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Pharm2: Module 2 > Antihypertensives part 1 > Flashcards

Antihypertensives part 1 Flashcards

(118 cards)

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1
Q

what is arterial blood pressure directly proportional to

A

Cardiac output and peripheral vascular resistance

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2
Q

what controls cardiac output and peripheral vascular resistance

A

Baroreflexes and Renin-Angiotensin-Aldosterone System (RAAS)

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3
Q

What are the types of Hypertension

A

Primary/essential HTN
Malignant HTN
Resistant HTN
Pulmonary HTN
Pseudo-HTN
White Coat/Office HTN
Isolated Systolic HTN

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4
Q

What is the BP for Stage 2 hypertension

A

140 or higher OR / 90 or higher

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5
Q

what is the BP for Stage 3 hypertension

A

Higher than 180 AND / OR / higher than 120

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6
Q

what are the end-stage complications of uncontrolled HTN

A

Heart Disease
Heart Failure
Stroke
Chronic Kidney Disease

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7
Q

What are the antihypertensive drug categories

A

Diuretic agents
ACE inhibitors
ARBs
Calcium Channel Blockers
Beta-adrenergic Blockers
Alpha-adrenergic Blockers

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8
Q

What are the categories of Diuretics

A

Distal Tubule Diuretics (Thiazides)
Loop Diuretics
Potassium Sparing Diuretics
Carbonic Anhydrase inhibitors
Osmotic Diuretics

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9
Q

What are Thiazides/distal tubule diuretics

A

Hydrochlorothiazide
Chlorthalidone
Metolazone
Indapamide

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10
Q

What is the MOA for Thiazides

A

Blocks reabsorption of Na+ and Cl- in the early segment of the distal convoluted tubule -> increase water retention -> increase urine
*most commonly used

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11
Q

What is the site of action for thiazides

A

*Distal tubule, proximal tubule

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12
Q

What is Hydrochlorothiazide

A

Thiazide diuretic
prototypical drug
ideal starting agent for HTN, chronic edema or idiopathic hypercalciuria
Can also treat CaOx stones and Meniere’s disease

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13
Q

What is the pharmacokinetics of Hydrochlorothiazide

A

oral - onset 2 hours
absorbed rapidly and eliminated unchanged

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14
Q

What are the AE/SE of hydrochlorothiazide

A

Increased toxicity of digitalis or lithium

hypokalemia, hyperuricemia, hyperglycemia, hypotension, hyponatremia, hypercalcemia

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15
Q

When is hydrochlorothiazide contraindicated?

A

in Gout

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16
Q

What drug combinations can cause hypokalemia with hydrochlorothiazide

A

if given with corticosteroids or ACTH

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17
Q

What is the outcome of combining HCTZ with alcohol, barbituates or narcotics

A

orthostatic hypotension

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18
Q

What is Chlorthalidone

A

thiazide - like diuretic
used for HTN, HF, hypercalciuria, diabetes

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19
Q

What are the pharmacokinetics of chlorthalidone

A

oral or IV (IV is rare)
long half-life, low bioavailability
excreted in urine unchanged

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20
Q

What are the SE/AE of Chlorthalidone

A

hyponatremia
hypochloremia
hypotension
hypokalemia

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21
Q

What is Metolazone

A

Thiazide-like diuretic
usually added to a loop diuretic in the tx of edema in HF
10x more potent than HCTZ
*Safe in renal insuff

