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NURS 304 > Adrenergic Agonists and Antagonists > Flashcards

Adrenergic Agonists and Antagonists Flashcards

1
Q

Adrenergic receptor subtypes

A

Alpha 1 and 2, Beta 1 and 2, dopamine

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2
Q

Adrenergic neurotransmitters

A

Norepinephrine, Epinephrine, Dopamine

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3
Q

Alpha-1 receptor function

A

ocular: mydriasis
Blood vessels: vasoconstriction
male genitals: ejaculation
Bladder: neck (sphincter) and prostate constrict while detrusor relaxes

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4
Q

Alpha-2 receptor function

A

located on presynaptic cell
minimal clinical significance
inhibits release of NE
Located in PNS and CNS

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5
Q

Beta-1 receptor function

A

we have one heart so “one=heart”
increases force of contraction
increases heart rate
increases velocity of conduction in AV node

kidneys: stimulates release of renin

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6
Q

Beta-2 receptor function

A

bronchial dilation
vasodilation in heart, lungs, liver, and skeletal muscles
relaxation of uterine smooth muscle
glycogenolysis in liver and skeletal muscle
enhanced contraction of skeletal muscle

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7
Q

Dopamine receptor function

A

Primarily in CNS

Only known function:
dilation of renal arteries - enhanced renal perfusion

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8
Q

Epinephrine

A

activates alpha 1, alpha 2, beta 1, beta 2

released from adrenal medulla

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9
Q

Norephinephrine

A

activates alpha 1, alpha 2, beta 1

released from post-ganglionic neurons in SNS

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10
Q

Dopamine

A

activates alpha 1, beta 1, and dopamine

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11
Q

Lifecycle of NE

A

synthesized in presynaptic terminal from a series of precursors

Stored in vesicles, released by action potential

Transmission by NE is terminated by dissociation from receptor and reuptake into presynaptic neuron terminal

  • recycled or
  • broken down by MAO
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12
Q

Lifecyle of Epinephrine

A

synthesized in adrenal medulla (NE –> Epinephrine)

Stored in vesicles in chromaffin cells of adrenal medulla –> activation of Nicotinic n receptors causes release of Epinephrine by adrenal medulla

travels in bloodstream to all parts of body
transmission terminated by hepatic metabolism (half life only 2-3 minutes)

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13
Q

Direct activation

A

receptor binding

most common

mimic natural transmitter

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14
Q

Indirect activation

A

mostly used for CNS effects

promotes NE release
inhibits NE uptake
inhibits NE inactivation

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15
Q

Catecholamines

A

endogenously produced

have a polar moeity which makes it hard to cross blood brain barrier

examples: epinephrine, NE, dopamine, dobutamine

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16
Q

Non-catecholamines

A

lack catechol group = much less polar

examples: ephedrine, phenylephrine, terbutaline

more CNS effects

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17
Q

Implications of catecholamines

A

cannot be used orally

rapidly metabolized by MAO and COMT (enzymes in intestinal wall and liver)

must be administered by continuous infusion

duration of action is BRIEF

cannot cross BBB –> minimal use in CNS

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18
Q

Implications of non-catecholamines

A

can be used orally

slowly metabolized by MAO
not degraded by COMT

duration of action is LONGER

Better at crossing BBB –> can cause CNS effects

19
Q

Receptor specificity is…

A

relative (NOT absolute)

LOW doses are best to be MORE selective for specific receptors

20
Q

Alpha 1 therapeutic applications

A

Hemostasis (via vasoconstriction, helpful during sutures)

Elevation of BP (ICU)

Mydriasis (eye drops for ophthalmic exam)

Nasal decongestion (constricts vessels in mucous membrane = reduced swelling; doesn’t have effect on nasal secretions)

21
Q

Alpha 1 receptor for local anesthetics

A

vasoconstriction is induced and allows:

  • decreased in anesthetic dosage
  • prolongs anesthesia
  • decreases systemic effects
  • Epi is mostly commonly used
  • Lidocaine + epi can be contained in same vial
22
Q

Alpha 1 receptor activation

3 ADVERSE EFFECTS

A

HTN (hypertension)

