1.

Botulinum toxin causes paralysis by

(A) Inhibiting choline acetyltransferase

(B) Blocking transport of choline into neurons

(C) Blocking release of acetylcholine from stor age vesicles

(D) Inhibiting acetylcholinesterase

(E) Blocking the synapse at ganglia

2. Which of the following neurotransmitters

interacts with guanethidine?

(A) Acetylcholine

(B) Epinephrine

(C) Dopamine

(D) Norepinephrine

(E) Serotonin

3. What is the mechanism of action of cocaine?

(A) Propagation of action of norepinephrine by

inhibiting its active transport from the

synapse

(B) Oxidative deamination of norepinephrine

in nerve terminals and the effector cells

(C) Inhibition of metabolism of norepinephrine

in nerve terminals

(D) Potentiation of tyrosine hydroxylase, the

rate-limiting enzyme in the synthesis of

norepinephrine

(E) Promotion of release of norepinephrine

from adrenergic nerve endings

4. What intracellular effect does albuterol, a

b2-agonist, produce?

(A) Allows passage of sodium through a ligand gated ion

channel

(B) Activates Gs-protein, resulting in stimula tion of

adenylyl cyclase

(C) Activates Gq-protein, resulting in increase of

phosphatidylinositol and calcium

mobilization

(D) Activates Gi-protein, resulting in inhibition

of adenylyl cyclase

(E) Binds to l-receptors in the specific areas of

the brain

5. What class of medications does bethanechol

belong to?

(A) Nicotinic blockers

(B) a-Agonists

(C) b1-Blockers
(D) b2-Blockers

(E) Muscarinic agonists

6. A 38-year-old farmer is brought to the ER by

his wife with symptoms of sudden difficulty

breathing, sweatiness, and anxiety. He was spray ing

insecticide when this happened. It has been

25 minutes since the symptoms started. The

patient is emergently intubated and given atro pine and

another medication that acts to reacti vate
acetylcholinesterase. What medication is it?

(A) Physostigmine

(B) Propranolol

(C) Pralidoxime

(D) Phenylephrine

(E) Pancuronium

7. Oxybutynin works by

(A) Inhibiting acetylcholinesterase at musca rinic and

nicotinic receptors

(B) Causing a neuromuscular blockade

(C) Antagonizing a1-adrenoceptors

(D) Binding to muscarinic receptors

(E) Activating b2-adrenoceptors

8. A 78-year-old man with Parkinson disease

experiences worsening of his symptoms. He is

already taking levodopa. Since the disease is

characterized by degeneration of dopaminergic

neurons, leading to the lack of inhibition of cho linergic

neurons, the addition of which medica tion is likely to help
alleviate the patient’s

symptoms?

(A) Benztropine

(B) Reserpine

(C) Doxazocin

(D) Timolol

(E) Tubocurarine

52

9. A 66-year-old woman with a long history of

heavy smoking presents to her doctor with com plaints of

shortness of breath and chronic

coughing that has been present for about 2 years

and has been worsening in frequency. The

doctor decides to prescribe a bronchodilator

agent that has minimal cardiac side effects,

since the patient also has an extensive cardiac

history. Which medication did the doctor likely

prescribe?
(A) Albuterol

(B) Prazosin

(C) Atenolol

(D) Ipratropium

(E) Pseudoephedrine

10. From the list below, choose the depolarizing

neuromuscular blocker most likely to be used in

‘‘rapid sequence intubation,’’ a procedure that

is done when the stomach contents have a high

risk of refluxing and causing aspiration.

