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Pharmacology > Cholinergic Agonists and Antagonists > Flashcards

Cholinergic Agonists and Antagonists Flashcards

1
Q

The muscarinic receptor is what kind of receptor?

A

GPCR

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2
Q

The nicotinic receptor is what kind of receptor?

A

Ligand gated ion channel

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3
Q

Generally, what functions does the parasympathetic NS have on the…eye, heart, bronchioles, GI tract, bladder?

A 
Pupillary constriction
Decreased chronotropy and inotropy
Bronchiole constriction
Increased GI motility
Stimulate bladder emptying
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4
Q

What does the M1 receptor do?

A

Activates myenteric plexus to stimulate peristalsis in gut

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5
Q

What does the M2 receptor do?

A

Decreases HR. It hyperpolarizes SA node pacemaker cells by opening K+ channels and allowing K+ to flow out of the cell.

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6
Q

What does the M3 receptor do?

A

Contracts ciliary muscle in the eye to allow for accomodation.
Bronchiole smooth muscle- leads to bronchoconstriction.
Activates bladder detrusor muscle to cause urination.
Stimulates secretions of GI tract, sweat glands, tear glands, and salivary glands.

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7
Q

How does the nicotinic receptor function? What binds the receptor and what does that cause?

A

Ligand gated ion channel. Two Ach molecules bind the receptor, inducing a conformational change to allow Na+ to flow through and depolarize the membrane.

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8
Q

Name the two kinds of nicotinic receptors and where they are located.

A

Nm = located in skeletal muscle; promotes skeletal muscle contraction

Nn = located on neurons in the CNS, parasympathetic and sympathetic ganglia

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9
Q

What is the one medical use for nicotine?

A

Smoking cessation!

Transdermal patch to help relieve smoking addiction

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10
Q

Nicotine is a selective agonist for what receptor?

A

Nn receptor

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11
Q

How is Succinylcholine used clinically?

A

Muscle relaxant

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12
Q

How does succinylcholine produce its physiological effects?

A

Succinylcholine is an Nm agonist. It binds the Nm receptors and activates them constitutively, preventing propagation of the action potential. Prolonged depolarization of the membrane prevents Na+ channels from leaving their inactive state, preventing the propagation of the action potential.

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13
Q

Will acetylcholine cross the BBB? Why or why not?

A

No!

It is positively charged.

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14
Q

Is acetylcholine useful medicinally?

A

Not really. Cholinesterases will degrade Ach very quickly.

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15
Q

Methacholine acts primarily at what kind of receptors?

A

Muscarinic

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16
Q

How is methacholine used clinically?

A

Used in the diagnosis of asthma. If a patient is given low doses of methacholine and experiences severe bronchoconstriction, then it is determined that he/she has asthma.

17
Q

Methacholine toxicity

A

Bronchiole constriction

18
Q

Contraindication for methacholine

A

Patient is taking a beta-blocker

19
Q

Carbachol has action at what receptors?

A

Nicotinic and muscarinic

20
Q

Where is carbachol used exclusively? Why?

A

In the eye! It can reduce pressure from ocular surgery and glaucoma. It is a topical miotic agent.

21
Q

What kind of receptors does bethanechol bind? What is special about bethanechol?

A

Binds muscarinic receptors. It is resistant to degradation by cholinesterases, so it has a long half life.

22
Q

How is bethanechol used clinically?

A

Used in cases of post-op urinary retention or neurogenic bladder atony. It helps patients urinate!

23
Q

Toxicity of bethanechol?

A

Bradycardia

Bronchoconstriction

24
Q

Contraindications of bethanechol?

A

Asthma
Peptic ulcers (can stimulate secretions in the lungs and gut)
Bradycardia

25
Q

Pilocarpine is a…

A

Nonselective muscarinic receptor agonist

26
Q

Indications of pilocarpine

A

Dry mouth in patients undergoing head/neck radiation
Sjogren’s Syndrome- antibodies attacking salivary glands
Glaucoma

27
Q

Toxicity of pilocarpine

A

Excess muscarinic activation can promote heart block due to high number of muscarinic receptors in the AV node

28
Q

What are the two kinds of cholinesterases? Where are they located?

A

Acetylcholinesterase- commonly located at the NMJ near nicotinic receptors.

Butrylcholinesterase- located in the plasma

29
Q

What do indirectly acting cholinomimetics do?

A

They inhibit cholinesterases, thereby increasing the half life of Ach

30
Q

Neostigmine Indications

A
  • Myasthenia gravis

- Reversal of non-depolarizing neuromuscular blockade

31
Q

Neostigmine Physiological effects

A

Increase activation of Nm receptors by increasing Ach concentration at the NMJ. Helps alleviate muscle weakness. Has some direct effects in activating the nicotinic receptor at the NMJ

32
Q

Neostigmine Toxicity

A

Muscarinic and Nicotinic excess

Pharmacology (67 decks)

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