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JOVY SKARSTEIN

GENERIC NAME MECHANISM OFACTION

INDICATIONS CONTRAINDICATION SIDE EFFECT HEALTHTEACHING

SIMVASTATIN

BRAND NAME:

ZOCOR

DOSAGE:

For Heterozygousfamilialhypercholesterolemia:

Children less than10 years:

5 mg once daily inthe eveningincreasing to 10 mgonce daily after 4weeks and to 20 mgonce daily after 8

weeks as tolerated.Children greater thanor equal to 10 years:10 mg once daily inthe eveningincreasing to 20 mg

-Simvastatins act

bycompetitivelyinhibitingHMG-CoA reductase,thefirst committedenzyme of theHMG-CoAreductase pathway.Because statinsare similar to HMG-CoA on amolecular level,

they take the placeof HMG-CoA in theenzyme andreduce the rate bywhich it is able toproducemevalonate,thenext molecule inthecascade thateventually

producescholesterol,as wellas a number ofother compounds.This ultimatelyreduces cholesterol

-Simvastatin is

indicated for thetreatment ofhypercholesterolemia.Simvastatin isindicated togetherwith lifestyle changes(diet, weight-loss,exercise) to reducethe amount ofcholesterol (a fat-likesubstance) and

certain other fattysubstances in yourblood. Simvastatin isin a class ofprescriptions calledHMG-CoA reductaseinhibitors (statins). Itworks by slowing theproduction ofcholesterol in the

body.

Buildup of cholesteroland fats along thewalls of your arteries(a process known as

-Hypersensitivity to

any component ofSimvastatin.-Active liver disease orunexplained persistentelevations of serumtransaminases

-Simvastatin

side effects thatyou shouldreport to yourhealth careprofessional ordoctor as soonas possible:- constipation;- difficultybreathing orswallowing;

- extremetiredness;- fever;- flu-likesymptoms;- hives;- hoarseness;- itching;- lack of energy;- loss of

appetite;- muscle pain,tenderness, orweakness;- nausea;- pain in the

-Instruct patient

to takemedication asdirected, not toskip doses ordouble up onmissed doses.

Advise patient toavoid drinkingmore than 1 qt ofgrapefruit

juice/day during

therapy.Medication helpscontrol but doesnot cure elevatedserumcholesterollevels.

-Advise patientthat this

medicationshould be usedin conjunctionwith dietrestrictions (fat,cholesterol,

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once daily after 6weeks and to 40 mgonce daily after 12weeks as tolerated.

10 to 17 years:

Initial dose: 10 mgorally once a day inthe evening.Maintenance dose: 10to 40 mg/day (themaximumrecommended dose is40 mg/day). Dosageincreases should bedone at intervals of 4weeks or more. UsualAdult Dose ofSimvastatin forHyperlipidemia:

Initial dose: 10 to 20mg orally once a dayin the evening.

Maintenance dose: 5to 40 mg orally once aday in the evening.

For patients at highrisk for a CHD event

via severalmechanisms.

Inhibitingcholesterol

synthesis

By inhibiting HMG-CoA reductase,statins block thepathway forsynthesizingcholesterol in theliver. This issignificant becausemost circulatingcholesterol comesfrom internalmanufacture ratherthan the diet. Whenthe liver can nolonger producecholesterol, levelsof cholesterol in theblood will fall.Cholesterol

synthesis appearsto occur mostly atnight,[47]so statinswith shorthalf-livesare usually taken atnight to maximize

atherosclerosis)decreases blood flowand, therefore, theoxygen supply to yourheart, brain, and other

parts of your body.Lowering your bloodlevel of cholesteroland fats may help todecrease yourchances of gettingheart disease, angina(chest pain), strokes,and heart attacks. Inaddition to taking acholesterol-loweringprescription, makingcertain changes inyour daily habits canalso lower yourcholesterol bloodlevels. You should eata diet that is low insaturated fat andcholesterol (seeSPECIAL DIETARY),

exercise 30 minuteson most, if not alldays, and lose weightif you are overweight.

A derivative of

upper right partof the stomach;- rash;- swelling of theface, throat,

tongue, lips,eyes, hands,feet, ankles, orlower legs;- unusualbleeding orbruising;- yellowing ofthe skin oreyes;

carbohydrates,alcohol),exercise, andcessation ofsmoking.

-Instruct patientto notify healthcare professionalif unexplainedmuscle pain,tenderness, orweaknessoccurs,especially ifaccompanied byfever or malaise.

-Advise patient towear sunscreenand protectiveclothing topreventphotosensitivityreactions (rare).

-Instruct patientto notify healthcare professionalof all Rx or OTCmedications,vitamins, or

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due to existing CHD,diabetes, peripheralvessel disease,history of stroke orother cerebrovascular

disease, therecommendedstarting dose is 40 mgorally once a day.

