This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.

Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.


Lovastatin

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
<applet load="" size="480" color="" frame="true" spin="on" Scene ="Lovastatin/Lovastatin/1" align="right" caption="Lovastatin, also known as Mevacor"/>
+
<applet load="" size="[450,380]" color="" frame="true" spin="on" Scene ="Lovastatin/Lovastatin/1" align="right" caption="Lovastatin, also known as Mevacor"/>
===Better Known as: Mevacor===
===Better Known as: Mevacor===
* Marketed By: Merck & Co. <br />
* Marketed By: Merck & Co. <br />
Line 13: Line 13:
===Pharmacokinetics===
===Pharmacokinetics===
-
{| class="wikitable" border="1" width="48%" style="text-align:center"
+
<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%">
-
|-
+
<tr>
-
! colspan="7" align="center"| Statin [[Pharmacokinetics]] at 10mg Dosage.<ref>PMID:11907637</ref><ref>PMID:15198967</ref><ref>PMID:12686673</ref><ref>PMID:18176327</ref><ref>PMID: 17452418</ref><ref>PMID:12895195</ref>
+
<td style="width:100%; vertical-align:top;border-width:0px; border-style:inset">
-
|-
+
<div style="height:100%; width: 100%">
-
! Parameter
+
{{:Statin Pharmacokinetics}}
-
! [[Atorvastatin]] (Lipitor)
+
</div>
-
! [[Fluvastatin]] (Lescol)
+
</td>
-
! [[Lovastatin]] (Mevacor)
+
</tr>
-
! [[Simvastatin]] (Zocor)
+
</table>
-
! [[Rosuvastatin]] (Crestor)
+
-
! [[Cerivastatin]] (Baycol)
+
-
|-
+
-
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
+
-
! 2.5
+
-
! 1
+
-
! 3
+
-
! 1.5
+
-
! 4
+
-
! 1.5
+
-
|-
+
-
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
+
-
! 27-66
+
-
! 448
+
-
! 10-20
+
-
! 7.3
+
-
! 4.34
+
-
! 3.43
+
-
|-
+
-
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
+
-
! 12
+
-
! 19-29
+
-
! 5
+
-
! 5
+
-
! 20
+
-
! 60
+
-
|-
+
-
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
+
-
! 80-90
+
-
! 99
+
-
! 95
+
-
! 95
+
-
! 88
+
-
! 99
+
-
|-
+
-
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
+
-
! 15-30
+
-
! 2
+
-
! 3
+
-
! 2.7
+
-
! 19
+
-
! 2.2
+
-
|-
+
-
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
+
-
! 104
+
-
! ~150
+
-
! 33
+
-
! 125
+
-
! 48
+
-
! 14.5
+
-
|-
+
-
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
+
-
! 154
+
-
! 198
+
-
! 800-4200
+
-
! 66
+
-
! 320
+
-
! 50-90
+
-
|-
+
-
! 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
+
-
! Hepatic <br />(CYP2C8)
+
-
|}
+
===References===
===References===

Revision as of 08:58, 10 December 2010

Lovastatin, also known as Mevacor

Drag the structure with the mouse to rotate

Better Known as: Mevacor

  • Marketed By: Merck & Co.
  • Major Indication: Hyperlipidemia & High Cholesterol (Hypercholesterolemia)
  • Drug Class: HMGR Inhibitor or Statin
  • Date of FDA Approval (Patent Expiration): 1991 (2001)
  • 2000 Sales: $520 Million
  • Importance: Was the first HMG-CoA Inhibitor. Statins are so ubiquitous, doctors have even suggested handing them out with fast food. See: the article
  • See Pharmaceutical Drugs for more information about other drugs and disorders

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.[1]

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

Retrieved from "http://52.214.119.220/wiki/index.php/Lovastatin"
Personal tools