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PubMed1998

Effect of temazepam on oxygen saturation and sleep quality at high altitude: randomised placebo controlled crossover trial.

OBJECTIVE: To determine the effects of temazepam on the quality of sleep and on oxygen saturation during sleep in subjects at high altitude. DESIGN: Randomised, blinded, crossover, placebo controlled trial. SETTING: Base camp at Mount Everest (altitude 5300 m). SUBJECTS: 11 members of British Mount Everest Medical Expedition recently arrived at base camp. INTERVENTION: Participants were randomly allocated to receive either temazepam 10 mg or placebo on their first night at base camp and the other treatment on the second night. MAIN OUTCOME MEASURES: Quality of sleep (assessed subjectively), mean arterial oxygen saturation value, and changes in saturation values (as measure of periodic breathing) while participants taking temazepam or placebo. RESULTS: All participants noted subjective improvements in sleep. Mean saturation value remained unchanged when temazepam was compared with placebo (74.65% v 75.70%, P = 0.5437). There were fewer changes in oxygen saturation when participants took temazepam and when measured as decreases > 4% below the mean value of saturation each hour (P = 0.0036, paired Student's t test (two tailed)). CONCLUSIONS: Participants taking temazepam at 5300 m showed no significant drop in mean oxygen saturation values during sleep. Both the number and severity of changes in saturation during sleep decreased and the quality of sleep improved. This may be a result of a reduction in the number of awakenings and might lead to greater respiratory stability and fewer episodes of periodic breathing. This has the effect of improving the quality of sleep and reducing the number of periods of desaturation during sleep.

Adult↗
PubMed1983

Pharmaco-EEG and Psychometric study of the effect of single doses of temazepam and nitrazepam.

A double-blind, daytime, placebo-controlled study was carried out in 12 healthy volunteers to investigate the effects of single doses of 5, 15 and 30 mg temazepam and of 5 and 10 mg nitrazepam on the EEG, psychomotor performance, subjective mental and emotional status, blood pressure and heart rate. Each subject received all 6 treatments in a random sequence at intervals of 1 week. The EEG tracings were evaluated quantitatively by spectral analysis. Psychomotor performance was assessed by means of the tapping test. Subjective mental and emotional status were assessed using the Bond and Lader analogue self-rating scale. Procedures were carried out before and at 1/2, 1, 2, 4, 6, 7, 8 and 9 h after drug administration, with the exception of the tapping test, which was carried out before and, again, after 2 and 7 h. EEG estimates of equipotency, based on magnitude of peak effect, were as follows: 15 mg temazepam approximately 5 mg nitrazepam; and 30 mg temazepam greater than or equal to 10 mg nitrazepam. At these approximately equipotent doses, temazepam had a somewhat earlier onset of action on the EEG, a clearly shorter duration of EEG action, and lesser impairment of psychomotor performance than nitrazepam. Qualitatively, both drugs had similar effects on the subjective mental and emotional states of the subjects. There were no clinically relevant changes in mean or individual sitting and standing blood pressure values. After temazepam, but not after nitrazepam, heart rate increased (maximal mean change 10 bpm) as part of a normal startle response to arousal. The results suggest that temazepam has less hangover potential than nitrazepam.

Adult↗
PubMed1993

Bioavailability of temazepam: comparison of four 7.5-MG capsules with a single 30-MG capsule.

