Pharm Block 2 Basics 6

Front 1

What are the statins to know?

Back 1

Lovastatin and Simvastatin

Front 2

How do lovastatin and simvastatin produce their effects

Back 2

HMG CoA reductase inhibitors

Front 3

What metabolic path are statins metabolized by?

Back 3

CYP3A4 metabolism

Front 4

What are the HMG CoA reductase inhibitors?

Back 4

lovastatin and simvastatin

Front 5

When do you use lovastatin and simvastatin? What does it do

Back 5

1) 1st line of defense against hypercholesterolemia, at risk for mi
2) decreases TG , LDL (20-55%), increases HDL (5 -10%)
3) upregulates LDL receptors
4) stabilizes plaques

Front 6

What is the bile acid binding resin drug?

Back 6

Cholestyramine

Front 7

What is the mechanism of action of cholestyramine?

Back 7

Cholestyramine is a bile acid binding resin -> binds bile and prevents its reabsorption. Reduced bile amounts causes increased conversion of cholesterol to bile. LDL receptor number is increased as a compensatory reaction

Front 8

Which drug works via: binding bile and preventing its reabsorption, causing increased conversion of cholesterol to bile

Back 8

Cholestyramine

Front 9

What drug treats elevated cholesterol, esecially LDL concentrations that are elevated due to poor diet

Back 9

Cholestyramine

Front 10

What change in the lipid profile do you see when examining cholestyramine

Back 10

HDL increases 4-5%
LDL decreaess 12-25%
TGs increase (transiently if the person has normal TG; significant if they have high TGs)

Front 11

What is the contraindication for cholestyramine?

Back 11

People with high TGs should not take cholestyramine. Cholestyramine can raise TG levels

Front 12

Which drug should not be taken in people with high TGs?

Back 12

Cholestyramine

Front 13

What is the mechanism of action of niacin/nicotinic acid?

Back 13

Decreases VLDL/TG synthesis
Inhibits FFA mobilization
Inhibits uptake of HDL-apoA1 (increased plasma HDL)

Front 14

Which drug decreases VLDL/TG synthesis, inhibits FFA mobilization, and inhibits uptake of HDL-apoA1

Back 14

Nicotinic acid/niacin

Front 15

What drug is indicated for reducing TGs 35-50%, LDL 25%, and HDL up 15-30%

Back 15

Nicotinic acid

Front 16

What effects does nicotinic acid have on the lipid profile?

Back 16

TG reduced 35-50%
LDL reduced 25%
HDL increased 15-30%

Front 17

What drug in combination with statins can cause myopathy?

Back 17

Niacin

Front 18

What is niacin used to treat?

Back 18

Hypertriglyceridemia and elevated LDL

Front 19

How do fibric acids/gemfibrozil work?

Back 19

PPAR activators.

This decreases FA synthesis
Increases Beta oxidation
Increases HDL
Increases LDL size

Front 20

What drugs are PPAR activators, in turn decreasing FA synthesis, Increasing beta oxidation, increasing HDL, increasing LDL size

Back 20

Fibric acids
Gemfibrozil

Front 21

What is the clinical use of fibrates/gemfibrozil?

Back 21

High TGs (>750 mg/dl)
or treat
HIgh TG and Low LDL (metabolic syndrome/type 2 diabetes)

Front 22

What drug treats extremely high TG levels
or
high TG levels and low LDL (seen in metabolic syndrome /type 2 diabetes)

Back 22

Fibric acids/ gemfibrozil

Front 23

What is the lipid profile of someone who takes gemfibrozil/fibric acids

Back 23

TGS down 30-50%
LDL down15-20%
Increased HDL 5-15%

Front 24

Which drug causes
TGS down 30-50%
LDL down 15-20%
Increased HDL 5-15%

Back 24

Fibric acids/gemfibrozil

Front 25

How does ezetimibe work?

Back 25

Inhibits NPCl1 (niemann pick cl like 1 protein), which results in reduced uptake of cholesterol from lumen.

Front 26

Which drug inhibits NPCl1 (niemann pick cl like 1 protein) which results in decreased uptake of cholesterol from the lumen

Back 26

Ezetimibe

Front 27

What is ezetimibe combined with for therapy?

Back 27

Statins or fibrates

Front 28

What is the lipid profile of someone who takes ezetimibe

Back 28

TG down 5%
LDL down 15-20%
HDL up 1-2%

Front 29

If TG goes down 5%
LDL down 15-20%
HDL up 1-2%
which drug did they take

Back 29

Ezetimibe

Front 30

Who do you give ezetimibe to?

