Cholinergic Pharmacology I Flashcards

1
Q

Types of cholinoceptor stimulants (2)

A

Direct-acting cholinomimetics

Indirect-acting cholinomimetics

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2
Q

Types of direct-acting cholinomimetic agonists (2)

A

Muscarinic and nicotinic

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3
Q

Types of muscarinic cholinoceptor agonists (2)

A

Choline esters and alkaloids

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4
Q

Types of nicotinic cholinoceptor agonists (1)

A

Alkaloids

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5
Q

Choline esters (4)

A

Acetylcholine
Methacholine
Carbachol
Bethanechol

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6
Q
Acetylcholine muscarinic effects:
Cardiovascular
Respiratory
Excretion
Urination
Eye
A

Cardio- low doses causes hypotension and reflex tachycardia
Respiratory- bronchial secretion and constriction
Excretion- salivation, lacrimation, sweating
Urination- bladder contraction
Eyes- short-lasting miosis

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7
Q

Acetylcholine nicotinic effects

A

Not commonly seen

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8
Q

Clinical use of acetylcholine (2)

A

Eye surgery- miosis

Provocation test in coronary angiography (Dx of coronary vasospasm)

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9
Q

Methacholine (provocholine) clinical use

A

Diagnosis of bronchiolar hypersensitivity/asthma through excessive bronchoconstriction via M3 receptors

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10
Q

Carbachol clinical use

A

Glaucoma: contracts ciliary muscle

Enlarges canal of schlemm, increases drainage, and decreases intraocular pressure

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11
Q

Bethanechol (urecholine) clinical use:

GI and GU

A

Genitourinary: increase detrusor tone, decrease outlet resistance of internal sphincter
Gastrointestinal: increase motility & secretion

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12
Q

Bethanechol acts primarily on which receptor

A

Acts on M3, weak M2 response

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13
Q

Bethanechol indications (3)

A
  1. Gastric atony after vagotomy to reduce reflux (increases lower esophageal sphincter tone);
  2. Gastric emptying abnormalities
  3. Urinary retention (in the absence of obstruction)
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14
Q

Type of muscarinic alkaloids (2)

A

Muscarine

Pilocarpine

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15
Q

Muscarine acts on which receptors? Why does it have longer duration of action than ACh?

A

Muscarine causes excessive activation of all muscarinic receptors (M1, M2, and M3)
Longer duration because it is not a choline ester so it is not broken down by AChE

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16
Q
Symptoms of muscarine poisoning
Excretion
GI
Respiratory
Vision
A

Excretion: salivation, sweating, lacrimation
GI: Abdominal pain, nausea, diarrhea
Respiratory: Dyspnea (due to constriction and secretion)
Vision: blurred vision due to M3 activation

17
Q

Pilocarpine (isoptocarpine, salagen) has predominant effects where?

A

Opthalmic M3 effects

18
Q

Clinical Uses for pilocarpine (2)

A

Glaucoma: Rx of choice because it works on wide and narrow-angle glaucoma
Test on autonomic state (e.g., pilocarpine hypersensitivity –> PANS dysfunction)

19
Q

Contraindications for direct-acting cholinoceptor agonists (3)

A

Peptic ulcers
GI tract disorders
Asthma

20
Q

What two types of drugs should not be used with muscarinic agonists?

A
  1. Antiarrhythmics

2. Tricyclic antidepressants

21
Q

What are the two nicotinic direct-acting agonists?

A
  1. Nicotine

2. Succinylcholine

22
Q

Nicotine Action on NM subtype receptors (3)

A

skeletal muscle contraction
fasciculations, spasm
depolarizing blockade

23
Q
Nicotine Action on NN subtype nicotinic receptors
Cardiac
Vascular
GI
Carotid bodies
Medullary emetic chemoreceptors
A
  1. Stimulate sympathetic & parasympathetic post-ganglionic neurons:
    Cardiac: increased heart rate (sympathetic > parasympathetic)
    Vascular: mostly sympathetic innervation -> peripheral vasoconstriction
    GI: increased gut motility & secretion
    Carotid bodies: increased respiratory rate
    Medullary emetic chemoreceptors: nausea & vomiting
24
Q

Indirect-acting cholinoceptor agonists- reversible (6)

A
  1. Edrophonium
  2. Neostigmine
  3. Pyridostigmine
  4. Physostigmine
  5. Donepezil
  6. Tacrine
25
Q

Edrophnium clinical use

A

Dx – myasthenia; used to differentiate myasthenia from cholinergic crisis

26
Q

Neostigmine and pyridostigmine

A

Rx – ileus, urinary retention, myasthenia, reversal of non-depolarizing NM blockers

27
Q

Physostigmine

A

Rx- antidote in atropine overdose; glaucoma

28
Q

Donepezil and tacrine

A

Rx- Alzheimers

29
Q

Treatment options for cholinesterase inhibitors (2)

A

Atropine and palidoxime (2-pam)

30
Q

DUMBBELS

A
D-Diarrhea
U- Urination
M- Miosis
B- Bronchiolar constriction
B- Bradycardia
E- Excitement/Emesis
L- Lacrimation
S- Sweating
S- Salivation