Antihypertensives part 2 Flashcards

1
Q

What are the different groups of sympathetic antagonist agents

A

Alpha
Beta
*mix of the two
Adrenergic blocking drugs

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2
Q

What are the sites of action for sympathoplegic drugs

A

Peripherally
Centrally
Ganglionic

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3
Q

What drugs block sympathetic system at the peripheral level

A

Prazosin
Doxazosin
Metoprolol
Pindolol

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4
Q

What drugs block the sympathetic system centrally

A

Clonidine

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5
Q

What drugs block the sympathetic system ganglionically

A

Trimethaphan

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6
Q

What is the indication for clonidine

A

Menopausal flushing
opioid/alcohol withdrawal
tourettes
2nd line for ADHD

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7
Q

What is the MOA for clonidine

A

Blocks release of norepinephrine and inhibits sympathetic outflow from the brain

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8
Q

What are the pharmacokinetics of clonidine

A

Oral
don’t take with food
crosses placenta
narrow TI
dose adjust for renal patients

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9
Q

What are some side effects / contraindications of clonidine

A

dysrhythmias
bradycardia
AV block
anorexia
confusion / delirium

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10
Q

Where are alpha 1 receptors found

A

smooth muscle

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11
Q

Where are alpha 2 receptors found

A

Brain stem AND smooth muscle

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12
Q

What are non-selective alpha blocker drugs

A

Phenoxybenzamine
Phentolamine

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13
Q

What is the indication of phenoxybenzamine

A

Sweating and HTN associated with pheochromocytoma

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14
Q

What is the MOA of phenoxybenzamine

A

Irreversible, non-selective blockade of peripheral alpha 1&2 receptors
-decrease vasoconstriction

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15
Q

What are the pharmacokinetics of phenoxybenzamine

A

Oral / IV
Long lasting effects

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16
Q

What are the side effects / adverse reactions of phenoxybenzamine

A

Reflex tachycardia
Orthostatic hypotension
nasal stuffiness / N/V
Inhibit ejaculation

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17
Q

What is the indication of phentolamine

A

Dx / Tx of pheochromacytoma
particular associated with HTN emergencies

Tx of dermal necrosis following extravasation of norepinephrine

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18
Q

What is the MOA of phentolamine

A

Reversible, non-selective blockade of peripheral alpha 1&2 receptors

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19
Q

What are the pharmacokinetics of phentolamine

A

IM or IV
effects last 4 hours

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20
Q

What are the side effects of phentolamine

A

Reflex tachy
orthostatic hypotension

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21
Q

What are the alpha-1 selective blockers

A

Prazosin
doxazosin

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22
Q

What are prazosin & Doxazosin used for

A

-HTN
-Benign prostatic hyperplasia d/t prostate muscle relaxation
-PTSD associated nightmares

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23
Q

What are the MOA of selective alpha-1 blockers

A

Selective a1 inhibition = decrease vasoconstriction

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24
Q

What are the side effects of prazosin and doxazosin

A

Dizziness
lack of energy
nasal congestion
HA
Drowsiness
orthostatic hypotension

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25
Q

What selective alpha 1 blocker is longest acting `

A

Doxazosin

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26
Q

What drugs are nonselective beta antagonists

A

Propranolol
nadolol
pindolol
timolol

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27
Q

What is the indication for propranolol

A

performance anxiety
postural tremor
migraine prophylaxis
thyrotoxicosis
portal HTN

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28
Q

What is the MOA of propranolol

A

Nonselective B1 & B2 inhibition

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29
Q

What is the pharmacokinetics of propranolol

A

oral admin 1x/day
extensively metabolized and excreted in urine

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30
Q

What are the adverse effects / side effects of propranolol and nadolol

A

Bronchoconstriction
dizziness
lethargy
visual disturbance
short term memory loss
vivd dreams

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31
Q

What is the indication of Nadolol

A

HTN
Management of chronic angina
more potent that propranolol (rarely used)

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32
Q

What is the MIA of nadolol

A

Non-selective Beta 1&2 inhibition

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33
Q

What are the pharmacokinetics of nadolol

A

Oral admin
1/2t of 14-24 hours

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34
Q

What is the indication of pindolol

A

HTN

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35
Q

What is the MOA of pindolol

A

PARTIAL beta 1&2 agonist

*at high doses, posses similar effects of epi

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36
Q

What are the adverse effects / contraindications of pindolol

A

Bronchoconstriction
Dizziness
Hallucinations
Short term memory loss
vivid dreams
*Avoid in patients with previous MI / angina

