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CVS II Pharmacology > ACh Agonists/Antagonists > Flashcards

ACh Agonists/Antagonists Flashcards

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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
cevimeline is used to treat ________
xerostomia
26
xerostomia can be treated with the muscarinic agonist, __________
cevimeline
27
what muscarinic agonist is used to treat glaucoma
pilocarpine
28
What is the MOA of pilocarpine
opens iridocorneal angle to treat glaucoma
29
what are the three synthetic reversible anticholinesterases that work on skeletal muscles
neostigmine, pyridostigmine, edrophonium
30
What two synthetic reversible anticholinesterases target the CNS
Donepezil and rivastigmine
31
what is the only naturally occurring reversible anticholinesterase?
Physostigmine
32
What are the common names for the irreversible anticholinesterases
tear gas and insecticides
33
what type of bond do reversible anticholinesterases form with AchE
ionic (weaker)
34
what is the MOA of anticholinesterases
inhibition of the hydrolyses of acetylcholine to acetic acid and choline
35
what type of bond do irreversible anticholinesterases form with AchE
covalent bond at esteric site
36
How does the MOA differ between carbamates and phosphates as it relates to irreversible anti-AchE
carbamates react with water quicker than phosphates, making them incapable of aging
37
What does aging mean as it relates to phosphates (anti-AchE)
resistant to hydrolysis due to the stability caused by the loss of alkyl group(s)
38
physostigmine/neostigmine has good oral absorption
physostigmine
39
physostigmine/neostigmine can cross the BBB
physostigmine (tertiary amine vs neostigmine being quaternary)
40
neostigmine can be used to treat eyes/myasthenia gravis?
myasthenia gravis. it cant cross BBB
41
neostigmine and (synthetic/natural) whereas physostigmine is (synthetic/natural)
synthetic; natural
42
what drug is used to Dx myasthenia AKA "tensilon test"
Edrophonium (this is used because in pts w MG, when you inject it you'll see improvement in muscle contraction
43
what is the antidote used in atropine overdose
physostigmine
44
what drugs can be used to reverse nondepolarizing NM blockers
Neostigmine, pyridostigmine
45
what two anti-AchE drugs are used to treat alzheimers
donepezil and rivastigmine
46
What is the treatment for OPC poisoning
Atropine, gastric lavage, airway maintenance/BP/fluid and electrolytes, cholinesterase reactivators (oximes)
47
what is the MOA of cholinesterase Reactivators (oximes)
provide reactive group of OH to the enzymes
48
Are oximes effective in carbamate poisoning?
NO
49
At what point are cholinesterase reactivators not effective for OPC poisoning?
once aging has set it (about 30 min)
50
what type of drugs are carbaryl and propoxur
carbamates
51
whats another name for carbaryl and propoxur
baygon (carbamates)
52
what type of drugs are echothiophate, parathion and malathion
organophosphorus compounds (OPC)
53
The drugs, tabun, sarin, and soman are otherwise known as _____
tear gas
54
what receptors do anticholinergic drugs target?
muscarinic (M1-5) and nicotinic (NN and NM)
55
nicotinic NN antagonists are otherwise known as
ganglion blockers
56
NM blockers are otherwise known as
neuromuscular blockers
57
what is the clinical use of the antiAch drug atropine
antispasmodic, antisecretory, OPC poison antidote, mushroom poisoning, antidiarrheal
58
what is the clinical use of the antiAch drug scopolamine
motion sickness (given as patch), causes sedation
59
what is the clinical use of the antiAch drug Ipratropium and Tiotropium
Asthma and COPD (inhalational)
60
what is the clinical use of the antiAch drug Tropicamide
Eye (topical) mydriatic (short-acting-- most widely used at the eye doctor)
61
what is the clinical use of the antiAch drug benztropine and trihexyphenidyl
CNS (lipid-soluble), used in parkinsonism and in EPS induced by antipsychotics
62
what is the clinical use of the antiAch drug oxybutynin
used in overactive bladder (urge incontinence)
63
atropine has a long duration of action for ____
eyes
63
what is the clinical use of the antiAch drugs TCA's, phenothiazines and antihistaminics
significant antimuscarinic action
64
can small doses of atropine be overcome by a large concentration of Ach/muscarinic agonist
yes
65
Atropine does not distinguish between M1, M2, or M3 TRUE or FALSE
True
66
atropine can cause loss of what eye reflex?
accommodation
67
Why is atropine hazardous in narrow angle glaucoma patients?
it causes a rise in IOP
68
is atropine safe for COPD and asthma patients
yes, it is a bronchodilator
69
what is the first line therapy for symptomatic bradycardia
atropine
70
what are the two contraindications of atropine
narrow angle glaucoma and BPH
71
what is the antidote for atropine poisoning (belladonna)
physostigmine (SC or IV)
72
what are the two selective ganglion agonists/stimulants
nicotine and varenicline
73
Ach, carbachol, pilocarpine are all examples of ganglion stimulants/blockers?
stimulants
74
what type of drug is hexamethonium
competitive ganglion blocker
75
what type of drug is mecamylamine
competitive ganglion blocker
76
what are the effects of mecamylamine and hexamethonium
tachycardia, vasodilation, hypotension, decreased venous return and decreased CO
77
what can varenicline and bupropion be used to treat
nicotine dependence
78
what is the MOA of varenicline
partial agonist of alpha4 B2 nicotinic receptors
79
what is the MOA of bupropion
inhibition of reuptake of NE and dopamine as well as a nicotinic ach antagonist

CVS II Pharmacology (9 decks)

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