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Pharmacology > 3.3 - Parasympathetic Drugs > Flashcards

3.3 - Parasympathetic Drugs Flashcards

1
Q

Parasymphathetic Drugs

A
  • Biosynthesis
  • Receptors
  • Parasympathomimetics
  • Parasympatholytics
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2
Q

Biosynthesis of ACh

A
  • Locations
  • Steps
  • Fate of ACh in the cleft
  • Drugs that interfere in the biosynthesis, storage, release and fate of ACh
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3
Q

Locations

A

– All pre ganglionic neurons
– Cholinergic, post-ganglionic neurons
– Somatic Nerves
– CNS

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4
Q

Steps

A

Choline ➡️1️⃣ Choline + AcCoA ➡️2️⃣ ACh ➡️ Vesicular storage throug VAT ➡️ Release

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5
Q

1️⃣

A

Active uptake

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6
Q

2️⃣

A

CHAT

– Choline Acetyltransferase

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7
Q

Fate of the ACh in the cleft

A
  • Binding to post-synaptic ®

* Metabolism by AChE

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8
Q

Drugs that interfere in the biosynthesis, storage, release and fate of ACh

A

— Active uptake of Choline
— Vesicular Storage of ACh
— Release of ACh (exocytosis)
— Metabolism by AChE

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9
Q

Active uptake of ACh: INHIBITOR

A

Hemicholinium

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10
Q

Vesicular Storage of ACh: INHIBITOR

A

Vesamicol

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11
Q

Release of ACh (exocytosis): STIMULATOR

A

Alpha-latrotoxin

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12
Q

Release of ACh (exocytosis): INHIBITOR

A

Botulinum toxin

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13
Q

Metabolism by AChE: INHIBITORS

A

Organophosphates

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14
Q

Receptors

A
  • Muscarinic Receptor

* Nicotinic Receptors

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15
Q

Muscarinic Receptor

A
  • M1
  • M2
  • M3
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16
Q

M1

A

– Location: Gastric Glands

– Effect: ⬆️ HCl secretion

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17
Q

M2

A

– Location: ❤️

– Effects: Bradycardia

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18
Q

M3

A

– Location: Exocrine Glands

– Effect: ⬆️ secretion

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19
Q

M3

A 
– Location: Smooth muscles
 — Gq linked — Contraction
– Effect:
 - 👀
 - Brochi
 - GIT
 - Urinary Bladder
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20
Q

👀

A

– Ciliary Muscle: ⬆️ Accomodation

– Circular Muscle: MIOSIS

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21
Q

Bronchi

A

BronchoCONSTRICTION

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22
Q

GIT

— Diarrhea

A

– Walls: CONTRACTION

– Sphincter: Relaxation

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23
Q

Urinary Bladder

— Urination/ Micturition

A

– Detrusor: Contraction

– Trigone & Sphincter: Relaxation

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24
Q

Nicotinic Receptors

A
  • NN – Neural

* NM – Muscular

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25
Q

NN

A

• Ganglion; CNS: Stimulation

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26
Q

NM

A

– Neuromuscular End Plates: Contraction

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27
Q

Parasympathomimetics

— Cholinergic agonists/ Cholinomimetics

A
  • Direct-acting

* Indirect-acting

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28
Q

Direct acting

A
  • Choline Esters

* Alkaloids

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29
Q

Choline Esters

A
  • Mixed (N or M)

* Muscarinic Only

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30
Q

Mixed

A
  • Acetylcholine
  • Carbachol
  • Methacholine
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31
Q

Muscarinic Only

A

Bethanechol (Urecoline)

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32
Q

Alkaloids

A
  • Mixed
  • Nicotinic Only
  • Muscarinic Only
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33
Q

Mixed (N or M)

A

Arecoline

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34
Q

Nicotinic Only

A
  • Nicotine
  • Lobeline
  • Varenicline
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35
Q

Muscarinic Only

A
  • Muscarine

* Pilocarpine

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36
Q

Indirect Acting
— prevent metabolism of ACh
— aka Anticholinesterases

A
  • Short acting
  • Intermediate acting
  • Very long Acting
  • CNS Acting
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37
Q

– aminoalcohol

– Reversible anticholinesterase

A

Edrophonium (Short acting)

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38
Q

DOA of Short Acting

A

15-30 mins

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39
Q

Intermediate acting

A
  • Physostigmine/ Eserine
  • Pyrodostigmine
  • Ambenonium
  • Demecarium
  • Neostigmine
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40
Q