OBJECTIVE: To compare the bioavailability of four temazepam 7.5-mg capsules (Restoril, Sandoz Pharmaceuticals) with that of a single temazepam 30-mg capsule. DESIGN: Single-dose, open-label, two-period, crossover (replicated Latin square). SETTING: Domiciled environment for clinical testing. PARTICIPANTS: Twenty-six healthy male volunteers aged 18-40 years; 25 completed the study. INTERVENTIONS: Subjects randomly received either four temazepam 7.5-mg capsules or one temazepam 30-mg capsule. Blood samples were drawn at various time points after each period (0-48 h), and analyzed for plasma concentration of temazepam. The washout period between doses was five days. MAIN OUTCOME MEASUREMENTS: Five parameters of both dosage forms were compared: (1) area under curve (AUC), (2) peak concentration (Cmax), (3) time to peak concentration (Tmax), (4) apparent rate constant for absorption, and (5) lag time for appearance of drug in plasma. Statistical procedures included ANOVA, power analysis, and confidence limits. RESULTS: The mean AUC for the four 7.5-mg capsules and one 30-mg capsule differed by less than 2 percent and the mean Cmax differed by less than 14 percent for the two dosage strengths; neither of these differences reached statistical significance (p > 0.05). The 7.5-mg capsules reached peak plasma concentrations significantly faster than the 30-mg dosage form (mean Tmax 1.18 and 1.73 h, respectively; p = 0.01). CONCLUSIONS: The two formulations of temazepam were bioequivalent with respect to the extent of bioavailability. Regarding the rate of absorption, however, the 7.5-mg capsules reached peak plasma concentrations significantly faster than the 30-mg dosage form.

Adolescent↗
PubMed2003

Improving daytime sleep with temazepam as a countermeasure for shift lag.

BACKGROUND: Working night shift (reverse cycle) presents problems to personnel due to the difficulty in maintaining alertness during the nighttime hours. When the shift must be worked several consecutive nights, a cumulative sleep debt is created. Appropriate countermeasures are required to help personnel obtain as much sleep as possible so they may perform their duties effectively. HYPOTHESIS: The objectives were to determine whether a hypnotic taken before daytime sleep would improve sleep quality, and to determine whether improved daytime sleep would increase alertness, reduce fatigue, and mitigate the usual performance decrements which occur on night shift. METHODS: Sixteen UH-60 Army aviators were randomly assigned to either a temazepam or a placebo group. Test sessions, consisting of vigilance assessments, flight simulation, and mood state questionnaires were administered during baseline, three nights of reverse cycle, and three days following a return to day shift. Temazepam (30 mg) was administered before daytime sleep to one group while another group received a lactose-filled capsule. RESULTS: Subjects who received temazepam slept longer and with less fragmentation than those who received placebo. Generally, the subjects in the temazepam group indicated more subjective alertness and less fatigue than those in the placebo group. Flight performance was not unequivocally improved by better daytime sleep, but the temazepam group performed better on the Psychomotor Vigilance Task than the placebo group. CONCLUSIONS: Temazepam is helpful in prolonging daytime sleep, with some attenuation of performance decrements during the night shift. However, physicians should be careful when administering this substance to ensure the aviator has a minimum of 8 h in which to sleep.

Administration, Oral↗
PubMed2001

Comparative efficacy of zolpidem and temazepam in transient insomnia.

This study compared hypnotic effects of zolpidem 10 mg, temazepam 15 mg and placebo in healthy adults. Two factors expected to promote insomnia, the 'first night effect' and a 2-hour phase advance, were combined in a single night laboratory-based double-blinded protocol. This was a multi-center study, with data collected in 13 sleep laboratories. Subjects with normal sleep histories and without prior sleep laboratory experience were randomly assigned to treatment groups. Medications were administered 15 min before lights out, with polysomnographic monitoring for 7.5 h. Subjective questionnaires and performance tests, digit symbol substitution test (DSST) and symbol copying test (SCT), were administered at study entry and after arising. 630 subjects completed the study and provided data analyzed using repeated measures ANOVAs. Neither agent significantly reduced objective sleep latency relative to placebo. Zolpidem reduced awakenings and wake after sleep onset (WASO); temazepam did not. Both agents improved sleep efficiency and most subjective sleep measures relative to placebo, with zolpidem superior for five of six subjective outcome measures compared to temazepam. SCT, morning sleepiness and morning concentration were not altered by any treatment. Zolpidem significantly reduced morning DSST performance; temazepam did not. Zolpidem 10 mg provided greater subjective hypnotic efficacy than temazepam 15 mg in this model of transient insomnia, with reduced polysomnographic awakenings and WASO. Impairment of DSST was seen with zolpidem but not temazepam. Copyright 2001 John Wiley & Sons, Ltd.

Journal Article↗
PubMed2001

Placental transfer of temazepam and fentanyl in early human pregnancy.

