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Pharmacology > CHAPT 11: ANTIHYPERTENSIVE AGENTS > Flashcards

CHAPT 11: ANTIHYPERTENSIVE AGENTS Flashcards

1
Q

the most common cardiovascular disease

A

hypertension

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2
Q

sustained arterial hypertension damages blood vessels in what organs?

A

kidney heart and brain

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3
Q

sustained arterial hypertension damages blood vessels in kidney heart and brain leads to an increased incidence of ___ __ __ __ _

A

renal failure
coronary disease
heart failure
stroke
dementia

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4
Q

Epidemiologic studies indicate that the risks of damage to
kidney, heart, and brain are directly related to the extent of ?

A

blood pressure elevation

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5
Q

normal blood pressure

A

< 120 / 80 mm Hg

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6
Q

BP of hypertension

A

≥ 140 / 90 mm Hg

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7
Q

Both systolic hypertension and diastolic hypertension are associated with end-organ damage; so-called ___

A

isolated systolic
hypertension

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8
Q

Patients in whom no specific cause of hypertension can
be found are said to have?

A

essential or primary hypertension

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9
Q

Patients with a specific etiology are said to have

A

secondary hypertension

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10
Q

In most cases, elevated blood pressure is associated with an
overall ___ through arterioles,
whereas ___ is usually normal.

A

increase blood flow, cardiac output

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11
Q

normal regulation of BP

A

BP = CP X PVR

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12
Q

physiologically, how does BP is maintained by the body?

A

moment-to-moment regulation of cardiac output and peripheral vascular resistance

book figure 11-1
1. resistance arterioles
2. capacitance venules
3. pump output heart

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13
Q

A fourth anatomic control
site to maintain BP in the body is, __, contributes to ___ by regulating the volume of intravascular fluid.

A

kidney, maintenance of blood pressure

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14
Q

a reflex mediated by autonomic nerves act in combination with humoral
mechanisms, including the renin-angiotensin-aldosterone system, to coordinate function at these four control sites and to maintain normal blood pressure.

A

baroreflex

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15
Q

responsible for rapid, moment-to-moment adjustments in blood pressure, such as in transition from a reclining to
an upright posture

A

baroreflexes

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16
Q

are stimulated by the stretch of the vessel walls brought about by the internal pressure (arterial blood pressure).

A

carotid baroreceptors

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17
Q

An organ that is primarily responsible
for long-term blood pressure control.

A

kidney

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18
Q

what happens when there is a reduction in renal perfusion?

A

it causes intrarenal redistribution of BF and increased reabsorption of salt and water.

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19
Q

decreased pressure in renal arterioles as well as sympathetic neural activity (via β adrenoceptors) stimulates production of ___ which increases production of ___

A

renin, angiotensin II

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20
Q

angiotensin II causes?

A
  1. direct constriction of resistance vessels
  2. stimulates aldosterone synthesis in adrenal cortex, which increases renal sodium absorption and intravascular BV.
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21
Q

a hormone released by the posterior pituitary gland that has the ability to regulate water reabsorption in the kidney

A

vasopressin

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22
Q

site of action of reserptine, guanethidine, guanadrel?

A

sympathetic nerve terminals

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23
Q

site of action of methyldopa, clonidine, guanabenz, guanfacine

A

vasomotor center

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24
Q

site of action of trimethaphan?

A

sympathetic ganglia

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25
Q

site of action of aliskiren

A

inhibits production of renin from angiotensinogen

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26
Q

antihypertensive agents which lower blood pressure by depleting the body of
sodium and reducing blood volume and perhaps by other
mechanisms.

A

diuretics

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27
Q

antihypertensive agents which lower blood pressure by reducing peripheral vascular resistance, inhibiting cardiac function, and increasing venous pooling in capacitance vessels.

A

sympathoplegic agents

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28
Q

antihypertensive agents which reduce pressure by relaxing vascular smooth muscle, thus dilating resistance vessels and—to varying degrees—increasing capacitance as well.

A

direct vasodilators

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29
Q

antihypertensive agents reduce peripheral vascular resistance and (potentially) blood volume.

A

agents that block production or action of angiotensin

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30
Q

most common adverse effect of diuretics

A

potassium depletion

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31
Q

drugs that are most effective when used concomitantly with a diuretic

A

sympathoplagic antihypertensive drugs

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32
Q

an analog of L-dopa and is converted to a-methyldopamine and a-methylepinephrine

A

methyldopa

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33
Q

where are a-methylnorepinephrine stored?

