Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0917801 (
insomnia
)
10,606
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
We studied sleep and daytime function in insomniac patients who took either flurazepam, 30 mg, triazolam, 0.5 mg, or placebo 30 minutes before bedtime. Subjects were 21 patients with either a primary or a secondary diagnosis of chronic psychophysiological
insomnia
or
insomnia
associated with personality disorder. Seven subjects were randomly assigned to each condition. The study used a three group by 9 week, double-blind design with three nocturnal sleep recordings each week. During week 1, subjects took no capsules; week 2, subjects took placebo; weeks 3 to 7, flurazepam, triazolam, or placebo; weeks 8 and 9, placebo. Daytime tests for alertness and performance were administered during weeks 1, 3, 5, 7, and 8. Flurazepam showed hypnotic efficacy for weeks 3 to 5.
Triazolam
showed hypnotic activity for weeks 3 to 7. Although not significant overall, discontinuation of flurazepam produced rebound
insomnia
in six of seven subjects sometime during the two withdrawal weeks. The relationship between plasma concentration of desalkylflurazepam, the principal active metabolite of flurazepam, and sleep disturbance suggested that the onset of the rebound
insomnia
depended on the rate of drug washout. Discontinuation of triazolam produced a significant rebound
insomnia
on the first and second nights of drug withdrawal. Placebo subjects showed improved sleep throughout weeks 2 to 9 of the study. Daytime testing revealed significantly decreased daytime alertness and decreased performance for flurazepam subjects during weeks 3 to 7, although these effects reverted toward baseline despite continued drug administration.
...
PMID:Comparative hypnotic effects of flurazepam, triazolam, and placebo: a long-term simultaneous nighttime and daytime study. 614 Nov 88
Three benzodiazepine derivatives are currently indicated specifically for the treatment of
insomnia
in the United States. Flurazepam is biotransformed to at least two rapidly appearing and rapidly eliminated intermediate metabolites which probably contribute to sleep induction. The final metabolite, desalkylflurazepam, appears slowly, but has a long half-life ranging from 40 to 150 h. This metabolite accumulates extensively during multiple dosage. Temazepam is a slowly absorbed drug and has an intermediate half-life in the range of 10-20 h.
Triazolam
has an intermediate absorption rate, but is rapidly eliminated (half-life 1.5-5 h) making it essentially non-accumulating. Understanding of the pharmacokinetics of benzodiazepine hypnotics can contribute to understanding of their clinical properties.
...
PMID:Pharmacokinetics of benzodiazepine hypnotics. 614 69
Three benzodiazepine derivatives are currently indicated specifically for the treatment of
insomnia
in the United States. Flurazepam is biotransformed to at least two rapidly appearing and rapidly eliminated intermediate metabolites which probably contribute to sleep induction. The final metabolite, desalkylflurazepam, appears slowly, but has a long half-life ranging from 40 to 150 h. This metabolite accumulates extensively during multiple dosage. Temazepam is a slowly absorbed drug and has an intermediate half-life in the range of 10-20 h.
Triazolam
has an intermediate absorption rate, but is rapidly eliminated (half-life 1.5-5 h) making it essentially non-accumulating. Understanding of the pharmacokinetics of benzodiazepine hypnotics can contribute to understanding of their clinical properties.
...
PMID:Pharmacokinetics of benzodiazepine hypnotics. 614 83
Most people attribute a restorative function to sleep. This is because experimental or clinical sleep disturbance is usually followed by annoying symptoms of fatigue and sleepiness the following day. Can these daytime changes be documented objectively? In the past several years, the Multiple Sleep Latency Test (MSLT) has been developed and validated as an objective quantitative measure of sleepiness. Multiple assessments of sleep latency yield a profile of sleepiness across the day. This profile changes in the predicted direction with acute total and partial sleep deprivation, chronic sleep deprivation, sleep satiation, and in comparisons between hypersomnia patients and controls. Sleep and wakefulness are complementary phases in the daily cycle of human existence. Adequacy of sleep and energetic wakefulness next day are interacting phases in this cycle.
