12_antilipemics_upd

8/9/2019 12_Antilipemics_upd

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Antilipemic Agents Antilipemic Agents


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Antihyperlipedemic Drugs Antihyperlipedemic DrugsDrugs used to lower lipid levelsDrugs used to lower lipid levels


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Hyperlipedemia

Hyperlipedemia

Abn ormal elevatio n of cholesterolAbn ormal elevatio n of cholesterola n d triglycerides i n the b looda n d triglycerides i n the b lood

A primary cause of atherosclerosisA primary cause of atherosclerosis


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Atherosclerosis AtherosclerosisCharacterized b y accumulatio n of Characterized b y accumulatio n of fatty deposits o n the i nn er walls of fatty deposits o n the i nn er walls of

arteries a n d arterioles throughoutarteries a n d arterioles throughoutthe b ody that reduces the b loodthe b ody that reduces the b loodsupply to vital orga n s resulti n g tosupply to vital orga n s resulti n g tostrokes, a n gi n a pectoris , myocardialstrokes, a n gi n a pectoris , myocardial

in farctio n a n d peripheral vascularin farctio n a n d peripheral vasculardiseasedisease


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Triglycerides and Cholesterol

Triglycerides and Cholesterol

Two primary forms of lipids i n theTwo primary forms of lipids i n theb loodb lood

WaterWater- -i n solu b le fats that must b ein solu b le fats that must b eb ou n d to apoprotei n s, specializedb ou n d to apoprotei n s, specializedlipidlipid--carryi n g protei n scarryi n g protei n sLipoprotei n is the the com b in atio n of Lipoprotei n is the the com b in atio n of triglyceride or cholesterol withtriglyceride or cholesterol withapoprotei napoprotei n


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Types of Lipoproteins

Types of Lipoproteins

LipidLipid Protei nProtei n Con te n tCon te n tLipoprotei n Classificatio nLipoprotei n Classificatio n Con te n tCon te n t

MostMost chylomicro nchylomicro n LeastLeast

veryvery- -low de n sity lipoprotei n low de n sity lipoprotei n (VLDL)(VLDL)

In termediateIn termediate- -de n sity lipoprotei nde n sity lipoprotei n(IDL)(IDL)

LeastLeast HighHigh--de n sity lipoprotei n (HDL)de n sity lipoprotei n (HDL) MostMost


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Hyperlipidemia is a major risk factorHyperlipidemia is a major risk factorfor atherosclerosis.for atherosclerosis.

Most of the evide n ce specificallyMost of the evide n ce specificallyimplicatesimplicates hypercholesterolemiahypercholesterolemia ..Elevated levels of serum cholesterolElevated levels of serum cholesterolare sufficie n t to stimulate lesio n are sufficie n t to stimulate lesio n developme n t.developme n t.


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CoronaryH

eart DiseaseCoronaryH

eart DiseaseThe risk of CHD i n patie n ts withThe risk of CHD i n patie n ts withcholesterol levels of 300 mg/dL is 3cholesterol levels of 300 mg/dL is 3

to 4 times greater than

that in

to 4 times greater than

that in

patie n ts with levels less tha n patie n ts with levels less tha n 300 mg/dL300 mg/dL


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Antilipemics AntilipemicsBile acid sequestra n tsBile acid sequestra n tsHMGHMG-- Co A reductase i n hi b itorsCo A reductase i n hi b itors

(HMGs or stati n s)(HMGs or stati n s)Fib ric acid derivativesFib ric acid derivativesNiaci n ( n icoti n ic acid)Niaci n ( n icoti n ic acid)


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Antilipemics: Bile Acid Antilipemics: Bile Acid

SequestrantsSequestrantscholestyrami n e (Questra n )cholestyrami n e (Questra n )colestipol hydrochloride ( Colestid)colestipol hydrochloride ( Colestid)

Also called b ile acidAlso called b ile acid- - b in di n g resi n sb in di n g resi n sa n da n dio nio n --excha n ge resi n sexcha n ge resi n s


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SequestrantsSequestrantsMecha n ism of Actio nMecha n ism of Actio n

Preve n t resorptio n of b ile acids from smallPreve n t resorptio n of b ile acids from smallin testi n ein testi n eBile acids are n ecessary for a b sorptio n Bile acids are n ecessary for a b sorptio n of cholesterolof cholesterol


