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할수있어 > 2 Lipid lowering drugs > Flashcards

2 Lipid lowering drugs Flashcards

1
Q

What is type I hyperlipoproteinaemia?

A

Familial hyperchylomicronemia

  • due to deficiency of lipoprotein lipase

↑ chylomicrons
cholesterol: +
TG: +++

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2
Q

What is type IIa hyperlipoproteinaemia?

A

Familial hypercholesterolemia

  • due to decreased number of normal LDL receptors

↑ LDL
cholesterol: +
TG: normal
risk of atherosclerosis: high

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3
Q

What is type IIb hyperlipoproteinaemia?

A

Familial combined (LDL + VLDL) hyperlipidemia

↑ LDL + VLDL
cholesterol: ++
TG: ++
risk of atherosclerosis: high

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4
Q

Name 5 classes of lipid lowering drugs + examples

Diet ↓ cholesterol & saturated fats ok

A
  1. Niacin aka Vitamin B3
  2. Fibrates - Gemfibrozil, Fenofibrate
  3. Resins - Cholestyramine
  4. HMG-CoA Reductase Inhibitors - Sim, Lo, Ator, Flu, Pra -vastatin
  5. Ezetimide

First line is statin

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5
Q

MoA of Niacin

A
  1. strongly inhibits lipolysis in adipose tissue
    → plasma TG (in VLDL) ↓ & plasma cholesterol (in VLDL and LDL) ↓
  2. ↑ HDL cholesterol levels 😊
  3. ↓ fibrinogen & ↑ t-PA → reverse thrombosis (atherosclerosis)
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6
Q

Niacin is used for which type of hyperlipoproteinaemia?

think TG!

A

Type IIb (high LDL + VLDL TG)
Type IV (high VLDL TG)

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7
Q

PK of niacin
a. route of administration
b. converted to what

A

a. oral administration
b. converted in the body to nicotinamide

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8
Q

Name 2 adverse effects of niacin

A
  1. an intense cutaneous flush and pruritus
  2. hyperuricemia and gout
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9
Q

Name 2 fibrates

A

gemfibrozil
fenofibrate

“fibr”

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10
Q

MoA of Fibrates

gemfibrozil, fenofibrate

A
  1. fibrates are ligands for PPAR-α → activates PPAR-α → increases activity of lipoprotein lipase → plasma TG levels decrease

VLDL levels decrease bc decreased secretion by liver

HDL levels rise moderately

PPAR-γ is pioglitazone (thiazolidinediones)

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11
Q

Fibrate is used for which type of hyperlipoproteinaemia?

A

hypertriglyceridemias with VLDL elevation
Type IIb, Type III

not useful for type IIa bc doesn’t target cholesterol

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12
Q

Name 4 adverse effects of fibrates

A
  1. GI effects: nausea
  2. skin rashes
  3. gallstones
  4. myositis
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13
Q

Name a bile acid binding resin

IMPT!!!

A

cholestyramine

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14
Q

MoA of cholestyramine

IMPT!!!

A

anion exchange resins bind negatively charged bile acids and bile salts in the small intestine
→ prevents reabsorption of bile acids at terminal ileum

lower bile acid concentration causes hepatocytes to increase conversion of cholesterol to bile acids → thus, intracellular cholesterol decreases

this activates increased hepatic uptake of cholesterol-containing LDL → plasma LDL ↓

may increase VLDL (bc less cholesterol) but have little effect on HDL

the only thing that increase HDL is niacin

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15
Q

Cholestyramine is used for which type of hyperlipoproteinaemia?

