Document Detail

General pharmacology of brotizolam in animals.
MedLine Citation:
PMID:  3718576     Owner:  NLM     Status:  MEDLINE    
Brotizolam (2-bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f]-1,2,4-triazolo [4,3-a]-1,4-diazepine, We 941, Lendormin) is a thienotriazolo-diazepine with profound sedative and hypnogenic properties. The side effects of the drug on general behavior, motocoordination, feeding pattern, body temperature, uropoietic and gastrointestinal functions, cardiovascular system, and respiration, as well as interactions with some biogenic amines are reported and discussed. The findings correlate with those known for other diazepines. Accordingly, effects on motocoordination were prominent, but were limited to an ataxia, whereas even extremely high doses scarcely eliminated the postural reflexes. Sleeping animals could invariably be woken and were capable of locomotion; thus, no comatose condition developed. The cardiovascular functions were not appreciably altered by brotizolam in anesthetized cats, while in conscious dogs minor fluctuations of blood pressure and heart rate occurred. Respiration was clearly inhibited when brotizolam was given intravenously. The cardiovascular effects of acetylcholine, norepinephrine, epinephrine, isoprenaline, and histamine were only slightly modulated. The orexigenic and hypothermic effects equalled those of other diazepines. The functions of kidney, stomach, and intestines were not affected. The entirety of the observations procured in ten different species suggest that brotizolam is well tolerated when given orally.
P Danneberg; R Bauer; K Böke-Kuhn; W Hoefke; F J Kuhn; E Lehr; A Walland
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Arzneimittel-Forschung     Volume:  36     ISSN:  0004-4172     ISO Abbreviation:  Arzneimittelforschung     Publication Date:  1986 Mar 
Date Detail:
Created Date:  1986-07-23     Completed Date:  1986-07-23     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  0372660     Medline TA:  Arzneimittelforschung     Country:  GERMANY, WEST    
Other Details:
Languages:  eng     Pagination:  540-51     Citation Subset:  IM    
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MeSH Terms
Azepines / pharmacology*
Biogenic Amines / pharmacology
Blood Pressure / drug effects
Body Temperature / drug effects
Drug Interactions
Eating / drug effects
Heart Rate / drug effects
Hemodynamics / drug effects
Hypnotics and Sedatives / pharmacology*
Macaca mulatta
Reflex / drug effects
Respiration / drug effects
Species Specificity
Reg. No./Substance:
0/Azepines; 0/Biogenic Amines; 0/Hypnotics and Sedatives; 57801-81-7/brotizolam

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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