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2nd Semester Final > Adrenergic Agonists Lecture PDF > Flashcards

Adrenergic Agonists Lecture PDF Flashcards

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1
Q

Sympathomimetic

A

An Adrenergic agonist drug that simulates sympathetic stimulation of the ANS

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2
Q

Sympatholytic

A

An adrenergic antagonist drug that inhibits sympathetic stimulation of the ANS

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3
Q

Inactivation of catecholamine adrenergic agonists occurs by ___ and ___ and as a result these drugs must be administered by ____

A

MAO, COMT, by continuous infusion

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4
Q

Catecholamines vs noncatecholamine drugs

A

Catecholamines are quickly inactivated by MAO and COMT and cannot cross BBB and therefore have minimal CNS effects, noncatecholamines are metabolized slowly and thus have longer half lives and can be delivered PO and can penetrate BBB, therefore have effect on CNS

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5
Q

Indirect acting adrenergic agonists and 2 examples

A

Tend to be noncatecholamines, cause release of NE from presynaptic terminals, inhibit its reuptake, and inhibit deactivation of it

  • amphetamines
  • ephedrine (which can do both)
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6
Q

Direct acting adrenergic agonists and 2 examples

A

Tend to be catecholamines, work by directly binding to and activating adrenergic receptors

  • epi
  • isoproterenol
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7
Q

Factors affecting responses to adrenergic agonists (3)

A
  • receptor distribution and sensitivity (there are more receptors of one type depending on the tissue thus causing the predominating effect)
  • receptor specificity (often at low to moderate doses and can see other activation when high doses)
  • potency
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8
Q

Cardiovascular changes that result from adrenergic stimulation are complex because they result from not only direct stimulation of the heart but also…

A

….compensatory baroreceptor reflexes

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9
Q

Epi cardiovascular effects

A
  • hr increase
  • BP increase
  • bronchodilation
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10
Q

Isoproterenol cardiovascular effects

A
  • HR increase

- bronchodilation

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11
Q

Norepi cardiovascular effects

A
  • HR increase
  • BP increase
  • no bronchodilation
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12
Q

Therapeutic applications of a1 stimulation (4)

A
  • hemostasis to prevent bleeding via vasoconstriction
  • nasal decongestants
  • mydriasis
  • elevation of BP in shock
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13
Q

cocaine overdose resulting in MI cause of death mechanism of action

A
  • Cocaine acts as an adrenergic agonist and has activity on a1 receptors
  • such potent activity results in coronary artery constriction (vasospasm) and lack of perfusion to the heart
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14
Q

Rhinitis medicamentosa

A

Rebound nasal congestion upon cessation of common use of decongestants

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15
Q

Example of a1 agonists in nasal sprays and oral decongestants

A
  • phenylephrine

- pseudoephedrine

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16
Q

a1 agonist ADR’s (3)

A
  • hypertension
  • necrosis at site of administration due to microvasospasm (can be counteracted by administration of an a1 blocking agent such as phentolamine)
  • bradycardia
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17
Q

a2 stimulation has minimal effect on ____ but larger effect on ____

A

PNS, CNS

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18
Q

Examples of a2 therapeutic agents (2)

A
  • clondine (directly binds a2 receptors)
  • a methyldopa (converted in adrenergic nerve terminals to a-methylnorepi released by adrenergic neuron and binds a2 receptors
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19
Q

B1 stimulation clinically relevant responses act on the…

A

…heart

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20
Q

Therapeutic applications of B1 stimulation (4)

A
  • cardiac arrest
  • heart failure
  • shock
  • AV heart block
21
Q

B1 agonist ADR’s (2)

A
  • altered heart rate or rhythm (tachycardia or arrhythmia)

- angina pectoris

22
Q

B2 stimulation therapeutic uses (2)

A
  • asthma

- delay of preterm labor

23
Q

examples of B2 selective agents (3)

A
  • albuterol
  • levabuterol
  • terbutaline (po for asthma or subQ for preterm labor)
24
Q

B2 agonists ADR’s (3)

A
  • hyperglycemia (not normally an issue unless diabetic)
  • tremor
  • at high doses may stimulate b1 receptors resulting in overstimulation of heart
25
Q

