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QuickView for Cerivastatin (compound)

Name: cerivastatin
PubChem Compound ID: 10600867
Molecular formula: C26H34FNO5
Molecular weight: 461.543 g/mol
Name: cerivastatin
Name (isomeric): DB00439
Drug Type: small molecule
Cerivastatin sodium; Cerivastatin, sodium salt
Brand: Baycol, Rivastatin, Lipobay
Category: Antilipemic Agents, Anticholesteremic Agents, Hydroxymethylglutaryl-CoA Reductase Inhibitors
CAS number: 145599-86-6
Indication: Used as an adjunct to diet for the reduction of elevated total and LDL cholesterol levels in patients with primary hypercholesterolemia and mixed dyslipidemia (Fredrickson Types IIa and IIb) when the response to dietary restriction of saturated fat and cholesterol and other non-pharmacological measures alone has been inadequate.
Pharmacology: Cerivastatin, a competitive HMG-CoA reductase inhibitor effective in lowering LDL cholesterol and triglycerides, is used to treat primary hypercholesterolemia and mixed dyslipidemia (Fredrickson types IIa and IIb).
Mechanism of Action:
Cerivastatin competitively inhibits hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the hepatic enzyme responsible for converting HMG-CoA to mevalonate. As mevalonate is a precursor of sterols such as cholesterol, this results in a decrease in cholesterol in hepatic cells, upregulation of LDL-receptors, and an increase in hepatic uptake of LD...
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Absorption: The mean absolute oral bioavailability 60% (range 39 - 101%).
Protein binding: More than 99% of the circulating drug is bound to plasma proteins (80% to albumin).
Biotransformation: Hepatic. Biotransformation pathways for cerivastatin in humans include the following: demethylation of the benzylic methyl ether to form Ml and hydroxylation of the methyl group in the 6'-isopropyl moiety to form M23.
Half Life: 2-3 hours
Toxicity: Rhabdomyolysis, liver concerns
Affected organisms: Humans and other mammals
Food interaction:
Grapefruit and grapefruit juice should be avoided throughout treatment as grapefruit can significantly increase serum levels of this product.
Take without regard to meals.
Drug interaction:
ClarithromycinThe macrolide, clarithromycin, may increase the toxicity of the statin, cerivastatin.
KetoconazoleIncreased risk of myopathy/rhabdomyolysis
ErythromycinThe macrolide, erythromycin, may increase the toxicity of the statin, cerivastatin.
RifabutinRifabutin may decrease the effect of cerivastatin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of cerivastatin if rifabutin is initiated, discontinued or dose changed.
FenofibrateIncreased risk of myopathy/rhabdomyolysis
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