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Pharmacology > VII - Cholinergic Pharmacology > Flashcards

VII - Cholinergic Pharmacology Flashcards

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1
Q

Primary neurotransmitter in all autonomic ganglia and at the synapses between parasympathetic post-ganglionic neurons and their effector cells

A

acetylcholine

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2
Q

Primary neurotransmitter at the somatic (voluntary) skeletal muscle neuromuscular junction

A

acetylcholine

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3
Q

Steps in Cholinergic Stimulation

A

synthesis, storage, release, termination

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4
Q

Cholinergic Stimulation: Step 1

A

SYNTHESIS - ACh is synthesized from acetyl CoA and choline by the enzyme choline acyltransferase (ChAT)

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5
Q

Cholinergic Stimulation: choline transport is inhibited by

A

hemicholinium

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6
Q

Cholinergic Stimulation: Step 2

A

STORAGE - ACh is actively transported into vesicles for storage by vesicle-associated transporter (VAT)

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7
Q

Cholinergic Stimulation: ACh vesicle storage is inhibited by

A

vesamicol

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8
Q

Cholinergic Stimulation: Step 3

A

RELEASE - entry of Ca triggers interaction among SNARE proteins (VAMPs, SNAPs)

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9
Q

Cholinergic Stimulation: alters synaptobrevins to prevent release of ACh

A

botulinum toxin

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10
Q

Cholinergic Stimulation: Step 4

A

TERMINATION - degradation of ACh into choline and acetate by acetylcholinesterase

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11
Q

Cholinergic Stimulation: inhibits acetylcholinesterase

A

Indirect-Acting Cholinomimetics: neostigmine, carbamates, organophosphates

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12
Q

Cholinergic drugs are not very useful for systemic therapy because

A

their effects are not sufficiently selective

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13
Q

Cholinoreceptors: nerve endings, Gq-coupled, increase IP3, DAG cascade

A

M1

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14
Q

Cholinoreceptors: heart, some nerve endings, Gi-coupled, decrease cAMP, activates K+ channels

A

M2

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15
Q

Cholinoreceptors: effector cells of smooth muscles, glands and endothelium, Gq-coupled, increase IP3, DAG cascade

A

M3

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16
Q

Cholinoreceptors: ANS ganglia, ion channel, depolarizes, action potential

A

Nn

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17
Q

Cholinoreceptors: neuromuscular end-plate, ion channel, depolarizes, action potential

A

Nm

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18
Q

Betanechol: Class

A

cholinomimetic - direct-acting, muscarinic

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19
Q

Betanechol: MOA

A

activates M3

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20
Q

Betanechol: Uses

A

bladder and bowel atony (post-op, spinal cord injury)

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21
Q

Betanechol: Side Effects

A

cyclospasm, diarrhea, urinary urgency, vasodilation, reflex tachycardia, sweating

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22
Q

Pilocarpine: Class

A

cholinomimetic - direct-acting, muscarinic

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23
Q

Pilocarpine: MOA

A

activates M3 in ciliary muscle (inc. aqueous humor outflow) and salivary glands (inc. salivation)

