Drugs for dyslipidaemias

Question 1

List the complications of atherosclerosis

Answer 1

cerebral infarction
Gangrene
Peripheral vascular disease with intermittent claudication
Aortic aneurysms-rupture causes sudden death
Mycocardial infarction, cardiac failure
Carotid atheroma-emboli causing transient ischaemic attacks or cerebral infarcts

Question 2

what types of lipids are in the blood?

Answer 2

LDL
HDL
Triglycerides
Total cholesterol

Question 3

Explain the primary dyslipidaemia

Answer 3

Primary forms are genetically determined
Familial hypercholesterolaemia

Question 4

explain the secondary Dyslipidaemia and list the examples

Answer 4

2 degree forms are consequences of other conditions/drugs
Typer 2 diabetes mellitus
Obesity
Alcoholism
Nephrotic syndrome’Chronic renal failure’Hypothyroidism
Liver disease and Drugs=isotetrinoin and protease inhibitors (!HIV tx)

Question 5

list drug that are HMG CoA reductase inhibitors (statins)

Answer 5

Atorvastatin
Simvastatin
Rosuvastatin

Question 6

name drugs that are bile acid sequestrants

Answer 6

Cholestyramine

Question 7

Name the drugs that are nicotinic acid and derivates

Answer 7

Acipomox, nicotinic acid

Question 8

Name drugs that are fibrates

Answer 8

Bezafibrates, fenofibrate, gemfibrozil

Question 9

List drugs that are inhibitors of cholesterol absorption

Answer 9

Ezetimibe

Question 10

MoA of bile acid binding resins

Answer 10

Increase LDL catabolism, Decrease cholesterol absorption

Question 11

effect on lipids of bile acid binding resins

Answer 11

decrease LDL

Question 12

MoA of nicotinic acid

Answer 12

decrease LDL and VLDL synthesis

Question 13

effects on lipids of nicotinic acid

Answer 13

Decrease TG, VLDL, LDL
Increase in HDL

Question 14

MoA of fibrates

Answer 14

Increase in VLDL clearance, decrease VLDL synthesis

Question 15

effects on lipids of fibrates

Answer 15

↓ TG ,↓ VLDL,↓LDL, ↑ HDL

Question 16

MoA of statins

Answer 16

↓ LDL synthesis, ↑ LDL catabolism

Question 17

effects on lipids for statin

Answer 17

↓ LDL

Question 18

MoA of ezetimibe

Answer 18

Blocks cholesterol absorption across
intestinal border

Question 19

effects on lipids of ezetimibe

Answer 19

decrease LDL

Question 20

statins: Indications

Answer 20

Adjunct to dietary therapy for lowering LDL and total cholesterol in dyslipidaemias where this is the major problem
Primary and secondary prevention of cardiovascular disease

Question 21

List the short acting statins

Answer 21

Simvastatin
Lovastatin
Pravastatin

Question 22

when to administer Statins

Answer 22

Administer at night to reduce peak cholesterol synthesis in early morning

Question 23

List the long acting statin

Answer 23

Rosuvastatin
Atorvastatin

Question 24

The statins are well absorbed and extracted by which organ?

Answer 24

Liver

Question 25

The statin have extensive first pass hepatic metabolism via what?

Answer 25

Cytochrome P450
Glucuronidation pathways

Question 26

Explain how Simvastatin become active

Answer 26

Simvastatin is a prodrug and is converted to its active form via hepatic metabolism

Question 27

List the contraindications of statins

Answer 27

Pregnancy and lactation
Hepatic disease or elevated serum transaminases
Drugs that inhibit CYP3A4

Question 28

List the statin adverse effects that are mild

Answer 28

Muscle pain (myalgia)
GI disturbance
Raised liver enzymes
Insomnia
Rash

Question 29

List the serious Statins adverse effects

Answer 29

Skeletal muscle damage (myositis-rhabdomyolysis)-class effect and dose-related, more common in patients with lean body mass and uncorrected hypothyroidism (monitor creatinine kinase level in blood)
Angioedema

Question 30

explain the excretion of simvastatin

Answer 30

excretion >60% secreted into the bile and eliminated in the faeces