More drug's unique properties Flashcards
Neprilysin inhibitor / ARB
Combo drug
Sacubitril/valsartan Entresto
Neprilysin is an enzyme that contributes to the breakdown of the biologically active natriuretic peptides. By blocking the enzyme we increase our endogenous ANP, BNP, and CNP
alpha1, alpha 2 antagonist Not used for long term treatment
phentolamine
Hypos - calc, mag, K, H = met. alkalosis, ototoxicity (avoid aminogylcosides)
furosemide
Treat Severe pulmonary arterial HTN
bosentan
Endothelin (ET) receptor antagonist
ambrisentan
HF with renal dysfunction who cannot tolerate ACEI. HTN emergencies in pregnancy
hydralazine
Dilation of coronary arteries, systemic (peripheral) arterioles
Dihydropyridine - bind to inactivated L-type
nifedipine
amlodipine
Aldosterone/mineralocorticoid receptor antagonist - potassium sparing metabolized by liver
spironolactone
alpha1, alpha 2 antagonist Irreversible
phenoxybenzamine
Teratogenic, Hyperkalemia
ARBs
Decreases systemic vascular resistance AND Na absorption by the kidney (by blocking formation of ATII)
aliskiren tekturna
No effect on bradykinin - minimal incidence of cough and angioedema. K sparing diuretics contraindicated
ARBs
Natriuretic peptide 6 actions
promote vasodilation
relax smooth muscle
increased capillary endothelial permeability
promote natriuresis increased renal Na excretion
promote increase in GFR
suppress SNS outflow
ARB what channel?
What type of receptor is it?
AT1
GQ
diuretic that leads to
Hyperglycemia, hypokalemia, metabolic alkalosis
Hydrochlorothiaze
Low dose - D1 - vasodilation, decreased SVR (afterload), increases renal blood flow and ANP/BNP; intermediate dose - Beta1 - increased contractility and HR; high dose - alpha1 - vasoconstriction
dopamine
longer half life than prazosin
terazosin
doxazosin
Hyperkalemia, met. Acidosis. Blocks androgen receptors (impotence and gynecomastia)
spironolactone
Initial treatment of HTN
propranolol
metoprolol
atenolol
Pro-drug - metabolized to release NO in the body. Requires mitochondrial aldehyde dehydrogenase (ALDH2) (sometimes missing in Chinese population)
nitroglycerin, glyceryl trinitrate
isosorbide dinitrate
isosorbide 5-mononitrate
Ventricular arrhythmias, thrombocytopenia (low blood platelet count)
milrinone
Prolong NMB, headache, dizziness, Peripheral edema, negative chronotropy/inotropy, overdose pulmonary edema
CCB
Renin inhibitor
aliskiren Tekturna
eNOS inhibitor
methylene blue
Short term severely decompensated HF and severely failing circulation. Bridge to cardiac transplantation
milrinone
Reversible lupus erythematosus-like syndrome (primarily in slow acetylators)
hydralazine
MAO and dopamine B-hydroxylase (caution in patients with MAOIs)
dopamine
Reduces systemic vascular resistance (afterload), increases RENAL blood flow
fenoldopam corlopam D1 agonist
Treatment of BPH
terazosin Hytrin alpha1 antagonist
Greater effect in arterioles over veins. Anesthetic induced vasodilation may be exacerbated
prazosin
Minipress
dyspnea, chest pain, hemolysis
methylene blue
AV block, bradyarrthymia, bronchospasm. Avoid in diabetics - decreases glycogenolysis and gluconeogenesis
labetalol
Pulmonary edema-initial increase in plasma volume due to oncotic pressure - increases preload
mannitol
Venous dilation equal to arteriolar dilation (balanced vasodilator). Short term administration (cyanide released during metabolism - avoid infusion rates above 2 mcg/kg/min)
sodium nitroprusside
HoTN, renal failure, teratogenic
aliskiren Tekturna
First line agent in HTN diabetics
captopril
lisinopril
ARBs
contraindicated in patient bilateral artery stenosis?
