Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Nitrazepam”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 73 records · Page 4Linked to original sources
PubMed1980

Residual effects of hypnotics: triazolam, flurazepam, and nitrazepam.

The residual effects of three hypnotics were investigated by the method of 24-h polygraphy (EEG, EMG, and EOG). The drugs were triazolam 0.25 mg and 0.5 mg, flurazepam 15 mg and 30 mg, nitrazepam 5 mg and 10 mg, and placebo. The subjects were healthy volunteers, eight men and eight women with an average age of 34.3 years. The number of total polygraphic records was 77. Triazolam 0.25 mg and 0.5 mg, flurazepam 30 mg, and nitrazepam 10 mg showed definited sleep inducing and sleep maintenance effects in night recordings. Flurazepam 15 mg and 30 mg and nitrazepam 5 mg and 10 mg were followed by residual effects in morning, afternoon and evening recording periods on the day after the administrations of the hypnotics. However, no effects were seen on the day after the administration of triazolam 0.25 mg and 0.5 mg except for some slight residual effects in the morning. Thus triazolam 0.25 mg and 0.5 mg produces less residual effect than do flurazepam 15 mg and 30 mg, and nitrazepam 5 mg and 10 mg, and 24-h polygraphy is useful for measuring the residual effects of hypnotics.

Adult↗
PubMed1984

Objective and subjective assessment of hangover during subacute administration of temazepam and nitrazepam to healthy subjects.

Fourteen, healthy students volunteered for a double-blind, cross-over trial of temazepam 20 mg (soft gelatine capsule), nitrazepam 10 mg (uncoated tablet) and placebo in matched formulations, single doses of each being given for 10 nights with a three-week wash-out period between each treatment. Residual drug effects were measured objectively (psychomotor skills) and subjectively (visual analogue scales) in the morning and afternoon of Days 0 (before the first tablet), 1 and 10. The subjects also recorded various events during each treatment period. Serum benzodiazepine concentrations were bioassayed in blood samples taken after the last assessment. Both benzodiazepines shortened sleep latency during the first few nights, and nitrazepam prolonged the duration of sleep. The residual effect of drowsiness was noted during the nitrazepam period, whilst temazepam proved less sedating. The 'morning after' effect was a subjective observation and not an objective measurement. The learning effect interfered with the complex objective assessments, and simple measurement of exophoria with the Maddox wing test provided the clearest objective evidence of drug effects. On Day 10 residual concentrations of nitrazepam were detectable in the serum whereas the level of temazepam was found to be low or negligible. It is concluded, that temazepam 20 mg in a soft gelatine capsule is a suitable hypnotic for subjects whose daily work requires constant alertness.

Activity Cycles↗
PubMed1987

A comparison of oral midazolam, nitrazepam and placebo in young and elderly subjects.

Twelve young and twelve elderly subjects received a single dose orally of midazolam 15 mg, nitrazepam 5 mg and placebo in a double-blind, crossover comparison. Midazolam acted rapidly, producing a deep sleep at 1 h in fifteen subjects compared to two after Nitrazepam and none after placebo. No comparison of psychomotor tests was possible at this time, but such tests showed that there was no detectable subjective or objective psychomotor impairment at 4 h postdose with either drug. However, the EEG scores strongly suggested that volunteers were more sleepy at 8 h after nitrazepam in comparison to placebo or midazolam. Both groups appeared to handle the drug in a similar manner, there being no significant differences between the groups in the plasma concentration time curves of nitrazepam, or midazolam. The elderly had higher concentrations of alpha-hydroxymidazolam. This accounted for a small proportion of the total plasma benzodiazepine concentration, and the mean area under the curve for midazolam and metabolite was not significantly different in the old from that in the young.

Adult↗
PubMed1992

Benzodiazepine-induced sedation and cortisol suppression. A placebo-controlled comparison of oxazepam and nitrazepam in healthy male volunteers.

The sedative and cortisol suppressing properties of oxazepam (45 and 60 mg) and nitrazepam (10 and 15 mg) were examined in eight healthy male subjects. The most clear differences between oxazepam and nitrazepam were those seen with respect to the time course and until maximal effect (Tmax) of the different measurements. Nitrazepam showed maximal sedation after 1 h, maximal benzodiazepine level (RRA), and reaction time prolongation after 2 h, and maximal cortisol suppression after 3 h. Oxazepam showed maximal sedation after 2 h, maximal benzodiazepine levels, reaction time prolongation and cortisol suppression after 3 h. After administration of oxazepam (both doses) a transient return to baseline levels of cortisol was demonstrated. Whereas the degree of sedation correlated significantly within drug groups with the concurrent benzodiazepine levels, the Tmax of sedation was recorded 1 h earlier than the peak blood concentration (RRA) for both nitrazepam and oxazepam. The time course for cortisol suppression for the two compounds differed clearly from the other measurements and was not related to the peak blood concentration.

