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Boards Prep > Cholinergics & Anticholinergics > Flashcards

Cholinergics & Anticholinergics Flashcards

1
Q

True/False. Acetylcholine is ALWAYS released by pre-ganglionic neurons.

A

True

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2
Q

What receptors are located at the neuromuscular junction?

A

Nicotinic

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3
Q

What type of receptors are located on sweat glands?

A

Muscarinic receptors stimulated by Ach released by the SANS

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4
Q

True/False. All cholinergic receptors are ligand-gated ion channels.

A

False. Nicotinic receptors are ligand-gated, with a fast excitatory response. Muscarinic receptors are G-protein receptors with a slower response and may be excitatory or inhibitory

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5
Q

What muscarinic receptor is always inhibitory? Where is it located?

A

M2 receptor on the heart

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6
Q

What muscarinic receptor is always excitatory?

A

M1 & M3

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7
Q

Where are M1 receptors found?

A

CNS, gastric glands

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8
Q

Where are M3 receptors found?

A

Bronchi, bladder, eye, GI tract, periphery

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9
Q

What is the MOA of botulinum toxin?

A

Prevents release of Acetylcholine into the synaptic cleft

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10
Q

What are the effects of PANS stimulation on the eye?

A

Accommodation of the lens for near vision, miosis (pupil constriction), decreased intraocular pressure due to outflow of aqueous humor

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11
Q

What effects are associated with PANS stimulation?

A

Increased peristalsis & secretion in the GI tract, decreased HR, bronchoconstriction, urination

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12
Q

Blood pressure decreases in response to a direct cholinergic agonist, but not an indirect agonist. Why is this?

A

Blood vessels are not innervated by the PANS, however, PANS stimulation of M3 receptors on endothelial cells leads to release of NO. This in turn causes vasodilation. Indirect agonists require AchE for effect, but none is present as the PANS does not innervate blood vessels.

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13
Q

Both muscarinic antagonists and alpha-1 agonists cause mydriasis (pupil dilation). How can you differentiate between the two?

A

Muscarinic antagonists will cause cycloplegia (paralysis of accommodation) since they bind and block M3 receptors

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14
Q

What is the difference between direct and indirect cholinergic agonists?

A

Direct agonists bind and act directly on cholinergic receptors. Indirect agonists inhibit the action of AchE, thus increasing availability of Ach

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15
Q

What are common clinical uses of direct cholinergic agonists?

A

Urinary retention, dry mouth, acute glaucoma

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16
Q

What direct muscarinic agonist is used to treat acute glaucoma?

A

Pilocarpine

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17
Q

These muscarinic agonists may be used to treat Sjogren’s Syndrome and dry mouth.

A

Pilocarpine & Cevimeline

18
Q

What is the site of action for Bethanechol?

A

Direct muscarinic agonist that acts on the GI tract & bladder

19
Q

What is the clinical use for Methacholine?

A

Diagnosis of bronchial airway hyperactivity

20
Q

Indirect cholinergic agonists are especially effective in treating what types of disorders?

A

Myasthenia gravis, muscle paralysis, Alzheimer’s disease

21
Q

Therapeutic doses of indirect cholinergic agonists can promote strength of muscle movements and cognition. What ADRs are associated with high does?

A

Muscle paralysis, disorientation, convulsions

22
Q

What indirect cholinergic agonists crosses the BBB and can treat atropine overdose?

A

Physostigmine

23
Q

What indirect cholinergic agonists are used for treatment of myasthenia gravis?

A

Neostigmine, Pyridostigmine

24
Q

What is the clinical use of Rivastigmine?

A

Indirect cholinergic agonist - treatment of Alzheimer’s disease

25
Q

What ADRs are associated with indirect cholinergic agonists?

A

Salivation, miosis (pupil constriction), bradycardia, diarrhea, muscle twitches, paralysis, convulsions

26
Q

What indirect cholinergic agonist may be used for clinical diagnosis of myasthenia gravis?

A

Edrophonium

27
Q

True/False. Organophosphates are irreversible AchE inhibitors

A

True - causes cholinergic crisis

28
Q

What drug can be administered as an antidote for cholinergic agonist overdoeses?

A

Atropine

29
Q

What drug, when administered soon after exposure to organophosphates, can regenerate AchE?

A

Pralidoxime

30
Q

What drug is used in smoking cessation and acts as a partial agonist to mediate the reward effect of nicotine on the brain?

A

Varenicline

31
Q

True/False. Anti-muscarinic drugs are administered locally to prevent unwanted side effects.

A

True - Anti-muscarinic drugs are non-selective for muscarinic receptors so they are administered locally to gain a level of selectivity

32
Q

What drug can be administered via transdermal patch to treat motion sickness?

A

Scopolamine

33
Q

What anti-muscarinic drugs are used in ophthalmic settings to induce mydriasis?

A

Cyclopentolate, tropicamide

34
Q

What is the clinical use for ipratropium?

A

Muscarinic antagonist - treat asthma & COPD

35
Q

What is the clinical use for Benztropine?

A

Treat tremors due to Parkinson’s disease

36
Q

What muscarinic antagonists can be used to treat irritable bowel syndrome?

A

Dicyclomine, hyoscyamine

37
Q

What is the clinical use for Oxybutynin?

A

Overactive bladder, urinary incontinence

38
Q

What ADRs are assoicated with muscarinic antagonists?

A

Hyperthermia, flushing, dry mucosa, blurred vision, constipation, urinary retention, tachycardia, disorientation

39
Q

What is the MOA of succinylcholine?

A

A neuromuscular blocker - continuous stimulation of the Nm receptor leads to paralysis to act as a muscle relaxant

40
Q

What is a major ADRs associated with depolarizing neuromuscular blockers?

A

Respiratory paralysis & death in patients with low or absent plasma AchE

41
Q

What are the non-depolarizing neuromuscular blockers?

A

Rocuronium, pancuronium, vecuronium

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