HYPOLIPIDEMIC DRUGS

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HYPOLIPIDEMIC DRUGS

  1. 1.  Drugs which lower the level of lipidsand lipoproteins in blood. Lipids are transported in plasma aslipoproteins. Lipoproteins are classified into sixclasses based on their particle size anddensity
  2. 2. LIPOPROTEIN FUNCTION1. Chylomicrons Dietary TG transport2. Chylomicrons.rem Dietary cholesteroltransport3. VLDL Endogenous TGtransport4. IDL Transportcholesterylesters andTG to liver5. LDL Transport cholesterolto tissues and liver6. HDL Removal of cholesterolfrom tissuesFUNCTIONS OF LIPOPROTEIN
  3. 3. HYPERLIPOPROTEINAEMIASDUETO•Single gene defect{or}•Multiplegenetic,dietary &physically relatedactivitiesDUE TO• Myxoedema• Nephroticsyndrome• Chronic alcholism• Diabetes
  4. 4. SOURCES OF CHOLESTEROL
  5. 5. HMG CoAHMG CoA reductaseMevalonic acid Decreases CH synthesis by inhibition of rate limiting HMGCoA reductaseLDL 20-55%HDL 5-15%TG 10-35%
  6. 6.  First clinically used statin Absorption is incomplete 1st pass metabolism extensive Excreted in bile T1/2 is short {1-4}hrs
  7. 7. Head ache ,nausea,bowelupsets,rashesSleep disturbancesIncreased serumtransaminaseMuscle tenderness & rise inCPK levels occurinfrequentlyMyopathy is more common.Adverse effects
  8. 8. 1st choice of drugs for Primary hyper lipidaemiawith raised LDL & total CH levels.Secondary hypercholesterolaemia.Used in patients with MI,angina,stroke to lowercholesterol levels.
  9. 9. BILE ACID SEQUESTRANTS:
  10. 10. • These are basic ion exchange resins supplied inchloride form• They are neither digested nor absorbed in gut• They bind to bile acids in the intestine• They increase faecal excretion of bile salts and CH• resins can retard atherosclerosis• Not popular clinically because they areunpalatable,have to be taken in large doses,causesflatulence and interfere with absorption of manyother drugs• Have poor patient acceptability
  11. 11. GEMFIBROZIL,BEZAFIBRATE,FENOFIBRATEActivity of lipoprotein lipase
  12. 12. • Effectively lowers Plasma TG level by enhancing breakdown &suppressing hepatic synthesis of TG‘sADDITIONAL ACTION: decreases level of clotting factor VII phospholipidcomplex & promotion of fibrinolysisPHARMACOKINETICS: completely absorbed orally ,Metabolized byglucuronidation & excreated in urineADVERSE EFFECT: Epigastric distress Skin rashes impotenceUSES: Drug of choice in patient with increased TG levels
  13. 13.  It lowers TG & LDL-CH It raises HDL-CH It is used in combination withstatins
  14. 14. Nicotinic acid
  15. 15.  To lower ldl-ch are statins. Statin therapy should be commenced at low dose. In adequate response,dose should be doubled at6 wks interval.Treatment based on LDL-CH level
  16. 16. Treatment of low HDL-CH level The primary approaches of therapy is to reduce LDL–CHlevel Nicotinic acid has highest efficacy to rise HDL-CH levelfollowed by fibrates
  17. 17.  Primary tg lowering drugs are fibrates andnicotinic acid Treatment depend on cause and severityTreatment of raised TG level

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