TABLE 1.
BZRA | F | t₁/₂ abs | Ka | Vd | CL | Kel | References |
---|---|---|---|---|---|---|---|
Alprazolam | 90 | 19.2 | 2.17 | 0.84 | 67.2 | 0.080 | Greenblatt and Wright (1993); Smith, Kroboth, Vanderlugt, Phillips, and Juhl (1984); Wright (1995) |
Brotizolam | 70 | 10.2 | 4.08 | 0.66 | 111 | 0.168 | Jochemsen, Wesselman, Hermans, Van Boxtel, and Breimer (1983); Langley and Clissold (1988); Scavone, Greenblatt, Harmatz, and Shader (1986) |
Clonazepam | 90 | 24.6 | 1.69 | 2.95 | 42 | 0.014 | Berlin and Dahlström (1975); Crevoisier, Delisle, Joseph, and Foletti (2003); Greenblatt et al. (2005); Wishart et al. (2018) |
Clorazepate | 91 | 18.6 | 2.24 | 1.28 | 13.2 | 0.010 | Ochs, Steinhaus, Locniskar, Knüchel, and Greenblatt (1982); Shader et al. (1981); Wishart et al. (2018) |
Diazepam | 94 | 31.8 | 1.31 | 1.83 | 21 | 0.011 | Divoll, Greenblatt, Ochs, and Shader (1983); Eatman et al. (1977); Greenblatt, Allen, Harmatz, and Shader (1980); Greenblatt, Harmatz, Friedman, Locniskar, and Shader (1989) |
Lorazepam | 90 | 32.4 | 1.28 | 1.15 | 57 | 0.050 | Greenblatt (1981); Greenblatt, Divoll, Harmatz, and Shader (1982); Wishart et al. (2018) |
Lormetazepam | 94 | 102 | 0.41 | 6.8 | 240 | 0.035 | Hildebrand, Hellstern, Hümpel, Hellenbrecht, and Saller (1990); Kampf, Huempel, Lerche, and Kessel (1981); Lombardo, Obach, Shalaeva, and Gao (2002) |
Midazolam | 50 | 18 | 2.31 | 1.3 | 330 | 0.253 | Greenblatt et al. (1984); Malacrida, Fritz, Suter, and Crevoisier (1992); Wishart et al. (2018) |
Nitrazepam | 100 | 16.2 | 2.57 | 2.55 | 54 | 0.021 | Greenblatt et al. (1985); Jochemsen et al. (1982) |
Oxazepam | 93 | 37.8 | 1.1 | 1.5 | 87 | 0.058 | Greenblatt (1981); Sonne et al. (1988) |
Temazepam | 95 | 117 | 0.36 | 1.4 | 71.4 | 0.051 | Divoll, Greenblatt, Harmatz, and Shader (1981); Schwarz (1979); Wishart et al. (2018) |
Zolpidem | 70 | 37.8 | 2.24 | 0.54 | 348 | 0.644 | Greenblatt et al. (2013); Langtry and Benfield (1990); Olubodun et al. (2002); Salvà and Costa (1995) |
Zopiclone | 80 | ‐ | 3.49 | ‐ | 228 | 0.172 | Caille, Du Souich, Spenard, Lacasse, and Vezina (1984); Fernandez, Martin, Gimenez, and Farinotti (1995); Gaillot, Heusse, Hougton, Aurele, and Dreyfus (1983); Noble, Langtry, and Lamb (1998) |
Abbreviations: BZRA, benzodiazepine receptor agonists; CL, Clearance rate (ml/h/kg); F, bioavailability (% of drug absorbed); Kel, elimination rate constant (h−1), calculated as Kel = CL/Vd; t₁/₂ abs, absorption half‐life (min); Ka, absorption rate constant (h−1), calculated as Ka = Ln (2)/t₁/₂ abs; Vd, Apparent volume of distribution (L/kg).