Cholinergic agonists and antagonists Flashcards

1
Q

choline esters

A

Direct-acting cholinergic agonists

  1. acetylcholine
  2. methacholine
  3. carbachol
  4. bethanechol
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2
Q

cholinomimetic alkaloids

A

Direct-acting cholinergic agonists

  1. muscarine
  2. pilocarpine
  3. nicotine
  4. lobeline
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3
Q

clinical uses of direct acting cholinergic agonists

A

Diseases of eye: glaucoma, accommodative esotropia
GI/GU disorders: postoperative ileus, congenital megacolon, urinary retention, esophageal reflux, xerostomia, Sjogren syndrome

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4
Q

acetylcholine indication

A

Intraocular use during surgery, causes miosis

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5
Q

bethanechol indications

A

Selective mAChR, primarily affects urinary and GI tracts
Used to treat urinary retention and heartburn
AE: UTIs if sphincter fails to relax

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6
Q

carbachol indications

A

Treatment for glaucoma, used to produce miosis during surgery or opthalmic exam

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7
Q

cevimeline indication

A

Treatment for xerostomia in Sjogren syndrome

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8
Q

methacholine

A

Selective and potent mAChR agonist for treatment of bronchiole airway hyperreactivity

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9
Q

pilocarpine

A

Pure mAChR agonist, treatment for xerostomia in Sjogren syndrome, miosis during opthalmic procedures, and glaucoma

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10
Q

varenicline

A

Partial nAChR agonist, high affinity and selectivity for a4b2 nAChRs (Nn)
Used for smoking cessation
AE: suicidal ideation

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11
Q

direct-acting muscarinic cholinergic agonist contraindications

A

Asthma, hyperthyroidism, coronary insufficiency, acid peptic disease

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12
Q

AChE inhibitor toxicity

A

SLUDGE, NMJ effects (muscle fasciculations followed by paralysis)
Treatment: atropine (muscarinic antagonist), pralidoxime (cholinesterase regernerator)

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13
Q

antimuscarinic for motion sickness

A

Scopolamine

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14
Q

antimuscarinics for respiratory disorders

A

Ipratropium

Tiotropium

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15
Q

antimuscarinics for GI disorders

A

Atropine
Dicycloamine
Glycopyrrolate
Hyoscyamine

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16
Q

antimuscarinics for movement disorders (uncharged to penetrate CNS)

A
Benztropine
Biperiden
Orphenadrine
Procyclidine
Trihexyphenidyl
17
Q

antimuscarinics in opthamology

A
Atropine
Cyclopentolate
Homatropine
Scopolamine
Tropicamide
18
Q

antimuscarinics for urinary disorders

A
Darifenacin
Oxybutynin
Solifenacin
Tolterodine
Trospium
19
Q

antimuscarinic for cholinergic poisoning

A

atropine (+ pralidoxime)