Affect↗
PubMed1985

The biliary elimination of amaranth, indocyanine green and nitrazepam in germ-free rats.

In anaesthetised bile duct-cannulated rats the overall rate of bile flow was 15-50% lower in both male and female germ-free (GF) rats. Except in the case of amaranth in female GF rats, this was reflected in a lower rate of biliary excretion of the three test xenobiotics, of which two (amaranth and indocyanine green) are excreted unchanged and one (nitrazepam) is excreted solely as metabolites. It was also noted that compared with conventional (CV) rats the relative liver weights (g/kg body weight) were about 20% lower in GF animals. After the intravenous injection of 14C-nitrazepam, thin-layer chromatographic separation of biliary nitrazepam-derived radioactivity revealed three loci (A, B and C in decreasing order of polarity). The relative proportions of A, B and C were similar in GF and CV rats, with C and B being the major and minor "metabolites" respectively. When 14C-nitrazepam was given intragastrically to non-anaesthetised rats, by 9 days about 20% and 70% of the dose had been recovered in the urine and faeces respectively of both GF and CV rats. The rate of elimination of urinary radioactivity was similar in GF and CV rats. However, faecal elimination was much slower in GF animals, for example after 24 hr the respective amounts of radioactivity excreted in GF and CV rats corresponded to 13% and 52% of the dose. These findings indicate that the indigenous bacterial population of an animal may indirectly affect the disposition of a xenobiotic whether or not it is metabolised by the bacteria.

Amaranth Dye↗
PubMed1994

Fluoxetine potentiates nitrazepam-induced behavioral sleep in young chicks.

Nitrazepam (0.5-10 mg/kg, IP) dose dependently induced behavioral sleep in day-old chicks. Fluoxetine (0.1-1 mg/kg) did not produce sleep in the young birds, but the 5-HT reuptake inhibitor (0.1 and 0.5 mg/kg) potentiated nitrazepam (0.5 and 1.0 mg/kg)-induced hypnosis. Doses (0.5 and 1 mg/kg) of the benzodiazepine that did not produce sleep in any or all the chicks, when administered alone, induced sleep in some or all the chicks in the presence of fluoxetine (0.1 and 0.5 mg/kg). Ketanserin (0.5 and 2.5 mg/kg) effectively antagonized the effect of fluoxetine on nitrazepam-induced behavioral sleep. These results suggest that enhancement of 5-HT level by fluoxetine may be the mechanism involved in the potentiation of nitrazepam-induced sleep in the young chicks.

Animals↗
PubMed1977

Nitrazepam premedication for minor surgery.

Sixty-one patients received nitrazepam 5 mg by mouth on the night before operation, followed by 2.5 mg given on the morning of operation and were compared with 60 patients who received no premedication. All were undergoing either therapeutic abortion, by dilatation and curettage, or explorative curettage. The plasma concentrations of nitrazepam were determined by gas chromatography and compared with the clinical effects of the drug. The premedicated patients slept better on the night before operation, and were more sedated and less apprehensive. Headache was more frequent following nitrazepam. There was no significant difference between the groups in respect of dizziness and nausea. The unpremedicated patients had a faster average heart rate. There was no obvious relationship between the plasma concentration of nitrazepam and the quality of sleep, degree of sedation, apprehension, excitement or headache.

Administration, Oral↗
PubMed1987

Zopiclone versus nitrazepam: a double-blind comparative study of efficacy and tolerance in elderly patients with chronic insomnia.

A randomized, double-blind, comparative trial of zopiclone versus nitrazepam was conducted in 74 geriatric chronic insomniac patients. Following a 7-day wash-out period, two parallel groups, successively received a placebo for 7 days, then either 7.5 mg zopiclone or 5 mg nitrazepam for another 7-day period. Efficacy on sleep was assessed by a sleep analogue scale and the Spiegel Sleep Questionnaire, residual effects by psychometric tests and tolerance by a standardized question, as well as by clinical and laboratory tests. Zopiclone and nitrazepam were more active than placebo on all tests of efficacy. In contrast with nitrazepam, zopiclone was devoid of effect on neurological function. In addition, the condition on awakening was better with zopiclone.

Aged↗
PubMed1977

Cerebrospinal-fluid concentrations of nitrazepam in man.

