Antianginals, Antihyperlipidemics

Front 1

Nitrates used as antianginals

Back 1

1. nitroglycerin (Minitran, Nitrostat)
2. isosorbide dinitrate (isordil)

Front 2

Calcium Channel blockers used as antianginals

Back 2

1. Nifedipine
2. Amlodipine
3. Verapamil
4. Diltiazem

Front 3

Beta blockers used as antianginals

Back 3

1. Propranolol
2. Nadolol
3. Timolol
4. Atenolol
5. Metoprolol

Front 4

A new class of drug used as an antianginal

Back 4

ranolazine (ranexa)

Front 5

3 major types of angina

Back 5

1. Atherosclerotic obstruction
2. Variant or Prinzmetal's angina
3. Unstable or Crescendo angina

Front 6

Atherosclerotic Obstruction

Back 6

large coronary arteries, produce classic angina pectoris, angina of effort or stable

Front 7

Variant or Prinzmetal's Angina

Back 7

reversible vasospastic reduction of flow mainly in large coronary arteries

Front 8

Unstable or Crescendo angina

Back 8

combines features of both other types of angina, result from sudden marked platelet aggregation. Can occur at rest as well as during exertion.

*may be an immediate precursor of myocardial infarction*

Front 9

Forms and duration of Nitroglycerin

Back 9

1. sublingual - minutes
2. transdermal - hours

Front 10

Can nitroglycerin can be taken orally? why or why not?

Back 10

No because it undergoes excessive 1st pass metabolism

Front 11

mechanism of action of nitrates

Back 11

1. become NO in the presence of smooth muscle cells and relaxes
2. peripheral vascular dilation results in reduced cardiac work thru reduced preload and afterload
3. reduces cardiac oxygen demand, not necessarily an increase in coronary flow

Front 12

uses for nitrates

Back 12

Sublingual tab - acute pain after it starts
Transderm patch - prevention of angina

Front 13

ADRs of nitrates

Back 13

orthostatic (postural) hypotension, throbbing headache, reflex increase in heart rate and contractility, Na and water retention, tolerance, fatal hypotension with PDE-5 inhibitors

Front 14

Mechanism of action for Calcium Channel blockers

Back 14

1. block calcium channels in cardiac muscle and arterial vascular smooth muscle leads to a reduction in afterload

Front 15

mechanism of action of verapamil and diltiazem

Back 15

reduce cardiac rate and contractility, reduce the cardiac oxygen demand

Front 16

mechanism of action of nifedipine and other dihydropyridines

Back 16

reduction in afterload, vasospasm in a coronary artery can be reversed

Front 17

Use of calcium channel blockers? use of dihydropyridines?

Back 17

1. preventative treatment in all forms of angina
2. treat acute anginal attack after its onset

Front 18

ADRs of verapamil and diltiazem

Back 18

1. congestive heart failure, atrioventricular block

Front 19

ADRs of dihydropyridines

Back 19

1. reflexly increase heart rate and contractility too much

Front 20

mechanism of action of Beta blockers for angina

Back 20

competitive antagonist of beta receptors

decrease heart rate, cardiac contractility, and BP ;
Most Important = inhibitory effects on heart rate and contractility which reduces cardiac oxygen demand

Front 21

uses of beta blockers in angina

Back 21

preventative treatment of angina, prevent exercise-induced angina, treating 'silent' ischemia

Front 22

ADRs of beta blockers in angina

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1. do not discontinue abruptly, can lead to rebound angina
2. high heart rate as a warning of severe hypoglycemic response may be masked
3. CNS = sedation, fatigue, sleep alterations

Front 23

2 proposed mechanism of actions for ranolazine (ranexa)

Back 23

1. shift source of fuel from fatty acid to glucose = demands less oxygen
2. selective inhibition of increased 'late' inward-directed sodium current caused by myocardial ischemia

Front 24

uses of ranolazine (Ranexa)

Back 24

often used in combo for symptoms of chronic stable angina

Front 25

ADRs of ranolazine (Ranexa)

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1. dizziness
2. headache
3. nausea
4. constipation

Front 26

Cholesterol Absorption Inhibitors

Back 26

Esetimibe (Zetia)

Front 27

Bile Acid Binding Agents

Back 27

1. Cholestyramine (Questran)
2. Colestipol (Colestid)
3. Colesevelam (Welchol)

Front 28

HMG-CoA Reductase Inhibitors

Back 28

1. Lovastatin (Mevacor)
2. Pravastatin (Pravachol)
3. Simvastatin (Zocor)
4. Atorvastatin (Lipitor)
5. Rosuvastatin (Crestor)

Front 29

Fibric Acid Analogues (Fibrates)

Back 29

1. Gemfibrozil (Lopid)
2. Fenofibrate (Tricor, Triglide)

Front 30

Other antihyperlipidemic drugs

Back 30

1. Niacin (Niacor, Niaspan)
2. Omega 3-Aci Ethyl Esters (Lovaza)

Front 31

Mechanism of Action of Esetimibe (Zetia)

