Dyslipemia Drugs (cholesterol) Flashcards Preview

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Flashcards in Dyslipemia Drugs (cholesterol) Deck (19):
1

HMG coA reductase inhibitors (statins)
PCSK9 inhibitors
Lamitopide
Bile acid sequestrants
Niacin
Fibrates
Ezetimibe
Omega 3 fatty acids
Herb and natural products

Drug therapy options

2

Statins

MOA: inhibits the enzyme HMG-CoA reductase which inhibits/slows down the production of cholesterol in the liver.
* flat dose response curve
-5-6% more LDL lowering by doubling dose
-dose at bedtime when liver makes most of the Cholesterol which will maximize effect
* Lipitor can be given in am: long t1/2

3

Statin
Adverse effects

* muscle toxicity: myalgia, myopathy/ Rhabdomyalgia
-heart burn/ dyspepsia
-headache
-taste disturbances
-diabetes?

4

Statin: risk factors for muscle toxicity

High statin/blood conc
Drug inx
SLCO1B1 genotype (pump)
Hyperthyroidism
Increase age
Hypoxia
Lots of exercise

5

PCSK9 Inhibitors
*injectable

MOA: inhibits activity of LDL-r to return to cell surface
1) Alirocimab (praluent)- 75-100mg SQ every 2 week
2) Evolocumab (repatha)- 140 mg every 2 weeks or 420 mg one a mth
* >40->60% LDL reduction with each
-effective with or without other therapy

6

Lamitapide (Juxtapid)

MOA: inhibits assembly of apo-B containing lipoproteins (VLDL and chyromicrons)
-LDL: ⬇️ 40-50%, TG: ⬇️45%
* close monitoring*
-homozygous familial cholesterolemia
* high risk of hepatotoxicty; monitor LFTs
* >90% with diarrhea, heart burn or N/V
- drug/dietary interaction risk
->$3000 a month

7

Bile Acid Sequestrants

MOA: bind with cholesterol containing bile acids in the intestines and then are eliminated in the stool.
-⬇️ TC, ⬇️ LDL, ⬆️ HDL, ⬆️⬇️ TG
-start with low dose and increase as needed and as tolerated
* may interfere with the absorption of other drugs
*Colesevam- may be tolerated better
*AEs: constipation, bloating, abd pain, unpleasant taste/texture (sand)

8

Niacin
MOA

Inhibition of:
-free fatty acid release from adipose tissue
-cAMP accumulation
-VLDL and LDL synthesis
-⬆️ LPL activity
* effect on lipids: ⬇️⬇️TC, ⬇️⬇️⬇️LDL, ⬆️⬆️ HDL, ⬇️⬇️⬇️TG

9

Niacin
Adverse effects

Flushing, pruitis, headache, fatigue, gastritis, abd pain, aggrevation of PUD
* impaired glucose control (hyperglycemia)
*⬆️ Uric acid concentrations

10

Niacin
Drug inx

Alcohol: ⬆️ risk of hepatotoxicty
* statins, fibrates: ⬆️ risk of hepatotoxicty and myalgias

*hepatotoxicty: with SR niacin, cut dose by 50% or limit to 2mg a day

11

Fibrates
MOA

Inhibition of cholesterol synthesis
-⬇️ TG synthesis
-inhibition of lipolysis in adipose tissue
-⬇️ production of VLDL/increase clearance
-⬆️ plasma and hepatic LDL activity
* effects on lipids: ⬇️ TC, ⬇️ LDL, ⬆️⬆️ HDL, ⬇️⬇️⬇️ TG

12

Fibrates
Dosing

Gemfibrozil: 600mg BID
Fenofibrate: dosing varies by product (fenofibrate, choline fenofibrate, fenofibric acid)

13

Fibrates
Adverse effects
Inx

Nausea, diarrhea, gallstones, phototoxcity

*statins: increase risk of hepatotoxicty/myalgias with station or niacin use
-protein binding displacement (warfarin)

14

Ezetimibe
MOA

Designed for use with statins
-cholesterol absorption inhibitor
-⬇️ LDL and ⬆️ HDL, little effect on TG
-10mg a day
* absorbed- undergoes phase 2 metabolism
-low drug inx risk

15

Ezetimibe
-when combined with a statin

Superior lowering of LDL
Statin x2= 5-6% additional LDL lowering
*adding ezetimibe = 20-25% additional LDL lowering!!

16

Omega 3 fatty acids

Products: vaslepa, lovaza, omtryg, epanova
-dosing varies by product
-prolonged bleeding/impaired platelet fxn

17

Herb/natural products

Fish oils
-red yeast rice: really works, like a statin, monitored and treated like a statin

18

LDL lowering

Statins, niacin, PCSK9 inhibitors: 50%>

Lamitopide, BAS: 25-50%>

EZ, fibrates, fish oil/O3:

19

⬆️HDL/⬇️TG

*niacin, fibrates, fish oil/O3

Statins, Lam, EZ, PCSK9, BAS