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Pharm > Sympathomimetics > Flashcards

Sympathomimetics Flashcards

1
Q

List the G-protein/effector/2nd messengers for alpha 1 receptors:

A
  • G-protein: Gq (stimulatory)
  • effector: Phospholipase C
  • 2nd messengers: IP3, DAG, Ca2+
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2
Q

List the G-protein/effector/2nd messengers for alpha 2 receptors:

A
  • G-protein: Gi (inhibitory)
  • effector: adenylate cyclase
  • 2nd messenger: cAMP
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3
Q

List the G-protein/effector/2nd messengers for beta 1 receptors:

A
  • G-protein: Gs (stimulatory)
  • effector: adenylate cyclase
  • 2nd messenger: cAMP
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4
Q

List the G-protein/effector/2nd messengers for beta 2 receptors:

A
  • G-protein: Gs (stimulatory)
  • effector: adenylate cyclase
  • 2nd messenger: cAMP
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5
Q

List the 5 2nd messengers involved in adrenergic G-protein coupled receptors:

A
  • cAMP
  • cGMP
  • IP3
  • Ca2+
  • DAG
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6
Q

Stimulation of alpha 1 receptors results in what effect on Ca2+?

A

increased Phospholipase C –> increased Ca2+

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7
Q

Simulation of alpha 2 receptors results in what?

A

inhibition of adenylate cyclase –> decreased cAMP

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8
Q

Stimulation of beta 1 receptors results in what?

A

stimulation of adenylate cyclase –> increased cAMP

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9
Q

Stimulation of beta 2 receptors results in what?

A

stimulation of adenylate cyclase –> increased cAMP

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10
Q

Beta 2 receptors are primarily found in the (heart/lungs) and have a (higher/lower/equal) affinity for Epi.

A
  • lungs
  • higher
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11
Q

Beta 1 receptors are primary found in the (heart/lungs) and have a (higher/lower/equal) affinity for Epi.

A
  • heart
  • equal
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12
Q

Stimulation of dopamine 1 receptors has what effect?

A
  • stimulation of adenylate cyclase in neurons and vascular smooth muscle
  • increased cAMP
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13
Q

Stimulation of dopamine 2 receptors results in what?

A
  • inhibition of adenylate cyclase
  • open K+ channels
  • decreased Ca2+ influx
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14
Q

Which dopamine receptors are centrally located?

A

dopamine 2

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15
Q

Where are the catecholamines synthesized?

A

Dopamine: CNS neurons
Epinephrine: 2nd order neurons of SNS in the adrenal medulla
Norepi: 2nd order neurons of the SNS, adrenal medulla, CNS neurons

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16
Q

Define “sympathomimetic”

A

a drug that mimics the effect of Epi and Norepi

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17
Q

How are sympathomimetics grouped?

A

by mode of action and spectrum of affected receptors

  • direct mode: directly interacts with and activates receptor
  • indirect mode: 1) displace catecholamines from adrenergic nerve ending OR 2) inhibition of reuptake of catecholamines
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18
Q

List the tissues where apha-1 receptors are located;

A

bladder sphincter
liver
pupil dilator muscle
uterus
vascular smooth muscle

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19
Q

List the tissues where alpha-2 receptors are located:

A

platelets
post-ganglionic sympathetic neurons
vascular smooth muscle

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20
Q

List the tissues where beta-1 receptors are located:

A

heart
pancreas

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21
Q

List the tissues where beta-2 receptors are located:

A

bladder wall
liver
vascular smooth muscle
uterus

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22
Q

List the tissues where beta-3 receptors are located:

A

adipose tissue

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23
Q

List the alpha-1 agonists:

A
  • Epi
  • Norepi
  • Phenylephrine
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24
Q

List the alpha-1 antagonists:

A
  • Phentolamine
  • Phenoxybenzamine
  • Prazosin
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25
Q

List the alpha-2 agonists:

A

Clonidine
Dexmedetomidine

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26
Q

List the alpha-2 antagonists:

A

Yohimbine

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27
Q

List the beta-1 agonists:

