ADRENOCEPTOR AGONISTS & SYMPATHOMIMETIC DRUGS

1. A bronchial smooth muscle contains what? Beta-2 receptor

2. Effects of non-selective beta receptor agonist?

- increased cardiac output,

- decrease peripheral arterial resistance
- decrease the mean pressure

3. Effects of relatively pure alpha agonist:

- reflex bradycardia
- increase peripheral arterial resistance

*Because alpha1-agonists produce systemic vasoconstriction, the work of the heart

increases.

4. Types of agents are beta receptor agonists:

* B1-agonists
- cardiac stimulants; used to treat cardiogenic shock, acute heart failure,
bradyarrhythmias

- Denopamine
- Dobutamine
- Dopexamine (β1 and β2)
- Epinephrine (non-selective)
- Isoprenaline, isoproterenol (β1 and β2)
- Prenalterol
- Xamoterol

*B2-agonists
- smooth muscle relaxants; used to treat asthma and COPD

- Arformoterol
- Buphenine
- Clenbuterol
- Dopexamine (β1 and β2)
- Epinephrine (non-selective)
- Fenoterol
- Formoterol
- Isoetarine
- Levosalbutamol (INN), levalbuterol (USAN)
- Orciprenaline (INN), metaproterenol (USAN)
- Pirbuterol
- Procaterol
- Ritodrine
- Salbutamol (INN), albuterol (USAN)
- Salmeterol
- Terbutaline

*B3-agonists
- Enhancement of lipolysis in adipose tissue, thermogenesis in skeletal muscle

- Amibegron
- Mirabegron
- Nevibolol
- Solabegron
- Vibegron

5. Types of Beta adrenoreceptor subtypes contained in all ff. tissues:

- Bronchial muscles
- Heart
- Fat cells

6. Effects of Beta1 receptor stimulation:

- increase heart contractility, heart conduction velocity and heart relaxation.
- Tachycardia

7. Efects of Beta2 receptor stimulation:

- relaxation of bladder, uterus
- tachycardia

8. What are Catecholamines?

- amines that function as neurotransmitters and hormones within the body. 
- Dopamine, epinephrine (adrenaline), and norepinephrine are the
main catecholamines.
9. Characteristics of Dobutamine:
- a direct-acting synthetic catecholamine.
- one of positive inotropic agent, that can increase myocardial contractility
- is a medication used in the treatment of cardiogenic shock and heart failure.
- Increased cardiac output without significantly increased heart rate.
- Onset of action: seen within 2 minutes.

10. Characteristics of Ephedrine:

- An alpha- and beta-adrenergic agonist.
- comes from the herb known as Ephedra.
- it is a mild CNS stimulant.
- It causes tachyphylaxis (lessening of drug effect with repeated doses) with re-
peated administration

11. Characteristics of Epinephrine:

- also known as adrenaline.
- active sympathomimetic hormone from the adrenal medulla.
- an alpha-Adrenergic Agonist, and beta-Adrenergic Agonist, and Catecholamine.
- drug of choice in the emergency treatment of severe acute anaphylactic reactions,
insect stings, food, or other allergens.

12. Characeristics of Methoxamine:

- An alpha-1 adrenergic agonist increases both systolic and diastolic blood pressure.
- Indicated for the treatment and management of hypotension.

13. Characteristics of Salmeterol:

- A selective ADRENERGIC BETA-2 RECEPTOR agonist that functions as a
BRONCHODILATOR when administered by inhalation.
- used in treatment of asthma and chronic obstructive pulmonary disease (COPD).

14. Compared with epinephrine, ephedrine produces what features?

- Ephedrine has greater stimulating effect upon the CNS.
- It has a longer duration of action.
- Ephedrine is effective when given orally.

15. Compared with epinephrine, norepinephrine produces what type of effects?

- norepinephrine can also make your blood vessels become narrower, increasing blood
pressure.
- norepinephrine has more of an effect on the blood vessels and mainly produced in the
nerves.
- Norepinephrine is continuously released into circulation at low levels while
epinephrine is only released during times of stress.

16. Direct effects on the heart are determined largely by:

- Beta-1 receptor

17. Distribution of alpha adrenoreceptor subtypes is associated with all of the following
tissues except those of:
- Heart, only upregulation in heart disease.

18. What are the common effects of Ephedrine?

- nervousness,insomnia, vertigo, headache, tachycardia, palpitation and sweating.
Some patients have nausea, vomiting and anorexia.

