Pharmacology -Antihyperlipidemics and Diuretics Flashcards

1
Q

Class: Lovastatin and other “statins”

A

HMG-CoA reductase inhibitor

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2
Q

MOA: Lovastatin and other “statins”

A
HMG-CoA reductase inhibitor;
Lovers liver cholesterol;
Raises LDL receptor expression;
Lowers plasma LDL
Lowered VLDL synthesis results in lowered triglycerides
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3
Q

Side Effects: Lovastatin and other “statins”

A

Myalgia
Myopathy
Rhabdomylasis
Hepatotoxicity

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4
Q

What interactions do statins have with gemfibrozil?

A

Increased rhabdomyolysis

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5
Q

Class: Cholestryramine, Colestipol, Colesevelam

A

Bile acid sequestrants

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6
Q

Use: Cholestryramine, Colestipol, Colesevelam

A

To decrease LDL, slight increase in TG and HDL

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7
Q

MOA: Cholestryramine, Colestipol, Colesevelam

A

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

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8
Q

In what state are Cholestryramine, Colestipol, Colesevelam contraindicated?

A

Hypertriglyceridemia

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9
Q

Side effects: Cholestryramine, Colestipol, Colesevelam

A

Vitamin K deficiency (malabsorption in the gut)

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10
Q

Class: Mannitol

A

Osmotic diuretic

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11
Q

Effect of Mannitol

A

increases urine volume

inhibits water reabsorption throughout the tubule but MOST in the PCT

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12
Q

Uses: Mannitol

A

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

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13
Q

Side effect: Mannitol

A

Acute hypovolemia

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14
Q

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

A

Sodium and bicarbonate

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15
Q

Use: Dorzolamide

A

Glaucoma
AMS
Metabolic alkalosis

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16
Q

Class: Dorzolamide

A

CA inhibitor

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17
Q

Side effects: Acetazolamide, Dorzolamide

A
Bicarbonaturia
Acidosis
Hypokalemia
Hyperchloremia
Parasthesias
Renal stones
Sulfonamide hypersensitivity
18
Q

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

A

Loop diuretic

19
Q

Class: Ethacrynic acid

A

Loop diuretic

20
Q

Uses: Loop diuretics ie torsemide, furosemide, bumetanide

A
acute pulmonary edema;
acute renal failure;
anion overdose;
HF;
hypercalcemic states;
HTN;
refractory edemas
21
Q

What is a major secondary effect of loop diuretics?

A

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

22
Q

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

A

Ethacrynic acid

23
Q

What diuretics cause HYPOcalcemia? HYPERcalcemia?

A

Loop diuretics cause HYPOcalcemia

Thiazide diuretics cause HYPERcalcemia

24
Q

What is a unique side effect of loop diuretics?

A

Ototoxicity (esp ethacrynic acid)

25
Q

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

A
Thiazides
ie Chlorothiazide
Hydrochlorothiazide
Metolazone
Indapamide
26
Q

Nephrogenic diabetes insipidus is treated best by what kind of diuretic

A
Thiazides
ie Chlorothiazide
Hydrochlorothiazide
Metolazone
Indapamide
27
Q

What is the best drug for increasing HDL levels?

A

Niacin (Nicotinic acid)

Not first line therapy anymore (statins are)

28
Q

What are the effects of Niacin?

A

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

29
Q

Side Effects: Niacin (Nicotinic acid)

A

pruritis
dyspepsia
hepatotoxicity
hyperuricemia (contraindications in gout patients)

30
Q

MOA: Niacin

A

decreases VLDL secretion

31
Q

What hypolipidemic markedly reduces VLDL?

A

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

32
Q

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

A

Gallstone formation

Do not use with statins bc of rhabdomyolysis risk

33
Q

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

A

HMG-CoA –> Mevalonate

inhibited by HMG-CoA reductase inhibitors (statins)

34
Q

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

A

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

35
Q

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

A

Longer half lives than the older statins

36
Q

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

A

Statins
ie atorvastatin
rosuvastatin

37
Q

Class: Ezetimibe

A
no class
inhibits enterocyte absorption of cholesterol in the intestine
--> reduces the amount of cholesterol delivered to the liver in the first place
38
Q

Use: Ezetimibe

A

Best when used synergistically with statins

as monotherapy, reduces LDL by 18%

39
Q

Class: Alirocumab

A

PCSK9 inhibitor

40
Q

Class: Evolucumab

A

PCSK9 inhibitor

41
Q

MOA: Alirocumab

Evolucumab

A

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

42
Q

Indications: Alirocumab

Evolucumab

A

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