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2020 CPR II Cardio Exam 1 > Drugs for Lipid Disorders (Staudinger) > Flashcards

Drugs for Lipid Disorders (Staudinger) Flashcards

1
Q

Dietary measures the management of hyperlipoproteinemia are initiated first unless the pt has evidence of what?

A

Coronary or peripheral vascular disease

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2
Q

The HMG-CoA reductase inhibitors used in management of lipid disorders end in which suffix?

A

-statin

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3
Q

What are the most effective agents in reducing LDL levels and best tolerated class of lipid lower agents?

A

HMG-CoA reductase inhibitors (statins)

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4
Q

Which HMG-CoA reductase inhibitor (statin) is almost completely absorbed when taken orally?

A

Fluvastatin

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5
Q

Statin absorption is enhanced by what?

A

Food

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6
Q

Which 3 HMG-CoA reductase inhibitors (statins) have the longest plasma half-lives of 19, 14, and 12 hours?

A
  • Rosuvastatin (19 hrs)
  • Atorvastatin (14 hrs)
  • Pitavastatin (12 hrs)
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7
Q

Which HMG-CoA reductase inhibitor is not metabolized by CYP450’s?

A

Pravastatin

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8
Q

What is the MOA of HMG-CoA reductase inhibitors (statins)?

Leads to what changes and overall net effect?

A
  • Inhibit HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis
  • Depletes intracellular supply of cholesterol –> cell then ↑ the # of cell-surface LDL-receptors = ↑ internalization of circulating LDL
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9
Q

List the HMG-CoA reductase inhibitors in descending order of potency starting with the most potent.

i.e., simvastatin, rosuvastatin, atovastatin, pitavastatin, lovastatin, pravastatin and fluvastatin

A

Atorvastatin = Rosuvasatin > Simvastatin > Pitavastatin = Lovastatin = Pravastatin > Fluvastatin

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10
Q

List the 4 non-lipid therapeutic benefits of HMG-CoA reductase inhibitors (statins)?

A
  • Plaque stabilization
  • Improvement of coronary endothelial function
  • Inhibition of platelet thrombus formation
  • Anti-inflammatory effects
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11
Q

When does the majority of cholesterol synthesis occur, thus, is when statins are taken for therapeutic effects?

A

Nightime

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12
Q

Statins are effective at lowering plasma cholesterol levels in all types of hyperlipidemia and can be used alone, or in combo with what 3 other agents?

A
  • Resins
  • Niacin
  • Ezetimibe
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13
Q

What may be seen in pt’s with liver disease or a hx of alcohol abuse if they taken a statin?

A

Elevations of serum aminotransferase activity (up to 3x normal)

*Levels decrease upon suspension of drug therapy

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14
Q

What may be seen in the muscle of patients who take a statin, especially in those with high level of physical activity?

A

Creatine kinase activity levels may increase

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15
Q

Which AE associated with the muscle can occur rarely and lead to renal injury in those on statins?

A

Rhabdomyolysis (leading to myoglobinuria)

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16
Q

There is an increased incidence of what AE in pt’s concomitantly taking statins and fibrates?

A

Myopathy

*Can also occur with monotherapy

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17
Q

Statins increase the levels of which anti-coagulant?

A

Warfarin

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18
Q

Statins are contraindicated in which subset of patients?

A

Women who are pregnant, lactating, or likely to become pregnant

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19
Q

Use of statins is not recommended in pt’s with what 2 underlying diseases?

A
  • Liver disease
  • Skeletal muscle myopathy
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20
Q

Use of statins in children is restricted to those with what?

A

Homozygous familial hypercholesterolemia and some pt’s w/ heterzygous disease

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21
Q

Niacin (nicotinic acid, Vit B3) decreases levels of which 3 lipids and increases what?

A
  • Decreases = TG’s, LDL, and Lp(a)
  • Increases = HDL
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22
Q

Niacin is converted to nicotinamide and incorporated into NAD, which is well absorbed, and is mainly distributed to which 3 tissues?

A
  • Hepatic
  • Renal
  • Adipose tissue
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23
Q

What is the MOA of niacin in reducing levels of lipids?

Net effect on FFA’s, LDL, VLDL, and HDL?

A
  • Inhibits lipolysis of TG’s in adipose tissue = ↓ circulating FFA’s
  • Reduced hepatic synthesis of VLDL and LDL
  • Catabolic rate for HDL is ↓
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24
Q

What is the effect of niacin on levels of tPA and fibrinogen?

