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Desmethyldiazepam pharmacokinetics: studies following intravenous and oral desmethyldiazepam, oral clorazepate, and intravenous diazepam. 1988

D J Greenblatt, and M K Divoll, and M H Soong, and H G Boxenbaum, and J S Harmatz, and R I Shader
Department of Psychiatry, Tufts University School of Medicine, Boston, Massachusetts.

After single 10-mg intravenous (IV) doses of desmethyldiazepam (DMDZ) to 12 healthy human volunteers, (mean age, 62 years) blood samples were obtained over the next 14 or more days. Mean kinetic variables were volume of distribution (Vd), 90 liters; elimination half-life (t1/2), 93 hours; and clearance, 12.3 mL/min. Vd was significantly correlated with body weight (r = .73, P less than .01) and with percent ideal body weight (r = .91, P less than .001). Eleven of the same subjects also received 5- to 15-mg doses of IV diazepam (DZ). Mean kinetic variables were Vd, 180 liters; t1/2, 83 hours; and clearance, 28 mL/min. Clearances of DZ and DMDZ were significantly correlated (r = .73, P less than .02). Based on area analysis, the extent of conversion of DZ to systemic DMDZ averaged 53%. After oral administration of DMDZ in tablet form (10 mg), or of clorazepate dipotassium in capsule form (15 mg), systemic availability of DMDZ from each of the oral dosage forms was not significantly different from 100%.

UI MeSH Term Description Entries
D007275 Injections, Intravenous Injections made into a vein for therapeutic or experimental purposes. Intravenous Injections,Injection, Intravenous,Intravenous Injection
D008297 Male Males
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D003009 Clorazepate Dipotassium A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions. Chlorazepate,Dipotassium Chlorazepate,4306-CB,Clorazepate,Clorazepate Monopotassium,Clorazepic Acid,Tranxene,Tranxilium
D003708 Nordazepam An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam. Dealkylprazepam,Demethyldiazepam,Deoxydemoxepam,Desmethyldiazepam,Nordiazepam,Calmday,N-Desalkylhalazepam,N-Descyclopropylmethyl-Prazepam,N-Descyclopropylmethylprazepam,N-Destrifluoroethylhalazepam,Nordaz,Norprazepam,Ro 5-2180,Tranxilium N,Vegesan,N Desalkylhalazepam,N Descyclopropylmethyl Prazepam,N Descyclopropylmethylprazepam,N Destrifluoroethylhalazepam,Ro 5 2180,Ro 52180
D003975 Diazepam A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity. 7-Chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one,Apaurin,Diazemuls,Faustan,Relanium,Seduxen,Sibazon,Stesolid,Valium
D005260 Female Females
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations

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