6 - Cholinergic Antagonists

Autonomic Nervous System

1. What are the major effects of sympathetic stimulation?
Fight or Flight

Increased heart rate

Increased heart contractility
Decreased GI motility
Dilation of peripheral blood vessels

2. What are the major effects of parasympathetic stimulation?

Rest and Digest

Decreased heart rate

Decreased heart contractility
Increased GI motility
Copious watery secretions

3. What are the most clinically important neurotransmitters?

Norepinephrine
Epinephrine
Dopamine
Serotonin

4. What are the most clinically important receptors in the autonomic and somatic nervous systems?
Nicotinic

Adrenergic

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5. What kind of cholinergic receptors are found on parasympathetic effector organs?

Antimuscarinic Agents
Atropine
Scopolamine
Ipratropium
Tiotropium
Tropicamide
Cyclopentolate
6. What sympathetic function is mediated by muscarinic receptors?

Atropine
7. What is the mechanism of action of atropine? (LP p55-58)
Binds
to muscarinic receptors
Blocks
from binding to the receptors and eliciting its usual response

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8. Fill in the blanks of the actions of atropine. (LP p55-58)

Organ System
Eye

Effect

Gastrointestinal

Respiratory

Cardiovascular

Urinary

Sweat Glands

9. Why isnt atropine used very often to dilate the eye? (LP p55-58)
Long lasting effect of

10. What medication is atropine combined with to treat diarrhea? (LP p55-58)

11. What is the mechanism of action of organophosphate poisoning? (LP p55-58)

In the synaptic cleft,
prevent the degradation of acetylcholine
Leads to an overdose of cholinergic activity in the body
Symptoms include
, drooling, mental status changes and fever

12. In what medical problem are the anti-secretory effects of atropine useful? (LP p55-58)

13. What are the adverse effects of atropine? (LP p55-58)

Hot as a hare: Increased body temperature
Dry as a bone:
Red as a beet: Flushed skin
Blind as a bat: Cycloplegia
Mad as a hatter: Disorientation/delirium
Bloated as a toad:

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Scopolamine
14. How does scopolamine differ from atropine? (LP p58)

15. What are the therapeutic uses of scopolamine? (LP p58)

Ipratropium and Tiotropium

16. How is ipratropium and tiotropium administered? (LP p58)

17. What are the benefits of ipratropium and tiotropium being inhaled agents? (LP p58)
Effects are only felt in the
No systemic absorption
Fewer
associated with antimuscarinics

18. What is the primary clinical use of ipratropium and tiotropium? (LP p58)

Tropicamide and Cyclopentolate

19. What is the therapeutic use of tropicamide and cyclopentolate? (LP p58)

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Quick Review 1
1. In what ophthalmologic disease should you not use atropine? (LP p55-58)

2. Which type of patient is more susceptible to the hyperpyrexia effects of atropine? (LP p58)

3. What are the two benefits of combining atropine with diphenoxylate to treat diarrhea?
Atropine will decrease
Atropine will decrease the likelihood of
of diphenoxylate

4. What is the most common way to administer scopolamine? (LP p58)

5. What are the effects of atropine on the respiratory system?

6. Which inhaled antimuscarinic has a longer half-life and can be dosed once per day?

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Ganglionic Blockers
Nicotine
Mecamylamine
1. What is the mechanism of action of the ganglionic blockers? (LP p59)
Block
receptors on both the
ganglia in the autonomic nervous system

and the

2. Why are there few clinical applications for ganglionic blockers? (LP p59)

Nicotine
3. What is the mechanism of action of nicotine? (LP p59)
Nicotine binds to nicotinic acetylcholine receptors in the CNS
Nicotine in the CNS will result in increased levels of
and this is
responsible for the euphoria and relaxation and addiction caused by nicotine consumption
Nicotine activates the
nervous system, resulting in epinephrine release

4. What is the half-life of nicotine? (LP p59)

5. What is the action of menthol on nicotine? (LP p59)

6. What are the adverse effects of nicotine? (LP p59)

Tremors
GI cramping
Diarrhea

Increased blood pressure

7. What are the effects of nicotine on pregnancy? (LP p59)

Spontaneous abortion

Placenta previa
Preterm labor

8. What is the mechanism of action of varenicline?

at 4 2 neuronal nicotinic acetylcholine receptor

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9. What are the adverse effects of varenicline?