A

adrenergic nerve vesicles where is stoichiometrically replaces norepinephrine and is released by nerve
stimulation to interact with postsynaptic adrenoceptors

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34
Q

clonidine binds to a nonadrenoceptor site where this receptor also mediate antihypertensive effects

A

imidazoline receptor

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35
Q

centrally active antihypertensive drugs that share the central α adrenoceptor-stimulating
effects of clonidine.

A

guanabenz and guanfacine

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36
Q

was widely used in the past but is now used primarily for hypertension during pregnancy

decreases peripheral vascular resistance, decrease HR and CO

A

methyldopa

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37
Q

methyldopa enters the brain via what transporter

A

aromatic amino acid transporter

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38
Q

usual oral dose of methyldopa produces its
maximal antihypertensive effect in what hour

A

4-6 hours, and the effect can persist for up to 24 hours

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39
Q

most common adverse effect of methyldopa

A

sedation, particularly at the onset of treatment.

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40
Q

another toxic effect of methyldopa that is mediated by inhibition of dopaminergic mechanism in the hypothalamus, resulting with an increased prolactin secretion that can occur in men and women

A

lactation

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41
Q

how do you reduce the toxicity of methyldopa

A

Discontinuation of the drug

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42
Q

drug that reduces blood pressure in the supine position and only rarely causes postural hypotension

A

clonidine

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43
Q

characteristics of clonidine

A
  1. it is lipid soluble (can easily enter the brain from the circulation)
  2. short half life
  3. orally, twice a day to maintain smooth BP level
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44
Q

toxicity of clonidine

A

dry mouth and sedation are common

patients who are at risk for mental depression.

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45
Q

drugs that lower blood pressure by preventing normal physiologic release of norepinephrine from postganglionic sympathetic
neurons.

A

adrenergic neuron blocking agents

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46
Q

a polar drug that can produce profound sympathoplegia effects in high enough doses that inhibits the release of norepinephrine from sympathetic nerve endings

A

guanethidine

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47
Q

is transported across the sympathetic nerve membrane by NET and uptake its essential for drugs action. It is concentrated in the transmitter vesicles, where it replaces norepinephrine and causes a gradual depletion of norepinephrine stores in the nerve ending.

A

guanethidine

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48
Q

half life of guanethidine

A

5 days

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49
Q

this toxicity is often associated with sympatomatic postural hypotension and hypotension following exercise.

in men, it may be associated with delayed retrograde ejaculation (into the bladder)

commonly causes diarrhea results from increased gastrointestinal motility

can produce hypertensive crisis by releasing catecholamines in patients with pheochromocytoma

A

Guanethidine

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50
Q

an alkaloid extracted from rauwolfa serpentina and was the first effective drugs used in treatment for hypertension.

A

reserpine

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51
Q

MOA that blocks VMAT transporter which causes a depletion of norepinephrine, epinephrine, dopamine and serotonin in CNS and PNS

A

reserpine

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52
Q

is reserpine reversible or irreversible?

A

irreversible; trace amounts of the drug remain bound to vesicular membranes for many days.

53
Q

reserpine readily enters the ___ and depletion of cerebral amine causes sedation, mental depression and parkinsonism symptoms

A

brain

54
Q

At lower doses used for treatment of mild hypertension, ___ lowers blood pressure by a combination of decreased cardiac
output and decreased peripheral vascular resistance.

A

reserpine

55
Q

low dose effect and high dose effect of reserpine

A

low dose - produces little postural hypotension
high dose - produce sedation, lassitude, nightmares and severe mental depression

56
Q

some toxic effects of reserpine

A

patient wish history of depression should not take reserpine

often produces mild diarrhea and GI cramps and increases gastric acid secretion

57
Q

the prototypical B blocking drug

A

propranolol

58
Q

was the first B blocker to be effective in hypertension and ischemic heart disease

A

propranolol

59
Q

is propranolol selective or non selective?

A

nonselective B blockade

60
Q

metoprolol is extensively metabolized by?

A

by CYP2D6 with high first pass elimination

61
Q

Resting bradycardia and a reduction in the heart
rate during exercise are indicators of what drug effect

A

propranolol’s B-blocking effect

62
Q

very widely used B blockers that is not extensively metabolized and is excreted primarily in the urine with a half-life of 6 hours

A

atenolol

63
Q

toxic effect of propranolol

A

since it is nonselective, it has effects on both B receptors

B1 - bradycardia, cardiac conduction disease

B2 - patients with asthma, peripheral vascular insufficiency and diabetes

can receive withdrawal syndrome after prolonged regular use ( B blockers should not be discontinued abruptly)

64
Q

drugs that are cardioselective and the most widely used B blockers in the treatment of hypertension

A

metoprolol and atenolol

65
Q

is approximately equipotent to propranolol in inhibiting stimulation of β1 adrenoceptors such as those in the heart but 50- to 100-fold less potent than propranolol in blocking β2 receptors.

