Document Detail

An integrated study of pharmacokinetics and pharmacodynamics of chlormethiazole in healthy young volunteers.
MedLine Citation:
PMID:  7286029     Owner:  NLM     Status:  MEDLINE    
Chlormethiazole ethanedisulphonate (0.8%) (Hemineurin, Astra) was administered to 10 healthy unpremedicated volunteers at a constant-rate infusion of 2.5 ml/min for 60 min (Phase 1, n = 5) and 113 min (Phase 2, n = 5). With one exception, chlormethiazole blood concentration-time data were described by a two-compartment open model. Total body clearance was the same in both phases (1.151 . min-1, SD 0.49; and 1.051 . min-1, SD 0.49; and 1.051 . min-1, SD 0.36 respectively) and was similar to the clearance of indocyanine green. No correlation was found between clearance, initial dilution volume (1371, SD 62; and 1251, SD 33 in 1 and 2 phases respectively) or volume of distribution at steady-state equilibrium (3081, SD 91; and 2241, SD 59) with either body weight or estimated lean tissue mass. Slow half-life was 289 min (SD 169) in Phase 1 and 253 min (SD 172) in Phase 2. Moderately heavy sedation associated with amnesia while retaining the ability to readily obey verbal commands was achieved in one subject of Phase 1 and 4 subjects of Phase 2 and occurred at a mean chlormethiazole ethanedisulphonate blood concentration of 9.2 mg . 1(-1) (SD 2.9). Transient nasal irritation was experienced by all subjects during the initial stages of infusion. A rise in pulse rate (33%, SD 8) was a prominent feature but blood pressure and respiratory rates were very stable.
L T Seow; L E Mather; J G Roberts
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  European journal of clinical pharmacology     Volume:  19     ISSN:  0031-6970     ISO Abbreviation:  Eur. J. Clin. Pharmacol.     Publication Date:  1981 Mar 
Date Detail:
Created Date:  1981-12-21     Completed Date:  1981-12-21     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1256165     Medline TA:  Eur J Clin Pharmacol     Country:  GERMANY, WEST    
Other Details:
Languages:  eng     Pagination:  263-9     Citation Subset:  IM    
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MeSH Terms
Chlormethiazole / adverse effects,  metabolism*,  pharmacology
Indocyanine Green / metabolism
Liver / metabolism
Metabolic Clearance Rate
Nose / drug effects
Tachycardia / chemically induced
Reg. No./Substance:
3599-32-4/Indocyanine Green; 533-45-9/Chlormethiazole

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