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Dr. Austin Adrenergic PART I

Total questions: 70

Worksheet time: 3hrs 40mins

Name
Class
Date
1.

Which of the following events occur on the Sympathetic Nervous System? Select all that apply

a)

Adrenal medulla secretes epinephrine and norepinephrine.

b)

Blood flow to skeletal muscles increases

c)

Stomach contraction are inhibited

d)

Hypothalamus activates sympathetic division of nervous system

e)

Heart rate, blood pressure and respiration increase

2.

Which of the following are the Receptors of the Sympathetic NS? Select all that apply

a)

Dopamine

b)

Adrenergic (adrenoreceptors)

c)

Muscarinic

d)

Acethylcholine

3.

Which of the following are TRUE about the Adrenergic (adrenoreceptors)? Select all that apply

a)

alpha (α1 α2) and beta (β1 β2 β3)

b)

D1-D5 (blood vessels, nephrons)

c)

G protein-coupled receptors

d)

endogenous neurotransmitters are agonists (varying selectivity)

4.

Which of the following are TRUE about Dopamine? Select all that apply

a)

alpha (α1 α2) and beta (β1 β2 β3)

b)

D1-D5 (blood vessels, nephrons)

c)

G protein-coupled receptors

d)

M3 (sweat glands)

5.

Which of the following are TRUE about Muscarinic receptors? Select all that apply

a)

G protein-coupled receptors

b)

Gi coupled

c)

M3 (sweat glands)

d)

D1-D5 (blood vessels, nephrons)

6.

The Net effect(s) of adrenergic receptor activity is determined by which of the following? Select all that apply

a)

Activity of ligand at receptor.

b)

Amount and distribution of receptor (s) on target tissue.

c)

Reflex and regulatory adjustments.

d)

None of the above are correct

7.

Adrenergic neurons utilize the amino acid tyrosine to synthesize catecholamine neurotransmitters.

a)

True

b)

False

8.

In most postganglionic neurons, ________ is final product, some converted to ___________ in adrenal medulla, synthesis ends at __________ in dopaminergic neurons.

a)

epinephrine (Epi=Adrenaline) , Acetylcholine, dopamine (D)

b)

norepinephrine (NE= Noradrenaline), epinephrine (Epi), dopamine (D)

9.

Which of the following oxidizes amine to carbonyl?

a)

Monoamine oxidase (MAO)

b)

Catechol-O-methyl transferase (COMT)

c)

Catecholamine

d)

Dopamine

10.

Which of the following has significant expression in hepatic tissue and methylates the meta (3 position) hydroxy group?

a)

Catechol-O-methyl transferase (COMT)

b)

Monoamine oxidase (MAO)

c)

Dopamine

d)

Cathecolamine

11.

Which of the following are considered the minimum requirements for binding ARs? Select all that apply

a)

Basic nitrogen

b)

Aromatic ring

c)

Carbon bridge (two C’s between 1. and 2.

d)

Cl

12.

Catecholamine neurotransmitters may be recycled or metabolized.

a)

True

b)

False

13.

Which of the following is predominantly cytosolic?

a)

Catechol-O-methyl transferase (COMT)

b)

Monoamine oxidase (MAO)

14.

Which of the following bound to outer membrane of mitochondria?

a)

Monoamine oxidase (MAO)

b)

Catechol-O-methyl transferase (COMT)

15.

Which of the following means dynamic antagonism and sympathetic tone (instead of antagonizing, the body can reduce the amount of agonist).

a)

No endogenous antagonist

b)

No endogenous agonist

16.

Which of the following explain why the effects of endogenous sympathomimetics (and drugs affecting SNS) are so complicated and are often dose dependent? Select all that apply

a)

Reflex and regulatory adjustments

b)

Amount and distribution of receptor (s) on target tissue.

c)

Activity of ligand at receptor.

d)

None of the above are correct

17.

Which of the following pathway is relevant when patients are taking monoamine oxidase inhibitors (MAOIs)?

a)

Dopa Decarboxylase

b)

Dopamine B-Hydroxylase

c)

Tyrosine Hydroxylase

d)

L-Amino acid Decarboxylase

18.

By which of the following are the domains of the G protein reversible binding achieved? Select all that apply

a)

ion-ion interactions

b)

H-bonding

c)

π interactions

d)

van der Waals interactions

19.

Know this !!!

a)

Yes

b)

No

20.