A
  • Dobutamine
  • Dopamine
  • Epi
  • Norepi
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28
Q

List the beta-2 antagonists:

A

Atenolol
Metoprolol

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29
Q

List the beta-2 agonists:

A

Albuterol
Terbutaline

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30
Q

List the beta-2 antagonists:

A

Propranolol

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31
Q

Receptor selectivity of phenylephrine:

A

A1 > A2&raquo_space;»» B

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32
Q

Receptor selectivity of clonidine:

A

A2 > A1&raquo_space;»> B

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33
Q

Receptor selectivity of norepi:

A

A1 = A2
B1&raquo_space; B2

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34
Q

Receptor selectivity of epinephrine:

A

A1 = A2
B1 = B2

35
Q

Receptor selectivity of dobutamine:

A

B1 > B2&raquo_space;»» A

36
Q

Receptor selectivity of isoproterenol:

A

B1 = B2&raquo_space;»> A

37
Q

Receptor selectivity of albuterol/terbutaline:

A

B2&raquo_space; B1&raquo_space;»> A

38
Q

Receptor selectivity of dopamine:

A

D1 = D2&raquo_space;» B&raquo_space; A

39
Q

What is the parent drug from which sympathomimetic drugs are derived?

A

Phenylethylamine

40
Q

2 effects sympathomimetics can have on the metabolism:

A

1) enhance glycogenolysis in the liver
2) metabolic acidosis (high presence)

41
Q

Sympathomimetic effects on blood vessels:

A

A: increase arterial resistance
B: increase smooth muscle relaxation

42
Q

Sympathomimetic effects on blood pressure:

A

pure A: increase peripheral arterial resistance, decrease venous capacitance (increase BP, decrease HR d/t baroreceptor increase vagal tone)

pure B: increase CO, decrease PVR (increased/decreased SBP with decreased DBP)

mixed: skeletal muscle bed relaxation (decreased DBP) + alpha constriction of arterial beds

43
Q

Sympathomimetic effects on heart:

A

B1: increase chronotropy, increase conduction velocity through AV node, increase contractility

44
Q

Sympathomimetic effects on respiratory tract:

A

B2: bronchodilation

45
Q

Sympathomimetic effects on eye:

A

A: mydriasis

46
Q

Sympathomimetic effects on GI tract:

A

A & B: relaxation

47
Q

Sympathomimetic effects on GU tract:

A

A & B: uterus
A: urinary continence (bladder base and urethral sphincter)

48
Q

Describe the order of events of formation of Epinephrine:

A

Tyrosine
Dihydroxyphenylalanine
Dopamine
Norepi
Epi

49
Q

Tyrosine –> DOPA is catalyzed by…

A

tyrosine hydroxylase

50
Q

DOPA –> Dopamine is catalyzed by…

A

DOPA decarboxylase

51
Q

Dopamine –> Norepi is catalyzed by…

A

dopamine-B-hydroxylase

52
Q

Norepi –> Epi is catalyzed by…

A

phenylethanolamine-N-methyltransferase

53
Q

What is the rate limiting step of catecholamine synthesis?

A

formation of DOPA from tyrosine by tyrosine hydroxylase

54
Q

The rate limiting step of catecholamine synthesis is regulated by what mechanism?

A

Norepinephrine negative feedback loop

55
Q

In what 3 ways are catecholamines removed from the site of action?

A

1) reuptake into the presynaptic nerve (80%)
2) reuptake by extraneuronal tissues (contain the MAO and COMT)
3) diffuse away from synaptic cleft (enters circulation and metabolized in kidney and livery by COMT and MAO)

56
Q

What is COMT short for?