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SequestrantsSequestrantsTherapeutic UsesTherapeutic Uses

hyperlipoprotei n emiahyperlipoprotei n emia

Relief of Relief of prurituspruritus associated with partialassociated with partialb iliaryb iliary o b structio n (ob structio n (cholestyrami n echolestyrami n e))


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SequestrantsSequestrantsS ide EffectsS ide Effects

Co n stipatio nCo n stipatio n

Heart b ur n , n ausea, b loati n gHeart b ur n , n ausea, b loati n g

These adverse effects te n d to disappearThese adverse effects te n d to disappearover timeover time


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Antilipemics: HMG Antilipemics: HMG- -CoA ReductaseCoA Reductase

Inhibitors (HMG

s or statins)Inhibitors (HMG

s or statins)lovastati n (Mevacor)lovastati n (Mevacor)pravastati n (Pravachol)pravastati n (Pravachol)

simvastati n (Zocor)simvastati n (Zocor)atorvastati n (Lipitor)atorvastati n (Lipitor)cerivastati n ( Baycol)cerivastati n ( Baycol)fluvastati n (Lescol)fluvastati n (Lescol)Most pote n t LDL reducersMost pote n t LDL reducers


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Antilipemics: Antilipemics:HMGHMG- -

CoA Reductase InhibitorsCoA Reductase InhibitorsMecha n ism of Actio nMecha n ism of Actio n

In hi b it HMGIn hi b it HMG-- CoA reductase, which is usedCoA reductase, which is usedb y the liver to produce cholesterolb y the liver to produce cholesterolLower the rate of cholesterol productio nLower the rate of cholesterol productio n


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Antilipemics: Antilipemics:HMGHMG- -CoA Reductase InhibitorsCoA Reductase Inhibitors

Therapeutic UsesTherapeutic UsesTreatme n t of Treatme n t of hyperlipidemiashyperlipidemias Reduce LDL levels b y 30 to 40%Reduce LDL levels b y 30 to 40% In crease HDL levels b y 2 to 15%In crease HDL levels b y 2 to 15% Reduce triglycerides b y 10 to 30%Reduce triglycerides b y 10 to 30%


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Antilipemics: Antilipemics:HMGHMG- -CoA Reductase InhibitorsCoA Reductase Inhibitors

S ide EffectsS ide EffectsMild, tra n sie n t GI distur b a n cesMild, tra n sie n t GI distur b a n ces

RashRashHeadacheHeadacheMyopathy (muscle pai n )Myopathy (muscle pai n )Elevatio n s i n liver e n zymesElevatio n s i n liver e n zymes


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Antilipemics: Fibric Acid Antilipemics: Fibric AcidDerivativesDerivatives

clofi b rateclofi b rategemfi b rozil (Lopid)gemfi b rozil (Lopid)

fe n ofi b rate ( Tricor)fe n ofi b rate ( Tricor)


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Antilipemics Antilipemics: : FibricFibric Acid AcidDerivativesDerivatives

Therapeutic UsesTherapeutic UsesTreatme n t of Treatme n t of hyperlipemiashyperlipemias

Treatme n t of Treatme n t of hyperlipidemiashyperlipidemias

Decrease the triglyceride levels a n d i n creaseDecrease the triglyceride levels a n d i n creaseHDL b y as much as 25%HDL b y as much as 25%


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Antilipemics: Fibric Acid Antilipemics: Fibric AcidDerivativesDerivatives

S ide EffectsS ide EffectsAb domi n al discomfortAb domi n al discomfort

DiarrheaDiarrheaNauseaNauseaBlurred visio nBlurred visio nIn creased risk of gallsto n esIn creased risk of gallsto n esProlo n ged prothrom b in timeProlo n ged prothrom b in timeLiver studies may show i n creasedLiver studies may show i n creasedfu n ctio nfu n ctio n


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Antilipemics: Niacin (Nicotinic Antilipemics: Niacin (Nicotinic Acid) Acid)

Vitami n BVitami n B33LipidLipid--loweri n g properties requireloweri n g properties require

much higher doses tha n whe n usedmuch higher doses tha n whe n usedas a vitami nas a vitami nEffective, i n expe n sive, ofte n used i n Effective, i n expe n sive, ofte n used i n com b in atio n with other lipidcom b in atio n with other lipid- -loweri n gloweri n gage n tsage n ts


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TriacylglycerolTriacylglycerol((--) Niaci n) Niaci n

