lipid lowering drugs/for dyslipidemia

Question 0

statins 
3 examples 
nature
MOA
effects
uses
pharmacokinetics
SEs

Answer 0

simavistatin, pravastatin, atorvastatin

nature: HMG-CoA reductase inhibitors
MOA: inhibit the RATE-LIMITING STEP in cholesterol synthesis
statins also increase expression of eNOS endothelial NO synthase to increase NO synthesis – cholesterol independent mechanism

• decrease endogenous hepatic cholesterol synthesis
• increase LDL receptor synthesis
• increase LDL clearance from plasma
• pleiotropic effects (notes)

uses

• hypercholestrolaemia chol >6.5mmol/L or LDL >3mmol/L
• familial and acquired
• secondary prevention for patients w MI, stroke and angina
• primary prevention based on age, gender, diabetics and smoking

simavistatin and pravastatin – specific and reversible inhibitors
atorvastin – irreversible inhibitors

SE

• well tolerated w minor SEs
• rash, sleep disturbances and muscle aches

Question 1

what are the drug groups for lipid lowering drugs>

Answer 1

statins and fibriates

lipid lowering drugs decrease cholesterol in circulation and is not a treatment for atherosclerosis

Question 2

fibriates 
examples 3 
nature 
MOA
consequences 
uses
SE

Answer 2

benzafibrate, fenofibrate, clofibrate

agonist at nuclear receptor PPAR

bind to specific sites on PPAR nuclear receptor - control/regulate transcription of genes involved in lipid metabolism

increase transcription of lipoprotein lipase apoA1 and apoA5

• increase TG hydrolysis from VLDL
• decrease hepatic VLDL synthesis
• increase hepatic LDL uptake
• decrease VLDL, TG LD and increase HDL

use

• patients intolerant to statins
• high risk patients w low HDL mixed dyslipidemia

SEs

• rhabdomyolosis
• clofibrate - gallstones
• abdominal pain and nausea