Updated: 7/6/2021

Sympathomimetics

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sympmathomimetics 
 
Direct Sympathomimetics
 
Drug Receptor Selectivity Clinical Applications
Epinephrine

β  > α
 

• Anaphylaxis
• Cardiac arrest

• Glaucoma (open angle)
• Asthma and broncho spasms
• Hypotension

Norepinephrine 

 

α1 > α2 > β

• Shock
• Severe hypotension (but ↓ renal perfusion)
• Causes reflex bradycardia
Midodrine Selective α1 agonist • Orthostatic hypotension
Phenylephrine α1 > α • Pupillary dilation and glaucoma (wide angle)
• Vaso constriction
• Nasal decongestion
Clonidine, α-methyldopa Centrally acting α2-agonists, ↓ central adrenergic outflow • Hypertension
• Does not ↓ blood flow to the kidney
Isoproterenol β1= β2 • Heart block
Dopamine

low dose (vasodilation, naturiesis): D1 = D2
medium dose (tachycardia): β1
high dose (vaso- constriction): α1 , inotropic and chronotropic

• Shock and ↑ renal perfusion
• Heart failure
Fenoldopam Selective D1 agonist • Hypertension
Bromocriptine Selective D2 agonist  • Parkinson's disease
• Prolactinemia
Dobutamine β1> β2, positive inotropic effect    • Cardiogenic shock
• Acute heart failure
• Cardiac stress testing
Metaproterenol, albuterol, salmeterol  Selective β2 agonists • Albuterol and metaproterenol for acute asthma
• Salmeterol for long-term treatment

Ritodrine

Terbutaline

Selective β2 agonists • Reduction of premature uterine contractions

 

 

Indirect Sympathomimetics
 
Drug
Mechanism
Clinical Applications
Amphetamine Releases stored catecholamines
  • Narcolepsy
  • Obesity
  • Attention deficit disorder
Ephedrine Releases stored catecholamines
  • Nasal decongestion
  • Urinary incontinence
  • Hypotension
Cocaine  Reuptake inhibitor
  • Causes vasoconstriction and local anesthesia

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Questions (13)
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(M1.PH.15.6000) In an attempt to create other selective dopamine 1 (D1) agonists, a small pharmaceutical company creates a cell-based chemical screen that involves 3 modified receptors - alpha 1 (A1), beta 1 (B1), and D1. In the presence of D1 stimulation, the cell produces an mRNA that codes for a fluorescent protein; however, if the A1 or B1 receptors are also stimulated at the same time, the cells will degrade the mRNA of the fluorescent protein thereby preventing it from being produced. Which of the following would best serve as a positive control for this experiment?

QID: 106941
1

Bromocriptine

19%

(40/209)

2

Dobutamine

11%

(24/209)

3

Dopamine

24%

(50/209)

4

Epinephrine

15%

(32/209)

5

Fenoldopam

26%

(55/209)

M 1 D

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(M1.PH.15.75) A 75-year-old male arrives by ambulance to the emergency room severely confused. His vitals are T 40 C, HR 120 bpm, BP 80/55 mmHg, RR 25. His wife explains that he injured himself about a week ago while cooking, and several days later his finger became infected, oozing with pus. He ignored her warning to see a doctor and even refused after he developed fever, chills, and severe fatigue yesterday. After being seen by the emergency physician, he was given antibiotics and IV fluids. Following initial resuscitation with IV fluids, he remains hypotensive. The ED physicians place a central venous catheter and begin infusing norepinephrine. Which of the following receptors are activated by norepinephrine?

QID: 106852
1

Alpha 1

6%

(5/77)

2

Alpha 2

3%

(2/77)

3

Alpha 1, Alpha 2, Beta 1

53%

(41/77)

4

Alpha 1, Alpha 2, Beta 1, Beta 2

22%

(17/77)

5

Alpha 1, Beta 1, Dopamine 1

8%

(6/77)

M 3 E

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(M1.PH.15.1) A high-throughput screen to identify new sympathomimetic compounds was developed such that a transgenic line of cells was created that contained the alpha-1 (red), alpha-2 (yellow), beta-1 (green) and beta-2 (blue) receptors. When each of the receptors was activated a different fluorescent protein was expressed and new compounds with different properties could be identified by the fluorescence that they induced. Compound 7583 selectively induced the expression of the blue fluorescent protein. Which of the following known sympathomimetic medications if administered would similarly result in expression of only the blue fluorescent protein?

QID: 107079
1

Albuterol

70%

(135/192)

2

Midrodrine

5%

(9/192)

3

Epinephrine

9%

(17/192)

4

Isoproterenol

10%

(20/192)

5

Fenoldopam

4%

(7/192)

M 1 D

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(M1.PH.13.46) A 58-year-old male is diagnosed with hypertension and started on daily propranolol after failing antihypertensive therapy with other medications. Three months later, his blood pressure appears to be adequately controlled on this therapy. While working in his garden one afternoon, the patient is stung by a wasp and experiences a severe anaphylactic reaction that is subsequently treated with epinephrine. Which of the following effects would be expected upon administration of this epinephrine treatment?

QID: 100562
1

Decreased bronchodilation

9%

(26/285)

2

Increased motility of the gastrointestinal tract

2%

(6/285)

3

Decreased heart rate

21%

(61/285)

4

Decreased blood pressure

7%

(19/285)

5

Increased heart rate

58%

(166/285)

M 3 E

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(M1.PH.13.107) An 82-year-old male with congestive heart failure experiences rapid decompensation of his condition, manifesting as worsening dyspnea, edema, and increased fatigue. Labs reveal an increase in his serum creatinine from baseline. As part of the management of this acute change, the patient is given IV dobutamine to alleviate his symptoms. Which of the following effects occur as a result of this therapy?

QID: 100623
1

Slowed atrioventricular conduction velocities

6%

(15/241)

2

Increased myocardial oxygen consumption

53%

(127/241)

3

Decreased heart rate

12%

(29/241)

4

Increased systemic vascular resistance due to systemic vasoconstriction

22%

(52/241)

5

Decreased cardiac contractility

5%

(12/241)

M 1 E

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(M1.PH.13.86) A 24-year-old male being treated for syphilis is given penicillin. Shortly after receiving the first dose the patient becomes dyspneic. Immediate assessment of the patient reveals a heart rate of 150 bpm and a blood pressure of 88/50. The first-line drug used in the treatment of this condition has what effect on alpha and beta autonomic receptors?

QID: 100602
1

Alpha-1 agonism, beta-1 agonism

43%

(122/286)

2

Alpha-1 agonism, beta-1 antagonism

22%

(64/286)

3

Alpha-1 antagonism, beta-1 agonism

20%

(57/286)

4

Alpha-1 antagonism, beta-1 antagonism

6%

(18/286)

5

Alpha-1 agonism, no effect on beta-1

6%

(17/286)

M 1 D

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(M1.PH.13.77) A 35-year-old male presents to his primary care physician with complaints of seasonal allergies. He has been using intranasal vasoconstrictors several times per day for several weeks. What is a likely sequela of the chronic use of topical nasal decongestants?

QID: 100593
1

Epistaxis

17%

(37/215)

2

Hypertension

9%

(19/215)

3

Permanent loss of smell

6%

(13/215)

4

Persistent nasal crusting

31%

(67/215)

5

Persistent congestion

31%

(67/215)

M 4 E

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Evidence (14)
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