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Cholinoceptor blocking drugs Flashcards

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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
What is the effect of hexamethonium/mecamylamine on veins?
Dilation, decreased CO
26
What is the effect of hexamethonium/mecamylamine on the heart?
tachycardia
27
What is the effect of hexamethonium/mecamylamine on iris?
Mydriasis
28
What is the effect of hexamethonium/mecamylamine on ciliary muscle?
cycloplegia
29
What is the effect of hexamethonium/mecamylamine on the GI tract?
Decreased tone, and motility
30
What is the effect of hexamethonium/mecamylamine on the bladder?
urinary retention
31
What is the effect of hexamethonium/mecamylamine on salivary glands?
Xerostomia
32
What is the effect of hexamethonium/mecamylamine on sweat glands?
Anhidrosis
33
How do depolarizing neuromuscular blocking agents like succinylcholine cause paralysis?
Overload the receptors by keeping channel open
34
How do non-depolarizing neuromuscular blocking agents like D-tubocurarine cause paralysis?
Block Nm receptors
35
All of the neuromuscular blocking drugs resemble what chemical?
Ach
36
Do neuromuscular blocking drugs cross the cell membrane?
No--ionized
37
What are the neuromuscular blocking drugs used for?
Facilitate tracheal intubation
38
Why don't the neuromuscular blocking drugs act on the CNS?
Have a quaternary N+
39
What is the MOA of d-tubocurarine (small doses and large)?
Prevents opening of nicotinic channel | small doses compete with Ach, large doses enter channel pore
40
What is phase 1 of the MOA of succinylcholine?
Binds to Nm, keeps channel open
41
What is phase 2 of the MOA of succinylcholine?
end plate is repolarized, but desensitized
42
What is the clinical use of succinylcholine?
Decreases neuromuscular transmission during anesthesia
43
What is the last muscle to be affected by succinylcholine?
diaphragm
44
What are the side effects of neuromuscular blockers?
Hypotension | Hyperkalemia
45
Hyper or hypokalemia with succinylcholine?
Hyperkalemia
46
What causes the hyperkalemia seen with succinylcholine?
Massive muscle contraction
47
What is the order of response to succinylcholine (which types are affected first/last)?
Larger muscles paralyzed first
48
How does tubocurarine produce hypotension?
Massive histamine release
49
What is the effect on the eye with succinylcholine?
Increased intraocular pressure
50
Why is muscle pain a side effect of succinylcholine use?
Large muscular contractions
51
What is the pathway of catecholamine synthesis? (5)
``` Y Dopa Dopamine Norepi Epi ```
52
In most sympathetic postganglionic pathways, what is the final product/neurotransmitter?
norepinephrine
53
What happens to norepinephrine in the adrenal medulla?
Converted to epinephrine
54
What is the rate limiting step in catecholamine synthesis?
Y to dopa by tyrosine hydroxylase
55
What is the drug that can interfere with catecholamine synthesis?
Metyrosine
56
People who eat fermented cheese cannot take with type of medications? Why?
Ones that interfere with catecholamine breakdown Tyramine in cheese will increase NE synthesis
57
What is the drug that inhibits the packaging of dopaminergic neurotransmitters?
Reserpine
58
Blocking catecholamine synthesis will result in hyper or hypotension?
Hypotension
59
What is the protein that takes up NE back into the neuron?
Norepinephrine transporter NET
60
The VAMP protein that releases catecholamines from the nerve terminal is inhibited by what?
Bretylium
61
What are the two routes of NE breakdown?
Reuptake via NET1 | Degradation by catechol-O-methyl transferase
62
What is the MOA of cocaine/Tricyclic antidepressants?
Inhibits NET1 transporter for dopamine/NE
63
Why does cocaine cause MI?
Increased NE d/t blockage of NET1
64
What is the MOA of MAOIs?
Cannot metabolize dopa via mitochondrial monoamine oxidase
65
What is the main source of peripheral vascular resistance in our bodies?
Arterioles
66
What is the MOA of alpha 1 receptors?
Gq--phospholipase C, PKC
67
What is the MOA of beta 1, beta 2 receptors?