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37
Q

What is the indication for timolol

A

Chronic glaucoma management (open angle)

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38
Q

What is the MOA of timolol

A

Non-selective beta 1&2 inhibition

reduces production of aqueous humor in the eye

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39
Q

What is the pharmacokinetics of timolol

A

Topical
oral can be used for HTN (rare)

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40
Q

What are the selective beta 1 sympathetic antagonists

A

Metoprolol
atenolol
nebivolol

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41
Q

What is the indication for metoprolol

A

HTN
Stable / unstable angina
acute MI
SVT / Vtach
Tachycardia
Chronic stable HF
Migraine prophylaxis

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42
Q

What is the pharmacokinetics of metoprolol

A

Oral
Extensively metabolized
1/2t = 3-4 hours

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43
Q

What are the side effects / contraindications of metoprolol

A

Bradycardia
decrease CO
AV heart block

**NOT approved for acute HF

44
Q

What is the indication of atenolol

A

Same as metoprolol just less effective

45
Q

What is the pharmacokinetics of atenolol

A

Excreted primarily in urine
1/2t = 6hours

46
Q

What are the side effects of atenolol

A

Bradycardia
reduced CO
AV heart block

47
Q

What is the indication for nebivolol

A

HTN
HF

48
Q

Which selective beta 1 blocker is MOST cardio selective

A

Nebivolol

49
Q

What is the side effects of nebivolol

A

Bradycardia
Reduced CO
AV heart block

50
Q

what does nebivolol stimulate

A

beta 3 receptors in peripheral vasculature = vasodilation from being nitric oxide potentiating

51
Q

Which drugs are both alpha and beta blockers

A

Carvedilol
Labetolol

52
Q

What is the indication for carvedilol

A

Primarily in chronic stable HF
-decreases mortality rates in patients after MI

53
Q

What is the MOA of carvedilol and labetolol

A

Nonselectively blocked alpha 1, beta 1, beta 2

peripheral vasodilation

54
Q

What is the pharmacokinetics of carvedilol

A

Oral
1x/day

55
Q

What is the pharmacokinetics of labetolol

A

Oral / IV
SAFE IN PREGNANCY (often used in preeclampsia)

can be taken up to 3x daily

56
Q

What are the side effects of labetolol and cavedilol

A

Orthostatic hypotension
dizziness
hypoglycemia

57
Q

Which drugs are cardio-selective calcium channel blockers? (non-dihydropyridines)

A

Verapamil
Diltiazem

58
Q

What is the indication of use for verapamil and diltiazem

A

stable / vasospastic angina
essential HTN
dysrhythmias

59
Q

What is the MOA for non-dihydropyridine ca2+ channel blockers

A

-Selectively blocks Ca2+ channels in the myocardium = decr arterial pressure, incr coronary perfusion, decr heart rate, decr AV nodal conduction, decr force of contraction

60
Q

What are the pharmacokinetics of verapamil

A

Oral or IV
hepatic metabolism
dose adjust for renal impairment

61
Q

What is the pharmacokinetics of diltiazem

A

oral
50% bioavailability
effects begin quickly and peak in 30min

62
Q

What are the side effects / contraindications of verapamil and diltiazem

A

Constipation
bradycardia
AV block
HF
hypotension
LE edema

Contra in patients with heart block and heart failure

63
Q

Which drugs are dihydropyridines

A

Nifedipine
amlodipine

64
Q

What is the indication for nifedipine

A

HTN
stable / vasospastic angina
migraine
reynauds

65
Q

What is the indication of amlodipine

A

HTN
Stable and vasospastic angina
**VERY COMMON

66
Q

What is the MOA of nifedipine and amlodipine

A

Blocks Ca2+ channels in arterioles (vasodilation)
-Does not alter conduction through AV node

67
Q

What are the side effects of nifedipine

A

-Flushing, dizziness, headache, LE edema, gingival hyperplasia, reflex tachycardia
-Avoid in pts w HF, grapefruit juice

68
Q

What is the side effects of amlodipine

A

Lightheadedness, hypotension, bradycardia, LE edema
-Avoid in pts w HF, grapefruit juice

69
Q

What drugs are venous vasodilators

A

Isosorbide dinitrate
Nitroglycerine

70
Q

what is the indication for nitroglycerine

A

All types of angina
severe HTN

71
Q

What is the MOA for venous vasodilators

A

Converted to nitric oxide in the body -> vasodilation -> decr cardiac O2 demand

72
Q

What is the indication for isosorbide dinitrate

A

angina prophylaxis
esophageal spasm
HF tx in black people in combo with hydralazine