A

Type IIa (Familial hypercholesterolemia)

Cholestyramine + Niacin: Type IIb (mixed)
Cholestyramine → cholesterol
Niacin → TG

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16
Q

Route of administration for cholestyramine

A

Oral only

Bile salt binding resin mah. Inject for what…lol…

17
Q

Name 2 adverse effects of cholestyramine

A
  1. GI effects: constipation, nausea and flatulence
  2. impaired absorption of vitamins A, D, E, K (fat-soluble)

if take cholestyramine long term, need vitamin supplement

18
Q

Name 5 HMG-CoA reductase inhibitors

A

Sim
Lo
Ator
Flu
Pra
-vastatin

first-line lipid lowering drugs

19
Q

MoA of statins

A

inhibits HMG-CoA reductase, rate-limiting step in cholesterol synthesis

depletes intracellular cholesterol → upregulates LDL receptors on cell surface → increase uptake of plasma LDL (bc LDL has cholesterol) → LDL levels ↓

20
Q

Name 2 clinical uses of statins

A
  • effective in lowering plasma cholesterol (LDL-C) levels in all types of hyperlipidemias 😍
  • reduce the risk of coronary events and mortality in patients with ischaemic heart disease
21
Q

PK of statins
a. route of administration
b. when to eat

A

a. oral administration with first pass extraction
b. given in the evening

cholesterol-making enzyme (HMG-CoA reductase) is most active at night

Why take statins in the evening?
Cholesterol synthesis rate is at its peak during fasting state (i.e. usually when sleeping)

22
Q

If patient has Type IIa (hypercholesterolemia) but intolerant to statin, what do you give?

statin not enough how 🥵

A

PCSK9 inhibitors
Evolo
Aliro
-cumab

PCSK9 inhibitors + statin > statin only 😲😊

23
Q

MoA of PCSK9 inhibitors

A

Inhibits PCSK9
→ reduced LDL receptor degradation
→ more LDL receptors to take in LDLs
→ plasma LDL ↓

PCSK9 targets LDL receptors for degradation in lysosomes

24
Q

Route of administration

A

IM injection! bc monoclonal Ab
dose every 2 or 4 weeks

25
Q

Name 1 contraindication and 2 adverse effects of PCSK9 inhibitors

A

Contraindicated in patients who develop hypersensitivity reactions

  1. Injection site inflammatory reactions (erythema, itch, swelling, pain or tenderness)
  2. Increased incidence of nasopharyngitis and sinusitis
26
Q

MoA of Omega-3-acid ethyl esters

Omacor: EPA + DHA ethyl esters

A
  1. ↓ hepatic TG production & ↑ TG clearance from VLDL
  2. inhibits diglyceride acyltransferase (responsible for TG biosynthesis)
  3. ↑ FFA breakdown
  4. ↑ lipoprotein lipase activity
27
Q

Omega-3-acid ethyl esters is used for which type of hyperlipoproteinaemia?

A
  1. drug + diet for Type IV (hypertriglyceridemia)
  2. drug + statins for Type IIb (when TG still high)
28
Q

Route of administation for Omega-3-acid ethyl esters

A

Oral, take with food
Metabolised by liver (as with all lipids)

29
Q

Name 1 contraindication and 3 adverse effects of Omega-3-acid ethyl esters

A

Contraindicated in patients who are allergic to fish lol (bc fish oil)
1. GI symptoms
2. In some patients, DHA lead to ↑ LDL-C
3. ↓ production of Thromboxane A2 → increase bleeding time

30
Q

What is Ezetimibe?

A

Inhibitor of intestinal sterol absorption

31
Q

MoA of ezetimibe

A

a selective inhibitor of cholesterol transport protein, NPC1L1

↓ absorption of both dietary cholesterol AND cholesterol in bile acids

32
Q

Will ezetimibe still be effective in lowering LDL even in the absence of dietary cholesterol?

A

Yes
There is cholesterol from bile acids that can be reabsorbed

bile acid uses NPC1L1 too

33
Q

Clinical use of ezetimibe

A

reduction of LDL

vytorin: ezetimibe + simvastatin is synergistic

34
Q

PK of ezetimibe

A

Oral
readily absorbed, conjugated in the intestinal wall to an active glucuronide

35
Q

Adverse effect of ezetimibe

A

Low incidence of reversible impaired hepatic function

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