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22
Q

what are the pharmacokinetics of Metolazone

A

oral admin
excreted in the urine unchanged

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23
Q

What are the SE/AE of Metolazone

A

hyponatremia
hypochloremia
hypotension
hypokalemia

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24
Q

What is Indapamide

A

Thiazide-like diuretic
HTN and Decompensated HF
Not commonly used

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25
What is the pharmacokinetics of Indapamide
oral admin Hepatic Metabolism, excreted in urine and bile
26
What are the AE/SE of Indapamide
hyponatremia hypochloremia hypotension hypokalemia
27
What are the loop diuretics
Furosemide (Lasix) Bumetanide (Bumex) Torsemide (Demadex)
28
What is the MOA for loop diuretics
blocks reabsorption of sodium and chloride in the thick segment of the ascending loop of Henle - prevents passive reabsorption of water Inhibit chloride reabsorption
29
What is the site of action for loop diuretics
Loop of Henle
30
What are the primary side effects of loop diuretics
Hyponatremia dehydration hypotension hypokalemia hyperglycemia dose-dependent ototoxicity -Caution in pts w sulfa allergy
31
What are the drug interactions with Furosemide (lasix)
Digoxin K+ sparing diuretics Lithium Antihypertensive agents NSAIDs
32
What is Furosemide (lasix)
Loop-diuretic - Most common good when needing to move large volumes of fluid - HF, decompression cirrhosis, acute pulmonary edema Hypercalcemia especially useful in severe renal impairment *thiazide can be added if needed
33
What are the pharmacokinetics of Furosemide (Lasix)
Oral admin Diuresis begins 60 minutes after admin and lasts 8 hours hepatic metabolism - renal excretion
34
What inhibits the effects of furosemide
probenecid and indomethacin
35
what types of drugs have increased toxicity with furosemide
ototoxic and nephrotoxic drugs and lithium
36
What is Bumetanide
Loop-diuretic - most potent used for edema caused by heart failure, chronic renal disease and cirrhosis hypercalcemia
37
what is the pharmacokinetics of Bumetanide
Oral admin onset: 30-60 minutes Duration: 4-6 hours
38
what can large doses of Bumetanide cause
severe myalgias
39
What is not an AE/SE of Bumetanide
no Ototoxicity reported
40
What are the drug interactions with Bumetanide
Digoxin K+ sparing diuretics lithium antihypertensive agents NSAIDs
41
What is Torsemide
Loop diuretic used for Edema caused by HF, chronic renal disease and cirrhosis HTN Hypercalcemia
42
What are the pharmacokinetics of Torsemide
Oral admin onset: within 60 minutes Duration: 6-8 hours
43
What are SE/AE of Torsemide
Headache and dizziness Hyponatremia hypochloremia Dehydration Hypotension Hypokalemia Hypoglycemia dose-dependent ototoxicity
44
what are the drug interactions with Torsemide
Digoxin K+ sparing diuretics Lithium Antihypertensive agents NSAIDs
45
What are K+ Sparing diuretics
Amiloride (Midamore) Spironolactone(aldactone) Trimterene (Dyrenium) Eplerenone (Inspra)
46
what is the MOA for K+ sparing diuretics
blocks the action of aldosterone in the distal nephron -> retention of K+ and increase the excretion of Na+ Also blocks androgen receptors-> blocks androgen synthesis (inhibits potassium secretion and influence sodium excretion- reduced K+ loss in urine)
47
what is the site of action for K+ sparing diuretics
Distal Tubule
48
What are the primary side effects of K+ sparing diuretics
Hyperkalemia Anuria(trimterene-rare)
49
what is spironolactone
aldosterone antagonist, K+ sparing used for HTN, edema in HF, ascites, cirrhosis, nephrotic syndrome, hyperaldosteronism, ache most commonly used with a thiazide/loop diuretic to counteract K+ wasting effects
50
What is the pharmacokinetics of Spironolactone
Oral admin Effects are delayed, can take up to 48 hours
51
What are the AE/SE of spironolactone
hyperkalemia, Endocrine effects (gynecomastia)
52
What are the interaction with Spironolactone
with drugs that raise K+ levels, increase risk for digitalis toxicity
53
What are other conditions that can be treated with Spironolactone
anti-androgen effects can treat chronically oily skin, acne, hirsutism
54
