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Cardiovascular II > Acetylcholine agonists and antagonists > Flashcards

Acetylcholine agonists and antagonists Flashcards

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
Q

Result of M3 receptor stimulation

A

Gq –> increase IP3 and DAG cascade

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26
Q

Result of M4 receptor stimulation

A

Gi –> decrease cAMP synthesis

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27
Q

Result of M5 receptor stimulation

A

Gq –> increase IP3 and DAG cascade

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28
Q

Gq muscarinic receptors

A

M1, M3, and M5

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29
Q

Gi muscarinic receptors

A

M2 and M4

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30
Q

Result of nicotinic receptor stimulation

A

Na/K depolarizing current

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31
Q

Agent that selectively blocks muscarinic receptors

A

Atropine

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32
Q

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.

A

M1

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33
Q

Muscarinic receptor type primarily located in heart and CNS. Mediates vagal bradycardia.

A

M2

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34
Q

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.

A

M3

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35
Q

Agents that can block nicotinic receptors

A

Tubocurarine
Hexamthonium

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36
Q

Agonists of Nm receptors

A

Ach
Carbachol (CCh)
Suxamethonium

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37
Q

Antagonists of Nm receptors

A

Tubocurarine
Atracurium

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38
Q

Agonists of Nn receptors

A

Ach
Carbachol (CCh)
Nicotine

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39
Q

Antagonists of Nn receptors

A

Trimethaptan
Hexamethonium

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40
Q

Affect of SA node hyperpolarization

A

Decrease in rate of diastolic depolarization, reduction in impulse generation –> bradycardia

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41
Q

Direct acting muscarinic receptors agonists

A

Ach
Bethanechol
Carbachol
Pilocarpine
Methacholine

42
Q

Drug of choice for neurogenic bladder

A

Bethanechol

43
Q

Direct acting nicotinic agonists

A

Nicotine
Varenicline

44
Q

Naturally occuring reversible anticholinesterase

A

Physostigmine

45
Q

Synthetic reversible anticholinesterases

A

Neostigmine
Pyridostigmine
Donepezil
Revastigmine
Edrophonium

46
Q

General classes of irreversible anticholinesterases

A

Organophosphorus compounds
Nerve gasses
Carbamate esters

47
Q

Organophosphorus compounds that cause irreversible inhibition of anticholinesterase

A

Echothiophate
Parathion
Malathion

48
Q

General mechanism of indirect acting cholinergic drugs (cholinomimetics)

A

Inhibit cholinesterase

49
Q

Nerve gasses that irreversibly inhibit cholinesterase

A

Tabun
Sarin
Soman

50
Q

Carbamate esters that irreversibly inhibit cholinesterase

A

Carbaryl
Propoxur/Baygon

51
Q

Mechanism of cholinesterase inhibition by carbamates

A

Carbamylates the active site of AchE

52
Q

Cholinergic drug used in diagnosis of myasthenia gravis

A

Edrophonium

53
Q

Cholinergic drugs used in treatment of myasthenia gravis

A

Neostigmine
Pyridostigmine

54
Q

Cholinergic drugs used to stimulate bladder and bowel after surgery

A

Bethanechol
Carbachol

55
Q

Cholinergic drugs used to lower IOP in chronic simple glaucoma

A

Pilocarpine
Physostigmine

56
Q

Cholinergic drug used as antidote in atropine poisoning

A

Physostigmine

57
Q

Cholinergic drugs used to improve cognitive function in Alzheimer’s disease

A

Rivastigmine
Galantamine
Donepezil

58
Q

Clinical uses of atropine

A

Antispasmodic
Antisecretory
Management of AchE inhibitor poisoning
Antidiarrheal
Ophthalmology

59
Q

Clinical use and main side effect of scopolamine

A

Motion sickness - side effect of sedation

60
Q

Anticholinergic drugs

A

Atropine
Scopolamine
Ipratropium
Tiotropium
Tropicamide
Benztropine
Trihexyphenidyl
Oxybutynin
TCAs
Phenothiazines
Antihistaminic

61
Q

Clinical uses of ipratropium and tiotropium

A

Asthma
COPD

62
Q

Clinical use of tropicamide

A

Topical in eye –> mydriatic

63
Q

Clinical uses of benztropine and trihexyphenidyl

A

Parkinsonism
EPS induced by antipsychotics

64
Q

Lipid soluble anticholinergics that act centrally

A

Benztropine
Trihexyphenidyl

65
Q

Clinical use of oxybutynin

A

Overactive bladder

66
Q

Anticholinergic highly selective, but not specific, for muscarinic receptors. Causes reversible blockade of cholinomimetic actions.

