Part 2.2.1 - Autonomic Drugs - Sympathetic drugs Part 1

Natural catecholamines except:

a. Posses catechol nucleus

b. Posses ethylamine side chains

c. Include Epinephrine, Norepinephrine, and Dopamine.

d. Endogenous

e. All

f. None

f. None

Catechol nucleus:

a. Benzene ring

b. With 2 OH group at para position

c. With 2 OH group at ortho position

d. a and b

e. a and c

e. a and c

The sympathetic post-ganglion particularly releases __________.

a. Dopamine
b. Epinephrine
c. Norepinephrine
d. Serotonin

c. Norepinephrine

The adrenal medulla produces __________ and _______.

a. Acetylcholine and Epinephrine
b. Norepinephrine and Epinephrine
c. Histamine and Epinephrine
d. Serotonin and Epinephrine

b. Norepinephrine and Epinephrine

In the brain, the endogenous substances include __________and __________.

a. Norepinephrine and Dopamine
b. Norepinephrine and Calcium
c. Norepinephrine and Potassium
d. Norepinephrine and Insulin

a. Norepinephrine and Dopamine

Biosynthesis of natural catecholamines except:

a. Amino acid precursor is glycine.

b. Tyrosine hydroxylase is the first enzyme needed thus the rate limiting step.

c. Dopamine is the first catecholamine synthesized.

d. Epinephrine is the last catecholamine synthesized.

e. None

a. Amino acid precursor is glycine.

Biosynthesis of natural catecholamines:

a) Amino acid precursor is TYROSINE.

b) Tyrosine hydroxylase is the first enzyme needed thus the rate limiting step.

c) Dopamine is the first catecholamine synthesized.

d) Epinephrine is the last catecholamine synthesized.

Convert tyrosine to dopa.

a. Tryosine hydroxylase

b. Dopa decarboxylase

c. Dopamine B-hydroxylase

d. 2PNMT

e. Epinephrine

a. Tryosine hydroxylase

Convert dopa to dopamine.

a. Tryosine hydroxylase

b. Dopa decarboxylase

c. Dopamine B-hydroxylase

d. 2PNMT

e. Epinephrine

b. Dopa decarboxylase

Convert dopamine to norepinephrine.

a. Tryosine hydroxylase

b. Dopa decarboxylase

c. Dopamine B-hydroxylase

d. 2PNMT

e. Epinephrine

c. Dopamine B-hydroxylase

Convert norpepinephrine to epinephrine.

a. Tryosine hydroxylase

b. Dopa decarboxylase

c. Dopamine B-hydroxylase

d. 2PNMT

e. Epinephrine

d. 2PNMT

Norepinephrine:

a. A fraction can reach the adrenal medulla

b. 2PNMT is present in the adrenal medulla

c. 2PNMT convert norepinephrine in the adrenal medulla synthesizing epinephrine.

d. a and b

e. b and c

f. All

f. All

Adrenal gland:

a. Gland superior to kidney

b. Cortex is the outer layer (Adrenal cortex)

c. Medulla is the inner layer (Adrenal medulla)

d. a and b

e. b and c

f. All

f. All

Mechanism of storage of neurotransmitter:

a. Exocytosis

b. Endocytosis

c. Vesicles

d. Vacuoles

c. Vesicles

Release of neurotransmitter:

I. Release from the nerve terminals is through a calcium-dependent exocytosis calcium entry

II. Release in the post-ganglionic endings

III. Release in the SNS except at thermoregulatory sweat glands

IV. In the brain, majority of neurotransmitter released is Epinephrine

V. In the peripheral organ, majority is Norepinephrine which is released from adrenal medullary chromaffin cells.

a. I, II, III

b. II, III, IV

c. I, II, V

d. III, IV

e. I, II, III, IV

a. I, II, III

Release of neurotransmitter:

I) Release from the nerve terminals is through a calcium-dependent exocytosis calcium entry.

II) Release in the post-ganglionic endings

III) Release in the SNS except at thermoregulatory sweat glands.

IV) In the brain, majority of neurotransmitter released is NOREPINEPHRINE.

V) In the peripheral organ, majority is EPINEPHRINE which is released from adrenal medullary chromaffin cells.

