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PubMed1990

Acute and carry-over effects of brotizolam compared to nitrazepam and placebo in monotonous simulated driving.

Eighteen healthy volunteers of both sexes, aged 20-35 years, were tested in the morning after three nights of medication with brotizolam 0.25 mg, nitrazepam 5 mg or placebo on a monotonous simulated driving task. The effect measures were subsidiary auditory reaction time and time outside road. Measurements of self-rated alertness were carried out as well. No effects were demonstrated from treatments on either measure. Nitrazepam however tended to score worst on all measures, except time outside road which could not be analysed with respect to statistical significance because of an insufficient number of subjects leaving the road. Twelve of the subjects were also tested immediately after drug intake on the first night of each medication period. Reaction time decrement was observed in both active drugs conditions with no difference between the two. The other measures, however non-significant, pointed in the same direction with the greatest decrement for nitrazepam.

Adult↗
PubMed1972

Effect of nitrazepam in chronic obstructive bronchitis.

The effect of nitrazepam on ventilatory capacity and arterial blood gas tensions was studied in a double-blind controlled crossover trial in six patients with chronic obstructive bronchitis in ventilatory failure (raised Paco(2)). Nitrazepam produced a fall in ventilatory capacity and worsening of the ventilatory failure. In the sixth patient, while on the active drug, the Pao(2) fell from 48 to 35 mm Hg while the Paco(2) tension rose from 59.5 to 68 mm Hg. It is suggested that nitrazepam is contraindicated in patients with severe chronic obstructive bronchitis.

Aged↗
PubMed1985

Prolonged use of nitrazepam for epilepsy in children with tuberous sclerosis.

A case note study of 90 children with tuberous sclerosis showed that 56 had taken nitrazepam for seizures for from one month to 13 years. In 38 children nitrazepam was withdrawn but only two had immediate major seizures. Given that sleepiness, deterioration in motor skills, or ataxia seems to be associated in some children with treatment with nitrazepam, doctors may wish to review their long term prescriptions of this drug in children with tuberous sclerosis.

Adolescent↗
PubMed1976

Nitrazepam and temazepam: a comparative trial of two hypnotics.

A specially designed sleep questionnaire was used to assess the performance of the two hypnotic drugs. Psychiatric patients were given 5 mg nitrazepam or 10 mg temazepam in identical capsules, and were allowed more if necessary. A double-blind cross-over design was used. We found that 5-2 mg nitrazepam showed few differences from 13-2 mg temezepam. The two regimes produced fairly similar reports on patient satisfaction, quality of sleep, number of awakenings, depth of sleep and other variables. Patients on nitrazepam were a little more clear-headed in the morning, though they tended to wake later, sleep longer, and take more sleep over the 24-hour period. No toxicity was found with either drug over the 434 patient days of administration. In view of the advantages of the benzodiazepine drugs over their predecessors, we feel that it is worth exploring further the use of temazepam as a sleep inducing drug.

Adult↗
PubMed1979

Comparative trial of a new hypnotic (Finorgal) with nitrazepam and triclofos sodium.

Thirty patients complaining of insomnia were studied in a double-blind trial with crossover of Finorgal, nitrazepam and triclofos sodium. Finorgal given as a hypnotic produced similar results to nitrazepam and triclofos sodium in terms of induction of sleep, duration and quality of sleep, dream recall and morning 'hangover'. Reported side-effects were not serious and occurred less frequently in association with Finorgal treatment than with nitrazepam or triclofos sodium. Laboratory investigations gave no indication of the development of any drug toxicity during the three-week period of the trial.

Administration, Oral↗
PubMed1995

Male reproductive toxicity study of nitrazepam in rats.

The main focus of this study is the optimal administration period concerning toxic effects on male fertility in rats. To assess functional and morphological changes induced in the testis by nitrazepam, male rats were administered the drug at doses of 0, 20, 40 or 80 mg/kg during pre-mating periods of 2, 4 or 9 weeks and then the 2 weeks of mating. At the end of the administration period the animals were sacrificed and sperm number, motility, abnormalities and histopathological changes in the testis were examined. Decreases in testis weight, epididymis weight, number of sperm in the testis and sperm motility were observed in the 40 and 80 mg/kg sections of the 2, 4 and 9 week pre-mating treated groups. Mating with untreated females revealed no adverse effects on copulation rate in any group; however, a remarkable decrease in pregnancy rate was noted in the 80 mg/kg section of the 2, 4 and 9 week treated groups. On histological examination, various degrees of localized necrosis in the seminiferous epithelium and Leydig cell hyperplasia were observed in the testis. No clear changes were observed in the 20 mg/kg section of the 2 week pre-mating administration group, but at the 4 week time point, necrosis of spermatogenic cells began to appear. The primary morphological event was evident in spermatocytes with necrosis of the cytoplasm observed from 4 weeks after administration of nitrazepam, although sperm motility and sperm head counts were unaffected. From these findings, examination of sperm characteristics and histopathological changes in the testis are important parameters for evaluation of drugs inducing testicular damage. We conclude that a 4 week administration period is sufficient to detect effects of nitrazepam on male fertility.

