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Pharmacology > Cholinergic Drugs (Exam 1) > Flashcards

Cholinergic Drugs (Exam 1) Flashcards

1
Q

What is a neuron made up of?

A
  1. Cell body or soma
  2. Dendrites
  3. Axon
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2
Q

Dendrites

A

Receive signals from other neurons

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3
Q

Axon

A

Sends out signal to surrounding neurons through axon terminal

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4
Q

Action Potential

A

Electrical signal that travels down axon
Created using Na+, Inhibited by K+

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5
Q

Depolarization

A

Voltage gated Na+ channels open
Na+ influx

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6
Q

Repolarization

A

Voltage gated Na+ channels close and K+ channels open
K+ efflux

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7
Q

Hyperpolarization

A

Voltage gated K+ channels close

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8
Q

Increased signaling occurs from drugs that…?

A
  • Increase concentration of neurotransmitter at synapse
  • Activate postsynaptic receptors
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9
Q

Decreased signaling occurs from drugs that…?

A
  • Decrease concentration of neurotransmitter at synapse
  • Decrease activation of postsynaptic receptors
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10
Q

Relationship between cholinergic signaling and heart rate

A

Inverse relationship
Increase cholinergic signaling, decrease heart rate

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11
Q

Relationship between adrenergic signaling and heart rate

A

Direct relationship
Increase adrenergic signaling, increase heart rate

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12
Q

Cholinergic

A

Acetylcholine (Ach) neurotransmitter

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13
Q

Cholinergic Receptors

A

Nicotinic (N1, N2)
Muscarinic (M1-M5)

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14
Q

Cholinomimetics

A

Enhance cholinergic signaling

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15
Q

Anticholinergics

A

Reduce cholinergic signaling

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16
Q

Synthesis of Ach

A

Synthesized from Acetyl-S-CoA and Choline by choline acetyltransferase (ChAT)

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17
Q

Sympathetic Nervous System

A

Fight or flight

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18
Q

Parasympathetic Nervous System

A

Rest and digest

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19
Q

Nicotinic Receptors (N)

A

Nn and Nm

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20
Q

Nn Receptor

A

Ganglia
Adrenal medulla

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21
Q

Nm Receptor

A

Neuromuscular

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22
Q

Muscarinic Receptor (M)

