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Pharmacology II Exam II CSV Drugs > Antihypertensives > Flashcards

Antihypertensives Flashcards

1
Q

How many children in the U.S. have hypertension?

A

4% of youth, and another 10% have elevated BP (prehypertension)

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2
Q

What is directly proportional to cardiac output and peripheral vascular resistance

A

Arterial blood pressure

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3
Q

Cardiac output and peripheral vascular resistance are controlled by what?

A

Baroreflexes and Renin-Angiotensin-Aldosterone System (RAAS)

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4
Q

Define primary or essential hypertension?

A

Hypertension with no identifiable cause

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5
Q

Define resistant hypertension?

A

Despite lifestyle modifications, diuretic and 2 other medications, no to little improvement in BP control (need to rule out secondary cause)

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6
Q

What is the goal of treatment in treating pulmonary hypertension?

A

Aimed at lessening symptoms and improving quality of life due to no cure

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7
Q

What are the end-stage complications of uncontrolled HTN?

A

Heart Disease
Heart Failure
Stroke
Chronic Kidney Disease

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8
Q

What are the types of diuretics used for hypertension?

A

Distal tubule diuretics (Thiazides)
K-sparing diuretics
Loop diuretics
Carbonic Anhydrase Inhibitors
Osmotic Diuretics

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9
Q

What is the general MOA of diuretics?

A

Increase water and sodium excretion to lower blood volume which in turn decrease BP

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10
Q

What is the MOA of Distal Tubule Diuretics (Thiazides)?

A

Inhibit sodium and chloride reabsorption in the distal tubule, resulting in mild diuresis (increases water and sodium exrection)

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11
Q

What is the site of action of Thiazides?

A

Proximal Tubule

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12
Q

What are the most commonly used diuretic?

A

Thiazides

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13
Q

What are the different Thiazides?

A

Hydrochlothiazide
Chlorthalidone
Metolazone
Indapamide

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14
Q

What is the use of hydrochlorthiazide?

A

Ideal starting agent for HTN, chronic edema, idiopathic hypercalcinuria

Treat kidney stones in Meniere’s disease, but inneffective in renal impairment

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15
Q

What is a severe side effect in hydrochlorthiazide?

A

Increases toxicity of digitalis or lithium

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16
Q

What are the contraindications of Hydrochlorothiazide?

A

Avoid in patients with gout

Can cause hypokalemia, especially if given with corticosteroids or ACTH

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17
Q

What are the side effects of Hydrochlorothiazide?

A

Hypokalemia
Hyperruricemia
Hyperglycemia
Hypotension
Hyponatremia
Hypercalcemia

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18
Q

When treated with Hydrochlorothiazide what co-administration can cause orthostatic hypotension?

A

Alcohol, Barbiturates, and Narcotics

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19
Q

What is the PK of Hydrochlorothiazide?

A

Oral admin, onset in 2 hours. Absorbed rapidly and eliminated primarily unchanged

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20
Q

What is the only Thiazide available in intravenous formulation, although use is very rare?

A

Chlorthalidone

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21
Q

What are the clinical uses of Chlorthalidone?

A

HTN, HF, hypercalciuria, diabetes

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22
Q

What is the MOA of Loop Diuretics?

A

Blocks reabsorption of sodium and chloride in the thick segment of the ascending loop of Henle, prevents passive reabsorption of water

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23
Q

What is the most commonly used loop diuretic?

A

Furosemide

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24
Q

What are the clinical uses of Furosemide?

A

Good when needing to move large volumes of fluid: HF, decomp cirrhosis, acute pulmonary edema
Hypercalcemia
Especially useful in severe renal impairment

Thiazide can be added if needed

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25
Q

What medications are loop diuretics?

A

Furosemide
Bumetanide
Torsemide

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26
Q

What is the MOA of K+ sparing diuretics?

A

Inhibit potassium secretion and influence sodium excretion (reduces potassium loss in the urine)

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27
Q

What is the site of action of K+ sparing diuretics?

A

Distal tubule

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28
Q

What are the side effects of K+ sparing diuretics?

A

Hyperkalemia, anuria (trimterene-rare)

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29
Q

What are the K+ sparing diuretics?

A

Amiloride
Spironolactone
Triameterne
Eplerenone

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30
Q

What are the clinical uses of Spironlactone as a diuretic?

A

HTN, edema in HF, ascities, cirrhosis, nephrotic syndrome, hyperaldosteronism, acne

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31
Q

Due to its anti-androgen effect what other conditions is spirnolactone prescribed?

