Session 4.2 - Hyperlipidaemia

Question 1

Atorvastatin

Simvastatin

Answer 1

Drug Class: Statins

Mechanism of Action: Inhibit HMG-CoA Reductase, decreasing hepatic cholesterol synthesis, increasing the LDL receptors, increasing the clearance of LDL-C from plasma into hepatocytes

Common Indicators: Hypercholesterolaemia
1° prevention = 20mg
2° prevention = 80mg

ADRs: Myalgia, Renal or Hepatic impairment, Pregnancy, Breastfeeding

Important drug-drug rxns: CYP 3A4 inhibitors –> {Amiodarone, Diltiazem, Macrolides, Amlodipine}

Question 2

Fenofibrate

Answer 2

Drug Class: Fibrate, Fibric acid dervative

Mechanism of Action: Activation of the nuclear transcription factor PPARα, which regulates the gene expression for lipoprotein lipase, increasing the production of lipoprotein lipase

Common Indicators: Hypercholesterolaemia, Low HDL, High risk of atheroma

ADRs: Photosensitivity, Gall bladder disease

Important drug-drug rxns: Warfarin - increases anticoagulation effects

Question 3

Ezetimibe

Answer 3

Drug Class: Cholesterol lowering drug

Mechanism of Action: Inhibits absorption of cholesterol at the brush border in the small intestine, decreasing plasma LDL-C concentration

Common Indicators: Hypercholesterolaemia, used in adjunct to statins

ADRs: Hepatic failure

Important drug-drug rxns: If used with statins - increased risk of rhabdomyolysis

Question 4

Alirocumab

Answer 4

Drug Class: Monoclonal antibody

Mechanism of Action: Monoclonal antibody binds to and inhibits PCSK9. This allows for more LDL-C re-uptake by the liver and facilitates a higher rate of clearance.

Common Indicators: Hypercholesterolaemia, High LDL-C

Question 5

Inclisiran

Answer 5

Mechanism of Action: Inhibits the translation of an enzyme needed for LDL receptor degradation
Resulting in decreased LDL-C