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N929: Advanced Pharmacology > Cardiovascular Week 2 > Flashcards

Cardiovascular Week 2 Flashcards

1
Q

What are 5 alpha antagonists?

A
  1. clonidine
  2. phenoxybenzamine
  3. phentolamine
  4. prazosin
  5. sildenafil
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2
Q

What are 6 beta antagonists?

A
  1. Atenolol
  2. Carvedilol
  3. Esmolol
  4. Labetalol
  5. Metoprolol
  6. Propanolol
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3
Q

What type of drug is used to treat

  • pheochromocytoma
  • hypertensive emergencies
  • chronic HTN
  • erectile dysfunction
A

alpha blockers

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4
Q

What type of drug is used to treat

  • HTN
  • ischemic heart disease
  • cardiac arrhythmias
  • heart failure
A

beta blockers

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5
Q

How do ACEi treat HTN?

A

decrease total body volume

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6
Q

How do ARBs treat HTN?

A

decrease total body water

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7
Q

What 6 drugs or class of drugs treat HTN by manipulating vascular tone?

A
  1. Ca channel blockers
  2. K channel openers
  3. Endothelin receptor antagonists
  4. Hydralazine
  5. Alpha 1 antagonists (clonidine)
  6. Beta antagonists
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8
Q

What does activation of a1 cause?

A
  • vasoconstriction

- relaxation of the GI tract

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9
Q

Where are a1 receptors found?

A

presynaptic

vasculature
heart
glands
gut

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10
Q

Where are a2 receptors found & what do they do?

A

presynaptic

  • peripheral vascular smooth muscle
  • coronaries
  • brain
  • *activation = inhibition of norepi release → inhibition of SNS = ↓BP/HR/↓CNS activity

postsynaptic

  • coronaries
  • CNS
    • activation causes constriction, sedation, analgesia
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11
Q

Where are B1 found?

A 
myocardium
SA node
vent-conduction system
coronaries
kidney
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12
Q

What does activation of B1 cause?

A
  • increase inotropy
  • increase chronotropy
  • ↑myocardial conduction - velocity
  • coronary relaxation
  • renin release
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13
Q

Where are B2 receptors found?

A

smooth muscle of vasculature, bronchial, uterus

  • smooth muscle of the skin
  • myocardium
  • coronaries
  • kidneys
  • GI tract
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14
Q

What do B2 receptors do when activated?

A

vasodilation

  • bronchodilation
  • uterine relaxation
  • gluconeogenesis
  • insulin release
  • k uptake by the cells
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15
Q

Is ephedrine a direct or indirect acting?

A

both

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16
Q

Is phenylephrine a direct or indirect acting agent?

A

direct

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17
Q

in the the treatment of HTN, what medications target HR?

2

A
  1. beta blockers

2. calcium channel blockers

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18
Q

in the treatment of HTN, what medications target contractility?
(2)

A
  1. beta-blockers

2. calcium channel blockers

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19
Q

in the treatment of HTN, what medications target venous tone?
(4)

A
  1. a1 antagonists
  2. ACEi
  3. ARB
  4. Nitroprusside
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20
Q

in the treatment of HTN, what medications target Na/H2O retention?

A
  1. diuretics
  2. ACEi
  3. ARB
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21
Q

in the treatment of HTN, what medications target the direct innervation of vascular smooth muscle cells to decrease SVR?

A
  1. a1 antagonists

2. a2 agonists

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22
Q

in the treatment of HTN, what medications target circulating regulators to decrease SVR?

A

a1 antagonists
a2 agonists
ACEi
ARB

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23
Q

in the treatment of HTN, what medications target local regulators to decrease SVR?

A
  1. endothelin antagonists
  2. nitroprusside
  3. ACEi
  4. ARB
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24
Q

in the treatment of HTN, what medications target local regulators to decrease SVR?

A
  1. endothelin antagonists
  2. nitroprusside
  3. ACEi
  4. ARB
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25
Q

What are the 2 biggest cardiovascular effects of anesthetics?

A
  1. decreased SVR = decreased BP

2. depressed myocardial contractility

26
Q

What are 4 types of receptors located in the peripheral nervous system?

A
  1. alpha
  2. beta
  3. nicotinic
  4. muscarinic
27
Q

Stimulation of beta receptor results in activation of

A

adenyl cyclase →

↑cAMP

28
Q

Increased cAMP from beta receptor activation causes..

