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Flashcards in HLD drugs Deck (77)
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1

High triglycerides can eventually result in what condition?

What is the recognized threshold (serum mg/dL)?

Pancreatitis

> 500 mg/dL

2

List the presently accepted values for desirable, borderline and high serum LDL-cholesterol.

  • Desireable: < 100 mg/dL
  • Borderline: 100-159 mg/dL
  • High: >190 mg/dL

3

List the presently accepted values for desirable serum HDL-cholesterol. (men vs. women).

  • Men: > 40 mg/dL
  • Women: > 50 mg/dL

4

List the presently accepted values for desirable, borderline, and high triglyceride levels. (Also, what is considered very high?)

  • Desirable: < 150 mg/dL
  • Borderline: 150-199 mg/dL
  • High: > 200 mg/dL (> 500 very high)

5

NCEP lipoprotein treatment goals: VERY HIGH RISK:

  • CV risk factors?
  • LDL goal?

 

  • Current CHD + other factors
  • < 70 mg/dL

6

NCEP lipoprotein treatment goals: HIGH RISK:

  • CV risk factors?
  • LDL goal?

  • Previous CHD, diabetes, > 2 risk factors
  • < 100 mg/dL (optional < 70)

7

NCEP lipoprotein treatment goals: MODERATELY HIGH RISK:

  • CV risk factors?
  • LDL goal?

  • > 2 risk factors. 10-20% ten-year risk
  • < 130 mg/dL (optional < 100 mg/dL)

8

NCEP lipoprotein treatment goals: MODERATE RISK:

  • CV risk factors?
  • LDL goal?

  • > 2 risk factors, < 10% ten-year risk
  • < 130 mg/dL

9

NCEP lipoprotein treatment goals: LOWER RISK:

  • CV risk factors?
  • LDL goal?

  • 0-1 risk factors
  • < 160 mg/dL

10

What's the DOC for treating pts w/elevated LDL-C?

Statins

11

Name the 6 different statins.

  1. Lovastatin
  2. Simavastatin
  3. Atorvastatin
  4. Fluvastatin
  5. Rosuvastatin
  6. Pravastatin

12

Statins: MoA?

Inhibits HMG-CoA reductase & triggers SREBP ts factor --> increased LDL-R expression and increased LDL clearance

13

Statins: indications?

High LDLs

14

Statins: toxic/adverse effects?

A. Myalgia/myopathy.

B. ***Rhabdomyolysis***

C. hepatitis.

D. Small risk T2DM.

15

What are some lab and physical signs that a pt has rhabdomyolysis?

  • Fever, malaise, diffuse myalgia and/or tenderness,
  • Marked elevation of serum [CK]
  • Myoglobin present in the urine (dark)

16

When are statins contraindicated?

Severe liver disease, pregnancy (teratogenic)

17

Which statins are metabolized by CYP3A4?

Which statins do not undergo CYP450 metabolism?

Which statins are glucuronidated in the liver?

ASL: atorvastatin, simvastatin, lovastatin

Pravastatin only

All statins

18

CYP3A4 inhibitors ___________ levels of Lovastatin, Simvastatin & Atorvastatin (ASL).

CYP3A4 inhibitors associated with increased risk of what disease?

Increase

Rhabdomyolysis

19

Describe the effect of statins on serum lipids.

v LDL (20-60%)

v TG (10-20%)

^ HDL (5-10%)

20

Give some eg's of CYP3A4 inhibitors.

Eric's red grape kept its clear fluid

  •   Immunosuppressants: cyclosporin &  tacrolimus
  •   Macrolide antibiotics: clarithromycin & erythromycin
  •   Ca2+-channel blockers: diltiazem & verapamil
  •   Anti-arrhythmia drugs: amiodarone
  •   Azole anti-fungals: itraconazole & ketoconazole
  •   HIV protease inhibitors: ritonavir, indinavir & nelfinavir
  •   Anti-coagulants: warfarin

21

Name some eg's of CYP3A4 inducers.

Phen-phen rifled St. John's glowing pink cars.

Phenytoin, Phenobarbitol, Rifampin, St. John's wort, Glucocorticoids, Pioglitazone, Carbamezapine.

Also: barbiturates and thiazolidnediones

22

CYP3A4 inducers ___________ levels of Lovastatin, Simvastatin & Atorvastatin (ASL).

Decrease (and therefore decrease their clinical efficacy)

23

Which of the statins are metabolized by CYP2C9?

Give some eg's of CYP2C9 inhibitors.

(less important than 3A4)

FR (France): fluvastatin, rosuvastatin

Ketoconazole, itraconazole, metronidazole, sulfinpyrazone

24

What transporter do statins use to enter the liver?

OATP2

25

What is the only statin that is FDA-approved for concurrent use w/cyclosporine in cancer tx?

Pravastatin

26

*How does gemfibrozil relate to statin use?

*What is the mech behind this?

  • Strongly associated with an increased risk of statin-induced myopathy and rhabodmyolysis

  1. Inhibits OATP2 transporter-mediated uptake of statins into the liver- can increase statin systemic bioavailability >2X

  2. Inhibits the glucuronidation of statins, which is involved in the metabolism and ultimate excretion of all statins (including Pravastatin)  - can cause an increase in the systemic levels of ALL STATIN drugs.

27

Which is the safest statin to sue when a pt has a weakned liver and why?

Pravastatin (due to dual hepatic/renal elimination)

28

Name the 3 bile acid-binding resins.

Cholestyramine, colestipole, colesevelam

29

Bile acid-binding resins: MoA?

Binds bile acids and prevents reabsorption --> increased cholesterol 7alpha-hydroxylase (rate-limiting enzyme in bile acid synthesis) --> decreased chol --> increased LDL-R --> increased LDL clearance.

30

When would a bile acid-binding resin be used in combination with a statin?

When instead of a statin?

  • Combo: increase LDL-lowering effect or to allow for lower statin dose to avoid drug interactions
  • When statins are contraindicated (e.g. pregnancy)