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ZHAO Jing, CAO Hong, XING Jun-bo. The fingerprint analysis on Chuanshentong injection by HPLC[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(2): 137-139. doi: 10.3969/j.issn.1006-0111.2013.02.016
Citation:
HOU Cheng, LU Guangzhao, ZHANG He, LU Ying, ZHONG Yanqiang, ZOU Hao. Evaluation of the effect of different routes of administrating flumazenil against hypnosis[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(1): 30-33,54. doi: 10.3969/j.issn.1006-0111.2018.01.006
Evaluation of the effect of different routes of administrating flumazenil against hypnosis
Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
Received Date: 2017-09-28
Rev Recd Date:
2017-10-23
Abstract
Objective To study the effect of flumazenil on hypnotic mice induced by diazepam and zolpidem, and to evaluate the possibility of flumazenil oral administration. Methods First, Kunming mice were injected intraperitoneally with normal saline and sodium pentobarbital (S + W), diazepam and pentobarbital sodium (D + W), zolpidem and pentobarbital sodium (Z + W). The hypnotic effect of diazepam and zolpidem on prolonging the sleep time of pentobarbital sodium would be verified by (D + W) group and (Z + W) group. Then the mice were injected intraperitoneally with flumazenil. The sleep time was used as the evaluation index to evaluate the effect of flumazenil against hypnosis. Finally, the oral administration of flumazenil was observed against hypnosis, which was evaluated by using sleep time as an index. Results Compared with the control group (S+W), the diazepam group (D+W) and the zolpidem group (Z+W) significantly prolonged the sleep time induced by pentobarbital sodium (P<0.001,P<0.05);After Intraperitoneal injection of flumazenil,compared with the diazepam group (D+W) and the zolpidem group (Z+W),the sleep time of the diazepam group[F(ip)+D+W] and the zolpidem group[F(ip)+Z+W] were significantly shorter (P<0.001, P<0.05);After oral administration of flumazenil, the sleep time of the diazepam group[F(ig)+D+W] and the zolpidem group[F(ig)+Z+W] were also significantly shorter (P<0.001,P<0.05). Conclusion Flumazenil, whether intraperitoneal injection or intragastric administration, could antagonize the hypnotic effect of diazepam and zolpidem. It was proved that oral administration of flumazenil had the same effect compared with intraperitoneal injection of flumazenil, which provided the possibility of preparation of oral administration of flumazenil.
Trotti LM, Saini P, Koola C, et al. Flumazenil for the treatment of refractory hypersomnolence:clinical experience with 153 patients[J]. J Clin Sleep Med, 2016, 12(10):1389-1394.
Forouzanfar F, Hosseini A, Amiri M S, et al. Potentiating effects of Perovskia abrotanoides Karel. on pentobarbital-induced sleep[J]. Avicenna J Phytomed, 2017, 7(3):214-222.
[9]
Koga N, Yamaguchi T, Lee KK, et al. Kososan,a standardized traditional Japanese herbal medicine, reverses sleep disturbance in socially isolated mice via GABAA-benzodiazepine receptor complex activation[J]. Phytomedicine, 2014, 21(5):697-703.
[10]
Roncari G, Ziegler WH, Guentert TW. Pharmacokinetics of the new benzodiazepine antagonist Ro 15-1788 in man following intravenous and oral administration[J]. Br J Clin Pharmacol, 1986, 22(4):421-428.
[11]
Klotz U, Kanto J. Pharmacokinetics and clinical use of flumazenil (Ro 15-1788)[J]. ClinPharmacokinet, 1988, 14(1):1-12.
[12]
Kasteleijn-Nolst Trenite DG, Groenwold RH, Schmidt B,et al. Single dose efficacy evaluation of two partial benzodiazepine receptor agonists in photosensitive epilepsy patients:A placebo-controlled pilot study[J]. Epilepsy Res, 2016, 122:30-36.
