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Pharm Exam 3 > HTN Drugs > Flashcards

HTN Drugs Flashcards

1
Q

What Class doe the following drugs belong?

Chlorthalidone
Hydrochlorothiazide (HCTZ)
Indapamide
Metolazone

A

Thiazide (Thiazide-like Diuretics) - weak diuretic

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2
Q

MOA of HCTZ and Chlorthalidone? and action site?

A

Na+ & Cl- are not reabsorbed = ↑ excretion.

Action site: Distal tubule

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3
Q

First line Thiazide for Uncomplicated HTN?

A

HCTZ

HCTZ is a better antihypertensive than it is a diuretic

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4
Q

Warnings for HCTZ?

A

Sulfa allergies [sulfonamide]

Dose in AM so pt does not pee all night . Check BMP after 2-3 wks

Drug interactions: Quinidine [Long QT]

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5
Q

Drug interactions for HCTZ?

A

Drug interactions: Quinidine [Long QT]

Decreases effects of: anticoags, uric acid agents, sulfonylureas, insulin

↑ effects of: anesthetics, digoxin, lithium, loop diuretics, Vit D

↓ by: NSAIDs, COX2s, BAS

↑ hypokalemia: Amphotericin B, corticosteroids

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6
Q

Indications for Chlorthalidone?

A

Similar to HCTZ, 10x greater potency at Na/Cl cotransporter!

Better for HTN than HCTZ?

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7
Q

ADRs for Chlorthalidone?

A

Same as HCTZ but more hypokalemia/electrolyte imbalance issues than HCTZ

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8
Q

1/2 life and elimination of Chlorthialidone?

A

Longer half life [47 hrs]

Eliminated: renal, bile, urine

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9
Q

What class do the following drugs belong?

Furosemide [Lasix]
Torsemide [Demadex]
Bumetanide [Bumex]

A

Loop Diuretics

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10
Q

Site of action for Loop Diuretics?

Furosemide, Torsemide, Bumetanide

A

Action site: Ascending Loop of Henle

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11
Q

1st line for diuretic for Acute pulmonary edema, CHF, Edema, Nephrotic syndrome, Cirrhosis, Chronic kidney dz, HTN, Severe hyperkalemia?

A

Furosemide [Lasix]

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12
Q

Contraindication for Furosemide [Lasix]?

A

Sulfa Allergy

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13
Q

Warnings for Furosemide?

A

Drug interactions: Aminoglycosides, some chemo drugs (ototoxicity)

↑ anticoagulant activity and dig arrhythmias
↑ lithium levels, 
NSAID, Sulfonylureas (hyperglycemia)
↓ diuretic response
Ampho B [nephrotoxicity]
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14
Q

ADRs for Furosemide (Lasix)?

A

Hypokalemia [Can precipitate arrhythmia], Hyponatremia, Hypomagnesemia, Hypocalcemia

Hyperuricemia, Hyperglycemia

Ototoxicity [Tinnitus, hearing loss, usually reversible], Sulfa allergy? ↑ LDL, TC, Tg. ↓ HDL.

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15
Q

MOA for Furosemide, Torsemide, Bumetanide?

Loop Diuretics

A

↑ urinary Na+ and Cl- excretion and Ca++ and Mg excretion

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16
Q

Is Bumetanide more or less potent than Furosemide?

A

Bumetanide is 40x more potent than furosemide

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17
Q

What Class do the following drugs belong?

Triamterene [Dyrenium]
Amiloride [Midamor]
Spironolactone [Aldactone]
Eplerenone [Inspra]

A

Potassium-Sparing Diuretics

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18
Q

MOA of Potassium-Sparing Diuretics?

Triamterene, Amiloride, Spironolactone, Epelerenone

A

Rarely used as monotherapy [combined w/ other diuretic to prevent K+ loss]

Na+ channel inhibitors

Loops & thiazides drive Na+ to collecting duct leading to ↑ K+ excretion

Amiloride and triamterene block Na+ channels, ↓ K+ excretion.

