Proteopedia

Lovastatin: Difference between revisions

← Older edit
David Canner (talk | contribs)
7,699 edits
No edit summary
No edit summary
 
(6 intermediate revisions by one other user not shown)
Line 1: Line 1:
<applet  load="" size="480" color="" frame="true"  spin="on" Scene ="Fluvastatin/Fluvastatin/1" align="right" caption="Fluvastatin, also known as Lescol"/>
<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 />
Line 6: Line 6:
* Date of FDA Approval (Patent Expiration): 1991 (2001)<br />
* Date of FDA Approval (Patent Expiration): 1991 (2001)<br />
* 2000 Sales: $520 Million
* 2000 Sales: $520 Million
* Why You Should Care: 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 />
* 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 />
* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information
* See [[Pharmaceutical Drugs]] for more information about other drugs and disorders
 
===Mechanism of Action===
===Mechanism of Action===
Lovastatin 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>
</StructureSection>
===Pharmacokinetics===
<table style="background: cellspacing="0px"  align="" cellpadding="0px" width="42%">
<tr>
<td style="width:100%; vertical-align:top;border-width:0px; border-style:inset">
<div style="height:100%; width: 100%">
{{:Statin Pharmacokinetics}}
</div>
</td>
</tr>
</table>


===Pharmacokinetics===
{| class="wikitable" border="1" width="48%" style="text-align:center"
|-
!  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>
|-
! Parameter
! [[Atorvastatin]] (Lipitor)
! [[Fluvastatin]] (Lescol)
! [[Lovastatin]] (Mevacor)
! [[Simvastatin]] (Zocor)
! [[Rosuvastatin]] (Crestor)
|-
! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)
! 2.5
! 1
! 3
! 1.5
! 4
|-
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)
! 27-66
! 448
! 10-20
! 7.3
!4.34
|-
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
! 12
! 19-29
! 5
! 5
! 20
|-
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
! 80-90
! 99
! 95
! 95
! 88
|-
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! 15-30
! 2
! 3
! 2.7
! 19
|-
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! 104
! ~150
! 33
! 125
! 48
|-
! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
! 154
! 198
! 800-4200
! 66
! 320
|-
! Equivalent LDL Reduction Dosage (mg)
! 10
! --
! 80
! 20
! 5
|-
! Metabolism
! Hepatic <br/>(CYP3A4)
! Hepatic <br/>(CYP2C9)
! Hepatic <br/>(CYP3A4)
! Hepatic <br/>(CYP3A4)
! Not <br/>Metabolized
|}
===References===
===References===
<references/>
<references/>
__NOEDITSECTION__
__NOEDITSECTION__
__NOTOC__
__NOTOC__

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

David Canner, Alexander Berchansky
Retrieved from "https://proteopedia.openfox.io/w/Lovastatin"