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Neuro II DF > Kruse Cholinergic Agonists and Antagonists DSA > Flashcards

Kruse Cholinergic Agonists and Antagonists DSA Flashcards

1
Q

choline esters

examples

structure and CNS

how its broken down

A

eg. acetylcholine, carbachol, bethanechol, methacholine
- contain permanently charged quarternary ammonium groups = poor CNS absorption
- hydrolized in GI tract and less active when given PO
- all hydrolyzed by cholinesterase

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2
Q

most rapid to least rapid hydrolyzation of choline esters by acetylcholinesterase

A

acetylcholine>methacoline>carbachol = bethanechol

AMC Blockbuster

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3
Q

choline esters MOA

A

agonists on cholinergic receptors

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4
Q

alkaloids

examples

strucutre and absorption

anomalies with absorption

A

muscarine, nicotine, pilocarpine

agents are uncharged tertirary amines (except muscarine) that are well absorbed from most sites of administration

(nicotine can go through skin)

-although muscarine is quaternary amine, it is higly toxic when ingested and can enter the brain

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5
Q

excretion of alkaloid cholinergic drugs

A

excreted by kidneys, acidification of urine accelerates clearance

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6
Q

MOA of alkaloids

A

act as agonists on cholinergic receptors

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7
Q

what is the primary effect of muscarinic agonists on peripheral vasculature

A

reduces resistance

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8
Q

GI and genitourinary tracts direct acting cholinergic effects

what receptors and what function of them

A

increased glandular secretions more salivary and gastric

  • M3 for contraction of smooth muscle
  • M2 reduces cAMP formation and reduces relaxation caused by adrenergic effects
  • sphincter relaxation is via NO signaling (M3 mACHRs)
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9
Q

the brain is richer in ____ ach receptors while the spinal cord contains predominantly __

A

muscarinic, nicotinic

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10
Q

excitatory mAChRs are involved in ___ while inhibitory mAChRs are involved in

A

learning and memory and seizure activity

tremors, hypothermia, and analgesia

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11
Q

nAChR causes receptor activation in _____ ___ and actions are similar in both ____

A

autonomic ganglia

symp, and parasymp ganglia

-initial response resembles simultaneous discharge of both parasymp and symp nervous systems

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12
Q

nAChR in CV system

A

nicotine is mainly sympathomimetic

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13
Q

nAChR in GI/GU

A

mainly parasympathomimetic (nausea, vomiting, diarrhea, voiding of urine)

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14
Q

clinical uses of direct acting cholinergic agonists

example of drug for one system

A

glaucoma
-musc stimulants cause contraction of cilirary body which = more outflow of aq humor and reduces intraocular pressure

accommodative esotropia in young children who are farsighted and overcompensate and eyes become crossed

GI/GU tract disorders
-postoperative ileus, atony or parlysis of stomoch or bowel after surgery, congenital megacolon, urinary retention, esophagueal reflux

  • example is bethanechol
    • as long as there is no obstruction or can cause perforation
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15
Q

what drugs are used to increase salivary secretion

A

pilocarpine and cevimeline

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16
Q

major contraindications to use mAChR agonists that are distributed systemically are

A

HACA

Hyperthyroidism
asthma
coronary insufficiency
acid-peptic disease

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17
Q

acute toxicity of nicotine

A

cns stimulation: convulsions progressing to coma and respiratory arrest

skeletal muscle end plate depolariztion leading to depol blockade and respiratory paralysis

hypertension

cardiac arrhythmias

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18
Q

treatment for acute toxicity

A

atropine for excess muscarinic stimulation from parasymp ganglia

anticonvulsants (diazepam) for CNS stimulation

19
Q

chronic nicotine toxicity

A

increased risk vascular disease

sudden coronary death

ulcer recurrences in smokers with peptic ulcer

20
Q

acetylcholine use

A

intraocular use during surgery and cuases miosis

21
Q

methacholine use

A

inhalation for diagnosis of bronchial airway hyperreactivity in pts who don’t have clinically apparent asthma

22
Q

bethanechol use

A

urinary retention and heartburn

selective mAChR

may produce UTI if sphincter fails to relax

23
Q

carbachol use

A

nonspecific cholinergic agonist used for glaucoma or to produce miosis during surgery or eye exam

24
Q

cevimeline use

A

oral tab used to treat xerostomia in pts with sjogren’s syndrome

metabolized via P450 pathway and eliminated in urine

25
Q

pilocarpine use

A

approved for xerostomia in pts with sjogren syndrome

used in head and neck cancer treatment related to xerostomia
miosis during eye procedures and for glaucoma

pure mAChR agonist

26
Q

varenicline use

A

(chantax)

FDA approved for smoking cessation

partial agonist that binds with high affinity and selectivity to a4B2 nicotinic acetylcholine receptors located in brain
-at lower level than nicotine

-stimulation and moderate sustained release of dopamine thought to reduce cravings and withdrawal symptoms

27
Q

side effects of varenicline

A

nausea is most common

serious side effects include neuropsychiatric symptoms like agitation, depression, suicidal ideation

28
Q

indirect acting cholinergic agonists
alcohols
subgroups

A

alcohols, binding is reversible, quat ammonium group, example edrophonium

carbamic acid esters, binding is reversible, quat or tert, examples are neostigmine, pyridostigmine, physostigmine, carbaryl

organophosphates

  • ecothiophate, parathion, malathion, sarin, soman, tabun
  • covalent binding to AChE and irreversible
29
Q

examples of quaternary and charged AChE inhibtiors

A

neostigmine, pyridostigmine, edrophonium, echothiophate, ambenonium

30
Q

tertirary and uncharged AChE inhibtiors

A 
physostigmine
donepezil
tacrine
rivastigmine
galantamine
31
Q

duration of action of alcohols

A

2-10 minutes

32
Q

duration of action of carbamic acid esters

A

30 minutes to 6 hours

33
Q

duration of action of organophosphates

A

hundreds of hours

34
Q

which AChE inhibitors are preferred to reverse paralyis induced by NMJ blocking drugs during anesthesia

A

neostigmine and edrophonium

35
Q

AChE inhibitor DDI: nondepolarizing NMJ blocking agents

A

give with AChE inhibitor and it diminishes block

-exception is mivacurium: metabolized by AChE, NMJ blockade is prolonged

36
Q

succinlycholine and AChE

A

ehance phase 1 blok and antagonize phase 2 block

37
Q

cholinergic agonist and AChE

A

enhance effect

38
Q

beta blockers and AChE

A

may enahnce bradycardic effects

39
Q

AChE and systemic corticosteroids

A

may enhance muscle weakness seen in pts with myasthenia gravis

40
Q

cholinesterase reactivor

A

praldoxime

41
Q

protope antimuscarinic compound is

A

atropine

42
Q

anticholinergic drugs, tertiary amines

A

atropine, tropicamide, benzotopine

43
Q

anticholinergic drugs, quat amines

A

ipratropium, glycopyrrolate

44
Q

mAChR antagonist given in parkinsons to reduce tremors, what drugs

A

benztropine and trihexyphenidyl

Neuro II DF (3 decks)

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