Gs--adenylate cyclase, increases cAMP
68
What is the MOA of alpha 2 receptors?
Gi-inhibits adenylate cyclase, decreases cAMP
69
What are the two receptors that decrease cAMP?
ALpha 2 | M2
70
What is the autoreceptor on the cholinergic system?
M2
71
What is the autoreceptor on the adrenergic system?
alpha2
72
What are the receptors that utilize the Gq protein?
H1 alpha1, V1, M1, M3
73
What are the receptors that utilize the Gs protein?
Beta 1, Beta2, D1, H2, V2
74
What are the receptors that utilize the Gi protein?
M2, alpha2, D2
75
alpha 1 activation in the eye causes what?
contraction
76
alpha 1 activation in the arterioles causes what?
contraction
77
alpha 1 activation in the veins causes what?
Contraction
78
alpha 1 activation in the bladder causes what?
contraction
79
alpha 1 activation in the male sex organ causes what?
ejaculation (contraction)
80
alpha 1 activation in the liver causes what?
glycogenolysis
81
alpha 1 activation in the kidney causes what?
Decreased renin release
82
alpha 2 activation in the prejunctional nerve terminals causes what?
decrease transmitter release and NE synthesis
83
alpha 2 activation in the platelets causes what?
aggregation
84
alpha 2 activation in the pancreas causes what?
Decreased insulin
85
beta 1 activation on the SA node causes wha?
Increased HR
86
beta 1 activation on the AV node causes wha?
increased conduction veloicty
87
beta 1 activation on the atrial and ventricular muscles causes wha?
increased force of contraction
88
beta 1 activation on the kidney causes wha?
Increased renin release
89
beta 1 activation on the purkinje fibers causes wha?
Increased automaticity
90
beta 2 activation on the blood vessels causes what?
vasodilation
91
beta 2 activation on the uterus causes what?
relaxation
92
beta 2 activation on the brochioles causes what?
dilation
93
beta 2 activation on the skeletal muscles causes what?
increased glycogenolysis, contractility
94
beta 2 activation on the liver causes what?
Increased glycogenolysis
95
beta 2 activation on the pancreas causes what?
Increased insulin synthesis
96
D1 activation in the kidney causes what?
Vasodilation--increased GFR
97
Which has a higher affinitiy for catecholamines: alpha or beta receptors. Why is this significant?
beta Is the cause for the dose dependent effects seen with catecholamines
98
What is the only place in the body that NE is converted to epineprhine?
Adrenal medulla
99
What does MOA-A degrade?
5HT, NE, and tyramine
100
What does MOA-B degrade?
dopamine
101
Phospholipase C activates what enzyme through Ca release?
PKC
102
What are the G coupled receptors for the Nn and Nm?
None--use Na/K channels
103
What is the adrenergic receptor you would want to activate if you wanted to increase GFR/urianry output?
D1
104
What are the receptors that you want to block in the eye to reduce aqueous humor production?
Beta 1, beta 2
105
What is the effect of activating alpha 1 receptor in the eye?
Mydirasis (dilation) d/t radial muscle activation
106
What is cycloplegia?
Impairment of the ciliar muscle of the eye, not allowing for accomodation
107
Why don't you see cycloplegia with use of alpha 1 agonists?
Ciliary muscle does not have an alpha 1 receptor
108
Why does atropine cause cycloplegia?
Inhibits M on the sphincter muscle
109
What is the equation for blood pressure?
TPR*CO : CO=HR*SV
110
Increasing blood pressure increases baroreceptor discharge to work on what part of the brain? What does this in turn do?
Vasomotor center--Decreases sympathetic tone/decreases vasoconstriction
111
What is the effect of the vasomotor center on the PANS to decrease blood pressure?
increase vagal tone
112
What are the three effects of the vasomotor center on the SANS in response to increased BP?
decreased vasoconstriction Decreased cardiac contraction Decreased HR
113
What is the receptor on blood vessels that increaes total peripheral resistance when activated? What happens to the heart rate when this happens?
alpha 1 reflex bradycardia

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