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21. CPR Exam 1 > 4. DSA Cholinergic Drugs > Flashcards

4. DSA Cholinergic Drugs Flashcards

1
Q

Receptor Type: M1
Location:
GPCR:
Mechanism:

A

Receptor Type: M1
Location: Nerves
GPCR: Gq/11
Mechanism: IP3/DAG cascade

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2
Q

Receptor Type: M2
Location: Heart, nerves, smooth muscle
GPCR:
Mechanism:

A

Receptor Type: M1
Location: Heart, nerves, smooth muscle
GPCR: Gi/o
Mechanism: Inhibit cAMP, activation of K+ channels

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3
Q

Receptor Type: M3
Location: Glands, smooth muscle, endothelium
GPCR:
Mechanism:

A

Receptor Type: M3
Location: Glands, smooth muscle, endothelium
GPCR: Gq/11
Mechanism: IP3/DAG

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4
Q

Receptor Type: M4
Location: CNS
GPCR:
Mechanism:

A

Receptor Type: M4
Location: CNS
GPCR: Gi/o
Mechanism: Inhibit cAMP

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5
Q

Receptor Type: M5
Location: CNS
GPCR:
Mechanism:

A

Receptor Type: M5
Location: CNS
GPCR: Gq/11
Mechanism: IP3/DAG

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6
Q

Receptor Type: NN
Location: postganglionic cell body, dendrites, CNS
GPCR:
Mechanism:

A

Receptor Type: NN
Location: postganglionic cell body, dendrites, CNS
GPCR: a/b only
Mechanism: Na/K+ depolarizing ion channel

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7
Q

In most organs, M3 is predominant. What predominates in the heart?

A

M2

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8
Q 
List the following's receptor as M3, M2 or M3/M2...
Heart
SA/AV Nodes
Atria
Ventricle
Eye
Blood Vessels
Endothelium
Glands (lacrimal, salivary, bronchial, sweat)
Lung
GI/GU
A 
Heart
SA/AV Nodes M2
Atria M2
Ventricle M2 (dec)
Eye M3/M2
Blood Vessels None
Endothelium M3
Glands (lacrimal, salivary, bronchial, sweat) M3/M2
Lung M3/M2
GI/GU M3/M2
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9
Q

Cholinergic agonists mimic the actions of ACh on nAChRs and mAChRs, classified based on their?

A

mechanism of actions

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10
Q 
What direct acting cholinergic agonists do the following?
agonists at cholinergic receptors
permanently charged
poor absorption and distribution to CNS
Metabolized by acetylcholinesterase
A

Choline Esters

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11
Q 
All of the following are?
Acetylcholine
Metacholine
Carbachol
Bethanechol
A

Choline Esters

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12
Q

What direct acting cholinergic agonists do the following?
agonist at cholinergic receptors
uncharged tertiary amines, well absorbed
Muscarin charged but can cross the BBB and is high toxic

A

Alkaloids

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13
Q

Muscarine
Pilocarpine (both mAChR)
Nicotine / Lobeline (nAChR)

A

Alkaloids

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14
Q

There are 3 groups of AChE inhibitors which are indirect acting cholinergic agonists.

1) alcohols (reversible)
2) carbamic acid esters (reversible but longer lasting)
3) ?

A

Organophosphates - irreversible (covalent bond)

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15
Q

Charged AChE inhibitors are insoluble in lipids, do not cross the BBB and have poor PO absorption while neutral AChE inhibitors…?

A

can cross BBB and are readily absorbed- most commonly organophosphates/tertiary agents

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16
Q

Cholinergic agonists help rest and digest, leading to pupillar constrction, salivation, constriction/secretion of bronchi, voiding of urine, slowing of heart and what in the GI tract? (3)

A

Gastric secretion increased, colic, diarrhea

17
Q

What is approved for intraocular use during surgery and causes miosis (reduced pupil size)?

A

Acetylcholine

18
Q

What is a selective mAChR agonist that primarily effects the urinary and GU tracts and can be used to treat patients with urinary retention and heartburn?

A

Bethanechol

19
Q

What is a nonspecific cholinergic agonist that is used for the treatment of glaucoma or to produce miosis during surgery or opthalmic examination?

A

Carbachol

20
Q

What is an oral tablet used to treat dry mouth (xerostomia) in patients with Sjogren syndrome?

A

Cevimeline

21
Q

What is approved for xerostomia treatment in patients with sjorgren or head and neck cancer treatment related xerostomia (PO), miosis during opthalmic procedures (topical) and for glaucoma (topical)?

A

Pilocarpine (pure mAChR agonist)

22
Q

What is FDA approved for smoking cessation, which binds with high affinity and selectivity to a42b2 nAChRs (NN)? MOA = stimulation and moderate sustained release of mesolimbic dopamine, thought to reduce craving and withdrawal symptoms.

A

Varenicline (Chantix)

SE: nausea, changes behavior, agitation, depressed mood, suicide

23
Q

Toxicity of direct acting muscarinic stimulants include nausea, vomiting, diarrhea, urinary urgency, slavation, sweating. These drugs are contraidication in people with? 4

A

asthma, hyperthyroidism, coronary insufficiency, and acid-peptic dz

24
Q

Toxicity of direct acting nicotonic stimulants includes cns stimulation, skeletal muscle end plate depolarization, respiratory paralysis, hypertension and cardiac arrhythmias. How can one get nicotine poisoning?

A

cigarettes and insecticides

25
Q

Some clinical uses of indirect-acting cholinergic agonists include glaucoma, myasthenia gravis, reversal of neuromuscular paralysis, AChE inhibitor toxicity, and what other 2 things?

A

dementia

Antidote to anticholinergic poisoning

26
Q

Cholinergic antagonists increase flight or fight, including, pupillary dilation, dry mouth, accelerated heart rate, relaxation of bronchi, and what regarding bladder and GI tract?

A

retention of urine

gastric secretion reduced, constipation

27
Q

What anticholinergic agents are used for motion sickness? 1

A

Scopolamine

28
Q

What anticholinergic agents are used for GI disorders? 4

A

Atropine
Dicyclomine
Glycopyrrolate
Hyoscyamine

29
Q

What anticholinergic agents are used for opthalmology? 5

A 
atropine
cyclopentolate
homatropine
scopolamine
tropicamide
30
Q

What anticholinergic agents are used for respiratory disorders? 2

A

Ipratropium

Tiotropium

31
Q

What anticholinergic agents are used for urinary disorders? 5

A 
Darifenacin M3
Oxybutynin M3
Solifenacin M3
Tolterodine M3
Trospium
32
Q

What anticholinergic agents are used for cholinergic poisoning? 1

A

Atropine (+ pralidoxime)

33
Q

What anticholinergic agents are used for movement disorders? 5

A 
Benztropine
Biperiden
Orphenadrine
Procyclidine
Trihexyphenidyl
34
Q

What are the overall effects of anticholinergic drugs?

A

general increase in sympathetic tone

35
Q

What are 3 contraindications when prescribing anticholinergic drugs?

A

glaucoma
Prostatic hyperplasia
Acid-peptic disease

21. CPR Exam 1 (26 decks)

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