Insomnia
can be seen as a perception of disturbed sleep with daytime consequences, but is essentially also a symptom. This paper reviews a number of issues in the diagnosis and treatment of
insomnia
. The dimensions, daytime consequences and longitudinal aspects of
insomnia
are considered. Most investigations to date have been geared towards the problem of chronic
insomnia
and yet we are all likely to suffer from transient
insomnia
at some point. Psychiatric and psychophysiological disorders have been shown to be the most frequent causes of disorders of initiating and maintaining sleep. Moreover, there is an apparent disparity between subjective and objective sleep parameters with, for example, objectively disturbed sleep in noncomplaining subjects. The criteria of hypnotic efficacy and the effects of triazolam and flurazepam on sleep and daytime alertness have been investigated in normals, chronic insomniacs and the elderly. In general, chronic insomniacs showed all degrees of daytime alertness regardless of nocturnal sleep parameters. About one-third could be classified as fully alert all day long in spite of their complaints. The effect of flurazepam and triazolam on sleep (improvement) was essentially the same. Daytime effects were most closely related to half-life. The long-acting benzodiazepine, flurazepam, impaired daytime alertness although nocturnal sleep was improved.
Triazolam
improved not only nighttime sleep but also daytime alertness.
...
PMID:Issues in the diagnosis and treatment of insomnia. 638 52
To critically assess and summarize the beneficial effects of benzodiazepine therapy for
insomnia
in community-dwelling elders, a systematic search was undertaken to review all published clinical trials and sleep laboratory studies. The risk of injury for benzodiazepine users was also reviewed. Ten studies met inclusion criteria for assessing benefit. There are no studies regarding the long-term effectiveness of benzodiazepines for the treatment of sleep disorders in the elderly. In the sleep laboratory setting, triazolam 0.125 mg, flurazepam 15 mg, and estazolam 1 mg improved sleep latency by 27 to 30 minutes and increased total sleep time by 47 to 81 minutes for the first 2 to 3 nights of treatment, compared with baseline measurements taken while the patients were receiving placebo. In contrast to these modest short-term benefits, there is an association between the use of benzodiazepines with a long half-life, eg, flurazepam, diazepam, and chlordiazepoxide, and an increased risk of hip fracture in the elderly.
Triazolam
can cause rebound
insomnia
as well as anterograde amnesia. Clinicians should discontinue their prescribing of long-acting benzodiazepines for elderly patients with
insomnia
. More research is needed on the effects of nondrug interventions as well as on short- and intermediate-acting benzodiazepines, such as oxazepam and temazepam, to treat
insomnia
in community-dwelling elderly.
...
PMID:Benzodiazepines for insomnia in community-dwelling elderly: a review of benefit and risk. 759 66
Triazolam
, commonly prescribed to treat
insomnia
, also can be used to reduce dental anxiety. Despite controversial reports in the lay press, triazolam can be used safely at low doses for short periods. The authors review research concerning the drug's safety and discuss its use in dentistry.
...
PMID:Using triazolam to reduce dental anxiety. 803 76
Sleep problems and nocturnal arterial oxygen desaturation are common in patients with chronic obstructive pulmonary disease (COPD). Hence, the safety and efficacy of new hypnotic agents must be ascertained in this group of patients. We performed a double-blind, randomized, single-dose, placebo and active drug controlled, crossover study in 24 patients with
insomnia
(subjective sleep latency > 30 minutes and sleep duration 4-6 hours) and mild to moderate COPD (mean FEV1 61 +/- 12(SD)% predicted) in order to establish the effects of zolpidem 5 mg and 10 mg on sleep and respiration and to compare these effects with triazolam 0.25 mg. Arterial oxygen saturation for the entire night, by hour and stage, and the apnea-hypopnea index for the entire night were not significantly different with placebo and the various drug conditions. Total sleep time and sleep efficiency were increased over placebo by all three drug conditions.
Triazolam
was more effective than zolpidem 5 mg but not zolpidem 10 mg, and there was no significant difference between zolpidem 5 mg and zolpidem 10 mg. Zolpidem 10 mg and triazolam both reduced the number of awakenings (> 15 seconds duration) per hour of sleep. Although there was a trend for triazolam to be more efficacious than zolpidem 10 mg, no statistically significant difference was found for any objective or subjective sleep variable. Likewise, zolpidem 10 mg tended to be more efficacious than zolpidem 5 mg, but the difference was only significant in terms of perceived sleep quality and ease of falling asleep.(ABSTRACT TRUNCATED AT 250 WORDS)
...