Is spironolactone safe during pregnancy
NO
55
What is Eplerenone
aldosterone antagonist, K+ sparing used to treat edema in HF, resistant HTN and hyperaldosteronism
56
What are the pharmacokinetics for Eplerenone
Oral admin Metabolized by CYP
57
What are the AE/SE for Eplerenone
Hyperkalemia Less risk for gynecomastia than spironolactone
58
What is Amiloride
non-aldosterone antagonists, K+ sparing 3rd or 4th line to tx HTN/HF may correct metabolic alkalosis caused by other diuretics
59
What is the pharmacokinetics of Amiloride
oral admin more rapid onset than spironolactone
60
What are the SE/AE of amiloride
Hyperkalemia Nausea Vomitting leg cramps dizziness diabetics may develop glucose intolerance
61
What is Triamterene
non-aldoserone antagonists, K+ sparing HTN/Edema produces mild diuresis can be used alone or in combo (thiazide diuretic to treat HTN)
62
What are the pharmacokinetics of Triamterene
Oral admin initial resposne develops within hours
63
what are the SE/AE of triamterene
May turn urine blue causes crystalluria and cast formation and decreased renal blood flow - caution with renal disease Hyperkalemia, N/V, leg cramps, dizziness
64
what are Carbonic Anhydrase inibitors
Acetazolamide (diamox)
65
What is the MOA for Acetazolamide
inhibits carbonic anhydrase in the proximal rental tubule -> promoting renal excretion of Na+, K+, bicarboate and water
66
what is the site of action for Acetazolamide
Proximal tubule
67
What are the pharamacokinetics of Acetazolamide
oral or IV admin Eliminated renally
68
What are the AE/SE of Acetazolamide
metabolic acidosis renal stones hyperammonemia in cirrhotic pts conta in pts with sulfa allergy
69
What is contraindicated with the use of Acetazolamide
Sulfa allergy
70
What is Acetazolamide used for
cardiac anhydrase inhibitor chronic open-angle glaucoma and prophylaxis of altitude sickness
71
What are osmotic diuretics
Mannitol (resectisol)
72
What is Mannitol
osmotic diuretic maintains urine flow following acute toxic ingestion of substrates capable of producing acute renal failure reduction of intracranial pressure glaucoma treatment
73
What is the MOA for Mannitol
increase concentration of filtrates in the kidney and blocks reabsorption of water
74
what is the site of actio for Mannitol
glomerulus/proximal convoluted tubule
75
what is the pharmacokinetics of Mannitol
IV admin Onset: 30-60 minutes Duration: 6-8 hours
76
what are the SE/AE of Mannitol
HA Nausea Dizziness Polydipsia Dehydration Confusion Chest pain
77
Is mannitol safe in pregnancy
YES
78
What is hypercacemia
when there is too much calcium within the blood normal serum calcium levels is ~8-10.5mg/dL
79
What are symptoms of severe hypercalcemia that require treatment
Neuomuscular effects: impaired concerntation, confusion, fatigue and muscle weakness GI effects: nausea, abd pain, anorexia, constipation Renal effects: polydipsia and polyuria resulting from nephrogenic diabetes insipidus and nephrolithiasis resulting from hypercalcemia Cardiovascular effects: HTN, vascular calcification, shorted QT interval
80
What is the safest and most effective treatment of hypercalcemic crisis
saline rehydration furosemide (lasix) diuresis
81
What should NOT be used to treat hypercalcemia
Thriazide Diuretics they can exacerbate hypercalemia by increasing tubular calcium resoprtion
82
What is nephrogenic diabetes insipidus
body makes enough vasopressin but your kidneys don't respond to the hormone as they should. As a result, too much fluid gets flushed out in your urine. Causes include: some medicines, especially those used to treat bipolar disorder link
83
how is nephrogenic diabetes insipidus diagnosed
based on uring and blood tests
84
what are the symptoms of nephrogenic diabetes insipidus
polyuria and plolydipsia (risk of dehyrdration)
85
What is the treatment of nephrogenic diabetes insipidus
directed towards individuals symptoms ensure proper fluid intake and reduce urine output HCTZ (inhibits amount of salt absobed by kidneys and reduces water loss)
86
What are renin-angiotensin-aldosterone system (RAAS) agents
Common: ACE inhibitors (ACEi) Angiotensin receptor blocker (ARBs) Aldosterone antagonists Less common: Renin inhibitor Endothelin Anatgonist
