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Cardiovascular II > Acetylcholine agonists and antagonists > Flashcards

Acetylcholine agonists and antagonists Flashcards

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1
Q

Function of ChAT enzyme

A

Synthesizes Ach from acetyl-CoA and choline in the nerve terminal

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2
Q

Enzyme that metabolizes Ach in the synaptic cleft and thereby terminates its action

A

Acetylcholinesterase (AchE)

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3
Q

Toxin that enters cholinergic nerve terminals and prevents the release of Ach, causing a neuromuscular blocking effect

A

Botulinum toxin

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4
Q

Presynaptic membrane protein required for the fusion of NT containing vesicles. Cleaved by botulinum toxin

A

SNAP - synaptosome associated protein

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5
Q

Presynaptic membrane protein that helps in vesicle transport and fusion at the plasma membrane. Cleaved by botulinum toxin.

A

VAMP - vesicle associated membrane protein

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6
Q

Therapeutic uses of botulinum toxin

A

Management of muscle dystonia and spasticity
Chronic pain and localized muscle spasms
Cosmetic use

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7
Q

Agent that enters presynaptic neuron to prevent packaging of Ach into vesicles

A

Vesamicol

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8
Q

Agent that prevents choline entry into presynaptic neuron, thereby limiting the production of Ach

A

Hemicholinium

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9
Q

Cholinesterase with a lower specificity for Ach compared to acetylcholinesterase. Found in blood plasma, liver, glia, and many other tissues. Main function is hydrolysis of ingested esters.

A

Butyrylcholinesterase (pseudocholinesterase)

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10
Q

Neuromuscular blocking agents, not including botulinum toxin

A

Atracurium
Cisatracurium
Pancuronium
Rocuronium
Vecuronium
Succinylcholine

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11
Q

Atracurium route of elimination

A

Plasma esterase

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12
Q

Cisatracurium route of elimination

A

Spontaneous chemical degradation

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13
Q

Pancuronium route of elimination

A

Renal excretion

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14
Q

Rocuronium route of elimination

A

Biliary and renal excretion

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15
Q

Vecuronium route of elimination

A

Biliary and renal excretion
Hepatic metabolism

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16
Q

Succinylcholine route of elimination

A

Plasma (butyryl) cholinesterase

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17
Q

Side effects of succinylcholine

A

Prolonged apnea
Hyperkalemia leading to MI
Postop myalgia
Malignant hyperthermia

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18
Q

Risk factor for prolonged apnea from succinylcholine

A

Genetic inheritance of atypical cholinesterase or deficiency of pseudocholinesterase –> results in slow metabolism

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19
Q

Risk factors for hyperkalemia side effect from succinylcholine

A

Unhealed muscle injury
Intra-abdominal infection
Paralysis/spinal cord injury
Child

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20
Q

Risk factor for malignant hyperthermia in succinylcholine use

A

Use with inhalation anesthetics

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21
Q

Muscarinic cholinergic receptor is what type of receptor?

A

GPCR

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22
Q

Nicotinic cholinergic receptor is what type of receptor?

