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Lovastatin

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<applet load="" size="480" color="" frame="true" spin="on" Scene ="Fluvastatin/Fluvastatin/1" align="right" caption="Fluvastatin, also known as Lescol"/>
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<StructureSection load='' size='340' side='right' caption='Lovastatin, also known as Mevacor' scene='Lovastatin/Lovastatin/1'>
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===Better Known as: Lescol===
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===Better Known as: Mevacor===
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* Marketed By: Novartis <br />
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* Marketed By: Merck & Co. <br />
* Major Indication: Hyperlipidemia & High Cholesterol ([[Metabolic Disorders|Hypercholesterolemia]])<br />
* Major Indication: Hyperlipidemia & High Cholesterol ([[Metabolic Disorders|Hypercholesterolemia]])<br />
* Drug Class: [[HMGR]] Inhibitor or Statin
* Drug Class: [[HMGR]] Inhibitor or Statin
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* Date of FDA Approval (Patent Expiration): 1993 (2011)<br />
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* Date of FDA Approval (Patent Expiration): 1991 (2001)<br />
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* 2000 Sales: $430 Million
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* 2000 Sales: $520 Million
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* Why You Should Care: Was largely replaced by [[Lipitor]]. Statins are so ubiquitous, doctors have even suggested handing them out with fast food. See: [http://www.bbc.co.uk/news/health-10955522 the article] <br />
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* Importance: Was the first HMG-CoA Inhibitor. Statins are so ubiquitous, doctors have even suggested handing them out with fast food. See: [http://www.bbc.co.uk/news/health-10955522 the article] <br />
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* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information
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* See [[Pharmaceutical Drugs]] for more information about other drugs and disorders
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===Mechanism of Action===
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Fluvastatin is an inhibitor of [[HMG-CoA Reductase]] (HMGR), a highly regulated enzyme responsible for the committed step in cholesterol synthesis. Fluvastatin outcompetes HMG-CoA, the substrate of HMGR, in binding to HMGR.<ref>PMID:7784310</ref>
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===Mechanism of Action===
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Lovastatin is rapidly hydrolyzed in vivo into its corresponding b-hydroxyacid, which is an inhibitor of [[HMG-CoA Reductase]] (HMGR), a highly regulated enzyme responsible for the committed step in cholesterol synthesis. Lovastatin outcompetes HMG-CoA, the substrate of HMGR, in binding to HMGR.<ref>PMID:7784310</ref>
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</StructureSection>
===Pharmacokinetics===
===Pharmacokinetics===
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{| class="wikitable" border="1" width="48%" style="text-align:center"
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<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%">
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|-
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<tr>
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! colspan="6" align="center"| Statin [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]] at 10mg Dosage. <ref>PMID:15198967</ref><ref>PMID:12686673</ref><ref>PMID:18176327</ref><ref>PMID: 17452418</ref><ref>PMID: 11907637</ref>
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<td style="width:100%; vertical-align:top;border-width:0px; border-style:inset">
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|-
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<div style="height:100%; width: 100%">
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! Parameter
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{{:Statin Pharmacokinetics}}
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! [[Atorvastatin]] (Lipitor)
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</div>
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! [[Fluvastatin]] (Lescol)
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</td>
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! [[Lovastatin]] (Mevacor)
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</tr>
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! [[Simvastatin]] (Zocor)
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</table>
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! [[Rosuvastatin]] (Crestor)
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|-
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! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)
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! 2.5
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! 1
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! 3
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! 1.5
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! 4
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|-
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! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)
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! 27-66
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! 448
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! 10-20
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! 7.3
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!4.34
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|-
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! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
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! 12
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! 19-29
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! 5
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! 5
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! 20
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|-
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! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
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! 80-90
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! 99
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! 95
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! 95
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! 88
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|-
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! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
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! 15-30
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! 2
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! 3
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! 2.7
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! 19
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|-
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! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
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! 104
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! ~150
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! 33
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! 125
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! 48
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|-
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! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
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! 154
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! 198
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! 800-4200
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! 66
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! 320
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|-
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! Equivalent LDL Reduction Dosage (mg)
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! 10
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! --
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! 80
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! 20
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! 5
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|-
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! Metabolism
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! Hepatic <br/>(CYP3A4)
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! Hepatic <br/>(CYP2C9)
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! Hepatic <br/>(CYP3A4)
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! Hepatic <br/>(CYP3A4)
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! Not <br/>Metabolized
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|}
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===References===
===References===
<references/>
<references/>
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Current revision

Lovastatin, also known as Mevacor

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Pharmacokinetics

Statin Pharmacokinetics at 10mg Dosage
Parameter Atorvastatin (Lipitor) Fluvastatin (Lescol) Lovastatin (Mevacor) Simvastatin (Zocor) Rosuvastatin (Crestor) Cerivastatin (Baycol)
Tmax (hr) 2.5 1 3 1.5 4 1.5
Cmax (ng/ml) 27-66 448 10-20 7.3 4.34 3.43
Bioavailability (%) 12 19-29 5 5 20 60
Protein Binding (%) 80-90 99 95 95 88 99
T1/2 (hr) 15-30 2 3 2.7 19 2.2
AUC (ng/ml/hr) 104 ~150 33 125 48 14.5
IC50 (nM) 154 198 800 66 320 50-90
Equivalent LDL Reduction Dosage (mg) 10 -- 80 20 5 --
Metabolism Hepatic
(CYP3A4) 		Hepatic
(CYP2C9) 		Hepatic
(CYP3A4) 		Hepatic
(CYP3A4) 		None Hepatic
(CYP2C8)

For References, See References

References

  1. ↑ Corsini A, Maggi FM, Catapano AL. Pharmacology of competitive inhibitors of HMG-CoA reductase. Pharmacol Res. 1995 Jan;31(1):9-27. PMID:7784310


Proteopedia Page Contributors and Editors (what is this?)

David Canner, Alexander Berchansky

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