A

Acne, chronically oily skin, hirsutism

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32
Q

What are the adverse effects of Spironolactone?

A

Gynecomastia

Increased risk for digitalis toxicity when co-administered

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33
Q

What are the contraindications of Spironolactone?

A

Pregnancy

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34
Q

What are the clinical uses of Eplernone?

A

Edema in HF, resistant HTN, hyperaldosteronism

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35
Q

What is the MOA of Amiloride?

A

Inhibit K+ loss by direct blockade of Na+/K+ exchange in the distal nephron

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36
Q

What are the clinical uses of Amiloride?

A

3rd-4th line to treat HTN, HF

Can be used to treat ascites as well as polyurea/polydisia due to lithium-induced nephrogenic diabetes insipidus

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37
Q

What is the only Carbonic Anhydrase Inhibitor?

A

Acetazolamide

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38
Q

What is the MOA of Acetazolamide?

A

Inhibits carbonic anhydrase in the proximal renal tubule, promoting renal excretion of Na+, K+, bicarbonate, and water

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39
Q

What are the clinical uses of Acetazolamide?

A

Cardiac anhydrase inhibitor
Chronic open-angle glaucoma
Prophylaxis of altitude sickness

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40
Q

What are the side effects of Acetazolamide?

A

Metabolic acidosis, renal stones, hyperammonemia in cirrhotic patients

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41
Q

What is the MOA of Osmotic Diuretic?

A

Promotes diuresis in kidneys by increasing the concentration of flitrates in the kidney and blocking reabsoprtion of water by kidney tubules

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42
Q

What is the site of action of osmotic diuretics (Mannitol)?

A

Glomerulus/proximal convoluted tubule

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43
Q

What are the clinical uses of Mannitol?

A

Maintains urine flow following acute toic ingestion of substances capable of producing acute renal failure

Reduction of intracranial pressure

Glaucoma

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44
Q

What are the side effects of Mannitol?

A

Headache, nausea, dizziness, polydipsia, confusion, chest pain

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45
Q

What are the neuromuscular effects of severe hypercalcemia?

A

Impaired concentration, confusion, fatigue, and muscle weakness

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46
Q

What are the GI effects of severe hypercalcemia?

A

Nausea, abdominal pain, anorexia, constipation, and rarely, peptic ulcer disease

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47
Q

What are the renal effects of hypercalcemia?

A

Polydipsia and polyuria resulting from nephrogenic diabetes insipidus, and nephrolithiasis resulting from hypercalciuria

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48
Q

What are the cardiovascular effects of hypercalcemia?

A

Hypertension, vascular calcification, shortened QT interval on electrocardiogram. Cardiac arrhythias are rare.

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49
Q

What is the treatment of hypercalcemic crisis?

A

Saline rehydration
Furosemide diuresis (low dose)

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50
Q

What diuretic class should NOT be used to treat hyercalcemia?

A

Thiazide diuretics, because they increase tubular calcium resorption

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51
Q

Describe the disease process of Nephrogenic Diabetes Insipidus?

A

Kidneys have partial or complete resistance to effects of antidiuretic hormone (vasopressin) - results in excretion of large amounts of diluted urine

52
Q

What are the symptoms of Nephrogenic Diabetes Insipidus?

A

Polyuria and polydipsia (risk of dehydration)

53
Q

What drugs can lead to Nephrogenic Diabetes Insipidus?

A

Lithium, Amphotericin B, Ofloxacin, Orlistat

Should stop medication

54
Q

What is the treatment of Nephrogenic Diabetes Insipidus?

A

Hydrochlorothiazide (inhibits amount of salt absorbed by kindeys and reduces water loss) - helps to correct the hypernatremia

Combination with Amiloride (helps maintain potassium level)

55
Q

What is the MOA of ACE Inhibitors?

A

Inhibits ACE, red levels of angiotensin II, suppress aldosterone excretion, decrease peripheral resistance and increase sodium and water excretion

Reduces both preload (promote natriuresis) and afterload (decrease vasoconstriction)

56
Q

What are the ACE Inhibitor drugs?

A

Enalapril
Captopril
Lisinopril

57
Q

What are ACE Inhibitors the first line treatment for?

A

Treatment of HTN with high risk of coronary disease, diabetes, stroke, heart failure, MI, or chronic kidney disease

Preferred in patients with diabetic nephropathy

58
Q

What are the side effects of ACE Inhibitors?

