Indication: For management as an adjunct to diet to reduce elevated total-C, LDL-C, apo B, and TG levels in patients with primary hypercholesterolemia and mixed dyslipidemia
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 LDL-cholesterol from the circulation.
Drug Category: Anticholesteremic Agents; Antilipemic Agents; ATC:C10AA06
ANTACID (Magnesium-Aluminum Hydroxide): Cerivastatin plasma concentrations were not affected by
co-administration of antacid.
CIMETlDINE: Cerivastatin plasma concentrations were not affected by co-administration of
cimetidine.
CHOLESTYRAMINE: The influence of the bile-acidsequestering agent cholestyramine on the
pharmacokinetits of cerivastatin sodium was evaluated in 12 healthy males in 2 separate randomized crossover studies.
In the first study, concomitant administration of 0.2 mg cerivastatin sodium and 12 g cholestyramine resulted in
decreases of more than 22% for AUC and 40% for Cmax when compared to dosing cerivastatin sodium alone.
However, in the second study, administration of 12 g cholestyramine 1 hour before the evening meal and 0.3 mg
cerivastatin sodium approximately 4 hours after the same evening meal resulted in a decrease in the cerivastatin AUC
of less than 8%, and a decrease in Cmax of about 30% when compared to dosing cerivastatin sodium alone.
Therefore, it would be expected that a dosing schedule of cerivastatin sodium given at bedtime and cholestyramine
given before the evening meal would not result in a significant decrease in the clinical effect of cerivastatin
sodium.
DIGOXIN: Plasma digoxin levels and digoxin clearance at steady-state were not affected by
co-administration of 0.2 mg cerivastatin sodium. Cerivastatin plasma concentrations were also not affected by
co-administration of digoxin.
WARFARIN: Co- administration of warfarin and cerivastatin to healthy volunteers did not result in
any changes in prothrombin time or clotting factor VII when compared to co-administration of warfarin and placebo.
The AUC and Cmax of both the (R) and (S) isomers of warfarin were unaffected by concurrent dosing of 0.3
mg cerivastatin sodium. Co-administration of warfarin and cerivastatin did not alter the pharmacokinetics of
cerivastatin sodium.
ERYTHROMYCIN: In hypercholesterolemic patients, steady-state cerivastatin AUC and Cmax increased
approximately 50% and 24% respectively after 10 days with co-administration of erythromycin, a known inhibitor of
cytochrome P450 3A4.
OTHER CONCOMITANT THERAPY: Although specific interaction studies were not performed, in clinical
studies, cerivastatin sodium was used concomitantly with angiotensin- converting enzyme (ACE) inhibitors,
betablockers, calcium-channel blockers, diuretics, and nonsteroidal anti-inflammatory drugs (NSAIDs) without evidence
of clinically significant adverse interactions.
Chemical IUPAC Name: 7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)pyridin-3-yl]-3,5-dihydroxy-hept-6-enoicacid
Chemical Formula: C26H34FNO5
Half Life: 2-3 hours
Drug Type: Approved Drug
# Accession No: APRD00102
CAS Registry Number: 145599-86-6
Cerivastatin News (When available)
Meta-Analysis Rules Out Statin Cancer PreventionJan 3, 2006 MedPage Today, The studies examined six statins - Mevacor (lovastatin), Lipitor (atorvastatin), Vytorin (simvastatin), Baycol (cerivastatin), Lescol (fluvastatin), and ...
Nexavar cleared in USA for kidney cancerDec 21, 2005 Pharma Times (subscription), ...which has struggled to overcome the problems caused by the 2001 withdrawal of its cholesterol-lowering drug Lipobay/Baycol (cerivastatin) and subsequent drug ...
Suit doubting cholesterol claims goes aheadDec 16, 2005 Winnipeg Free Press (subscription), The women are suing Bayer Inc., the maker of Baycol. ... Five months later, Bayer confirmed that almost 100 deaths were linked to Baycol. ...
Studies: Statins Don't Cut Risk of Colon, Other CancersJan 9, 2006 ACS News Center, The specific statins studied included atorvastatin (Lipitor, Caduet), cerivastatin (Baycol), fluvastatin (Lescol), lovastatin (Advicor, Altoprev, Mevacor ...
Nexavar cleared in USA for kidney cancerDec 21, 2005 Pharma Times (subscription), ...business, which has struggled to overcome the problems caused by the 2001 withdrawal of its cholesterol-lowering drug Lipobay/Baycol (cerivastatin) and ...
NEWS SNAP:Bayer Healthcare Fills Its Pipeline -2Jan 5, 2006 Business Online, The company was hit hard by market removal of cholesterol-lowering drug Lipobay/Baycol in 2001 and the patent expirationfor antibiotic drug Ciprobay in 2003 in ...
2005 Year-End Report on Federal JudiciaryJan 1, 2006 Leading The Charge, ...liability filings. The District of Minnesota reported a large drop in cases involving the anti-cholesterol drug Baycol. The Central ...
Meta-Analysis Rules Out Statin Cancer PreventionJan 3, 2006 MedPage Today, The studies examined six statins - Mevacor (lovastatin), Lipitor (atorvastatin), Vytorin (simvastatin), Baycol (cerivastatin), Lescol (fluvastatin), and ...
Bayer shares rise on US approval for key drugDec 21, 2005 Reuters The company's pharma division is hamstrung by having few big-selling drug prospects, a $1 billion recall of cholesterol drug Baycol and generic competition for ...
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