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CVS II Pharmacology > ACh Agonists/Antagonists > Flashcards

ACh Agonists/Antagonists Flashcards

1
Q

where does Botulinum toxin bind

A

presynaptically to cholinergic nerve terminals

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2
Q

what is the MOA of BoNT

A

cleaves SNAP and VAMP to decrease Ach release

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3
Q

what are the uses of BoNT

A

cosmetic, muscle spasms, dystonia and spasticity

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4
Q

what splits Ach into Choline

A

Acetylcholinesterase (AChE) and butyrylcholinesterase (pseudo cholinesterase)

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5
Q

What’s the difference between true vs. pseudo AChE

A

True: very fast, works @ all cholinergic sites, more sensitive to physostigmine
Pseudo: slower, works primarily in plasma, more sensitive to organophosphates

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6
Q

What is the route of elimination for Atracurium

A

plasma esterase

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7
Q

What is the route of elimination for Cisatracurium

A

Spontaneous chemical degredation-Laudanosine (Hofmann elimination)

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8
Q

What is the route of elimination for pancuronium

A

renal excretion

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9
Q

What is the route of elimination for Rocuronium

A

Biliary and renal excretion

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10
Q

What is the route of elimination for Vecuronium

A

Biliary and renal excretion; hepatic metabolism

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11
Q

What is the route of elimination for succinylcholine (depolarizing)

A

Plasma butyryl (pseudo cholinesterase)

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12
Q

What is the suffix for the majority of Nm blockers

A

“curium” or “curonium” (exception succinylcholine)

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13
Q

name a Nm blocker with the shortest duration of action

A

Succinylcholine

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14
Q

one side effect of succinylcholine is hyper/hypokalemia

A

hyperkalemia via efflux from muscles

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15
Q

What are the major side effects of succinylcholine

A

prolonged apnea, hyperkalemia, postoperative myalgia, malignant hyperthermia

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16
Q

What drug blocks muscarinic receptors

A

Atropine

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17
Q

What are Ach actions on the heart (M2)

A

SA node hyperpolarization, reduced force of contraction

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18
Q

What are Ach actions on the blood vessels (M3)

A

Penile erection, otherwise limited to skin of face and neck (vasodilation)

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19
Q

What are Ach actions on smooth muscle (M3)

A

Contraction of all SM; i.e. voiding of bladder, diarrhea, etc.; can induce asthma attack

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20
Q

What are Ach actions on the glands (M3)

A

Increased secretions

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21
Q

What are Ach actions on the eye (M3)

A

miosis (constriction); increased outflow and reduced IOP

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22
Q

What side effects can you expect in a patient taking a cholinergic drug

A

SLUDGE MOBBB
salivation, lacrimation, Urination, defecation, gastrointestinal distress, emesis, bradycardia, bronchorrhea, bronchospasm

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23
Q

What is the MOA of bethanechol and what are its clinical uses

A

muscarinic agonist; ileus, urinary retention

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24
Q

______ is used as a broncho provocative test

A

methacholine (muscarinic agonist)

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25
Q

cevimeline is used to treat ________

A

xerostomia

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26
Q

xerostomia can be treated with the muscarinic agonist, __________

A

cevimeline

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27
Q

what muscarinic agonist is used to treat glaucoma

A

pilocarpine

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28
Q

What is the MOA of pilocarpine

A

opens iridocorneal angle to treat glaucoma

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29
Q

what are the three synthetic reversible anticholinesterases that work on skeletal muscles

A

neostigmine, pyridostigmine, edrophonium

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30
Q

What two synthetic reversible anticholinesterases target the CNS

A

Donepezil and rivastigmine

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31
Q

what is the only naturally occurring reversible anticholinesterase?

A

Physostigmine

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32
Q

What are the common names for the irreversible anticholinesterases

A

tear gas and insecticides

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33
Q

what type of bond do reversible anticholinesterases form with AchE

A

ionic (weaker)

34
Q

what is the MOA of anticholinesterases

A

inhibition of the hydrolyses of acetylcholine to acetic acid and choline

35
Q

what type of bond do irreversible anticholinesterases form with AchE

A

covalent bond at esteric site

36
Q

How does the MOA differ between carbamates and phosphates as it relates to irreversible anti-AchE

A

carbamates react with water quicker than phosphates, making them incapable of aging

37
Q

What does aging mean as it relates to phosphates (anti-AchE)

A

resistant to hydrolysis due to the stability caused by the loss of alkyl group(s)

38
Q

physostigmine/neostigmine has good oral absorption

A

physostigmine

39
Q

physostigmine/neostigmine can cross the BBB

A

physostigmine (tertiary amine vs neostigmine being quaternary)

40
Q

neostigmine can be used to treat eyes/myasthenia gravis?