Back 31

1. inhibits absorption of dietary and biliary cholesterol, inhibits a specific protein-mediated transport system
2. less cholesterol delivered by chylomicrons and enhances uptake of LDL from the circulation thereby decreasing plasma concentration
3. also may increase HDL

Front 32

Uses of Ezetimibe (Zetia)

Back 32

used alone or in combo to treat mostly high LDL

Front 33

ADRs and interactions for Ezetimibe (Zetia)

Back 33

ADRs: diarrhea and abdominal pain

INT: increase of liver enzymes when taken with statins

Front 34

Mechanism of Action for Bile Acid Binding Resins

Back 34

1. exchange chloride for bile acids
2. bile acid-resin complex cannot be reabsorbed = more cholesterol is converted to bile acid
3. increases hepatic LDL receptor numbers

Front 35

Uses of Bile Acid Binding Resins

Back 35

used along with diets and other drugs for treatment of mostly high LDL ; may aggravate other types by plasma conc. of VLDL

Front 36

ADRs of Bile Acid Binding Resins

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1. Do not cause systemic toxicity
2. Gi adverse reactions (bloating, nausea, constipation, etc)
3. bad taste

Front 37

Drug and Nutrient Interaction with Bile Acid Binding Resins

Back 37

1. thiazides, antibiotics, barbiturates, zetia, and certain statins
2. fat soluble vitamins and iron absorption

Front 38

Class of drugs for hyperlipidemia that undergo extensive 1st pass metabolism

Back 38

HMG - CoA Reductase Inhibitors

Front 39

Mechanism of Action for the "statins"

Back 39

1. an enzyme is inhibited which is the rate limiting step of hte biosynthesis of cholesterol
2. reduces overall systemic availability of cholesterol
3. Increases the number of LDL receptors and lowers plasma LDL conc
4. Also lowers VLDLs and IDLs and may increase HDL

Front 40

Uses of the "statins"

Back 40

1. used alone or as adjunct to diet and other drugs to lower LDLs
2. more effective than all other drugs at reducing LDL cholesterol

Front 41

ADRs to HMG - CoA Reductase Inhibitors (Statins)

Back 41

*usually well tolerated, ADRs are mild and transient
constipation, diarrhea, ab pain, headache, dizziness, rash, blurred, vision, nausea

Front 42

which antihyperlipidemic drug class can cause liver dysfunction and it is recommended to have liver function tests performed?

Back 42

STATINS

Front 43

which antihyperlipidemic drug class can cause myopathy because of an increased plasma creatine kinase level

Back 43

HMG - CoA Reductase Inhibitors (Statins)

Front 44

When are 'statins' contraindicated?

Back 44

in active liver disease and pregnancy

Front 45

mechanism of action of Niacin

Back 45

inhibits intracellular lipolysis in fat cells presumably by inhibiting the intracellular lipase activity of adipocytes = reduces plasma VLDL and increases HDL considerably

Front 46

uses for Niacin (Niacor, Niaspan)

Back 46

decreases plasma VLDL and LDL and extremely increases HDL

*can be the least expensive, available OTC*

Front 47

ADRs of Niacin

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1. flushing, itching, burning of the skin (most common)
2. hypotension, increased liver enzymes, mild hyperglycemia, glucose intolerance, GI disturbances, peptic ulcers, elevated plasma uric acid

Front 48

mechanism of action of Fibrates (Gemfibrozil and Fenofibrates)

Back 48

1. increased clearance of VLDL
2. increased enzymes for oxidation of FFAs in liver so less FFAs available for VLDL production

*increase hepatic LDL and decrease plasma LDL, decrease VLDL, increase HDL moderately

Front 49

uses of Fibrates

Back 49

primary hyperlipidemias with high VLDL AND also hypertriglyceridemia secondary to some defect in apolipoprotein E

Front 50

ADRs of Gemfibrozin and Fenofibrates

Back 50

1. gallstone formation (rare, serious)
2. GI upset and nausea (most common)
3. risk of myopathy if taken with statins

Front 51

Mechanism of Action of Omega 3 Fatty Acids (Lovaza)

Back 51

1. inhibit hepatic synthesis of TGs from endogenous FFAs
2. increase beta oxidation of eFFA
3. decreased delivery of eFFA to liver
4. decreased synthesis of eFFA
5. decreased activity of TG-synthesizing enzymes
6. may increase HDL slightly

Front 52

Uses of Omega 3 Fatty Acids (Lovaza)

Back 52

an adjunct to diet to reduce high plasma TG levels, decreases VLDL, in combo with statins to treat both LDL and VLDL

Front 53

ADRs of Omega 3 Fatty Acids (Lovaza)

Back 53

1. symptoms of the flu and/or infections
2. mild GI distress
3. taste perversion and "fishy" belching
4. inhibit platelet aggregation, cause bleeding