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Cardiopulm Exam 1 > Cholinergic Drugs > Flashcards

Cholinergic Drugs Flashcards

1
Q

Individual direct-acting agents:

Approved for intraocular use during surgery and causes miosis (reduction in pupil size)

A

Acetylcholine

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2
Q

Individual direct-acting agents:

  • Selective mAChR agonist that primarily affects the urinary and GU tracts
  • Can be used to treat patients with urinary retention and heartburn
  • Little cardiovascular stimulation
  • May produce urinary tract infection if sphincter fails to relax
A

Bethanechol

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3
Q

Individual direct-acting agents:

•Nonspecific cholinergic agonist that is used for the treatment of glaucoma or to produce miosis during surgery or ophthalmic examination

A

Carbachol

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4
Q

Individual direct-acting agents:

•Oral tablet used to treat dry mouth (xerostomia) in patients with Sjögren syndrome

A

Cevimeline

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5
Q

Individual direct-acting agents:

  • Approved for xerostomia treatment in patients with Sjögren syndrome or head and neck cancer treatment related xerostomia (PO), miosis during ophthalmic procedures (topical), and for glaucoma (topical)
  • Pure mAChR agonist
A

Pilocarpine

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6
Q
  • FDA approved for smoking cessation ***
  • Partial agonist that binds with high affinity and selectivity to α4β2 nAChRs (NN)
  • MOA: stimulation and subsequent moderate, sustained release of mesolimbic dopamine are thought to reduce craving and withdrawal symptoms associated with smoking cessation
A

Varenicline (Chantix)

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7
Q

What are some adverse effects to Varenicline (Chantix)?

A
  • Nausea is most common adverse effect;
  • serious adverse effects include neuropsychiatric symptoms, including changes in behavior, agitation, depressed mood, suicidal ideation, and attempted and completed suicide
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8
Q

Anticholinergic agents:

Drugs used for motion sickness

A

Scopolamine

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9
Q

Anticholinergic agents:

Drugs for gastrointestinal disorders

A
  • Atropine
  • Dicyclomine
  • Glycopyrrolate
  • Hyoscyamine
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10
Q

Anticholinergic agents:

Drugs used in ophthalmology

A
  • Atropine
  • Cyclopentolate
  • Homatropine
  • Scopolamine
  • Tropicamide
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11
Q

Anticholinergic agents:

Drugs used for respiratory disorders

A
  • Ipratropium

* Tiotropium

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12
Q

Anticholinergic agents:

Drugs used for urinary disorders

A
  • Darifenacin
  • Oxybutynin
  • Solifenacin
  • Tolterodine
  • Trospium
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13
Q

Anticholinergic agents:

Drugs used for cholinergic poisoning

A

Atropine (+ pralidoxime)

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14
Q

Anticholinergic agents:

Drugs used for movement disorders

A
  • Benztropine
  • Biperiden
  • Orphenadrine
  • Procyclidine
  • Trihexyphenidyl
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15
Q

Anticholinergics for CNS disorders:

What drugs are used for Parkinson disease?

A
  • mAChR antagonists can reduce tremors
  • Not as effective as standard dopaminergic therapy (often used in combination)
  • Tertiary amines benztropine, trihexyphenidyl, and procyclidine
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16
Q

Anticholinergics for CNS disorders:

What drugs are used for motion sickness?

A

Scopolamine – PO, injection, transdermal

17
Q

Anticholinergics for CNS disorders:

What drugs are used for anesthesia?

A
  • Atropine is given to block responses to vagal reflexes induced by surgical manipulation of visceral organs
  • Atropine or glycopyrrolate is paired with the cholinesterase inhibitor neostigmine to block its parasympathetic effects
18
Q

List of Direct-acting cholinomimetics

A
  • Acetylcholine
  • Bethanechol
  • Carbachol
  • Cevimeline
  • Methacholine
  • Pilocarpine
  • Varenicline (Chantix)
19
Q

List of Cholinesterase inhibitors

A
  • Ambenonium
  • Donepezil
  • Echothiophate
  • Edrophonium
  • Galantamine
  • Neostigmine
  • Physostigmine
  • Pyridostigmine
  • Rivastigmine
  • Tacrine
20
Q