DOA of Internediate acting

A

2-8 hrs; < 24 hrs

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41
Q

Chemical of Intermediate Acting

A

Carbamates

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42
Q

Interaction to AChE of Intermediate acting

A

Reversible

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43
Q

Very Long Acting

A
  • Echothiophate
  • Malathion
  • Parathion
  • Nerve Gases (Tabun, Sarin, Soman)
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44
Q

DOA of Very Long Acting

A

> 24 hrs (days — weeks)

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45
Q

Chemical of Very Long acting

A

Organophosphates

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46
Q

Interaction to AChe of Very Long Acting

A
  • 24-48 hrs: Potentialy Reversible

* > 48 hrs: Irreversible

47
Q

CNS acting

A
  • Donepezil
  • Tacrine
  • Rivastigmine
  • Galantamine
48
Q

Clinical uses: Parasympathomimetics

A
  • Mgt of Alzheimer’s Disease
  • Mgt of Myasthenia Gravis
  • Mgt of Anticholinergic Poisoning
  • Mgt of NMB Toxicity
  • Mgt of Non-obstructive Ileus
  • Mgt of Smoking Cessation
  • Mgt of Glaucoma
  • Mgt of Urinary Retention
  • Pulmonary Challenge Test
49
Q

Mgt of Alzheimer’s Disease

A

CNS Acting

  • Donepezil
  • Tacrine
  • Rivastigmine
  • Galantamine
50
Q

– Autoimmune
– ⬆️ antibody-AcR
– Progressive Muscle Weakness

A

Myasthenia Gravis

51
Q

Diagnosis for Myasthenia Gravis

A
  • Immunologic

* Pharmacologic

52
Q

Immunologic

A

⬆️ antibody-AcR

53
Q

Pharmacologic

A

Edrophonium — Tensilon Test

54
Q

Tx: Myasthenia Gravis

A
  • Immunosuppression

* ⬆️ Muscle Strength

55
Q

Immunisuppression

A

Prednisone

56
Q

⬆️ Muscle Strength

A
  • Pyridostigmine
  • Ambenonium
  • Neostigmine
57
Q

Mgt of Anticholinergic Poisoning

A
  • Control of Peripheral s/sx

* Control of Central s/sx

58
Q

Control of PERIPHERAL s/sx

A
  • Neostigmine

* Pilocarpine

59
Q

Control of Central s/sx

A

BZDs

60
Q

Mgt of NMB Toxicity

A
  • Neostigmine

* Edrophonium

61
Q

Mgt of non-obstructive Ileus

A
  • Pilocarpine

* Physostigmine

62
Q

Mgt of Smoking Cessation

A
  • Nicotine
  • Lobeline
  • Varenicline
63
Q

Mgt of Galucoma

A
  • Demecarium
  • Echotiophate
  • Carbachol
  • Pilocarpine
64
Q

Pulmonary Challenge Test

A

Methacholine

65
Q

S/E: Parasympathomimetics

A

DUMBELS

66
Q

D

A

Diarrhea

67
Q

U

A

Urination

68
Q

M

A

Miosis (contraction)

69
Q

B

A

— Bradycardia

— Bronchoconstriction

70
Q

E

A

— Enuresis

— Excitation

71
Q

L

A

Lacrimation

72
Q

S

A

— Salivation

— Sweating

73
Q

Tx: DUMBELS

A
  • Atropine (principal)

* Pralidoxime (cholinesterase regenerator)

74
Q

Parasympatholytics

— aka Cholinergic Antagonists

A
  • Antimuscarinic

* Antinicotinics

75
Q

Antimuscarinics

A
  • Atropine

* Others

76
Q

Atropine

— antimuscarinic/ anticholinergic

A
  • M1 blockade
  • M2 blockade
  • M3 blockade
  • CNS effects
77
Q

M1 blockade

A

⬇️ HCl secretion

78
Q

M2 blockade

A

Tachycardia (Vagolytic)

79
Q

M3 blockade

A
  • Excorine

* Smooth muscles

80
Q

Exocrine

A

⬇️ secretion (xerostomia, anhidrosis — hyperthermia, flushing)

