Cardio Pharmacology I Flashcards
B-blockers must be used with caution in what and are contraindicated in what?
decompensated heart failure
contraindicated in cardiogenic shock
what drugs are protective against diabetic nephropathy?
ACE inhibitors/ARBs
What drugs can be used for hypertension in pregnancy? (4)
Hydralazine, labetalol, methyldopa, nifedipine
Amlodipine and the other ‘dipines’ have what mechanism of action?
Block voltage-dependent L-type calcium channels of cardiac and smooth muscle -> decreasing muscle contractility
difference between dihydropyridines and non-dihydropyridines?
dihydropyridines act on vascular smooth muscle
non-dihydropyridines act on heart
name the non-dihydropyridines
diltiazem, verapamil
amlodipine = nifedipine > diltiazem > verapamil in regards to what function?
action on vascular smooth muscle
verapamil > diltiazem > amlodipine = nifedipine in regards to what function?
action on heart
which calcium channel blocker can be used for subarachnoid hemorrhage (prevents cerebral vasospasm)?
Nimodipine
which calcium channel blocker can be used for hypertensive urgency or emergency?
Clevidipine
Dihydropyridines can be use for what indications? (3)
hypertension, angina (including Prinzmetal), Raynaud phenomenon.
which dihydropyridine cannot be used for their normal indications?
Nimodipine
Non-dihydropyridines can be used for what indications? (3)
hypertension, angina, atrial fibrillation/flutter.
Adverse effects of cardiac depression, AV block, hyperprolactinemia, constipation are associated with what class of drugs?
Non-dihydropyridine CCB
Adverse effects of peripheral edema, ushing, dizziness, gingival hyperplasia are associated with what class of drugs?
Dihydropyridine CCB
Mechanism of Hydralazine?
increases cGMP -> smooth muscle relaxation. Vasodilates arterioles > veins; afterload reduction.
Why is hydralazine frequently co-administered with a B-blocker?
to prevent reflex tachycardia.
What are the indications for Hydralazine? (3)
Severe hypertension (particularly acute), HF. hypertension in pregnancy.
What do you coadminister hydralazine with for HF?
organic nitrates
What are the contraindications for Hydralazine and why? (2)
Angina and CAD
compensatory tachycardia
What cardiac drug is known to cause drug-induced Lupus like syndrome?
Hydralazine
clevidipine, fenoldopam, labetalol, nicardipine, nitroprusside can all be used in what scenario?
Hypertensive Emergency
Mechanism of Nitroprusside?
Short acting; cGMP via direct release of NO
Adverse effect of Nitroprusside?
Can cause cyanide toxicity (releases cyanide)
What cardiac drug used in hypertensive emergency is a D1 receptor agonist?
Fenoldopam
What cardiac drug is used postoperatively as an antihypertensive?
Fenoldopam
What is the effect of Fenoldopam on the body?
coronary, peripheral, renal, and splanchnic vasodilation.
decreases BP and increases natriuresis.
Mechanism of Nitrates?
Vasodilator by increasing NO in vascular smooth muscle -> increase in cGMP and smooth muscle relaxation.
Dilate veins»_space; arteries.
decreases preload.
What are the indications for Nitrates?
Angina, acute coronary syndrome, pulmonary edema.
What is Monday disease and it occurs with what drug class?
Nitrates
industrial exposure: development of tolerance for the vasodilating action during the work week and loss of tolerance over the weekend -> tachycardia, dizziness, headache upon reexposure.
What is the goal of anti-anginal therapy?
reduction of myocardial O2 consumption (MVO2)
What are the determinants of MVO2 targeted in anti-anginal therapy? (4)
end-diastolic volume, BP, HR, contractility
What B-blockers are contraindicated in angina?
Pindolol and acebutolol—partial β-agonists contraindicated in angina.
What drug Inhibits the late phase of sodium current thereby reducing diastolic wall tension and oxygen consumption?
Ranolazine
How does Ranolazine effect heart rate and contractility?
Does not affect heart rate or contractility
What drug do you use for angina refractory to all other medications?
Ranolazine
What drug has the side effects of constipation, dizziness, headache, nausea, QT prolongation?