Little effect on Na+ excretion, may ↓ uric acid excretion

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19
Q

CI for Potassium-Sparing Diuretics?

A

Renal Failure

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20
Q

ADRs for Potassium-Sparing Diuretics?

Triamterene, Amiloride, Spironolactone, Epelerenone

A

Hyperkalemia→ can be lethal!

Triamterene: N/V, leg cramps, dizziness, photosensitivity, hyperglycemia, interstitial nephritis, nephrolithiasis

Amiloride: N/V/D, HA

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21
Q

What Class doe the following drugs belong?

Captopril (Capoten)
Enalapril (Vasotec)
Lisinopril (Zestril, Prinivil)
Benazepril (Lotensin)
Fosinopril (Monopril)
Trandolapril (Mavik)
Ramipril (Altace)
Quinapril (Accupril)
Perindopril (Aceon)
A

ACE Inhibitors —- RAAS drugs

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22
Q

How do ACEs work?

A

ACE enzyme: converts angiotensin I to angiotensin II

Angiotensin II→ Vasoconstrictor, stimulates synthesis/release of aldosterone [leads to Na+/K+ retention→ ↑ B/P, inactivates bradykinin breakdown

ACE converts bradykinin to an inactive peptide → more bradykinin → more NO → vasodilation! + cough :[

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23
Q

How do ACE inhibitors work?

A

ACE inhibitors→ Vasodilator ↓ B/P b/c it blocks ACE enzyme

Increased: vasodilation (arterial & venous)

Reduces: arterial & venous pressure, ventricular afterload & preload and blood volume [natriuretic, diuretic], morbidity & mortality post MI [improves ventricular function post MI]

↓ sympathetic activity, ↓ cardiac/vascular hypertrophy

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24
Q

What is the 1st line for HTN [not for general black population]
CKD
Reduce major CVD outcomes in pts w/ diabetes

A

ACE inhibitors (-opril)

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25
Q

What class do the following drugs belong to?

Losartan (Cozaar)
Valsartan (Diovan)
Candesartan (Atacand)
Eprosartan (Teveten)
Irbesartan (Avapro)
Olmesartan (Benicar)
Telmisartan (Micardis)
A

Angiotensin Receptor Blockers (ARBs)

-sartan

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26
Q

MOA of ARBs? (-sartan)

A

Blocks: type 1 angiotensin II receptors on blood vessels and the heart and stimulation of vascular smooth muscle contraction

Do not increase bradykinin [No cough, angioedema]

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27
Q

Contraindication for ACE inhibitors and ARBs?

A

PREGNANCY!

esp. ACE inhibitors (fetal/neonatal mortality!)

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28
Q

ADRs for Angiotension-Converting-Enzyme inhibitors?

A

Dry cough
hyperkalemia [renal insufficiency, w/ concomitant K+-sparing diuretics]
↓ renal fxn [renal stenosis, pre-existing renal disease]
first dose hypotension
ANGIOEDEMA

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29
Q

ADRs for ARBs?

A

Hyperkalemia

Rhabdomyolysis

30
Q

The following drug belongs to what class?

Aliskiren [Tekturna]

A

Direct Renin Inhibitors

31
Q

MOA of Aliskiren?

A

Direct inhibition of renin secretion [renin secretion is rate limiting step in RAAS]

*ACEI/ARBs = incomplete blockade of RAAS

32
Q

Indication for Direct Renin Inhibitors?

A

Not first line:

Take ACEI off if you use this in DM & renal insufficiency

33
Q

ADRs and Warnings for Direct Renin Inhibitors?

Aliskiren

A

Drug intxn: ↑ [] by cyclosporine, itraconazole

Angioedema, hyperkalemia, renal impairment.

34
Q

What class do the following drugs belong to?