Neurotransmitter is release in the SNS except at thermoregulatory sweat glands.

a. True

b. False

a. True

Majority of neurotransmitter in the brain.

a. Epinephrine

b. Norepinephrine

c. Dopamine

d. a and b

e. b and c

f. All

b. Norepinephrine

Majority of neurotransmitter in the peripheral organs.

a. Epinephrine

b. Norepinephrine

c. Dopamine

d. a and b

e. b and c

f. All

a. Epinephrine

Agent that can block storage of neurotransmitter:

a. Reserpine

b. Tyramine

c. Ephedrine

d. Amphetamine

e. All

a. Reserpine

Agents that can alter exocytosis of NE except:

a. Guanethedine

b. Guanadrel

c. Bretylium

d. Tyramine

e. Reserpine

f. None

e. Reserpine

Agents that enhance exocytosis of NE except:

a. Tyramine

b. Ephedrine

c. Ampethamine

d. Methamphetamine

e. Angiotensin II

f. None

f. None

Agents that inhibits release of NE:

a. Guanethedine

b. Guanadrel

c. Bretylium

d. All

e. None

d. All

Agents that decrease sympathetic effect:

a. Guanethedine

b. Guanadrel

c. Bretylium

d. All

e. None

d. All

Agents that increase sympathetic effect except:

a. Tyramine

b. Ephedrine

c. Ampethamine

d. Angiotensin II

e. Methamphetamine

f. None

f. None

Termination of neurotransmitter may be through:

a. Reuptake

b. Diffusion

c. Metabolism

d. a and b

e. b and c

f. All

f. All

Reuptake inhibitors:

a. Increase NE in synapse

b. Increase NE binding to receptor

c. Increase sympathetic effect

d. a and b

e. b and c

f. All

f. All

Termination:

a. Metabolism -> Reuptake -> Process Passive Diffusion

b. Passive Diffusion -> Metabolism -> Reuptake Process

c. Reuptake -> Process Passive Diffusion -> Metabolism

b. Passive Diffusion -> Metabolism -> Reuptake Process

[Termination]

The ____ is responsible for the transport of catecholamines to the storage vesicles, maintaining their cytosolic concentration low.

a. NET
b. EMT
c. VMAT
d. COMT

c. vesicular monoamine transporter (VMAT)

[Termination]

After catecholamines are released into the synaptic cleft, they may be reuptaken into the presynaptic terminal. This reuptake process is carried out by the __________.

a. MAO
b. COMT
c. EMT
d. NET

d. noradrenaline transporter (NET)

[Termination]

Catecholamines can also be transported into extraneuronal cells after release into the synaptic cleft. The most important transporter involved in this process is the __________.

a. EMT
b. VMAT
c. NET
d. MAO

a. extraneuronal monoamine transporter (EMT)

[Termination]

Catecholamines are metabolized by intracellular enzymes after their release and reuptake. One important enzyme is located in the outer membrane of mitochondria in neurons and extraneuronal cells. This enzyme is called __________.

a. NET
b. COMT
c. MAO
d. VMAT

c. MAO

[Termination]

___is another enzyme responsible for catecholamine metabolism. Unlike MAO, this enzyme is mainly located in extraneuronal cells.

a. EMT
b. COMT
c. NET
d. VMAT

b. COMT- Catechol-O-methyl transferase

[Termination]

____are the two main enzymes responsible for catecholamine metabolism. Their enzymatic actions lead to the formation of several products after breakdown of catecholamines.

a. EMT and MAO
b. COMT and MAO
c. NET and COMT
d. VMAT and COMT

b. COMT and MAO

Receptor causes contraction of vascular smooth muscle

a. Beta2 receptor
b. Dopaminergic2 receptor
c. Alpha1 receptor
d. Beta3 receptor

c. Alpha1 receptor

Alpha1 receptor stimulation in the radial muscles of the iris causes ________.

a. Miosis
b. Mydriasis
c. Sedation
d. Tremors

b. Mydriasis

Contraction of pilomotor smooth muscles produces ________.

a. Vasodilation
b. Tremors
c. Goosebumps
d. Hypokalemia

c. Goosebumps

-Contraction (piloerection)

Alpha1 receptor stimulation in prostatic smooth muscles may lead to ________.

a. Bronchodilation
b. Urinary retention
c. Lipolysis
d. Sedation

b. Urinary retention

Alpha2 receptors are primarily ________ linked.

a. Gs-linked
b. Gi-linked
c. Gq-linked
d. Na-linked

b. Gi-linked

→ Autoregulation (Inhibits further release of NE from the vesicles)

Central stimulation of Alpha2 receptors causes ________.

a. Tremors
b. Bronchodilation
c. Sedation
d. Lowers BP

c. Sedation

Peripheral stimulation of Alpha2 receptors causes ________.

a. Tremors
b. Bronchodilation
c. Sedation
d. Lowers BP

d. Lowers BP

Which receptor increases force of cardiac contraction?