Animals↗
PubMed1975

Comparative metabolic study of nimetazepam and its desmethyl derivative (nitrazepam) in rats.

1. Nimetazepam distributed more rapidly in the brain than its desmethyl derivative (nitrazepam). The brain concentration of the active metabolites of the former was about twice that of the latter at 1h after oral administration. 2. At least four kinds of reactions were involved in the biotransformation of nimetazepam and its desmethyl derivative (nitrazepam) : (i) demethylation at N-1, (ii) hydroxylation at C-3, (iii) reduction of the nitro group at C-7 to the amino group and (iv) subsequent acetylation of the amino group. 3. The 1-N-demethylation of nimetazepam was slow compared with the other three reactions. 4. Nimetazepam was rapidly hydroxylated at C-3, while the 3-hydroxylation of its desmethyl derivative (nitrazepam) was very slow. 5. The reduction of the nitro group at C-7 and subsequent acetylation were important routes for the excretion of these drugs.

Acetylation↗
PubMed1998

Pharmacodynamics and pharmacokinetics of a single oral dose of nitrazepam in healthy volunteers: an interethnic comparative study between Japanese and European volunteers.

Potential interethnic differences in drug disposition and effects between Japanese and white subjects hamper the registration in Japan of medications already used in Western countries. This double-blind, placebo-controlled, crossover study was conducted to compare the pharmacodynamics and pharmacokinetics of a single oral dose of nitrazepam (5 mg) in age- and sex-matched Japanese (n = 8) and white (n = 8) healthy volunteers. The study was performed in centers in Japan and the Netherlands using the same methods and study design. Subjects were individually matched for gender, age, and body stature. Drug effects were measured by means of saccadic and smooth pursuit eye movements and visual analog lines obtained from the scales of Bond and Lader. There were no pharmacokinetic differences between the Japanese and white subjects. Clearance of nitrazepam was 0.91 +/- 0.165 mL/min/kg and 1.17 +/- 0.492 mL/min/kg, and half-life (t1/2) was 22.1 +/- 4.96 hours and 21.5 +/- 7.51 hours for the Japanese and European groups, respectively. Pharmacokinetic parameters showed no significant correlation with age, height, or weight. The average time-effect curves for the different parameters were comparable between groups. Compared with placebo, both groups showed similar significant reductions in average peak velocity and increases in saccadic inaccuracy and reaction time. Visual analog scores showed clear sedation in the white subjects, but insignificant effects in the Japanese subjects. Smooth pursuit did not change significantly in either group. Slope and intercept of the concentration-effect relationships for saccadic peak velocity showed considerable intersubject variability, but no clear differences between groups. The pharmacokinetics and pharmacodynamics of nitrazepam were similar in matched healthy Japanese and white subjects. Interethnic comparative studies are feasible, and provide meaningful information about potential racial differences in disposition and action of drugs. Such studies can form a rational basis for comparative clinical trials.

Administration, Oral↗
PubMedDate not supplied

Intrastrain variations in anxiolytic effect of nitrazepam in mice.

This study investigated the individual differences in the baseline anxiety and anxiolytic effect of nitrazepam in Balb/c mice. Initially mice were sorted according into low, intermediate and high anxiety groups (LA, IA and HA) based on the number of entries to and time spent in open arms in elevated plus maze. Later, anxiolytic effect of nitrazepam (2 mg/kg, p.o) in LA, IA and HA mice was evaluated using hole board and light/dark tests. In Hole board test, LA mice made more number of head dippings and spent more time during head dippings, while HA mice made less number of head dippings and spent less time during head dipping when compared to that of IA mice. In light/dark test LA mice made more reentries to and spent more time in bright compartment, while HA mice made few reentries to and spent less time in bright compartment. Results suggest that mice of a single strain differ in their baseline anxiety and anxiolytic effect of nitrazepam.