Ranolazine
Mechanism of Statins?
Inhibit conversion of HMG- CoA to mevalonate, a cholesterol precursor
Statins decrease mortality in what patients?
CAD patients
Toxicity of Statins?
Hepatotoxicity/Hepatitis (increases LFTs), myopathy
when are statins more susceptible to causing myopathy?
especially when used with fibrates or niacin
What enzyme do statins inhibit?
HMG-CoA Reductase
How do statins change LDL, HDL, and TG levels?
decreases LDL a lot
increases HDL
decreases TG
Name the bile acid resins (3)
Cholestyramine, colestipol, colesnvelam
start with “Coles”
What drugs prevent intestinal reabsorption of bile acids making the liver use cholesterol to make more?
Cholestyramine, colestipol, colesnvelam
Bile acid resins
What drugs decrease the absorption of other drugs and decrease the absorption of fat-soluble vitamins?
Cholestyramine, colestipol, colesnvelam
Bile acid resins
How do bile acid resins change LDL, HDL, and TG levels?
decreases LDL a lot
slightly increases HDL
slightly increases TG
What drug prevents cholesterol absorption at small intestine brush border?
Ezetimibe
What adverse effects does Ezetimibe have?
Rare LFTs, diarrhea
How does Ezetimibe change LDL, HDL, and TG levels?
decreases LDL a lot
no change in HDL and TG
Name the Fibrates (3)
Gemfibrozil, bezafibrate, fenofibrate
“fibr” in the middle
What group of drugs upregulate LPL -> increases TG clearance?
Fibrates
What group of drugs activates PPAR-α to induce HDL synthesis?
Fibrates
What are the adverse effects of Fibrates?
Myopathy (risk with statins), cholesterol gallstones, hepatitis
How do Fibrates change LDL, HDL, and TG levels?
decrease LDL
increase HDL
decrease TG a lot
What vitamin is Niacin?
B3
Mechanism of Niacin (B3)? (2)
Inhibits lipolysis (hormone- sensitive lipase) in adipose tissue; reduces hepatic VLDL synthesis
What lipid lowering drug causes a red, flushed face?
Niacin
WHICH adverse effect OF WHAT lipid lowering drug is decreased by NSAIDs or long-term use?
red, flushed face adverse effect of Niacin (B3)
What lipid lowering agent causes hyperglycemia and hyperuricemia?
Niacin (B3)
How does Niacin change LDL, HDL, and TG levels?
decreases LDL a lot
increases HDL a lot
decreases TG
Digoxin directly inhibits what?
Na+/K+ ATPase
Digoxin indirectly inhibits what?
Na+/Ca++ exchanger
What is the net effect of digoxin’s inhibition of the transporters?
increased Ca++ concentration inside the myocyte -> positive inotropy (contractility)
How does Digoxin increase cardiac contractility?
detailed explanation
by inhibition of the gradient formed by the Na/K ATPase, Ca++ is no longer released from cell -> accumulation of Ca++. This causes the SR to have Ca++-dependent Ca++ release, which then increases Troponin C binding Ca++ -> increased cardiac contraction
Why does Digoxin cause a decrease in HR?
stimulates Vagus Nerve
indication for Digoxin use?
HF and atrial fibrillation
Explain why Digoxin works for its two indications
HF - increases contractility, helps the heart pump
Atrial Fib - decreases conduction at AV node and depresses SA node
what type of adverse reactions are seen with Digoxin?
cholinergic - due to vagus nerve stimulation
What odd side effect occurs with digoxin? (think Van Gogh)
blurry yellow vision
What electrolyte disorder can be caused by digoxin?
Can lead to hyperkalemia, which indicates poor prognosis.
Why does renal failure predispose someone to digoxin toxicity?
decreases excretion
Why does hypokalemia predispose someone to digoxin toxicity?
no competition for digoxin binding at K+-binding site on Na+/K+ ATPase
What drugs that displace digoxin from tissue-binding sites, and decreased clearance
verapamil, amiodarone, quinidine
What are the antidotes for digoxin toxicity? (4)
Slowly normalize K+, cardiac pacer, anti-digoxin Fab fragments, Mg2+
