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Pharmacology > Exam2Lec2AdrenergicPharmacology > Flashcards

Exam2Lec2AdrenergicPharmacology Flashcards

1
Q

Which class of receptors are adrenergic receptors?

A

G protein-coupled (GPCR)

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2
Q

Which catecholamines do adrenergic receptors target?

A

1) Norepinephrine
2) Epinephrine

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3
Q

Does adrenergic receptors stimulate the PNS or SNS?

A

Sympathetic NS

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4
Q

How does an α1 receptor affect most vascular smooth muscle?

A

Contraction

by vasoconstriction

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5
Q

What is the G protein for an α1 receptor?

A

Gq

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6
Q

How does an α2 receptor affect the postsynaptic CNS?

A

Decreases SNS tone

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7
Q

How does an α2 receptor affect the presynaptic ANS?

A

Decreases NT release

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8
Q

What is the G protein for an α2 receptor?

A

Gi

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9
Q

What are the G proteins for a β1 receptor?

A

Gs, Gi

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10
Q

How does a β1 receptor affect the heart?

A

Increases force and rate

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11
Q

How does a β1 receptor affect the juxtaglomerular cells?

A

Increases renin release = retains fluid

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12
Q

What are the G proteins for a β2 receptor?

A

Gs, Gi

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13
Q

How does a β2 receptor affect skeletal muscle blood vessels?

A

Relaxation

by vasodilation

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14
Q

How does a β2 receptor affect the bronchial smooth muscle?

A

Relaxation

by bronchodilation

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15
Q

How does a β2 receptor affect the liver?

A

Glycogenolysis and gluconeogenesis = increases blood glucose

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16
Q

Which drug is an α1 agonist?

A

Phenylephrine = vasoconstriction

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17
Q

Which drugs are α2 agonists?

A

Clonidine and Methyldopa = decrease SNS tone

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18
Q

Which drugs are non-selective β agonist (β1 + β2)?

A

Isoproterenol and Dobutamine

“I would DIe to be Beta
B1: incr HR
B2: smooth m dilation

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19
Q

Which drug is a β2 agonist?

A

Albuterol = dilates bronchial smooth muscle

good for asthma

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20
Q

Which drug is a non-selective α antagonist (blocks α1 and α2)?

A

Phentolamine = vasodilation & increases HR

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21
Q

Which drug is an α1 antagonist?

A

Prazosin

effect: vasodilate muscle instead of constrict

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22
Q

Which drugs are non-selective β antagonists (β blockers)?

A

PropranOLOL

PROPs being a B antag
B1: decr HR
B2: bronchoconstriction

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23
Q

Which drugs are β1 antagonists (β blockers)?

A

AtenoOLOL and MetoprOLOL = decrease HR

Oh Lol At Me then

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24
Q

Which drugs are mixed α1/β antagonists?

A

CarvediLOL and LabetaLOL

LOL=funny bc it is both
CARVed a LABel to MIX up an antagonist

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25
Q

What is the oral usability of epinephrine?

A

completely ineffective

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26
Q

Is the duration of action of epinephrine long or short?

A

short

b/c naturally made in body

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27
Q

Does epinephrine have good or poor penetration of the CNS?

A

poor

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28
Q

Why is phenylephrine better than epinephrine?

A

More stable and is not broken down as fast

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29
Q

If given phenylephrine, is it okay to give an MAO inhibitor?

A

No bc you will now have a buildup of epi causing effect and phenylephrine (A1 agonists) causing effects .

mao breaks down epi

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30
Q

What is the primary effect of α1 agonist?

A

vasoconstriction of most vascular smooth muscle

By stim α1

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31
Q

What are the clinical uses of α1 selective agonists and mention how they are useful for each one.

A

● Nasal congestion = decreases inflammation markers
● Hypotension = vasoconstriction = increases BP
● Hemorrhoids = vasoconstriction = stops inflammation of markers to swollen/inflamed veins
● Dilates pupils

phenylephrine

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32
Q

What are the adverse effects of phenylephrine?

A

● Angina
● Anxiety
● Bradycardia
● HTN
● Tissue necrosis

“BHAAT” like epi but w/o the C so instead of CHAAT, its BHAAT

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33
Q

What are the contraindications of phenylephrine?

A

● Vfib
● Tachycardia
● HTN

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34
Q

What are the interactions of phenylephrine?

A

MAO inhibitors = breaks down NE

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35
Q

Phenylephrine Overview
A. Class
B. Effect
C. TX
D. SE
E. Contraindication
F. Interactions

A

A. class: alpha 1 agonist
B. effect: vasoconstriction
C. tx: nasal congestion, hypotension,hemorroids, dilate eye
D. se: angina, bradycardia, HTN, necrosis
E. contraindication: Vfib, tachy, HTN
F. interactions: MAOI

“BHAAT” for SE
dont want to give to someone with heart probs bc raises BP

36
Q

What are the α2 selective agonist drugs?