a. Beta1 receptor
b. Beta2 receptor
c. Alpha2 receptor
d. Dopaminergic2 receptor

a. Beta1 receptor

Increased heart rate is also known as positive ________.

a. Dromotropism
b. Inotropism
c. Chronotropism
d. Lipolysis

c. Chronotropism

Increased force of contraction is also known as positive ________.

a. Dromotropism
b. Inotropism
c. Chronotropism
d. Lipolysis

b. Inotropism

Increased AV nodal conduction is also known as positive ________.

a. Dromotropism
b. Inotropism
c. Chronotropism
d. Lipolysis

a. Dromotropism

Beta1 receptor stimulation in the kidneys increases ________ secretion.

a. Dopamine
b. Renin
c. Insulin
d. Potassium

b. Renin

Target: Kidneys (Renal Juxtaglomerular Apparatus)

Response: RAAS activation = Increased BP

Bronchodilation is mainly caused by stimulation of ________ receptors.

a. Alpha1
b. Beta2
c. Beta3
d. Dopaminergic2

b. Beta2

Relaxation of the uterus caused by Beta2 receptors is called ________.

a. Lipolysis
b. Tocolysis
c. Sedation
d. Mydriasis

b. Tocolysis

Targeting blood vessels (skeletal muscles) caused by Beta2 receptors leads to:

a. vasodilation

b. vasoconstriction

a. vasodilation

Beta receptors are primarily ________ linked.

a. Gs-linked
b. Gi-linked
c. Gq-linked
d. Na-linked

a. Gs-linked

qiss:

A1 - q

A2 - i

B1 - s

B2 - s

Beta2 receptor stimulation in skeletal muscle cell membranes may cause ________.

a. Hyperkalemia
b. Hypokalemia
c. Sedation
d. Ileus

b. Hypokalemia

Contraction of neuromuscular endplates due to Beta2 stimulation produces ________.

a. Tremors
b. Goosebumps
c. Vasodilation
d. Sedation

a. Tremors

Beta3 receptors primarily stimulate ________ in adipocytes.

a. Sedation
b. Bronchodilation
c. Lipolysis
d. Vasoconstriction

c. Lipolysis

Dopaminergic1 receptors are primarily ________ linked.

a. Gi-linked
b. Gq-linked
c. Gs-linked
d. Na-linked

c. Gs-linked

Dopaminergic1 receptors are mainly located in the ________ blood vessels.

a. Coronary and cerebral
b. Renal and splanchnic
c. Pulmonary and hepatic
d. Peripheral and cutaneous

b. Renal and splanchnic

-Vasodilation (⬆GFR = Diuresis)

Dopaminergic2 receptors are primarily ________ linked.

a. Gs-linked
b. Gi-linked
c. Gq-linked
d. Ca-linked

b. Gi-linked

Central stimulation of D2 receptors causes ________.

a. Perception and behavior

b. Modulation of motor activity

c. Relaxation

a. Perception and behavior

&

b. Modulation of motor activity

Peripheral stimulation of D2 receptors causes ________.

a. Perception and behavior

b. Modulation of motor activity

c. Relaxation

c. Relaxation (ileus; no peristalsis)

The catechol group is also known as ________.

a. 1,2-dihydroxybenzene
b. 3,4-dihydroxybenzene
c. 2,4-dihydroxybenzene
d. 1,4-dihydroxybenzene

b. 3,4-dihydroxybenzene

Catecholamines or Non-catecholamines

___1. Not metabolized by MAO and COMT

___2. High potency in activating Alpha and Beta receptors

___3. Longer half-lives

___4. Do not penetrate the CNS

___5. Metabolized by MAO and COMT

___6. Administered orally

___7. No catechol

Non-catecholamines___1. Not metabolized by MAO and COMT

Catecholamines ______2. High potency in activating Alpha and Beta receptors

Non-catecholamines___3. Longer half-lives

Catecholamines ______4. Do not penetrate the CNS

Catecholamines ______5. Metabolized by MAO and COMT

Non-catecholamines___6. Administered orally

Non-catecholamines___7. No catechol

Catecholamines or Non-catecholamines

___1. Phenylephrine

___2. Dopamine

___3. Norepinephrine

___4. Methoxamine

___5. Amphetamine

___6. Epinephrine

___7. Ephedrine

___8. Isoproterenol

Non-catecholamines___1. Phenylephrine

Catecholamines ______2. Dopamine

Catecholamines ______3. Norepinephrine

Non-catecholamines___4. Methoxamine

Non-catecholamines___5. Amphetamine

Catecholamines ______6. Epinephrine

Non-catecholamines___7. Ephedrine

Catecholamines ______8. Isoproterenol

Binds and activate more than 1 general type of adrenergic receptor

a. Direct-acting: Non-selective

b. Direct-acting: Selective

a. Direct-acting: Non-selective

Binds and activates 1 general type of adrenergic receptor

a. Direct-acting: Non-selective

b. Direct-acting: Selective

b. Direct-acting: Selective

[Direct-acting: Non-Selective]