The concentrations of nitrazepam in the plasma and cerebrospinal-fluid (CSF) of 38 neurological patients were determined by gas chromatography 2-36 hours after a single 5 mg oral dose. The percentage ratio between the mean CSF and the plasma concentrations increased from 8.0% at 2 hours to 15.6% at 36 hours. This percentage rise was significant (P less than 0.001). The maximum concentration of nitrazepam in the plasma was 36.7 +/- 5.7 ng/ml (at 2 hours) and CSF 3.0 +/- 0.3 ng/ml (at 4 hours). During the beta-phase the half-life of nitrazepam in plasma was about 27 hours and in the CSF markedly longer about 68 hours, indicating a very slow elimination of nitrazepam from the CSF.

Administration, Oral↗
PubMed1978

Degree of sedation obtained with various doses of diazepam and nitrazepam.

Using critical flicker fusion (CFF) determination and estimation of drowsiness in eight healthy volunteers the sedative-hypnotic effects of diazepam and mitrazepam were studied. Three dose levels of each drug were used, so that dose-effect curves could be produced. The most reliable results were obtained with the CFF method, and significant dose-effect relations could be demonstrated. The CFF deviation after diazepam initially related well to the concentration in blood serum, but after 4--6 hours the CFF depression vanished rapidly, while the drug concentration remained high. After nitrazepam the signs of drowsiness occurred similarly, while the drug concentration in serum showed on an average a slower rise. The effects began to disappear before the nitrazepam concentration had reached a peak. A rapid tachyphylaxis at the receptor sites seems to be responsible for this incongruity. Nitrazepam exerted significantly stronger sedative effects than diazepam, particularly when the respective serum concentrations were taken into account. This confirms that nitrazepam should be a more efficient sleeping drug, although diazepam also has considerable sedative-hypnotic action.

Adult↗
PubMed1979

Urinary elimination of nitrazepam and its main metabolites.

Nitrazepam and its main metabolites, 7-aminonitrazepam and 7-acetamidonitrazepam, free and conjugated, were determined in the human urine after a single oral dose of 5 mg. The determinations were performed by GLC method using 63Ni-EC-detector for unchanged nitrazepam and nitrogen selective detector for the metabolites. Unchanged nitrazepam was poorly eliminated through the kidneys (about 1% of the dose). The interindividual variation of total excreted urinary metabolites was large ranging between 848-4933 microgram (17-99% of the dose during 7 days). Of this amount conjugated metabolites made up 57%. The urinary half-lives of free and conjugated-7-aminonitrazepam were (mean and ranges) 44 (23-65) and 46 (25-69) hrs, and of 7-acetamidonitrazepam 12 (5-31) and 18 (5-46) hrs, respectively. The half-lives of the excreted amounts of the metabolites did not correlate with any pharmacokinetic parameter of unchanged nitrazepam in serum.

Administration, Oral↗
PubMed1986

The carry-over effects of triazolam compared with nitrazepam and placebo in acute emergency driving situations and in monotonous simulated driving.

Eighteen healthy volunteers of both sexes, aged 20-34, were tested in the morning while undertaking real car driving avoidance manoeuvres and during monotonous simulated driving after 1 and 3 nights of medication with triazolam 0.25 mg, nitrazepam 5 mg or placebo. The study was a double-blind, randomized, cross-over study, where a minimum of 7 days wash-out separated the 3 treatment periods. Nitrazepam was found to impair performance in the simulated task after 1 but not after 3 nights of medication. Performance in the triazolam condition was not significantly different from the other conditions on this task on either day. However, after one night of medication triazolam tended to score worse than placebo but better than nitrazepam. In real car driving a tendency was noted for nitrazepam to score worst, whereas the difference between placebo and triazolam was hardly noticeable. The same tendency appeared on both days.

Automobile Driving↗
PubMed1989

Difference spectrophotometric assay of nitrazepam in tablet formulations.

A difference spectrophotometric procedure is described for the assay of nitrazepam in tablet formulations. The method is based on the measurement of absorbance at 282 nm of a solution of the tablet extract in 0.1 M hydrochloric acid (pH 1) relative to that of an equimolar solution in 0.1 M sodium hydroxide (pH 13). The method is precise and selective for nitrazepam in the presence of the tablet excipients and 2-amino-5-nitrobenzophenone, the principal hydrolysis product of nitrazepam. The absence of a constant isosbestic point in the difference spectrum of nitrazepam during hydrolysis in alkaline solution indicates the presence of a previously unrecognized intermediate hydrolysis product.

Hydrogen-Ion Concentration↗
PubMed1977

Increased sensitivity to nitrazepam in old age.

