P-glycoprotein inhibitors improve effective dose and time of pregabalin to inhibit intermittent cold stress-induced central pain

Pregabalin (PGB) is a valuable therapeutic drug against chronic pain. Here we attempted to perform the combinatorial drug therapy with P-glycoprotein (P-gp) inhibitors to lower therapeutic dosage of PGB in the intermittent cold stress-induced fibromyalgia-like pain model. Single intracerebroventricu...

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Main Authors:	Takehiro Mukae, Wakako Fujita, Hiroshi Ueda
Format:	Article
Language:	English
Published:	Elsevier 2016-05-01
Series:	Journal of Pharmacological Sciences
Subjects:	Pregabalin Fibromyalgia P-glycoprotein
Online Access:	http://www.sciencedirect.com/science/article/pii/S1347861316000037

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spelling	doaj-b80b70893ced499c81629138219f5d942020-11-25T00:28:43ZengElsevierJournal of Pharmacological Sciences1347-86132016-05-011311646710.1016/j.jphs.2016.01.002P-glycoprotein inhibitors improve effective dose and time of pregabalin to inhibit intermittent cold stress-induced central painTakehiro Mukae0Wakako Fujita1Hiroshi Ueda2Department of Pharmacology and Therapeutic Innovation, Nagasaki University Graduate School of Biomedical Sciences, 1-14 Bunkyo-machi, Nagasaki 852-8521, JapanDepartment of Frontier Life Sciences, Nagasaki University Graduate School of Biomedical Sciences, 1-7-1 Sakamoto, Nagasaki 852-8588, JapanDepartment of Pharmacology and Therapeutic Innovation, Nagasaki University Graduate School of Biomedical Sciences, 1-14 Bunkyo-machi, Nagasaki 852-8521, JapanPregabalin (PGB) is a valuable therapeutic drug against chronic pain. Here we attempted to perform the combinatorial drug therapy with P-glycoprotein (P-gp) inhibitors to lower therapeutic dosage of PGB in the intermittent cold stress-induced fibromyalgia-like pain model. Single intracerebroventricular (i.c.v.) PGB injection exerted long-lasting anti-hyperalgesic effects for 72 h, while the effect of PGB given intraperitoneally (i.p.) disappeared within 3 h. Importantly, the pretreatment with P-gp inhibitors markedly prolonged the PGB (i.p.) effects, which lasted for 72 h. These results suggest that the combinatorial treatment with P-gp inhibitor enables the prolongation of dose-interval for PGB.http://www.sciencedirect.com/science/article/pii/S1347861316000037PregabalinFibromyalgiaP-glycoprotein
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Takehiro Mukae Wakako Fujita Hiroshi Ueda
spellingShingle	Takehiro Mukae Wakako Fujita Hiroshi Ueda P-glycoprotein inhibitors improve effective dose and time of pregabalin to inhibit intermittent cold stress-induced central pain Journal of Pharmacological Sciences Pregabalin Fibromyalgia P-glycoprotein
author_facet	Takehiro Mukae Wakako Fujita Hiroshi Ueda
author_sort	Takehiro Mukae
title	P-glycoprotein inhibitors improve effective dose and time of pregabalin to inhibit intermittent cold stress-induced central pain
title_short	P-glycoprotein inhibitors improve effective dose and time of pregabalin to inhibit intermittent cold stress-induced central pain
title_full	P-glycoprotein inhibitors improve effective dose and time of pregabalin to inhibit intermittent cold stress-induced central pain
title_fullStr	P-glycoprotein inhibitors improve effective dose and time of pregabalin to inhibit intermittent cold stress-induced central pain
title_full_unstemmed	P-glycoprotein inhibitors improve effective dose and time of pregabalin to inhibit intermittent cold stress-induced central pain
title_sort	p-glycoprotein inhibitors improve effective dose and time of pregabalin to inhibit intermittent cold stress-induced central pain
publisher	Elsevier
series	Journal of Pharmacological Sciences
issn	1347-8613
publishDate	2016-05-01
description	Pregabalin (PGB) is a valuable therapeutic drug against chronic pain. Here we attempted to perform the combinatorial drug therapy with P-glycoprotein (P-gp) inhibitors to lower therapeutic dosage of PGB in the intermittent cold stress-induced fibromyalgia-like pain model. Single intracerebroventricular (i.c.v.) PGB injection exerted long-lasting anti-hyperalgesic effects for 72 h, while the effect of PGB given intraperitoneally (i.p.) disappeared within 3 h. Importantly, the pretreatment with P-gp inhibitors markedly prolonged the PGB (i.p.) effects, which lasted for 72 h. These results suggest that the combinatorial treatment with P-gp inhibitor enables the prolongation of dose-interval for PGB.
topic	Pregabalin Fibromyalgia P-glycoprotein
url	http://www.sciencedirect.com/science/article/pii/S1347861316000037
work_keys_str_mv	AT takehiromukae pglycoproteininhibitorsimproveeffectivedoseandtimeofpregabalintoinhibitintermittentcoldstressinducedcentralpain AT wakakofujita pglycoproteininhibitorsimproveeffectivedoseandtimeofpregabalintoinhibitintermittentcoldstressinducedcentralpain AT hiroshiueda pglycoproteininhibitorsimproveeffectivedoseandtimeofpregabalintoinhibitintermittentcoldstressinducedcentralpain
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P-glycoprotein inhibitors improve effective dose and time of pregabalin to inhibit intermittent cold stress-induced central pain

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