Spironolactone (Aldactone)
Spironolactone/HCTZ (Aldactazide)
Eplerenone (Inspra)

A

Aldosterone Antagonists

35
Q

MOA of Spironolactone?

A

Aldosterone mineralocorticoid derived from cholesterol

Spironolactone competitive antagonist for androgen receptors (Mineralocorticoid receptor blocker)

  • Displaces testosterone from binding sites
  • Increases testosterone clearance
  • Increases estradiol production
36
Q

MOA for Eplerenone?

A

More selective for aldosterone receptors

37
Q

Indications for Eplerenone?

A

Post-MI CHF, HTN

Fewer anti-androgen side effects

38
Q

Indications for Spironolactone?

A

Edema due to HF, cirrhosis, nephrotic syndrome
HTN [compelling indication post-MI or HF]
primary hyperaldosteronism
severe HF
LV dysfunction [with ACEI/ARB, diuretic, beta blocker]

Off label: hyperandrogenism [Hirsutism, PCOS, congenital adrenal hyperplasia - CAH]

39
Q

ADRs for Spironolactone?

A 
Hyperkalemia
gynecomastia
mastodynia
erectile dysfunction
stevens-johnson
GI bleed
40
Q

ADRs for Eplerenone?

A

Hyperkalemia (CI in renal impairment)

41
Q

What class do the following drugs belong to?

Verapamil
Diltiazem

A

Calcium Channel Blockers

42
Q

MOA of Calcium Channel Blockers?

Verapamil
Diltiazem

A

Cardiac effects: Primary action: heart→ reduce Ca++ entry in the heart [Dihydropyridines have minimal effects on Ca++ entry in heart muscle]
Slow pacemaker activity - HR decreases, slows conduction b/n atria & ventricles. Lessens strength of contraction - decreased SV. Class IV antiarrhythmics

Vascular effects: lesser effect on arterioles and more depression of heart [no tachy!]

43
Q

Indications for Verapamil?

A

Angina, arrhythmia, HTN

Reduces afterload and myocardial contractility, improves LV diastolic fxn

44
Q

Contraindications for Verapamil?

Calcium Channel Blocker

A

Heart failure!

severe LV dysfunction, hypotension/shock, sick sinus syndrome [unless pt has pacer], 2nd or 3rd degree AV block, WPW, Lown-Ganong-Levine syndrome, pre-existing systolic HF, conduction defects or bradycardia, B-blockers

45
Q

Drug Interactions for Verapamil?

A

Drug intxn: EtOH, P450 - grapefruit juice, Digoxin, Lithium

P450!

46
Q

Indications for Diltiazem?

A

Angina - inc exercise tolerance due to increased O2 demand

Less potent vasodilator and inotrope than verapamil

IV: ↓ BP and PVR and HR
Oral: decreases HR, BP

47
Q

Contraindications for Diltiazem?

Calcium Channel Blocker

A

Similar to Verapamil…
Heart failure! -

severe LV dysfunction, hypotension/shock, sick sinus syndrome [unless pt has pacer], 2nd or 3rd degree AV block, WPW, Lown-Ganong-Levine syndrome, pre-existing systolic HF, conduction defects or bradycardia, B-blockers

48
Q

What out for liver problems with Diltiazem!

A

It is also a P450 substrate and inhibitor (like Verapamil)

Avoid grapefruit juice with CCB (Diltiazem/Verapamil)

49
Q

What Class do the following Drugs belong to?

Amlodipine [Norvasc]
Nifedipine [Procardia]
Clevidipine [Cleviprex]
Nimodipine [Nimotop]
Felodipine [plendil]
Nicardipine [Cardene]
A

Calcium Channel Blockers: Dihydropyridines

-ipine

50
Q

All of the Dihydropyrides that we learned about are P450 drugs!

A

Amlodipine (P450)
Nifedipine (P450)
Clevidipine (P450)

51
Q

Amlodipine MOA?

