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90 Cards in this Set
- Front
- Back
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What are the side effects of the HMG CoA reductase inhibitors?
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Headache, rash, GI upset, myositis (rarely rhabdomyolysis), increased liver enzymes, teratogen
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What are the effects of the statin drugs?
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Increase in cellular LDL receptors
Increased LDL uptake Decreased circulating LDL Decreased VLDL synthesis Increased HDL |
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How does niacin work?
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Inhibits an enzyme needed for VLDL & TG synthesis
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What are the effects of niacin?
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Decreased VLDL & TG synthesis --> Increaed HDL
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What is the most potent increaser of HDL?
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Niacin
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What drug causes the side effect of cutaneous flushing and how can it be prevented?
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Niacin.
ASA can prevent it. |
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What are the side effects of niacin?
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Flushing
Increased uric acid Increased liver enzymes Increased insulin resistance |
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What are the bile acid binding resins?
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cholestyramine, colestipol, colesevelam
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How do the bile acid binding resins work?
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Highly charged cationic resins that irreversibly bind bile acids
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What are the side effects of the bile acid binding resins?
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Constipation
Gritty texture |
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How do the fibrates work?
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Bind to PPA receptor in cytosol--> migrates to nucleus--> binds to DNA response elements--> alters apolipoprotein synthesis
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What are the effects of the fibrates?
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Decreased VLDL
Increased lPL Increased HDL |
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What are the most effect TG lowering agents?
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Fibrates
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What are the fibrates?
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gemfibrozil
fenofibrate |
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What are the side effects of the fibrates?
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Nausea, diarrhea (GI effects)
Gallstones Some anticoagulant effect |
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How do the omega 3 fatty acids work?
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Decreased TG synthesis
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What are the side effects of the omega 3 fatty acids?
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fish tast
GI upset |
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What is ezetimibe?
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Blocks cholesterol receptors in intestine to prevent cholesterol absorption
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What are the side effects of ezetimibe?
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Flatulence
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What does sitostanol do?
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Decreased cholesterol uptake
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What drug works by decreasing pancreatic lipase?
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Orlistat
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What is a side effect of orlistat?
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Anal leakage
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What is vytorin?
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Statin + ezetimibe
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What is advicor?
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Niacin + statin
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What type of vessel to nitrates MOST affect?
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Veins
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What are the effects of nitrates?
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Venous relaxation--> increased venous capacitance, decreased ventricular preload, decreased CO, decreased heart size, decreased MVO2
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What is the important cause of the antianginal effects of nitrates?
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Decreased MVO2
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Intracoronary injection of nitrates is used for what?
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Variant angina (vasospasm)
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How are nitrates metabolized?
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In the LIVER by nitrate reductase
Nitroglycerin: metabolized to 2 dinitro derivatives (both w/significant activity) and 2 mononitro derivatives. Isosorbide dinitrate: metabolized to 5 mononitrate derivative (100% bioavailabity of derivative)-->significant 1st past effect |
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What drug needs breaks to prevent tolerance development?
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Nitrates (transdermal & infusion)
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What drug works by decreasing pancreatic lipase?
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Orlistat
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What is a side effect of orlistat?
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Anal leakage
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What is vytorin?
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Statin + ezetimibe
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What is advicor?
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Niacin + statin
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What type of vessel to nitrates MOST affect?
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Veins
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What are the effects of nitrates?
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Venous relaxation--> increased venous capacitance, decreased ventricular preload, decreased CO, decreased heart size, decreased MVO2
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What is the important cause of the antianginal effects of nitrates?
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Decreased MVO2
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Intracoronary injection of nitrates is used for what?
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Variant angina (vasospasm)
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How are nitrates metabolized?
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In the LIVER by nitrate reductase
Nitroglycerin: metabolized to 2 dinitro derivatives (both w/significant activity) and 2 mononitro derivatives. Isosorbide dinitrate: metabolized to 5 mononitrate derivative (100% bioavailabity of derivative)-->significant 1st past effect |
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What drug needs breaks to prevent tolerance development?
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Nitrates (transdermal & infusion)
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How are nitrates excreted?
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Mostly via kidney as glucuronide derivatives of dinitro metabolites
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How is nitroglycerin activated?
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Glutathione-S-transferase releases nitrite ion-->NO-->activates guanylyl cyclase-->increasedNO
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What causes nitrate tolerance and how can tolerance be overcome?
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Decreased tissue SH-->tolerance.
Can be overcome with acetylcysteine |
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What are the side effects of the ntirates?
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Throbbing headache & temporal artery pulsations, orthostatic hypotension & syncope
Indirect effects d/t compensatory mechanisms: tachycardiac & increased contractility, reflex vasoconstriction, retention of salt & water, |
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When are nitrates contraindicated?
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in cases of increased ICP
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When is intracoronary injection of nitrates indicated?
