Cerivastatin resources


DRUG INFO
Cerivastatin

Drug Name: Cerivastatin

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

Brand Names/Synonyms: Baycol; Cerivastatin; Cerivastatin Sodium; Cerivastatin, Sodium Salt; None; Rivastatin, Baycol, Lipobay

Dosage Forms: tablets

Absorption: 60% (range 39 - 101% )

Interactions: DrugBank: Interactions for Cerivastatin

Interactions for Cerivastatin:


Immunosuppressive Drugs, Fibric Acid Derivatives, Niacin (Nicotinic Acid, Erythromycin, Azole Antifungals:

Skeletal Muscle.

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 Prevention  Jan 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 cancer  Dec 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 ...

Health Canada Mandates New Warnings on Statins Regarding Risk of ...  Jan 14, 2006
Newsinferno.com, Over the past year, however, the FDA found that Baycol, a statin which was taken off the market in August of 2001, increased the risk of this potential muscle ...

FDA Needs More Independence, Authority To Protect Consumers, NEJM ...  Jan 12, 2006
Kaiser network.org, Ray, who has served as an expert witness in trials for liability cases for Merck's Vioxx and Bayer's Baycol cholesterol drug, suggests splitting the drug ...

Suit doubting cholesterol claims goes ahead  Dec 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 Cancers  Jan 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 cancer  Dec 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 ...

Bayer May Pay $385 Mln for Rights to Nuvelo Clot Drug (Update2)  Jan 5, 2006
Bloomberg Bayer's pharmaceutical business, in recovery after the 2001 withdrawal of its Baycol anti-cholesterol drug, obtained US approval for a new cancer drug in ...

Bayer May Pay $385 Mln for Rights to Nuvelo Clot Drug (Update3)  Jan 5, 2006
Bloomberg ...heart attack, she said. Bayer's drug business is in recovery since its Baycol cholesterol drug was pulled in 2001. To contact the ...

NEWS SNAP:Bayer Healthcare Fills Its Pipeline -2  Jan 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 Judiciary  Jan 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 Prevention  Jan 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 drug  Dec 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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