Circulation Exam I Drugs

Acetazolamide

inhibits CA

causes metabolic acidosis (HCO3- excreted)

Uses: glaucoma, altitude, metabolic alkalosis

Loop diuretics (3)

furosemide, bumetanide, torsemide

loop diuretics MOA and uses

inhibit NKCC2 in TAL

powerful natriuresis

increased urinary Ca2+ and Mg2+

Uses: severe congestion (HF, pulmonary edema)

Thiazide drugs (4)

hydrochlorothiazide

chlorthalidone

indapamide

chlorothiazide (IV)

thiazide drugs MOA and uses

inhibit NCC in early DCT

decreased urinary Ca2+ (more reabsorbed) → NCX

Uses: chronic HTN

potassium-sparing diuretics (4)

spironolactone, eplerenone

amiloride, triamterene

MR antagonists drugs (2)

spironolactone, eplerenone

ENaC blocker drugs (2)

amiloride and triamterene

MR antagonist MOA and uses

decrease ENaC and Na+/K+-APTase gene expression

Na+ not coming in, K+ not going out

• potassium-sparing

Uses: oppose loop/thiazide K+ secretion

ENaC blocker MOA and uses

block apical Na+ entry

reduced K+ and H+ secretion (potassium-sparing)

Uses: oppose loop/thiazide K+ secretion

mannitol MOA and uses

IV drug, retains water in tubular lumen

Uses: elevated intracranial pressure, not for HTN

ADH agonist drugs (2)

vasopressin and desmopressin

ADH agonist MOA and uses

promotes APQ2 insertion to increase water reabsorption

Uses: water retention and hyponatremia

• Vasopressin can cause vasoconstriction and HTN

ADH antagonists drugs

tolvaptan and conivaptan

ADH antagonists MOA

V2 antagonists

block ADH binding to prevent APQ2 insertion

• hold onto water

alpha-2 agonist drugs (2)

clonidine and methyldopa

clonidine uses

resistant HTN → have to taper off

• rebound sympathetic activation and severe HTN)

methyldopa uses

HTN in pregnancy

hydralazine MOA and uses

vasodilator, causes lots of Na+ and water retention

direct arteriolar relaxation

Uses: difficult to control/resistant HTN

Minoxidil MOA and uses

vasodilator → prodrug → K+ channel opening

• makes Ca2+ channel less likely to open

very potent

Uses: resistant HTN, hair growth (hypertrichosis)

• watch out for pericardial effusion

• start furosemide (VOLUME RETENTION/PULMONARY EDEMA)

labetolol

IV alpha-1 and beta-blocker

lowers resistance without reflex tach

not cardioselective

esmolol

IV beta-1 selective blocker

used for immediate HR control (not BP)

ester, quickly metabolized

ACE inhibitor drugs (common ending)

-pril

• benazepril, enalapril, lisinopril, etc.

ACE inhibitor MOA

blocks conversion of angiotensin I → II

• lowers vasoconstriction and aldosterone-mediated Na+ retention

reduces bradykinin breakdown (vasodilation) → excess causes cough/angioedema

Angiotensin II Receptor Blocker (ARB) drugs (ending)

-sartan

• candesartan, irbesartan, losartan, etc.

ARBs MOA

block angiotensin II receptors

• reduces vasoconstriction, aldosterone release, sympathetic effects

does not inhibit bradykinin breakdown (less cough than ACE)

ARBs side effects

hyperkalemia (K+ not secreted), kidney effects, and fetal toxicity, angioedema

Aliskiren

directly inhibits renin

not commonly used in HTN

do not combine with ACE inhibitor or ARB

Aliskiren side effects

hyperkalemia, kidney dysfunction, angioedema, fetal toxicity

L-type Ca2+ channel blocker drugs

amlodipine, nifedipine, diltiazem, verapamil

L-Type Ca2+ channel blocker MOA

reduce Ca2+ entry (no contraction) → arteriolar dilation

Dihydropyridine CCB drugs

amlodipine, felodipine, nifedipine, nisoldipine

Dihydropyridine CCB MOA and side effects

arterial dilation with little direct AV-node suppression

ankle edema, flushing, HA, gingival hyperplasia

Nondihydropyridine CCB drugs

ER diltiazem, SR verapamil

Nondihydropyridine CCB MOA and side effects

slow HR and AV conduction → reduce contractility

constipation (verapamil)

Aprocitentan (Tryvio) MOA and uses

antagonist of endothelin receptors

• reduces vasoconstriction, lowering BP

used for tx of resistant HTN (last line)

beta blockers, cardioselective (3)

metoprolol, atenolol, esmolol

Nonselective beta blockers (2)

propranolol, nadolol

alpha 1 and beta blockers (2)

carvedilol, labetolol

NO-mediated beta blocker (1)

nebivolol

nitroprusside MOA and SE

IV drug

NO donor → arterial and venous dilation

light sensitive, hypotension

Nicardipine/clevidipine MOA and SE

IV drug

DHP CCB → reduce arterial resistance

reflex tach

Fenoldopam MOA and SE

IV drug

D1 agonist → arteriolar dilation

tach, increased intraocular pressure

thiazide-type drug (1)

hydrochlorothiazide

thiazide-like drugs (2)

chlorthalidone and indapamide

increased potency and longer half-life

Which beta blockers are cleared by the kidneys? (2)

atenolol and nadolol

nebivolol

beta-1antagonist

vasodilation via NO release

beta blocker drug interactions

CYP2D6

cimetidine

amiodarone

ritonavir

digoxin

SSRIs

St John’s wort

diltiazem/verapamil

alpha 1 antagonist drugs (2)

doxazosin, prazosin

alpha 1 antagonist MOA and uses

inhibit efferent sympathetic activity

avoids reflex tach

useful with BPH

central alpha 2 agonist drugs (3)

clonidine, methyldopa, guanfacine

central alpha 2 agonist MOA and SE

stimulate central alpha 2 autoreceptors → decrease NE, HR, CO, PVR

withdrawal syndrome→ TAPER

SE: sedation, depression, dry mouth

postganglionic sympathetic inhibitors

deplete NE from nerve terminals → decreased CO and PVR

Reserpine

Stage 1 HTN

(130-139)/(80-89)

Stage 2 HTN

(>140)/(>90)

4 first-line therapies

thiazides

ACE-i OR ARBs

CCB

class for CKD with proteinuria

ACE-i or ARB

class for DM with proteinuria

ACE-i or ARB

class for secondary stroke prevention

ACE-i or ARB

thiazide

AVOID with bronchospastic disease and depression

beta blockers

AVOID with dyslipidemia

beta blockers, diuretics

AVOID with DM

beta blockers, high dose diuretics

AVOID with gout

diuretics

beta blockers okay in HF? (3)

carvedilol, metoprolol suucinate, bisoprolol

CCB okay for HF

amlodipine, felodipine

2 first-line therapies for older adults?

thiazide and CCB

preferred agents in pregnancy (2)

labetalol and nifedipine SR

resistant HTN definition

BP > goal despite 3 BP meds

OR

BP at goal but requires >/= 4 meds

drugs to avoid in bilateral renal stenosis?

ACE/ARB

pre-eclampsia drugs

labetalol

hydralazine

nifedipine

angina/MI drugs

esmolol, nitroglycerin

aortic dissection drugs

esmolol, labetalol

acute pulmonary edema drugs

nitroprusside

nitroglycerin

clevidipine

pre-eclampsia drugs to avoid

ACEI, nitroprusside

acute pulmonary edema drugs to avoid

beta blockers