Unit 4: Cholinergic Agonists Flashcards

1
Q

2 targets of drug action for cholinergic agonists

A
  1. Postsynaptic receptor

2. Acetylcholinesterase enzyme

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2
Q

Acetylcholinesterase does what?

A

Breaks down acetylcholine

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3
Q

Where are nicotinic and muscarunic receptors found?

A
  1. All autonomic ganglia have nicotinic receptors
  2. All neuromuscular junction receptors are nicotinic
  3. All parasympathetic target organs have muscarunic receptors
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4
Q

Cholinergic agonists are divided into the following 2 groups

A
  1. Choline esters

2. Alkaloids

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5
Q

The alkaloids are ______ derivatives. What is important to note regarding alkaloids and cholinesterases?

A

Plant

Cholinesterases do not metabolize alkaloids

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6
Q

BETHANECHOL indication

A

Urinary retention

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7
Q

Nicotine does what to nicotinic receptors?

A

It is a direct agonist

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8
Q

Nicotine indications

A

Used therapeutically to help patients stop smoking

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9
Q

Cholinergic agonists generally have what effects?

A

Muscarinic

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10
Q

Cholinesterase inhibitors are broken into what 2 groups? How are these groups related to solubility?

A

Reversible (water soluble)

Irreversible (lipid soluble)

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11
Q

The REVERSIBLE INHIBITORS are used to treat what diseases?

A
  1. Myasthenia gravis

2. Alzheimer’s dementia

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12
Q

The reversible cholinesterase inhibitors tend to end with what?

A
  • STIGMINE

- NIUM

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13
Q

The irreversible cholinesterase inhibitors are referred to as

A

Nerve gases

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14
Q

What effect do cholinesterase inhibitors have on acetylcholine?

A

They increase acetylcholine

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15
Q

Activation of MUSCARINIC RECEPTORS:

Effect on the EYE

A

Miosis (constriction of pupil)

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16
Q

Activation of MUSCARINIC RECEPTORS:

Effect on the CV SYSTEM

A

Decrease heart rate

17
Q

Activation of MUSCARINIC RECEPTORS:

Effect on the RESPIRATORY SYSTEM

A

Bronchial constriction, increased secretions

18
Q

Activation of MUSCARINIC RECEPTORS:

Effect on the GI SYSTEM

A

Increased motility

Sphincter relaxation

19
Q

Activation of MUSCARINIC RECEPTORS:

Effect on the GU SYSTEM

A

Relaxation of sphincters

Bladder wall contraction

20
Q

Activation of MUSCARINIC RECEPTORS:

Effect on the GLANDS

A

Increased secretions

21
Q

Cholinergic agonists act on:

A

Postsynaptic receptor—some on the muscarinic one, some on the nicotinic one

22
Q

Cholinesterase inhibitors act on:

A

Breaking down cholinesterase and therefore increasing acetylcholine

23
Q

Choline esters have what in their name?

A

-CHOL-

24
Q

What is important to note about the lipid soluble cholinesterase inhibitors?

A

They rapidly cross all membranes, including the blood brain barrier

25
Q

What is Myasthenia Gravis?

A

An immune disease causing a loss of acetylcholine receptors, resulting in muscle weakness

26
Q

How does Alzheimer’s relate to acetylcholine?

A

There is a deficiency of cholinergic neurons

27
Q

EDROPHONIUM is used to …

A

Diagnose myasthenia gravis

28
Q

How does EDROPHONIUM work?

A

For patients with myasthenia gravis, the drug dramatically improves muscle strength

For patients without myasthenia gravis, it causes increased secretions and GI cramping from increased GI motility

29
Q

What is NEOSTIGMINE used to treat?

A

Myasthenia gravis

30
Q

What is PYRIDOSTIGMINE used to treat?

A

Myasthenia gravis

31
Q

Why is EDROPHONIUM—and not NEOSTIGMINE OR PYRIDOSTIGMINE—used to diagnose (vs treat) myasthenia gravis?

A

It is short acting. NEOSTIGMINE and PYRIDOSTIGMINE are both longer acting than ERDOPHONIUM.

32
Q

What drugs treat nerve gas poisoning?

A

PRALIDOXIME and ATROPINE

33
Q

SLUDGE…

A
Salivation
Lacrimation
Urination
Diaphoresis
GI Upset
Emesis