Effect of sleep on quazepam kinetics

  title={Effect of sleep on quazepam kinetics},
  author={James M. Hilbert and Menger Chung and Gary Maier and Richard Gural and Samson Symchowicz and Nicola Zampaglione},
  journal={Clinical Pharmacology \& Therapeutics},
The effect of sleep on quazepam kinetics was studied in 12 normal adult men. In a randomized two‐way crossover design, each subject received one 15‐mg quazepam tablet either at night just before sleep or in the morning after a night's sleep. Blood samples were drawn before and at specified times (to 120 hr) after dosing. To assure that blood collection did not interfere with sleep, blood was drawn by an indwelling catheter from a large arm vein. Plasma concentrations of quazepam and its two… 
Quazepam kinetics in the elderly
Comparison of these data with reported kinetic data in young subjects shows that t½βs of quazepam and 2‐oxoquzepam increased only slightly or not at all with age, but that the t½ β of N‐desalkyl‐2‐oxquazep am in the elderly was more than twice that in youngSubjects.
Time effects of food intake on the pharmacokinetics and pharmacodynamics of quazepam.
The dosing of quazepam after a long period of ordinary fasting might reduce its efficacy because a 3 h interval between the timing of the evening meal and bedtime administration of hypnotics is regarded as normal in daily life.
Hypnotic effects of low doses of quazepam in older insomniacs.
Analyses of plasma concentrations of quzepam and its metabolites suggested the continued drug effects on sleep during recovery are due to the metabolite desalkylflurazepam, and the safety evaluation done by means of adverse drug event assessments and postsleep questionnaires was minimal.
Pharmacokinetics of temazepam after day-time and night-time oral administration
It is concluded that a chronopharmacokinetic effect was seen for temazepam; however it is unlikely to be of any clinical significance.
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.
Quazepam. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in insomnia.
Preliminary evidence suggests that quazepam 15 to 30 mg is as effective as flurAZepam and triazolam in usual therapeutic doses, and causes minimal rebound insomnia following its withdrawal, unlike rapidly eliminated benzodiazepines such as triazlam.
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.
Comparison of short and long half‐life benzodiazepine hypnotics: Triazolam and quazepam
The 0.25 mg dose of triazolam, which is being prescribed increasingly, has a profile of side effects that is similar to that of the 0.5 mg dose, and is associated with sleep and mood disturbances whereas quazepam exerted carryover effectiveness.
Excretion of Quazepam Into Human Breast Milk
The excretion of quazepam, 2‐oxoquazpeam, and N‐desalkyl‐2‐xoquzepam into human breast milk was studied in four lactating nonpregnant volunteers and the concentrations of the three compounds found in milk appeared to depend on their relative lipophilicities, which were determined by log P values.
Effects of quazepam as a preoperative night hypnotic: comparison with brotizolam
The preoperative night hypnotics, quazepam and brotizolam improved sleep before surgery; the frequency of nocturnal awakening and dreaming decreased, and the total duration of sleep the night before surgery increased.


Effect of sleep on bioavailability of tetracycline.
Questions are raised as to the predictability of bioavailability studies in ambulatory subjects relative to the actual use of drug products, which are frequently administered during conditions of bed rest or sleep.
The Effect of a New Benzodiazepine on the Polygraphically Monitored Sleep of Normal Volunteers
The subjective quality of sleep was improved by the new benzodiazepine hypnotic, and one subject reported that he felt lethargic the day after the largest dose.
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.
Circadian Changes of Drug Disposition in Man
The roles presumably played by circadian rhythms in drug metabolising liver enzymes and kidney function are summarized, and the practical implications of chronopharmacokinetics, aiming both to improve in a quantitative manner the metabolic fate of a drug and its effectiveness, are discussed.
The acute effects of quazepam in the sleep of chronic insomniacs
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  • 1982
The effect of 15 and 20 mg
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Time - of - day effects on diazepam kinetics after oral dosing
  • IRCS Med Sci
  • 1980
The effect of 15 and 20 mg of quazepam ( SCH - 16134 ) on the sleep of chronic insomniacs
  • CUIT Ther Res
  • 1979
A package of computer programs for pharmacokinetic modeling
  • Biometrics
  • 1974