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PubMed1976

Preference studies of triazolam with standard hypnotics in out-patients with insomnia.

One hundred and four patients suffering from insomnia took part in four different two-night double-blind crossover trials of triazolam. In three separate studies, triazolam 0-5 mg was compared to placebo, flurazepam 30 mg and chloral hydrate 500 mg. Triazolam 0-5 mg was found to be preferred and to be superior to placebo, flurazepam and chloral hydrate in the treatment of insomnia. Analysis of sleep questionnaire data showed triazolam to be superior to the other treatments on the following: How much did the medication help you sleep, onset of sleep, duration of sleep and number of awakenings. Additionally, triazolam was superior to chloral hydrate on the feeling in the morning parameter. In another comparison of triazolam 0-25 mg to flurazepan 15 mg, triazolam was not significantly better than flurazepam on any of the efficacy parameters except that the patients felt more alert the morning following triazolam that following flurazepam. On all efficacy endpoints, trends for all parameters favoured triazolam 0-25 mg over flurazepam 15 mg. Untoward side-effects in these four studies were minimal.

Adolescent↗

PubMedDate not supplied

Urinary screening for alpha-OH triazolam by FPIA and EIA with confirmation by GC/MS.

Triazolam is a very short-acting triazolobenzodiazepine with sedative-hypnotic properties. Approximately 2% of an oral dose is excreted unchanged in the urine. The major urinary metabolite is alpha-hydroxytriazolam glucuronide (70% of the dose). The objective of this study was to characterize the reactivity of alpha-hydroxytriazolam in the urine benzodiazepine assay by fluorescence polarization immunoassay (FPIA; Abbott TDx) in comparison with enzyme immunoassay (EIA; Syva EMIT d.a.u. benzodiazepine assay). alpha-OH triazolam at 300 ng/mL gave a response equivalent to the 200-ng/mL nordiazepam Abbott calibrator. In the EMIT assay, alpha-OH triazolam gave a response equivalent to the 300-ng/mL calibrator (Syva) at 100-200 ng/mL. Both immunoassays gave positive results in 9 out of 9 urine specimens collected from individuals receiving triazolam. Confirmation was performed by analyzing for alpha-OH triazolam after enzymatic hydrolysis and formation of a TMS derivative for GC/MS. All urine specimens were positive for alpha-OH triazolam. In conclusion, both the FPIA and EIA immunoassay screening assays are acceptable for detecting the presence of alpha-OH triazolam in the urine of patients receiving therapeutic doses of triazolam.

Fluorescence Polarization↗

PubMed1978

Comparative efficacy of triazolam, flurazepam and placebo in out-patients insomniacs.

The short-term hypnotic efficacy of triazolam was compared to that of flurazepam and placebo in 120 out-patient insomniacs. Each patient was studied with a two-night, double-blind crossover trial. Triazolam (0.5 mg) was compared to placebo and flurazepam (30 mg). Triazolam (0.25 mg) was compared to flurazepam (15 mg and 30 mg). Triazolam (0.5 mg) was preferred to both placebo and flurazepam (30 mg). Triazolam (0.5 mg) was superior to placebo in improving quality of sleep, shortening sleep onset, increasing sleep duration, and reducing the number of night-time awakenings. Triazolam (0.5 mg) was superior to flurazepam (30 mg) in speeding sleep onset and increasing the quality of sleep. Triazolam (0.25 mg) was preferred to flurazepam (15 mg) and was significantly better than flurazepam on all sleep questions. Triazolam (0.25 mg) was preferred by more patients than flurazepam (30 mg) and was judged equally efficacious on individual sleep questions. Reports of side-effects were minimal for both drugs.

Adult↗

PubMed1978

[Effects of triazolam on conditioned behavior in rats (author's transl)].

