Clinical pharmacokinetics of the newer benzodiazepines. 1983

D J Greenblatt, and M Divoll, and D R Abernethy, and H R Ochs, and R I Shader

New benzodiazepine derivatives continue to be developed and introduced into clinical use. The pharmacokinetic properties of these newer drugs can best be understood by their categorisation according to range of elimination half-life and pathway of metabolism (oxidation versus conjugation). Clobazam and halazepam are long half-life (and therefore accumulating) anxiolytics metabolised by oxidation. Alprazolam and clotiazepam also are oxidised compounds but have short to intermediate half-life values and therefore produce considerably less accumulation. Temazepam and lormetazepam are hypnotic agents with intermediate half-lives but metabolised by conjugation. The most unique of the newer benzodiazepines are the ultra-short half-life (oxidised) compounds midazolam, triazolam and brotizolam, which are essentially non-accumulating during multiple dosage.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008140 Lorazepam A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. Apo-Lorazepam,Ativan,Donix,Duralozam,Durazolam,Idalprem,Laubeel,Lorazep Von Ct,Lorazepam Medical,Lorazepam-Neuraxpharm,Lorazepam-Ratiopharm,Novo-Lorazem,Nu-Loraz,Orfidal Wyeth,Sedicepan,Sinestron,Somagerol,Temesta,Tolid,Témesta,WY-4036,Apo Lorazepam,Lorazepam Neuraxpharm,Lorazepam Ratiopharm,Medical, Lorazepam,Novo Lorazem,Nu Loraz,Von Ct, Lorazep,WY 4036,WY4036,Wyeth, Orfidal
D008874 Midazolam A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH. Dormicum,Midazolam Hydrochloride,Midazolam Maleate,Ro 21-3981,Versed,Hydrochloride, Midazolam,Maleate, Midazolam,Ro 21 3981,Ro 213981
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000078306 Clobazam A benzodiazepine derivative that is a long-acting GABA-A RECEPTOR agonist. It is used as an antiepileptic in the treatment of SEIZURES, including seizures associated with LENNOX-GASTAUT SYNDROME. It is also used as an anxiolytic, for the short-term treatment of acute ANXIETY. 1-Phenyl-5-methyl-8-chloro-1,2,4,5- tetrahydro-2,4-diketo-3H-1,5-benzodiazepine,Frisium,HR 376,LM-2717,Onfi,Urbanyl,LM 2717,LM2717
D000525 Alprazolam A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238) Alprazolan,Alprox,Apo-Alpraz,Cassadan,D-65MT,Esparon,Kalma,Novo-Alprazol,Nu-Alpraz,Ralozam,Tafil,Trankimazin,U-31,889,Xanax,Apo Alpraz,D65MT,Novo Alprazol,Nu Alpraz,U31,889
D001381 Azepines Seven membered heterocyclic rings containing a NITROGEN atom. Hexamethyleneimines
D001569 Benzodiazepines A group of two-ring heterocyclic compounds consisting of a benzene ring fused to a diazepine ring. Benzodiazepine,Benzodiazepine Compounds
D001570 Benzodiazepinones
D013693 Temazepam A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. Hydroxydiazepam,Methyloxazepam,Norkotral Tema,3-Hydroxydiazepam,Apo-Temazepam,Dasuen,Euhypnos,Gen-Temazepam,Levanxol,Nocturne,Normison,Normitab,Nortem,Novo-Temazepam,Nu-Temazepam,Oxydiazepam,PMS-Temazepam,Planum,Pronervon T,Remestan,Restoril,Ro-5-5345,SaH 47-603,Signopam,Temaze,Temazep Von Ct,Temtabs,Tenox,WY-3917,3 Hydroxydiazepam,Apo Temazepam,Gen Temazepam,Novo Temazepam,Nu Temazepam,PMS Temazepam,Ro 5 5345,Ro55345,SaH 47 603,SaH 47603,Tema, Norkotral,Von Ct, Temazep,WY 3917,WY3917

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