A

Clonidine and Methyldopa

decr SNS, think PNS effects

37
Q

Stimulation of the α2 receptors in the medulla has what type of effects?

A

Sympatholytic
● No reflex tachycardia

38
Q

What are the net effects of α2 agonists?

A

● Decreased BP
● Decreased HR
● Decreased cardiac output

still an agonists, it just activates Gi thats inhibitory

39
Q

What is the first line of therapy for HTN during pregnancy?

A

Methyldopa

this is a prodrug that needs to be activated so its safer

40
Q

Why is clonidine used more often than methyldopa?

A

More potent

41
Q

Why is clonidine not used for pregnancy?

A

Catagory C for pregnancy = risk cannot be ruled out

for cat C we are determing benefits vs risk

42
Q

Why is methyldopa the first line therapy for HTN during pregnancy?

A

Pro drug = only effective in the brain = safer

43
Q

Clonidine can also treat several CNS disorders such as?

A
  • ADHD
  • Mitigate drug withdrawal
  • Severe pain
44
Q

Clonidine is effective in both the ____ and the ____.

A

periphery, brain

effect everywhere with dose

45
Q

What drug class is Clonidine and Methyldopa?

A

α2 agonist

46
Q

What are the adverse effects of clonidine?

A
  • Dry mouth
  • Sedation
  • Depression
  • Orthostatic hypotension
47
Q

What is the effect of Clonidine?

A

Decreases SNS tone

48
Q

What are the contraindications for Clonidine?

A
  • Depression
  • Caution: Sudden withdrawal causes hypertensive crisis
49
Q

What are the adverse effects of Methyldopa?

A
  • Sedation
  • Depression
  • Tolerance
50
Q

What are the contraindications for Methyldopa?

A
  • Depression
  • MAO inhibitory therapy = increases NE
51
Q

Clondine/Methyldopa Overview
A. Class
B. Effect
C. TX
D. SE
E. Contraindication
F. Notes

A

A.α2 agonist
B. decr BP, HR, CO (sns tone)
C. HTN
D. Hypotension, depression, sedation
E. DEPRESSSION, MAO inhib, sudden withdrawl
F. Note: methyldopa is FIRST LINE for therapy . Clonidine is more potent
Clonidine=periphery, Methyldopa=prodrug

52
Q

What drug class is Isoproterenol?

A

Non-selective β agonist = agonist at both β1and β2 receptors

potent vasodilater (B2)
bronchodilator (B2)
positive inotropic and chronotropic agent (B1)

53
Q

What are the clinical uses for Isoproterenol?

A
  • Cardiac arrest
  • AV block
  • Bradycardia
  • Torsade de pointes
54
Q

What are the adverse effects of Isoproterenol?

A

Arrythmias (common)

55
Q

True or false, Isoprotenerol is NOT a first line agent for use in bronchospasm during anesthesia or shock (cardiogenic, hypovolemic, or septic)

A

TRUE

CARDIOGENIC-DOPA
SEPTIC -NOREPI

56
Q

Isoproterenol Overview
A. Type
B. Effect
C. Use
D. SE

A

A. β agonist (non-selective)
B. vasodilation, bronchodilator, incr HR
C. torsade pointes
D. arrythimas

57
Q

What drug does this graph represent?

A

isoproterenol

58
Q

Dobutamine Overview
A. Type
B. Effect

A

A. β agonist (non selective)
B. incr HR (inotropic (force) more than chronotropic (rate)), no net change in resistance

racemix mixture
greater force/contractility than HR

59
Q

Albuterol Overview
A. Type
B. Effect
C. Use
D. SE
E. Contraindications

A

A. β2 agonist (selective)
B. vasodilation of smooth and skel muscle
C. Asthma/bronchospasms, premature labor
D. tremors, tachy (direct and reflec), CNS stimulation
E. Hyperglycemia

short-action-acute bronchospasm
stimulates glucogenolysos dont give to DM

60
Q

Can you give albuterol to a diabetic pt (hyperglycemic)?

A

NO

61
Q

What is the non-selective α ANTAGONIST drug?

A

Phentolamine

causes vasodilation, incr SNS, incr NT

62
Q

What is the α1 selective ANTAGONIST drug?

A

Prazosin

causes vasodilation

63
Q

Phentolamine Overview
A.Type
B. Effect
C. Use
D. SE

A

A. Type: A Antagonist
B. Effect: Vasodilation
C. Use: Anesthesia Reversal
D. SE: Reflux Tachy, tolerance

vasodilation triggers incr HR (reflex tachy)

64
Q

With phentolamine, heart rate increase is more pronounced when what occurs?