The placental transfer of temazepam and fentanyl was studied in 37 women undergoing surgical termination of pregnancy between 12 and 17 weeks. The women received temazepam 10 mg, approximately 1 h pre-operatively and fentanyl 2 &mgr;g/kg intravenously, at induction of anaesthesia. A single 2 ml fetal blood sample was taken from each anaesthetized subject using an ultrasound-guided trans-abdominal puncture at either 5, 10, 15 or 20 min after administration of fentanyl. A maternal blood sample was collected simultaneously and both were assayed for temazepam and fentanyl. Both drugs were detected in all fetal serum samples. Fetal:maternal (F:M) drug concentration ratio was 0.38 for temazepam, which did not change between 60 and 120 min after oral administration to the mother. Overall F:M ratio for fentanyl was 1.87 for fentanyl, which increased from 1.42 at 5 min to 2.6 at 20 min. F:M ratio of fentanyl concentrations increased with time (r = 0.48, P < 0.003), whereas F:M ratio of temazepam concentrations did not change significantly with time, between 50 and 120 min after the drug was administered to the mother (r = 0.32, P = 0.06). F:M ratios changed with gestational age of the fetus for both drugs, increasing as gestational age increased in the case of temazepam (r = 0.47, P = 0.003) and decreasing in the case of fentanyl (r = 0.38, P = 0.02). These changes can be explained by variation in uterine blood flow, trophoblast membrane thickness and feto-placental metabolism. These results also indicate that the in-vitro study of these drugs is unlikely to reflect the in-vivo situation in early pregnancy.

Journal Article↗
PubMed1996

Pharmacokinetic aspects of rectal formulations of temazepam.

An in vitro/in vivo study was carried out with different rectal formulations of temazepam. Pharmacokinetic data were determined in a cross-over study in 10 volunteers after rectal administration of 10 mg temazepam as a polyethylene glycol based suppository (selected from in vitro data), a liquid-filled capsule and a micro-enema respectively, using oral administration of a liquid-filled capsule as a reference. Serum levels of temazepam indicate an instantaneous and complete release from the micro-enema (Frel = 0.94 +/- 0.21, Cmax 205 +/- 36.9 micrograms/l, tmax 0.49 +/- 0.31 hour) and a slower but complete release of temazepam from the suppository (Frel = 1.10 +/- 0.25, Cmax 202 +/- 41.3 micrograms/l, tmax 1.48 +/- 0.41 hour). A high interindividual variation in absorption profiles was observed after rectal administration of the liquid-filled capsule (Frel 0.72 +/- 0.36, Cmax 182 +/- 122 micrograms/l, tmax 4.08 +/- 4.28 hour), which makes it less suitable for rectal use. The micro-enema and suppository appear to be useful as rectal formulations for temazepam.

Administration, Rectal↗
PubMed1987

Pharmacokinetics of temazepam after day-time and night-time oral administration.

The pharmacokinetic disposition of temazepam was compared after a day-time and night-time dose in an open randomised crossover study. Twelve healthy male volunteers received a single oral dose of 20 mg temazepam in a soft gelatine capsule at 0900 h or 2200 h. Blood samples were taken immediately before dosing and at selected times over the 36-h period after each dose. The absorption of temazepam was slower after evening administration; the absorption half-life and time to reach maximal plasma concentration being 0.53 h and 1.67 h respectively, compared to 0.38 h and 1.02 h following morning administration. Considering distribution characteristics, evening administration produced a lower peak plasma temazepam concentration (362 ng/ml) compared with a day-time level of 510 ng/ml. Distribution half-life after night-time administration was increased compared with day-time administration (1.76 h vs 1.03 h). A significantly higher percentage of the drug, relative to Cmax, remained in the plasma at 8 and 24 h after evening dosing (39.3 and 15.4% compared to 24.7 and 11.2% following day-time administration). In spite of the half-lives of absorption, distribution and elimination all being longer after the evening dose, the overall bioavailability, as measured by the area under the curve (AUC) was comparable after the two times of administration. Similarly the difference in the mean residence time (MRT) of the two doses was within accepted limits. It is concluded that a chronopharmacokinetic effect was seen for temazepam; however it is unlikely to be of any clinical significance.