PMID:Effects of zolpidem and triazolam on sleep and respiration in mild to moderate chronic obstructive pulmonary disease. 834 92
Triazolam
(TZ) is a triazolobenzodiazepine used in the treatment of
insomnia
that possesses significant anticonvulsant properties. Despite the widespread use of this drug, detailed pharmacokinetic-pharmacodynamic information is lacking, especially with respect to inhibition of seizure activity. TZ disposition has been described previously by methods with limited specificity, and the concentration-anticonvulsant effect relationship has not been characterized. The current studies were undertaken to examine TZ disposition with a specific HPLC method, and to evaluate the relationship between anticonvulsant effect and concentration in Sprague-Dawley rats. TZ pharmacokinetics were characterized after bolus or infusion administration; in a separate experiment, TZ pharmacodynamics were assessed with pentylenetetrazol-induced seizures. The systemic disposition of TZ could be described with a two-compartment model; systemic clearance ranged from 2.45 to 5.30 L/h/ kg, steady-state volume of distribution ranged from 2.10 to 4.02 L/kg, and mean residence time ranged from 47 to 65 min. The concentration-effect relationship was well described by a simple Emax model: Emax, expressed as the ratio of post-TZ to pre-TZ threshold convulsant doses of pentylenetetrazol, was 9.9 +/- 0.7, and the EC50 values were 10.0 +/- 4.6 ng/mL and 34.8 +/- 9.0 ng/g in serum and whole brain tissue, respectively. Under single-dose conditions, TZ is a very potent anticonvulsant in the rat pentylenetetrazol seizure model.
...
PMID:Anticonvulsant pharmacodynamics and disposition of triazolam in rats. 887 93
The dependence liability of benzodiazepines in the context of their use as hypnotics (i.e. by
insomnia
patients as pre-sleep medications) is unresolved. A recent study found that insomniacs self administer capsules at bedtime at a high rate, with triazolam (0.25 mg) taken as often as placebo. This study sought to determine if differential self administration would develop when multiple capsules are available nightly. Eighteen men and women, age 21-45 years, with
insomnia
complaints (nine with objective sleep disturbance and nine without) were studied, 1 week with placebo and 1 week with triazolam (0.25 mg). The two conditions were administered double-blind and presented in a counter-balanced order with a week between conditions. In each condition, after 3 consecutive sampling nights of the available single capsule for that condition, subjects could self administer 0-3 capsules before bed on the 4 subsequent nights.
Triazolam
was self administered as many nights as placebo, but the number of placebo capsules self administered was twice that of triazolam capsules. The objective insomniacs self administered more capsules than the subjective insomniacs and neither group differentially choose triazolam over placebo. The number of triazolam capsules taken nightly was stable and the number of placebo capsules variable. It is concluded that insomniacs show no short-term escalation of triazolam dose, but do choose an increased and variable number of placebos, a pattern which is interpreted as being
insomnia
relief-seeking behavior.
...
PMID:Hypnotic self administration and dose escalation. 888 81
Twenty-four men and women with
insomnia
, age 21-50 years, self administered hypnotics under a single-choice with placebo, single-choice with triazolam (0.25 mg), or forced-choice of placebo versus triazolam (0.25 mg) paradigm. Subjects received 4- sampling nights of placebo or triazolam in the single-choice conditions or 2 nights of each in the forced-choice condition. Then on 7 choice nights they could self administer a capsule, or not, in the single-choice conditions, or were required to choose one of two color-coded capsules in the forced-choice condition. In the single-choice conditions, subjects chose placebo 80% of nights and triazolam 77% of nights, while in the forced-choice condition triazolam was chosen on 86% of nights. Thus, the self administration of triazolam did not vary significantly between single or forced choice conditions, but that of placebo did. Placebo rate was high when it was the only alternative, but low when competing with triazolam. On sampling nights, compared to placebo, triazolam produced a significant increase in total sleep time, a reduction in latency to sleep, wake after sleep onset, and percentage stage 1 sleep.
Triazolam
, relative to placebo, also improved mood in the morning on some sampling nights. For subjects choosing capsules < 100% of opportunities (n = 14), on nights a capsule was chosen versus nights none was chosen (regardless of whether placebo or triazolam was the choice), self-ratings 30 min before bedtime on the Profile of Mood States vigor scale were significantly higher.
...
PMID:Hypnotic self administration: forced-choice versus single-choice. 934 77
<< Previous
1
2
3
4
Next >>