Animals↗
PubMed1991

[Comparison of solid phase and liquid-liquid extraction of diazepam and nitrazepam].

We have developed a new extraction technique for nitrazepam and diazepam using Samplex C-18 column. The blood-extractions containing diazepam and nitrazepam were diluted with acetonitrile-water 7:3 eluent. Diazepam and nitrazepam were isolated using liquid-liquid extraction technique. The blood-extracts were diluted with chloroform-ethanol 1:1 and they were evaluated by using OPLC method. Evaluation was done by TLC-scanner (Shimadzu). The efficiency and sensitivity of the methods have been compared.

Chromatography↗
PubMed1990

Immediate and overnight effects of zopiclone 7.5 mg and nitrazepam 5 mg with ethanol, on psychomotor performance and memory in healthy volunteers.

The effects of ethanol (0.2-0.4 g/kg) taken in conjunction with a single nocturnal dose of zopiclone 7.5 mg or nitrazepam 5 mg, on the early morning performance were investigated by means of psychomotor tests in 9 female volunteers. While there was no noticeable difference in the Choice Reaction Time (CRT) for any of the drug-ethanol combinations and ethanol alone, the zopiclone combination appeared to be initially more sedative in the Critical Flicker Fusion test (CFF). Both drug combinations impaired short-term memory and induced retrograde amnesia to the same extent, although only the nitrazepam-ethanol treatment caused further anterograde amnesia as compared to ethanol alone. Finally, both drug-ethanol combinations exhibited equivalent hypnotic properties as assessed by the Leeds Sleep Evaluation Questionnaire (LSEQ) without any more residual effects than with ethanol alone. These results suggest neither zopiclone, nor nitrazepam potentiate the effects of ethanol at the doses used.

Adolescent↗
PubMed1990

Comparative effects of rifampin and/or probenecid on the pharmacokinetics of temazepam and nitrazepam.

The pharmacokinetics of nitrazepam and temazepam were investigated in 16 healthy volunteers before and after seven days of the administration of rifampin 600 mg/d and/or probenecid 500 mg/d. In order to determine the endoplasmatic reticulum enzyme function, 6-beta-hydroxycortisol excretion and antipyrine pharmacokinetic parameters were evaluated. After the administration of rifampin, the total body clearance of antipyrine and nitrazepam increased by 87% and 83%, respectively. After the combined treatment with rifampin and probenecid, the elimination of the two drugs was also increased, even though to a lesser extent (33%, 31%). After the administration of probenecid only, the total clearances of antipyrine and nitrazepam were decreased by 22% and 25%, respectively. The urinary clearance of the antipyrine metabolites also decreased. In norantipyrine and 4-OH-antipyrine, this was due to a significant reduction of glucuronide fraction (211 +/- 32 to 159 +/- 26 mg, and 259 +/- 39 to 191 +/- 25 mg). The sulphate fraction of norantipyrine increased by 18% and that of 4-OH-antipyrine by 21%. Apart from a reduced excretion of the glucuronide fraction, the pharmacokinetics of temazepam were neither altered significantly by probenecid nor by rifampin. According to the outcome of this investigation, probenecid seems to bring about not merely an inhibition of phase II but also an inhibition of phase I metabolization.

17-Hydroxycorticosteroids↗
PubMed1988

A double-blind comparison between nitrazepam, lorazepam, lormetazepam and placebo as preoperative night sedatives.

Benzodiazepines are used as hypnotics to reduce anxiety and give a good night's sleep on the night prior to surgery. In a double-blind procedure, patients were given either lorazepam (2 mg or 4 mg), lormetazepam (1 mg or 2 mg), nitrazepam 10 mg or placebo. Measures were taken of sleep, anxiety, memory and after-effects. There was no evidence that the drugs reduced anxiety, nor evidence of amnesia. Quality and length of sleep was shown to be better for nitrazepam (P less than 0.05), lorazepam 2 mg (P less than 0.05) and lorazepam 4 mg (P less than 0.01), compared with placebo. However, significantly higher ratings of clumsiness and confusion as after-effects were found with nitrazepam (P less than 0.05), and clumsiness (P less than 0.005), slurred speech and blurred vision (P less than 0.01), sleepiness, nausea, weakness and confusion (P less than 0.05) with lorazepam 4 mg. It was concluded that lorazepam 2 mg produced the greatest net benefit.