Administration, Oral↗
PubMed1991

Direct high pressure liquid chromatographic analysis and preliminary pharmacokinetics of enantiomers of oxazepam and temazepam with their corresponding glucuronide conjugates.

Three high pressure liquid chromatographic systems for the separation of oxazepam, temazepam and their glucuronides (system A), the separation of their R,S glucuronide diastereomers (system B) and the chiral separation of the parent drugs (system C) are described. Preliminary pharmacokinetics of R,S-oxazepam and R,S-temazepam in a human volunteer reveal that the protein binding of the glucuronides is lower than that of the parent drugs, but that there is no difference in protein binding between the R-oxazepam/temazepam and S-oxazepam/temazepam and their corresponding glucuronides. The S-glucuronide is the main metabolite formed and excreted by man. The plasma ratio R/S-glucuronide is 1:1 for both oxazepam and temazepam. The renal clearance of R-temazepam, and S-temazepam are similar, and those of R-oxazepam and S-oxazepam tend to be different.

Chromatography, High Pressure Liquid↗
PubMed1989

Temazepam withdrawal in elderly hospitalized patients: a double blind randomised trial comparing abrupt versus gradual withdrawal.

31 of 36 elderly mainly confused hospitalized patients (69-98 years) taking temazepam 10 mgs nocte for more than one month completed a double blind randomised placebo controlled trial comparing abrupt versus gradual withdrawal of temazepam. Hours of sleep were recorded for all patients during a 7 day baseline period while taking temazepam 10 mg nocte. Then the abrupt withdrawal (AW) group (n = 15) received placebo for 10 nights and the gradual withdrawal (GW) group (n = 16) received temazepam 5 mg for the first 4 nights, 2 mg for the next 4 nights and placebo for the last 2 nights. There was no significant difference in mean hours of nightly sleep during the baseline period between the AW group (5.9 +/- 1.1 SD) and GW group (5.8 +/- 1.1 SD) and between the baseline and withdrawal periods in each group (withdrawal periods, AW 5.6 +/- 1.2, GW 5.6 +/- 1.0). There was no rebound insomnia when temazepam was withdrawn either abruptly or gradually in long-term hospitalised elderly patients and may not be effective as a long-term hypnotic.

Aged↗
PubMed1989

Substitution of temazepam and midazolam in pentobarbital-dependent rats.

The ability of temazepam and midazolam to substitute for pentobarbital and thus maintain the physical dependence state was used to assess the potential dependence liability of these two benzodiazepine compounds. Male Sprague-Dawley rats, weighing 175-200 g and having ad lib access to food and water, were determined to be dependent on pentobarbital following 12 days of continuous, intraperitoneal infusion of pentobarbital using an escalating drug infusion schedule. On day 13 (substitution phase) the pentobarbital was replaced with either temazepam, midazolam or vehicle and the rats were infused for an additional 24 hours. This was followed on Day 14 (withdrawal phase) by a 24 hr saline infusion period. Rats were observed for changes in overt behavior and alterations of body weight during both Day 13 and Day 14. Preliminary potency estimation studies had indicated that both drugs were more potent and longer acting than was pentobarbital. Temazepam, in doses of 32.5, 65 and 130 mg/kg/24 hr, was demonstrated to substitute for pentobarbital and provided dose-dependent suppression of overt behavioral signs indicative of withdrawal. Temazepam also suppressed the weight loss typically observed during withdrawal. Substitution of saline for temazepam resulted in an increased incidence of withdrawal signs and an approximate 10% decline in body weight. Midazolam, in doses of 60 and 120 mg/kg/24 hr, also substituted for pentobarbital and suppressed both overt behavior and weight loss. Following saline substitution on Day 14, a mild withdrawal syndrome was evident although body weight was noted to remain near control values.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1986

Quazepam and temazepam: effects of short- and intermediate-term use and withdrawal.