A

Nicotinic

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23
Q

Result of M1 receptor stimulation

A

Gq receptor –> Increase IP3 and DAG cascade

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24
Q

Result of M2 receptor stimulation

A

Gi –> decrease cAMP synthesis

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25
Result of M3 receptor stimulation
Gq --> increase IP3 and DAG cascade
26
Result of M4 receptor stimulation
Gi --> decrease cAMP synthesis
27
Result of M5 receptor stimulation
Gq --> increase IP3 and DAG cascade
28
Gq muscarinic receptors
M1, M3, and M5
29
Gi muscarinic receptors
M2 and M4
30
Result of nicotinic receptor stimulation
Na/K depolarizing current
31
Agent that selectively blocks muscarinic receptors
Atropine
32
Muscarinic receptor type primarily present in gastric glands, CNS, and autonomic ganglia. Mediates gastric acid secretion and relaxation of LES. Role in learning, memory, and motor functions.
M1
33
Muscarinic receptor type primarily located in heart and CNS. Mediates vagal bradycardia.
M2
34
Muscarinic receptor type primarily located in visceral smooth muscle, glands, vascular endothelium, iris, and ciliary muscles. Mediates visceral smooth muscle contraction, vasodilation, constriction of pupil, and contraction of ciliary muscle.
M3
35
Agents that can block nicotinic receptors
Tubocurarine Hexamthonium
36
Agonists of Nm receptors
Ach Carbachol (CCh) Suxamethonium
37
Antagonists of Nm receptors
Tubocurarine Atracurium
38
Agonists of Nn receptors
Ach Carbachol (CCh) Nicotine
39
Antagonists of Nn receptors
Trimethaptan Hexamethonium
40
Affect of SA node hyperpolarization
Decrease in rate of diastolic depolarization, reduction in impulse generation --> bradycardia
41
Direct acting muscarinic receptors agonists
Ach Bethanechol Carbachol Pilocarpine Methacholine
42
Drug of choice for neurogenic bladder
Bethanechol
43
Direct acting nicotinic agonists
Nicotine Varenicline
44
Naturally occuring reversible anticholinesterase
Physostigmine
45
Synthetic reversible anticholinesterases
Neostigmine Pyridostigmine Donepezil Revastigmine Edrophonium
46
General classes of irreversible anticholinesterases
Organophosphorus compounds Nerve gasses Carbamate esters
47
Organophosphorus compounds that cause irreversible inhibition of anticholinesterase
Echothiophate Parathion Malathion
48
General mechanism of indirect acting cholinergic drugs (cholinomimetics)
Inhibit cholinesterase
49
Nerve gasses that irreversibly inhibit cholinesterase
Tabun Sarin Soman
50
Carbamate esters that irreversibly inhibit cholinesterase
Carbaryl Propoxur/Baygon
51
Mechanism of cholinesterase inhibition by carbamates
Carbamylates the active site of AchE
52
Cholinergic drug used in diagnosis of myasthenia gravis
Edrophonium
53
Cholinergic drugs used in treatment of myasthenia gravis
Neostigmine Pyridostigmine
54
Cholinergic drugs used to stimulate bladder and bowel after surgery
Bethanechol Carbachol
55
Cholinergic drugs used to lower IOP in chronic simple glaucoma
Pilocarpine Physostigmine
56
Cholinergic drug used as antidote in atropine poisoning
Physostigmine
57
Cholinergic drugs used to improve cognitive function in Alzheimer's disease
Rivastigmine Galantamine Donepezil
58
Clinical uses of atropine
Antispasmodic Antisecretory Management of AchE inhibitor poisoning Antidiarrheal Ophthalmology
59
Clinical use and main side effect of scopolamine
Motion sickness - side effect of sedation
60
Anticholinergic drugs
Atropine Scopolamine Ipratropium Tiotropium Tropicamide Benztropine Trihexyphenidyl Oxybutynin TCAs Phenothiazines Antihistaminic
61
Clinical uses of ipratropium and tiotropium
Asthma COPD
62
Clinical use of tropicamide
Topical in eye --> mydriatic
63
Clinical uses of benztropine and trihexyphenidyl
Parkinsonism EPS induced by antipsychotics
64
Lipid soluble anticholinergics that act centrally
Benztropine Trihexyphenidyl
65
Clinical use of oxybutynin
Overactive bladder
66
Anticholinergic highly selective, but not specific, for muscarinic receptors. Causes reversible blockade of cholinomimetic actions.
Atropine/hyoscyamine
67
CNS effects of atropine