A

First dose hypotension, dizziness, proteinuria, rash, tachycardia, hyperkalemia, headache, cough, angioedema

59
Q

What is the PK of Enalapril?

A

Oral is prodrug, once ingested converted to enalaprilat

IV form is enalaprilat

60
Q

What are the severe side effects of Captopril?

A

Causes agranulocytosis or neutropenia (not commonly given)

61
Q

Per Francis, what is the best ACE Inhibitor that he would want on a deserted island to treat hypertension?

A

Lisinopril

62
Q

If someone has an angioedema reaction to an ACE Inhibitor can they be prescribed another ACE Inhibitor?

A

No

63
Q

What are the Angiotensin Receptor Blocker (ARB) agents?

A

Losartan
Valsartan
Candesartan
Olmesartan

64
Q

What is the MOA of ARB agents?

A

Blocks angiotensin II receptors in blood vessels, adrenals, and other tissues, dilation of arterioles and veins

65
Q

What is the primary clinical use of ARB’s?

A

HTN and HF

66
Q

What are the side effects of ARB’s?

A

Dry cough, hyperkalemia, skin rassh, hypotension, altered taste

67
Q

What is the only Renin Inhibitor agent?

A

Aliskiren

68
Q

what is the MOA of Aliskiren?

A

Binds tightly with renin and thereby inhibits the cleavage of angiotension into angiotensin I

Can influence the entire RAAS

69
Q

When is Aliskiren contraindicated?

A

Pregnancy

70
Q

Adrenergic blocking drugs have what effects on the heart?

A

Decrease blood pressure
Decrease heart rate and force of contraction

71
Q

What are the three sites of action of sympathoplegic drugs?

A

Blocks at 3 different levels

Peripherally
Centrally
Ganglionically

72
Q

What are the indications of alpha-blockers in hypertension?

A

Moderately hypertensive patients, pheochromocytoma, BPH, Raynaud’s disease, clonidine withdrawal

73
Q

What are the toxicities of alpha-blockers?

A

Fluid retention, headache, nasal stuffiness, dry mouth

74
Q

What are the indications of beta-blockers in hypertension?

A

Angina, hypertension, secondary prophylaxis in MI, arrhythmias

75
Q

What are the toxicities of beta-blockers?

A

Rebound hypertension with sudden withdrawal, bronchoconstriction, GI upset, fatigue, nightmares, decreased libido

76
Q

Alpha adrenergic receptor antagonists inhibit the effects of

A

Catecholamines (norepinephrine. epinephrine, dopamine)

77
Q

What is the MOA of Phenoxybenzamine?

A

Irreversible noncompetitive blocker of peripheral alpha 1 and alpha 2 adrenergic receptors

78
Q

What are the indications of Phenoxybenzamine?

A

Used in treatment of sweating and hypertension associated with pheochromoctoma

Only effective reflex tachycardia

79
Q

What is pheochromocytoma?

A

A rare, usually benign tumor on top of the adrenal glands (release too much norepi and epi)

80
Q

What is the primary indication of Phentolamine?

A

Pheochromocytoma

81
Q

What are the other indications for Phentolamine?

A

Dermal necrosis or hypertensive crisis after clonidine withdrawal

82
Q

What are the two Alpha-1 Selective Blockers?

A

Prazosin and Doxazosin

83
Q

What are the four Nonselective Beta Blockers?

A

Propranolol
Nadolol
Pindolol
Timolol

84
Q

What are the indications to use Propranolol?

A

Performance anxiety
Postural tremor
Migraine prevention
Thyrotoxicosis
Portal hypertension

85
Q

What are the CNS effects of Propranolol?

A

Depression
Dizziness
Lethargy/fatigue
Weakness
Hallucinations/Vivid dreams
Memory loss
Visual distrurbances

86
Q

Is Nadolol typically used in practice?

A

No

87
Q

What is the only use for Pindolol in the U.S.?

A

HTN, should be avoided in patients with prior MI or angina due to sympathomimetic effects

88
Q

What are the Beta-1 Selective Sympathetic Antagonists?

A

Metoprolol
Atenolol
Nebivolol

89
Q

What is a very common Beta-1 Selective Antagonist due to its many indications and less bronchial constriction than propranolol?

A

Metoprolol

90
Q

Why is Atenolol less effective than Metoprolol?

A

Less effective in preventing complications of HTN, though it has the same indications

91
Q

What mixed alpha and beta blocker is considered safe in pregnancy and used to manage hypertension in pre-eclampsia?

A

Labetalol

92
Q

When should calcium channel blockers be avoided?

