Cholesterol Final Study

Question 1

Statins

Answer 1

MOA: inhibit HMG-CoA-reductase
(decrease hepatic cholesterol –> upregulation of LDL-R –> increase hepatic uptake of LDL
* as decrease cholesterol in hepatocytes –> decreased VLDL synthesis –> decrease TGs

AEs: Hepatotox
SKM tox (rhabdomyolysis –> renal tox)

CI: pregnancy

Question 2

Cholestyramine, Colestipol, Colesevelam

Answer 2

BA Sequestrants

MOA: bind BA in intestine –> decrease BA in circulation –> increase BA synthesis in liver
(decrease hepatic cholesterol –> upregulation of LDL-R –> increase hepatic uptake of LDL)

AEs: no systemic abs
-GI (constipation, bloating)
-interferes with abs of other meds

Question 3

Ezetimibe

Answer 3

NPC1C1 Inhibitor

MOA: inhibit NPC1C1 transporter –> decrease cholesterol delivery to liver
(decrease hepatic cholesterol –> upregulation of LDL-R –> increase hepatic uptake of LDL)

AEs: minimal AEs

Question 4

Alirocumab, Evolocumab

Answer 4

PSCK-9 Inhibitor
MOA: mab against PSCK9 –> decrease LDL-r degradation

*SC injection

AEs:
injection site/allergic rxn

Question 5

Niacin

Answer 5

MOA: activates niacin-rs (Gi) on adipocytes –> decrease FA release from adipose tissue –> hepatic TG synthesis –> decrease VLDL –> LDL

AEs: flushing, itching, headache
hepatotox
hyperglycemia
hyperuricemia

*increase SKM tox with statins

Question 6

Fenofibrate, Gemfibrozil

Answer 6

Fibrates

MOA: activate PPRA(alpha)-r (nuclear-r) –> increase LPL –> increase clearance of VLDL –> decrease TG synthesis –> decrease VLDL

AEs:
GI
Gallstones
SKM tox with statins (Gem)