermented cheese cannot take with type of medications? Why?

A

Ones that interfere with catecholamine breakdown

Tyramine in cheese will increase NE synthesis

57
Q

What is the drug that inhibits the packaging of dopaminergic neurotransmitters?

A

Reserpine

58
Q

Blocking catecholamine synthesis will result in hyper or hypotension?

A

Hypotension

59
Q

What is the protein that takes up NE back into the neuron?

A

Norepinephrine transporter NET

60
Q

The VAMP protein that releases catecholamines from the nerve terminal is inhibited by what?

A

Bretylium

61
Q

What are the two routes of NE breakdown?

A

Reuptake via NET1

Degradation by catechol-O-methyl transferase

62
Q

What is the MOA of cocaine/Tricyclic antidepressants?

A

Inhibits NET1 transporter for dopamine/NE

63
Q

Why does cocaine cause MI?

A

Increased NE d/t blockage of NET1

64
Q

What is the MOA of MAOIs?

A

Cannot metabolize dopa via mitochondrial monoamine oxidase

65
Q

What is the main source of peripheral vascular resistance in our bodies?

A

Arterioles

66
Q

What is the MOA of alpha 1 receptors?

A

Gq–phospholipase C, PKC

67
Q

What is the MOA of beta 1, beta 2 receptors?

A

Gs–adenylate cyclase, increases cAMP

68
Q

What is the MOA of alpha 2 receptors?

A

Gi-inhibits adenylate cyclase, decreases cAMP

69
Q

What are the two receptors that decrease cAMP?

A

ALpha 2

M2

70
Q

What is the autoreceptor on the cholinergic system?

A

M2

71
Q

What is the autoreceptor on the adrenergic system?

A

alpha2

72
Q

What are the receptors that utilize the Gq protein?

A

H1 alpha1, V1, M1, M3

73
Q

What are the receptors that utilize the Gs protein?

A

Beta 1, Beta2, D1, H2, V2

74
Q

What are the receptors that utilize the Gi protein?

A

M2, alpha2, D2

75
Q

alpha 1 activation in the eye causes what?

A

contraction

76
Q

alpha 1 activation in the arterioles causes what?

A

contraction

77
Q

alpha 1 activation in the veins causes what?

A

Contraction

78
Q

alpha 1 activation in the bladder causes what?

A

contraction

79
Q

alpha 1 activation in the male sex organ causes what?

A

ejaculation (contraction)

80
Q

alpha 1 activation in the liver causes what?

A

glycogenolysis

81
Q

alpha 1 activation in the kidney causes what?

A

Decreased renin release

82
Q

alpha 2 activation in the prejunctional nerve terminals causes what?

A

decrease transmitter release and NE synthesis

83
Q

alpha 2 activation in the platelets causes what?

A

aggregation

84
Q

alpha 2 activation in the pancreas causes what?

A

Decreased insulin

85
Q

beta 1 activation on the SA node causes wha?

A

Increased HR

86
Q

beta 1 activation on the AV node causes wha?

A

increased conduction veloicty

87
Q

beta 1 activation on the atrial and ventricular muscles causes wha?

A

increased force of contraction

88
Q

beta 1 activation on the kidney causes wha?

A

Increased renin release

89
Q

beta 1 activation on the purkinje fibers causes wha?

A

Increased automaticity

90
Q

beta 2 activation on the blood vessels causes what?

A

vasodilation

91
Q

beta 2 activation on the uterus causes what?

A

relaxation

92
Q

beta 2 activation on the brochioles causes what?

A

dilation

93
Q

beta 2 activation on the skeletal muscles causes what?

A

increased glycogenolysis, contractility

94
Q

beta 2 activation on the liver causes what?

A

Increased glycogenolysis

95
Q

beta 2 activation on the pancreas causes what?

A

Increased insulin synthesis

96
Q

D1 activation in the kidney causes what?

A

Vasodilation–increased GFR

97
Q

Which has a higher affinitiy for catecholamines: alpha or beta receptors. Why is this significant?

A

beta

Is the cause for the dose dependent effects seen with catecholamines

98
Q

What is the only place in the body that NE is converted to epineprhine?

A

Adrenal medulla

99
Q

What does MOA-A degrade?

A

5HT, NE, and tyramine

100
Q

What does MOA-B degrade?

A

dopamine

101
Q

Phospholipase C activates what enzyme through Ca release?

A

PKC

102
Q

What are the G coupled receptors for the Nn and Nm?

A

None–use Na/K channels

103
Q

What is the adrenergic receptor you would want to activate if you wanted to increase GFR/urianry output?

A

D1

104
Q

What are the receptors that you want to block in the eye to reduce aqueous humor production?

A

Beta 1, beta 2

105
Q

What is the effect of activating alpha 1 receptor in the eye?

A

Mydirasis (dilation) d/t radial muscle activation

106
Q

What is cycloplegia?

A

Impairment of the ciliar muscle of the eye, not allowing for accomodation

107
Q

Why don’t you see cycloplegia with use of alpha 1 agonists?

A

Ciliary muscle does not have an alpha 1 receptor

108
Q

Why does atropine cause cycloplegia?

A

Inhibits M on the sphincter muscle

109
Q

What is the equation for blood pressure?

A

TPRCO : CO=HRSV

110
Q

Increasing blood pressure increases baroreceptor discharge to work on what part of the brain? What does this in turn do?

A

Vasomotor center–Decreases sympathetic tone/decreases vasoconstriction

111
Q

What is the effect of the vasomotor center on the PANS to decrease blood pressure?

A

increase vagal tone

112
Q

What are the three effects of the vasomotor center on the SANS in response to increased BP?

A

decreased vasoconstriction
Decreased cardiac contraction
Decreased HR

113
Q

What is the receptor on blood vessels that increaes total peripheral resistance when activated? What happens to the heart rate when this happens?

A

alpha 1

reflex bradycardia

Pharm (73 decks)

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