__________ is a non-selective adrenergic agonist that acts on α₁, β₁, and β₂ receptors.

a. Dopamine
b. Epinephrine
c. Norepinephrine
d. Lidocaine

b. Epinephrine

[Direct-acting: Non-Selective]

Epinephrine acts on these receptors:

a. α₁

b. β₁

c. β₂

d. D₁

a. α₁

b. β₁

c. β₂

[Direct-acting: Non-Selective]

Epinephrine is commonly used for ___,_____, and_____

a. Glaucoma
b. Septic shock
c. Anaphylaxis
d. Acute heart failure

e. Anaphylactic shock

f. Anaphylactoid reaction

c. Anaphylaxis

e. Anaphylactic shock

f. Anaphylactoid reaction

[Direct-acting: Non-Selective]

Epinephrine may be used as a cardiac __________.

a. vasodilator
b. depressant
c. stimulant
d. blocker

c. stimulant

[Direct-acting: Non-Selective]

Epinephrine is used as a local vasoconstrictor together with __________.

a. Dipivefrin
b. Dopamine
c. Lidocaine
d. Digoxin

c. Lidocaine

[Direct-acting: Non-Selective]

Prodrug of Epinephrine used to treat glaucoma by lowering intraocular pressure

a. Dipivefrin
b. Dopamine
c. Epinephrine
d. Norepinephrine

a. Dipivefrin

[Direct-acting: Non-Selective]

Norepinephrine acts on these receptors:

a. α₁

b. β₁

c. β₂

d. D₁

a. α₁

b. β₁

[Direct-acting: Non-Selective]

_______ primarily acts on α₁ and β₁ receptors and is indicated for septic shock.

a. Norepinephrine
b. Epinephrine
c. Dopamine
d. Lidocaine

a. Norepinephrine

[Direct-acting: Non-Selective]

Norepinephrine is commonly used for ___.

a. Glaucoma
b. Septic shock
c. Anaphylaxis
d. Acute heart failure

e. Anaphylactic shock

f. Anaphylactoid reaction

b. Septic shock

[Direct-acting: Non-Selective]

Dopamine acts on these receptors:

a. α₁

b. β₁

c. β₂

d. D₁

a. α₁

b. β₁

d. D₁

[Direct-acting: Non-Selective]

____acts on α₁, β₁, and D₁ receptors.

a. Norepinephrine
b. Epinephrine
c. Dopamine

c. Dopamine

[Direct-acting: Non-Selective]

Dopamine may be used as an alternative treatment for __________ shock.

a. septic
b. anaphylactic
c. cardiogenic
d. hypovolemic

c. cardiogenic

[Direct-acting: Non-Selective]

Dopamine is indicated for____

a. Glaucoma
b. Septic shock
c. Anaphylaxis
d. Acute heart failure

e. Anaphylactic shock

f. Anaphylactoid reaction

d. Acute heart failure

[Direct-acting: Non-Selective]

Digital necrosis is a toxic effect associated with __________ receptor stimulation.

a. α₁
b. β₂
c. D₁
d. M₂

a. α₁

[Direct-acting: Non-Selective]

Ventricular tachyarrhythmias are toxic effects associated with __________ receptor stimulation.

a. α₁
b. β₁
c. β₂
d. D₁

b. β₁

[Direct-acting: Selective]

____-selective agonist commonly used for hypotension, nasal and ophthalmic congestion.

a. β₂-selective
b. α₂-selective
c. α₁-selective
d. D₁-selective

c. α₁-selective

ex: Phenylephrine

[Direct-acting: Selective]

Methoxamine belongs to the group of __________ agonists.

a. β₂-selective
b. α₂-selective
c. α₁-selective
d. D₁-selective

c. α₁-selective

[Direct-acting: Selective]

Phenylephrine and Propylhexedrine belong to the group of __________ agonists.

a. β₂-selective
b. α₂-selective
c. α₁-selective
d. D₁-selective

c. α₁-selective

[Direct-acting: Selective]

Tetrahydrozoline, Oxymetazoline, Nafazoline belong to the group of __________ agonists.