19. Epinephrine decreases intracellular camp levels by acting on where?

- Alpha-2 receptor

20. Epinephrine is used in the treatment of what disorders?

- open-angle glaucoma, anaphylactic shock, asthma attacks.

21. What are the effects of Epinephrine?

- anxiety, apprehensiveness,
 restlessness, tremor, weakness, 
dizziness, sweating, palpitations,
nausea and vomiting, headache, and respiratory difficulties.

22. Hyperglycemia induced by epinephrine is due to what?

- Gluconeogenesis (beta2)
- Inhibition of insulin secretion (alpha2)
- Stimulation of glycogenolysis (beta2)

23. In which of the following tissues both alpha and beta 1 adrenergic stimulation
produces the same effect?
- Blood vessels.
*Beta1 receptors on kidney promote renin release, which increases blood pressure.
Alpha1 receptor activation increases vas-
cular resistance too.

24. Indicate the agent of choice in the emergency theraphy of anaphylactic shock:
- Epinephrine.
25. Indicate the alpha-2 selective agonist:
- Guanabenz

26. Indicate the beta-1 selective agonist:

- Dobutamine

27. Indicate the direct-acting symphathomimetic, which is an alpha-1, alpha-2, beta-1

receptor agonist?
- Noradrenaline

28. Indicate the drug, which is a direct-acting both alpha and beta receptor agonist:
Epinephrine & Norepinephrine

29. Indicate the indirect-acting sympathomimetic agent:

- Ephedrine

30. Indicate the long-acting topical decongestant agents:

- Xylometazoline (alpha-1)

31. Indicate the sympathomimetic agent, which is combined with a local anesthetic to
prolong the duration of infiltration nerve block:
- Epinephrine

32. Indicate the sympathomimetic drug, which is used in a hypotensive emergency:

- Norepinephrine / Phenylephrine

33. Indicate the sympathomimetic, which may be useful in the management of cardiac
arrest:
- Epinephrine

34. Indicate the sympathomimetic, which cause hypotension, presumably because of

cloni-dine-like effect:
- Isoproterenol
* beta1,2 agonist increases HR, which decreases blood pressure re-
flexively "Isoproterenol is a nonselective β agonist; it activates both β1 and β2 re-
ceptors. The net effect is to maintain or slightly increase systolic pressure and to
lower diastolic pressure, so that mean blood pressure is decreased

35. Indirect action includes all of the following properties EXCEPT:

- Interaction with adrenoreceptors

36. What is Isoproterenol?

- Nonselective beta receptor agonist
- used mainly as bronchodilator and heart stimulant.

37. What are the actions of Isoproterenol?

- Stimulates both β1 and β2 adrenergic receptors.

38. Norepinephrine produces what?

-

39. Sympathetic stimulation is mediated by:

- release of norepinephrine from nerve terminals & adrenal medulla
- activation of Adrenorceptors on postsynaptic sites

40. The adverse effects of sympathomimetics:

- Ventricular arrhythmias
- Cerebral hemorrhage or pulmonary edema
- Myocardial infraction

41. The effects of sympathomimetics on blood pressure are associated with their effects
on:
- heart rate
- peripheral resistance
- cardiac output

42. Which of the following agents is a nonselective beta receptor agonist?

- Isoproterenol

43. Which of the following agents is an alfa1 alfa2 beta 1 beta 2 receptor agonist?
- Epinephrine

44. Which of the following agents is an alpha1-selective agonist?

- Phenylephrine, Methoxamine

45. Which of the following agents is an alpha-2 selective agonist agonist with ability to
promote constriction of the nasal mucosa?
- Oxymetazoline
46. Which of the following direct-acting drugs is a relatively pure alpha agonist, an
effective mydriatic and decongestant and can be used to raise blood pressure?
- Phenylephrine - alpha1 agonist

47. Which of the following drugs causes bronchodilation without significant cardia
stimulation?
- Terbatuline -Beta2 selective

48. Which of the following effects is associated with beta3-receptor stimulation?

- Lipolysis

49. Which of the following is related to direct beta1-adrenoreceptro stimulation?

- Tachycardia

50. Which of the following statement is not correct?

a) Alpha agonists cause miosis

b) Alpha agonists cause mydriasis
c) Beta antagonists decrease the production of aqueous humor
d) Alpha agonists increase the outflow of aqueous humor from the eye

a.) Alpha agonists cause miosis

51. Which of the following statements is not correct?

Nasal Muscosa blood vessels have predominantly beta receptors and constrict in the
presence of epinephrine and norepinephrine - (alpha receptors predominantly)
52. Which of the following statements is not correct?
a) Epinephrine acts on both alpha- and beta-receptors
b) Norepinephrine has a predominantly beta action
c) Phenylephrine has a predominantly alpha action
d) Isoproterenol has a predominantly beta action

*Norepinephrine has a predominantly beta action - mixed alpha and beta agonist

53. Which of the following sympathomimetics acts indrectly?

- Ephedrine - releases catecholamines, inhibits MAO, as well as direct activation of

alpha and beta adrenoreceptors.

