Fluvastatin

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{| class="wikitable" border="1" width="48%" style="text-align:center"
{| class="wikitable" border="1" width="48%" style="text-align:center"
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|-
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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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! colspan="7" align="center"| Statin [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|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>
|-
|-
! Parameter
! Parameter
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! [[Simvastatin]] (Zocor)
! [[Simvastatin]] (Zocor)
! [[Rosuvastatin]] (Crestor)
! [[Rosuvastatin]] (Crestor)
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! [[Cerivastatin]] (Baycol)
|-
|-
! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)
! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)
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! 1.5
! 1.5
! 4
! 4
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! 1.5
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! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)
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! 10-20
! 10-20
! 7.3
! 7.3
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!4.34
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! 4.34
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! 3.43
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|-
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
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! 5
! 5
! 20
! 20
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! 60
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! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
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! 95
! 88
! 88
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! 99
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! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
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! 2.7
! 2.7
! 19
! 19
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! 2.2
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! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
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! 125
! 125
! 48
! 48
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! 14.5
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! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
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! 66
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! 50-90
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! Equivalent LDL Reduction Dosage (mg)
! Equivalent LDL Reduction Dosage (mg)
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! 20
! 20
! 5
! 5
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! --
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! Metabolism
! Metabolism
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! Hepatic <br/>(CYP3A4)
! Hepatic <br/>(CYP3A4)
! Not <br/>Metabolized
! Not <br/>Metabolized
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! Hepatic <br />(CYP2C8)
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|}
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===References===
===References===
<references/>
<references/>
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Revision as of 18:25, 29 November 2010

Fluvastatin, also known as Lescol

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Better Known as: Lescol

  • Marketed By: Novartis
  • Major Indication: Hyperlipidemia & High Cholesterol (Hypercholesterolemia)
  • Drug Class: HMGR Inhibitor or Statin
  • Date of FDA Approval (Patent Expiration): 1993 (2011)
  • 2000 Sales: $430 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: the article
  • The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information

Mechanism of Action

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.[1]

Pharmacokinetics

Statin Pharmacokinetics at 10mg Dosage.[2][3][4][5][6][7]
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) 154 198 800-4200 66 320 50-90
Equivalent LDL Reduction Dosage (mg) 10 -- 80 20 5 --
Metabolism Hepatic
(CYP3A4) 		Hepatic
(CYP2C9) 		Hepatic
(CYP3A4) 		Hepatic
(CYP3A4) 		Not
Metabolized 		Hepatic
(CYP2C8)

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
  2. ↑ Park JW, Siekmeier R, Lattke P, Merz M, Mix C, Schuler S, Jaross W. Pharmacokinetics and pharmacodynamics of fluvastatin in heart transplant recipients taking cyclosporine A. J Cardiovasc Pharmacol Ther. 2001 Oct;6(4):351-61. PMID:11907637
  3. ↑ Bellosta S, Paoletti R, Corsini A. Safety of statins: focus on clinical pharmacokinetics and drug interactions. Circulation. 2004 Jun 15;109(23 Suppl 1):III50-7. PMID:15198967 doi:10.1161/01.CIR.0000131519.15067.1f
  4. ↑ Lins RL, Matthys KE, Verpooten GA, Peeters PC, Dratwa M, Stolear JC, Lameire NH. Pharmacokinetics of atorvastatin and its metabolites after single and multiple dosing in hypercholesterolaemic haemodialysis patients. Nephrol Dial Transplant. 2003 May;18(5):967-76. PMID:12686673
  5. ↑ Kiser JJ, Gerber JG, Predhomme JA, Wolfe P, Flynn DM, Hoody DW. Drug/Drug interaction between lopinavir/ritonavir and rosuvastatin in healthy volunteers. J Acquir Immune Defic Syndr. 2008 Apr 15;47(5):570-8. PMID:18176327 doi:10.1097/QAI.0b013e318160a542
  6. ↑ Li P, Callery PS, Gan LS, Balani SK. Esterase inhibition by grapefruit juice flavonoids leading to a new drug interaction. Drug Metab Dispos. 2007 Jul;35(7):1203-8. Epub 2007 Apr 23. PMID:17452418 doi:10.1124/dmd.106.013904
  7. ↑ Renders L, Haas CS, Liebelt J, Oberbarnscheidt M, Schocklmann HO, Kunzendorf U. Tacrolimus and cerivastatin pharmacokinetics and adverse effects after single and multiple dosing with cerivastatin in renal transplant recipients. Br J Clin Pharmacol. 2003 Aug;56(2):214-9. PMID:12895195


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David Canner, Alexander Berchansky

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