List of Cholinesterase regenerator

A

Pralidoxime

21
Q

List of Ganglion blockers

A

Mecamylamine

22
Q

ACh Receptors: M1

  • Location
  • Structural features
  • Mechanism
A
  • Location: Nerves
  • Structural features: GPCR, Gq/11
  • Mechanism: IP3, DAG cascade
23
Q

ACh Receptors: M2

  • Location
  • Structural features
  • Mechanism
A
  • Location: Heart, nerves, smooth muscle
  • Structural features: GPCR, Gi/o
  • Mechanism: Inhibition of cAMP production, activation of K+ channels
24
Q

ACh Receptors: M3

  • Location
  • Structural features
  • Mechanism
A
  • Location: Glands, smooth muscle, endothelium
  • Structural features: GPCR, Gq/11
  • Mechanism: IP3, DAG cascade
25
Q

ACh Receptors: M4

  • Location
  • Structural features
  • Mechanism
A
  • Location: CNS
  • Structural features: GPCR, Gi/o
  • Mechanism: Inhibition of cAMP production
26
Q

ACh Receptors: M5

  • Location
  • Structural features
  • Mechanism
A
  • Location: CNS
  • Structural features: GPCR, Gq/11
  • Mechanism: IP3, DAG cascade
27
Q

ACh Receptors: Nm

  • Location
  • Structural features
  • Mechanism
A
  • Location: Skeletal muscle neuromuscular junction
  • Structural features: Pentamer, α2β8 and y/ε
  • Mechanism: Na+, K+ depolarizing ion channel
28
Q

ACh Receptors: Nn

  • Location
  • Structural features
  • Mechanism
A
  • Location: Postganglionic cell body, dendrites, CNS
  • Structural features: α and β only. Examples: (α4)2(β4)3; (α7)5
  • Mechanism: Na+, K+ depolarizing ion channel
29
Q
  • Approved for intraocular use during surgery and causes miosis (reduction in pupil size)
  • Rarely given systemically
A

Acetylcholine

30
Q
  • Administered by inhalation for the diagnosis of bronchial airway hyperreactivity in patients
    who do not have clinically apparent asthma
  • Rarely used due to need for emergency resuscitation equipment, oxygen, and medications
    to treat severe bronchospasm (e.g., B2 adrenergic receptor agonists)
A

Methacholine

31
Q
  • Can be used to treat patients with urinary retention and heartburn
  • Selective mAChR agonist
  • Little cardiovascular stimulation
  • May produce urinary tract infection if sphincter fails to relax
A

Bethanechol

32
Q

Nonspecific cholinergic agonist that is used for the treatment of glaucoma or to produce mitosis during surgery or ophthalmic examination

A

Carbachol

33
Q
  • Oral tablet used to treat dry mouth (xerostomia) in patients with Sjögren’s syndrome
  • Metabolized via P450 pathways and eliminated in urine
A

Cevimeline

34
Q
  • Approved for xerostomia treatment in patients with Sjögren’s syndrome or head and neck cancer treatment related xerostomia (PO), miosis during ophthalmic procedures (topical), and for glaucoma (topical)
  • Pure mAChR agonist
A

Pilocarpine

35
Q
  • FDA approved for smoking cessation
  • Partial agonist that binds with high affinity and selectivity to α4β2 nicotinic acetylcholine
    receptors located in the brain to stimulate receptor-mediated activity, but at a substantially lower level than nicotine
  • Stimulation and subsequent moderate, sustained release of mesolimbic dopamine are
    thought to reduce craving and withdrawal symptoms associated with smoking cessation (reward pathway)
  • Greater than 90% eliminated in urine as unchanged drug
  • Nausea is most common adverse effect; serious adverse effects include neuropsychiatric
    symptoms, including changes in behavior, agitation, depressed mood, suicidal ideation, and attempted and completed suicide
  • Treatment comes with the following warning: If patients, their families, or caregivers notice agitation, depressed mood, or changes in behavior that are not typical for the patient or if the patient has suicidal thoughts or actions, the patient should stop taking it and contact their healthcare professional.
A

Varenicline

Cardiopulm Exam 1 (13 decks)

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