Using the diagram which of the following statements best describe number 1 ? Select all that apply

a)

Not essential for activity

b)

removal increases stability (COMT) and increases lipophilicity

c)

removal of para (4’) OH modulates β activity (general ↓) and (↑ in β2 selectivity)

d)

Decreases lipophilicity and CNS penetration; enhances binding at α and β receptors

21.

Using the diagram which of the following statements best describe number 2 ?

a)

Not essential for activity

b)

R substitution decreases

rate of MAO inactivation

c)

Decreases lipophilicity and CNS penetration; enhances binding at α and β receptors

d)

Needed for activity

22.

Using the diagram which of the following statements best describe number 3 ? Select all that apply

a)

“R” stereochemistry here enhances binding at α and β receptors

b)

Needed for activity (basic nitrogen)

c)

R substitution decreases

rate of MAO inactivation;

alkyl groups increase β selectivity; larger groups increase β2 selectivity

d)

Not essential for activity

23.

Using the diagram which of the following statements best describe number 1 ?

a)

“R” stereochemistry here enhances binding at α and β receptors

b)

Not essential for activity

c)

Methylation increases stability (MAO) and lipophilicity

d)

All of the above are correct

24.

Using the diagram which of the following statements best describe number 2 ?

a)

Methylation increases stability (MAO) and lipophilicity

b)

“R” stereochemistry here enhances binding at α and β receptors

c)

Not essential for activity

d)

Decreases lipophilicity and CNS penetration

25.

Using the diagram which of the following statements best describe the red areas? Select all that apply

a)

Needed for activity

b)

aromatic ring

c)

basic nitrogen

d)

two carbon spacer

26.

Which of the following best describes the Rule of thumb for receptor selectivity?

a)

the smaller the derivative, the greater the β2 selectivity

b)

the larger the derivative, the greater the β2 selectivity

27.

Which of the following statements are TRUE about the Receptor Selectivity? Select all that apply

a)

Alkyl substituents on nitrogen increase β selectivity (extended hydrophobic pocket)

b)

Para-hydroxyl (4’) more important for β activity

c)

Alkyl substituents on nitrogen decrease β selectivity (extended hydrophobic pocket)

d)

Para-hydroxyl (4’) NOT important for β activity

28.

Para-hydroxyl (4’) more important for β activity and also affects β1 vs β2 selectivity.

a)

True

b)

False

29.

Which of the following statements best describe this image ?

a)

Contraction of arterial strips (alpha 1 receptor)

b)

Relaxation of bronchial smooth muscle (beta 2 receptor)

c)

Augmented contraction of heart (beta 1 receptor)

d)

All of them are correct

30.

Which of the following statements best describe this image ?

a)

Contraction of arterial strips (alpha 1 receptors)

b)

Relaxation of bronchial smooth muscle (beta 2 receptor)

c)

Augmented contraction of heart (beta 1 receptor)

d)

All of them are correct

31.

Which of the following statements best describe this image ?

a)

Relaxation of bronchial smooth muscle (beta 2 receptor)

b)

Contraction of arterial strips (alpha 1 receptors)

c)

Augmented contraction of heart (beta 1 receptor)

d)

All of the above are correct

32.

Which of the following the cardiovascular effects of agonists include? Select all that apply

a)

α1: vasoconstriction

b)

α2: decreases central sympathetic outflow

c)

β1: increases heart rate and contractility

d)

β2: airway and vascular dilation

33.

Which of the following statements are TRUE about the Direct Acting of Sympathomimetic? Select all that apply

a)

endogenous catecholamines

b)

bind the adrenergic receptors (ARs)

c)

α1 and β agonists, α2 antagonist

d)

do not bind the ARs

34.

Which of the following statements are TRUE about the Indirect Acting of Sympathomimetic? Select all that apply

a)

releasing agents

b)

do not bind the ARs

c)

reuptake inhibitors

d)

MAO/COMT inhibitors

e)

multiple MOA (or amphetamine-like)

35.

Which of the following statements are TRUE about Sympathomimetics? Select all that apply

a)

Direct acting and Indirect acting only

b)

Direct acting can be Selective or Non Selective

c)

Direct acting, Indirect acting and Mixed acting

d)

Norepinephrine is a Non Selective under the direct acting

36.

Which of the following is a Non Selective (Direct Acting) under Sympathomimetics?

a)

Dopamine

b)

Epinephrine

c)

Norepinephrine

d)

Phenylephrine

37.

Which of the following statements are TRUE about Endogenous Catecholamines? Select all that apply

a)

no oral availability; do not cross BBB; COMT and MAO substrates

b)

will generally be used in emergency/critical care settings (hemodynamic support

inotropic support)

c)

CV adverse reactions (hemodynamics, palpitations, arrhythmias)

d)

CNS adverse reactions (headache, anxiety)

e)

pregnancy category C

38.