Effects of triazolam on various types of conditioned behavior were investigated and compared mainly with diaepam in rats. The active conditioned avoidance response of the rat in a Shuttle box was inhibited by triazolam and diazepam only at large doses. The passive avoidance response in a step-down method was not affected by either triazolam or diazepam, but was markedly suppressed by chlorpromazine. The low rate response of hypothalamic self-stimulation behavior was markedly increased by triazolam at doses ranging from 2 to 40 mg/kg p.o., but was suppressed at doses over 80 mg/kg p.o. The high rate response was unaffected by triazolam even at doses of 40 approximately 180 mg/kg p.o. The low rate response was increased by diazepam at doses of 1 approximately 10 mg/kg p.o. and was suppressed at 80 mg/kg p.o. The high rate response was reduced by diazepam at 180 mg/kg p.o. In the conflict situation of the rat subjected to food reward and foot-shock punishment, the lever press response in the unpunished period was reduced by triazolam at doses of 1 approximately 5 mg/kg p.o., whereas that in the punished period was markedly increased. Similar effects were observed with diazepam at doses of 15 approximately 20 mg/kg p.o. Triazolam appeared to be 10 approximately 15 times more potent than diazepam in this anticonfluct effect. Thus, triazolam appears to be a potent antianxiety agent.

Animals↗

PubMed1978

[Behavioral and EEG effects of triazolam in comparison with those of diazepam (author's transl)].

Triazolam was 4 to 5 times as potent as diazepam in reducing hyperemotionality of either septal-lesioned or olfactory bulbectomized rats (O.B. rats), and in suppressing muricide in O.B. rats. This agent was equipotent with diazepam in inhibiting fighting behavior of long-term isolated mice, but was longer in duration of action. Triazolam was approximately 4 times more potent than diazepam in preventing pentetrazol convulsion, but was 10 times less potent in inhibiting maximal electroshock convulsion in mice. The muscle relaxant effect of triazolam as assessed by the inclined screen test was 34 times, and the effect on rotarod performance was 17 times more potent than that of diazepam in mice. Triazolam (0.2 approximately 0.5 mg/kg i.v.) changed the EEG to a drowsy pattern in unanesthetized rabbits with a chronic electrode implant, and suppressed the EEG arousal response to auditory stimulation and electrical stimulation given to either the mesencephalic reticular formation or posterior hypothalamus. The limbic afterdischarges induced by either hippocampal or amygdaloid stimulation were also markedly inhibited by triazolam. These EEG effects of triazolam were qualitatively similar to, but were 4 to 5 times more potent than those of diazepam. These results indicate that triazolam is a potent tranquilizer with a longer duration of action, and the muscle relaxant effect is considerable as compared with diazepam.

Aggression↗

PubMed1979

Metabolism of 8-chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo [4,3-alpha] [1,4]benzodiazepine, triazolam, a new central depressant. II. Identification and determination of metabolites in rats and dogs.

1. Eight metabolites of triazolam have been identified, namely, triazolam, dichlorotriazolobenzophenone (DCTB), 1'-hydroxytriazolam, dichloro-alpha-hydroxytriazolobenzophenone (1'-hydroxy-DCTB), Ar-hydroxytriazolam, 4-hydroxytriazolam, Ar-1'-dihydroxytriazolam and 1',4-dihydroxytriazolam. 2. Major metabolites found in the urine were 1',4-dihydroxytriazolam, 1'-hydroxy-DCTB and DCTB in rats; 1'-hydroxytriazolam, 4-hydroxytriazolam and conjugated 1'-hydroxytriazolam in dogs. 3. Major metabolites found in the faeces were 4-hydroxytriazolam in rats; 1'-hydroxytriazolam and 4-hydroxytriazolam in dogs. 4. Conjugated 4-hydroxytriazolam was the major metabolite in both the original and reabsorbed bile of rats. 5. Major metabolites in free form in the plasma were 4-hydroxytriazolam and 1'-hydroxytriazolam in rats; triazolam and 1'-hydroxytriazolam in dogs. 6. The major metabolite in the brain was triazolam, but those in the liver were 4-hydroxytriazolam and triazolam, and in the kidneys were 4-hydroxytriazolam and 1',4-dihydroxytriazolam. 7. Major metabolites in the urine, faeces, plasma and brain after 7-, 14- or 21-day repeated dosing in rats were not much different in type and ratio from those after single dosing. 8. Unchanged triazolam and 1'-hydroxytriazolam were the major metabolites in the plasma, placenta, foetus and amniotic fluid in pregnant rats. 9. There was no change in hepatic aniline hydroxylase and aminopyrine-N-demethylase activity from controls in rats given oral dose of [14C]triazolam for 14 days.