Abstract: Objective To study the effect of flumazenil on hypnotic mice induced by diazepam and zolpidem, and to evaluate the possibility of flumazenil oral administration. Methods First, Kunming mice were injected intraperitoneally with normal saline and sodium pentobarbital (S + W), diazepam and pentobarbital sodium (D + W), zolpidem and pentobarbital sodium (Z + W). The hypnotic effect of diazepam and zolpidem on prolonging the sleep time of pentobarbital sodium would be verified by (D + W) group and (Z + W) group. Then the mice were injected intraperitoneally with flumazenil. The sleep time was used as the evaluation index to evaluate the effect of flumazenil against hypnosis. Finally, the oral administration of flumazenil was observed against hypnosis, which was evaluated by using sleep time as an index. Results Compared with the control group (S+W), the diazepam group (D+W) and the zolpidem group (Z+W) significantly prolonged the sleep time induced by pentobarbital sodium (P<0.001,P<0.05);After Intraperitoneal injection of flumazenil,compared with the diazepam group (D+W) and the zolpidem group (Z+W),the sleep time of the diazepam group[F(ip)+D+W] and the zolpidem group[F(ip)+Z+W] were significantly shorter (P<0.001, P<0.05);After oral administration of flumazenil, the sleep time of the diazepam group[F(ig)+D+W] and the zolpidem group[F(ig)+Z+W] were also significantly shorter (P<0.001,P<0.05). Conclusion Flumazenil, whether intraperitoneal injection or intragastric administration, could antagonize the hypnotic effect of diazepam and zolpidem. It was proved that oral administration of flumazenil had the same effect compared with intraperitoneal injection of flumazenil, which provided the possibility of preparation of oral administration of flumazenil.
ZHAO Jing, CAO Hong, XING Jun-bo. The fingerprint analysis on Chuanshentong injection by HPLC[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(2): 137-139. doi: 10.3969/j.issn.1006-0111.2013.02.016
Citation:
HOU Cheng, LU Guangzhao, ZHANG He, LU Ying, ZHONG Yanqiang, ZOU Hao. Evaluation of the effect of different routes of administrating flumazenil against hypnosis[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(1): 30-33,54. doi: 10.3969/j.issn.1006-0111.2018.01.006
Trotti LM, Saini P, Koola C, et al. Flumazenil for the treatment of refractory hypersomnolence:clinical experience with 153 patients[J]. J Clin Sleep Med, 2016, 12(10):1389-1394.
Forouzanfar F, Hosseini A, Amiri M S, et al. Potentiating effects of Perovskia abrotanoides Karel. on pentobarbital-induced sleep[J]. Avicenna J Phytomed, 2017, 7(3):214-222.
[9]
Koga N, Yamaguchi T, Lee KK, et al. Kososan,a standardized traditional Japanese herbal medicine, reverses sleep disturbance in socially isolated mice via GABAA-benzodiazepine receptor complex activation[J]. Phytomedicine, 2014, 21(5):697-703.
[10]
Roncari G, Ziegler WH, Guentert TW. Pharmacokinetics of the new benzodiazepine antagonist Ro 15-1788 in man following intravenous and oral administration[J]. Br J Clin Pharmacol, 1986, 22(4):421-428.
[11]
Klotz U, Kanto J. Pharmacokinetics and clinical use of flumazenil (Ro 15-1788)[J]. ClinPharmacokinet, 1988, 14(1):1-12.
[12]
Kasteleijn-Nolst Trenite DG, Groenwold RH, Schmidt B,et al. Single dose efficacy evaluation of two partial benzodiazepine receptor agonists in photosensitive epilepsy patients:A placebo-controlled pilot study[J]. Epilepsy Res, 2016, 122:30-36.
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ZHAO Jing, CAO Hong, XING Jun-bo. The fingerprint analysis on Chuanshentong injection by HPLC[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(2): 137-139. doi: 10.3969/j.issn.1006-0111.2013.02.016
ZHAO Jing, CAO Hong, XING Jun-bo. The fingerprint analysis on Chuanshentong injection by HPLC[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(2): 137-139. doi: 10.3969/j.issn.1006-0111.2013.02.016
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