The drug shown below selective binds to which receptor?

a)

α2

b)

β1

c)

α1

d)

β2

39.

Which of the following statements are TRUE about Direct Acting: α1 Agonists? Select all that apply

a)

two major classes: phenylethanolamines, imidazolines

b)

Mediate vasoconstriction

c)

Mediate vasodilation

d)

Only one class

40.

Which of the following statements are TRUE about this image? Select all that apply

a)

Mediate vasoconstriction

b)

phenylethanolamine

c)

removal of 4’ hydroxy groups

d)

Direct Acting: α1 Agonist

41.

Which of the following statements are TRUE about this image? Select all that apply

a)

strong bases (ionized)

b)

imidazoline

c)

potent vasoconstrictors, topical use only

d)

alkyl substitution at one or both   ortho positions required

e)

bulky, lipophilic groups at other positions enhance α1 selectivity

42.

Which of the following statements are TRUE about this image? Select all that apply

a)

α selectivity (peripheral)- poor CNS penetration

b)

Phenylephrine (Sudafed PE®)

c)

IV, oral, intracavernous administration

d)

Use for hypotension, nasal decongestant

and ischemic priapism

e)

Adverse reactions such as mydriasis / blurred vision and CV (Hypertension and Arrhytmias)

43.

Which of the following α1 Selective Imidazolines its use should be restricted to ≤ 3 days?

a)

Oxymetazoline (Afrin®)

b)

Tetrahydrozoline (Visine®)

c)

Naphazoline (Redness Relief®)

d)

Xylometazoline

44.

Overuse of medications α1 Selective Imidazolines has possible Breakthrough systemic effects.

a)

True

b)

False

45.

A patient looking for a α1 Selective Imidazoline for redness relief on the eyes must use which of the following drugs?

a)

Naphazoline

b)

Xylometazoline

c)

Tetrahydrozoline (Visine®)

d)

Oxymetazoline (Afrin®)

46.

Which of the following statements are TRUE about Direct Acting: β Agonists? Select all that apply

a)

Increase cardiac output

b)

Use for – inotropic support, bradycardia, arrhythmias, AV nodal block

c)

Increase smooth muscle relaxation and ADR for hypokalemia

d)

usually inhalation or IV administration and induce insulin release

e)

Selectivity =

4’ hydroxy and size of R group on amine

47.

Which of the following statements are TRUE about Isoproterenol/Isoprenaline (Isuprel®)? Select all that apply

a)

β selectivity (1 and 2)

b)

Metabolism: COMT, conjugation

longer duration than endogenous catecholamines

c)

Metabolism: COMT, conjugation

d)

bronchodilation, ↑ HR and contractility

↑ systolic BP, ↓ diastolic BP

e)

shorter duration than endogenous catecholamines

48.

Which of the following is predominantly alpha agonist that causes vasoconstriction and increased systolic and diastolic BP with a reflex tachycardia?

a)

Isoproterenol

b)

Norepinephrine

49.

Which of the following is a B2 agonist and also a vasodilator which strongly increases cardiac force and rate (B1 agonist). Mean arterial pressure falls.

a)

Isoproterenol

b)

Norephinephrine

50.

We can say Epinephrine combines both actions of Norepinephrine and Isoproterenol .

a)

True

b)

False

51.

Which of the following statements are TRUE about Dobutamine (Dobutrex®)? Select all that apply

a)

β1 ≥ β2 activity

b)

net effect: ↑ HR and contractility; mild vasodilation

c)

stereochemistry: R-(+) isomer β1/β2 agonist and α1 antagonist; S-(-) isomer β1 and α1 agonist (racemic administration)

d)

Indicated for decompensated systolic heart failure

52.

Which of the following statements are TRUE about Direct Acting: β2 Agonists? Select all that apply

a)

β2 selectivity enhanced by modification of catechol group and large R group on amine

b)

Mediate bronchodilation

c)

long acting β2 agonists (LABAs) utilize very large, lipophilic R groups

d)

Used for respiratory conditions

e)

resorcinol or hydroxymethyl group (these changes also increase stability by decreasing susceptibility to COMT and MAO)

53.

