cerivastatin; rivastatin (Baycol, Lipobay)
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Introduction
Tradename: Baycol. Removed from US market 2001[3] Withdrawn from worldwide market Aug 8, 2001[2].
Indications
- adjunct to diet in treatment of primary hypercholesterolemia & mixed dyslipidemia
Contraindications
- pregnancy or lactation
- hepatic disease
- concurrent administration of GEMFIBROZIL (Lopid)
Dosage
- 0.4 mg QD in the evening
- may be given with or without food
Tabs: 0.2, 0.3, 0.4 mg.
store tabs below 77 degrees F; protect from moisture.
Dosage adjustment in renal failure
- creatinine clearance < 60 mL/min, start 0.2-0.3 mg QD
Pharmacokinetics
- absolute bioavailability is 60%
- metabolized to pharmacologically active metabolites
- eliminated in the urine & feces as metabolites
- terminal elimination 1/2life is 2-3 hours
- effects on cholesterol seen in 1 week
- maximal effects on cholesterol seen in 4 weeks
- time to peak serum concentration 2.5 hours
- peak serum levels: 0.2 mg 2.4 ug/L; 0.3 mg 3.8 ug/L; 0/4 mg 5.5 ug/L
- linear elimination kinetics 0.04-0.4 mg QD
- protein-binding > 99%
- volume of distribution 0.3 L/kg
elimination via liver
elimination via kidney
protein binding = >99 &
1/2life = 2-3 hours
Monitor
- liver function tests: initially, at 6 & 12 weeks, then semiannually
- creatine kinase as indicated
Adverse effects
- similar to other statins
- common
- cardiovascular (2%)
- headache
- gastrointestinal
- abdominal pain, dyspepsia (6%), diarrhea (4%)
- genitourinary
- RHABDOMYOLYSIS with acute renal failure (reason for removal from US market)[3]
- mild elevations in serum transaminases
- musculoskeletal
- increases in creatine kinase (5X)
- rhabdomyolysis 0.05%[4]
- drug adverse effects of HMG CoA reductase inhibitors
- drug adverse effects of anti-hyperlipidemic agents
Drug interactions
- in combination with GEMFIBROZIL increases incidence of RHABDOMYOLYSIS to 9%[4]
- zidovudine: mild increased in zidovudine level
- cholestyramine decreases availability of cerivastatin
- increased risk of rhabdomyolysis with
- cyclosporine, erythromycin, gemfibrozil, fluconazole, itraconazole, ketoconazole, mibefradil, niacin
- any drug which inhibits cyt P450 3A4 can increase cerivastatin levels
- any drug which induces cyt P450 3A4 can diminish cerivastatin levels
- drug interaction(s) anticonvulsants with statins
- drug interaction(s) of statins with vitamin D
- drug interaction(s) of statins with SSRIs
- drug interaction(s) of statins with influenza virus vaccines
- drug interaction(s) of statins with macrolide
- drug interaction(s) of statins with antiviral protease inhibitors
- drug interaction(s) of statins with fibrates
Mechanism of action
- inhibition of HMG CoA reductase
- maximal effect (0.3 mg/day)
- total cholesterol: decrease of 19%
- LDL cholesterol: decrease of 28%
- HDL cholesterol: increase of 10%
- triglycerides: decrease of 13%
More general terms
Additional terms
References
- ↑ Micromedex
- ↑ 2.0 2.1 http://www.baycol.com/Dear_HealthCare_Letter_Baycol_pull.jpg http://www.press.bayer.com/News/news.nsf/ID/NT0000E072
- ↑ 3.0 3.1 3.2 Prescriber's Letter 8(9):50 2001
- ↑ 4.0 4.1 4.2 Psaty BM, Furberg CD, Ray WA, Weiss NS. Potential for conflict of interest in the evaluation of suspected adverse drug reactions: use of cerivastatin and risk of rhabdomyolysis. JAMA. 2004 Dec 1;292(21):2622-31. Epub 2004 Nov 22. Review. PMID: https://www.ncbi.nlm.nih.gov/pubmed/15572720
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=446156
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5287419
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=60873
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2676
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=60872
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=528100