Animals↗

PubMed1992

Detoxification for triazolam physical dependence.

The clinical characteristics of a series of patients who developed physical dependence to triazolam has not previously been described. We report five cases of high-dose triazolam abuse in which the daily dosage ranged from 5 to 15 mg (100-300 mg diazepam equivalent) and the duration of use ranged from 3 months to 5 years. Physical dependence usually occurs in the context of a history of alcohol or other drug abuse, a history of panic attacks or anxiety disorder, substitution of triazolam for a longer-acting benzodiazepine, or inappropriate use of triazolam as an anxiolytic agent given as multiple daily doses. A rational approach to the pharmacotherapy of triazolam withdrawal is described. Treatment to replace the triazolam with a long half-life CNS depressant and strategies for this pharmacologic therapy are discussed. The abuse liability of triazolam may be no greater and is most likely less than that of some other benzodiazepines.

Adult↗

PubMed1977

Multiclinic double-blind comparison of triazolam and flurazepam for seven nights in outpatients with insomnia.

In this two-clinic seven-day double-blind study, 0.5 mg triazolam (Halcion) was compared to flurazepam (Dalmane) in the treatment of insomnia. Two clinical investigators completed 118 outpatients, 61 on triazolam and 57 on flurazepam. Five patients, four on triazolam and one on flurazepam, discontinued because of side effects; and three patients, one on triazolam and two on flurazepam, discontinued because of ineffectiveness of the medication. Analysis of pooled data for the 110 evaluable patients showed that 0.5 mg triazolam was significantly better than 30 mg flurazepam on the following parameters: (1) how much the medication helped the patients sleep, (2) onset of sleep, (3) duration of sleep, (4) evaluation of duration of sleep, and (5) feeling of restfulness in the morning. The trend for all other parameters favored triazolam treatment, but the values did not reach statistical significance. Side effects were similar in both groups, with drowsiness being reported most frequently. No change in efficacy indicating tolerance development during the seven days of drug administration was observed in either group.

Adolescent↗

PubMed1992

Caffeine moderately antagonizes the effects of triazolam and zopiclone on the psychomotor performance of healthy subjects.

To determine whether caffeine antagonizes the decremental effects of triazolam and zopiclone on human performance, oral single doses of 0.250 mg triazolam, 7.5 mg zopiclone, or respective placebos, with and without 300 mg caffeine, were given to parallel groups of student volunteers in two double-blind studies. Objective tests and subjective visual analogue ratings were done at baseline and 30 min. and 90 min. after the intake. In Study I, triazolam produced drowsiness at 30 min. but did not differ from the placebo in other tests. Caffeine induced alerting effects in various tests and differed from triazolam in some (digit substitution, drowsiness, calmness, mental slowness) but not all variables measured. Caffeine and triazolam were interpreted as being antagonists. In Study II, zopiclone impaired digit substitution and flicker fusion, produced exophoria and lowered systolic blood pressure. Caffeine differed from zopiclone in several test functions, but it also differed from caffeine + zopiclone whereas zopiclone differed from caffeine + zopiclone only in two tests (Maddox wing, systolic blood pressure). Thus, zopiclone counteracted the effects of caffeine more easily than caffeine counteracted the decremental effects of zopiclone. We conclude that triazolam may not differ importantly from diazepam as regards their antagonism towards caffeine, whereas further research on the antagonism between zopiclone and caffeine needs to be done.