Which of the following statements are TRUE about Albuterol (Ventolin®), Levalbuterol (Xopenex®) which causes ADR like CNS (excitement, nervousness) CV disturbances (high doses) tremor

paradoxical asthma exacerbation? Select all that apply

a)

Metabolism: conjugation

peak effect 10-120 minutes; duration 2-6 hours

b)

β2 selectivity

c)

Indications are for –bronchospasm/asthma

prevention of exercise induced asthma

hyperkalemia (off label)

d)

S-(+) isomer: pro-inflammatory and slower clearance than R-(-) isomer

e)

short acting β2 agonist (SABA)

54.

Which of the following Extended Duration β2 Agonists drugs have a Boxed Warning: asthma-related death? Select all that apply

a)

Albuterol

b)

Levalbuterol

c)

Salmeterol (Serevent®)

d)

Vilanterol (Breo®/Anoro® Ellipta®)

55.

Which of the following drugs have a Boxed warning: asthma-related death (and pediatric and adolescent hospitalization)?

a)

Salmeterol (Serevent®)

b)

Vilanterol (Breo®/Anoro® Ellipta®)

56.

Which of the following Extended Duration β2 Agonists is NOT indicated for asthma and only for COPD?

a)

Vilanterol

b)

Anoro® Ellipta®

c)

Breo Ellipta

d)

Salmeterol (Serevent®)

57.

Which of the following Extended Duration β2 Agonists is a Long-acting β2 agonist (LABA) (highly β2 selective, partial agonist), slow onset (0.5-2 hours); long duration (12 hours)?

a)

Salmeterol (Serevent®)

b)

Vilanterol (Breo®/Anoro® Ellipta®)

58.

Which of the following Extended Duration β2 Agonists is a Long-acting β2 agonist (LABA) (ultra-long acting), faster onset (<1 hour); very long duration (up to 24 hours)?

a)

Vilanterol (Breo®/Anoro® Ellipta®)

b)

Salmeterol (Serevent®)

59.

Which of the following β2 Agonists drugs are considered Short-Acting (3-4h)? Select all that apply

a)

Albuterol

b)

Salmeterol

c)

Vilanterol

d)

Levalbuterol

60.

Which of the following statements are TRUE with this image? Select all that apply

a)

Olodaterol

b)

Selective binds to alpha receptor

c)

selective binds to B2 receptor

d)

Ultra Long-Acting (~24 hours)

e)

Vilanterol is under this classification

61.

We can say all LABAs have the Boxed Warning for asthma-related death when used as monotherapy controller meds.

a)

True

b)

False

62.

Which of the following β2 Agonists drugs have the Boxed Warning for asthma-related death when used as monotherapy controller meds? Select all that apply

a)

Salmeterol

b)

Oladaterol

c)

Formoterol

d)

Vilanterol

e)

Albuterol

63.

Which of the following statements are TRUE about Mirabegron (Myrbetriq®) Select all that apply

a)

ADRs:

hypertension

UTI

headache and muscle pain

b)

Direct Acting:β3 Agonist

c)

Indication is for overactive bladder (OAB)

d)

relaxes detrusor muscle in bladder

metabolic effects: lipolysis

64.

. Ephedrine (Akovaz) and Pseudoephedrine (Sudafed) are considered Mixed Acting Sympathomimetics and are diastereomers.

a)

True

b)

False

65.

Which of the following statements are TRUE about Ephedrine (Akovaz®) and Pseudoephedrine (Sudafed®) with ADR like CV (HR and BP), CNS (insomnia, anxiety, mania) ? Select all that apply

a)

not metabolized by COMT or MAO

b)

ephedrine: hypotension, N/V prevention

pseudoephedrine: nasal congestion

c)

Direct action: non-selective α and β agonist

d)

pseudoephedrine: weaker agonist than ephedrine; less BBB penetration

e)

Regulation: Combat Methamphetamine Epidemic Act of 2005

OTC sales restrictions (for example: max 3.6 g/day, 9.0 g/month)

66.

A substance that inhibits activity of the sympathetic nervous system

a)

Sympathomimetics

b)

Sympatholytics

67.

Which of the following statements are TRUE about Sympatholytics? Select all that apply

a)

Direct (peripherally) acting: bind the ARs

b)

Indirect acting: principal activity at presynaptic adrenergic receptors (ARs) –or– do not bind AR

α2 agonists (centrally acting)

c)

A substance that inhibits activity of the sympathetic nervous system

d)

Ephedrine and pseudoephedrine are diastereomers

68.

We can say Direct (peripherally) acting Sympatholytics: bind the ARs and are antagonists.

a)

True

b)

False

69.

We can say Indirect acting Sympatholytics do not bind AR and are agonists.

a)

True

b)

False

70.

Understand this

a)

Yes

b)

No

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