Drugs for dyslipidaemias 2

Question 1

List Drug-interactions of simvastatin

Answer 1

concomitant use associated with rhabdomyolysis amlodipine & amiodarone
(simvastatin dose should not exceed 20mg daily) diltiazem and verapamil
(simvastatin dose should not exceed 10mg daily) Fibrates and nicotinic acid
* Protease inhibitors

Question 2

Durg of choice for patients on protease inhibitors

Answer 2

Atorvastatin

Question 3

when using atorvastatin what happen to cholesterol synthesis

Answer 3

Cholesterol synthesis is suppressed for 24 hours

Question 4

half life of atorvastatin

Answer 4

Long half-life

Question 5

List fibrates drugs

Answer 5

Bezafibrates
Fenofibrate
Gemfibrozil

Question 6

List common adverse effects of Fibrates

Answer 6

GI, Pruritis, Rash

Question 7

List the unusual but severe adverse effects of Fibrates

Answer 7

Unusual but severe: rhabdomyolysis cause renal failure (excretion of
muscle proteins (myoglobin))

Question 8

Unusual but severe: rhabdomyolysis cause renal failure (excretion of muscle proteins (myoglobin)) is more common in patients with what?

Answer 8

More common in patients with renal impairment, because of reduced protein
binding and impaired drug elimination.

Question 9

List cautions for fibrates

Answer 9

Cautions:
* Gall stones and gall bladder disorders
* PUD
* Hyperthyroidism
* Hypoalbuminaemic states (95% protein binding)
* Cardiovascular disease
* Avoid in patients with renal impairment and alcoholics – predisposed to
hypertriglyceridaemia, at risk for severe muscle inflammation and injury

Question 10

Fibrates is contra-indicated where?

Answer 10

Contraindicated:
* Severe renal and hepatic failure
* Primary biliary cirrhosis
* Pregnancy and lactation

Question 11

explain the excretion of bezafibrate

Answer 11

94% excreted in the kidneys (40% unchanged)

Question 12

take bezafibrate after what?

Answer 12

meals

Question 13

drugs interactions of bezafibrate

Answer 13

Drug interactions:
* Warfarin – increased anticoagulant effect, reduce warfarin dose by half, then
adjust dose according to INR
* Statins – increased risk of rhabdomyolysis
* Sulphonylureas – increased risk of hypoglycaemia
* Cholestyramine – administer 2 hours apart

Question 14

MoA of Bile acid binding resins

Answer 14

• MoA:
• Bind to bile acids in the intestine and
  prevent reabsorption and enterohepatic
  recircula􀆟on → ↓absorp􀆟on of exogenous
  cholesterol & ↑ metabolism of exogenous
  cholesterol into bile acids by the liver
• ↑ expression of LDL receptors in liver cells
  → ↑ removal of LDL from the blood → ↓
  LDL in plasma

Question 15

List the common+dosed related side effect for bile acid binding resins

Answer 15

GI symptoms, nausea, abdominal bloating, constipation, diarrhoea

Question 16

The drug class that is inconvenient to use

Answer 16

Bile acid binding resins

Question 17

The bile acid binding resins interfere with absorption of what?

Answer 17

Interfere with absorption of fatsoluble
vitamins and drugs; warfarin,
digoxin, chlrorothiazide – take 1 hour
before or 4-6 hours after

Question 18

Lis the adverse effects of nicotinic acid when using normal doses

Answer 18

AE: normal doses = flushing (produc􀆟on of PGD₂; ↓ by taking
Nicotinic acid 30 min after aspirin), palpitations, GI disturbances

Question 19

Explain the adverse effects of nicotinic acid at high doses

Answer 19

AE: high doses = liver function disorders, impairment of glucose
tolerance & precipitate gout

Question 20

MOA of Nicotinic acid

Answer 20

MOA: inhibit hepa􀆟c TG produc􀆟on & VLDL secre􀆟on → (indirect) ↓
LDL & ↑ HDL.

Question 21

Acipimox is the derivate of what?

Answer 21

Nicotinic acid

Question 22

MOA of Ezetimibe

Answer 22

MoA: inhibits the intestinal absorption of cholesterol and related
plant sterols; ↓ LDL by 15%

Question 23

what happen if ezetimibe is synergy with statins

Answer 23

Synergy with statins:
* ↓ in hepa􀆟c cholesterol due to inhibi􀆟on of de novo synthesis +
* ↓ delivery of dietary cholesterol to liver = more LDL receptor upregulation
than with statin alone
* Inegy® = ezetimibe + simvastatin

Question 24

adverse effect of ezetimibe

Answer 24

Adverse effects
* Common:
* Headache
* Abdominal pain
* Diarrhoea

Question 25

adverse effect of ezetimibe combined with statin

Answer 25

• Combined with statin:
• Constipation, nausea & flatulence
• ↑ ALT/AST
• Myalgia & rhabdomyolysis

Question 26

Contraindications of ezetimibe

Answer 26

Contraindications
* Moderate to severe hepatic
impairment
* Children < 10 years