Lovastatin: Difference between revisions

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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"/>
<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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* 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 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 />
* 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. Fluvastatin 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===
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<div style="height:100%; width: 100%">
{{:Statin Pharmacokinetics}}
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===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/>
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Latest revision as of 15:43, 10 January 2024

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]

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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