lipid lowering drugs - bile acid sequestrants, cholesterol absorption inhibitors, fibrates

Question 1

MOA of bile acid seq

Answer 1

bind bile acids, preventing their reabsorption
this promotes hepatic conversion of cholesterol into bile acids
resultant increased LDL receptor activity of liver cells increases clearance of LDL-C from plasma

Question 2

cautions for all bile acid sequestrants - they interfere with the absorption of fat soluble vitamins e.g. …. so supplements of the following may be required when treatment is prolonged

Answer 2

supplements of vitamins A, D, K, and folic acid may be required when treatment is prolonged

Question 3

common SE for all bile acid sequestrants (5)

Answer 3

Constipation; gastrointestinal discomfort; headache; nausea; vomiting

Question 4

BAS - use in pregnancy and BF

Answer 4

used with caution as although the drugs are not absorbed, they may cause fat-soluble vitamin deficiency on prolonged use.

Question 5

colestryramine - important note on how to take it in regards to other drugs

Answer 5

Manufacturer advises take other drugs at least 1 hour before, or 4–6 hours after, colestyramine.

Question 6

important advice on how to take colesevelam in regards to other drugs

Answer 6

Manufacturer advises take 4 hours before, or after, other drugs.

However, they may be taken at the same time as the statin and ezetimibe if this combination treatment is used

Question 7

Colesevelam and ciclosporin - monitoring

Answer 7

Patients receiving ciclosporin should have their blood-ciclosporin concentration monitored before, during, and after treatment with colesevelam.

Question 8

Counselling on admin for all bile acid sequestrants

Answer 8

avoid other drugs at same time

however for coleveselam, it can be taken at the same time as statin and ezetimibe

Question 9

Why are they contraindicated in biliary obstruction (Bile acid seq)

Answer 9

not likely to be effective

Question 10

colestipol - how to take it in regards to other drugs

Answer 10

Manufacturer advises take other drugs at least 1 hour before, or 4 hours after, colestipol.

Question 11

name the 3 bile acid sequestrants

Answer 11

colestyramine
coleveselam
colestipol

Question 12

MOA ezetimibe

Answer 12

inhibits intestinal absorption of cholesterol
when used alone, modest effect on lowering LDL-C with little effect on other lipoproteins

Question 13

Ezetimibe & fibrates - severe interaction. What is it?

Answer 13

increased risk of gallstones
discontinue if gallstones develop

Question 14

max dose of fenofibrate with concurrent use of a statin

Answer 14

200mg

Question 15

how do fibrates work

Answer 15

decrease serum triglycerides
have a variable effect on LDL-C

Question 16

a patient is photosensitive to ketoprofen. can they take fenofibrate

Answer 16

no
fenofibrate is contraindicated if photosensitivity to ketoprofen

Question 17

pt has Hx gall bladder disease. Are fibrates suitable?

Answer 17

no contraindicated in gall bladder disease

Question 18

Severe interaction with statins and fibrates

Answer 18

increases the risk of rhabdomyolysis when given with statins
adjust fenofibrate dose to max 200mg when given with statins

Question 19

fibrates interaction with coumarins - what is the interaction

Answer 19

severe
fibrates predicted to increase AC effect of warfarin, phenindione, acenocoumarol
monitor INR and adjust dose

Question 20

Fenofibrate interaction with Cs

Answer 20

Fenofibrate increases the risk of nephrotoxicity when given with Ciclosporin. Manufacturer advises monitor renal function.

Question 21

Fenofribate interaction with colchicine

Answer 21

Colchicine increases the risk of rhabdomyolysis when given with Fenofibrate. Manufacturer makes no recommendation.

Question 22

Fenofibrate interaction with SUs and insulin

Answer 22

Fenofibrate is predicted to increase the risk of hypoglycaemia
no recommendation or class of severity

Question 23

Ursodeoxycholic acid interaction with fenofibrate

Answer 23

Fenofibrate is predicted to decrease the efficacy of Ursodeoxycholic acid. Manufacturer advises avoid.

Question 24

fibrates are mainly used in who?

Answer 24

Fibrates are mainly used in those whose serum-triglyceride concentration is greater than 10 mmol/litre or in those who cannot tolerate a statin (specialist use).

Question 25

monitoring with fibrates

Answer 25

advised to monitor hepatic transaminases every 3 months during 1st year and periodically thereafter
discontinue treatment if levels increase to >3x ULN
monitor serum creatinine during the first 3 months of treatment and periodically thereafter
interrupt treatment if Cr level 50% above ULN

Question 26

T or F - correct hypothyroidism before initiating treatment

Answer 26

true

Question 27

fibrates use in RI and myotoxicity

Answer 27

avoid in severe RI
special care needed in pt with renal disease - progressive increases in serum Cr of failure to follow dosage guidelines may result in myotoxicity (rhabdomyolosis)
discontinue if myototixicty suspected or CK conc increases signficiantly

Question 28

when fibrates are used in combo with statin, consider monitoring

Answer 28

liver function and creatine kinase

Question 29

monitoring for ciprofibrate

Answer 29

Liver function tests recommended every 3 months for first year (discontinue treatment if significantly raised).

Question 30

name the 4 fibrates

Answer 30

bezafibrate
ciprofibrate
fenofibrate
gemfibrozil

Question 31

nicotinic acid - how does it work

Answer 31

in doses of 1.5-3g daily it lowers both cholesterol and triglyceride conc by inhibiting synthesis
also increases HDL-C

Question 32

discontinue bempedoic acid if the folllowing occurs (2)

Answer 32

• liver transaminases at least 3x ULN and persists at this
• hyperuricaemia accompanied with symptoms of gout occur

Question 33

how does bempedoic acid work

Answer 33

ACL inhibitor which inhibits cholesterol synthesis in liver , thereby lowering LDL-C

Question 34

true or false - bempedoic acid common SE if hyperuricaemia and gout

Answer 34

true

Question 35

true or false - nicotinic acid increases HDL-C

Answer 35

true