87
What are ACE inhibitors
Enalapril Captopril Lisinopril
88
What is suppressed with ACE inhibitors
suppressed synthesis of angiotensin II suppressed aldosterone, resulting in natriuresis Decreased peripheral vascular resistance
89
What are ACE inhibitors the first line treatment of
HTN in pts with high coronary disease risk, diabetes, stroke, heart failure, myocardial infarction or chronic kidney disease preferred in pts with diabetic nephropathy b/c glucose levels are not affected and drugs are renoprotective
90
What is the MOA for ACE inhibitors
inhibits ACE -> reduces levels of angiotensin II -> suppresses aldosterone excretion -> decreases peripheral resistance AND increases sodium and water excretion
91
What is enalapril
RAAS - ACE inhibitor used for treatment of HTN with pts w/ increased CAD risk, DM, stroke, MI, HF, CKD preferred in pts with diabetic nephropathy
92
what are the pharmacokinetics of Enalapril (Prinivil)
oral (prodrug- undergoes hepatic metabolism), IV admin dose adjust in kidney disease
93
What are the AE/SE of ACE inhibitors
First dose hypotension, cough, hyperkalemia, renal failure, angioedema, neutropenia
94
What are the interactions and contraindications for ACE inhibitors
Contra in pregnancy Interactions w diuretics, antihypertensives, drugs that raise K+ levels, lithium, NSAIDs
95
What is Captopril (Capoten)
RAAS- ACE inhibitor Tx of HTN in pts w incr CAD risk, DM, stroke, MI, HF, CKD -Preferred in pts w diabetic nephropathy -Not common 1st line agent
96
What is a unlikely SE/AE of captopril
infrequently causes agranulocytosis or neutropenia
97
What are the pharmacokinetics of Captopril
oral admin, 2-3 times per day dose adjust in kidney disease DOES NOT undergo hepatic conversion to active metabolites
98
What is Lisinopril
RAAS- ACE inhibitor used to treat HTN and HF Preferred in pts w diabetic nephropathy, can cause some lowering of blood sugars
99
What are the pharmacokinetics of ACE inhibitors
oral admin - once daily dose adjust in kidney disease DOES NOT undergo hepatic conversion to active metabolites
100
What are Angiotensin Receptor Blockers (ARB)
Losartan Valsartan Candesartan Olmesartan
101
What is the MOA of ARB medications
Blocks angiotensin II receptors in blood vessels, adrenals and other tissues -> dilation of arterioles and veins
102
What is Losartan (Cozaar)
RAAS - ARB used to treat: HTN stroke prevention Diabetic nephropathy reduces serum uric acid levels
103
What are the pharmacokinetics of Losartan
oral, once daily dosing extensive first-pass hepatic metabolism (converstion to active metabolite)
104
Are ARB medications safe in pregnancy
NO
105
What are the AE/SE of ARB medications
Angioedema and renal failure Drug interactions: additive effect w antihypertensive drugs
106
What is Valsartain
1st IRB approved for HF HTN
107
What are the pharmacokinetics of Valsartan
oral admin, TWICE daily dosing
108
What is Candesartain
RAAS- ARB used to treat HTN and HF once daily dosing inactive metabolites
109
What is Olmesartan
RAAS-ARB used to treat HTN once daily dosing inactive metabolites significant mean blood pressure reduction
110
What are Renin Inhibitors
Aliskiren inhibits renin, acting early in the RAAS
111
what is the MOA for Aliskiren
binds tightly with renin and thereby inhibits the cleavage of angiotensinogen into angiotensin I can influence entire RAAS
112
What are the pharmacokinetics of Alikiren
oral admin - metabolized by CPY3A4 bioavailability low, doing wiht high fat meal makes it lower half-life 24 hours
113
what are the AE/SE of Aliskiren
diarrhea, cough, angioedema Contraindicated in pregnancy
114
What are Endothelin Antagonists
Ambrisentan Bosentan
115
What is the MOA for Ambrisentan
selectively blocks type A endothelin receptors
116
What is the MOA for Bosentan
Nonselectively blocks endothelin receptors
117
What are the uses for ambrisentan
treatment of pulmonary arterial hypertension (PAH) improve exercise ability, delay clinical worsening of PAH can be used in combo with tadalafil
118
What are the SE/AE of Ambrisentan
edema, nasal congestion, palpitations, abdominal pain, constipation

Pharm2: Module 2 (4 decks)

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