81
Q

Smooth muscles

A

– 👀
– Bronchi
– GIT
– Urinary Bladder

82
Q

👀

A

— Ciliary Muscle: Cycloplegia

— Circular Muscle: Mydriasis

83
Q

Bronchi

A

Bronchodilation

84
Q

GIT

A

Ileus/ Constipation

85
Q

Urinary Bladder

A

Urinary Retention

86
Q

CNS Effects

A

– Confusion
– Agitation
– Disorientation
– Acute psychosis

87
Q

Others

A
  • CNS
  • Eyes
  • Bronchi
  • GIT
  • Urinary Bladder
88
Q

CNS

A
  • Scopolamine
  • Biperiden
  • Trihexyphenidyl
  • Benztropine
89
Q

👀

A
  • Homatropine
  • Anistropine
  • Cyclopentolate
90
Q

Bronchi

— 1st line in COPD

A
  • Ipratropium
  • Tiotropium
  • Oxytropium
91
Q

GIT

A
  • Pirenzepine

* Telenzepine

92
Q

Urinary Bladder

A
  • Methscopolamine
  • Glycopyrrolate
  • Hyoscine
  • Dicycloverine
  • Oxybutinine
  • Scopolamine
93
Q

Clinical Uses: Antimuscarinics

A
  • Mgt of Symptomatic Bradycardia
  • Mgt of Cholinergic Poisoning
  • Given with Diphenpxylate to ⬇️ addiction
  • Mgt of Motion Sickness
  • Mydriatics/ Cycloplegics
  • Mgt of Parkinsonism & EPS
  • Mgt of Bronchial Asthma & COPD
  • Mgt of Hyperacidity
  • Mgt of Hypermotility disorder & Urinary Incontinence
94
Q

Mgt of Symptomatic Bradycardia

A

Atropine

95
Q

Mgt of Cholinergic Poisoning

A

Atrpoine

96
Q

Given with Diphenoxylate to minimize addiction to Diphenoxylate

A

Atropine

97
Q

Mgt of Motion Sickness

A

Scopolamine

98
Q

Mydriatics/ Cycloplegics

A

-👀-acting
– Homatropine
– Anistropine
– Cyclopentolate

99
Q

Mgt of Parkinsonism & EPS

A
  • Biperiden
  • Benztropine
  • Trihexyphenidyl
100
Q

Mgt of Brochial Asthma & COPD

A
  • Bronchi acting
    – Ipratropium
    – Tiotropium
    – Oxytropium
101
Q

Mgt of Hyperaciditt

A

Pirenzepine

102
Q

Mgt of Hypermotility & Urinary Incontinence

A 
- Urinary Bladder
– Methscopolamine
– Glycopyrrolate
– Hyoscine
– Dicycloverine
– Oxybutinine
– Scopolamine
103
Q

Antinicotinics

A
  • Ganglionic Blockers (NN)

* Neuromuscular Blockers (NM)

104
Q

Ganglionic Blockers

— Vasodilation - HYPOtension

A
  • Trimethaphan
  • Hexamethonium
  • Maccamylamine
105
Q

Neuromuscular Blockers
— aka Skeletal Muscle Relaxants
— use:
- ✔️ anesthetic agents (prior to surgery)
- ✔️ Mgt of spastic diseases (Spastic Cerebral Palsy)

A
  • Depolarizing/ Non-competitive/ Irreversible NMB

* non-depolarizing/ Competitive/ Reverisble NMB

106
Q

Depolarizing/ Non-competitive/ Irreversible NMB

A

Succinylcholine

107
Q

– MOA: IRREVERSIBLY stimulates NM receptors
– Effects:
- Initial: Tremors (Tetany)
- Final: Paralysis

A

Succinylcholine

108
Q

Non-depolarizing/ Competitive/ Reversible NMB

A
  • Isoquinoline (-curium)

* Steroidal (-curoniun)

109
Q

Isoquinoline (-curium)

A
  • Atracurium

* Tubocurarine

110
Q

Steroidal (-curonium)

A
  • Pancuronium

* Rocuronium

111
Q

MOA: Non-depolarizing/ Competitive/ Reversible NMB

A

Immediately blocks NM receptor

— IMMEDIATE EFFECT

112
Q

S/E: Neuromuscular Blockers

A

• Respiratory/ Diaphragmatic Paralysis
– Tx:
- Neostigmine
- Edrophonium

113
Q

S/E: Succinylcholine

A 
– Myalgia
– Myositis
– Rhabdomyolysis
– Malignant Hyperthermia 
    — Tx: Dantrolene
114
Q

S/E: Tubocurarine

A

Anaphylaxis

— Tx: Epinephrine

Pharmacology (21 decks)

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