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CPR > Cholinergic Drugs > Flashcards

Cholinergic Drugs Flashcards

1
Q

Biperiden

A

a. Antimuscarinic drug

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2
Q

Carbachol

A

a. Direct-acting cholinomimetics
b. treats glaucoma; produce miosis during surgery
c. both nACh and mACh agonist

carACHOL glauCOMA - alcohol puts you in a comma

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3
Q

What are common compounds with anticholinergic properties?

A

anticholinergic agents (atropine), antihistamines, tricyclic antidepressants, sleep aids, cold preparations

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4
Q

Solifenancin

A

a. mAChR (M3) antagonist

b. used to treat GU excess problems with longer acting ability, and less side effects (dry mouth and constipation)

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5
Q

What do quaternary AChE inhibitors act on? organophosphates and tertiary AChE inhibitors?

A

a. mainly skeletal muscle (no CNS activity, and less effect at autonomic effects sites and ganglia)
b. ubiquitous effects at both peripheral and central cholinergic sites,

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6
Q

Tolterodine

A

a. mAChR (M3) antagonist

b. used to treat GU excess problems with longer acting ability, and less side effects (dry mouth and constipation)

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7
Q

Endrophonium

A

a. Cholinesterase inhibitor (1)

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8
Q

Pilocarpine

A

a. Direct-acting cholinomimetics
b. treats dry mouth; can also treat glaucoma
c. pure mAChR agonist

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9
Q

Neostigmine

A

a. Cholinesterase inhibitor (2)

b. used to treat MG; NAChR agonist; charged, and doesn’t go to the CNS

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10
Q

What do we see in children that are given a normal dose atropine?

A

“atropine fever” (body temperature is elevated only if large doses are administered in adults)

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11
Q

Trihexyphenidyl

A

a. Antimuscarinic drug

b. treat PD tremor

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12
Q

What is miosis?

A

pupil constriction

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13
Q

What drugs are choline esters?

A

a. acetylcholine, bethanechol, carbachol, methacholine
b. CHARGED
c. hydrolyzed by AChE (a>m>b=c)

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14
Q

Drugs used for respiratory disorders (asthma, COPD)

A
  • Ipratropium (first line tx for asthma/COPD)

- Tiotropium (longer bronchodilator action than ipratropium)

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15
Q

What do we see with ODs of pilocarpine and choline esters?

A

predictable muscarinic effects (nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation, bronchial constriction) and are blocked by antimuscarinic compounds such as atropine

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16
Q

Trospium

A

a. Antimuscarinic drug (non selective)

b. used to treat GU excess problems

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17
Q

How do you treat Direct-acting cholinomimetic toxicity?

A

treat toxicity with atropine or anticonvulsants (diazepam or benzodiazepine)

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18
Q

Pralidoxime

A

a. cholinesterase regenerator
b. antidote for organophosphate warfare
c. regenerates active enzyme from the organophosphorus-cholinesterase complex via removal of the phosphorous group from the active site of the enzyme

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19
Q

What drugs are alkaloids?

A

a. muscarine, nicotine, pilocarpine
b. uncharged (except muscarine)
c. muscarine is highly toxic when ingested (mushrooms) and enters the brain

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20
Q

Pyridostigmine

A

a. Cholinesterase inhibitor (2)

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21
Q

How do Direct-acting cholinomimetic work?

A

they mimic ACh - bind to mAChR and nAChRs

a. Choline Esters -

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22
Q

Galantamine

A

a.

b. treat AD

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23
Q

Oxybutynin

A

a.

b. used to treat GU excess problems

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24
Q

What M R do you select to treat urinary problems?

A

M3

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25
Q

Ambenonium

A

a. Cholinesterase inhibitor

26
Q

Benzotropine

A

a. Antimuscarinic drug

b. tertiary amine; tx PD tremor

27
Q

Physostigmine

A

a. Cholinesterase inhibitor (2)

b. treat AD; antidote to anticholinergic agents OD (crosses BBB); uncharged, and goes into CNS

28
Q

Procyclidine

A

a. Antimuscarinic drug

29
Q

Darifenancin

A

a. mAChR (M3) antagonist

b. used to treat GU excess problems with longer acting ability, and less side effects (dry mouth and constipation

30
Q

Drugs used in ophthalmology

A
  • Atropine
  • Cyclopentolate
  • Homatropine
  • Scopolamine
  • Tropicamide
31
Q

Antimuscarinic agents are contraindicated in what patients?

A

glaucoma, acid peptic dx

*used with caution in men with hx of prostatic hyperplasia (bc of urinary retention)

32
Q

Varenicline

A

a. Direct-acting cholinomimetics
b. helps with smoking cessation
c. nACH agonist (partial); binds Rs in brain to stimulate receptor-mediated activity, but at a substantially lower level than nicotine
d. aka Chantix

33
Q

Dicyclomine

A

a. Antimuscarinic drug

34
Q

What are the three subgroups of AChE inhibitors?

