Pharmacology -Antihyperlipidemics and Diuretics

Question 1

Class: Lovastatin and other “statins”

Answer 1

HMG-CoA reductase inhibitor

Question 2

MOA: Lovastatin and other “statins”

Answer 2

HMG-CoA reductase inhibitor;
Lovers liver cholesterol;
Raises LDL receptor expression;
Lowers plasma LDL
Lowered VLDL synthesis results in lowered triglycerides

Question 3

Side Effects: Lovastatin and other “statins”

Answer 3

Myalgia
Myopathy
Rhabdomylasis
Hepatotoxicity

Question 4

What interactions do statins have with gemfibrozil?

Answer 4

Increased rhabdomyolysis

Question 5

Class: Cholestryramine, Colestipol, Colesevelam

Answer 5

Bile acid sequestrants

Question 6

Use: Cholestryramine, Colestipol, Colesevelam

Answer 6

To decrease LDL, slight increase in TG and HDL

Question 7

MOA: Cholestryramine, Colestipol, Colesevelam

Answer 7

Complexation of bile salts in the gut decreasing LDL in the blood

Question 8

In what state are Cholestryramine, Colestipol, Colesevelam contraindicated?

Answer 8

Hypertriglyceridemia

Question 9

Side effects: Cholestryramine, Colestipol, Colesevelam

Answer 9

Vitamin K deficiency (malabsorption in the gut)

Question 10

Class: Mannitol

Answer 10

Osmotic diuretic

Question 11

Effect of Mannitol

Answer 11

increases urine volume

inhibits water reabsorption throughout the tubule but MOST in the PCT

Question 12

Uses: Mannitol

Answer 12

Decrease IOP in glaucoma;
Decrease intracerebral pressure
Reopen kidney fx in oliguric state (ie rhabdomyolysis from a statin)

Question 13

Side effect: Mannitol

Answer 13

Acute hypovolemia

Question 14

Acetazolamide increases which two solutes in the lumen of the PCT?

Answer 14

Sodium and bicarbonate

Question 15

Use: Dorzolamide

Answer 15

Glaucoma
AMS
Metabolic alkalosis

Question 16

Class: Dorzolamide

Answer 16

CA inhibitor

Question 17

Side effects: Acetazolamide, Dorzolamide

Answer 17

Bicarbonaturia
Acidosis
Hypokalemia
Hyperchloremia
Parasthesias
Renal stones
Sulfonamide hypersensitivity

Question 18

The Na/K/2Cl symporter is acted on by what kind of diuretic?

Answer 18

Loop diuretic

Question 19

Class: Ethacrynic acid

Answer 19

Loop diuretic

Question 20

Uses: Loop diuretics ie torsemide, furosemide, bumetanide

Answer 20

acute pulmonary edema;
acute renal failure;
anion overdose;
HF;
hypercalcemic states;
HTN;
refractory edemas

Question 21

What is a major secondary effect of loop diuretics?

Answer 21

They vasodilate by increasing prostaglandins –> further diuresis and lower TPR

Question 22

What is the only diuretic option for a patient allergic to sulfa drugs?

Answer 22

Ethacrynic acid

Question 23

What diuretics cause HYPOcalcemia? HYPERcalcemia?

Answer 23

Loop diuretics cause HYPOcalcemia

Thiazide diuretics cause HYPERcalcemia

Question 24

What is a unique side effect of loop diuretics?

Answer 24

Ototoxicity (esp ethacrynic acid)

Question 25

The Na/Cl symporter in the distal tubule is the site of action of what kinds of diuretics?

Answer 25

``` Thiazides ie Chlorothiazide Hydrochlorothiazide Metolazone Indapamide ```

Question 26

Nephrogenic diabetes insipidus is treated best by what kind of diuretic

Answer 26

``` Thiazides ie Chlorothiazide Hydrochlorothiazide Metolazone Indapamide ```

Question 27

What is the best drug for increasing HDL levels?

Answer 27

Niacin (Nicotinic acid) | Not first line therapy anymore (statins are)

Question 28

What are the effects of Niacin?

Answer 28

HDL up 30% LDL down 25% TG down 40%

Question 29

Side Effects: Niacin (Nicotinic acid)

Answer 29

pruritis dyspepsia hepatotoxicity hyperuricemia (contraindications in gout patients)

Question 30

MOA: Niacin

Answer 30

decreases VLDL secretion

Question 31

What hypolipidemic markedly reduces VLDL?

Answer 31

Fibric acid derivatives (fibrates) ie Clofibrate (no longer used) Gemfibrozil Fenofibrate

Question 32

What is a major side effect of fibric acid derivaties such as gemfibrozil and fenofibrate?

Answer 32

Gallstone formation Do not use with statins bc of rhabdomyolysis risk

Question 33

What is the rate-limiting step in the synthesis of cholesterol?

Answer 33

HMG-CoA --> Mevalonate | inhibited by HMG-CoA reductase inhibitors (statins)

Question 34

What are the effects on HDL, LDL, VLDL by statins?

Answer 34

HDL up 10% VLDL down 25% LDL down 50%

Question 35

Why use the newer statins such as atorvastatin and rosuvastatin??

Answer 35

Longer half lives than the older statins

Question 36

What is the first-line therapy for patients with elevated LDL levels?

Answer 36

Statins ie atorvastatin rosuvastatin

Question 37

Class: Ezetimibe

Answer 37

``` no class inhibits enterocyte absorption of cholesterol in the intestine --> reduces the amount of cholesterol delivered to the liver in the first place ```

Question 38

Use: Ezetimibe

Answer 38

Best when used synergistically with statins | as monotherapy, reduces LDL by 18%

Question 39

Class: Alirocumab

Answer 39

PCSK9 inhibitor

Question 40

Class: Evolucumab

Answer 40

PCSK9 inhibitor

Question 41

MOA: Alirocumab | Evolucumab

Answer 41

PCSK9 is an endopeptidase that targets LDL receptors for degradation and is inhibited by these mABs. Therefore more LDL is removed from circulation.

Question 42

Indications: Alirocumab | Evolucumab

Answer 42

For patients with refractory hypercholesterolemia, or on maximal doses of statins that still need LDL reduction