CPT S3 Steroids & Cholesterol

Question 1

Describe the metabolism of the combined oral contraceptive pill

Answer 1

Metabolised by CYP450 enzymes in the liver

Therefore affected by enzyme inducing and inhibiting drugs

Question 2

Give some examples of adverse effects of the COCP

Answer 2

Venous thromboembolism
MI
Hypertension
Decreased glucose tolerance
Increased risk of stroke in women who get focal migraines
Headaches
Mood swings
Cholestatic jaundice
Increased gallstone incidence
Precipitate porphyria 
Endometrial hyperplasia and cancer
Breast tenderness

Question 3

Give the mode of action of the progesterone only pill

Answer 3

Adverse effect on cervical mucous

Adverse effect on endometrium

Question 4

Give some adverse effects of the POP

Answer 4

Acne
Depression, PMS, lack of concentration
Weight gain
Nausea
Irritability

Question 5

Describe the action of the combined oral contraceptive pill

Answer 5

Suppression of ovulation
Inhibition of FSH and LH
Adverse effect on cervical mucous
Adverse effect on endometrium

Question 6

Define an atheroma

Answer 6

Infiltration of LDLs into the tunica intima of an artery.

Question 7

Give some effects of oxidated LDL

Answer 7

Macrophage motility inhibition
T cell activation
Endothelial cell toxicity
Enhanced platelet aggregation

Question 8

Give some classes of lipid-lowering drugs

Answer 8

Statins
Fibrates
Nicotinic acids
Plant sterols
Cholesterol lipase inhibitors
Resins
Omega-3 fatty acids

Question 9

Name a statin

Answer 9

Simvastatin

Question 10

Give the mechanism of action of statins

Answer 10

Inhibits cholesterol synthesis in hepatocytes
Increased clearance of IDL and LDL
Decreased formation of VLDL and LDL

Question 11

Give some indications for statin therapy

Answer 11

CVS risk prevention

Familial hypercholesterolaemia

Question 12

Give some adverse drug reactions for statins

Answer 12

Increased transaminase
Myopathy
General: arthralgia, GI upset, headache

Question 13

What is the mechanism of action of fibric acid derivatives?

Answer 13

PPARα agonist
Increases activity of lipoprotein lipase
Greatly reduces triglyceride production
Variable reduction in LDLs

Question 14

Give some side effects of fibric acids

Answer 14

GI upset
Cholelithiasis
Myositis
Abnormal LFTs

Question 15

Give some contraindications for fibric acid derivatives

Answer 15

Gallbladder disease
Renal dysfunction
Hepatic dysfunction
Statin use

Question 16

What are the actions of nicotinic acids?

Answer 16

Decreases VLDL
Increases HDL (especially HDL-C
Inhibits lipoprotein A synthesis

Question 17

Give some side effects of nicotinic acid

Answer 17

Flushing
Itching
Headache
GI upset
Hepatotoxicity
Peptic ulcer activation
Hyperglycaemia and decreased insulin sensitivity

Question 18

Give some contraindications of nicotinic acid

Answer 18

Active liver disease
Unexplained LFT elevation
Peptic ulcer disease

Question 19

Give the mechanism of action of ezetimibe

Answer 19

Selective inhibition of intestinal cholesterol absorption
Therefore:
-Decreased intestinal delivery of cholesterol to the liver
-Increased expression of hepatic LDL receptors
-Decreased cholesterol content of atherogenic particles

Question 20

Give and explain some side effects of ezetimibe

Answer 20

Headache
Abdominal pain
Diarrhoea
These are mostly GI ADRs because ezetimibe circulates enterohepatically so systemic exposure is limited

Question 21

What needs to be considered when prescribing fibric acid derivatives and statins?

Answer 21

Increased incidence of rhabdomyolysis and myopathy with concomitant use
Benefits vs risk analysis
Mostly gemfibrozil responsible for this effect
Statins plus fibric acid derivatives highly effective in lowering TGCs, LDLs and VLDL levels whilst increasing HDL

Question 22

Give some examples of dietary supplements that have a positive effect on lipid profile

Answer 22

Fish oils
Fibre
Plant sterols
Vitamin C and E
Alcohol (on HDL)

Question 23

Give some dietary factors which have a negative effect on lipid profile

Answer 23

High fat/cholesterol diet

Alcohol (on TGs)