A

myasthenia gravis. it cant cross BBB

41
Q

neostigmine and (synthetic/natural) whereas physostigmine is (synthetic/natural)

A

synthetic; natural

42
Q

what drug is used to Dx myasthenia AKA “tensilon test”

A

Edrophonium (this is used because in pts w MG, when you inject it you’ll see improvement in muscle contraction

43
Q

what is the antidote used in atropine overdose

A

physostigmine

44
Q

what drugs can be used to reverse nondepolarizing NM blockers

A

Neostigmine, pyridostigmine

45
Q

what two anti-AchE drugs are used to treat alzheimers

A

donepezil and rivastigmine

46
Q

What is the treatment for OPC poisoning

A

Atropine, gastric lavage, airway maintenance/BP/fluid and electrolytes, cholinesterase reactivators (oximes)

47
Q

what is the MOA of cholinesterase Reactivators (oximes)

A

provide reactive group of OH to the enzymes

48
Q

Are oximes effective in carbamate poisoning?

49
Q

At what point are cholinesterase reactivators not effective for OPC poisoning?

A

once aging has set it (about 30 min)

50
Q

what type of drugs are carbaryl and propoxur

A

carbamates

51
Q

whats another name for carbaryl and propoxur

A

baygon (carbamates)

52
Q

what type of drugs are echothiophate, parathion and malathion

A

organophosphorus compounds (OPC)

53
Q

The drugs, tabun, sarin, and soman are otherwise known as _____

54
Q

what receptors do anticholinergic drugs target?

A

muscarinic (M1-5) and nicotinic (NN and NM)

55
Q

nicotinic NN antagonists are otherwise known as

A

ganglion blockers

56
Q

NM blockers are otherwise known as

A

neuromuscular blockers

57
Q

what is the clinical use of the antiAch drug atropine

A

antispasmodic, antisecretory, OPC poison antidote, mushroom poisoning, antidiarrheal

58
Q

what is the clinical use of the antiAch drug scopolamine

A

motion sickness (given as patch), causes sedation

59
Q

what is the clinical use of the antiAch drug Ipratropium and Tiotropium

A

Asthma and COPD (inhalational)

60
Q

what is the clinical use of the antiAch drug Tropicamide

A

Eye (topical) mydriatic (short-acting– most widely used at the eye doctor)

61
Q

what is the clinical use of the antiAch drug benztropine and trihexyphenidyl

A

CNS (lipid-soluble), used in parkinsonism and in EPS induced by antipsychotics

62
Q

what is the clinical use of the antiAch drug oxybutynin

A

used in overactive bladder (urge incontinence)

63
Q

atropine has a long duration of action for ____

63
Q

what is the clinical use of the antiAch drugs TCA’s, phenothiazines and antihistaminics

A

significant antimuscarinic action

64
Q

can small doses of atropine be overcome by a large concentration of Ach/muscarinic agonist

65
Q

Atropine does not distinguish between M1, M2, or M3 TRUE or FALSE

66
Q

atropine can cause loss of what eye reflex?

A

accommodation

67
Q

Why is atropine hazardous in narrow angle glaucoma patients?

A

it causes a rise in IOP

68
Q

is atropine safe for COPD and asthma patients

A

yes, it is a bronchodilator

69
Q

what is the first line therapy for symptomatic bradycardia

70
Q

what are the two contraindications of atropine

A

narrow angle glaucoma and BPH

71
Q

what is the antidote for atropine poisoning (belladonna)

A

physostigmine (SC or IV)

72
Q

what are the two selective ganglion agonists/stimulants

A

nicotine and varenicline

73
Q

Ach, carbachol, pilocarpine are all examples of ganglion stimulants/blockers?

A

stimulants

74
Q

what type of drug is hexamethonium

A

competitive ganglion blocker

75
Q

what type of drug is mecamylamine

A

competitive ganglion blocker

76
Q

what are the effects of mecamylamine and hexamethonium

A

tachycardia, vasodilation, hypotension, decreased venous return and decreased CO

77
Q

what can varenicline and bupropion be used to treat

A

nicotine dependence

78
Q

what is the MOA of varenicline

A

partial agonist of alpha4 B2 nicotinic receptors

79
Q

what is the MOA of bupropion

A

inhibition of reuptake of NE and dopamine as well as a nicotinic ach antagonist

CVS II Pharmacology (9 decks)

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