(A) Baclofen

(B) Succinylcholine

(C) Neostigmine

(D) Homatropine

(E) Pralidoxime

11. Ephedra (ephedrine) causes increased

blood pressure by

(A) Indirect action on cholinergic receptors

(B) Blockade of adrenergic receptors

(C) Stimulation of release of epinephrine

(D) Inhibition of reuptake of catecholamines

(E) Direct action on dopamine receptors

12. A 34-year-old carpenter presents to the ER

after an accident in which he inadvertently

chopped off the tip his index finger. He is taken

to the OR for reattachment of the digit, and after

sedation, a local anesthetic is administered

around the site of the injury. The local anes thetic used in
the procedure did not contain

any epinephrine, as it usually does for most sur gical

procedures. The reason for this is

(A) Epinephrine causes increased blood loss

during delicate surgery

(B) Epinephrine causes swelling of the tissues,

making surgery more challenging

(C) Epinephrine is contraindicated in emer gency surgery

(D) Epinephrine causes vasoconstriction, which

can lead to vascular ischemia in digits

(E) Epinephrine can cause hypotension when

administered with sedative agents

13. A 7-year-old boy is brought in by his parents

for complaints of hyperactivity at school. He is

also inattentive and impulsive at home. After a

detailed interview, the physician decides to give

the boy amphetamine-containing medication

for presumed attention hyperactivity disorder.

Amphetamine

(A) Inhibits epinephrine reuptake

(B) Indirectly acts on norepinephrine receptors

(C) Blocks effects of norepinephrine

(D) Directly acts on cholinoreceptors

(E) Inhibits serotonin reuptake

14. Which of the following medications is used

to prevent premature labor?

(A) Tamsulosin

(B) Cevimeline

(C) Atracurium

(D) Tolterodine

(E) Terbutaline

15. What significant side effect of terazosin

should the doctor warn a 69-year-old patient

about?

(A) Bronchospasm

(B) Postural hypotension

(C) Heart failure

(D) Sedation
(E) Drug abuse

16. A floor nurse pages you about a patient who

is having chest pain. You order an electrocar diogram and

rush to see the patient. He

describes the pain as tight pressure and is

demonstrably sweating and gasping for air. The

ECG comes back with acute ST-segment eleva tions in

inferior leads, and you diagnose a myo cardial infarction.
You start giving the patient

oxygen and give him sublingual nitroglycerin

and morphine for pain. You also give him

another medication, which you have read may

prolong his survival in this dire situation. What

class of medication is it?

(A) b-Blocker

(B) a-Agonist

(C) Muscarinic agonist

(D) Neuromuscular blocker

(E) Dopamine agonist

17. A 35-year-old woman presents to your office

for a regular check-up. Her only complaint is

recurrent migraine headaches, which have

increased in frequency over the years. On exam ination, her
blood pressure is elevated at

Chapter 2 Drugs Acting on the Autonomic Nervous System

53

150/70. You decide to start her on antihyperten sive therapy

that is also used for prophylaxis of

migraines. Which medication is it?

(A) Clonidine

(B) Prazosin

(C) Hydrochlorothiazide

(D) Propranolol

(E) Verapamil

18. In contrast to propranolol, metoprolol

(A) Is used for the management of

hypertension

(B) Has greater selectivity for b2-adrenoceptors

(C) May be beneficial for the acute treatment of

migraine headache

(D) Is less likely to precipitate bronchoconstric tion in

patients with asthma

19. Intravenous administration of epinephrine

to a patient results in a severe decrease in dia stolic

pressure and an increase in cardiac output.
Which of the following drugs might the patient

have previously taken that could account for this

unexpected effect?

(A) Propanolol

(B) Atropine

(C) Phenylephrine

(D) Prazosin

20. Which of the following drugs is used to

diagnose myasthenia gravis?

(A) Atropine

(B) Neostigmine

(C) Bethanechol

(D) Edrophonium

(E) Pralidoxime

21. Pilocarpine reduces intraocular pressure in

patients with glaucoma because it

(A) Activates nicotinic cholinoceptors

(B) Blocks muscarinic cholinoceptors

(C) Selectively inhibits peripheral activity of

sympathetic ganglia

(D) Inhibits acetylcholinesterase

22. Prolonged apnea may occur following

administration of succinylcholine to a patient

with a hereditary deficiency of which of the fol lowing

enzymes?