Dopamine receptor stimulation function

A

-activates peripheral dopamine receptors causing dilation of mesenteric and renal vasculature to treat shock and improve renal perfusion

26
Q

Pathophys of anaphylaxis

A

-severe allergy characterized by hypotension, bronchoconstriction, and laryngeal edema, largely due to histamine and leukotrienie release

27
Q

Anaphylaxis treatment DOC and mech of action to treat hypotension, laryngeal edema, and bronchoconstriction

A
  • Epinephrine subQ
  • B1 stimulation increases cardiac output raising BP, a1 promotes vasoconstriction that can elevate BP and suppress laryngeal edema, B2 counteracts bronchoconstriction
28
Q

Epinephrine (adrenalin) therapeutic uses (4)

A
  • restore cardiac function in cardiac arrest
  • produce mydriasis
  • treat bronchospasm
  • treat anaphylaxis
29
Q

Epinephrine/norepi/isoproternol ADR’s (4)

A
  • hypertensive crisis
  • arrhythmias
  • angina pectoris
  • hyperglycemia
30
Q

Epinephrine/norepi/isoproternol drug interactions (3)

A
  • MAO inhibitors intensify
  • tricyclic antidepressants intensify
  • a/B adrenergic blocking agents inhibit action
31
Q

Epi dosing ratio for oral/inhalation, subq/im, and IV/intracardiac

A

1: 100 oral or inhalation
1: 1000 subq, im
1: 10,000 IV or intracardiac

32
Q

Norepinephrine (levophed) mech of action and therapuetic uses (2)

A

-only activates a1 and B1 receptors, equivalent on B1 receptors but less potent on a1 receptors

  • used in hypotensive states
  • cardiac arrest
33
Q

Isoproternol (isuprel) mech of action and therapeutic uses (2)

A

-acts only on B1 and 2 receptors

  • cardiac stimulant to treat AV heart block or cardiac arrest
  • bronchodilator
34
Q

Dopamine intropin mech of action

A

functions as neurotransmitter in brain and precursror of synthesis of NE in peripheral nerve endings

35
Q

Dopamine (intropin) administration and therapeutic uses (3)

A

-IV

  • Low doses to increase renal flow
  • moderate doses to increase CO
  • high doses to produce vasoconstriction (heart failure and shock)
36
Q

Dobutamine (dobutrex) therapeutic use (1) and ADR’s (1)

A
  • only indicated for heart failure or stress testing

- Increase AV conduction putting caution in using with afib

37
Q

Phenylephrine (neosynephrine) mechanism of action and therapeutic uses (2)

A

-selective a1 agonist that performs vasoconstriction

  • nasal decongestant
  • IV infusion to provide local vasoconstriction
38
Q

Ephedrine

A

Acts similar to epi but response is slower and lasts 10x longer but must less potent

39
Q

Albuterol (ventolin) mech of action and therapuetic use (1)

A
  • selectively stimulates B2 receptors with much less stimulation of heart than isoproternol
  • asthma for relaxation of bronchial smooth muscle
40
Q

Ephedrine is both a __ and ___ acting adrenergic agonist

A

direct, indirect

41
Q

Heart primarily has ___ adrenergic receptors

A

B1

42
Q

Blood vessels primarily have ____ adrenergic receptors

A

a1

43
Q

Vascular beds in skeletal muscle have both a1 and B2 receptors. What will NE cause as a net response and why?

A

Vasodilation due to a greater number of B2 receptors and greater sensitivity

44
Q

Drugs that stimulate a1 receptors (5)

A
  • epi
  • NE
  • phenylephrine
  • ephedrine
  • dopamine
45
Q

Drugs that stimulate a2 receptors (3)

A
  • epi
  • NE
  • ephedrine
46
Q

Drugs that stimulate B1 receptors (5)

A
  • epi
  • norepi
  • isoproterenol
  • dopamine
  • ephedrine
47
Q

Drugs that stimulate B2 receptors (4)

A
  • epi
  • isoproterenol
  • terbutaline
  • ephedrine
48
Q

Dopamine (intropin) ADR (1) and drug interactions (2)

A

-vasoconstriction resulting in anginal pain and hypertension

  • MAO inhibitors intensify effect
  • diuretics complement effects

2nd Semester Final (207 decks)

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