Titre du document / Document title

The antinociceptive effect of zolpidem and zopiclone in mice

Auteur(s) / Author(s)

PICK Chaim G. ⁽¹⁾ ; CHERNES Yakov ⁽²⁾ ; RIGAI Tova ⁽¹⁾ ; RICE Kenner C. ⁽³⁾ ; SCHREIBER Shaul ⁽⁴⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Department of Anatomy and Anthropology, Tel-Aviv University Sackler Faculty of Medicine, Tel-Aviv, 69978, ISRAEL
⁽²⁾ Psychiatric Division, The Chaim Sheba Medical Center, Tel HaShomer and Tel Aviv University Sackler Faculty of Medicine, Tel Aviv, ISRAEL
⁽³⁾ Laboratory of Medicinal Chemistry NIDDK, National Institutes of Health, Department of Health and Human Services, Bethesda, MD 20892-0815, ETATS-UNIS
⁽⁴⁾ Department of Psychiatry, Tel Aviv Sourasky Medical Center and Tel Aviv University Sackler Faculty of Medicine, Tel-Aviv, ISRAEL

Résumé / Abstract

Zolpidem and zopiclone are two of a newer hypno-sedative class of drugs, the Z compounds. Their use for the treatment of short-term insomnia has been expanding constantly during the last two decades. The Z compounds are considered to cause less significant rebound insomnia or tolerance than the conventional hypnotic benzodiazepines. Their possible antinociceptive effect and interaction with the opioid system has not been studied yet. Our results demonstrate a significant difference between the antinociceptive properties of zopiclone and zolpidem when injected s.c. in the hotplate analgesic assay in mice. Zopiclone induced a weak, dose-dependent antinociceptive effect, antagonized only by the α₂-adrenergic receptor antagonist yohimbine. Zolpidem induced a weak, biphasic dose-dependent antinociceptive effect, antagonized primarily by the non-selective opioid antagonist naloxone and by yohimbine. The weak antinociceptive effect of both drugs, evident only at very high doses (far beyond those used clinically to induce sleep), implies no clinical use for zopiclone or zolpidem in the management of pain. However, the possible interaction of zolpidem with the opioid system should be further investigated (in behavioral models, which do not overlap with the acute-pain antinociception model we used), both for possible side effects in special populations (i.e. elderly) and for possible drug-drug interactions, in order to minimize possible hazards and maximize clinical beneficial effects of its use for sleep.

Revue / Journal Title

Pharmacology, biochemistry and behavior   ISSN 0091-3057   CODEN PBBHAU 

Source / Source

2005, vol. 81, n^o3, pp. 417-423 [7 page(s) (article)] (1 p.1/4)

Langue / Language

Anglais

Editeur / Publisher

Elsevier, New York, NY, ETATS-UNIS  (1973) (Revue)

Mots-clés anglais / English Keywords

Cyclopyrrolone derivatives ; Gabaergic agonist ; Gabaergic receptor A ; Agonist ; Vertebrata ; Mammalia ; Rodentia ; Sedative ; Drug interaction ; Analgesia ; Opioid peptide ; Opiates ; Mouse ; Animal ; Zopiclone ; Hypnotic ; Zolpidem ; Analgesic ;

Mots-clés français / French Keywords

Imidazopyridine dérivé ; Cyclopyrrolone dérivé ; Stimulant gabaergique ; Récepteur gabaergique A ; Agoniste ; Vertebrata ; Mammalia ; Rodentia ; Sédatif ; Interaction médicamenteuse ; Analgésie ; Peptide opioïde ; Opiacés ; Souris ; Animal ; Zopiclone ; Hypnotique ; Zolpidem ; Analgésique ;

Mots-clés espagnols / Spanish Keywords

Ciclopirrolona derivado ; Estimulante gabaérgico ; Receptor gabaminérgico A ; Agonista ; Vertebrata ; Mammalia ; Rodentia ; Sedante ; Interacción medicamentosa ; Analgesia ; Péptido opioide ; Opiados ; Ratón ; Animal ; Zopiclona ; Hipnótico ; Zolpidem ; Analgésico ;

Mots-clés d'auteur / Author Keywords

Zopiclone ; Zolpidem ; Opioids ; Hotplate ; Mice ; Antinociception ; Drugs interaction ;

Localisation / Location

INIST-CNRS, Cote INIST : 16578, 35400013229787.0010