Mood changes
Depression

Mecamylamine
10. What is the therapeutic use of mecamylamine?
Used to lower blood pressure in

situations

Neuromuscular Blocking Drugs

Tubocurarine
Pancuronium
Mivacurium
Metocurine
Doxacurium

Atracurium
Cisatracurium
Vecuronium
Rocuronium
Pipercuronium

Succinylcholine

11. What is the mechanism of action of the nondepolarizing agents? (LP p59-61)
Bind to the nicotinic receptors without
the cell
Prevents
from binding
Prevents the depolarization of the muscle cell membrane and inhibits muscle contraction

12. How can you overcome the actions of the nondepolarizing agents? (LP p59-61)

13. When using the nondepolarizing agents which muscle are affected first and last? (LP p59-61)
Rapidly contracting muscles first, like
muscles
Then the fingers, then the limbs, neck and trunk muscles
The
is paralyzed last

14. What are the therapeutic uses of the nondepolarizing agents? (LP p59-61)
Adjuvant in
Facilitate intubation

15. Which nondepolarizing agents are metabolized in the liver? (LP p59-61)

16. Which nondepolarizing agent can cause an increase in heart rate? (LP p59-61)

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17. Which drugs can enhance the effects of the nondepolarizing agents? (LP p59-61)
Halogenated hydrocarbon anesthetics

Calcium-channel blockers

18. What is the mechanism of action of the depolarizing agents? (LP p61-63)
Attach to the nicotinic receptor and act just like
They
the cell just like acetylcholine

19. What is the first effect of the depolarizing agents on the body? (LP p61-63)
Transient
of the muscles (fasciculations)
Called

20. What is the second effect of the depolarizing agents on the body? (LP p61-63)
Gradual repolarization which is then resistant to
flaccid paralysis
Called

and you get

21. What are the therapeutic uses of succinylcholine? (LP p61-63)

Rapid endotracheal intubation

treatment

22. What are the adverse effects of succinylcholine? (LP p61-63)

Hyperthermia: malignant hyperthermia (muscle rigidity and hyperpyrexia) can occur when given with
, an inhaled anesthetic

: results from loss of tissue potassium during depolarization. Risk

is worse in patients with burns, muscle trauma or spinal cord injuries
Post-op muscle pain

: from direct stimulation of muscarinic cholinoceptor stimulation

Apnea: some patients have a deficiency in plasma cholinesterase and are thus more prone to have
prolonged paralysis of the diaphragm

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Quick Review 2
1. What is responsible for the addiction of nicotine?
Increased levels of

in the brain

2. Which neuromuscular blocking agent acts very similarly to acetylcholine by depolarizing the cell? (LP p61-63)

3. The neuromuscular blocking agents affect which muscles last? (LP p60-63)

4. What is the effect of halothane on nondepolarizing agents? (LP p61)

5. What is the potential adverse effect of combining halothane with a depolarizing agent? (LP, p63)

6. Which nondepolarizing agent is the fastest acting and is therefore very useful for tracheal intubation in
patients with gastric contents? (LP, p62)

7. Which nondepolarizing agent has the fastest recovery time and is therefore useful for short surgical
procedures? (LP, p62)

8. Which nondepolarizing agent spontaneously degrades in plasma and is the only nondepolarizing agent that
does not need to be reduced in patients with renal failure? (LP, p62)

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End of Session Quiz

1. Why arent cholinesterase inhibitors as effective at overcoming the effects of high-dose neuromuscular
blockers?

2. Match the following clinical descriptions with the most appropriate therapeutic agent: (LP p57-63)
Choices: atropine, scopolamine, succinylcholine, cisatracurium, varenicline

A 53-year-old with ESRD is in the ICU and needs mechanical ventilation

A 27-year-old woman who gets motion sickness is going boating for a day
A 13-year-old childs eyes need to be measured for refractive errors
A 31-year-old man wants to quit smoking
A 47-year-old man with bipolar disorder is about to undergo ECT

3. Match the drug to the adverse effect. (LP p57-63)

Atropine

Induces histamine release

Nicotine

Dry mouth

Turbocurarine

Hyperkalemia

Succinylcholine

Tachycardia

4. Match the agents below with their mechanism of action. (LP p55-63)
Nicotine

Ipratropium

a. Antimuscarinic agents

Scopolamine

Vecuronium

b. Ganglionic blockers

Tubocurarine

Mecamylamine

c. Neuromuscular blockers

Atropine

Succinylcholine

5. What are the adverse effects of atropine? (LP p55-58)

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6. Which two antimuscarinic drugs are beneficial because their effects are only felt in the lungs, have no
systemic absorption, and have fewer side effects?

7. A 32-year-old farmer presents with diaphoresis, watery eyes, drooling, and vomiting. What was he exposed
to? How do you manage this problem?

8. What are the adverse effects of succinylcholine? (LP p61-63)

9. Both the depolarizing and nondepolarizing agents are similar to what neurotransmitter? How are their
mechanisms of action different?

10. A patient has undergone surgery with the aid of a nondepolarizing agent. What can be used to reverse the
effects of the nondepolarizing agent?

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