Hypolipidaemic Drugs Flashcards
(22 cards)
How many classes of drugs
5
Which are they
HMG-CoA reductase inhibitors/statins
Lipoprotein lipase activators/fibrates
Sterol absorption inhibitor
Lipase and triglyceride synthesis inhibitor
Bile acid sequestrants
Examples of HMG-COA reductase inhibitors
High efficacy: Rosuvastatin, Atorvastatin
Low efficacy: Lovastatin, simvastatin
Examples of Fibrates
Gemfibrozil
Bezafibrate
Example of sterol uptake inhibitor
Ezetimibe
Example of bile acid sequestrants
Colestipol
Cholestyramine
Example of lipase and triglyceride synthesis inhibitor
Nicotinic acid
MOA of statins
HMG-CoA converted to mevolonate by HMG-COA reductase
Statins inhibit HMG COA reductase
ADR of statins
Most common: muscle aches
Can cause myopathy
GIT complaints, headache, rashes, sleep disturbances uncommon
Liver damage very rare
Uses of statins
- Primary and secondary hyperlipidemias
- In ASCVD patients (angina, MI, ACS)
- Secondary Prophylaxis of MI
- Prevent thromboembolism
MOA of bile acid sesquestrants
Bind bile acids in the intestine and interrupt enterohepatic circulation. Hence faecal excretion of both bile and CH increased
MOA of fibrates
Activate key enzyme for degradation of VLDL - lipoprotein lipase
Results in lowering of circulating TGs
Effect achieved by effect on PPAR-alpha receptor which enhances lipoprotein lipase synthesis and fatty acid oxidation
What is PPAR-alpha
Peroxisome proliferator activator receptor alpha
ADR of fibrates
Epigastric pain, diarrhea
Skin rashes body ache
Myopathy and hepatitis uncommon
Why is gemfibrozil and statins not given together
Increases risk of myopathy
MOA of nicotinic acid
Inhibits intracellular lipolysis by lipase in adipocytes and decrease flow of FFA from adipose tissue to liver which reduces FFA availability for synthesis of TGs and VLDL
Actions of Nicotinic acid
Decreases TG, VLDL
Modest fall in LDL-CH
Increases HDL-CH
ADR of Nicotinic acid
Cutaneous vasodilation hence causes marked flushing, heat, itching due to release of PGD2
Dyspepsia and can lead to ulcer
Hyperglycemia and DM
Dryness and hyperpigmentation
Hyperuricemias
Arrhythmias
Uses of Nicotinic acid
Lower VLDL and raise HDL
Control acute pancreatitis associated with severe hyper triglyceridemias
MOA of ezetimibe
Inhibits intestinal absorption of dietary and intestinal CH absorption by interfering with CH transport protein called NPC1L1
Life style modifications for hyperlipidemia
Low fat low carb diet
Limitation of saturated and trans fat
Exercise
Weight control
Smoking cessation
No alcohol
High intensity, moderate and low intensity therapy
Rosuvastatin and Atorvastatin high intensity
Rozat: 10-40mg high 5-10mg moderate no low