A

metoprolol

66
Q

nonselective β-receptor antagonists, are not appreciably metabolized and are excreted to a considerable extent
in the urine.

A

nadolol and carteolol

67
Q

are β1-selective blockers that are primarily metabolized in the liver but have long half lives.

A

betaxolol and bisoprolol

68
Q

are partial agonist B blockers with some intrinsic sympathomimetic activity. they lower BP but are rarely used in hypertension

A

pindolol, acebutolol and penbutolol

69
Q

has both B blocking and vasodilating effects.

formulated as a racemix mixture of four isomers

S,S and R,S - inactive isomers
S,R - potent a blocker
R,R - potent B blockers

A

labetalol

70
Q

has a 3:1 ratio of β:α antagonism after oral dosing. Blood pressure is lowered by reduction of systemic vascular resistance (via
α blockade)

A

labetalol

71
Q

useful in treating the hypertension of pheochromocytoma and hypertensive emergencies

A

labetalol

72
Q

similar to labetalol, has a racemix mixture but has different isomers

S- - nonselective B adrenoceptor blocker
S- and R+ - equal a blocking potency

A

carvedilol

73
Q

a non selective B adrenoceptor blocker that reduces mortality in patients with heart failure and is
therefore particularly useful in patients with both heart failure and
hypertension.

A

carvedilol

74
Q

a β1-selective blocker with vasodilating properties
that are not mediated by α blockade.

A

Nebivolol

75
Q

β1-selective blocker that is rapidly metabolized
via hydrolysis by red blood cell esterases. and is administered by intravenous infusion.

A

Esmolol

76
Q

3 drugs that produce most of their antihypertensive effects by selectively blocking α1 receptors in arterioles
and venules.

These agents produce less reflex tachycardia when
lowering blood pressure than do nonselective α antagonists such
as phentolamine.

A

Prazosin, Terazosin and doxazosin

77
Q

are useful in diagnosis and treatment of pheochromocytoma and in other clinical situations associated with exaggerated release of catecholamines

A

phentolamine and phenoxybenzamine

78
Q

oral vasodilators that are used for long term outpatient therapy of hypertension

A

hydralazine and minoxidil

79
Q

parenteral vasodilatory which are used to treat hypertensive emergencies: the calcium channel blockers

A

nitroprusside and fenoldopam

80
Q

where are nitrates used?

A

mainly in ischemic heart disease

81
Q

a hydrazine derivative, dilates arterioles but not
veins. it is more effective when combined with nitrates in heart failure and with both hypertension and heart failure

A

hydralazine

82
Q

is hydralazine absorbed and rapidly metabolized by the liver during the first pass?

A

yes, so that its bioavailability is low (averaging 25%)

83
Q

characteristics of rapid acetylators

A

have greater first pass metabolism

lowers BP

less antihypertensive efefct

84
Q

mechanism of action of vasodilators

release of nitric oxide from drug or endothelium

A

nitroprusside, hydralazine, nitrates, histamine, acetylcholine

85
Q

mechanism of action of vasodilators

reduction of calcium influx

A

verapamil, diltiazem, nifedipine

86
Q

mechanism of action of vasodilators

hyperpolarization of cell membrane through opening of potassium channels

A

minoxidil and diazoxide

87
Q

mechanism of action of vasodilators

activation of dopamine receptors

A

fenoldopam

88
Q

common adverse effect of hydralazine

A

headache, nausea, anorexia, palpitations, sweating and flushing

89
Q

very efficacious orally active vasodilator. results from the opening of potassium channels in smooth muscle
membranes by minoxidil sulfate, the active metabolite.

A

minoxidil

90
Q

active metabolite of minoxidil

A

minoxidil sulfate

91
Q

causes rebound hypertension

A

clonidine

92
Q

releases NO from endothelial cells to dilate BV

A

hydralazine

93
Q

like hydralazine, ____ dilates arterioles but not veins

A

minoxidil

94
Q

use of topical minoxidil

A

to correct baldness

95
Q

a powerful parenterally administered
vasodilator that is used in treating hypertensive emergencies as
well as severe heart failure.

dilates both arterial and venous vessels. Activates guanylyl cyclase.