A
  • Fibrinogen levels are decreased
  • tPA levels are increased
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25
What can be taken before the administration of niacin to reduce the AE of nicain cutaneous flushing?
Aspirin or 1x daily ibuprogen
26
Niacin may cause toxicity of which organ as an AE? Levels of what should be monitored at baseline?
- **Hepatotoxicity** - Monitor **liver function** (aminotransferases)
27
Niacin should be avoided in pt's with what 2 underlying diseases?
- Hepatic disease - Active peptic ulcer
28
Why should niacin be used with caution in pt's with diabetes mellitus?
Due to **niacin-induced** insulin resistance --\> hyperglycemia
29
Which cutaneous AE's may be associated with the use of niacin?
- Pruritus - Acanthosis nigricans - Rashes - Dry skin or mucous membranes
30
How many times is niacin doses per day?
2-3x daily (half-life is ~60 mins)
31
Which enzyme inside of adipose tissues is inhibited by Niacin?
Hormone-sensitive lipase
32
What are the 2 Fibric acid derivatives (fibrates) used for lipid disorders?
- Fenofibrate - Gemfibrozil
33
Dietary changes suffice for lipid management can only be made after weight has stabilized for how long?
1 month
34
Dietary management of hyperlipoproteinemia includes limiting total calories from fat to what % of daily intake? Saturated fats \< what %? Cholesterol less than how many mg/day?
- Limit total calories from fat to **20-25%** - Saturated fats to **\<8%** - Cholesterol **\<200 mg/day**
35
Which fibric acid derivtive (fibrate) has the longest half-life (20 hours)?
Fenofibrate
36
Fibric acid derivatives (fibrates) act as agonists for which receptor? When activated what is the function of this receptor?
- Agonists for **nuclear receptor**, **PPARα** ---\> binds DNA - **↑ expression** of genes for **lipoprotein lipase, apo A-I, apo A-II** - **↓ expression** of **apo C-III**
37
What are the major effects of fibric acid derivatives (fibrates) on levels of lipids (TG's, LDL, VLDL, and HDL)?
- **Major** effect = ↑ **oxidation** of **FA's** in **liver** and **striated MUSCLE** - **↑ lipolysis of TG** via **lipoprotein lipase**, while intracellular lipolysis in adipose tissue is ↓ - **VLDL** and **LDL** levels ↓ and **TG's** ↓ ↓ ↓ - **HDL** levels ↑ moderately
38
Fibrates are useful in the management of which 3 lipid disorders?
- **Hypertriglyceridemias** where **VLDL predominates** - **Dysbetalipoproteinemia** - **Hypertriglyceridemia** resulting from tx w/ **viral protease inhibitors** (i.e., saquinavir, indinair, or nelfinavir for HIV therapy)
39
What are the common GI AE's of fibrates?
- Mild GI disturbances are **most common** AE's - ↑ risk of **cholelithiasis** (due to ↑ in cholesterol content of bile)
40
Due to the possible GI AE's (cholelithiasis) fibrates should be used with caution in which patients?
- Pt's w/ **biliary tract disease** - Those at high risk (i.e., **women**, **obese**, and **Native Americans**)
41
AE of fibrates in the liver?
Increased serum transaminases (up to 3x normal)
42
AE's of the muscle associated with Fibrates? Should evaluate pt for what?
- **Myositis** can occur (evaluate for muscle weakness and tenderness) - **Myopathy** and **rhabdomyolysis** (↑ risk when **fibrates** and **statins** combined)
43
Fibrates may potentiate the actions of what class of drugs?
Anti-coagulants (i.e., Warfarin)
44
Fibrates should be avoided in pt's with what underlying dysfunctions? Safe for pregnancy?
- Avoided in pt's with **hepatic** or **renal** dysfunction - Safety has **NOT** been established in **pregnant** or **lactating** women
45
What are the 3 bile acid sequestrants (resins) used for lipid disorders?
- **Coles**tipol - **Choles**tyramine - **Coles**evelam
46
Which class of drugs used for lipid disorders are insoluble in water; neither absorbed nor metabolically altered by the intestine; and totally excreted in the feces?
Bile acid sequestrants (resins)
47
What is the MOA of bile acid sequestrants (resins) used for lipid disorders?
- Bind to **negatively** charged **bile acids** and **↑ bile acid excretion** up to **ten-fold** - ↑ excretion of bile acids **enhances** converstion of **cholesterol** --\> **bile acids** in the **liver** via **7**α-**hydroxylation**
48
How does the decline in hepatic cholesterol caused by bile acid sequestrants (resins) lead to decreased levels of LDL?
