Effect of Rosuvastatin on Warfarin Pharmacodynamics and Pharmacokinetics

Simonson, Steven G.; Martín, Paul; Mitchell, Patrick; Lasseter, Kenneth C.; Gibson, Gordon L.; Schneck, Dennis W.

doi:10.1177/0091270005278224

Cited by 41 publications

(25 citation statements)

References 30 publications

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“…Two studies have shown a significant increase in INR, whereas 1 study did not. [141][142][143] The mechanism of the rosuvastatin interaction is not completely established, although CYP2C9 seems a likely contributor. Several studies have demonstrated no interaction with warfarin for pitavastatin 130,142 and atorvastatin.…”

Section: Anticoagulants Warfarinmentioning

confidence: 99%

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

Wiggins¹,

Saseen²,

Page³

et al. 2016

Circulation

249

194

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A drug-drug interaction (DDI) is a pharmacokinetic or pharmacological influence of 1 medication on another that differs from the known or anticipated effects of each agent alone.1 A DDI may result in a change in either drug efficacy or drug toxicity for 1 or both of the interacting medications.2 Pharmacokinetic DDIs result in altered absorption, distribution, metabolism, or excretion of a medication. A pharmacodynamic DDI occurs when 1 medication modifies the pharmacological effect of another in an additive, a synergistic, or an antagonistic fashion.It is estimated that ≈2.8% of hospital admissions occur as a direct result of DDIs. 3 However, the actual incidence of hospitalization secondary to clinically significant DDIs is likely to be highly underestimated because medication-related issues are more commonly reported as adverse drug reactions. Complex underlying disease states also may make recognizing a DDI more challenging, further contributing to a lower reported incidence. The overall clinical impact of a DDI can range from mild to life-threatening. Therefore, not all DDIs require a modification in therapy. The variability in the clinical significance of a DDI depends on both medication-specific and patient-specific factors. Medication-specific factors include the individual pharmacokinetic characteristics of each medication implicated in the DDI (eg, binding affinity, half-life [t 1/2 ]), dose of the medications, serum concentrations, timing and sequence of administration, and duration of therapy. Patient-specific factors include age, sex, lifestyle, genetic polymorphisms causing differences in enzyme expression or activity, and disease impairment affecting drug metabolism (eg, hepatic or renal impairment, cardiac failure) or predisposition to differences in efficacy or safety (eg, statin intolerance in patients with a history of myopathy). Clinically significant DDIs are usually preventable. To optimize patient safety, healthcare providers must have an understanding of the mechanisms, magnitude, and potential consequences of any given DDI. Interpreting this information will assist clinicians in the safe prescribing of medications and permits careful consideration of the benefits and risks of concomitant medications.Statins reduce morbidity and mortality in patients with known atherosclerotic cardiovascular disease (ASCVD) and in many primary prevention patients.4-9 Current guidelines recommend high-intensity statin therapy in all patients with ASCVD age ≤75 years and moderate-to high-intensity statin therapy in patients with ASCVD and age >75 years, diabetes mellitus, and familial hypercholesterolemia and in primary prevention patients with 10-year ASCVD risk ≥7.5%.10 Given the important role of statins in patients with ASCVD and those at high ASCVD risk, combination therapy with statins and other cardiovascular medications is highly likely, and potentially significant DDIs must be considered in patients treated with statins.Another important aspect of prescribing medications in combination is evalu...

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Section: Anticoagulants Warfarinmentioning

confidence: 99%

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

Wiggins¹,

Saseen²,

Page³

et al. 2016

Circulation

249

194

View full text Add to dashboard Cite

show abstract

“…Therefore, although pharmacokinetic interactions are not predicted on the basis of the routes of metabolism, it is important to confirm a lack of clinically significant interaction via clinical pharmacokinetic studies. In addition, as there is evidence for pharmacodynamic interaction of some drugs (for example, rosuvastatin [29]) with warfarin without concomitant changes in pharmacokinetics, pharmacodynamic parameters were also evaluated for warfarin (plasma prothrombin time) in the presence and absence of dapagliflozin.…”

Section: Introductionmentioning

confidence: 99%

Lack of Pharmacokinetic Interactions Between Dapagliflozin and Simvastatin, Valsartan, Warfarin, or Digoxin

Kasichayanula

Chang²,

Liu

et al. 2012

Adv Therapy

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“…1 Literature survey reveals that CYP 2C9 enzymes metabolize it very minutely; even then it has shown interaction with some drugs with adverse effects. 12 Interaction of rosuvastatin is reported with glimepiride (Galani and Vyas, 2010), 27 clopidogrel 28 and gemfibrozil. 14 Warfarin has supporting impact on rosuvastatin.…”

Section: Discussionmentioning

confidence: 99%

“…12 Gemfibrozil affects the phar macodynamics activity of rosuvastatin. 13,14 It in combination with digoxin may cause rhabdomyolysis 15,16 while supporting anticoagulant effect of warfarin is seen with rosuvastatin. 17 Studies carried out by Edwin and coworkers in 2015 reported decrease in trace elements level in CAD patients.…”

Section: Introductionmentioning

confidence: 96%

Synthesis and Spectroscopic Characterization of Metal Complexes of Rosuvastatin

Tabassum¹,

Arayne²,

Sultana³

2017

IJPER

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Context: Rosuvastatin is a cholesterol lowering drug. It belongs to class statin. It is prescribed to the patients of coronary artery disease; atherosclerosis; thrombosis; increased low-density-lipoprotein; lipid and triglyceride. Aims:It is a newer drug in market and studies over the pharmacodynamics and pharmacokinetics are in progress. Statin therapy is a long term treatment for which its behavior in the presence of other agents is necessary. For this purpose present study is based on the interaction of the drug with essential and trace elements present in human body or co-administered during multivitamin therapy. Settings and Design: Complexes of rosuvastatin with Cd(II), Cr(II), Mn(II), Fe(III), Co(II), Ni(II) and Zn(II) i.e., metals commonly present in multivitamins, were synthesized in laboratory. Methanolic solution of rosuvastatin with metal chloride salts was reacted. Methods and Material: Reaction between drug and metals was carried out in thermostat at 80 o C for five hours with timely TLC monitoring for completion of reaction. These newly synthesized complexes were identified by IR and NMR spectroscopy and CHN elemental microanalysis and the structure of complexes was proposed. Results: Analyses suggest two molecules of rosuvastatin co-ordinate with the central metal atom through their carboxylic group. CS Chem3D ultra suggests square planner structure of the complex. Conclusions: Synthesis of compounds proposes that rosuvastatin can bind to metals as ligand through its pharmocophore site that may lead to reduced activity of drug and metal both. The study is precursor to in vitro and in vivo study of interaction of drug and metals.

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Effect of Rosuvastatin on Warfarin Pharmacodynamics and Pharmacokinetics

Cited by 41 publications

References 30 publications

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

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

Lack of Pharmacokinetic Interactions Between Dapagliflozin and Simvastatin, Valsartan, Warfarin, or Digoxin

Synthesis and Spectroscopic Characterization of Metal Complexes of Rosuvastatin

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