Part 2 of Drug Dyslipdemia Flashcards
Atorvastatin
What is the half-life of atorvastatin and how does it affect cholesterol synthesis?
A: Atorvastatin has a long half-life, and cholesterol synthesis is suppressed for 24 hours after taking the drug.
Are clinically relevant drug interactions common with atorvastatin?
Clinically relevant drug interactions with atorvastatin are less common and problematic compared to other statins.
Why is atorvastatin considered the drug of choice for patients on protease inhibitors?
Atorvastatin is the drug of choice for patients on protease inhibitors because it has fewer clinically relevant drug interactions, making it safer and more effective for these patients.
Fibrates
- Bezafibrate* (Bezalip®) * Fenofibrate
- Gemfibrozi
Fibrates: mechanism of action
PPARα (peroxisome proliferator-activated receptor α) agonists:
increase transcription for genes for lipoprotein lipase, ApoproteinA1
and ApoproteinA5
* Stimulate the β-oxidative degradation of fatty acids →enhance lipoprotein
lipase ↑ hydrolysis of TG in chylomicrons and VLDL parƟcles → liberate FFAs
for storage in fat or for metabolism in striated muscle, increase hepatic LDL
uptake
* ↓ hepaƟc VLDL producƟon & ↑hepaƟc LDL uptake
* ↓plasma CRP and fibrinogen levels, * improve glucose tolerance, * ↓ vascular smooth muscle inflammaƟon (inhibiƟng expression of
transcription factor nuclear factor KappaB
Fibrates: adverse effects
- Common: GI, pruritis and rash
- Unusual but severe: rhabdomyolysis cause renal failure (excretion of
muscle proteins (myoglobin)) * More common in patients with renal impairment, because of reduced protein
binding and impaired drug elimination
Fibrates: cautions and contraindication
Cautions: * Gall stones and gall bladder disorders
* PUD
* Hyperthyroidism
* Hypoalbuminaemic states (95% protein binding) * Cardiovascular disease
what to avoid when taking Fibrates
Avoid in patients with renal impairment and alcoholics – predisposed to hypertriglyceridaemia, at risk for severe muscle inflammation and injury
Contraindicated:
- Severe renal and hepatic failure
- Primary biliary cirrhosis
- Pregnancy and lactation
Fibrates: cautions and contraindications
Rang and Dale’s pharmaco
Bezafibrate
Bezafibrate is a lipid-lowering drug that belongs to the class of fibrates.
What is the mechanism of action of Bezafibrate?
Bezafibrate stimulates the β-oxidative degradation of fatty acids, enhances lipoprotein lipase activity to increase hydrolysis of triglycerides in chylomicrons and VLDL particles, liberates free fatty acids for storage in fat or for metabolism in striated muscle, decreases hepatic VLDL production, and increases hepatic LDl uptake
How does Bezafibrate work
Pharmacokinetics: 94% excreted in the kidneys (40% unchanged) * Take after meals
* 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 hypogly
What is a bile acid binding resin?
Bile acid binding resins are a type of medication used to lower cholesterol levels in the blood.
How do bile acid binding resins work?
Bile acid binding resins work by binding to bile acids in the intestines, preventing them from being reabsorbed into the bloodstream. This forces the liver to use more cholesterol to produce bile acids, leading to a decrease in cholesterol levels in the blood.
Bind to bile acids in the intestine and
prevent reabsorption and enterohepatic
recirculaƟon → ↓absorpƟon of exogenous
cholesterol & ↑ metabolism of exogenous
cholesterol into bile acids by the liver
Can bile acid binding resins be used alone or in combination with other medications?
Bile acid binding resins can be used alone or in combination with other cholesterol-lowering medications, such as statins, to achieve optimal cholesterol control.
