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
M3 activation on the bladder results in what?
Relaxation
26
M3 activation on the bronchioles results in what?
Contraction/bronchospasm
27
M2 activation on the SA node results in what?
decreased HR
28
M2 activation on the AV node results in what?
Decreased conduction velocity
29
M3 activation in the stomach results in what?
motility/cramps
30
M3 activation in the intestines results in what?
Contraction= diarrhea
31
M3 activation on blood vessels results in what?
Vasodilation
32
Why must drugs that act on nicotinic receptors be used carefully?
Because every presynaptic nerve uses nicotinic receptors
33
What are the two types of direct acting cholinoceptor agonists?
Muscarinic | Nicotinic
34
What are the two types of indirect acting cholinoceptor stimulants?
Reversible | Irreversible
35
Muscarinic or nicotinic direct acting cholinoceptor stimulant: ACh?
Muscarinic
36
Muscarinic or nicotinic direct acting cholinoceptor stimulant: muscarinic?
Muscarinic
37
Muscarinic or nicotinic direct acting cholinoceptor stimulant: methacholine?
Muscarinic
38
Muscarinic or nicotinic direct acting cholinoceptor stimulant: nicotine?
Nicotinic
39
Muscarinic or nicotinic direct acting cholinoceptor stimulant: succinylcholine?
Nicotinic
40
Muscarinic or nicotinic direct acting cholinoceptor stimulant: bethanechol?
Muscarinic
41
Muscarinic or nicotinic direct acting cholinoceptor stimulant: carbachol?
Muscarinic
42
Reversible or irreversible indirect acting cholinoceptor: edrophonium
Reversible
43
Reversible or irreversible indirect acting cholinoceptor: neostigamine
reversible
44
Reversible or irreversible indirect acting cholinoceptor:physostigmine
Reversible
45
Reversible or irreversible indirect acting cholinoceptor: echothiophate
Irreversible
46
Reversible or irreversible indirect acting cholinoceptor: malathion
Irreversible
47
Reversible or irreversible indirect acting cholinoceptor: parathion
Irreversible
48
Reversible or irreversible indirect acting cholinoceptor: denepezil
Reversible
49
Reversible or irreversible indirect acting cholinoceptor: sarin
Irreversible
50
All of the choline esters are what type of molecule?
Cationic quaternary ammonium (insoluble in lipids)
51
Why are direct acting cholinoceptor agonists poorly absorbed in the GI tract and CNS?
insoluble in lipids
52
Addition of what functional group to methacholine and bethanechol increases their half life?
methyl
53
carbachol and bethanechol are not susceptible to which enzyme?
Cholinesterase
54
What are the two choline esters that are not susceptible to acetylcholine esterase?
Carbachol | Bethanechol
55
Methacholine has more muscarinic, or nicotinic action?
Muscarinic
56
Bethanechol has more muscarinic or nicotinic action?
muscarinic
57
What are the effects of choline esters on the cardiovascular system?
Hypotension | Bradycardia
58
What are the effects of choline esters on the GI system? (3)
- Increased tone and contractility of gut - Increased acid secretion - n/v/d
59
What are the effects of choline esters on the GU system?
Involuntary urination
60
What are the effects of choline esters on the eyes?
Miosis | Contraction of ciliary muscle for near vision
61
What are the effects of choline esters on the respiratory system?
bronchoconstriction
62
What are the effects of choline esters on glands?
Increased secretions
63
What are homeostatic reflexes?
reflexes that respond to a stimulus to maintain homeostasis
64
Why does ACh have limited clinical use?
Fast degradation
65
What are the nicotinic effects of ACh?
not commonly seen since does not penetrate fat
66
How does ACh cause vasodilation?
Acts on M3 receptors to produce NO
67
What is the clinical use of methacholine?
Diagnosis of bronchiolar hypersensitivity via M3 receptors
68
What is the use of carbachol? MOA?
Activates both nicotinic and muscarinic cholinoceptors, Open canal of schlemm to decrease intraocular pressure
69
What is the effect of high doses of carbachol?
cardiac arrest
70
What are the clinical uses of Bethanechol? What receptor does it act on?
Acts on M3 to increase detrusor tone, and increase gastric motility (gastric atony Gastric emptying, urinary retention)
71
Muscarine is found in what?
Mushrooms
72
What is the MOA of muscarine?
Directly activates all Muscarininc, ACh receptors with x100 potency
73
What are the symptoms of muscarine ingestion?
Increase secretions Abdominal pain, n/v/d Cardiac arrest
74
What is the MOA of pilocarpine?
Direct agonist of M3
75
What is pilocarpine used for in the eye? MOA?
Contraction of the iris sphincter muscle and ciliary muscles Relieves glaucoma
76
What is pilocarpine used for when not used in the eye?
Tests autonomic state
77
Why should you not use choline agonists when there are peptic ulcers, GI tract disorders, or asthma?
Causes increased HCl secretion, and bronchoconstriction
78
What are the three major drugs that have antimuscarinic properties?
Quinidine Procainamide TCA
79
What are the two direct acting nicotinic drugs?
Nicotine | Succinylcholine
80
Nicotine acts on what receptors? What does this cause?
Nm--skeletal muscle contractions Nn--lots o stuff
81
What is the effect of nicotine when it activates Nn receptors on the: heart?
Increases HR
82
What is the effect of nicotine when it activates Nn receptors on the: vasculature?
Peripheral vasoconstriction
83
What is the effect of nicotine when it activates Nn receptors on the: GI tract?
Increased gut motility
84
What is the effect of nicotine when it activates Nn receptors on the: Carotid bodies?
Increased respiratory rate
85
What is the effect of nicotine when it activates Nn receptors on the: medullary emetic chemoreceptors?
N/v
86
What is the effect of nicotine on the hypothalamus?
Increases cortisol, causing pleasant feeling
87
What is the MOA of indirect acting cholinomimetics?
Inhibit AchE
88
Is edrophonium short or long lasting?
Short
89
What are the clinical use of edrophonium?
Dx myasthenia gravis by blocking AchE
90
What is the MOA of myasthenia gravis?
Autoimmune attack against the nicotinic receptor
91
What are the two drugs used to treat myasthenia gravis?
Neostigmine | Pyridostigmine
92
What is the antidote for atropine overdose?
Physostigmine
93
Neostigmine is contraindicated with what condition?
Bladder obstruction
94
How do anti-AchE drugs work to treat glaucoma?
open canal of schlemm
95
What are the two cholinesterase inhibitors used in treating alzheimer's? MOA?
Tacrine | Dopenezil
96
What is the neurotransmitter that is decreased in alzheimer's?
Dopamine
97
What are the symptoms of cholinesterase inhibitor intoxication?
DUMBBELSS
98
What are the components of the DUMBBELSS mnemonic for cholinesterase intoxication?
``` Diarrhea Uncontrolled urination Miosis of eye Bronchiolar constriction Bradycardia Excitation of nervous system Lacrimation Sweating Salivation ```
99
What is the drug used to treat cholinesterase intoxication? MOA?
Atropine | Muscarinic receptor antagonist
100
What is the MOA of pralidoxim (2-PAM)?
Dephosphorylates the AChE