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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1995-3-6
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pubmed:abstractText |
The antihypertensive effects of a new transdermal delivery system for clonidine (clonidine tape; M-5041T) were investigated in spontaneously hypertensive rats and normotensive Wistar-Kyoto rats. In spontaneously hypertensive rats, M-5041T, at doses of 0.5-4.5 mg/kg (1.25-11.25 cm2/kg), produced a dose-dependent decrease of both systolic blood pressure and heart rate for 24 hr during transdermal application. These significant hypotensive effects lasted for 24 hr following the patching of M-5041T on the back of the animals at a dose of 4.5 mg/kg. In normotensive Wistar-Kyoto rats, the hypotensive and bradycardic effects of M-5041T were weak compared with those in spontaneously hypertensive rats. In both rat strains, M-5041T (4.5 mg/kg) caused behavioral changes such as sedation, piloerection and exophthalmos, accompanied by hypotensive effects. Both M-5041T (1.5 mg/kg) and clonidine (50 micrograms/kg, subcutaneously and 100 micrograms/kg, orally) induced similar hypotensive effects, accompanied by sedation. The hypotensive effects following transdermal M-5041T or systemic clonidine administrations were correlated with the time courses of the plasma clonidine concentration. In contrast to clonidine administered subcutaneously or orally, M-5041T produced a gradual increase in the plasma clonidine concentration, which persisted at a consistent level for at least 12 hr thereafter. Significant hypotensive effects lasted for 12 and 24 hr following M-5041T patching at 1.5 and 4.5 mg/kg, respectively. The present findings suggest that M-5041T can serve as an efficient and useful antihypertensive transdermal delivery system to achieve persistent blood pressure control.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:issn |
0301-4533
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
327
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
294-308
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:7848013-Administration, Cutaneous,
pubmed-meshheading:7848013-Administration, Oral,
pubmed-meshheading:7848013-Animals,
pubmed-meshheading:7848013-Behavior, Animal,
pubmed-meshheading:7848013-Blood Pressure,
pubmed-meshheading:7848013-Bradycardia,
pubmed-meshheading:7848013-Clonidine,
pubmed-meshheading:7848013-Disease Models, Animal,
pubmed-meshheading:7848013-Dose-Response Relationship, Drug,
pubmed-meshheading:7848013-Drug Delivery Systems,
pubmed-meshheading:7848013-Gas Chromatography-Mass Spectrometry,
pubmed-meshheading:7848013-Half-Life,
pubmed-meshheading:7848013-Heart Rate,
pubmed-meshheading:7848013-Hypertension,
pubmed-meshheading:7848013-Injections, Subcutaneous,
pubmed-meshheading:7848013-Male,
pubmed-meshheading:7848013-Rats,
pubmed-meshheading:7848013-Rats, Inbred SHR,
pubmed-meshheading:7848013-Rats, Inbred WKY
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pubmed:articleTitle |
Antihypertensive effects of a new transdermal delivery system for clonidine (M-5041T) in spontaneously hypertensive rats.
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pubmed:affiliation |
Central Research Laboratories, Maruho Co., Ltd., Osaka, Japan.
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pubmed:publicationType |
Journal Article,
Comparative Study
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