54. Which of the following sympathomimetics is a beta2-selective agonist?

- Terbutaline

55. Which of the following sympathomimetics is an effective mydriatic?

- Phenylephrine -alpha1 pupillary dilator muscle

56. Which of the following sympathomimetics is preferable for the emergency therapy
of cardiogenic shock?
- Dobutamine -beta1 agonist so specific to the heart

57. Which of the following sympathomimetics is preferable for the treatment of chronic
orthostatic hypotension?
- Midodrine - alpha1 agonist

58. Which of the following sympathomimetics is related to short-acting topical

decongestant agents?
- Phenylephrine - alpha1

59. Which of the following sympathomimetics is used in the therapy of bronchial

asthma?
- Formoterol (Beta-2 agonist)

60. Which of the following topical decongestant agents is an alfa1-selective agonists?

- Phenylephrine

61. Types of Alpha-receptor stimulatants:

- Alpha-1 & Alpha-2 agonist

Additional Information
  Beta adrenoreceptor subtypes are contained in all of the following tissues
EXCEPT:
a) Bronchial muscles
b) Heart
c) Pupillary dilator muscle
d) Fat cells

Pupillary dilator muscle - a beta antagonist will decrease aqueous humor outflow

 Catecholamine includes the following EXCEPT:

a) Ephedrine
b) Epinephrine
c) Isoproterenol
d) Norepinephrine

Ephedrine - no catechol

 A relatively pure alpha agonist causes all of the following effects EXCEPT:
a) Increase peripheral arterial resistance
b) Increase venous return
c) Has no effect on blood vessels
d) Reflex bradycardia

 A nonselective beta receptor agonist causes all of the following effects EXCEPT:
a) Increase cardiac output
b) Increase peripheral arterial resistance
c) Decrease peripheral arterial resistance
d) Decrease the mean pressure

Increase peripheral arterial resistance - Isoproterenol example

 All of the following agents are beta receptor agonists EXCEPT:

a) Epinephrine
b) Isoproterenol
c) oxymetazoline
d) Dobutamine

Oxymetazoline - alpha agonist, a nasal decongestant

  Beta1 receptor stimulation includes all of the following effects EXCEPT:
a) Increase in heart contractility
b) Bronchodilation
c) Tachycardia
d) Increase in conduction velocity in the atrioventricular node

 Beta2 receptor stimulation includes all of the following effects EXCEPT:

a) Stimulation of renin secretion
b) Fall of potassium concentration in plasma
c) Relaxation of bladder, uterus
d) Tachycardia

 Which of the following agents is an alpha2-selective agonist?

a) Norepinephrine
b) Clonidine
c) Ritodrine
d) Ephedrine

 Epinephrine produces all of the following effects EXCEPT:

a) Positive inotropic and chronotropic actions on the heart (beta1 receptor)
b) Increase peripheral resistance (alpha receptor)
c) Uterine contraction
d) Skeletal muscle blood vessel dilatation (beta2 receptor)

Uterine contraction - beta2 receptors cause relaxation

 Epinephrine produces all of the following effects EXCEPT:

a) Decrease in oxygen consumption
b) Bronchodilation
c) Hyperglycemia
d) Mydriasis

Decrease in oxygen consumption - increase in HR cycles blood faster and more oxygen
uptake

 Characteristics of oxymetazoline include all of the following EXCEPT:

a) It is a direct-acting alpha1-receptor agonist
b) It increases heart rate, contractility and cardiac output
c) It causes reflex bradycardia
d) It increases total peripheral resistance

 Isoproterenol is:
a) Both an alpha- and beta-receptor agonist
b) beta1-selective agonist
c) beta2-selective agonist
d) Nonselective beta receptor agonist

 Isoproterenol produces all of the following effects EXCEPT:

a) Increase in cardiac output
b) Fall in diastolic and mean arterial pressure
c) Bronchoconstriction
d) Tachycardia

 Characteristics of dobutamine include all of the following EXCEPT:

a) It is a relatively beta1-selective synthetic catecholamine
b) It is used to treat bronchospasm
c) It increases atrioventricular conduction
d) It causes vasodilation in renal blood vessels by acting on D1 receptors.