(A) Glucose-6-phosphate dehydrogenase

(B) Plasma cholinesterase

(C) Monoamine oxidase

(D) Cytochrome P4503A

(E) Acetylcholinesterase

23. Dantrolene is the drug of choice to treat ma lignant

hyperthermia caused by succinylcholine

because dantrolene

(A) Blocks Ca2 release from sarcoplasmic

reticulum

(B) Induces contraction of skeletal muscle

(C) Increases the rate of succinylcholine

metabolism

(D) Inhibits succinylcholine binding to nicotinic

receptors

(E) Acts centrally to reduce fever

24. A drug that acts at prejunctional a2-adreno ceptors and

is used to treat hypertension is

(A) Clonidine

(B) Methoxamine
(C) Metaproterenol

(D) Dobutamine

(E) Dopamine

25. Drug X causes an increase in blood pressure

and a decrease in heart rate when administered

to a patient intravenously. If an antagonist at

ganglionic nicotinic receptors is administered

first, drug X causes an increase in blood pres sure and an

increase in heart rate. Drug X most

likely is

(A) Propranolol

(B) Norepinephrine

(C) Isoproterenol

(D) Terbutaline

(E) Curare

26. Poisoning with an insecticide containing an

acetylcholinesterase inhibitor is best managed

by administration of which one of the following

agents?

(A) Physostigmine

(B) Bethanechol

(C) Propranolol
(D) Pilocarpine

(E) Atropine

27. Receptor actions of acetylcholine are mim icked by

nicotine at which one of the following

sites?

(A) Adrenal medullary chromaffin cells

(B) Urinary bladder smooth muscle cells

(C) Iris circular (constrictor) muscle

(D) Heart sinoatrial pacemaker cells

28. Muscarinic cholinoceptor agonists may

cause vasodilation through the release of

endothelial

54 Pharmacology

(A) Histamine

(B) Norepinephrine

(C) Acetylcholine

(D) Nitric oxide

29. Emergency treatment of acute heart failure

is best managed with which of the following

drugs?

(A) Metaproterenol

(B) Phenylephrine
(C) Dobutamine

(D) Norepinephrine

(E) Isoproterenol

30. Which one of the following agents, when

applied topically to the eye, would cause both

mydriasis and cycloplegia?

(A) Phenylephrine

(B) Carbachol

(C) Prazosin

(D) Atropine

31. Neostigmine would be expected to reverse

which one of the following conditions?

(A) Paralysis of skeletal muscle induced by a

competitive, nondepolarizing muscle

relaxant

(B) Paralysis of skeletal muscle induced by a

depolarizing muscle relaxant

(C) Cardiac slowing induced by stimulation of

the vagus nerve

(D) Miosis induced by bright light

32. The direct cardiac effects of dobutamine

would be blocked by which one of the following

agents?

(A) Prazosin

(B) Metoprolol

(C) Clonidine

(D) Isoproterenol

33. Topical application of timolol to the eye

would be expected to induce which of the

following?

(A) Miosis

(B) Mydriasis

(C) Decreased formation of aqueous humor

(D) Increased outflow of aqueous humor

34. Phenylephrine is used to treat patients with

nasal mucosa stuffiness because it causes

vaso constriction by

(A) Blocking nicotinic cholinoceptors

(B) Blocking b-adrenoceptors

(C) Stimulating a-adrenoceptors

(D) Stimulating muscarinic cholinoceptors

Chapter 2 Drugs Acting on the Autonomic Nervous System

55

Answers and Explanations

1. The answer is C. Botulinum toxin blocks calcium-
dependent exocytosis of acetylcholine from

storage vesicles, producing paralysis. Common sources of

botulinum toxin include canned

home goods and, in cases of infant botulism, honey. The

condition is life threatening, and urgent

care is necessary. Choline acetyltransferase is an enzyme

catalyzing synthesis of acetylcholine

from an acetate and choline. Sodium-dependent transport of

choline can be blocked by hemi cholinium. Enzyme
acetylcholinesterase is responsible for catalyzing hydrolysis
of acetylcholine.

