Table 3.
Benzodiazepine Receptor Agonist (BzRA) Drugs1
| Class/Drug | TMax (hours) | Elimination Half Life (hours) |
Usual Hypnotic Dose (mg) |
Approved for Insomnia |
Comments |
|---|---|---|---|---|---|
| Benzodiazepine | |||||
| Triazolam | 1 – 2 | 2 – 6 | 0.125 – 0.25 | Yes | Early reports of adverse effects were likely dose-related |
| Temazepam | 1 – 2 | 8 – 22 | 15 – 30 | Yes | Metabolized mainly by conjugation (no CYP-related drug interactions) |
| Estazolam | 1.5 – 2 | 10 – 24 | 1 – 2 | Yes | Triazolo ring structure similar to triazolam |
| Quazepam | 2 – 3 | 48 – 120 | 7.5 – 15 | Yes | Active metabolite (Ndesalkylflurazepam) accumulates with repeated dosing |
| Flurazepam | 1.5 – 4.5 | 48 – 120 | 15 – 30 | Yes | Active metabolite (Ndesalkylflurazepam) accumulates with repeated dosing |
| Alprazolam | 0.6 – 1.4 | 6 – 20 | No | Often noted for significant withdrawal |
|
| Lorazepam | 0.7 – 1 | 10 – 20 | 1 – 4 | No | Metabolized by conjugation (no CYP-related drug interactions) |
| Clonazepam | 1 – 2.5 | 20 – 40 | 0.5 – 3 | No | Often used for other sleep disorders including RLS, parasomnias |
| Non-Benzodiazepine | |||||
| Zaleplon | 1 (0.5 – 2) | 1 (0.8 – 1.3) | 5 – 20 | Yes | Shortest-acting BzRA |
| Eszopiclone | 1.5 (0.5 – 2) | 6 (5 – 8) | 1 – 3 | Yes | ~30% may have unpleasant taste or side-effects |
| Zolpidem – Oral tablet |
1.6 (0.5 – 1.5) | 2.5 (1.4 – 4.5) | 5 – 10 | Yes | Most widely-prescribed hypnotic |
| Zolpidem: Extended Release (Ambien CR®) |
1.5 (1.5 – 2.0) | 2.8 (1.6 – 4.5) | 6.25 – 12.5 | Yes | Higher concentrations 3-8 hours post dose than traditional zolpidem |
| Zolpidem: Sublingual (Intermezzo®) |
0.6 (0.6 – 1.3) | 2.5 (1.4 – 3.6) | 1.75 – 3.5 | Yes | Buffer permits increased buccal absorption, lower dose |
| Zolpidem: Sublingual (Edluar®) |
1.4 (0.5 – 3.0) | 2.7 ( 1.5 – 6.7) | 10 | Yes | Mainly absorbed via GI tract |
| Zolpidem: Oral Spray (Zolpimist®) |
0.9 | 2.8 (1.7 – 8.4) | 10 | Yes | Bioequivalent to tablets in terms of Cmax, Tmax, t1/2 |