Usual Adult Dosefor CardiovascularRisk Reduction:

Initial dose: 10 to 20mg orally once a dayin the evening.Maintenance dose: 5to 40 mg orally once aday in the evening.

For patients at highrisk for a CHD eventdue to existing CHD,diabetes, peripheralvessel disease,

history of stroke orother cerebrovasculardisease, therecommendedstarting dose is 40 mgorally once a day.

their effect. Studieshave showngreater LDL andtotal cholesterolreductions in the

short-actingsimvastatin takenat night rather thanthe morning,[48][49]but have shown nodifference in thelong-actingatorvastatin.[50]

Increasing LDLuptakeIn rabbits,hepatocytes (livercells) sense thereduced levels ofliver cholesteroland seek tocompensate bysynthesizingLDLreceptors to drawcholesterol out of

the circulation.

[51]

This isaccomplished viaprotease enzymesthat cleave aprotein called

lovastatin and potentcompetitive inhibitor of3-hydroxy-3-methylglutarylcoenzyme A

reductase(hydroxymethylglutarylCOA reductases),which is the rate-limiting enzyme incholesterolbiosynthesis. It mayalso interfere withsteroid hormoneproduction. Due to theinduction of hepaticLDL receptors, itincreases breakdownof LDL cholesterol.

herbal productsbeing taken andconsult healthcare professionalbefore taking any

new medications.

-Advise patient tonotify health careprofessional ofmedicationregimen beforetreatment orsurgery.

-Instruct femalepatients to notifyhealth careprofessionalpromptly ifpregnancy isplanned orsuspected.

Emphasize theimportance of

follow-up examsto determineeffectiveness andto monitor forside effects.

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"membrane-boundsterol regulatoryelement bindingprotein", whichmigrates to the

nucleus andcauses increasedproduction ofvarious otherproteins andenzymes, includingtheLDL receptor.The LDL receptorthen relocates tothe livercellmembrane andbinds to passingLDL andVLDLparticles (the "badcholesterol" linkedto disease). LDLand VLDL aredrawn out ofcirculation into theliver, where thecholesterol is

reprocessed intobile salts. Theseare excreted, andsubsequentlyrecycled mostly byan internal bile salt

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circulation.

Other effectsSimvastatin exhibitaction beyond lipid-

lowering activity inthe prevention ofatherosclerosis.TheASTEROIDtrial showed directultrasoundevidence ofatheromaregression duringstatin therapy.[52]Researchershypothesize thatstatins preventcardiovasculardisease via fourproposedmechanisms (allsubjects of a largebody of biomedicalresearch):[53]

1. Improveendothelialfunction

2. Modulateinflammatoryresponses

http://en.wikipedia.org/wiki/Atherosclerosishttp://en.wikipedia.org/wiki/ASTEROID_trialhttp://en.wikipedia.org/wiki/ASTEROID_trialhttp://en.wikipedia.org/wiki/Intravascular_ultrasoundhttp://en.wikipedia.org/wiki/Atheromahttp://en.wikipedia.org/wiki/Statin#cite_note-Nissen2006-52http://en.wikipedia.org/wiki/Statin#cite_note-Nissen2006-52http://en.wikipedia.org/wiki/Statin#cite_note-Nissen2006-52http://en.wikipedia.org/wiki/Cardiovascular_diseasehttp://en.wikipedia.org/wiki/Cardiovascular_diseasehttp://en.wikipedia.org/wiki/Statin#cite_note-Furberg-53http://en.wikipedia.org/wiki/Statin#cite_note-Furberg-53http://en.wikipedia.org/wiki/Statin#cite_note-Furberg-53http://en.wikipedia.org/wiki/Endotheliumhttp://en.wikipedia.org/wiki/Inflammationhttp://en.wikipedia.org/wiki/Inflammationhttp://en.wikipedia.org/wiki/Endotheliumhttp://en.wikipedia.org/wiki/Statin#cite_note-Furberg-53http://en.wikipedia.org/wiki/Cardiovascular_diseasehttp://en.wikipedia.org/wiki/Cardiovascular_diseasehttp://en.wikipedia.org/wiki/Statin#cite_note-Nissen2006-52http://en.wikipedia.org/wiki/Atheromahttp://en.wikipedia.org/wiki/Intravascular_ultrasoundhttp://en.wikipedia.org/wiki/ASTEROID_trialhttp://en.wikipedia.org/wiki/ASTEROID_trialhttp://en.wikipedia.org/wiki/Atherosclerosis

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3. Maintainplaquestability

4. Preventthrombus

formation

Statins may evenbenefit thosewithout highcholesterol. In2008, the JUPITERstudy showedfewer strokes,heart attacks, andsurgeries even for

patients who hadno history ofhighcholesterol or heartdisease, but onlyelevatedC-reactiveprotein levels.There were also20% fewer deaths(mainly fromreduction in cancer

deaths) thoughdeaths fromcardiovascularcauses were notreduced.

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