3.3 - Parasympathetic Drugs Flashcards
1
Q
Parasymphathetic Drugs
A
- Biosynthesis
- Receptors
- Parasympathomimetics
- Parasympatholytics
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
3
Q
Locations
A
– All pre ganglionic neurons
– Cholinergic, post-ganglionic neurons
– Somatic Nerves
– CNS
4
Q
Steps
A
Choline ➡️1️⃣ Choline + AcCoA ➡️2️⃣ ACh ➡️ Vesicular storage throug VAT ➡️ Release
5
Q
1️⃣
A
Active uptake
6
Q
2️⃣
A
CHAT
– Choline Acetyltransferase
7
Q
Fate of the ACh in the cleft
A
- Binding to post-synaptic ®
* Metabolism by AChE
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
9
Q
Active uptake of ACh: INHIBITOR
A
Hemicholinium
10
Q
Vesicular Storage of ACh: INHIBITOR
A
Vesamicol
11
Q
Release of ACh (exocytosis): STIMULATOR
A
Alpha-latrotoxin
12
Q
Release of ACh (exocytosis): INHIBITOR
A
Botulinum toxin
13
Q
Metabolism by AChE: INHIBITORS
A
Organophosphates
14
Q
Receptors
A
- Muscarinic Receptor
* Nicotinic Receptors
15
Q
Muscarinic Receptor
A
- M1
- M2
- M3
16
Q
M1
A
– Location: Gastric Glands
– Effect: ⬆️ HCl secretion
17
Q
M2
A
– Location: ❤️
– Effects: Bradycardia
18
Q
M3
A
– Location: Exocrine Glands
– Effect: ⬆️ secretion
19
Q
M3
A
– Location: Smooth muscles — Gq linked — Contraction – Effect: - 👀 - Brochi - GIT - Urinary Bladder
20
Q
👀
A
– Ciliary Muscle: ⬆️ Accomodation
– Circular Muscle: MIOSIS
21
Q
Bronchi
A
BronchoCONSTRICTION
22
Q
GIT
— Diarrhea
A
– Walls: CONTRACTION
– Sphincter: Relaxation
23
Q
Urinary Bladder
— Urination/ Micturition
A
– Detrusor: Contraction
– Trigone & Sphincter: Relaxation
24
Q
Nicotinic Receptors
A
- NN – Neural
* NM – Muscular
25
NN
• Ganglion; CNS: Stimulation
26
NM
– Neuromuscular End Plates: Contraction
27
Parasympathomimetics
| — Cholinergic agonists/ Cholinomimetics
* Direct-acting
| * Indirect-acting
28
Direct acting
* Choline Esters
| * Alkaloids
29
Choline Esters
* Mixed (N or M)
| * Muscarinic Only
30
Mixed
* Acetylcholine
* Carbachol
* Methacholine
31
Muscarinic Only
Bethanechol (Urecoline)
32
Alkaloids
* Mixed
* Nicotinic Only
* Muscarinic Only
33
Mixed (N or M)
Arecoline
34
Nicotinic Only
* Nicotine
* Lobeline
* Varenicline
35
Muscarinic Only
* Muscarine
| * Pilocarpine
36
Indirect Acting
— prevent metabolism of ACh
— aka Anticholinesterases
* Short acting
* Intermediate acting
* Very long Acting
* CNS Acting
37
– aminoalcohol
| – Reversible anticholinesterase
Edrophonium (Short acting)
38
DOA of Short Acting
15-30 mins
39
Intermediate acting
* Physostigmine/ Eserine
* Pyrodostigmine
* Ambenonium
* Demecarium
* Neostigmine
40
DOA of Internediate acting
2-8 hrs; < 24 hrs
41
Chemical of Intermediate Acting
Carbamates
42
Interaction to AChE of Intermediate acting
Reversible
43
Very Long Acting
* Echothiophate
* Malathion
* Parathion
* Nerve Gases (Tabun, Sarin, Soman)
44
DOA of Very Long Acting
> 24 hrs (days — weeks)
45
Chemical of Very Long acting
Organophosphates
46
Interaction to AChe of Very Long Acting
* 24-48 hrs: Potentialy Reversible
| * > 48 hrs: Irreversible
47
CNS acting
* Donepezil
* Tacrine
* Rivastigmine
* Galantamine
48
Clinical uses: Parasympathomimetics
* 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
Mgt of Alzheimer's Disease
CNS Acting
- Donepezil
- Tacrine
- Rivastigmine
- Galantamine
50
– Autoimmune
– ⬆️ antibody-AcR
– Progressive Muscle Weakness
Myasthenia Gravis
51
Diagnosis for Myasthenia Gravis
* Immunologic
| * Pharmacologic
52
Immunologic
⬆️ antibody-AcR
53
Pharmacologic
Edrophonium — Tensilon Test
54
Tx: Myasthenia Gravis
* Immunosuppression
| * ⬆️ Muscle Strength
55
Immunisuppression
Prednisone
56
⬆️ Muscle Strength
* Pyridostigmine
* Ambenonium
* Neostigmine
57
Mgt of Anticholinergic Poisoning
* Control of Peripheral s/sx
| * Control of Central s/sx
58