captopril
lisinopril
patients dependent on angiotensin 2 to maintain GFR
COMT (caution in COMT Inhibitor patients - Parkinsons)
dobutamine
combo drug used for HF
Sacubitril/valsartan Entresto
May precipitate - kidney stones
triamterene
Low dose - Beta1 - positive inotrope, lusitrope, chronotrope, and dromotrope, also vasodilation in SKM; High dose - alpha1 - generalized peripheral vasoconstriction increasing afterload
epi
hepatic metabolism, vasopressin receptor agonist
Vasopressin
four drugs for HTN crisis
Labetalol-b1/b2-a1
fenoldopam-D1 receptor agonist
sodium nitroprusside-no donor
furosemide-loop diuretic
Beta1 - Positive inotrope, chronotrope, lusitrope. Beta2 - peripheral vasodilation and hypotension. No activity on alpha
isoproterenol
renal metabolism
Teratogenic, Hyperkalemia, dry cough, angioedema, first dose HoTN - acute renal failure. May precipitate profound refractory HoTN in presence of vasodilating anesthetics - use V1 agonists
captopril
lisinopril
Contraindicated with PVD and COPD/asthma
propranolol
Headache, flushing, peripheral edema, reflex tachycardia
minoxidil
metabolized by renal OAT
Hydrochlorothiazide
chlorothiazide
Renal metabolism
verapamil decreases ______clearance by blocking the P-glycoprotein energy dependent efflux transporter (renal secretion)
digoxin
More selective than spironolactone - less anti-androgenic side effects
eplerenone Inspra
good for treating intraoperative hypotension exacerbated in a patient taking ace inhibitors receiving anesthesia VIA
terlipressin
Arteriolar smooth muscle relaxation, increases renal blood flow - NOT coronary arteries or venous smooth muscle.
hydralazine
Positive inotrope (improves diastolic dysfunction), vasodilation. Blocks metabolism of cAMP (inotropic effects), cGMP (vasodilatory effects)
milrinone
Contradications - ACE, ARBs, renal insufficiency with hyperkalemia
Spironolactone
eplerenone
amiloride
triamterene
Low dose - Beta1 - positive inotrope, lusitrope, chronotrope, and dromotrope, also alpha1 - vasoconstriction with increased afterload. Little effect on Beta2
norepi
Inhibits pulmonary vasoconstriction and may cause V/Q mismatch, rebound hypertension, coronary steal, cyanide toxicity
sodium nitroprusside
Liddle’s syndrome (super ENaC Na channel)
amilrode midamor
triamtrene dyrenium
More effective with frequent channel openings - SA, AV, cardiac myocytes
Non-dihydropyridine -bind to open conformation L-type
diltiazem
verapamil
Decrease ATII and increase bradykinin levels. Vasodilatory effects - RENAL PROTECTIVE. Avoid K sparing diuretics, NSAIDs. Contraindicated in patients with bilateral renal artery stenosis - dependent on ATII to maintain GFR by constriction of efferent arteriole
captopril
lisinopril
V2 selective agonist. Relieves PDPH, DOC for central DI, treatment of bleeding disorders
desmopressin
No reflex tachycardia
labetalol
What happens when the AT1 receptor is activated?
7
- aldosterone secretion from adrenal cortex
- Na reabsorption from renal PCT
- Renal vasoconstriction-efferent arteriole
- direct vasoconstriction
- SNS discharge
- Release of catecholamines from adrenal medulla
- release of ADH (vasopressin) from pos pituitary
Low dose - Vasodilate VEINS and coronary arteries. High dose - decrease arteriolar resistance. Prefers epicardial coronary arteries and minimizes coronary steal
nitroglycerin, glyceryl trinitrate
isosorbide dinitrate
isosorbide 5-mononitrate
HTN emergencies and severe HF, Controlled hypotension during anesthesia to reduce bleeding
sodium nitroprusside
Prevent vasoplegic syndrome in CP bypass. Treatment for methemoglobinemia
methylene blue
To correct drug-induced kaliuresis and hypokalemia. Secondary HTN to hyperaldosteronism
Spironolactone
Inhibits Na/K ATPase on sarcoplasmic reticulum - less Na extracellular means less Na available for the Na/Ca exchanger = more Ca available to be stored and released intracellularly. Positive inotrope (from Ca), negative chronotropy, dromotropy
digoxin
HTN primarily, adjunct in HF; first line agent for African American patients
hydrochlorothiazide
HTN emergencies
labetalol
Opens ATP modulated K channels (inhibits influx of Ca through VGCC). Acts primarily on arterial smooth muscle cells - no effect on venous system
minoxidil