Adrenergic Agonists And Antagonists Flashcards

1
Q

Low doses of atropine cause ________

A

↑ secretion of acetylcholine because it blocks the pre synaptic M2 receptor which normally inhibits the release of acetylcholine

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2
Q

NE does not cause bronchodilation because the ____ receptors are mainly found in bronchial smooth muscle respond to _____

A

β2; epinephrine

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3
Q

_________ express almost exclusively α1 receptors and thus NE and epinephrine cause ______

A

Skin blood vessels; constriction

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4
Q

________ and _______ receptors are found in smooth muscles of blood vessels in skeletal muscle

A

β2 and α1

β2 is a vasodilator
α1 is a vasoconstrictor

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5
Q

Low concentration of epinephrine will cause ________ in the blood vessels supplying skeletal muscle

A

Vasodilation; β2 are more sensitive to epinephrine than α1 receptors are

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6
Q

What do you expect to see in the vessels supplying skeletal muscle when giving a high dose of epinephrine?

A

Vasoconstriction: both α1 and β2 receptors will be activated but the α1 response is stronger than β2

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7
Q

What are the classes of adrenergic agonists?

A
  • direct acting: endogenous catecholamines, β and α agonists
  • indirect acting: releasing agents, uptake inhibitors
  • mixed acting
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8
Q

At low concentrations of epinephrine, it will activate mainly ____ and_____

A

β1 (found in the heart) and β2

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9
Q

Large doses of epinephrine cause an ↑ in BP due to:

A
  • ↑ ventricular contraction (β1 effect)
  • ↑ HR (β1 effect)
  • vasoconstriction (α1 effect)
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10
Q

What is the effect on blood pressure (diastolic and systolic) when given a low dose of epinephrine

A
  • diastolic pressure ↓ because: ↓ in peripheral resistance because β2 receptors are more sensitive
  • systolic pressure ↑ because: ↑ cardiac contractile force (β1 effect)
  • HR ↑ (β1 effect)

NO CHANGE IN MEAN BLOOD PRESSURE

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11
Q

The effects of epinephrine on blood pressure depends on the dose and ratio of the _____ and____ response in various vascular beds

A

α1; β2

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12
Q

Epinephrine is the drug of choice for _______

A

Anaphylactic shock

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13
Q

NE has little action on _____ receptors

A

β2

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14
Q

What are the cardiovascular effects due to NE?

A
  • peripheral vasoconstriction (α1)
  • ↑ cardiac contractility (β1)
  • ↑ systolic AND diastolic pressure → ↑ BP
  • baroreceptor reflex will kick in an cause BRADYCARDIA
  • CO is unchanged or ↓
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15
Q

What is the effect of NE on cardiac output?

A

Unchanged or ↓ :

CO = HR x SV (SV ↑ and HR ↓)

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16
Q

NE is used to treat _____

A

Shock because it ↑ blood pressure

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17
Q

If atropine is given before NE, then NE will cause ___________

A

Tachycardia

Atropine will block the M2 receptors in the heart (↓ HR) so then no baroreceptor reflex response → ↑ HR

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18
Q

What receptors can dopamine activate

A

Dose dependent but can activate: dopamine receptors, β and α receptors

Dopamine 1 receptors > β1 receptors > α1 receptors

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19
Q

What is the CVS effect on LOW rate of infusion of dopamine?

A

Activates D1 receptors in the renal and other vascular beds:

  • vasodilation
  • ↑ GFR
  • ↑ in renal blood flow
  • ↑ in sodium excretion
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20
Q

With intermediate rates of infusion of dopamine, it will activate _______ receptors in the heart causing ________ and also causes release of NE from nerve terminals

A

β1 receptors (NE does not effect β2 receptors);

↑ cardiac output

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21
Q

Intermediate rate of infusion of dopamine on:

Systolic pressure
Diastolic pressure
MAP
PVR

A

SBP: ↑
DBP: not changed significantly because only β1 is activated
MAP: ↑
PVR: unchanged

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22
Q

What is the effect of HIGH rates of dopamine infusion?

A
  • with high rates will also activate vascular α1 receptors → vasoconstriction → ↑ BP and TPR
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23
Q

High rates of dopamine infusion also activates _______ receptors

A

α1 receptors in the vasculature

24
Q

For treating shock, _______ to _______ rates of dopamine infusion are used

A

Intermediate to high

25
Q

What are some clinical uses for dopamine?