A

catechol-O-methyltransferase

57
Q

Describe the effects of Epinephrine:

A
  • positive inotropic and chronotropic actions on heart
  • vasoconstriction
  • decreased total peripheral resistance (–> DBP) in skeletal muscle beds
58
Q

Dose/onset/duration of Epi:

A
  • dose: 10-100mcg bolus; 0.01-0.2 mcg/kg/min
  • onset: 30-60 sec
  • duration: 5-10 min
59
Q

Describe the effects of Norepi:

A
  • vasoconstriction
  • increased SBP, DBP, coronary blood flor
  • ? decreased HR
  • decreased blood flow to major organs
60
Q

Dose/onset/duration of Norepi:

A
  • dose: 0.04-0.4 mcg/kg/min
  • onset: <1 min
  • duration: 2-10 min
61
Q

Describe the effects of dopamine:

A

D1: vasodilation, increased renal/mesenteric/coronary/cerebral BF
D2: inhibits Norepi release
B1: increase myocardial contractility/SV/CO, inotropic
A: vasoconstriction

62
Q

Describe the effects of Isoproterenol:

A
  • pure B1 & B2 agonist
  • positive chronotropic and inotropic effects
  • increased rate of cardiac pacemaker discharge
  • potent vasodilator (decreased SVR & pulm VR)
  • increase CO, decrease DBP, slight increase SBP
  • potent relaxation of bronchial smooth muscle
63
Q

Which sympathomimetic is used in inhaler form in the cath lab?

A

Isoproterenol

64
Q

Describe the effects of Dobutamine:

A
  • selective B1 agonist
  • increased myocardial rate and force of contraction
  • facilitates AV conduction
65
Q

“Sympathectomy” is another name for what?

A

spinal anesthesia

66
Q

Why might a patient get nauseated after receiving a spinal?

A

increased vagal activity after sympathectomy causes increased peristalsis of the GI tract

(treat the BP w/ Ephedrine and the nausea should improve)

67
Q

What is the MOA of Phenylephrine?

A
  • pure A agonist
  • acts directly on the receptors
68
Q

Describe the effects of Phenylephrine:

A
  • intense peripheral vasoconstriction
  • increased SBP, DBP
  • reflex bradycardia
  • decongestant
69
Q

What is the MOA of Ephedrine?

A
  • both A and B stimulation
  • mixed direct and indirect actions
  • prevents breakdown of NE by MAO –> increased release of stored NE
70
Q

Describe the effects of Ephedrine:

A
  • increased CO, BP, HR
71
Q

Why should Ephedrine be used cautiously in patients on MAOIs?

A

MAOIs sensitize the patient to indirectly acting sympathomimetics –> hypertensive emergency

72
Q

Where does Vasopressin act on the body?

A

direct action on vascular smooth muscle

73
Q

What are some precautions to using vasopressin?

A
  • reduction in CO, myocardial contractility, and coronary BF
74
Q

Describe albuterol’s MOA:

A
  • short-acting B2 agonist
  • inhaled
  • used for rapid relief of wheezing, bronchospasm, and airflow obstruction
75
Q

Describe Salmeterol/Formoterol’s MOA:

A
  • long-acting B2 agonist
  • always used in combination therapy
76
Q

What are 2 side effects of inhaled B2 agonists?

A
  • tremors
  • tachycardia
77
Q

What drug is a quick treatment for hyperkalemia?

A

inhaled Albuterol

78
Q

Describe the MOA and uses of Terbutaline:

A
  • B2 agonist
  • tocolytic
79
Q

What is the MOA of selective phosphodiesterase inhibitors?

A
  • decrease hydrolysis of cAMP
  • augmentation of myocardial performance independent of the SNS
80
Q

Describe the effects of selective phosphodiesterase inhibitors:

A
  • positive inotropic effects
  • vascular and smooth muscle relaxation
81
Q

What patients would benefit from selective phosphodiesterase inhibitor therapy?

A

acute cardiac failure needing increased myocardial contractility and vasodilation

82
Q

What drug class does Milrinone belong to? What is this drug used for?

A
  • selective phosphodiesterase inhibitor
  • has minimal effect on HR and myocardial O2 consumption
  • beneficial for LV dysfunction after cardiac sx
83
Q

Ionized calcium is a potent (chronotrope/inotrope).

A

inotrope

84
Q

What does the drug Levosimenden do?

A
  • increases contractility by increasing the sensitivity of the myocardium to Ca2+
  • increases CO
  • decreases SVR and pulm VR

Pharm (19 decks)

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