fluvastatin (Lescol)
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Introduction
Tradename: Lescol.
Indications
Contraindications
- pregnancy (potentially teratogenic, risk may be small)
Dosage
Tabs: 20 & 40 mg; Lescol XL 80 mg (sustained release).
Pharmacokinetics
- extensive 1st pass metabolism to active & inactive forms
- active forms not circulated systemically
- absolute bioavailability 24%
- maximum plasma levels in < 1 hour after oral dose[6]
- protein binding 98%
- metabolized by cyt P450 2C9 (CYP2C9) & to a lesser extent CYP2C8 & CYP3A4[6]
- not a prodrug; no active metabolites[6]
- elimination 1/2life is 1.2 hours; 3 hours[6]
- 90% excreted in the feces, 5% in the urine[6]
elimination via liver
protein binding = 98 %
1/2life = 1.2 hours
Monitor
(see HMG CoA reductase inhibitor)
Adverse effects
- gastrointestinal
- musculoskeletal
- CNS: headache, dizziness, insomnia, fatigue
- skin: rash
- Respiratory: cough
- postentially teratogenic
- drug adverse effects of HMG CoA reductase inhibitors
- drug adverse effects of anti-hyperlipidemic agents
Drug interactions
- avoid fluvastatiin in combination with gemfibrozil
- limit dose of fluvastatin to 40 mg QD with coadministration of cyclosporine, tacrolimus, everolimus, sirolimus
- any drug which inhibits cyt P450 2C9 can increase fluvastatin levels
- any drug which induces cyt P450 2C9 can diminish fluvastatin levels
- close monitoring for myalgia with coadministration of colchicine[6]
- 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
More general terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
- ↑ 4.0 4.1 Do All Statins Need to be Taken in the Evening? Prescriber's Letter 10(12):70 2003 Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=191206&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 5.0 5.1 5.2 Deprecated Reference
- ↑ 6.0 6.1 6.2 6.3 6.4 6.5 6.6 Wiggins BS, Saseen JJ, Page RL 2nd et al Recommendations for Management of Clinically Significant Drug-Drug Interactions With Statins and Select Agents Used in Patients With Cardiovascular Disease. A Scientific Statement From the American Heart Association. Circulation. 2016;134:00-00 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27754879 <Internet> http://circ.ahajournals.org/content/circulationaha/early/2016/10/17/CIR.0000000000000456.full.pdf
- ↑ Department of Veterans Affairs, VA National Formulary
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=56718
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=446155
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5287418
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=1548972
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=56719
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3404
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5281101