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fluvastatin (Lescol)

Tradename: Lescol. Indications: - hypercholesterolemia (increased LDL) - arteriosclerosis [5] - coronary artery disease - myocardial infarction - transient ischemic attack - ischemic stroke - prevention of cardiovascular disease [5] Contraindications: - pregnancy (potentially teratogenic, risk may be small) Dosage: 1) start 20-40 mg PO QHS [4] 2) maximum 80 mg/day, given 40 mg BID 3) Geriatrics: maximum 40 mg/day Tabs: 20 & 40 mg; Lescol XL 80 mg (sustained release). Pharmacokinetics: 1) extensive 1st pass metabolism to active & inactive forms a) active forms not circulated systemically b) absolute bioavailability 24% c) maximum plasma levels in < 1 hour after oral dose [6] 2) protein binding 98% 3) metabolized by cyt P450 2C9 (CYP2C9) & to a lesser extent CYP2C8 & CYP3A4 [6] 4) not a prodrug; no active metabolites [6] 4) elimination 1/2life is 1.2 hours; 3 hours [6] 5) 90% excreted in the feces, 5% in the urine [6] Monitor: (see HMG CoA reductase inhibitor) Adverse effects: 1) gastrointestinal - nausea/vomiting, dyspepsia - diarrhea, constipation, abdominal cramps, flatulence - hepatitis - increased serum transaminases 2) musculoskeletal a) myopathy - myalgias - increased serum creatine kinase - rhabdomyolysis - renal failure b) arthropathy 3) CNS: headache, dizziness, insomnia, fatigue 4) skin: rash 5) Respiratory: cough 6) postentially teratogenic Drug interactions: 1) avoid fluvastatiin in combination with gemfibrozil 2) limit dose of fluvastatin to 40 mg QD with coadministration of cyclosporine, tacrolimus, everolimus, sirolimus 3) any drug which inhibits cyt P450 2C9 can increase fluvastatin levels 4) any drug which induces cyt P450 2C9 can diminish fluvastatin levels 5) close monitoring for myalgia with coadministration of colchicine [6]

Interactions

drug interactions drug adverse effects (more general classes) monitor with HMG CoA reductase inhibitors (statins)

Related

cytochrome P450 2C9; cytochrome P450 BP-1; cytochrome P450 MP-4; S-mephenytoin-4-hydroxylase; limonene 6-monooxygenase; limonene 7-monooxygenase (CYP2C9, CYP2C10)

General

hydrophilic statin

Properties

INHIBITS: HMG CoA reductase MISC-INFO: elimination route LIVER protein-binding 98% 1/2life 1.2 HOURS pregnancy-category X safety in lactation -

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: 220233 (subscription needed) http://www.prescribersletter.com
  3. Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
  4. Do All Statins Need to be Taken in the Evening? Prescriber's Letter 10(12):70 2003 Detail-Document#: 191206 (subscription needed) http://www.prescribersletter.com
  5. Deprecated Reference
  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 PMID: 27754879 http://circ.ahajournals.org/content/circulationaha/early/2016/10/17/CIR.0000000000000456.full.pdf
  7. Department of Veterans Affairs, VA National Formulary