Bile acids and Cholesterol Absorption inhibitors , PCSK9 inhibitor

Question 1

Name the Bile Acid Absorption Inhibitors

Answer 1

-Resins-

Cholestyramine (“Cho”lobetser”amine”)
Colestipol
Colesevelam

Question 2

Resins MOA

Answer 2

-resins interrupt bile acid recycling and promote synthesis of new bile acids, depleting cholesterol stores

• causing HMG CoA reductase to synthesis more cholesterol
  (“Activating HMG crude ore reducer”)
• causing upregulation of LDL receptor and uptake of circulating LDL
  (“Activating LoaD L receptor”)

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(“Empty gold stores”)

Question 3

Resins are used in patients with …

Answer 3

primary hypercholesteremia

• since the introduction of statins, now have only a minor role for this indication

Question 4

Resins Side Effects

Answer 4

-bile acid resins (cholestyramine, colestipol, colesevelam) cause hypertryglycemia

(increased VLDL’s)
(“Cho”lobster”amine scaring airship away”)

• do not use this in hypocholesteremia with concomitant hypertriglycemia

-can cause cholesterol gall stones
(“Sea”gall” stones”)

-bile acid resins can cause constipation and bloating.

• do not use in pts with diverticulitis, or preexisting bowel disease
  (“Cho”lobster”mine clamping pipe”)

​- impair absorption of fat soluble vitamins A, D, E, K
(Cho”lobster”mine on DEcK-A”)

-bile acid resins decrease statin absorption-administer 4 hours apart

(“Cho”lobster”amin clashing with statin punk”)

Question 5

Ezetimibe MOA

(“Z-shaped eel”)

Answer 5

-blocks intestinal absorption of cholesterol decreasing chylomicron carrier
(“Z shaped eel blocking gold delivery at intestinal airbase”)

-restricts liver’s access to exogenous cholesterol
(“Empty chest delivery”)

-causing HMG CoA reductase to synthesize more cholesterol
(“Activating HMG crude ore reducer”)

-causing upregulation of LDL receptors and uptake
of circulating LDL
(“Sunken LDL ship”)

Question 6

What are the Benefits of using Ezetimibe

Answer 6

• Doesn’t cause Gallstones
• Doesnt cause Hypertriglyceridemia

Question 7

Ezetimibe Side Effects

Answer 7

-may cause increased liver function tests (LFT’s)
(“Raised LFT flag”)

-may cause diarrhea / steatorrhea
(“Z shaped eel shitting oily water”)

Question 8

Name a PCSK9 inhibitor

Answer 8

Evolocumab

(“Steam-ctopus man”)

Question 9

Evolocumab MOA

(“Steam-ctopus man”)

Answer 9

-PCSK9 normally causes degradation of LDL receptors
(“Pesky “9” crabs inhibiting LoaD L receptor workers”)

-Evolocumab binds PCSK9 and prevents degradation of LDL receptors, increasing uptake of circulating LDL
(“Steam-octopus man removing pesky crabs”)

• Many PCSK9 inhibitors (evolcumab) are antibodies
  (“Steam-ctopus man with antibody-shaped claws”)