Stimulates an ↑ **in hepatic LDL receptors** ---\> ↑ LDL clearance
49
Why is the combined use of a statin w/ a bile acid sequestrant (resin) useful?
- Bile acid resins cause an ↑ in the conversion of cholesterol to bile acids for excretion, which ↓ cholesterol levels - ↓ cholesterol leads to upregulation of HMG-CoA reductase, which enhances cholesterol synthesis, but **can be reduced with a statin**
50
What are 3 therapeutic uses for bile acid sequestrants (resins)?
1. Pt's w/ **primary hypercholesterolemia** (↓ LDL by 20%) 2. **Monotherapy** or in combo w/ **niacin** for tx of **Type IIa** and **IIb** **hyperlipidemias** 3. Relief of **pruritus** in pt's who have **bile salt accumulation** (i.e., biliary tract obstruction)
51
Most common AE's of bile acid sequestrants (resins)?
GI effects (i.e.m constipation, nausea, and flatulence)
52
High doses of bile acid sequestrants (resins) impair the absorption of what? Which drugs specifically?
- Absorption of **fat-soluble vitamins** (ADEK) - Numerous drugs, including **tetracycline, phenobarbital, digoxin, warfarin, pravastatin, fluvastatin, aspirin,** and **thiazide diuretics**
53
As a result of impaired absorption of other meds with bile acid sequestrants (resins) excpet for niacin, when should other drugs be dosed?
1 hour before or at least 2 hours after
54
Bile acid sequestrants (resins) should be avoided or used with caution in pt's with what 3 underlying diseases?
- Diverticulitis - Preexisting bowel disease - Cholestasis
55
What is the cholesterol absorption inhibitor used for lipid disorders?
Ezetimibe
56
What is the MOA of Ezetimibe?
- **Selectively** **inhibits** intestinal absorption of **cholesterol** and **phytosterols** (plant sterols) - Thru inhibition of **NPC1L1 transport protein** in **intestinal brush border**
57
Why is Ezetimibe effective even in the absence of dietary cholesterol?
Inhibits reabsorption of cholesterol excreted in bile
58
How much Ezetimibe is absorbed and what is the half-life?
- Highly water **insoluble**; majority excreted in feces - **22-hour** half-life
59
Which lipoproteins does Ezetimibe have an affect on?
- ↓ LDL (18%) and TG's (6%) - ↑ HDL (1.3%)
60
Ezetimibe can be used for primary hypercholesterolemia how?
- As a **monotherapy** - In **combo** with **HMG-CoA reductase inhibitors**
61
Ezetimibe can be used for homozygous familial hypercholesterolemia in combo with?
**Atorvastatin** or **Simvastatin**
62
Ezetimibe can be used in combo with what other drug to treat mixced hyperlipidemia?
Fenofibrate
63
Avoid administration of ezetimibe with what class of drug due to impaired ezetimibe absorption?
Bile acid sequestrants
64
Which class of drugs will lower LDL levels the greatest?
Statins
65
Which class of drugs causes the greatest increase in HDL?
Niacin
66
Which class of drugs causes the greatest decrease in TG's?
Fibrates
67
What is the MOA of lomitapide as a drug for homozygous familial hypercholesterolemia?
- Directly binds to and **inhibits** **MTP** in the lumen of ER. - **Prevents** assembly of **apo-B** containing lipoproteins in **entorocytes** and **hepatocytes** ---\> **↓ chylomicrons and VLDL** - **↓ plasma LDL-C** concentrations
68
Lomitapide is a substrate and inhibitor of what?
CYP3A4
69
AE's of Lomitapide?
- GI sx's - Elevated liver aminotransferase levels - Hepatic fat accumulation
70
What is the MOA of Mipomersen used for tx of homozygous familial hypercholesterolemia?
Antisense oligonucleotide that targets **apoB-100** **mRNA** and **disrupts its function**
71
AE's associated with Mipomersen?
- Injection site rxns (administered SQ 1x/week) - Flu-like sx's - HA - Elevation of liver enzymes \>3x the upper limit (discontinue if elevations persist or accompanied by clinical sx's, such as hepatic steatosis)
72
What are the 2 PCSK9 inhibitors used as lipid-lowering agents?
1. Alirocu**mab** 2. Evolocu**mab**
73
What is the MOA of the PCSK9 inhibitors (-mab's)?
- **Inhibits** the catabolism of LDL-receptor - ↑ amount of LDL removed from blood stream
74
What is the clinical indication for use of PCSK9 inhibitors?
Familial hypercholesterolemia **not** responsive to oral therapy
75
What are some of the AE's associated with the PCSK9 inhibitors?
- **Myalgia** - **Neuro effects:** delirium, dementia - **Nasopharyngitis**, flu-like sx's

2020 CPR II Cardio Exam 1 (31 decks)

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