Acetylcholine synapses at the ganglia of many neurons and

tissues, and this step is not blocked

by botulinum toxin.

2. The answer is D. Guanethidine blocks the release of

norepinephrine from storage vesicles into

the nerve terminals. Acetylcholine release can be blocked

by botulinum toxin. Epinephrine, do pamine, and serotonin
release can be blocked by other agents (beyond the scope of
this chap ter), but not by guanethidine.

3. The answer is A. Cocaine is a potent inhibitor of

norepinephrine uptake, a process that normally

terminates norepinephrine’s action. Oxidative deamination

of norepinephrine in nerve termi nals and the effector cells
describes the action of monoamine oxidase, which is
targeted by cer tain antidepressant medications. Inhibition
of metabolism of norepinephrine in nerve terminals

describes catechol-O-methyltransferase, which is found in

nerve and other effector cells. Poten tiation of tyrosine
dehydroxylase would, in fact, cause excessive amounts of
norepinephrine to

accumulate; however, this enzyme is not affected by

cocaine. Norepinephrine release can be

blocked, not promoted, by agents such as bretylium and

guanethidine.

4. The answer is B. b2-agonists, like albuterol, activate Gs-

protein, which results in stimulation of

adenylyl cyclase, with subsequent increase in intracellular

cAMP. Passage of sodium via ligand gated ion channel is
manifested by nicotinic acetylcholine receptors. Activation
of Gq-protein

resulting in increase of phosphatidylinositol and calcium

mobilization refers to the mechanism

of action of muscarinic receptors type M1 and M3, as well as

a1-adrenoceptors. Activation of

Gq-protein resulting in increase of phosphatidylinositol and

calcium mobilization refers to

mechanism of action of M2-cholinoceptors and a2-

adrenoceptors. Finally, binding to

l-receptors in the specific areas of the brain describes the

action of opioid agents.
5. The answer is E. Bethanechol is a type of muscarinic
receptor agonist that is used clinically to

ameliorate urinary retention. Nicotinic blockers such as

trimethaphan are rarely used in clinical

practice because of the lack of selectivity. a-Agonists such

as epinephrine can be used in man agement of acute
bronchospasm (anaphylaxis). b1-Blockers do not have direct
effects on bron chial smooth muscle. b2-Agonists such as
albuterol are used for treatment of asthma.

6. The answer is C. Acetylcholinesterase reactivator

pralidoxime has to be given within 30 minutes

of exposure to insecticide because of the effects of ‘‘aging’’

(i.e., strengthening of the alkylphos phoryl-serine bond
formed between AChE and organophosphate). Physostigmine
is a cholines terase inhibitor that is occasionally used in
atropine or scopolamine poisoning. Propranolol is a

b-blocker used for hypertension as well as other indications.

Phenylephrine is an a-agonist used

for hypotensive emergencies. Pancuronium is a

nondepolarizing inhibitor of acetylcholine that

is used for muscle paralysis.

7. The answer is D. Oxybutynin acts by binding to

muscarinic receptors located on the detrusor

muscle of the bladder, suppressing involuntary contraction

of the muscle. Acetylcholinesterase
inhibitors such as edrophonium are used for myasthenia
gravis. Neuromuscular blockers such

as succinylcholine are used for anesthesia. a1-Antagonists

such as terazosin are used for benign

prostatic hypertrophy. b2-Agonists such as terbutaline can

be used to suppress premature labor.

56

8. The answer is A. Benztropine, an antimuscarinic agent, is

used as an adjunct for treatment of

Parkinson disease. Reserpine is a norepinephrine uptake

inhibitor occasionally used for treat ment of hypertension.
Doxazocin, an a-blocker, is used for benign prostatic
hyperplasia. Timo lol is a b-blocker used for glaucoma.
Tubocurarine is a neuromuscular blocker used in

anesthesia.