Two answers:
b) It is used to treat bronchospasm - it treats heart failure
d) It causes vasodilation in renal blood vessels by acting on D1 receptors.

 Characteristics of salmeterol include all of the following EXCEPT:

a) It is a potent selective beta2 agonist
b) It causes uterine relaxation
c) It stimulates heart rate, contractility and cardiac output
d) It is used in the therapy of asthma

 Characteristics of ephedrine include all of the following EXCEPT:

a) It acts primarily through the release of stored cathecholamines
b) It is a mild CNS stimulant
c) It causes tachyphylaxis (lessening of drug effect with repeated doses) with repeated
administration
d) It decreases arterial pressure

 Ephedrine causes:
a) Miosis
b) Bronchodilation
c) Hypotension
d) Bradycardia

 Compared with epinephrine, ephedrine produces all of the following features

EXCEPT:
a) It is just a direct-acting sympathomimetic
b) It has oral activity
c) It is resistant to MAO and has much longer duration of action
d) Its effects are similar to epinephrine, but it is less potent

 Indicate the sympathomimetic drug, which is used in a neurogenic hypotensive

emergency:
a) Xylometazoline
b) Ephedrine
c) Terbutaline
d) Phenylephrine

 Which of the following sympathomimetics is used in the therapy of bronchial

asthma?
a) Formoterol
b) Norepinephrine
c) Methoxamine
d) Dobutamine

Formoterol -beta 2 selective, long acting

 The adverse effects of sympathomimetics include all of the following EXCEPT:

a) Drug-induced parkinsonism
b) Cerebral hemorrhage or pulmonary edema
c) Myocardial infarction
d) Ventricular arrhythmias

 Which of the following are probable signs of the anaphylactic reaction to bee
stings?
(A) Bronchodilation, tachycardia, hypertension, vomiting, diarrhea
(B) Bronchospasm, tachycardia,hypotension,laryngeal edema
(C) Diarrhea, bradycardia, vomiting
(D) Laryngeal edema, bradycardia, hypotension, diarrhea (E) Miosis, tachycardia,
vomiting, diarrhea
Bronchospasm, tachycardia, hypotension, laryngeal edema -reflex tachycardia due
to hypotension, otherwise all parasympathetic effects

 If this child has signs of anaphylaxis, what is the treatment of choice?

(A) Diphenhydramine (an antihistamine)
(B) Ephedrine
(C) Epinephrine
(D) Isoproterenol
(E) Methylprednisolone (a corticosteroid)

 A group of volunteers are involved in a phase 1 clinical trial of a new autonomic

drug. When administered by intravenous bolus, the blood pressure increases.
When given orally for 1 week, the blood pressure decreases. Which of the
following standard agents does the new drug most resemble?
(A) Atropine
(B) Clonidine
(C) Phentolamine (an α blocker)
(D) Phenylephrine
(E) Propranolol (a β blocker)

 Your 30-year-old patient has moderately severe new onset asthma, and the
physician prescribes a highly selective β2 agonist inhaler to be used when
needed. In considering the possible drug effects in this patient, you would note
that β2 stimulants can cause:
(A) Direct stimulation of renin release
(B) Hypoglycemia
(C) Itching due to increased cGMP (cyclic guanine monophosphate) in mast cells
(D) Skeletal muscle tremor
(E) Vasodilation in the skin

Skeletal muscle tremor - albuterol side effect

 Direct acting- selective:

*a1- Phenylephrine
*a2- Clonidine
*B1- Dobutamine
*B2- Terbutaline
 Direct-acting- non-selective:
*a1,a2- Oxymetazoline
*B1,B2- Isoproterenol
*a1,a2,B1,B2- Epinephrine
*a1,a2,B1- Norepinephrine

 Mixed acting ephedrine:

- (a1,a2,B1,B2 and releasing agent)

 Indirect acting- releasing agents

*Amphetamine
*Tyramine

 Indirect acting- uptake inhibitor:

*Cocaine

 Indirect acting- MAO/COMT inhibitors:

*Pargyline
*Entacapone