Adult↗
PubMed1981

Differential inhibition by diazepam and nitrazepam of UDP-glucuronyltransferase activities in rats.

To assess the role of the N-alkyl group in the interaction of N-alkylated compounds on UDP-glucuronyltransferases, the effect of diazepam and nitrazepam, an N-desmethyl derivative of the diazepam class was studied on morphine, p-nitrophenol and testosterone glucuronidation in rats. Diazepam competitively inhibited the UDP-glucuroyltransferase activity for morphine in hepatic microsomes. The k value for morphine was 0.3 mM and the Ki for diazepam was about 0.23 mM. Also, diazepam administration to male rats reduced the glucuronyltransferase activity for morphine in rat hepatic microsomes in a dose effect relationship. Nitrazepam had no significant effect on morphine UDP-glucuronyltransferase activity in vitro or in in vivo experiments. Neither diazepam nor nitrazepam produced any effect on p-nitrophenol or testosterone glucuronidation in liver microsomal preparations. Single or repeated doses of these benzodiazepines did not change cytochrome P-450, RNA or protein contents of hepatic microsomes. It is suggested that morphine glucuronyltransferase contains an active site for binding of the N-methyl group present in the substrate. Such a binding site would be absent or in effective in p-nitrophenol and testosterone glucuronyltransferases. The reported inhibition of morphine metabolism by diazepam may account for an enhancement of morphine pharmacological effects.

Animals↗
PubMed1982

Anti-metrazol effects of nitrazepam during ontogenesis in the rat.

Anti-metrazol effect of nitrazepam was studied in male rats aged 7, 12, 18 and 90 days. Nitrazepam protected all age groups against seizures elicited by metrazol (80 mg/kg s.c.); the 50%-protective dose decreased from 165.7 micrograms/kg in adult rats to 70.2 micrograms/kg in 7-day-old animals. The sensitivity of 7-day-old and adult rats to metrazol is nearly the same, so that we may conclude that nitrazepam exhibits higher anti-metrazol potency in 7-day-old rats than in adult ones.

Age Factors↗
PubMed1980

[Study of vigilance after ingestion of zopiclone in comparison with nitrazepam and placebo (author's transl)].

Increasing importance is being given to the residual effects of hypnotics on the day following absorption; with zopiclone, a new hypnotic, we have studied vigilance 9, 12 and 15 hours after a single evening dose of 10 mg, on a double-blind basis in comparison with 10 mg of nitrazepam and a placebo. The assessment of vigilance is based on responses to self-rating questionnaires and psychometric tests. Twenty-one healthy subjects forming a homogeneous group as regards age, I.Q., and vigilance were included in this study. Each subject received the three products in random distributed order, with an interval of three months between each trial. The results of these tests reveal modifications which, particularly 9 hours after administration, reflect a modification in vigilance, appearing to be more marked with nitrazepam than with zopiclone. Thus, from the point of view of the residual effects of hypnotics on vigilance, it is possible to position the products tested in the following order: placebo -- zopiclone -- nitrazepam.

Arousal↗
PubMedDate not supplied

Pharmacodynamics and pharmacokinetics of psycholeptic drugs in the course of radiation disease. Effect of premedication with metanabol on dynamics and kinetics of nitrazepam.

The effect of metanabol given to rats before irradiation (600 R) on exploring motility and cataleptic action of nitrazepam was investigated. The level of nitrazepam in the blood plasma and urine was determine. Most evident radioprotective effect of metanabol was found on 3rd day after irradiation. The drug inhibited the inhibited the increased response of the rats to the anticonvulsive action of nitrazepam and prevented the pharmacokinetic disturbances appearing in the course of radiation disease.

Animals↗
PubMed1970

Persistent behavioural and electroencephalographic changes after single doses of nitrazepam and amylobarbitone sodium.

In a double-blind cross-over trial the effects of nitrazepam (5 and 10 mg.), amylobarbitone sodium (100 and 200 mg.), and placebo were compared in normal healthy young people. Though they reported a good night's sleep and adjudged themselves to be alert after all four drug treatments, behavioural tests showed their performance to be significantly impaired 13 hours after treatment with nitrazepam or amylobarbitone, and E.E.G. records showed more drowsiness and light sleep 18 hours after treatment with nitrazepam than with amylobarbitone or placebo. E.E.G. fast activity was more plentiful after drugs in either dosage than with placebo.

Adolescent↗