The effects of a single 10 mg oral dose of nitrazepam were compared with those of a placebo in healthy young and old people. Both the young and the elderly slept better on three successive nights after nitrazepam but they felt less awake at 12 and 36 hours (P less than 0-01). Elderly people made significantly more mistakes in a psychomotor test than did the young, despite similar plasma concentrations of nitrazepam and half lives in the two groups. This difference in response to psychomotor testing is probably explained by an increased sensitivity of the ageing brain to the action of nitrazepam.

Adult↗
PubMed1994

Effects of zopiclone, triazolam, and nitrazepam on standing steadiness.

We examined the effects of the nonbenzodiazepine hypnotic zopiclone and the benzodiazepine hypnotics triazolam and nitrazepam on standing steadiness. Eight healthy volunteers received placebo, zopiclone (7.5 mg), triazolam (0.25 mg), and nitrazepam (5 mg) in a random-order, double-blind crossover design. Postural sway was assessed before and 1 and 2 h after drug administration using a stabilometer connected to a microcomputer. Triazolam significantly impaired standing steadiness. Zopiclone also impaired standing steadiness but the degree of impairment seemed to be less marked. Nitrazepam 5 mg had no significant effects on postural sway. Triazolam 0.25 mg, zopiclone 7.5 mg, and nitrazepam 5 mg, which are reported to be equipotent to each other as hypnotics, are not equipotent with respect to their effects on postural sway.

Adult↗
PubMed1984

A multicentre hospital study to compare the hypnotic efficacy of loprazolam and nitrazepam.

A multicentre, parallel group hospital study was carried out in 190 subjects with insomnia to compare the efficacy, incidence of hangover and the side-effects of loprazolam and nitrazepam. Following 2 nights single-blind phase on placebo, loprazolam (1.0 mg), nitrazepam (5.0 mg) or placebo was administered double-blind for 7 consecutive nights. Visual analogue scales and questions were used to rate efficacy. There was no statistically significant difference between loprazolam and nitrazepam for 'ease of getting to sleep', 'restfulness of sleep' and 'depth of sleep'. Like nitrazepam, loprazolam diminished the number of periods of wakefulness and made it 'easier to get to sleep again'. Subjective evaluation showed that hangover was not a feature of loprazolam. It did not affect morning alertness and patients thought they had improved balance and co-ordination while on this drug. These findings are in keeping with the evidence of other workers who have shown only minimal psychomotor impairment, if any, with loprazolam (1.0 mg). There was no statistically significant difference between treatments with respect to frequency or incidence of side-effects.

Adolescent↗
PubMed1996

Nitrazepam for refractory infantile spasms and the Lennox-Gastaut syndrome.

Infantile spasms and the Lennox-Gastaut syndrome are considered to be age-specific pediatric epileptic syndromes and together constitute a significant percentage of medically resistant seizures in childhood. Twenty children, ages 4 to 28 months (median, 12 months), with medically refractory infantile spasms or the Lennox-Gastaut syndrome, were treated with the investigational benzodiazepine nitrazepam in an open-label study. Daily dosage of nitrazepam ranged from 0.5 to 3.5 mg/kg, with a median dosage of 1.5 mg/kg, divided into two doses per day. Side effects included pooling of oral secretions (12 children) and sedation (six children); however, no serious side effects were seen. Responses to nitrazepam were as follows: five complete responses (cessation of all seizures), seven partial responses (greater than 50% reduction of seizures), and eight with no response. Median duration of response was 9 months (range, 4 to 16 months) in children with infantile spasms and 14 months (range, 8 to 26 months) in children with the Lennox-Gastaut syndrome. Nitrazepam is an effective anticonvulsant in this small cohort of children with medically refractory infantile spasms and the Lennox-Gastaut syndrome, resulting in a 25% response rate and only modest side effects.

Administration, Oral↗
PubMed1989

The effects of nitrazepam and flunitrazepam on oxygen desaturation during sleep in patients with stable hypoxemic nonhypercapnic COPD.

Serious respiratory depression has been described in COPD patients receiving hypnotics during acute exacerbations. There are few studies quantifying the effects of hypnotics on oxygenation during sleep in patients with stable hypoxemic COPD. In this study, the effects of single therapeutic doses of nitrazepam and flunitrazepam on SaO2, apneas during sleep and other sleep variables were measured in 14 COPD patients. All patients used theophylline. Sleep-induced decrease in mean SaO2 was 1.3 percent after placebo, 1.4 percent after nitrazepam and 1.9 percent after flunitrazepam (no significant differences). Sleep apneas were not more common or longer after nitrazepam or flunitrazepam, but sleep quality seemed to improve. It is concluded that oxygenation during sleep in these nonobese patients with stable hypoxemic nonhypercapnic COPD, all on maintenance theophylline therapy, was affected very little by single therapeutic doses of nitrazepam or flunitrazepam.

Aged↗