9. The answer is D. Ipratropium bromide is used extensively

for chronic obstructive pulmonary

disease (COPD), which is the most likely diagnosis in this

case. It acts by antagonizing musca rinic receptors in
bronchial smooth muscle, thereby causing bronchodilation.
Albuterol is also

used for treatment of COPD; however, it can cause adverse

cardiac effects such as tachycardia

and is not recommended in this case. Prazosin is an a-

blocker used for benign prostatic hyper trophy (BPH).
Atenolol is a b-blocker used for hypertension.
Pseudoephedrine is an a-agonist

used for nasal congestion.

10. The answer is B. Succinylcholine is a depolarizing

neuromuscular blocker that is used in rapid sequence
intubation, as well as other procedures. It quickly relaxes all
muscles in the body,

allowing a prompt intubation to prevent the reflux of gastric

contents into the trachea. Baclofen

is a centrally acting skeletal muscle relaxant used for

spasticity. Neostigmine is an indirect-acting

cholinergic agonist used for treatment of myasthenia gravis

and reversal of neuromuscular

blockade. Homatropine is an antimuscarinic agent used for

induction of mydriasis for ophthal mologic examinations.
Pralidoxime is an acetylcholinesterase reactivator used for
organophos phate poisoning.

11. The answer is C. Ephedrine acts indirectly to release

norepinephrine from nerve terminals,

causing effects similar to those of catecholamines,

including elevated blood pressure. This

potentially dangerous agent has been removed from the OTC

market because of an increasing

number of deaths being reported as caused by this agent. An

example of an indirect-acting cho linergic agonist is
edrophonium, which is used for diagnosis of myasthenia
gravis. Some adreno ceptor blockers, such as atenolol, are
used for treatment of hypertension. Catecholamine

reuptake inhibition is a property of some antidepressant

medications. Dopamine receptor ago nists are used in
treatment of Parkinson disease.

12. The answer is D. Epinephrine is contraindicated as an

anesthetic adjuvant for surgeries involv ing most facial
structures, digits, and the penis, because of the risk of
vascular compromise. This

agent causes decreased blood loss for most other surgeries

because of vasoconstriction.

Although local anesthetic agents such as Marcaine or

Xylocaine can cause mild local tissue swel ling, epinephrine
does not; either way, it is not a contraindication for hand
surgery. Epinephrine

causes elevated blood pressure when administered

systemically; however, it has no systemic

side effects when administered locally.

13. The answer is B. Amphetamine and similar compounds

are stimulants used for treatment of

attention-deficit/hyperactivity disorder (ADHD) in which they

are thought to act centrally to

increase attention span. Currently there is no medication on

the U.S. market that inhibits reup take of epinephrine.
Blocking of the effects of norepinephrine will not alleviate
symptoms of
ADHD. Direct-acting cholinoceptor agonists are not used in
treatment of ADHD. Serotonin

reuptake inhibitors are used for depression and some other

conditions.

14. The answer is E. Terbutaline, a b2-agonist, is used to

suppress premature labor because of its

ability to stop uterine contractions. Tamsulosin, an a1-

blocker, is used for benign prostatic hy pertrophy.
Cevimeline, a cholinergic agonist, is used for Sjogren
syndrome. Atracurium a non- €

depolarizing muscular blocker, is used for anesthesia.

Tolterodine, a muscarinic blocker, is used

for urinary incontinence.

15. The answer is B. a1-Adrenoceptor agonists such as

terazosin may cause significant postural

hypotension, and should be prescribed carefully in the

elderly population. Bronchospasm is

a possible side effect of b-blockers. b-Blockers can also

produce heart failure in some

patients. Sedation is common with the use of some agents

such as propranolol. Drug abuse

can be observed in patients using centrally acting

adrenoreceptor agonists such as

amphetamine.
Chapter 2 Drugs Acting on the Autonomic Nervous System
57

16. The answer is A. b-Blockers such as atenolol are now

part of management of acute myocar dial infarction, along
with oxygen, nitroglycerin, and morphine. They reduce
sympathetic

activity and heart contractility, thereby reducing the oxygen

demand. a-Agonists such as

phenylephrine are used in management of hypotension due

to shock. Muscarinic agonists

such as pilocarpine can be used in management of

glaucoma. Neuromuscular blockers

such as atracuronium are used in anesthesia. Dopamine

agonists are used in management

of Parkinson disease.