Anti-Anxiety Agents↗

PubMed1979

Metabolism of 8-chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo [4,3-alpha] [1,4] benzodiazepine, triazolam, a new central depressant. I. Absorption, distribution and excretion in rats, dogs and monkeys.

1. Peak radioactivity in the blood was reached at 30 min after i.p. and 1 h after oral dosing of [14C]triazolam to rats. In dogs, peak blood level was observed at 30 min after oral dosing. 2. Daily dosing of triazolam to male rats for 21 days caused a gradual increase in blood level, with peak at 1 h after dosing. 3. The rate of binding of triazolam plus its metabolites to plasma protein of rats was about 30% at 15 min and 6 h. 4. In rats, the majority of the activity of the intra-intestinally administered [14C]triazolam was found in the small intestines in 6 h. 5. About 58% of the oral dose and 77% of the i.p. dose were recovered in the bile of rats in 48 h after dosing. When the bile from one rat was introduced into the duodenum of a second rat, approximately 37% was recovered in the bile of the second animal in 24 h. 6. In male rats, high radioactivity was seen in the liver, kidneys, adrenals and heart, and low in the CNS. By 96 h after dosing, radioactivity in the liver, blood and kidneys was very low, and was undetectable in other tissues and organs. Radioactivity levels in tissues after daily dosing for 7, 14 and 21 days did not differ appreciably from single administration. 7. In monkeys, activity was high in the liver, kidneys and skin following oral administration and low in the CNS. 8. After oral administration of [14C]triazolam to pregnant rats, the activity in the uterus and placenta was higher than that in the maternal blood. The activity in the foetus was low. 9. In rats given [14C]triazolam orally or i.p., 85% and 12% of the oral dose, and 82% and 14% of the i.p. dose were recovered in the faeces and urine, respectively, in 96 h. The rate of cumulative faecal and urinary excretion after repeated dosing was similar to the single dosing with 80% and 14% of the activity recovered, respectively, in faeces and urine in 6 days. In dogs, 50% of the oral dose was found in the faeces and 40% in the urine. 10. Radioactivity in the milk of rats was maximal at 4 h after oral dosing. It declined to 34% of the peak level 48 h later.

Animals↗

PubMed1992

Comparative clinical profiles of triazolam versus other shorter-acting hypnotics.

The efficacy, safety, and performance of triazolam was compared with those of other shorter-acting hypnotics acting on the gamma-aminobutyric acid (GABA) receptor--zopiclone, zolpidem, midazolam, brotizolam, temazepam, lormetazepam, and loprazolam. In all, 5506 patients participated in 38 clinical and epidemiologic studies, of whom 2462 were treated with triazolam in parallel-design and crossover studies. To provide clinically relevant comparisons, only studies using comparator agents in doses equipotent to the triazolam doses were included. Two general findings emerged. First, "serious" central nervous system side effects, such as excitement and violence, were not demonstrated for any of the hypnotic agents, including triazolam. Other central nervous system side effects, such as depression and irritability, were reported with equal frequencies for all the hypnotics reviewed. Rebound insomnia, reported intermittently with most of these agents, was short-lived and not clinically significant. So-called early morning insomnia was noted only once and does not appear to be a valid clinical entity. Daytime anxiety was not observed in large numbers of triazolam-treated subjects studied, which is contrary to claims that the drug is anxiogenic. Second, a remarkable similarity was found among all of these shorter-acting agents in terms of efficacy, side effects, and performance-related effects. This was particularly of note for zopiclone and zolpidem. Although claims have been made suggesting differences, evaluation of the studies herein showed that these nonbenzodiazepine hypnotics were indistinguishable from triazolam and other benzodiazepine hypnotics in their clinical and pharmacologic activity. Thus, different chemical structures did not a priori predict different clinical profiles when drugs share a similar mechanism of action.

