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Antihyperlipidemic Agents. Hyperlipidemia  Hyperlipidemia is the most prevalent indicator for susceptibility to atherosclerotic heart disease.  it is.

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Presentation on theme: "Antihyperlipidemic Agents. Hyperlipidemia  Hyperlipidemia is the most prevalent indicator for susceptibility to atherosclerotic heart disease.  it is."— Presentation transcript:

1 Antihyperlipidemic Agents

2 Hyperlipidemia  Hyperlipidemia is the most prevalent indicator for susceptibility to atherosclerotic heart disease.  it is a term used to describe elevated plasma levels of lipids that are usually in the form of lipoproteins.

3 Lipoproteins Metabolism

4 Lipid-lowering drugs can be classified into:  Sequestering agents (Bile acids sequestrants)  Inhibitor of de novo cholesterol biosynthesis. (HMG-CoA Reductase inhibitors)  Alteration of cholesterol metabolism  Inhibition of lipoprotein synthesis.  Miscellaneous.

5 1-Sequestering agents (Bile acids sequestrants)

6 Cholestyramine Resin (Questran)  It is a styrene copolymer with divinylbenzene with quaternary ammonium functional groups.

7 Colestipol HCl (Colestid)  It is a high-molecular-weight, insoluble, granular copolymer.  It reduces cholesterol levels without affecting triglycerides.

8 Colesevelam (Welchol)  It does not possess Cl- ion (as in Cholestyramine and colestipol) and is not an anion-exchange resin.

9 2-Inhibitor of de novo cholesterol biosynthesis (HMG-CoA Reductase inhibitors).

10

11 Lovastatin (Mevacor)  It is a potent inhibitor of HMG-CoA reductase.  For inhibitory effect on HMG-CoA reductase, the lactone ring must be hydrolyzed to the open-ring heptanoic acid

12 Simevastatin (Zocor)  It is an analogue of Lovastatin.

13 3-Alteration of cholesterol metabolism

14 Dextrothyroxine sodium (Choloxin) O-(4-Hydroxy-3,5-diiodsophenyl)-3,5-diiodo-D- tyrosine monosodium hydrate.

15 Clofibrate (Atromid-S) Ethyl 2-(p-chlorophenoxy)-2-methylpropionate

16 Clofibrate is prepared by Williamson synthesis.

17 Gemfibrozil (Lopid) 5-(2,5-Dimethylphenoxy)-2,2-dimethyl pentanoic acid  It is structurally similar to clofibrate.  Its mechanism of action and use are similar to those of clofibrate.

18 Finofibrate (Tricor) 2-[4-(4-Chlorobenzoyl)phenoxy]-2-methylpropanoic acid 1- methylethyl ester.  It has structural features represented in clofibrate.

19 Structure-activity relationship of fibrates

20 4-Inhibition of lipoprotein synthesis.

21 Probucol (Lorelco) 4,4-[(1-Methylethyliden)-bis thio-[2,6-bis(1,1- dimethyethyl)] phenol.  Probucol has high lipophilic characters with strong antioxidant properties.

22 Nicotinic acid, Niacin 3-Pyridine carboxylic acid.  It has the ability to inhibit lipolysis (i.e. prevent the release of free fatty acids and glycerol from fatty tissues).

23 Pentaerthritol tetranicotinate  Pentaerthritol tetranicotinate is an example of molecular association in which a tetra- replicate of nicotinic acid was developed (Molecular replication).

24 5-Miscellaneous.

25 β-Sitosterol  Sitosterol is a plant sterol, whose structure is identical with that of cholesterol, except for the substituted ethyl group on C-24 of its side chain.  The drug inhibits the absorption of dietary cholesterol from the gastrointestinal tact.


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