Control of PERIPHERAL s/sx
* Neostigmine
| * Pilocarpine
59
Control of Central s/sx
BZDs
60
Mgt of NMB Toxicity
* Neostigmine
| * Edrophonium
61
Mgt of non-obstructive Ileus
* Pilocarpine
| * Physostigmine
62
Mgt of Smoking Cessation
* Nicotine
* Lobeline
* Varenicline
63
Mgt of Galucoma
* Demecarium
* Echotiophate
* Carbachol
* Pilocarpine
64
Pulmonary Challenge Test
Methacholine
65
S/E: Parasympathomimetics
DUMBELS
66
D
Diarrhea
67
U
Urination
68
M
Miosis (contraction)
69
B
— Bradycardia
| — Bronchoconstriction
70
E
— Enuresis
| — Excitation
71
L
Lacrimation
72
S
— Salivation
| — Sweating
73
Tx: DUMBELS
* Atropine (principal)
| * Pralidoxime (cholinesterase regenerator)
74
Parasympatholytics
| — aka Cholinergic Antagonists
* Antimuscarinic
| * Antinicotinics
75
Antimuscarinics
* Atropine
| * Others
76
Atropine
| — antimuscarinic/ anticholinergic
* M1 blockade
* M2 blockade
* M3 blockade
* CNS effects
77
M1 blockade
⬇️ HCl secretion
78
M2 blockade
Tachycardia (Vagolytic)
79
M3 blockade
* Excorine
| * Smooth muscles
80
Exocrine
⬇️ secretion (xerostomia, anhidrosis — hyperthermia, flushing)
81
Smooth muscles
– 👀
– Bronchi
– GIT
– Urinary Bladder
82
👀
— Ciliary Muscle: Cycloplegia
| — Circular Muscle: Mydriasis
83
Bronchi
Bronchodilation
84
GIT
Ileus/ Constipation
85
Urinary Bladder
Urinary Retention
86
CNS Effects
– Confusion
– Agitation
– Disorientation
– Acute psychosis
87
Others
* CNS
* Eyes
* Bronchi
* GIT
* Urinary Bladder
88
CNS
* Scopolamine
* Biperiden
* Trihexyphenidyl
* Benztropine
89
👀
* Homatropine
* Anistropine
* Cyclopentolate
90
Bronchi
| — 1st line in COPD
* Ipratropium
* Tiotropium
* Oxytropium
91
GIT
* Pirenzepine
| * Telenzepine
92
Urinary Bladder
* Methscopolamine
* Glycopyrrolate
* Hyoscine
* Dicycloverine
* Oxybutinine
* Scopolamine
93
Clinical Uses: Antimuscarinics
* 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
Mgt of Symptomatic Bradycardia
Atropine
95
Mgt of Cholinergic Poisoning
Atrpoine
96
Given with Diphenoxylate to minimize addiction to Diphenoxylate
Atropine
97
Mgt of Motion Sickness
Scopolamine
98
Mydriatics/ Cycloplegics
-👀-acting
– Homatropine
– Anistropine
– Cyclopentolate
99
Mgt of Parkinsonism & EPS
* Biperiden
* Benztropine
* Trihexyphenidyl
100
Mgt of Brochial Asthma & COPD
- Bronchi acting
– Ipratropium
– Tiotropium
– Oxytropium
101
Mgt of Hyperaciditt
Pirenzepine
102
Mgt of Hypermotility & Urinary Incontinence
```
- Urinary Bladder
– Methscopolamine
– Glycopyrrolate
– Hyoscine
– Dicycloverine
– Oxybutinine
– Scopolamine
```
103
Antinicotinics
* Ganglionic Blockers (NN)
| * Neuromuscular Blockers (NM)
104
Ganglionic Blockers
| — Vasodilation - HYPOtension
* Trimethaphan
* Hexamethonium
* Maccamylamine
105
Neuromuscular Blockers
— aka Skeletal Muscle Relaxants
— use:
- ✔️ anesthetic agents (prior to surgery)
- ✔️ Mgt of spastic diseases (Spastic Cerebral Palsy)
* Depolarizing/ Non-competitive/ Irreversible NMB
| * non-depolarizing/ Competitive/ Reverisble NMB
106
Depolarizing/ Non-competitive/ Irreversible NMB
Succinylcholine
107
– MOA: IRREVERSIBLY stimulates NM receptors
– Effects:
- Initial: Tremors (Tetany)
- Final: Paralysis
Succinylcholine
108
Non-depolarizing/ Competitive/ Reversible NMB
* Isoquinoline (-curium)
| * Steroidal (-curoniun)
109
Isoquinoline (-curium)
* Atracurium
| * Tubocurarine
110
Steroidal (-curonium)
* Pancuronium
| * Rocuronium
111
MOA: Non-depolarizing/ Competitive/ Reversible NMB
Immediately blocks NM receptor
| — IMMEDIATE EFFECT
112
S/E: Neuromuscular Blockers
• Respiratory/ Diaphragmatic Paralysis
– Tx:
- Neostigmine
- Edrophonium
113
S/E: Succinylcholine
```
– Myalgia
– Myositis
– Rhabdomyolysis
– Malignant Hyperthermia
— Tx: Dantrolene
```
114
S/E: Tubocurarine
Anaphylaxis
| — Tx: Epinephrine