A

a. alcohols: short acting - 2-10 min; + charged
b. carbonic acid esters (long acting - .5-6 hours); + charged or neutral
c. organophosphates (irreversible); neutral

35
Q

Orphenadrine

A

a. Antimuscarinic drug

36
Q

Of the subgroups of AChE inhibitors, which can cause CNS problems?

A

organophosphates, and some carbonic esters

  • others have no CNS distribution
37
Q

Ipratropium

A

a. Antimuscarinic drug

b. inhalation agent to tx asthma and COPD (only used for this)

38
Q

What are neostigmine and edrophonium preferred for?

A

to reverse paralysis induced by neuromuscular blocking drugs during surgery

*AChE Inhibitors

39
Q

Methacholine

A

a. Direct-acting cholinomimetics
b. causes bronchial hyperactivity, and is used in asthma testing (would exacerbate symptoms)
c. no nACh activity

40
Q

Atropine

A

a. Antimuscarinic drug
b. antidote for organophosphate warfare; tertiary amine; causes mydriasis and decrease lacrimal secretion; most sensitive tissues are salivary, bronchial, and sweat glands
c. Atropine or glycopyrrolate is paired with neostigmine to block parasympathetic effects during reversal of skeletal muscle relaxation

41
Q

What is the MOA of ganglion blockers?

A

competitively block the action of ACh and similar agonists at nAChRs of both parasympathetic and sympathetic autonomic ganglia (block all autonomic outflow)

*Urination hesitancy and possible urinary retention in men with prostatic hyperplasia;
Erection and ejaculation may be prevented

42
Q

Acetycholine

A

a. Direct-acting cholinomimetics

b. causes mitosis

43
Q

Mecamylaine

A

a. ganglion blocker (uncharged)

b. treat hypertension and is being investigated for use in smoking cessation therapy

44
Q

Cevimeline

A

a. Direct-acting cholinomimetics
b. treats dry mouth
c. Metabolized via P450 pathways and eliminated in urine

45
Q

Homatropine

A

a. mAChR antagonist

b. used to prevent synechia formation in uveitis and iritis

46
Q

Bethanechol

A

a. Direct-acting cholinomimetics
b. treats non-obstructive GU/GI problems; heartburn
c. can produce UTI if sphincter doesn’t relax

47
Q

Can an uncharged or charged drug enter the CNS?

A

uncharged

48
Q

What happens when succinylcholine is given with an AChE inhibitor? corticosteroids with AChE inhibitor?

A

a. enhance phase 1 block and antagonize phase 2 block

b. may enhance muscle weakness seen in patients with myasthenia gravis

49
Q

Pyridostigmine

A

a. Cholinesterase inhibitor (2)

b. pretreatment with pyridostigmine reduces the incapacitation and mortality associated with nerve agent poisoning

50
Q

What types of parasympathetic receptors does the brain contain? SC?

A

a. mAChRs mainly

b. nAChRs mainly

51
Q

Scopolamine

A

a. Antimuscarinic drug
b. tx motion sickness
c. has marked CNS effects (drowsiness and amnesia)

52
Q

Oxybutynin

A

a. mAChR (M3) antagonist

b. used to treat GU excess problems

53
Q

How do the parasympathetics innervate the smooth muscle of BVs?

A

they don’t –> they release EDFR, which is largely NO –> activation of guanylyl cyclase and increased cGMP –> relaxation

54
Q

Donepezil

A

a. Cholinesterase inhibitor

b. treat AD

55
Q

Tacrine

A

a. Cholinesterase inhibitor

b. used to treat AD, but not anymore

56
Q

What are contraindications for Direct-acting cholinomimetics?

A

acid peptic disease, asthma, hyperthyroidism, coronary insufficiency

57
Q

Pralidoxime

A

a. cholinesterase regenerator

b. antidote for organophosphate warfare

58
Q

What organophosphate does NOT get to the CNS?

A

echothiophate - due to its charge

59
Q

Hyoscyamine

A

a. Cholinesterase inhibitor

60
Q

What do we see with nicotinic poisoning?

A

a. acute - effects include CNS stimulation (convulsions progressing to coma and respiratory arrest), skeletal muscle end plate depolarization leading to depolarization blockade and respiratory paralysis, and hypertension and cardiac arrhythmias
b. chronic - increased risk of vascular disease, sudden coronary death, and ulcer recurrences in smokers with peptic ulcer

61
Q

Glycopyrrolate

A

a. cholinergic antagonist

b. helps reverse paralysis with neostigmine, helps GI problems

CPR (22 decks)

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