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24
Q

Pilocarpine: Uses

A

glaucoma, Sjorgen syndrome, Sicca syndrome

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25
Pilocarpine: Side Effects
miosis, BOV (cyclospasm)
26
Nicotine: Similar Drug
Varenicline
27
Nicotine: Class
cholinomimetic - direct-acting, nicotinic
28
Nicotine: MOA
activates Nn and Nm
29
Nicotine: Uses
smoking cessation
30
Nicotine: Side Effects
generalized ganglionic stimulation: hypertension, tachycardia, nausea, vomiting, diarrhea
31
Nicotine: Overdose
convulsions, paralysis, coma
32
CNS stimulation, miosis, spasm of accomodation, bronchocostriction, excessive GIT/GUT smooth muscle activity, increased secretory activity, vasodilation
Muscarinic Toxicity
33
Muscarine and similar alkaloids are found in these mushrooms
Inocybe, Amanita muscaria
34
Symptoms of Mushroom Poisoning
nausea, vomiting, diarrhea
35
ganglionic stimulation, blockade of neuromuscular end-plate depolarization (fasciculations, paralysis), CNS toxicity (convulsions, CNS depression)
Nicotinic Toxicity
36
Bind to cholinesterase and undergo hydrolysis releasing the alcohol portion
Indirect-Acting Cholinomimetics
37
The _____ portion of indirect-acting cholinomimetics is retained and slowly released to prevent binding and hydrolysis of endogenous acetylcholine which amplifies ACh effects.
acidic portion
38
Edrophonium: Class
cholinomimetic - indirect-acting
39
Edrophonium: MOA
inhibits acetylcholinesterase, amplifies endogenously released ACh
40
Edrophonium: Uses
diagnosis of Myasthenia Gravis (Tensilon Test), differentiation of cholinergic crisis and myasthenic crisis
41
Side Effects: miosis, salivation, nausea, vomiting, diarrhea, bradycardia
Edrophonium, Neostigmine, Rivastigmine
42
Edrophonium: IV
very short-acting
43
Neostigmine: Similar Drugs
pyridostigmine, physostigmine
44
Neostigmine: Class
cholinomimetic - indirect-acting
45
Neostigmine: MOA
inhibits acetylcholinesterase, amplifies endogenously released ACh
46
Neostigmine: Uses
treatment of Myasthenia Gravis, reversal of non-depolarizing neuromuscular blockade, Ogilvie syndrome, glaucoma (physostigmine)
47
Side Effects: miosis, salivation, nausea, vomiting, diarrhea, bradycardia
Edrophonium, Neostigmine, Rivastigmine
48
Neostigmine: muscarinic effects are blocked by
Atropine
49
Autoimmune destruction of nicotinic ACh receptors, fluctuating muscle, weakness, ocular symptoms, bulbar symptoms, proximal muscle weakness
Myasthenia Gravis
50
Myasthenia Gravis: acute worsening of symptoms due to infection, stress or undermedication
myasthenic crisis
51
Myasthenia Gravis: excessive activation of cholinoreceptors, skeletal muscle weakness, parasympathetic signs due to overmedication
cholinergic crisis
52
Edrophonium _____ muscle strength in myasthenic crisis.
improves
53
Edrophonium _____ muscle strength in cholinergic crisis.
weakens
54
Rivastigmine: Similar Drugs
galantamine, donepezil, tacrine
55
Rivastigmine: Class
cholinomimetic - indirect-acting
56
Rivastigmine: MOA
inhibits acetylcholinesterase, amplifies endogenously released ACh
57
Rivastigmine: Uses
Alzheimer's Disease
58
Side Effects: miosis, salivation, nausea, vomiting, diarrhea, bradycardia
Edrophonium, Neostigmine, Rivastigmine
59
Organophosphate Poisoning Symptoms
diarrhea, urination, miosis, bronchospasm, bradycardia, excitation (skeletal muscle, CNS), lacrimation, sweating, salivation
60
Atropine: Class
cholinergic antagonist - muscarinic
61
Atropine: MOA
competitively blocks all muscarinic receptors
62
Atropine: Uses
antidote for organophosphate poisoning (first choice), mydriatic, cycloplegic, bradycardia, hypersalivation
63
Side Effects: tachycardia, mydriasis, cycloplegia, skin flushing, delirium, hallucinations
Atropine
64
Atropine: No effect on _____ of organophosphate toxicity
nicotinic signs
65
Pralidoxime: Class
cholinesterase regenerator, antidote
66
Pralidoxime: MOA
binds with phosphorus of organophosphate, breaks organophosphate bond with cholinesterase
67
Pralidoxime: Uses
antidote for organophosphate poisoning and nerve gas poisoning (sarin, tabun)
68
Pralidoxime: Side Effects
muscle weakness
69
Pralidoxime: Administration
must be administered before 6-8 hours of organophasphate bond with cholinesterase occurs
70
Prototype non-selective muscarinic blocker, found in Atropa belladonna, tertiary amine that readily crosses membrane barriers
Atropine
71
Atropine: Similar Drugs
homatropine, cyclopentolate, tropicamide
72
Benztropine: Similar Drugs
biperiden, trihexyphenidyl
73
Benztropine: Class
cholinergic antagonist - muscarinic
74
Benztropine: MOA
competitively blocks all muscarinic receptors, restores neurotransmitter balance in the basal ganglia
75
Benztropine: Uses
Parkinson's Disease
76
Benztropine: Side Effects
BOV, dry eyes, constipation, dry mouth, urinary retention
77
Benztropine: Reduces _____ more than bradykinesis or rigidity
tremors
78
Muscarinic Antagonists for Parkinsonism
trihexyphenidyl, benztropine, biperiden
79
Ipratropium: Similar Drugs
tiotropium
80
Ipratropium: Class
cholinergic antagonist - muscarinic
81
Ipratropium: MOA
blocks muscarinic receptors in bronchial smooth muscle, prevents vagal-stimulated bronchoconstriction
82
Ipratropium: Uses
asthma, COPD
83
Ipratropium: Side Effects
dry mouth, cough, nasal dryness
84
Ipratropium: More effective and less toxic than _____ in patients with COPD and heart disease
beta-agonists
85
Preferred bronchodilator in patients with COPD and heart disease, less likely to cause tachycardia and cardiac arrythmias
Ipratropium
86
Scopolamine: Class
cholinergic antagonist - muscarinic
87
Scopolamine: MOA
competitively blocks all muscarinic receptors, antagonizes histamine and serotonin
88
Scopolamine: Uses
motion sickness
89
Scopolamine: Side Effects
drowsiness, BOV, dry eyes, constipation, dry mouth, urinary retention
90
Scopolamine: Application
transdermal patch
91
Hyperthermia, cutaneous vasodilation, decreased secretions, tachycardia, intraventricular conduction block, constipation, BOV, CNS toxicity
Atropine Toxicity - HOT as a hare, DRY as a bone, RED as a beet, BLIND as a bat, MAD as a hatter
92
Contraindications for Muscarine Blockers
infants, hyperthermia (decreased sweating), acute angle closure glaucoma, benign prostatic hyperplasia
93
Competitive pharmacologic antagonists at nicotinic ACh receptors, first successful agents for HPN, adverse blockade
Ganglion Blockers
94
Hexamethonium: Similar Drugs
trimethaphan
95
Hexamethonium: Class
cholinergic antagonist - nicotinic
96
Hexamethonium: MOA
competitively blocks Nn nicotinic ACh receptors
97
Hexamethonium: Uses
hypertension (obsolete), hypertensive emergencies
98
Hexamethonium: Side Effects
postural hypotension, dry mouth, BOV, constipation, sexual dysfunction
99
Important for producing complete skeletal muscle relaxation in surgery
Neuromuscular Blockers
100
Neuromuscular Blockers: Non-Depolarizing
tubocurarine, pancuronium, atracurium, vecuronium
101
Neuromuscular Blockers: Depolarizing
succinylcholine

Pharmacology (34 decks)

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