Two benzodiazepine hypnotics, one with an intermediate elimination t1/2 (temazepam, 15 mg) and the other with a long t1/2 (quazepam, 15 mg), were evaluated in 22- night sleep laboratory studies. The effectiveness and side effects of these benzodiazepines were assessed during short- and intermediate term use. Subjects were also assessed for the presence of rebound insomnia after abrupt withdrawal. Quazepam, 15 mg, was significantly effective in improving sleep both with short- and intermediate-term use, but the effectiveness of temazepam was considerably less. Although temazepam was effective for maintaining sleep with short-term use, there was rapid development of tolerance for this effect with intermediate-term use. Temazepam did not produce any behavioral side effects during either drug condition. The only side effect associated with quazepam was a significant degree of daytime sleepiness. After its withdrawal, temazepam was associated with some sleep and mood disturbance on the first withdrawal night, whereas quazepam had carryover effectiveness.

Adult↗
PubMed2006

Temazepam triggers the release of vasopressin into the rat hypothalamic paraventricular nucleus: novel insight into benzodiazepine action on hypothalamic-pituitary-adrenocortical system activity during stress.

We investigated the influence of a representative classical benzodiazepine on the regulation of the hypothalamic-pituitary-adrenocortical (HPA) axis activity both under basal conditions and stress. Adult male Wistar rats were intravenously administered with temazepam (0.5, 1, and 3 mg/kg body weight) and plasma concentrations of corticotropin (ACTH) and vasopressin (AVP) were measured in blood samples collected via chronically implanted jugular venous catheters. Simultaneously, the release of AVP within the hypothalamic paraventricular nucleus (PVN) was monitored via microdialysis. Plasma AVP levels remained unaffected by the different treatment conditions. Temazepam blunted the stressor exposure-induced secretion of ACTH in a dose-dependent manner. Concurrently, and also in a dose-dependent manner temazepam enhanced the intra-PVN release of AVP, known to originate from magnocellular neurons of the hypothalamic neurohypophyseal system. Furthermore, temazepam did not affect the in vitro secretion of ACTH from the adenohypophyseal cells. Taken together, the results of this study suggest that temazepam modulates the central nervous regulation of the HPA axis by altering intra-PVN AVP release. An increasingly released AVP of magnocellular origin seems to provide a negative tonus on ACTH secretion most probably via inhibiting the release of ACTH secretagogues from the median eminence into hypophyseal portal blood.

Adrenal Cortex Hormones↗
PubMed2000

Gastric decontamination performed 5 min after the ingestion of temazepam, verapamil and moclobemide: charcoal is superior to lavage.

AIMS: The aim was to study the efficacy of gastric lavage and activated charcoal in preventing the absorption of temazepam, verapamil and moclobemide when gastric decontamination was performed immediately after ingestion of the drugs. METHODS: Nine healthy volunteers took part in a randomized cross-over study with three phases. The subjects were administered single oral doses of 10 mg temazepam, 80 mg verapamil and 150 mg moclobemide. Five minutes later, they were assigned to one of the following treatments: 200 ml water (control), 25 g activated charcoal as a suspension in 200 ml water or gastric lavage. Plasma concentrations and the cumulative excretion into urine of the three drugs were determined up to 24 h. RESULTS: The mean AUC(0,24 h) of temazepam, verapamil and moclobemide was reduced by 95.2% (P < 0.01), 92.8% (P < 0.01) and 99. 7% (P < 0.01), respectively, by activated charcoal compared with control. Gastric lavage did not reduce significantly the AUC(0,24 h) of these drugs. The 24 h cumulative excretion of temazepam, verapamil and moclobemide into urine was reduced significantly (P < 0.05) by charcoal but not by gastric lavage. Charcoal reduced the AUC(0,24 h), Cmax and urinary excretion of all three drugs significantly more than lavage. CONCLUSIONS: Activated charcoal is very effective and gastric lavage can be rather ineffective in preventing the absorption of temazepam, verapamil and moclobemide when the treatment is given very rapidly after ingestion of the drugs, before tablet disintegration has occurred.

Absorption↗
PubMed2003

Neurobehavioural performance effects of daytime melatonin and temazepam administration.