A

M1, M2, M3, M4, M5

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23
Q

M1 Receptor

A

Gastric
Ganglia
CNS

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24
Q

M2 Receptor

A

Heart
CNS

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25
M3 Receptor
Eye GIT Bladder Bronchus Glands CNS
26
M4 Receptor
CNS
27
M5 Receptor
CNS
28
Nicotinic Ach Receptor Properties
- 5 subunits , 2 bind Ach - Opens ion channels, K+ out Na+ in - Acetylcholinesterase stops signal
29
Acetylcholinesterase (AChE)
Primary enzyme responsible for synaptic acetylcholine breakdown
30
Butyrylcholinesterase (BChE)
Enzyme that can break down acetylcholine mainly found in bloodstream
31
Breakdown of ACh by AChE
Rapidly broken down via ester hydrolysis into acetate and choline
32
Choline Acetyltransferase (ChAT)
Enzyme responsible for acetylcholine synthesis
33
Vesicular ACh Transporter (VAT or VAChT)
Responsible for ACh uptake in storage vesicles
34
Presynaptic M2 Receptors
Function as autoreceptors Can be located postsynaptically
35
Cholinergic signaling in the eye
M3 Receptor Contraction of iris circular muscle causing miosis; increase outflow of aqueous humor
36
Cholinergic signaling in the heart
M2 Receptor Reduction in heart rate and contractility
37
Cholinergic signaling in the blood vessels
M3 Receptor Can cause vasodilation
38
Cholinergic signaling in the lungs
M3 Receptor Contraction of bronchiolar smooth muscle leading to bronchoconstriction
39
Cholinergic signaling in the GI tract
M3 Receptor Increases digestion and digestive secretions
40
Cholinergic signaling in the bladder
M3 Receptor Detrusor muscle contraction Urinary sphincter relaxation Facilitation of urination
41
Spastic paralysis
Caused by drugs that enhance cholinergic signaling at NMJ
42
Flaccid paralysis
Caused by drugs that block cholinergic signaling at NMJ
43
Cholinergic signaling affect on learning and memory
Activation of receptors in hippocampus enhances learning and memory
44
Cholinergic signaling affect on reward pathways
Activation of nicotinic receptors in VTA activates dopaminergic neurons and stimulates dopamine release
45
Cholinergic signaling affect on regulating sleep-wake cycles
Cholinergic signaling increases REM sleep but also wakefulness; important in establishing circadian rhythms
46
Cholinergic signaling affect on motor control and normal movement
Cholinergic - dopaminergic balance in striatum is important for normal movement
47
Cholinergic signaling affect on appetite suppression
Activation of nicotinic receptors in brain can reduce appetite
48
Acetylcholinesterase inhibitors
Increase cholinergic signaling in brain Used to treat Alzheimer's
49
Muscarinic receptor antagonists
Decrease bronchoconstriction - used to treat asthma and COPD Decrease urination - used to treat overactive bladder
50
Nicotine receptor agonist at Nn
Enhance alertness, reduces appetite, causes addiction - recreational drug
51
Nicotinic receptor blockers at NMJ Nm
Cause muscle paralysis - used during surgery to facilitate endotracheal intubation, treats painful muscle spasms
52
Direct Acting Cholinomimetics
Act as agonists at muscarinic and/or nicotinic receptors
53
Indirect Acting Cholinomimetics
Increase cholinergic signaling without directly activating receptors Inhibitors of acetylecholinesterase
54
Antimuscarinic drugs
Act as antagonists at muscarinic receptors
55
Antinicotinic drugs
Act as antagonists at nicotinic receptors
56
Cholinesterase regenerator drugs
Used in organophosphate poisoning which remove covalently bound phosphate group from acetylcholinesterase enzyme
57
Choline Esters
Highly hydrophilic due to quaternary amine Poor oral absorption, low ability to cross BBB
58
Beta-methyl group
Provides steric hinderance against cholinesterase hydrolysis but reduces potency at nicotinic receptors
59
Choline Esters with Beta-methyl Group
Selective for muscarinic receptors and less susceptible to cholinesterase hydrolysis Longer half life
60
Alkaloids
Naturally occurring compounds containing at least one nitrogen and having alkaline properties Not susceptible to hydrolysis because of the ester
61
Drugs that contain a tertiary amine...
- Cross biological membranes easily - Urinary excretion is increased if urine becomes acidic
62
Indirectly Acting Reversible Cholinergic Drugs
- Carbamates - Acridine
63
Indirectly Acting Irreversible Cholinergic Drugs
- Organophosphates - Carbamates
64
Atropine
Prototypical muscarinic antagonist Nonselective Can treat acetylcholinesterase inhibitor poisoning
65
Ganglion Blocking Drugs
Treatment of hypertension Block Nn receptors Reduce sympathetic outflow
66
Neuromuscular-blocking drugs
Producing skeletal muscle relaxation Block Nm receptors
67
Direct Acting Cholinergic Agonist Indications
Urinary retention after surgery or postpartum Glaucoma
68
Direct Acting Cholinergic Agonist Adverse Effects Muscarinic
Salvation, flushing, bronchospasm, sweating, nausea, abdominal pain
69
Direct Acting Cholinergic Agonist Adverse Effects Nicotinic
Fasciculations, respiratory arrest
70
Direct Acting Nicotinic Agonist Adverse Effects
Vomiting, convulsions, hypertension, cardiac arrhythmias
71
Muscarinic Receptor Antagonist Adverse Effects
PNS- dry mouth, blurred vision, tachycardia, urinary retention, constipated SAS- Inhibition of sweating CNS- restlessness, confusion, hallucinations

Pharmacology (18 decks)

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