Statins / HMG-CoA reductase inhibitors

Question 1

HMG-CoA reductase inhibitors also known as…

Answer 1

Statins

Question 2

MOA: HMG-CoA reductase inhibitors / Statin

Answer 2

Drugs for Dyslipidaemia
* Inhibit HMG-CoA reductase
* increase hepatic cholesterol uptake
* reduce cholesterol, LDL
* small increase in HDL

Competitively inhibit 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (a rate-limiting enzyme in cholesterol synthesis). Increase hepatic cholesterol uptake from blood, reduce concentrations of total cholesterol, LDL and triglyceride (modest), and produce a small increase in HDL concentrations.

Question 3

Indication: Statin / HMG-CoA reductase inhibitor

Answer 3

• Hypercholesterolaemia
• High risk of coronary heart disease, with or without hypercholesterolaemia

Used in low doses for primary CVD prevention (high risk CVD patients with no pt Hx of CVD yet)
Used in high doses for secondary prevention of CVD (pt with recent CVD Hx)

Question 4

Adverse reactions
Statins / HMG-CoA reductase inhibitor

Answer 4

• mild GI symptoms
• headache
• sleep disturbance
• dizziness

Muscle symptoms (myalgia, myopathy, rhabdomyolysis)
Risk of myopathy (with or without CK elevation) and rhabdomyolysis is dose-related. Risk is also increased by age, illness (see Precautions) and certain drug interactions (see Statins).

Muscle symptoms are more likely in the first 4–6 weeks after starting or increasing the dose of a statin. Statin-associated muscle symptoms are often difficult to differentiate from other causes; for further information see www.nps.org.au/​sams.

There have been very rare reports of an autoimmune necrotising myopathy, generally with CK concentration >10 times ULN and anti-HMG-CoA reductase autoantibodies, which does not resolve solely on stopping the statin.

An effect on ocular muscles may cause visual disturbances (eg diplopia or blurred vision).

Aminotransferase concentrations
Elevated aminotransferases occur in 0.5–2% of patients treated with statins; it is dose-dependent, generally responds to a reduction in dosage.

Diabetes
Statins are associated with a slightly increased risk for new-onset diabetes which appears highest in those who are already more likely to develop diabetes.

A meta-analysis reported that, on average, treating 255 patients with statins for 4 years resulted in 1 additional case of diabetes (while possibly preventing >5 major coronary events).

Question 5

Practice points
Statins / HMG-CoA reductase inhibitor

Answer 5

• do not stop if symptoms of ACS
• 1st choice for hypercholesterolaemia
• TIMING : simvastatin better at night, must be taken consistently
• Monitor Creatine (affects muscle issues)

Question 6

Drug Class

Atorvastatin

Answer 6

Statin / HMG-CoA reductase inhibitor

Question 7

Drug Class

Fluvastatin

Answer 7

Statin / HMG-CoA reductase inhibitor

Question 8

Drug Class

Pravastatin

Answer 8

Statin / HMG-CoA reductase inhibitor

Question 9

Drug Class

Rosuvastatin

Answer 9

Statin / HMG-CoA reductase inhibitor

Question 10

Drug Class

Simvastatin

Answer 10

Statin / HMG-CoA reductase inhibitor

Question 11

Generic names of Statins / HMG-CoA reductase inhibitors

Answer 11

Atorvastatin
Fluvastatin
Pravastatin
Rosuvastatin
Simvastatin