A

↑ kinase activation & phosphorylation

29
Q

B1,2,3 receptors are what kind of GPCR?

A

Gs

30
Q

In the physiological response of Beta receptors, increased cAMP results in…

A

relaxation of smooth muscle & stimulation of cardiac contractility

31
Q

What are the second messengers of a1 activation?

A

PLC
IP3 & DAG
PKC & increased free Ca2+

32
Q

What are the second messengers of a2 activation?

A
  1. inhibition of adenylate cyclase
  2. ↓cAMP
  3. ↑K conduction
33
Q

What does ↓cAMP from a2 activation cause?

A

smooth muscle contraction

- K hyperpolarization

34
Q

What does PLC, IP3/DAG, & PKC/↑ free Ca2+ from a1 activation cause?

A

smooth muscle vasoconstriction

35
Q

a2 is excitatory or inhibitory?

A

inhibitory

36
Q

a1 is excitatory or inhibitory?

A

excitatory

↑Ca++ → calmodulin activation → ↑actin/myosin interaction → sm muscle contraction

37
Q

a2 is excitatory or inhibitory?

A

inhibitory

↓cAMP → ↓norepinephrine release

38
Q

In the treatment of HTN, what 4 classes of drugs targets the SNS?

A
  1. B-antagonists
  2. a1 antagonists
  3. mixed a/B antagonists
  4. centrally acting a2 agonists
39
Q

In the treatment of HTN, what 3 classes of drugs target the RAAS

A
  1. ACEi
  2. ARB
  3. Diuretics
40
Q

In the treatment of HTN, what classes of drugs target endothelium derived mediator and/or ion channel modulators?

A
  1. direct vasodilators (nitroprusside, hydralazine)
  2. calcium channel antagonists
  3. potassium channel opener
41
Q

What is a normal BP?

A

120/80

42
Q

What is the treatment threshold for those <60yr
or
>60yr with renal dz or diabetes?

A

140/90 or greater

43
Q

What is the treatment threshold for those >60yr w/o DM or renal dz?

A

150/90 or greater

44
Q

What is the first line therapy for HTN treament?

A

thiazide diuretic UNLESS there is a “compelling indication”

45
Q

Why do most patients require at least 2 medications to reach their BP goal?

A

physiological compensations

46
Q

What is the threshold for a hypertensive URGENCY?

A

DBP >120 with evidence of

progressive end organ DAMAGE

47
Q

What is the goal when a patient has a hypertensive urgency? & what medication is used?

A

goal, decrease DBP to 100-105 w/n 24 hours

Clonidine

48
Q

What is the threshold for a hypertensive CRISIS?

A

DBP >120 with evidence of end organ FAILURE

49
Q

What is the goal when a patient has a hypertensive CRISIS?

A

decrease DBP 100-105 ASAP

50
Q

What 4 medications can be used to treat a hypertensive crisis?

A
  1. Nitroprusside
  2. Nitroglycerin
  3. Labetalol
  4. Fenoldapam
51
Q

What are the three competitive alpha antagonists?

A

Phentolamine, Prazosin, Yohimibine

52
Q

What is an alpha antagonist that covalently binds and is difficult to overcome?

A

phenoxybenzamine

53
Q

When must you give an a antagonist?

A

BEFORE you B-block a

pheochromocytoma or local anesthetic toxicity

54
Q

What are 2 non-selective alpha antagonists?

A

phenoxybenzamine

phentolamine

55
Q

What are 5 a1 selective antagonists?

A 
prazosin
terazosin
doxazosin
aifuzosin
tamsulosin
56
Q

What is 1 a2 selective antagonist?

A

yohimbine

57
Q

What are 5 non-selective FIRST generation beta antagonists?

A 
Nadolol
Penbutolol
Pindolol
Propranolol
Timolol
58
Q

What are 5 B1 selective beta antagonists?

A 
acebutolol
atenolol
bisoprolol
esmolol
metoprolol
59
Q

What are 4 non-selective THIRD generation beta antagonists?

A

Carteolol
Carvedilol
Bucindolol
Labetolol

60
Q

What are 3 B1 selective THIRD generation beta antagonists?

A

betaxolol
caliprolol
nebivolol

61
Q

What are the mixed a and B antagonists?

A

labetalol

carvedilol

N929: Advanced Pharmacology (6 decks)

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