a. β₂-selective
b. α₂-selective
c. α₁-selective
d. D₁-selective

c. α₁-selective agonist

[Direct-acting: Selective]

________ may occur when nasal decongestants are used for more than 3 days.

a. Hypertension
b. Rhinitis medicamentosa
c. Hyperkalemia
d. Hepatotoxicity

b. Rhinitis medicamentosa

[Direct-acting: Selective]

A systemic toxic effect of α₁-selective agonists is __________.

a. Tremors
b. Sedation
c. Hypertension
d. Hepatotoxicity

e. Urinary retention

c. Hypertension

[Direct-acting: Selective]

A systemic toxic effect of α₁-selective agonists common in patients with BPH

a. Tremors
b. Sedation
c. Hypertension
d. Hepatotoxicity

e. Urinary retention

e. Urinary retention

[Direct-acting: Selective]

α₁-selective agonist when used for more than 5 days may lead to

a. Tolerance

b. Addition

c. Withdrawal

a. Tolerance

[Direct-acting: Selective]

___is a rapid-acting α₂-selective agonist used for hypertensive crisis.

a. Methyldopa
b. Clonidine
c. Guanabenz
d. Brimonidine

b. Clonidine

[Direct-acting: Selective]

Clonidine may also be used as an alternative treatment for __________.

a. Asthma
b. Glaucoma
c. ADHD
d. COPD

c. ADHD

[Direct-acting: Selective]

A toxic effect of Clonidine is withdrawal-induced __________.

a. hyperkalemia
b. hypertension
c. sedation
d. tremors

b. hypertension

[Direct-acting: Selective]

_______ is FDA-approved for use in pregnant women with hypertension.

a. Methyldopa
b. Clonidine
c. Apraclonidine
d. Guanfacine

a. Methyldopa

[Direct-acting: Selective]

Sedation and hepatotoxicity are toxic effects associated with __________.

a. Methyldopa
b. Fenoldopam
c. Isoproterenol
d. Salmeterol

a. Methyldopa

[Direct-acting: Selective]

(+) Coombs test is a toxic effect associated with __________.

a. Methyldopa
b. Fenoldopam
c. Isoproterenol
d. Salmeterol

a. Methyldopa

[Direct-acting: Selective]

Methyldopa belongs to the group of __________ agonists.

a. β₂-selective
b. α₂-selective
c. α₁-selective
d. D₁-selective

b. α₂-selective agonist

[Direct-acting: Selective]

These are centrally acting α₂-selective agonists:

a. Guanfacine

b. Guanabenz

c. Brimonidine

d. Apraclonidine

a. Guanfacine

b. Guanabenz

[Direct-acting: Selective]

These are α₂-selective agonists used as anti-glaucoma agents.

a. Guanfacine

b. Guanabenz

c. Brimonidine

d. Apraclonidine

c. Brimonidine

d. Apraclonidine

__________ is a non-selective β agonist used as an alternative during shock states.

a. Dobutamine
b. Isoproterenol
c. Fenoldopam
d. Methoxamine

b. Isoproterenol

Isoproterenol, an inotropic agent, may be used in the management of acute __________ failure.

a. renal
b. liver
c. heart
d. respiratory

c. heart

[Direct-acting: Selective]

___is the first-line β₁-selective agonist for cardiogenic shock.

a. Dobutamine
b. Clonidine
c. Terbutaline
d. Nafazoline

a. Dobutamine

[Direct-acting: Selective]

Dobutamine may be used for a pharmacologic stress test together with __________.

a. Dipyridamole
b. Lidocaine
c. Salmeterol
d. Ritodrine

a. Dipyridamole

[Direct-acting: Selective]

Dobutamine may be used for management of

a. Acute Heart Failure

b. Septic Shock

c. Glaucoma

d. BPH

a. Acute Heart Failure

[Direct-acting: Selective]

SABA or LABA

___a. Terbutaline

___b. Salmeterol

___c. Pirbuterol

___d. Formoterol

___e. Salbutamol/Albuterol

___f. Bambuterol

___g. Indacaterol

___h. Metaproterenol

SABA a. Terbutaline

LABA b. Salmeterol

SABA c. Pirbuterol

LABA d. Formoterol

SABA e. Salbutamol/Albuterol

LABA f. Bambuterol

LABA g. Indacaterol

SABA h. Metaproterenol

[Direct-acting: Selective]

__________ is a β₂-selective agonist used as a tocolytic for preterm labor.

a. Clonidine
b. Ritodrine
c. Dobutamine
d. Apraclonidine

b. Ritodrine and Isoxsuprine