Zaleplon and triazolam in humans: acute behavioral effects and abuse potential

  title={Zaleplon and triazolam in humans: acute behavioral effects and abuse potential},
  author={Craig R Rush and Joseph M. Frey and Roland R. Griffiths},
Abstract Zaleplon, a pyrazolopyrimidine that is under development as a hypnotic, produces its pharmacological effects at the benzodiazepine-recognition site on the GABAA benzodiazepine-receptor complex. Unlike most benzodiazepines, zaleplon binds selectively to the BZ1 (ω1) subtype of the benzodiazepine receptor. The present study compared the acute subject-rated effects, performance-impairing effects, and abuse potential of zaleplon and triazolam, a triazolobenzodiazepine hypnotic, in 14… 

Acute behavioral effects and abuse potential of trazodone, zolpidem and triazolam in humans

Examination of the acute behavioral effects and abuse potential of three drugs commonly used to treat sleep disorders, trazodone, zolpidem and triazolam, and placebo in ten male volunteers with histories of alcohol and drug abuse suggests that traZodone has less abuse potential than triazolate, and may be a viable alternative to benzodiazepine hypnotics in individuals with historiesof alcohol or drug abuse.

Relative Abuse Liability of Indiplon and Triazolam in Humans: A Comparison of Psychomotor, Subjective, and Cognitive Effects

The data suggest that although the abuse potential of indiplon is not different from that of triazolam at these doses, psychomotor and cognitive impairment after large doses ofIndiplon might be less.

Pharmacodynamic profile of Zaleplon, a new non‐benzodiazepine hypnotic agent

It is shown that zaleplon 10 mg has little or no residual effect when administered in the middle of the night, as late as 1 h before waking, and is devoid of impairment of driving abilities as assessed by actual driving 4’h after dose administration.

Comparative Pharmacokinetics and Pharmacodynamics of Short-Acting Hypnosedatives

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  • 2004
While zaleplon may be best indicated for the delayed onset of sleep, zolpidem and zopiclone may be better indicated for maintaining a complete night’s sleep.

Clinical evaluation of zaleplon in the treatment of insomnia

Efficacy studies show that zaleplon is a suitable hypnotic for sleep initiation purposes, but it is less effective in sleep maintenance when compared with other hypnotics, and comparisons with new nonbenzodiazepine hypnotics should determine the importance of zalePLon in the future treatment of insomnia.

Zaleplon - a review of a novel sedative hypnotic used in the treatment of insomnia

  • W. Heydorn
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    Expert opinion on investigational drugs
  • 2000
It appears zaleplon possesses a reduced risk of tolerance compared to triazolam, is less likely to potentiate the effects of ethanol and is unlikely to produce amnestic effects, according to preclinical studies.

Ramelteon: a novel hypnotic lacking abuse liability and sedative adverse effects.

Ramelteon demonstrated no significant effects indicative of potential for abuse or motor and cognitive impairment at up to 20 times the recommended therapeutic dose and may represent a useful alternative to existing insomnia medications.

A follow-up study of the acute behavioral effects of benzodiazepine-receptor ligands in humans: comparison of quazepam and triazolam.

  • C. RushJ. Ali
  • Psychology, Biology
    Experimental and clinical psychopharmacology
  • 1999
Across a sufficient range of doses, the performance-impairing effects of quazepam were similar to those of triazolam, and quzepam and triazlam produced comparable dose-dependent performance impairment and increased ratings of drug effect and drowsy.

Evaluation of the subjective and reinforcing effects of diphenhydramine, levetiracetam, and valproic acid

Diazepam produced a significantly greater effect than placebo on the Addiction Research Center Inventory–Morphine-Benzedrine Group and the Next Day Questionnaire measures ‘Take Again’ and ‘Willing to Pay’, and levetiracetam significantly increased the crossover point on the Multiple Choice Procedure, whereas diazepam did not.



Zolpidem and triazolam in humans: behavioral and subjective effects and abuse liability.

Overall, this study shows that although zolpidem produces many effects in common with triazolam, it also has a unique profile of effects distinguishable from classic benzodiazepine agonists.

Comparison of the pharmacological profiles of the hypnotic drugs, zaleplon and zolpidem.

Zolpidem, triazolam, and temazepam: behavioral and subject-rated effects in normal volunteers.

Zolpidem, triazolam, and temazepam produced orderly dose- and time-related impairment of learning, recall, and performance, and increased subject- and observer-rated estimates of strength of drug effect.

Abecarnil and alprazolam in humans: behavioral, subjective and reinforcing effects.

Comparisons of the behavioral, subjective and reinforcing effects of abecarnil to those of the benzodiazepine alprazolam in 14 healthy males with histories of sedative drug abuse suggest that abec Carnil may have less potential for abuse in a sedative-abusing population.

Behavioral Pharmacology of Zolpidem Relative to Benzodiazepines A Review

  • C. Rush
  • Psychology, Biology
    Pharmacology Biochemistry and Behavior
  • 1998

Trazodone and triazolam: acute subject-rated and performance-impairing effects in healthy volunteers

Trazodone may be a viable alternative to benzodiazepine hypnotics like triazolam, especially when needing to minimize drug-induced impairment, and should be considered in a clinically relevant population such as individuals with histories of drug abuse.

Aspects of benzodiazepine receptor structure and function with relevance to drug tolerance and dependence.

It is demonstrated that subchronic administration of alprazolam (a high-efficacy agonist) results in strong withdrawal reactions upon injection of a benzodiazepine receptor antagonist in mice and monkeys, and indicates that partial and receptor subtype 1-selective agonists differ from full, non-selectives agonists in their liability to induce drug dependence and tolerance upon chronic administration.

Zolpidem behavioral pharmacology in baboons: self-injection, discrimination, tolerance and withdrawal.

The withdrawal, discriminative stimulus effects and tolerance shown with zolpidem were similar to those shown previously with benzodiazepines under similar conditions.

Discriminative stimulus effects of zolpidem in pentobarbital-trained subjects: II. Comparison with triazolam and caffeine in humans.

The results suggest that humans can acquire and maintain a pentobarbital-placebo discrimination, and this discrimination is pharmacologically specific and suggest that despite the somewhat unique biochemical profile of zolpidem, its discriminative stimulus, subject-rated and performance-pairing effects are similar to those of classic sedative/hypnotic compounds like the barbiturates and benzodiazepines.

Lorazepam and meprobamate dose effects in humans: behavioral effects and abuse liability.

The behavioral effects of benzodiazepines can be differentiated from those of other types of sedative/anxiolytics and that MEP displays characteristics of a barbiturate-like profile of action.