Lipid Lowering Drugs

Question 1

7 Classes of drugs for Lipid Lowering

Answer 1

Statins
Cholesterol absorption inhibitor (Ezetimibe)
Fibrates (Gemfibrozil)
Bile acid sequestrants (Cholestyramine )
PCSK9 Inhibitors
Omega 3 fatty acids
Niacin (vit B3)

Question 2

Statins MOA

Answer 2

HMG CoA reductase inhibitors
inhibit cholesterol synthesis
increase hepatic LDL receptors

Question 3

Uses of statins

Answer 3

Hyperlipidemias
Lower coronary events in IHD patients

Question 4

Cholesterol absorption inhibitor MOA

Answer 4

Inhibit absorption of cholesterol (dietary & biliary) by blocking human sterol transport protein NPC1L1

Question 5

Fibrates MOA

Answer 5

Ligand for PPAR-alpha
Lower TG, Increase HDL, Lower VLDL

Question 6

Fibrates uses

Answer 6

In elevated VLDL
especially hypertriglyceridemia (type IV), dysbetalipoproteinemia (type III)

Question 7

Bile acid sequestrants MOA

Answer 7

Bind bile salts/acids
Decrease reabsorption
Increase hepatic bile production, deplete hepatic cholesterol, increase hepatic LDL receptors, lower systemic LDL

Question 8

Bile acid sequestrants Uses

Answer 8

In increased LDL
Type IIa (hypercholesterolemia)
Type IIb (with niacin)

Question 9

PCSK9 Inhibitor MOA

Answer 9

Prevent dissociation of LDL receptor, increase lysosomal degreadation of LDL

Question 10

PCSK9 Uses

Answer 10

Familial Hypercholesterolaemia (Type IIa)
Atherosclerotic CVD requiring additional LDL-C lowering after being on diet control & maximum tolerated statin therapy

Question 11

Omega 3 FA MOA

Answer 11

Lower TG levels by increasing beta oxidation
Decrease synthesis, inhibit diglyceride acyltransferase, increase TG clearance from VLDL

Question 12

Omega 3 FA uses

Answer 12

Adjunct to diet for treatment of Type IV (hypertriglyceridemia)
Type II (with statins)

Question 13

Route of administration of lipid-lowering drugs

Answer 13

All PO except for PCSK9 (IV)

Question 14

Statins ADR

Answer 14

GI distress
hepatotoxicity
myotoxicity
pregnancy (cat X)

Question 15

Cholesterol Absorption Inhibitor ADR

Answer 15

Common: diarrhea, flatulence
rhabdomyolysis (when combined with statins)
reversible hepatotoxicity (low incidence)

Question 16

Fibrates ADR

Answer 16

GIT (nausea)
skin rashes
gall-stones
myositis

Question 17

Bile acid binding resins ADR

Answer 17

GI effects: constipation, nausea, flatulence
impaired absorption of vitamin A, D, E, K

Question 18

PCSK9 Inhibitor ADR

Answer 18

Contraindicated: hypersensitivity reactions
Injection site inflammatory reactions (erythema, itchiness, swelling, pain)
nasopharyngitis & sinusitis

Question 19

Omega 3 FA ADR

Answer 19

Contraindicated: allergic to fish (from fish oil)

GIT: abdominal distension, pain, constipation, diarrhoea, dyspepsia, flatulence (most common)

May cause increased LDL-C (monitor levels in familiar hypercholesterolaemia)

Lower proportion of thromboxane A2 (increased bleeding time)

Question 20

Name of Statin

Answer 20

Simvastatin, Lovastatin

Question 21

Name of Cholesterol absorption inhibitor

Answer 21

Ezetimibe

Question 22

Name of bile acid sequestrant

Answer 22

Cholestyramine

Question 23

Name of PCSK9 Inhibitors

Answer 23

Evolocumab
Alirocumab