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pitavastatin; nisvastatin; itavastatin (Livalo)
FDA approved 2009, release expected 2010
Indications:
- treatment of hypercholestolemia
Pharmacokinetics:
- maximum plasma levels 1/1/5 hours after oral dose
- bioavailability 43-51%
- protein binding 99%
- only slightly lipophilic
- metabolized by CYP2C9 & to a lesser extent CYP2C8
- not a prodrug; no active metabolites
- 1/2 life of 12 hours
- renal excretion 15%
Adverse effects:
- constipation
- myalgia
- arthralgia
- back pain
Drug interactions:
- avoid use of pitavastatin in combination with cyclosporine, tacrolimus, everolimus, sirolimus [2]
- close monitoring for myalgia with coadministration of colchicine [2]
- acceptable for use with gemfibrozil [2]
Mechanism of action:
- inhibition of HMG CoA reductase
- drug's base structure has a unique cyclopropyl group, which may lead to greater LDL cholesterol clearance & plasma cholesterol reduction compared with other statins
Interactions
drug adverse effects of HMG CoA reductase inhibitors
monitor with HMG CoA reductase inhibitors (statins)
General
lipophilic statin
Database Correlations
PUBCHEM correlations
References
- Prescriber's Letter 17(6): 2010
CHART: Characteristics of the Various Statins
CHART: Clinically Significant Statin Drug Interactions
Detail-Document#: 260611
(subscription needed) http://www.prescribersletter.com
- 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