Overall --> stimulant Stimulates medullar centers Depresses vestibular excitation Blocks basal ganglia cholinergic overactivity
68
CVS effects of atropine
Tachycardia --> blocks M2 in SA node Increases conduction rate in AV node
69
Ocular effects of atropine
Mydriasis Cycloplegia and abolition of light reflex Photophobia and blurring of near vision IOP rises Dry eye Anesthetic action on cornea (local)
70
Respiratory effects of atropine
Bronchodilation and reduction in airway resistance Antagonizes vagal mediated overactivity due to histamines, leukotrienes, etc.
71
Urinary effects of atropine
Relaxation of ureter and bladder --> urine retention in BPH Increase bladder capacity and controls detrusor hyperreflexia --> neurogenic bladder
72
Visceral smooth muscle effects of atropine
Relaxation Constipation Relief of GIT spasms
73
Effect of atropine on glands
Decreases salivary, sweat, tracheobronchial, and lacrimal secretions Decreases acid, pepsin, and mucus secretions in stomach
74
Effect of atropine on temperature and mechanism
Increases Decreased sweating and stimulation of temp regulating center in hypothalamus
75
First-line therapy for symptomatic bradycardia in the absence of reversible causes
Atropine
76
Drug used to block muscarinic effects of neostigmine used in myasthenia gravis, decurarization, and cobra envenomation
Atropine
77
Contraindications of anticholinergic use
Narrow angle glaucoma --> precipitates angle closure BPH --> urinary retention
78
Symptoms of belladonna poisoning
Dry mouth Dry, flushed, hot skin Fever Dilated pupils and photophobia Urinary retention Excitement, psychosis, delirium, hallucinations Hypotension Weak, rapid pulse Respiratory depression Convulsions and coma
79
Diagnosis of belladonna poisoning
SubQ methacholine 5 mg or neostigmine 1 mg
80
Treatment of belladonna poisoning
Gastric lavage with tannic acid Symptom management Physostigmine Other supportive measures
81
Signs and symptoms of organophosphate poisoning
Tearing, drooling, incontinence Fall in BP Tachycardia or bradycardia Muscular fasciculations and weakness Respiratory paralysis Excitement, tremor, convulsions, and coma
82
Treatment of organophosphate poisnoning
Gastric lavage Supportive measures --> airway, BP, fluid, electrolytes Atropine --> specific antidote Cholinesterase reactivators --> oximes
83
Dosing of atropine antidote in organophosphate poisoning
2 mg IV every 10 minutes until dry mouth or atropinization Maximum of 200 mg/day
84
Oximes
Pralidoxime Obidoxime
85
Mechanism of oximes
Provides OH group to free AchE esteratic site --> reactivates phosphorylated enzymes
86
When are oximes not effective
Carbamate poisoning
87
Selective ganglion agonists (Nn)
Nicotine - small doses Varenicline
88
Non-selective ganglion agonists (Nn)
Ach Carbachol Pilocarpine Anticholinesterases
89
Competitive ganglion blockers (Nn)
Hexamethonium Mecamylamine
90
Persistent ganglion depolarizers with blocking action (Nn)
Nicotine - large doses Anticholinesterases - larger doses
91
Effects of ganglion blockers (Nn) on CVS
Tachycardia Vasodilation Hypotension Decreased venous return and CO
92
Adverse effects of nicotine replacements used in treatment of nicotine dependence
HA Dyspepsia Abdominal cramps Loose motion
93
Partial agonist of alpha-4 beta-2 nicotinic receptors that reduces nicotine cravings and withdrawal symptoms
Varenicline
94
Adverse effects of varenicline
Mood changes Irrational behavior Sleep disorder Agitation Suicidal thoughts
95
Treatment options for nicotine dependence
Counseling Nicotine replacement Varenicline Bupropion
96
Adverse effects of PDE5 inhibitors
HA Flushing Nasal congestion Visual disturbance -- blue-green tinge
97
Interactions of PDE5 inhibitors
Do not use with nitrites --> profound hypotension and reflex tachycardia Reduced initial dose with CYP3A4 inhibitors
98
Drug used for treating pulmonary arterial HTN. Sensitizes sGC to NO and directly stimulates sGC without NO to increase IC levels of cGMP.
Riociguat
99
Drug interaction of riociguat
Do not use with phosphodiesterase inhibitors --> hypotension
100

Cardiovascular II (29 decks)

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