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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
What class do the following drugs belong to? ``` Losartan (Cozaar) Valsartan (Diovan) Candesartan (Atacand) Eprosartan (Teveten) Irbesartan (Avapro) Olmesartan (Benicar) Telmisartan (Micardis) ```
Angiotensin Receptor Blockers (ARBs) | -sartan
26
MOA of ARBs? (-sartan)
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]
27
Contraindication for ACE inhibitors and ARBs?
PREGNANCY! esp. ACE inhibitors (fetal/neonatal mortality!)
28
ADRs for Angiotension-Converting-Enzyme inhibitors?
Dry cough hyperkalemia [renal insufficiency, w/ concomitant K+-sparing diuretics] ↓ renal fxn [renal stenosis, pre-existing renal disease] first dose hypotension ANGIOEDEMA
29
ADRs for ARBs?
Hyperkalemia | Rhabdomyolysis
30
The following drug belongs to what class? Aliskiren [Tekturna]
Direct Renin Inhibitors
31
MOA of Aliskiren?
Direct inhibition of renin secretion [renin secretion is rate limiting step in RAAS] *ACEI/ARBs = incomplete blockade of RAAS
32
Indication for Direct Renin Inhibitors?
Not first line: Take ACEI off if you use this in DM & renal insufficiency
33
ADRs and Warnings for Direct Renin Inhibitors? | Aliskiren
Drug intxn: ↑ [] by cyclosporine, itraconazole Angioedema, hyperkalemia, renal impairment.
34
What class do the following drugs belong to? Spironolactone (Aldactone) Spironolactone/HCTZ (Aldactazide) Eplerenone (Inspra)
Aldosterone Antagonists
35
MOA of Spironolactone?
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
MOA for Eplerenone?
More selective for aldosterone receptors
37
Indications for Eplerenone?
Post-MI CHF, HTN Fewer anti-androgen side effects
38
Indications for Spironolactone?
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
ADRs for Spironolactone?
``` Hyperkalemia gynecomastia mastodynia erectile dysfunction stevens-johnson GI bleed ```
40
ADRs for Eplerenone?
Hyperkalemia (CI in renal impairment)
41
What class do the following drugs belong to? Verapamil Diltiazem
Calcium Channel Blockers
42
MOA of Calcium Channel Blockers? Verapamil Diltiazem
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
Indications for Verapamil?
Angina, arrhythmia, HTN | Reduces afterload and myocardial contractility, improves LV diastolic fxn
44
Contraindications for Verapamil? | Calcium Channel Blocker
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
Drug Interactions for Verapamil?
Drug intxn: EtOH, P450 - grapefruit juice, Digoxin, Lithium | P450!
46
Indications for Diltiazem?
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
Contraindications for Diltiazem? | Calcium Channel Blocker
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
What out for liver problems with Diltiazem!
It is also a P450 substrate and inhibitor (like Verapamil) Avoid grapefruit juice with CCB (Diltiazem/Verapamil)
49
What Class do the following Drugs belong to? ``` Amlodipine [Norvasc] Nifedipine [Procardia] Clevidipine [Cleviprex] Nimodipine [Nimotop] Felodipine [plendil] Nicardipine [Cardene] ```
Calcium Channel Blockers: Dihydropyridines | -ipine
50
All of the Dihydropyrides that we learned about are P450 drugs!
Amlodipine (P450) Nifedipine (P450) Clevidipine (P450)
51
Amlodipine MOA?
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
Nifedipine MOA?
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
Clevidipine MOA?
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
Pregnancy Category of Amlodipine and Nifedipine?
Category C
55
ADRs for Amlodipine and Nifedipine?
Edema, dizziness, flushing, palpitation, fatigue, nausea, abdominal pain
56
ADRs for Nifedipine, Clevidipine, Amlodipine? | Calcium Channel Blockers: Dihydropyridines
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
The following drugs are first line for HTN in pregnancy. What class do they belong to? Propranolol, Atenolol, Metoprolol, Carvedilol, Labetalol
Beta Blockers
58
MOA of Beta Blockers?
Beta adrenergic receptor antagonists
59
Indications for use of Beta Blockers? | -olol
MI HF HTN
60
Contraindications for Beta Blockers?
Contraindicated in hypoperfusion (preshock) or heart failure [Sx: cold extremities, cyanosis, oliguria, decreased mentation
61
Warnings with Beta Blockers?
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
What Class do the following drugs belong to? Clonidine Methyldopa
ALPHA AGONISTS Centrally acting sympatholytics
63
What do Alpha Receptors do in the body?
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
MOA of Clonidine?
Partial agonist, low efficacy, high affinity. Exact MOA unknown
65
MOA of Methyldopa?
A2 agonist
66
Indication for Methyldopa???
HTN in pregnancy!
67
Indication for Clonidine?
HTN Decrease diarrhea in pts w/ diabetic neuropathy Substance withdrawal [↓ cravings & sympathetic nervous activity] Post menopausal hot flashes [patch] ADHD
68
ADRs for Clonidine? | Alpha Agonist
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
Drug interactions for Clonidine?
``` Drug interactions: Digoxin beta blockers CCBs - bradycardia EtOH barbiturates - CNS depression TCAs - hypotensive effect minimized Antipsychotics - orthostasis ```
70
ADRs and drug interactions of Methyldopa? | Alpha Agonist
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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