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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
Q

M3 Receptor

A

Eye
GIT
Bladder
Bronchus
Glands
CNS

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26
Q

M4 Receptor

A

CNS

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27
Q

M5 Receptor

A

CNS

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28
Q

Nicotinic Ach Receptor Properties

A
  • 5 subunits , 2 bind Ach
  • Opens ion channels, K+ out Na+ in
  • Acetylcholinesterase stops signal
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29
Q

Acetylcholinesterase (AChE)

A

Primary enzyme responsible for synaptic acetylcholine breakdown

30
Q

Butyrylcholinesterase (BChE)

A

Enzyme that can break down acetylcholine mainly found in bloodstream

31
Q

Breakdown of ACh by AChE

A

Rapidly broken down via ester hydrolysis into acetate and choline

32
Q

Choline Acetyltransferase (ChAT)

A

Enzyme responsible for acetylcholine synthesis

33
Q

Vesicular ACh Transporter (VAT or VAChT)

A

Responsible for ACh uptake in storage vesicles

34
Q

Presynaptic M2 Receptors

A

Function as autoreceptors
Can be located postsynaptically

35
Q

Cholinergic signaling in the eye

A

M3 Receptor
Contraction of iris circular muscle causing miosis; increase outflow of aqueous humor

36
Q

Cholinergic signaling in the heart

A

M2 Receptor
Reduction in heart rate and contractility

37
Q

Cholinergic signaling in the blood vessels

A

M3 Receptor
Can cause vasodilation

38
Q

Cholinergic signaling in the lungs

A

M3 Receptor
Contraction of bronchiolar smooth muscle leading to bronchoconstriction

39
Q

Cholinergic signaling in the GI tract

A

M3 Receptor
Increases digestion and digestive secretions

40
Q

Cholinergic signaling in the bladder

A

M3 Receptor
Detrusor muscle contraction
Urinary sphincter relaxation
Facilitation of urination

41
Q

Spastic paralysis

A

Caused by drugs that enhance cholinergic signaling at NMJ

42
Q

Flaccid paralysis

A

Caused by drugs that block cholinergic signaling at NMJ

43
Q

Cholinergic signaling affect on learning and memory

A

Activation of receptors in hippocampus enhances learning and memory

44
Q

Cholinergic signaling affect on reward pathways

A

Activation of nicotinic receptors in VTA activates dopaminergic neurons and stimulates dopamine release

45
Q

Cholinergic signaling affect on regulating sleep-wake cycles

A

Cholinergic signaling increases REM sleep but also wakefulness; important in establishing circadian rhythms

46
Q

Cholinergic signaling affect on motor control and normal movement

A

Cholinergic - dopaminergic balance in striatum is important for normal movement

47
Q

Cholinergic signaling affect on appetite suppression

A

Activation of nicotinic receptors in brain can reduce appetite

48
Q

Acetylcholinesterase inhibitors

A

Increase cholinergic signaling in brain
Used to treat Alzheimer’s

49
Q

Muscarinic receptor antagonists

A

Decrease bronchoconstriction - used to treat asthma and COPD
Decrease urination - used to treat overactive bladder

50
Q

Nicotine receptor agonist at Nn

A

Enhance alertness, reduces appetite, causes addiction - recreational drug

51
Q

Nicotinic receptor blockers at NMJ Nm

A

Cause muscle paralysis - used during surgery to facilitate endotracheal intubation, treats painful muscle spasms

52
Q

Direct Acting Cholinomimetics

A

Act as agonists at muscarinic and/or nicotinic receptors

53
Q

Indirect Acting Cholinomimetics

A

Increase cholinergic signaling without directly activating receptors
Inhibitors of acetylecholinesterase

54
Q

Antimuscarinic drugs

A

Act as antagonists at muscarinic receptors

55
Q

Antinicotinic drugs

A

Act as antagonists at nicotinic receptors

56
Q

Cholinesterase regenerator drugs

A

Used in organophosphate poisoning which remove covalently bound phosphate group from acetylcholinesterase enzyme

57
Q

Choline Esters

A

Highly hydrophilic due to quaternary amine
Poor oral absorption, low ability to cross BBB

58
Q

Beta-methyl group

A

Provides steric hinderance against cholinesterase hydrolysis but reduces potency at nicotinic receptors

59
Q

Choline Esters with Beta-methyl Group

A

Selective for muscarinic receptors and less susceptible to cholinesterase hydrolysis
Longer half life

60
Q

Alkaloids

A

Naturally occurring compounds containing at least one nitrogen and having alkaline properties
Not susceptible to hydrolysis because of the ester

61
Q

Drugs that contain a tertiary amine…

A
  • Cross biological membranes easily
  • Urinary excretion is increased if urine becomes acidic
62
Q

Indirectly Acting Reversible Cholinergic Drugs

A
  • Carbamates
  • Acridine
63
Q

Indirectly Acting Irreversible Cholinergic Drugs

A
  • Organophosphates
  • Carbamates
64
Q

Atropine

A

Prototypical muscarinic antagonist
Nonselective
Can treat acetylcholinesterase inhibitor poisoning

65
Q

Ganglion Blocking Drugs

A

Treatment of hypertension
Block Nn receptors
Reduce sympathetic outflow

66
Q

Neuromuscular-blocking drugs

A

Producing skeletal muscle relaxation
Block Nm receptors

67
Q

Direct Acting Cholinergic Agonist Indications

A

Urinary retention after surgery or postpartum
Glaucoma

68
Q

Direct Acting Cholinergic Agonist Adverse Effects Muscarinic

A

Salvation, flushing, bronchospasm, sweating, nausea, abdominal pain

69
Q

Direct Acting Cholinergic Agonist Adverse Effects Nicotinic

A

Fasciculations, respiratory arrest

70
Q

Direct Acting Nicotinic Agonist Adverse Effects

A

Vomiting, convulsions, hypertension, cardiac arrhythmias

71
Q

Muscarinic Receptor Antagonist Adverse Effects

A

PNS- dry mouth, blurred vision, tachycardia, urinary retention, constipated
SAS- Inhibition of sweating
CNS- restlessness, confusion, hallucinations

Pharmacology (15 decks)

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