A

With mixed A1 and A2 antag b/c of diminished A2 feedback in heart (remember A2 in presynaptic terminal)

A2 antag incr SNS, NE that binds to B receptors (incr HR)

65
Q

HR incr greater in phetolamine or prazosin?

A

Phentolamine

66
Q

A1 antag causes what 3 things?

A

Vasodilation
Decr BP
Incr HR

67
Q

Prazosin Overview
A. Type
B. Effect
C. Use
D. SE
E. Contraindication

A

A. Type: A1 Antagonist
B. Effect: Vasodilation
C. Use: BPH
D. SE: Reflux Tach
E. Contraindication: Angina, MI, BB withdrawals

BPH=benign prostatic hyperplasia

68
Q

Is Prazosin use as a first line for Hypertension?

A

NO

69
Q

What cardiovascular effects do you see with non selective Beta blockers (propranolol)?

A

Negagtive inotropic, dromotropic (conduction speed) and chronotropic effect
decr rening release
block of B2 may incr perip resistance

opposite of SNS, so think parasymp

70
Q

What are some CNS and eye effects of B antagonists (non selective)

A

CNS: anxiolytic, maybe decr HTN
eye: decr aq humor production and eye pressure

71
Q

What is more prominent in B1/B2 antagonists than in B1 selective antags?

A

Bronchoconstriction”spasm” in the lungs and inhibited lipolysis and glucogenolysis

not good for hyperglycemic (DM)

72
Q

Propranolol Overview
A. Type
B. Effect
C. Use
D. SE
E. Contraindication
F. Withdrawal

A

Propranolol
A. Type: B Antagonist (non selective)
B. Effect: Negative inotropic and chronotropic
C. Use: HTN post MI/other cardiac uses
D. SE: Hyperglycemia, bronchoconstriction
E. Contraindication: Asthma, DM, Hyperthyroidism, preg
F. Withdrawal: Rebound HTN

stop taking beta blockers, incr in NE, B receptors are sensitive, Hypertension sky rockets

73
Q

What can be used as 1st line use for hypertension and over 60?

A

Thiazide, ACEI, ARB, CCB

NOT BETA BLOCKER (not indicated as 1st line therapy for age 60 and above)

74
Q

When are Beta blockers first line therapy for hypertension?

A
  • Ischemic heart disease
  • Recent STEMI or non-STEMI (ST-elevation myocardial infarction)
  • Left ventricular systolic dysfunction
  • some arrythmias

if there is a history of these, THEN you use Beta blockers as 1st line use

75
Q

Since Beta 1 antags have no B2 activity, they are preferred in patients with what conditions?

A

Bronchospasm
Diabetes
Peripheral vascular disease

76
Q

If you have a history of DM and astham, which antagonist can you give?

A

B1

77
Q

Which b1 antag drug is used for heart failure where 1 of 3 recommend, long -acting form: succinate for success?

A

Metoprolol

78
Q

Are B1 antags safe with pregnancy?

A

NO

79
Q

Beta 1 antags have less effects on what?

A

Glucose levels

80
Q

Atenolol and Metoprolol
A. Type
B. Effect
C. Use
D. Withdrawal
E. Notes

A

A. Type: B1 Antagonist
B. Effect: Negative inotropic and chronotropic
C. Use: HTN post MI/other cardiac uses
D. Withdrawal: Rebound HTN
E. Notes: Not B2 so can use for DM and Asthma. Metoprolol has a longer half-life.

81
Q

Which mixed a1/b antag is used for heart failure where 1 of 3 recommend?

A

Carvedilol

82
Q

Which mixed a1/b antag can be used ffor HTN emergency in pregnancy?

A

1 is still methyl dopa

Labetalol

83
Q

Do mixed A1/B antags have more or less reflec tachycardia than A1 antags?

A

LESS b/c of B2

84
Q

Do mixed A1/B antags have more or less peripheral vasoconstriction than with Beta blockers?

A

LESS b/c of A1

85
Q

Carvedilol and Labetalol Overview
A. Type
B. Effect
C. Use
D. Withdrawal
E. Notes

A

A. Type: A1/B Antagonist
B. Effect: Negative inotropic and chronotropic, Vasodilation
C. Use: HTN post MI/other cardiac uses
D. Withdrawal: Rebound HTN
E. Notes: LESS REFLEX TACHY

86
Q

In a paitient with which of the following conditions would propranolol be contraindicated?
A.Tachy
B.Hypertension
C.Constipation
D.Asthma
E.Migraines

A

Asthma

propranolol=non selective B antag
B2 antag effect=bronchoconstriction

Pharmacology (26 decks)

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