73
Q

What is the pharmacokinetics of nitroglycerine

A

Sublingual
IV, path, or ointment also available
-pro-drug

74
Q

What is the pharmacokinetics of isosorbide dinitrate

A

Sublingual / oral taken daily

75
Q

What are the side effects / contraindications of nitroglycerine and Isosorbide dinitrate

A

HA
Hypotension
tachycardia
*tolerance can rapidly develop
* drug interactions with PDE-5i

76
Q

What are arterial vasodilator drugs

A

Hydralazine
Diazoxide
minoxidil

77
Q

What is the indication of hydralazine

A

Essential HTN
Almost always given w/ beta blocker
-used to decrease after load in pts. w/ HF

78
Q

What is the MOA of hydralazine

A

-Exact MOA unknown
-Selective dilation of arterioles -> decr peripheral resistance and decr BP

79
Q

What is the pharmacokinetics of hydralazine

A

oral / IV
Inactivated by acetylation
*dose adjust in acetylators

80
Q

What is the side effects / contraindications of hydralazine

A

Postural hypotension
HA
N
reflex tachy
SLE syndrome

81
Q

What is the indication of minoxidil

A

Patient with severe HTN who are unresponsive to safer drugs

*stimulant for hair growth

82
Q

What is the MOA for minoxidil

A

Opens K+ channels in vascular smooth muscle -> K+ flows out, decr cells ability to contract -> arteriolar dilation -> decr periph resistance and decr BP

83
Q

What is minoxidil metabolized into

A

minoxidil sulfate

84
Q

What are the side effects of minoxidil

A

Reflex tachycardia
Na+ / H2O retention
excessive hair growth

85
Q

What is the indication of Diazoxide

A

Acute / malignant HTN
Hypoglycemia (prevents insulin release from pancreas)

86
Q

What is the MOA of Diazoxide

A

Long acting K+ channel opener = Na+ and water retention

87
Q

What is the side effects of diazoxide

A

Excessive hypotension
-some cases resulted in stroke and MI

88
Q

What drugs are vasodilators for both arteries and veins

A

Nitroprusside

89
Q

What is the indication for sodium Nitroprusside

A

HTN emergencies

90
Q

What is the MOA for Nitroprusside

A

Breaks down and releases nitric oxide, activates guanylate cyclase = catalyze the production of cyclic GMP = relaxation in smooth muscles in arterioles and veins to decrease BP

91
Q

What is the pharmacokinetics of nitroprusside

A

Continuous IV infusion
*Effects begin w/in seconds

92
Q

What are the side effects of nitroprusside

A

Cyanide poisoning
thiocyanate toxicity

93
Q

What agents are centrally acting (alpha 2 blockers)

A

Clonidine
Methyldopa

94
Q

what is the indication of clonidine

A

Menopausal flushing
opioid / alcohol withdrawal / Tourettes

*second line agent for ADHD

95
Q

What is the indication for methyldopa

A

Mostly for HTN during pregnancy

96
Q

What is the MOA of clonidine and methyldopa

A

Agonist at centrally located a2 receptors = inhibits further release of norepi and inhibits sympathetic outflow from the brain

97
Q

What are the side effects of clonidine

A

Rebound hypertension
lethargy
sedation
xerostoma
constipation

98
Q

What are the side effects of mehtyldopa

A

Sedation
occasional lactation

*Long term can lead to autoimmune hemolytic anemia

99
Q

Which patients should be started on combination therapy immediately for hypertension

A

BP is greater than 20mmHg above systolic goal OR 10mmHg above diastolic goal

100
Q

What drug classes are best for treating high risk angina pectoris

A

Beta blockers (1st choice)`
calcium channel blockers

101
Q

What drug classes are best for treating hypertension in diabetics

A

Diuretics
ACE inhibitors
ARBs

102
Q

Which drugs should be used for treating HTN in someone who had a stroke

A

ACE inhibitors

103
Q

Which drugs should be used for treating HTN in HF

A

Diuretics
Beta blockers
ACE-i
ARBs
Aldosterone receptor antagonists

104
Q

Which drugs should be used to treat HTN in someone with a history of MI

A

Beta clockers
ACE-i
Aldosterone receptor antagonists

105
Q

If someone has CKD, how would you treat NTN

A

ACE-i
ARBs