Possible Interaction of Zopiclone and Nefazodone

  title={Possible Interaction of Zopiclone and Nefazodone},
  author={Christopher P Alderman and Markus G. Gebauer and Andrew L. Gilbert and John T. Condon},
  journal={Annals of Pharmacotherapy},
  pages={1378 - 1380}
OBJECTIVE: To describe a case in which concurrent treatment with nefazodone was associated with an elevation in the plasma concentration of zopiclone, possibly resulting in enhanced hypnosedative efficacy. CASE REPORT: An 86-year-old white woman was treated with nefazodone for depression. Zopiclone was also introduced for the management of insomnia, but she subsequently experienced morning drowsiness. The concentration of zopiclone in plasma was subsequently measured eight hours after… Expand
5 Citations
Comparative Pharmacokinetics and Pharmacodynamics of Short-Acting Hypnosedatives
  • D. Drover
  • Medicine
  • Clinical pharmacokinetics
  • 2004
While zaleplon may be best indicated for the delayed onset of sleep, zolpidem and zopiclone may be better indicated for maintaining a complete night’s sleep. Expand
Hypnosedatives and anxiolytics
Alprazolam impaired cognitive performance and subjective sedation in a dose-dependent manner and has been compared with diazepam in 37 patients, who were randomized into two groups. Expand
A review of the common properties of drugs with idiosyncratic hepatotoxicity and the "multiple determinant hypothesis" for the manifestation of idiosyncratic drug toxicity.
  • Albert P. Li
  • Biology, Medicine
  • Chemico-biological interactions
  • 2002
Common properties of drugs that cause idiosyncratic liver toxicity are reviewed and it is proposed that these common properties may be useful experimental endpoints for the prediction and therefore avoidance of the selection of drug candidates with idiosyncratic drug toxicity for further development. Expand
New-generation, non-SSRI antidepressants: Drug-drug interactions and therapeutic drug monitoring. Part 2: NaSSAs, NRIs, SNDRIs, MASSAs, NDRIs, and others.
After the development of "classical" tricyclic antidepressants and monoamine oxidase inhibitors, numerous other classes of antidepressant drugs have been introduced onto the market, usually identified by their mechanism of activity. Expand


Concentrations and effects of zopiclone are greatly reduced by rifampicin.
Zopiclone may show a reduced hypnotic effect when used concomitantly with rifampicin or other potent inducers of CYP3A4 such as phenytoin and carbamazepine. Expand
Effect of itraconazole on the pharmacokinetics and pharmacodynamics of zopiclone
Itraconazole has a statistically significant pharmacokinetic interaction with zopiclone but this is only of limited clinical importance, at least in young adults. Expand
The effect of erythromycin on the pharmacokinetics and pharmacodynamics of zopiclone.
The interaction between erythromycin and zopiclone resulted mainly in accelerated absorption which may lead to a faster hypnotic effect in patients. Expand
Pharmacokinetics of zopiclone and its enantiomers in Caucasian young healthy volunteers.
Determination of concentrations of zopiclone enantiomers in plasma showed that zopicLone pharmacokinetics is stereoselective with AUC0-->infinity values of 691.3 and 209.5 ng.ml-1, and Quantities of (+)-zopiclones excreted in urine were always higher compared with its antipode (-)-zopylone for the 12 volunteers. Expand
Cytochrome P-450 3A4 and 2C8 are involved in zopiclone metabolism.
Recombinant CYP2C8 had the highest enzymatic activity toward zopiclone metabolism into both its metabolites, followed by CYP 2C9 and 3A4, and CYP3A4 contributes significantly to ND-Z formation. Expand
Nefazodone, meta-chlorophenylpiperazine, and their metabolites in vitro: cytochromes mediating transformation, and P450-3A4 inhibitory actions
The complex parallel biotransformation pathways of nefazodone are mediated mainly by human cytochrome P450-3A, whereas clearance of mCPP is mediated by P 450-2D6, and two of its hydroxylated metabolites are potent 3A inhibitors. Expand
Inhibition of cytochrome P450 by nefazodone in vitro: studies of dextromethorphan O- and N-demethylation.
In vivo data, as well as in vitro data based on "pure' CYP3A3/4 substrates, provide evidence for clinically relevant CYP2D6-mediated inhibition by NEF, OH-NEf, and pOH-NEF, and the findings for DMO O-demethylation indicate that NEF and metabolites are weak inhibitors of this reaction. Expand
Pharmacokinetic-Pharmacodynamic Consequences and Clinical Relevance of Cytochrome P450 3A4 Inhibition
The clinical importance of any drug interaction depends on factors that are drug-, patient- and administration-related and is likely to be dependent on interindividual differences in CYP3A4 tissue content, pre-existing medical conditions and, possibly, age. Expand
Enantioselective determination of zopiclone and its metabolites in urine by capillary electrophoresis.
Urine samples of two volunteers after oral administration of 7.5 mg zopiclone were investigated and the S-(+)-enantiomers of zopicLone and its metabolites were always excreted in higher amounts than the R-(-)- enantiomers. Expand
Pharmacokinetic drug interactions of new antidepressants: a review of the effects on the metabolism of other drugs.
A "primer" on drug metabolism is included herein, which serves as a basis for understanding these interactions, and appropriate cautions are recommended for concurrent administration of these new antidepressants and other drugs most frequently prescribed to elderly patients. Expand