A

Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle.

52
Q

Nifedipine MOA?

A

The mechanism by which nifedipine reduces arterial blood pressure involves peripheral arterial vasodilatation and, consequently, a reduction in peripheral vascular resistance. … Nifedipine is a peripheral arterial vasodilator which acts directly on vascular smooth muscle.

53
Q

Clevidipine MOA?

A

Clevidipine is a dihydropyridine L-type calcium channel blocker. L-type calcium channels mediate the influx of calcium during depolarization in arterial smooth muscle.

Most selective for smooth muscle, primarily used for HTN due to reduction of PVR

54
Q

Pregnancy Category of Amlodipine and Nifedipine?

A

Category C

55
Q

ADRs for Amlodipine and Nifedipine?

A

Edema, dizziness, flushing, palpitation, fatigue, nausea, abdominal pain

56
Q

ADRs for Nifedipine, Clevidipine, Amlodipine?

Calcium Channel Blockers: Dihydropyridines

A

Flushing, HA, hypotension, reflex tachycardia

Edema: Direct arteriolar dilatation without venous dilation
I
ncreased hydrostatic pressure
Fluid shifts to gravity dependent compartments
More common in DHP CCBs due to potency of vasodilation. Worse at end of day. Improves with LE elevation

57
Q

The following drugs are first line for HTN in pregnancy. What class do they belong to?

Propranolol, Atenolol, Metoprolol, Carvedilol, Labetalol

A

Beta Blockers

58
Q

MOA of Beta Blockers?

A

Beta adrenergic receptor antagonists

59
Q

Indications for use of Beta Blockers?

-olol

A

MI
HF
HTN

60
Q

Contraindications for Beta Blockers?

A

Contraindicated in hypoperfusion (preshock) or heart failure [Sx: cold extremities, cyanosis, oliguria, decreased mentation

61
Q

Warnings with Beta Blockers?

A

Avoid ISA beta blockers, caution w/ asthma, taper doses up and down

Can lead to lifethreatening Bronchoconstriction in COPD patients.

Can delay recovery from hypoglycemia in T1DM and blunt hypoglycemic sx

62
Q

What Class do the following drugs belong to?

Clonidine
Methyldopa

A

ALPHA AGONISTS

Centrally acting sympatholytics

63
Q

What do Alpha Receptors do in the body?

A

Block sympathetic activity within the brain

Activate a2 receptors: Decrease heart rate and contractility

Reduced sympathetic output to the vasculature: decreases sympathetic vascular tone, vasodilation, reduced systemic vascular resistance [decreases arterial pressure

64
Q

MOA of Clonidine?

A

Partial agonist, low efficacy, high affinity. Exact MOA unknown

65
Q

MOA of Methyldopa?

A

A2 agonist

66
Q

Indication for Methyldopa???

A

HTN in pregnancy!

67
Q

Indication for Clonidine?

A

HTN

Decrease diarrhea in pts w/ diabetic neuropathy

Substance withdrawal [↓ cravings & sympathetic nervous activity]

Post menopausal hot flashes [patch]

ADHD

68
Q

ADRs for Clonidine?

Alpha Agonist

A

IV and patch: rebound Hypertension!

Dry mouth, sedation, erectile dysfunction, dizziness, constipation, bradycardia, less ADRs with patch
abrupt d/c: nervousness, HA, agitation, tremor, rebound HTN

69
Q

Drug interactions for Clonidine?

A 
Drug interactions: 
Digoxin
beta blockers
CCBs - bradycardia
EtOH
barbiturates - CNS depression
TCAs - hypotensive effect minimized
Antipsychotics - orthostasis
70
Q

ADRs and drug interactions of Methyldopa?

Alpha Agonist

A

Fatigue, sedation, HA, weakness [transient]
Hemolytic anemia
Liver failure
Edema - treat with diuretic

Drug interactions: lithium

Pharm Exam 3 (3 decks)

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