Azabicyclo Compounds↗

PubMed1977

Multi-clinic cross-over comparison of triazolam (Halcion) and placebo in the treatment of co-existing insomnia and anxiety in anxious out-patients.

In this multi-clinic double-blind cross-over designed study, forty-five anxious and insomniac out-patients received either triazolam (Halcion) 0.25 mg or placebo at bedtime. After seven days the medications were crossed over. The dosage was doubled after nights 2 and 9 if good sleep was not produced. Three patients dropped out, two on placebo (one for side effects and one for lack of efficacy) and one on triazolam (due to misunderstanding instructions). Analysis of sleep questionnaire data showed superiority of triazolam to placebo (p less .001) in all parameters. The incidence of dreams was not affected. Analysis of antianxiety efficacy showed that triazolam was superior to placebo (p less than .001) in all parameters, both physician's and self ratings. Thus, either triazolam or a good night's sleep significantly relieved the patient's anxiety. No side effects or abnormal laboratory values of significance were attributable to triazolam.

Adolescent↗

PubMed1975

Comparison of the hypnotic activity of triazolam, flurazepam hydrochloride, and placebo.

Triazolam, 0.4 and 0.8 mg, flurazepam, 15 and 30 mg, and placebo were compared in a double-blind, randomized 5-night crossover study in 25 inpatient insomniacs. These patients all complained difficulty falling asleep; all said they usually slept less than 5 hr a nigh and woke up too early in the morning. Results of the patients' global evaluation of the medications shows that all of the treatments were rated significantly higher than placebo, with the exception of triazolam, 0.4 mg, which was not significantly different from flurazepam, 15 or 30 mg, or from placebo. In subjective evaluation of sleep onset, only triazolam, 0.4 and 0.8 mg, was rated faster than placebo. All 4 active medications increased duration of sleep. Triazolam, 0.8 mg, and flurazepam, 30 mg, were rated as providing deeper sleep than placebo while all treatments except flurazepam, 15 mg, decreased the number of awakenings below that on placebo. A significant dose-response curve was obtained with triazolam and flurazepam for some of the parameters. Very few adverse effects were reported. One patient reported feeling groggy and drowsy on 0.4 mg triazolam while 2 reported nightmares on placebo.

Adult↗

PubMed1978

A clinical comparison of triazolam with placebo and with secobarbital in insomniac patients.

Seventy-six out-patient insomniacs participated in three different two-night, double-blind crossover trials investigating the hypnotic efficacy andsafety of triazolam. Triazolam 0.5 mg was compared to placebo in one trial conducted K Kay Okawa, MD, and triazolam 0.5 mg was compared to secobarbital 100 mg in trials conducted by K Kay Okawa, MD and George S Allen, MD. The results of the later two studies were combined and the data analyzed jointly. Triazolam 0.5 mg was found to be preferred and to be significantly better than both placebo and secobarbital 100 mg in the treatment of insomnia. Analysis of sleep questionnaire data showed triazolam to be superior to either placebo or secobarbital on the following parameters: how much the medication helped the patients sleep; onset of sleep; duration of sleep; and number of nocturnal awakenings. No differences were observed between treatments in any trial with regard to the patient's feeling of alertness the next morning. The side-effects reported for all treatments did not significantly interfere with the patient's ability to function.

Adult↗

PubMed1978

Multi-clinic double-blind comparison of triazolam (Halcion) and placebo administered for 14 consecutive nights in outpatients with insomnia.

In this multi-clinic double-blind study, patients suffering from insomnia were treated with triazolam 0.5 mg (Halcion) or placebo for 14 days. Four investigators treated 239 patients, 122 on triazolam and 117 on placebo. Thirty-nine patients, 10 on triazolam and 29 on placebo, dropped out for ineffectiveness of the medication and 32 patients, 16 in each group, dropped out for side effects. Analysis of pooled efficacy data showed that triazolam was significantly better than placebo on all efficacy parameters measured, including how much the medication helped the patients sleep, onset of sleep, duration of sleep, duration compared to usual, number of nocturnal awakenings, and feeling of restfulness in the morning. Triazolam did not produce evidence of tolerance development after 2 weeks of treatment. The same variety of side effects occurred on each treatment and primarily included drowsiness, grogginess, headaches, impaired coordination nausea, and dizziness.