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Variant angina
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How do the beta blockers treat angina?
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Decreased MVO2 by:
Decreasing HR, BP, and contractility Decreased HR increases diastolic perfusion-->increased coronary perfusion |
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What drug is useful in silent ischemia?
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Beta blockers
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What are absolute contraindications to beta blockers?
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Severe bradycardia
High degree of AV block |
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What are the beta blocker selective for beta-1?
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Atenolol
Betaxolol Esmolol Metoprolol Bisoprolol Nebivolol Acebutolol |
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What are the nonselective beta blockers?
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Carvedilol
Labetalol Nadolol Propranolol Timolol |
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What is a second generation beta blocker?
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Bisoprolol
Selective Beta blocker |
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How long does it take for bisoprolol to reach peak concentration?
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2-4 hours
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What is the bioavailability of bisoprolol?
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80%
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How is bisoprolol eliminated?
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50/50 renal/non-renal
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What is the half-life of bisoprolol?
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8-12 hours
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What is a 3rd generation beta blocker?
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Nebivolol
Additional effect: vasodilation |
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What beta blocker is metabolized by CYP2D6?
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Nebivolol
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How long does it take for nebivolol to reach peak concentrations?
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1.5-6 hours
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What is the bioavailability of nebivolol?
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Depends on CYP2D6 polymorphisms.
Most ppl are extensive metabolizers=12% bioavailability Poor metabolizers have 96% bioavailability |
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How much of nebivolol binds to serum proteins?
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98%
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What is the addition effect of nebivolol?
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Stimulates release of NO from endothelial cells-> vasodilation
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What are the side effects of beta blockers and how can they be offset?
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S/E: increased EDV (d/t decreased HR), increased ejection time
Offset by nitrate use |
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What drug has no role in variant angina treatment?
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Beta blockers
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What drug can exacerbate angina upon abrupt discontinuation?
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Beta blockers
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What Ca channel blockers are more selective for heart muscle?
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Diltiazem & verapamil
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What Ca channel blockers are more selective for vascular smooth muscle?
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DHPs
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What DHP works on cerebral vasculature?
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Nimodipine
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How do the Ca channel blockers work?
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Block L-type Ca channels by binding to the channel inside the sarcolemma
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When do Ca channel blockers bind more effectively?
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When membrane is depolarized
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What are the effects of Ca channel blocker use on smooth muscle?
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Long-lasting smooth muscle relaxation
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What are the effects of Ca channel blocker use on the heart muscle?
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Decreased contractility
Decreased SA node rate Decreased AV node conduction velocity |
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What drug effects ARTERIOLES the most?
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DHPs (nifedipine)
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What are the beneficial effects of calcium channel blockers on vascular smooth muscle?
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Decreased BP
Decreased peripheral vascular resistance (esp. for exertional angina) Decreased coronary arterial tone (esp. for variant angina) |
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What Ca channel blocker affects women's HR more than men's HR?
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Diltaizem decreased BP more in women than in men (or is more likely to)
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What Ca channel blocker has more effect on the SA & AV nodes?
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Verapamil
Diltaizem too (at least more then DHPs) |
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What Ca channel blockers have the least depressant effect on the heart?
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DHPs
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What is the order of Ca channel blockers' effects on Na channel block?
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Verapamil>diltiazem>>DHPs
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Why might Ca channel blockers be useful especially post-MI?
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Decreased Ca influx may be good b/c ischemic cells have TOO much Ca
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Why is skeletal muscle not affected by Ca channel blockers?
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Skeletal muscle is not dependent on transmembrane Ca influx for contraction
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What might nimodipine be good for?
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Preventing cerebral vasospasm & infarct after subarachnoid hemorrhage
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What drug may reduce mortality after subarachnoid hemorrhage?
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Nimodipine
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What drug may be a useful chemotherapy adjuvant? Why?
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Verapamil can block P170 glycoprotein @ high dosages to increased effects of chemo
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What are the side effects of Ca channel blockers?
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D/t XS inhibition of Ca channels: cardiac depression & arrest, bradycardia, AV block, CHF
Flushing, dizziness, nausea, constipation |
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What drug can cause MI if released too quickly?
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Nifedipine
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What is a side effect of DHPs?
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Reflex tachycardia
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What antianginal drug can interact with digoxin & why?
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Verapamil b/c it can increase digoxin levels.
Use with caution. |
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What antianginal drug interacts with sildenafil & why?
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Nitrates b/c sildenafil blocks cGMP breakdown by phosphodiesterase-->sildenfil + nitrates = too much cGMP-->severe hypotension & MIs
Use sildenfil at least 6 hrs after nitrates |
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What drugs are used for variant angina?
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Nitrates
Ca channel blockers |
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What drugs are used in the treatment of unstable angina?
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Aspirin
Nitrates & beta blockers Ca channel blockers (refractory only) PCI |