Exogenous melatonin is a potential treatment for circadian disruption and insomnia. Hence, it is important to determine and quantify neurobehavioural performance effects associated with its use. The present study compared neurobehavioural performance following administration of melatonin and the benzodiazepine temazepam, using a within-subjects design. Following a training day, 16 healthy, young subjects (six males, 10 females; mean age +/- SEM, 21.4 +/- 6 years) participated in a 3-day protocol. After sleeping overnight in the laboratory, subjects completed a battery of tests at hourly intervals between 08:00 and 11:00 hours and at two hourly intervals between 13:00 and 17:00 hours. The neurobehavioural performance tasks included: unpredictable tracking, spatial memory, vigilance and logical reasoning. Subjective sleepiness was measured at hourly intervals using a visual analogue scale. At 12:00 h subjects were administered a capsule containing 5 mg melatonin, 10 mg temazepam or placebo, in a randomized, double-blind crossover fashion. A significant drug x time interaction was evident on the unpredictable tracking, spatial memory and vigilance tasks (P < 0.05). Greater changes in performance were evident following temazepam administration than melatonin administration, relative to placebo. Administration of melatonin or temazepam significantly elevated subjective sleepiness levels, relative to placebo (P </= 0.05). The present findings demonstrate that melatonin administration induces a smaller deficit in performance on a range of neurobehavioural tasks than temazepam. Given melatonin's soporific and chronobiotic properties, these results suggest that melatonin may be preferable to benzodiazepines in the management of circadian and sleep disorders.

Adult↗
PubMed2003

Association of benzodiazepine injection with the prescription of temazepam capsules.

Temazepam capsules have become a popular choice for benzodiazepine injection by injecting drug users, and serious vascular and tissue damage leading to ulcers and gangrene can result. We compared the self-reported benzodiazepine injecting behaviour of 91 heroin users with their Pharmaceutical Benefits Schedule (PBS) records for the preceding 5 years. We found that individuals prescribed PBS temazepam capsules were more likely to report injecting benzodiazepines than individuals who had either not been prescribed PBS temazepam capsules or had been prescribed PBS temazepam tablets. These results provide empirical support for the argument to limit the prescription and supply of temazepam capsules in Australia.

Adolescent↗
PubMed1986

Temazepam and trimeprazine compared with placebo as premedication in children. An investigation extended into the first 2 weeks at home.

Temazepam, trimeprazine and placebo were compared as premedication in 85 children undergoing routine otolaryngological operations. Premedication with trimeprazine caused significantly more sedation than temazepam or placebo in patients on arrival in the anaesthetic room (P less than 0.02). Recovery time was significantly longer after trimeprazine than temazepam or placebo (P less than 0.012). Significantly more children (P less than 0.05) failed to recall a picture shown immediately before induction after trimeprazine and temazepam than with placebo. Fewer patients vomited after operation with trimeprazine than with temazepam or placebo (P less than 0.01). The majority of children exhibited some behavioural problem during the first 2 weeks at home, although this rarely lasted for more than a few days. More children exhibited apathetic/withdrawn behaviour after receiving placebo (P less than 0.05), although the significance of this should be interpreted with caution.

Anesthesia Recovery Period↗
PubMed1996

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

Zolpidem is an imidazopyridine hypnotic that is biochemically distinct from classic benzodiazepine agonists in that it may be selective for the BZ1 receptor subtype and shows a different pattern of distribution of binding sites. The present study compared the learning, recall, performance, subject-rated and observer-rated effects of zolpidem, triazolam, and temazepam in 11 healthy humans. Placebo, zolpidem (5, 10, and 20 mg/70 kg), triazolam (0.125, 0.25, and 0.50 mg/70 kg), and temazepam (15, 30, and 60 mg/70 kg) were administered orally in a randomized, double-blind, cross-over design. 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. The absolute magnitude of these effects at peak effect were comparable across the three compounds. The time to maximal drug effect was faster with zolpidem (0.5-1.0 hours) than with triazolam (1.5-2.0 hours) or temazepam (2-3 hours). These results suggest that despite the somewhat unique benzodiazepine receptor-binding profile of zolpidem, its behavioral and subject-rated effects are similar to those of benzodiazepine hypnotics (i.e., triazolam and temazepam).

Adult↗