Adolescent↗

PubMed1975

Triazolam in insomniac family practice patients.

Triazolam, 0.5 mg, a benzodiazepine with hypnotic properties, was compared to secobarbital, 100 mg, and placebo in a 1-wk study conducted with 100 insomniac family practice patients. Considerable sensitivity to differential treatment effects was demonstrated for these family practice patients as well as for a research methodology that combines a crossover design, permitting preference ratings, with a between-patient design. In almost all sleep parameters, assessed with a variety of subjective techniques, triazolam and secobarbital were shown to be significantly more effective than placebo. Triazolam was consistently and often significantly indicated to be a more effective hypnotic, particularly for reducing nocturnal awakening, than secobarbital. Analysis of self-report emotional distress data revealed that present insomniac patients were slightly more emotionally symptomatic than other nonpsychiatric populations. Triazolam was followed by the greatest and secobarbital the least relief of emotional symptoms and triazolam emerged as an especially effective hypnotic for initially more depressed insomniac patients. Present findings suggest that type and degree of emotional symptomatology may affect the response of insomniac patients to hypnotics.

Benzodiazepines↗

PubMedDate not supplied

Hypnotic efficacy of triazolam: sleep laboratory evaluation of intermediate-term effectiveness.

Triazolam (U-33030), an investigational hypnotic drug, was evaluated in seven insomniac subjects in the sleep laboratory. The protocol consisted of 22 consecutive nights: four placebo nights for adaptation and baseline, two weeks of drug administration (0.5 mg triazolam) for short- and intermediate-term drug effectiveness, and four placebo nights for withdrawal effects. With short-term drug use, both sleep induction and sleep maintenance improved, with total wake time decreasing markedly--a 45 per cent decrease from baseline. At the end of two weeks of drug use, none of the efficacy parameters was significantly decreased from baseline; there was only a 17 per cent decrease in total wake time. Following drug withdrawal, sleep difficulty significantly increased above baseline levels. Two of the subjects experienced episodes of amnesia during the drug administration period. The per cent of REM sleep decreased significantly during both short and intermediate drug conditions. Following drug withdrawal, the per cent of REM sleep was similar to baseline. Slow-wave (stages 3 and 4) sleep was significantly decreased for both drug conditions; and following drug withdrawal, it returned completely to the baseline leve. These data indicate that triazolam is effective for short-term use, loses most of its effectiveness with intermediate-term use, and its withdrawal is followed by a significant sorsening of sleep. These findings are discussed in relation to the potential labeling and promotion of triazolam. Finally, the findings of amnesia associated with triazolam administration need to be more thoroughly evaluated.

Electroencephalography↗

PubMed1975

Comparison of triazolam and methyprylon as a hypnotic in insomniacs.

The hypnotic effect of a new triazolobenzodiazepine, triazolam (0.5 mg) and methyprylon was compared in 30 outpatient volunteers with insomnia using the preference technique. On the first night of the 2 night trial, triazolam or methyprylon was given on a double-blind basis and on the 2nd night the outpatients received the alternate medication. Following each trial night the patients were interviewed in regard to their sleep. Of the 28 patients who completed the study, 21 patients preferred triazolam, 5 preferred methyprylon and 2 had no preference (p = 0.001). Analysis of the various sleep parameters showed that triazolam helped the patients sleep more than methyprylon (p = 0.026), there were fewer awakenings on triazolam (p = 0.064), a longer duration of sleep (p = 0.064) and a better feeling in the a.m. (p = 0.020). The sleep onset was the same after both medications. The number and severity of the side effects was considerably higher after methyprylon.

Adolescent↗