Drugs for dyslipidaemias 2 Flashcards
List Drug-interactions of simvastatin
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
Durg of choice for patients on protease inhibitors
Atorvastatin
when using atorvastatin what happen to cholesterol synthesis
Cholesterol synthesis is suppressed for 24 hours
half life of atorvastatin
Long half-life
List fibrates drugs
Bezafibrates
Fenofibrate
Gemfibrozil
List common adverse effects of Fibrates
GI, Pruritis, Rash
List the unusual but severe adverse effects of Fibrates
Unusual but severe: rhabdomyolysis cause renal failure (excretion of
muscle proteins (myoglobin))
Unusual but severe: rhabdomyolysis cause renal failure (excretion of muscle proteins (myoglobin)) is more common in patients with what?
More common in patients with renal impairment, because of reduced protein
binding and impaired drug elimination.
List cautions for fibrates
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
Fibrates is contra-indicated where?
Contraindicated:
* Severe renal and hepatic failure
* Primary biliary cirrhosis
* Pregnancy and lactation
explain the excretion of bezafibrate
94% excreted in the kidneys (40% unchanged)
take bezafibrate after what?
meals
drugs interactions of bezafibrate
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
MoA of Bile acid binding resins
- MoA:
- Bind to bile acids in the intestine and
prevent reabsorption and enterohepatic
recirculaon → ↓absorpon 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
List the common+dosed related side effect for bile acid binding resins
GI symptoms, nausea, abdominal bloating, constipation, diarrhoea
The drug class that is inconvenient to use
Bile acid binding resins
The bile acid binding resins interfere with absorption of what?
Interfere with absorption of fatsoluble
vitamins and drugs; warfarin,
digoxin, chlrorothiazide – take 1 hour
before or 4-6 hours after
Lis the adverse effects of nicotinic acid when using normal doses
AE: normal doses = flushing (producon of PGD₂; ↓ by taking
Nicotinic acid 30 min after aspirin), palpitations, GI disturbances
Explain the adverse effects of nicotinic acid at high doses
AE: high doses = liver function disorders, impairment of glucose
tolerance & precipitate gout
MOA of Nicotinic acid
MOA: inhibit hepac TG producon & VLDL secreon → (indirect) ↓
LDL & ↑ HDL.
Acipimox is the derivate of what?
Nicotinic acid
MOA of Ezetimibe
MoA: inhibits the intestinal absorption of cholesterol and related
plant sterols; ↓ LDL by 15%
what happen if ezetimibe is synergy with statins
Synergy with statins:
* ↓ in hepac cholesterol due to inhibion of de novo synthesis +
* ↓ delivery of dietary cholesterol to liver = more LDL receptor upregulation
than with statin alone
* Inegy® = ezetimibe + simvastatin
adverse effect of ezetimibe
Adverse effects
* Common:
* Headache
* Abdominal pain
* Diarrhoea
adverse effect of ezetimibe combined with statin
- Combined with statin:
- Constipation, nausea & flatulence
- ↑ ALT/AST
- Myalgia & rhabdomyolysis
Contraindications of ezetimibe
Contraindications
* Moderate to severe hepatic
impairment
* Children < 10 years