Adipose TissueAdipose TissueFatty AcidsFatty Acids

LiverLiverFatty AcidsFatty Acids

TriacylglycerolTriacylglycerol

VLDLVLDL


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Antilipemics: Niacin (Nicotinic Acid) Antilipemics: Niacin (Nicotinic Acid)

Mecha n ism of Actio nMecha n ism of Actio nThought to i n crease activity of lipase, whichThought to i n crease activity of lipase, whichb reaks dow n lipidsb reaks dow n lipidsReduces the meta b olism or cata b olism of Reduces the meta b olism or cata b olism of cholesterol a n d triglyceridescholesterol a n d triglyceridesIn hi b it lipolysis i n the adipose tissue,resulti n gIn hi b it lipolysis i n the adipose tissue,resulti n g

in decreased hepatic VLDL sy n thesis.in decreased hepatic VLDL sy n thesis.


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Therapeutic UsesTherapeutic UsesEffective i n loweri n g triglyceride, totalEffective i n loweri n g triglyceride, totalserum cholesterol, a n d LDL levelsserum cholesterol, a n d LDL levelsIn creases HDL levelsIn creases HDL levelsEffective i n the treatme n t of Effective i n the treatme n t of hyperlipidemiashyperlipidemias


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S ide EffectsS ide EffectsFlushi n g (due to histami n e release)Flushi n g (due to histami n e release)

PruritusPruritusGI distressGI distress


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Antilipemics: Nursing Antilipemics: NursingImplicationsImplications

Before b egi nn in g therapy, o b tai n aBefore b egi nn in g therapy, o b tai n athorough health a n d medicatio n thorough health a n d medicatio n history.history.Assess dietary patter n s, exerciseAssess dietary patter n s, exerciselevel, weight, height, V S , to b accolevel, weight, height, V S , to b accoa n d alcohola n d alcohol

use, family history.use, family history.Assess for co n trai n dicatio n s,Assess for co n trai n dicatio n s,co n ditio n s that require cautious use,co n ditio n s that require cautious use,

a n d drug i n teractio n s.a n d drug i n teractio n s.


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Co n trai n dicatio n s i n clude b iliaryCo n trai n dicatio n s i n clude b iliaryo b structio n , liver dysfu n ctio n , activeo b structio n , liver dysfu n ctio n , activeliver disease.liver disease.Ob tai n b aseli n e liver fu n ctio n Ob tai n b aseli n e liver fu n ctio n studies.studies.Patie n ts o n lo n gPatie n ts o n lo n g--term therapy mayterm therapy mayn eed suppleme n tal fatn eed suppleme n tal fat- -solu b lesolu b levitami n s ( A, D, K).vitami n s ( A, D, K).Take with meals to decrease GITake with meals to decrease GI

upset.upset.


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Clofi b rate ofte n causes co n stipatio n; Clofi b rate ofte n causes co n stipatio n; in struct patie n ts to i n crease fi b er a n din struct patie n ts to i n crease fi b er a n dfluid i n take to offset this effect.fluid i n take to offset this effect.To mi n imize side effects of n iaci n , startTo mi n imize side effects of n iaci n , starto n low i n itial dose a n d gradually i n creaseo n low i n itial dose a n d gradually i n creaseit,it,

a n d take with meals.a n d take with meals.S mall doses of aspiri n or N S AIDs may b eS mall doses of aspiri n or N S AIDs may b etake n 30 mi n utes b efore n iaci n totake n 30 mi n utes b efore n iaci n to

mi n imize cuta n eous flushi n g.mi n imize cuta n eous flushi n g.


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In form patie n ts that these age n tsIn form patie n ts that these age n tsmay take several weeks to showmay take several weeks to showeffective n ess.effective n ess.In struct patie n ts to report persiste n tIn struct patie n ts to report persiste n tGI upset, co n stipatio n , a bn ormal orGI upset, co n stipatio n , a bn ormal oru n usual b leedi n g, a n d yellowu n usual b leedi n g, a n d yellow

discoloratio n of the ski n .discoloratio n of the ski n .


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Mon itor for side effects, i n cludi n gMon itor for side effects, i n cludi n gin creased liver e n zyme studies.in creased liver e n zyme studies.

Mon itor for therapeutic effects:Mon itor for therapeutic effects: Reduced cholesterol a n d triglycerideReduced cholesterol a n d triglyceridelevelslevels

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