Presentation on Antihyperlipidemic agents.pdf

Hyperlipidemia, also known as high cholesterol or lipid disorder, is a condition that occurs when there are high levels of lipids, or fats, in the blood. 
These lipids include cholesterol and triglycerides.
This can increase your risk of heart attack and stroke because blood can’t flow through your arteries easily.

1. By-
Dr. Prerana B. Jadhav
M. Pharm, Ph.D.
Pharmaceutical Chemistry
Assistant Professor,
SanjivaniCollege of Pharmaceutical Education and
Research, Kopargaon.
Antihyperlipidemic
agents

2. Introduction
•Hyperlipidemia,alsoknownashighcholesterolorlipid
disorder,isaconditionthatoccurswhentherearehigh
levelsoflipids,orfats,intheblood.
•Theselipidsincludecholesterolandtriglycerides.
•Thiscanincreaseyourriskofheartattackandstroke
becausebloodcan’tflowthroughyourarterieseasily.

3. •Badcholesterol(LDL)isthemostdangeroustype
becauseitcauseshardenedcholesteroldeposits
(plaque)tocollectinsidebloodvessels.
•Thismakesitharderforbloodtogetthrough,which
createsriskforastrokeorheartattack.
•VLDLisalsocalledbadbecauseitcarriestriglycerides
thataddtoarteryplaque.

4. Complications associated with Hyperlipidemia
•Heart attack
•Stroke
•Coronary heart disease
•Carotid artery disease
•Sudden cardiac arrest

5. Antihyperlipidemicagents
•Antihyperlipidemicagents,alsoknownaslipid-
loweringagents,hypolipidemicagents,or
cholesterol-loweringdrugs,areagroupof
medicationsthathelpstomanagehyperlipidemia,or
highlevelsoflipidsintheblood.
•Theyworkbyloweringthelevelsoflipoproteinsand
lipids,likecholesterol,intheblood.
•

6. •HMGCo-Areductaseinhibitors:
Lovastatin,Simvastatin,Atorvastatin
•Misc.class:
Ezetimibe,Clofibrate

7. HMG Co-A reductaseinhibitors
•Drugsinthisclassofhypolipidemicagentsinhibitthe
enzymeHMG-CoAreductase,responsibleforthe
conversionofHMG-CoAtomevalonateinthesynthetic
pathwayforthesynthesisofcholesterol.
•StatinscompetitivelyinhibittheHMG-CoAreductase
enzyme.Statinsbindtotheactivesiteoftheenzyme
andchangeitsstructure.

8. Lovastatin
•Thedrugwasobtainedoriginallyfromthefermentationproductsof
thefungiAspergillusterreusandMonascusruber.
•LovastatinwasoneoftwooriginalHMG-CoAreductaseinhibitors.
Theotherdrug,mevastatin(formerlycalledcompactin),was
isolatedfromculturesofPenicilliumcilliumcitrum.
•ForinhibitoryeffectsonHMG-CoAreductase,thelactoneringmust
behydrolyzedtotheopen-ringheptanoicacid.

9. Lovastatin

10. Simvastatin
•HavingstructuralsimilaritywirhLovastatin.
•Bothdrugsinprodrugformreachtheliver
unchangedafteroraladministration,wherethey
undergoextensivemetabolismtoseveralopen
ringhydroxyacids.
•BioavailabilityofSimavastatinispoorthan
Lovastatin.

11. Simavastatin

12. Atorvastatin
•Italsopossessheptanoicacidsidechainwhichiscriticalfor
inhibitionofHMG-CoAreductase.
•Althoughthesidechainislesslipophilicthanlactoneform,
thehighamountoflipophilicsubstitutioncausesthisagent
tohaveslightlyhigherlevelofCNSpenetration.
•Marketedascombinationtherapywithamlodipinfor
managementofhighcholesterolandhighbloodpressure.

13. Atorvastatin

14. Ezetimibe
•Itactbydecreasingcholesterolabsorptionin
theintestinebyblockingtheabsorptionofthe
sterolatthebrushborder.
•Itismarketedascombinationproductwith
simvastatin.

15. Clofibrate
•Clofibrateishydrolyzedrapidlyto2-p-chlorophenoxy-2-
methylpropionicacidbyesterasesinvivoand,boundtoserum
albumin,circulatesinblood.Theacidhasbeeninvestigatedasa
hypolipidemicagent.Itisabsorbedmoreslowlyandtoasmaller
extentthanistheester.
•Clofibratecanlowerplasmaconcentrationsofbothtriglycerides
andcholeterol
•Clofibrateinhibitstheincorporationofacetateintothesynthesis
ofcholesterol,betweentheacetateandmevalonatestep.

16. Clofibrate