Back 30

Those who are resistant to statins

or
combine with statins to really reduce LDL 60%

Front 31

What drug is given to those who are resistant to statins or combined with statins to really reduce LDL 60%

Back 31

Ezetimibe

Front 32

What does heparin treat

Back 32

initial treatment of DVT
initial treatment of unstable angina/mi

Front 33

Which drug is used for initial treatment of DVT, initial treatment of mi/unstable angina

Back 33

Heparin

Front 34

What is the mechanism of action of heparin

Back 34

Heparin binds and potentiates antithrombin III, which inhibits coagulation factors ii, ixa, xa.

Front 35

Which drug binds and potentiates antithrombin III, inhibiting coagulation factors II, IXa, Xa?

Back 35

Heparin

Front 36

What does enoxaparin/dalteparin treat?

Back 36

Acute DVT
Acute Unstable angina MI
Hip replacement surgery

Front 37

Which drug could you give that treats acute DVT, acute Unstable MI, used in hip replacement surgery

Back 37

enoxaparin
dalteparin

Front 38

What is the mechanism of action of enoxaparin/dalteparin?

Back 38

Binds and potentiates antithrombin III just like heparin, but inhibits factor Xa much more.

Front 39

Which drug is low molecular weight heparin?

Back 39

Enoxaparin
Dalteparin

Front 40

Which drug binds and potentiates antithrombin III, but inhibits factor Xa much more

Back 40

Enoxaparin
Dalteparin

Front 41

What is protamine sulfate used for?

Back 41

To reverse heparin after cardiopulmonary bypass

Front 42

Which drug is used to reverse heparin after cardiopulmonary bypass?

Back 42

Protamine sulfate

Front 43

What is the mechanism of action of protamine sulfate?

Back 43

Binds heparin and forms inactive complex.

Protamine = positively charged.

Front 44

Which drug is positively charged and forms an inactive complex with heparin to inactivate it

Back 44

Protamine sulfate

Front 45

What is warfarin used to treat?

Back 45

Long term treatment of venous thromboembolism disease

Prophylaxis against thromboembolism in patients with a fib, dilated cardiomyopathy, and prosthetic heart valves

Front 46

Which drug is used to treat venous thromboembolism disease as well as prophylaxis in patients with a fib, dilated cardiomyopathy, or prosthetic valves against thromboembolism

Back 46

Warfarin

Front 47

What is the mechanism of warfarin?

Back 47

Vitamin k epoxide reductase inhibitor -> no activation of factors 2, 7, 9, 10

Front 48

Which drug is a vitamin k epoxide reductase inhibitor -> no activation of factors 2, 7, 9, 10

Back 48

Warfarin

Front 49

What is dabigatran used to treat?

Back 49

Thrombophylaxis in patients undergoing knee/hip surgery

Reduce risk of stroke and systemic embolism in ptnts with Afib

Front 50

What drug is used for thromboprophylaxis in patients who have undergone knee or hip replacement procedures

and for

prevention of stroke and systemic embolism in patients with afib?

Back 50

Rivaroxaban and Dabigatran

Front 51

What is the mechanism of action of dabigatran

Back 51

Binds and inhibits thrombin to prevent thrombin induced platelet aggregation.

Front 52

What drug binds and inhibits thrombin to prevent thrombin induced platelet aggregation

Back 52

Dabigatran

Front 53

What is the mechanism of action of rivaroxaban?

Back 53

Reversible binding with factor Xa

Front 54

What is rivaroxaban used to treat?

Back 54

Thrombophylaxis in patients who underwent hip/knee surgery

Reduce risk of stroke and systemic embolism in patients with a fib

Front 55

What is lepirudin used to treat?

Back 55

Lepirudin is used to treat heparin induced thrombocytopenia

Front 56

What drug treats heparin induced thrombocytopenia

Back 56

Lepirudin

Front 57

What is the mechanism of action of lepirudin?

Back 57

Lepirudin is a thrombin inhibitor

Front 58

Which drug is a thrombin inhibitor

Back 58

Dabigatran and lepirudin

Front 59

What is tissue plasminogen activator used for/atleplase?

Back 59

Acute MI, stroke, DVT

Front 60

What drug is used for acute mi, stroke, dvt?

Back 60

Tissue plasminogen activator/atleplase

Front 61

What is the mechanism for tissue plasminogen activator/atlepase?

Back 61

Activates fibrin bound plasminogen. Plasmin degrades fibrin clots

Front 62

Which drug activates fibrin bound plasminogen. Plasmin degrades fibrin clots.

Back 62

Tissue plasminogen activator/atleplase

Front 63

What is aminocaproic acid used for?

Back 63

Procoagulant - reduce hemorrhage in surgery. Reduce Urinary tract bleeding.

Front 64

Which drug is a procoagulant that reduces hemorrhage in surgery and reduces ut bleeding

Back 64

aminocaproic acid

Front 65

How does aminocaproic acid work

Back 65

competitive inhibitor of plasminogen-fibrin

Front 66

Which drug is a competitive inhibitor of plasminogen-fibrin

Back 66

Aminocaproic acid