A

sodium nitroprusside

96
Q

an effective and relatively long-acting potassium channel opener that causes hyperpolarization in smooth muscle
and pancreatic β cells.

A

diazoxide

97
Q

a peripheral arteriolar dilator used for hypertensive
emergencies and postoperative hypertension. It acts primarily as an
agonist of dopamine D1 receptors, resulting in dilation of peripheral arteries and natriuresis

A

fenoldopam

98
Q

what is natriuresis

A

secretion of sodium in urine

99
Q

has the greatest depressant effect on the heart and may
decrease heart rate and cardiac output.

A

verapamil

100
Q

family of dihydropyridine

A

amlodipine, felodipine, isradipine, nicardipine, nifedipine, nisoldipine and nitridipine

101
Q

agents that are more selective as vasodilators and have less cardiac depressant effect than verapamil and diltiazem

A

difedipine and other dihydropyridine agents

102
Q

what acts on angiotensinogen to yield the inactive precursor decapeptide angiotensin I?

A

Renin

103
Q

Angiotensin I is primarily converted by ____ to the arterial vasoconstrictor ___

A

endothelial ACE (kininase II) , Angiotensin II

104
Q

where does angiotensin III being converted?

A

in the adrenal gland

105
Q

what activity does angiotensin II has?

A

vasoconstrictor and sodium-retention activity

106
Q

Three classes of drugs that act specifically on the renin-angiotensin system?

A

ACE inhibitors
Losartan and other non-peptide antagonist
Aliskiren

107
Q

Drugs that are aldosterone receptor inhibitors

A

Spironolactone, eplerenone

108
Q

This class of drugs inhibbit the converting enzyme peptidyl dipeptidase that hydrolyzes angiotensin I to angiotensin II and inactivates bradykinin

A

Angiotensin-converting enzyme (ACE) inhibitors

109
Q

a bradykinin B2 receptor antagonist that blunts the blood pressure lowering effect of captopril

A

Icatibant

110
Q

An ACE inhibitor oral prodrug that is converted by hydrolysis to converting enzyme inhibitor, enalaprilat

A

Enalapril

111
Q

Cleaves kininogen to release bradykinin (a potent vasodilator)

A

Kallikrein

112
Q

what inhibits the breakdown of bradykinin to inactive metabolites

A

ACE inhibitors

113
Q

Why ACE inhibitors are useful in treating patients with chronic kidney disease?

A

They diminish proteinuria and stabilize renal function.

114
Q

Toxicity of ACE inhibitors

A

Severe hypotension in patients who are taking diuretics

Risk of fetal hypotension, anuria and renal failure for pregnant females during second and third trimester

115
Q

First marketed blockers of the angiotensin II type (AT1) receptor.

A

Losartan and valsartan

116
Q

A more selective blockers of angiotensin effects than ACE inhibitors . And also why?

A

Angiotensin receptor blocking agents. Because there are enzymes other than ACE that are capable of generating angiotensin II

117
Q

Are commonly used in patients who have had adverse reaction to ACE inhibitors

A

Angiotensin receptor blocking agents

118
Q

Why does combining ACE inhibitor and ARB or aliskiren inhibited?

A

Though they are useful for complete inhibition of renin-angiotensin system, they are not recommended due to toxicity levels

119
Q

What is proteinuria

A

Abnormal amounts of protein in the urine

120
Q

3 Initial step in treating hypertension may be nonpharmacologic.

A

Sodium restriction.
Weight reduction
Regular exercise

121
Q

Reasonable dietary goal (sodium intake) in treating hypotension

A

70-100 mEq of sodium per day

122
Q

Underlying pathologic process in malignant hypertension

A

Progressive arteriopathy with inflammation and necrosis of arterioles

123
Q

Summary: MOA

Activates a2 adrenoceptors

A

Clonidine and methyldopa

124
Q

Summary: MOA

Blocks aldosterone receptor in renal collecting tubule

A

Spironolactone and eplerenone

125
Q

Summary: MOA

Selectively blocks a1 adrenoceptors

A

Prazosin, terazosin, doxazosin

126
Q

Widely used B1 selective blockers

A

Metoprolol and atenolol

127
Q

nonselective prototype B blocker

A

Propranolol

128
Q

Summary: MOA

Blocks AT1angiotensin receptors

A

Losartan

129
Q

Summary: MOA

Inhibits enzyme activity of renin

A

Aliskiren

Pharmacology (15 decks)

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