A
  • treatment of severe CHF

- cardiogenic and septic shock

26
Q

Example of a non selective β adrenergic agonist

A

Isoproterenol

27
Q

When giving _____________ the baroreceptor reflex and the direct action of the drug is the SAME DIRECTION

A

Isoprotenerol

↑ in HR due to the baroreceptor reflex AND the drug

28
Q

Effects of isoprotenerol on:

CO
PVR
Diastolic pressure
Systolic pressure
MAP
A
CO: ↑ (β1) (also ↑ in HR, force of contraction) 
PVR: ↓ (β2)
Diastolic pressure: ↓ 
Systolic pressure: same or slight ↑ 
MAP: ↓
29
Q

What is the difference between the MAP in giving low dose of epinephrine and giving isoproterenol?

A

MAP for low dose epinephrine is unchanged while for isoprotenerol it is ↓

30
Q

What would you give someone isoproterenol for?

A

Emergencies to stimulate HR in bradycardia or heart block

31
Q

What kind of drug is dobutamine?

A

Predominantly a β1 agonist but on the vascular smooth muscle it is a alpha agonist or an α1 antagonist

it is a potent inotrope

32
Q

Dobutamine causes a less ↑ in _____ and less ↓ in ________ compared to isoproterenol

A

HR; PVR

33
Q

Dobutamine causes mild vasoconstriction/vasodilation

A

Vasodilation

34
Q

Why would you give someone dobutamien?

A

It is used for the dobutamine stress echocardiogram for patients who cannot run or be active. It ↑ myocardial O2 consumption like if you were exercising

Management of acute heart failure and cardiogenic shock

35
Q

What are the types of β2 agonists

A

Short acting: albuterol

Long acting: salmeterol and formoterol

36
Q

Which β2 agonist would you use to manage acute asthma symptoms?

A

Albuterol (short acting)

37
Q

What are some adverse effects of β2 adrenergic agonists?

A

Restlessness, tremor, apprehension, anxiety and tachycardia

38
Q

__________ is an α1 selective adrenergic agonists

A

Phenylephrine

39
Q

What are some clinical uses for phenylephrine ?

A
  • nasal decongestant
  • used to ↑ BP In hypotension from vasodilation in shock or anesthesia
  • ONLY mydriasis (dilation) WITHOUT cycloplegia (muscarinic antagonists have both mydriasis and cycloplegia)
  • used to ↑ BP to terminate episodes of supraventricular tachycardia
40
Q

What are the α2 selective adrenergic agonists?

A
  • clonidine
  • methyldopa
  • brimonidine
41
Q

________ is a partial α2 agonist and acts on the ________________ and thus reduces _________ outflow and thus _________ blood pressure

A

Clonidine; central presynaptic α2 adrenoreceptors; sympathetic; ↓ blood pressure

42
Q

What is the net effect of clonidine on blood pressure?

A

↓ blood pressure because it ↓ sympathetic outflow

43
Q

IV infusion of clonidine can cause _______

A

Acute RISE in BP due to activation of α2 receptors in the vascular smooth muscle (transient vasoconstriction)

NOT SEEN ORALLY

44
Q

Which of the α2 agonists is a prodrug?

A

Methyldopa; it is taken up by noradrenergic neurons

45
Q

What is the drug of choice for treatment of hypertension during pregnancy?

A

Methyldopa (↓ BP)

46
Q

What is the use of bromidine?

A

It is a highly selective α2 agonist

Given ocularly to lower intracolar pressure in glaucoma;
Reduces aqueous humor production and ↑ outflow

47
Q

What α2 agonist is given to lower intraocular pressure in glaucoma patients?

A

Bromidine (given topically)

48
Q

What are the releasing agents of indirect acting adrenergic agonists?

A
  • amphetamine
  • methylphenidate
  • tyramine
49
Q

_________ is the structural analog of amphetamine

A

Methylphenidate

50
Q

What is the MOA of cocaine

A

It is a uptake inhibitor that blocks monoamine reuptake and so they accumulate in the synaptic space

51
Q

Atomoxetine is a selective inhibitor of _______________ and is indicated for treatment of _______

A

NE reuptake transporter ; ADHD

52
Q

Which of the uptake inhibitors is selective?

A

Atomoxetine (cocaine is NOT selective)

53
Q

Modafinil is used for the treatment of ____________

A

Narcolepsy

54
Q

Modafinil is an uptake inhibitor that ↑ synaptic concentrations of _____ and ↓ concentrations of ______

A

↑: NE, dopamine, sertonin, and glutamate

↓ : GABA levels

55
Q

What are the two mixed acting adrenergic agonists?

A
  • ephedrine

- pseudoephedrine

56
Q

What are some uses for ephedrine?

A

Pressor agent for spinal anesthesia

Used in myasthenia gravis