Dislipidemia Drugs- Melissa (3)* Flashcards Preview

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Flashcards in Dislipidemia Drugs- Melissa (3)* Deck (59)
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1

4 disease states that raise cholesterol levels:

1. Biliary Disease
2. Renal Disease
3. Hypothyroidism
4. Diabetes Mellitus *respond well to STATINS*

2

Three disease states that raise TG levels:

1. Alcoholism
2. Renal Disaese
3. Diabetes Mellitus

3

Ideal levels:
1. cholesterol
2. LDL-C
3. TG

Cholesterol: UNDER 200
LDL-C: UNDER 100 (acceptable = 100-129)
TG: UNDER 150

4

Primary causes of hyperlipidemia (2)

diet
genetics

5

3 secondary causes of hyperlipidemia:

Drugs (Propranolol, HTZ), Disease (DM), ETOH abuse

6

What is the first line therapy in hyperlipidemia?

DIET MODIFICAITON:
- Decrease fat (TGs, etc.), carbs, ETOH
- Increase exercise--> ^HDL prodxn

7

Cholestyramine, Colesnvelam, Colestipol
Drug Class, ROA, MOA?

Resins: Aways start with chol/col

ROA:
PO w/ lots of fluid; NOT ABSORBED GI--> NO bioavailability!

MOA:
Bind bile acids in sm. intestine-->
^ Fecal bile acid excretion-->
DECREASE neg. feedback on *7a-HYDROXYLASE*-->
^ Liver conversion cholesterol--> bile acid -->
DECREASE circulating cholesterol

8

How is Colesevelam administered? Why is this important?

Administered as a capsule w/ liquid; becomes gel in GI tract
*Less GI sx*; better patient compliance

9

Therapeutic use for Resin drugs?
How long do they take for max effect?
What is max effect?

- Tx ^ cholesterol (~combo treatment for ^ TG/^C pts)
- 4 weeks to max effect= 20% reduction plasma LDL-C

10

Which patient populations can take resins safely (2)?
Why is this relevant?

preggos/ nursing; kiddos +6yrs

*Good alternative to statins which cannot be used in pregnancy or in children under 8yoa

11

Resins ADRs; when are they worse?

GI sx: bloating, constipation, abdominal pain
*Worse if patients don't take enough fluid!

12

DD interactions with resins--what is the cause?
How do we avoid this?

Resins compromise absorption of fat sol vitamins and drugs
*Take drug 1 hr before or 4 hrs after resin

13

MOA for all statin drugs?
Recall the two ultimate effects:

Competitive inhib. HMG-CoA Reductase (RLS cholesterol synth.)--> DECREASE *INDOGENOUS* CHOLESTEROL SYNTH. --> **^ LDL-Rs in LIVER** + **^ HDL levels**

14

Therapeutic use for ALL statin drugs (2)?
Time to max effect?

Hypercholesterolemia; combo tx. in patients with ^ TGs
**2 weeks to max effect

15

Which two drugs are the most effective statins and can be used to treat ^ TGs?
Why are they so effective (2)?

Atorvastatin, Rosuvastatin
- Longer t 1/2
- ^ LDR # the most--> LDLR binds APOE--> ^ IDL clearance (w/TGs)

16

Which statin drug can treat kids 8+ yoa?
Why?
What is the age cut off for all other statin drugs?

Pravastatin 8+ yoa (less side effects)
Other Statins 10+ yoa

Pr= Prim, little sister (maybe 8 years old in the first hunger games movie?)

17

At what time of day does cholesterol synth. peak?
Which statin drugs are taken at night (3)?

Cholesterol synth. peaks b/w 12-2AM
Lova-, Fluva-, Simvastatin

Leah is Fast aSLeep at night. (LFS = night time drugs)
**This was a good one, thank you! :)**

18

Which statin drug should be taken at dinner (w. food)?

Lovastatin

Leah Loves Food!
Take the "L" drug with food!
**Also excellent, thank you!!**

19

Which two statin drugs can not be taken with food (dec. absorption)?

Prava-, Pitavastatin

Both start with "P". Don't take the "p" drugs when you eat your "peas".
**PRAy for PITA but don't eat it!**

20

Two prominent ADRs of statin drugs:

-Hepatic dysfunciton (^ALT, AST)
-Myalgia (^CPK) ***STOP DRUG***

21

Factors that increase hepatic ADRs of statin drugs (3)

-^dose statin
-gemfibrosil or nicotinic acid
-CYP3A4 inhibitors (ketoconazole, erythromycin)

22

Which two statins cause the LEAST ADRs?

Fluvastatin, Pravastain (KIDDOS 8+ yoa!)
--> Consequently, these are also the least potent/ cause the smallest cholesterol reduction.

23

3 contraindications for statins:

-PREGGOS X!!!/ nursing
-Liver disease
-Kiddos under 8/10

24

Which two statins are prodrugs?
Two potential factors compromising their safety of use?

Lova-, Simvastatin
CYP3A4 inhibitors, Grapefruit juice
*Atorvastatin not prodrug, but met. by CYP3A4

"LOve SIMone; she's a pro."
or "Leah's SIMply a PRO at school :)"

25

Which 2 statins are metabolized by CYP2C9?

Rosuva-, Fluvastatin

It would be *Freaking *Ridiculous 2 C 9 monkeys at the BCC!

26

Which statin is metabolized by CYP2D6?
2 clinical implications?

Simvastatin
1. CYP2D6*4 allele--> slow metabolizers--> longer t 1/2
2. SCLO1B1 SNP--> poor hepatic uptake--> ^ plasma levels
--> more ADRs (MSK pain!)

27

SCLO1B1 SNP: clinical significance?

Simvistatin; low hepatic absorption and more MSK pain!
Give these patients lower Simvastatin doses.

28

Ezetimibe:
MOA?
Describe administration regimen?

Targets *DIETARY cholesterol*
Once daily dosing

MOA:
INHIBIT NPC1L1 transporter--> DECREASE cholesterol absorption at brush boarder enterocytes (sm. intestine)

29

Therapeutic uses for Ezetimibe (2) :

Hypercholesterolemia (decrease LDL-C 20%) independently or combo tx

*DOUBLE Statin effectiveness*

30

2 ADRs of Ezetimibe:

Diarrhea with fatty meals; Hepatic dysfxn.

*Your poops come out too EZ :)*💩