Bradycardia (reflex bradycardia): an increased BP can signal cardiac inhibitory signal in medulla = stimulates lower HR

-risk of local cell death (necrosis) when used with anesthesia or if IV extravasates; cause: prolonged vasoconstriction

23
Q

Beta 1 Therapeutic Applications

A

cardiac arrest

acute heart failure

shock

AV block

24
Q

Beta 1

3 ADVERSE EFFECTS

A

tachycardia

angina/chest pain

dysrhythmia

25
Q

Beta 2 therapeutic applications

A

relax smooth muscle of bronchi (Asthma, albuterol)

Relax uterine smooth muscle (delay preterm labor)

26
Q

Beta 2

2 ADVERSE EFFECTS

A

Hyperglycemia (in diabetics)

Tremor

27
Q

Dopamine therapeutic applications

A

at low doses –> dilates renal vasculature

at high doses –> enhances cardiac performance; will activate all adrenergic receptors (ICU drug)

28
Q

Anaphylactic shock:

Cause? S/S? Treatment?

A

Cause : Severe Allergy

S/S: HTN, bronchial constriction, edema of glottis

Treatment: Epinephrine (IM; fewer ADE than IV)

29
Q

Adrenalin uses

A

mimic epinephrine

IM, SQ, IV, topically (catecholamine, cannot be taken orally)

used in anaphylaxis, cardiac arrest, increase BP in shock

used for local vasoconstriction

inhaled for treat croup symptoms and for asthma if other treatments ineffective

30
Q

Adrenalin

ADVERSE EFFECTS

A

shakiness, anxiety, sweating, tachycardia, HTN

31
Q

Levophed

A

mimics NE

activates A1, A2, B1

32
Q

Isoproterenol

A

potent nonselective beta-adrenergic agonist

low affinity for alpha-adrenergic receptors. Systemic effects:

lowering of peripheral vascular resistance and diastolic pressure

positive inotropic and chronotropic effects

prevention of bronchoconstriction

33
Q

Phenylephrine

A

alpha 1 agonist

newest product

only activates A1

34
Q

Alpha Blockers

Therapeutic Applications

A

BPH: allows PSNS to take over = increased urination

Pheochromocytoma: catecholamine secreting tumor of adrenal medulla = excessive secretion of epinephrine; blockers serve to lessen the symptoms by blocking receptors

Raynaud’s disease: prevents vasoconstriction of fingertips and toes

Reverse toxicity caused by alpha 1 agonists

35
Q

Phentolamine

A

Non-selective alpha blocker

blocks A1 an A2

uses:
hypertensive crisis

treats pheochromocytoma, given IV or IM

36
Q

Prazosin

A

alpha 1 BLOCKER

uses:
BPH

Nightmares from PTSD (CNS effect)

37
Q

Alpha Blockers

4 ADVERSE EFFECTS

A

Orthostatic hypotension

Reflex tachycardia

Nasal congestion

Inhibition of ejaculation

38
Q

Propranolol

A

Non-selective BETA blocker

Blocks Beta 1 and Beta 2

contraindicated in asthma, COPD, SOB

overt cardiac failure, severe bradycardia

39
Q

Metoprolol

A

Blocks Beta 1 receptors (cardioselective)

Used for HTN, heart failure

40
Q

Beta blockers

Therapeutic applications

A 
Angina Pectoris
HTN
Cardiac dysrhythmias (by slowing down HR)
MI (during rehab and thereafter)
HF (useful much of time but not all the time)
Migraine
Hyperthyroidism
Stage fright
Glaucoma
41
Q

Beta 1 blockage

Therapeutic consequences

A

Reduced HR
Reduced force of contraction
Reduced velocity of impulse conduction

42
Q

Beta Blockers

ADVERSE EFFECTS

A 
Bradycardia
AV heart block
Reduced CO (cardiac output)
HF, symptoms of CHF
Hypotension
Inhibition of glycogenolysis
Bronchial constriction
Drowsiness, depression
43
Q

Albuterol

A

Beta 2 agonist

44
Q

Dobutamine

A

Beta 1 agonist

NURS 304 (4 decks)

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