Comparison of short and long half‐life benzodiazepine hypnotics: Triazolam and quazepam

  title={Comparison of short and long half‐life benzodiazepine hypnotics: Triazolam and quazepam},
  author={Anthony Kales and Edward O. Bixler and Antonio Vela‐bueno and Constantin R. Soldatos and Douglas E Nikiaus and Rocco L. Manfredi},
  journal={Clinical Pharmacology \& Therapeutics},
Two benzodiazepine hypnotics, triazolam, 0.25 mg, with a short elimination t1/2, and quazepam, 15 mg, with a long t1/2, were evaluated in 22‐night sleep laboratory studies. Quazepam improved sleep significantly during both short‐ and intermediate‐term use. Daytime sleepiness, which decreased with continued use, was the side effect most often associated with quazepam dosing. In contrast, triazolam dosing did not significantly improve any of the major sleep efficiency parameters, and there was a… 
Quazepam: Hypnotic Efficacy and Side Effects
  • A. Kales
  • Medicine, Psychology
  • 1990
Quazepam is a benzodiazepine hypnotic that can be useful in the adjunctive pharmacologic treatment of insomnia and is more effective with short‐term use, and with continued use it maintains its efficacy in contrast to both of these drugs which show rapid development of tolerance.
Reintroduction of quazepam: an update on comparative hypnotic and adverse effects.
  • N. Moniri
  • Psychology, Biology
    International clinical psychopharmacology
  • 2019
The purpose of this review is to provide an update on distinguishing features of quazepam with regard to its pharmacology, pharmacokinetics, sleep efficacy and potential adverse effects compared to other agents used for insomnia.
Pharmacokinetic determinants of dynamic differences among three benzodiazepine hypnotics. Flurazepam, temazepam, and triazolam.
Healthy adult volunteers (n = 52) received single oral doses of flurazepam hydrochloride (15 mg), temazepam (15 mg), triazolam (0.25 mg), or placebo in a parallel, double-blind study. Sedative
Benzodiazepine hypnotics and insomnia.
In summary, it is proposed that the more frequent or severe side effects associated with the newer triazolo-benzodiazepines are related to an interaction of several factors, including rapid
Rebound insomnia after only brief and intermittent use of rapidly eliminated benzodiazepines
It is indicated that even under conditions of brief, intermittent use and withdrawal, triazolam and, to a lesser degree, temazepam produce rebound insomnia after abrupt withdrawal, thereby predisposing to drug‐taking behavior and increasing the potential for drug dependence.
Comparison of hangover effects among triazolam, flunitrazepam and quazepam in healthy subjects: A preliminary report
Subjective hangover effects assessed by SSS and SEQ in the morning were prominent for flunitrazepam and quazepam relative to triazolam, whereas objective indices such as MSLT or activity counts obtained in actigraphy indicated a marked hangover effect of quazEPam compared with the other two compounds restrictively in the afternoon, which were nearly in accordance with their pharmacokinetic profiles.
Temazepam 7.5 mg: effects on sleep in elderly insomniacs
Temazepam, 7.5 mg is effective in elderly subjects with short-term use and has a minimum of adverse effects and its low propensity for producing rebound insomnia, can be effectively used in this manner.
The Future of Anxiolytic Drug Therapy
  • F. Ayd
  • Psychology, Medicine
  • 1990
Despite a lack of study evidence demonstrating that benzodiazepines have continuing therapeutic efficacy beyond 6 months for anxiety and 4 weeks for insomnia, an unknown number of patients have taken Benzodiazepine for extended periods, in some cases for up to 25 years or more.
Rebound Insomnia: A Critical Review
The results indicate that rebound insomnia is a distinct possibility after discontinuation of triazolam in both insomniacs and normal controls and is greater with the short half-life as compared with the long half- life benzodiazepines.
Rebound insomnia and newer hypnotics
  • M. Lader
  • Psychology, Medicine
  • 2005
Present evidence, while limited, is consistent with claims of less rebound potential than older benzodiazepine hypnotics of equivalent duration of action, but further rigorous studies are essential before these claims can be totally accepted.


Quazepam and flurazepam: Long‐term use and extended withdrawal
The data suggest that the optimal dose of quazepam is 15 mg, and some loss of effectiveness was noted during long‐term use of both doses of quzepam and, to a lesser extent, of flurazepams.
Quazepam and temazepam: Effects of short‐ and intermediate‐term use and withdrawal
Although temazepam was effective for maintaining sleep with short‐term use, there was rapid development of tolerance for this effect with intermediate‐ term use, and quazEPam had carryover effectiveness.
Effectiveness of hypnotic drugs with prolonged use: Flurazepam and pentobarbital
Pentobarbital was found to be effective in inducing and maintaining sleep only with short‐term drug administration, which strongly suggests that it is of limited value for insomniac patients who require nightly medication beyond short-term use.
Dose‐response studies of quazepam
The efficacy and comparatively less severe side effects of the 7.5‐and 15‐mg doses of quazepam suggest that these doses may be optimal when the drug is considered for the adjunctive treatment of insomnia.
Dose—Response Studies of Lormetazepam: Efficacy, Side Effects, and Rebound Insomnia
There was less efficacy on the later drug nights, indicating a potential for the development of tolerance over a relatively short period of time, and following drug withdrawal, there was a dose‐related worsening of sleep above baseline levels (rebound insomnia).
Hypnotic Efficacy of Triazolam: Sleep Laboratory Evaluation of Intermediate‐Term Effectiveness
The data indicate that triazolam is effective for short-term use, loses most of its effectiveness with intermediate- term use, and its withdrawal is followed by a significant sorsening of sleep.
Midazolam: dose-response studies of effectiveness and rebound insomnia.
There was less effectiveness on the last 3 drug nights, indicating a potential for the development of tolerance over a relatively short period of time and following withdrawal there was a marked dose-related worsening of sleep above baseline levels (rebound insomnia).
Quazepam, A New Benzodiazepine Hypnotic: Intermediate‐Term Sleep Laboratory Evaluation
Data regarding long-term safety or tolerance of the drug suggest that quazepam is well tolerated and that its pharmacological effects are similar to those of other benzodiazepines.
Effectiveness of Temazepam with Short‐, Intermediate‐, and Long‐Term Use: Sleep Laboratory Evaluation
Effectiveness of 30 mg temazepam for inducing and maintaining sleep was evaluated in the sleep laboratory in six insomniac subjects under conditions of short-, intermediate-, and long-term drug administration, and effectiveness was not demonstrated for sleep maintenance.
Sleep laboratory studies of flurazepam: A model for evaluating hypnotic drugs
The results from six separate evaluations of flurazepam 30 mg in the sleep laboratory were combined to determine the effectiveness of the drug in inducing and maintaining sleep and its effects on