17. The answer is D. The b-blocker propranolol is a good

choice for an antihypertensive medica tion; however, it is
also successfully used for other indications, such as
prophylaxis of migraine

headaches, situational anxiety, and hyperthyroidism-induced

palpitations. The other choices

are all acceptable antihypertensive medications, but from

this list, only propranolol is used for

migraine prophylaxis.

18. The answer is D. Metoprolol is more selective at b1-

adrenoceptors, which are more abundant in
the heart than in the lungs. Like propranolol, it may be
beneficial in the prophylaxis of migraine.

19. The answer is D. Prazosin is the only drug listed that

blocks postjunctional a1-adrenoceptors

and inhibits epinephrine-mediated vasoconstriction.

20. The answer is D. Edrophonium, which will increase

muscle strength in untreated myasthenic

patients, is the preferred acetylcholinesterase inhibitor

(Tensilon test) because it has a short du ration of action.

21. The answer is B. Pilocarpine is a muscarinic

cholinoceptor agonist.

22. The answer is B. Plasma cholinesterase is responsible

for the rapid inactivation of

succinylcholine.

23. The answer is A. In patients with malignant

hyperthermia, a rare hereditary disorder, an

impaired sarcoplasmic reticulum is unable to sequester

calcium. The sudden release of calcium

results in extensive muscle contraction that can be reduced

with dantrolene.

24. The answer is A. Clonidine acts at prejunctional a2-

adrenoceptors and is used to treat hyper tension.
Methoxamine is a non-selective a-adrenoceptor agonist.
Metaproterenol is a selective
b2-adrenoceptor agonist. Dobutamine is a relatively
selective b1-adrenoceptor agonist. Dopa mine activates
both pre-junctional and postjunctional dopamine receptors
and also

b1-adrenoceptor.

25. The answer is B. In the absence of a nicotinic receptor

antagonist, norepinephrine may result in

a reflex baroreceptor-mediated increase in vagal activity.

The presence of such an agent

unmasks the direct stimulant effect of norepinephrine on

heart rate.

26. The answer is E. Atropine blocks the effects of increased

acetylcholine resulting from cholines terase inhibition.
Physostigmine indirectly activates cholinoceptors;
bethanechol and pilocar pine directly activate
cholinoceptors. Propanolol is a b-adrenoceptor antagonist.

27. The answer is A. Nicotinic cholinoceptors are found in

adrenal medullary chromaffin cells. At

the other sites, acetylcholine activates muscarinic

cholinoceptors.

28. The answer is D. The release of nitric oxide activates

guanylate cyclase, increasing guanosine

30

,50

-monophosphate (cyclic GMP) and sequestering calcium.

This leads to a relaxation of vas cular smooth muscle.
29. The answer is C. Dobutamine, a relatively selective b1-
adrenoceptor agonist, increases cardiac

output and lowers peripheral resistance. Metaproterenol has

a relatively more selective action

on the respiratory system than the cardiovascular system.

Phenylephrine and norepinephrine

increase peripheral resistance. Isoproterenol increases

heart rate.

30. The answer is D. Atropine produces both mydriasis and

cycloplegia (the inability to accommo date for near vision).
Phenylephrine causes mydriasis without cycloplegia.
Carbachol causes

pupillary constriction. Prazosin is an a-adrenoceptor

antagonist.

58 Pharmacology

31. The answer is A. Acetylcholine accumulation due to

neostigmine inhibition of cholinesterase

will reverse the action of the competitive neuromuscular

blocking agents.

32. The answer is B. The b1-adrenoceptor antagonist

metoprolol blocks the b1-adrenoceptor activ ity of
dobutamine.

33. The answer is C. b-Adrenoceptor blocking agents such

as timolol reduce aqueous humor

formation.
34. The answer is C. Phenylephrine activates a-
adrenoceptors, producing vasoconstriction