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Lovastatin

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Current revision (12:43, 10 January 2024) (edit) (undo)
 
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<applet load="" size="[450,380]" color="" frame="true" spin="on" Scene ="Lovastatin/Lovastatin/1" align="right" caption="Lovastatin, also known as Mevacor"/>
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<StructureSection load='' size='340' side='right' caption='Lovastatin, also known as Mevacor' scene='Lovastatin/Lovastatin/1'>
===Better Known as: Mevacor===
===Better Known as: Mevacor===
* Marketed By: Merck & Co. <br />
* Marketed By: Merck & Co. <br />
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===Mechanism of Action===
===Mechanism of Action===
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>
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===
<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%">
<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%">

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


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