A

Atropine/hyoscyamine

67
Q

CNS effects of atropine

A

Overall –> stimulant
Stimulates medullar centers
Depresses vestibular excitation
Blocks basal ganglia cholinergic overactivity

68
Q

CVS effects of atropine

A

Tachycardia –> blocks M2 in SA node
Increases conduction rate in AV node

69
Q

Ocular effects of atropine

A

Mydriasis
Cycloplegia and abolition of light reflex
Photophobia and blurring of near vision
IOP rises
Dry eye
Anesthetic action on cornea (local)

70
Q

Respiratory effects of atropine

A

Bronchodilation and reduction in airway resistance
Antagonizes vagal mediated overactivity due to histamines, leukotrienes, etc.

71
Q

Urinary effects of atropine

A

Relaxation of ureter and bladder –> urine retention in BPH

Increase bladder capacity and controls detrusor hyperreflexia –> neurogenic bladder

72
Q

Visceral smooth muscle effects of atropine

A

Relaxation
Constipation
Relief of GIT spasms

73
Q

Effect of atropine on glands

A

Decreases salivary, sweat, tracheobronchial, and lacrimal secretions

Decreases acid, pepsin, and mucus secretions in stomach

74
Q

Effect of atropine on temperature and mechanism

A

Increases
Decreased sweating and stimulation of temp regulating center in hypothalamus

75
Q

First-line therapy for symptomatic bradycardia in the absence of reversible causes

A

Atropine

76
Q

Drug used to block muscarinic effects of neostigmine used in myasthenia gravis, decurarization, and cobra envenomation

A

Atropine

77
Q

Contraindications of anticholinergic use

A

Narrow angle glaucoma –> precipitates angle closure

BPH –> urinary retention

78
Q

Symptoms of belladonna poisoning

A

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
Q

Diagnosis of belladonna poisoning

A

SubQ methacholine 5 mg or neostigmine 1 mg

80
Q

Treatment of belladonna poisoning

A

Gastric lavage with tannic acid
Symptom management
Physostigmine
Other supportive measures

81
Q

Signs and symptoms of organophosphate poisoning

A

Tearing, drooling, incontinence
Fall in BP
Tachycardia or bradycardia
Muscular fasciculations and weakness
Respiratory paralysis
Excitement, tremor, convulsions, and coma

82
Q

Treatment of organophosphate poisnoning

A

Gastric lavage
Supportive measures –> airway, BP, fluid, electrolytes
Atropine –> specific antidote
Cholinesterase reactivators –> oximes

83
Q

Dosing of atropine antidote in organophosphate poisoning

A

2 mg IV every 10 minutes until dry mouth or atropinization
Maximum of 200 mg/day

84
Q

Oximes

A

Pralidoxime
Obidoxime

85
Q

Mechanism of oximes

A

Provides OH group to free AchE esteratic site –> reactivates phosphorylated enzymes

86
Q

When are oximes not effective

A

Carbamate poisoning

87
Q

Selective ganglion agonists (Nn)

A

Nicotine - small doses
Varenicline

88
Q

Non-selective ganglion agonists (Nn)

A

Ach
Carbachol
Pilocarpine
Anticholinesterases

89
Q

Competitive ganglion blockers (Nn)

A

Hexamethonium
Mecamylamine

90
Q

Persistent ganglion depolarizers with blocking action (Nn)

A

Nicotine - large doses
Anticholinesterases - larger doses

91
Q

Effects of ganglion blockers (Nn) on CVS

A

Tachycardia
Vasodilation
Hypotension
Decreased venous return and CO

92
Q

Adverse effects of nicotine replacements used in treatment of nicotine dependence

A

HA
Dyspepsia
Abdominal cramps
Loose motion

93
Q

Partial agonist of alpha-4 beta-2 nicotinic receptors that reduces nicotine cravings and withdrawal symptoms

A

Varenicline

94
Q

Adverse effects of varenicline

A

Mood changes
Irrational behavior
Sleep disorder
Agitation
Suicidal thoughts

95
Q

Treatment options for nicotine dependence

A

Counseling
Nicotine replacement
Varenicline
Bupropion

96
Q

Adverse effects of PDE5 inhibitors

A

HA
Flushing
Nasal congestion
Visual disturbance – blue-green tinge

97
Q

Interactions of PDE5 inhibitors

A

Do not use with nitrites –> profound hypotension and reflex tachycardia

Reduced initial dose with CYP3A4 inhibitors

98
Q

Drug used for treating pulmonary arterial HTN. Sensitizes sGC to NO and directly stimulates sGC without NO to increase IC levels of cGMP.

A

Riociguat

99
Q

Drug interaction of riociguat

A

Do not use with phosphodiesterase inhibitors –> hypotension

100
Q
A

Cardiovascular II (29 decks)

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