A

Avoid in acute coronary syndrome, pre-existing conduction disorders, symptomatic hypotension

93
Q

Are Non-dihydropyridines cardio-selective or vascular selective?

A

Cardio-selective

94
Q

Are Dihydropyridines cardio-selective or vascular selective?

A

Vascular selective

95
Q

Verapamil mainly affects the

A

myocardium

96
Q

When is Verapamil not recommended?

A

Patients with sick sinus syndrome, AV nodal disease, or heart failure

97
Q

When is Diltiazem indicated?

A

Anti-arrhythmic effect, cam also lower BP

98
Q

According to Francis, what is the best and most common anti-hypertensive?

A

Amlodapine; has greater effect on smooth muscle in peripheral vasculature and has minimal effect on cardiac conduction

99
Q

When is Amlodapine not recommended?

A

Heart Failure

100
Q

What are the two venous vasodilators?

A

Isosorbide dinitrate
Nitroglycerin

101
Q

Of the venous vasodilators, which is the prodrug and converted to nitric oxide in the body?

A

Nitroglycerin

102
Q

Nitroglycerin is usually given sublingually but can be administered via what other routes?

A

IV/fluid
Ointment
Patch

103
Q

What are the indications for Isosorbide dinitrate?

A

Prophylaxis of acute angina
Esophageal spasm
HF in black patients with Hydralazine

104
Q

Hydralazine in combination with nitrates are effective in treating

A

heart failure

105
Q

What is the most characteristic side effect associated with Hydralazine?

A

Lupus-like syndrome (malar like rash)

106
Q

What arterial vasodilator causes salt and water retention?

A

Diazoxide

107
Q

What is the most significant side effect associated with Diazoxide?

A

Excessive hypotension (some cases can result in stroke and myocardial infarction)

NOT A FRIENDLY DRUG!

108
Q

What is the MOA of Minoxidil?

A

Hyperpolarization of cell membranes through opening of potassium channels, which allows for greater blood flow and oxygenation to hair follicles

109
Q

Due to acting both on venous and arterial vasculature, this drug is most commonly used in hypertensive emergencies due to drastically dropping blood pressure?

A

Nitroprusside

110
Q

What are the two centrally acting agents?

A

Clonidine
Methyldopa

111
Q

What is the MOA of Clonidine and Methyldopa?

A

Block sympathetic activity by binding to and activating centrally-located alpha 2 adrenoreceptors reducing sympathetic outflow

112
Q

When treating hypertension with either Clonidine or Methyldopa what do you need to be cautious of?

A

Rebound after withdrawal of medication

113
Q

What are the indications for Clonidine?

A

Treatment of HTN, menopausal flushing, opioid or ETOH withdrawal, Tourette’s syndrome, 2nd line agent for ADHD

114
Q

What is the primary indication for Methyldopa?

A

Hypertension during pregnancy

115
Q

What condition can Methyldopa treatment lead to?

A

Autoimmune hemolytic anemia if used for long duration

116
Q

What are the three initial therapy agents in treating hypertension?

A

Thiazide diuretics, ACEi, ARB’s

117
Q

What two anti-hypertension classes can’t be used together due to the high risk of kidney failure?

A

ACEi and ARB’s

118
Q

What drug classes should be used in a patient with hypertension and concomitant high angina pectoris risk?

A

B-blockers
Ca2+ channel blockers

119
Q

What drug classes should be used in a patient with hypertension and concomitant diabetes?

A

ACE inhibitors
ARB’s

Diuretics second line

120
Q

What drug classes should be used in a patient with hypertension and concomitant recurrent stroke?

A

ACE inhibitors

121
Q

What drug classes should be used in a patient with hypertension and concomitant heart failure?

A

All anti-hypertensives

122
Q

What drug classes should be used in a patient with hypertension and concomitant chronic renal disease?

A

ACE inhibitors and ARBs

123
Q

What is the disease process of Nephrogenic Diabetes Insipidus?

A

Kidneys have partial or complete resistance to effects of antidiuretic hormone (vasopressin), results in large amounts of diluted urine

124
Q

What are the symptoms of Nephrogenic Diabetes Insipidus?

A

Polyuria and Polydipsia

125
Q

What is the treatment for Nephrogenic Diabetes Insipidus and how does it help correct hyponatremia?

A

Hydrochlorothiazide, it inhibits amount of salt absorbed by kidneys and reduces water loss

Pharmacology II Exam II CSV Drugs (4 decks)

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