Triazolam Research Articles

Triazolam see Midazolam/triazolam

Triazolam see Midazolam/triazolam

Confidentiality of Upjohn's triazolam documents

Confidentiality of Upjohn's triazolam documents

Triazolam fails to induce sleep in suprachiasmatic nucleus-lesioned rats

Rats with suprachiasmatic nuclei (SCN) lesions did not show increased sleep after triazolam (TRZ) injections at any dose from 0.2 to 1.6 mg/kg, whereas 0.4 mg/kg TRZ given intact rats in the middle of their activity phase significantly increased sleep. Across SCN-lesioned and intact rats, the amount of sleep before and after TRZ 0.4 mg/kg was negatively correlated. SCN-lesioned rats did not have a circadian activity-dominant period and so did not accumulate a biological sleep debt. Their lack of response to TRZ may have resulted from the absence of a sleep debt compared to intact rats injected in the middle of their activity phase. These data support our hypothesis that the homeostatic process controlling sleep gates benzodiazepine hypnotic efficacy.

The safety of triazolam should not be judged on media reporting

The safety of triazolam should not be judged on media reporting

Triazolam see Flurazepam/triazolam

Triazolam see Flurazepam/triazolam

Diazepam and triazolam self-administration in sedative abusers: concordance of subject ratings, performance and drug self-administration

The reinforcing effects of diazepam (DZ), triazolam (TZ) and placebo were examined in eight male subjects with histories of sedative abuse. DZ (40 or 80 mg), TZ (1.0 or 2.0 mg) and placebo were each individually available for oral self-administration using a double-blind within-subject design. After an initial sampling exposure, subjects could self-administer a single dose of drug on each of 6 days by completing a progressively increasing bicycle riding requirement. All subjects initially self-administered DZ and TZ but a decreasing number of subjects continued to self-administer drugs on the remaining days; there was no difference between DZ and TZ in the total number of self-administrations. Placebo was self-administered only by one subject on two occasions. Performance measures showed that TZ produced greater memory impairment than DZ and that DZ produced residual psychomotor impairment on the next day. With repeated dosing, evidence of tolerance was seen for both drugs on psychomotor and memory performance and subject ratings of drug liking. A few modest correlations of drug self-administration and subject-ratings were obtained, suggesting some correspondence of subject verbal and drug self-administration behaviors, but these measures did not covary in a completely consistent manner.

Triazolam withdrawal

Triazolam withdrawal

You don't have to be a neuroscientist to forget everything with triazolam--but it helps

You don't have to be a neuroscientist to forget everything with triazolam--but it helps

Temperature dependence and GABA modulation of [ 3H]triazolam binding in the rat brain

The hypnotic triazolam (TZ), a triazolobenzodiazepine displays a short physiological half life and has been used for the treatment of insomnia related to anxiety states. Our major objectives were the direct measurement of the temperature dependence and the gamma-aminobutyric acid (GABA) effect of [ 3H]TZ binding in the rat brain. Saturation studies showed a shift to lower affinity with increasing temperatures (K d = 0.27±08 nM at 0°C; K d = 1.96±0.85 nM at 37°C) while the B max values remained unchanged (1220±176 fmoles/mg protein at 0°C and 1160±383 fmoles/mg protein at 37°C). Saturation studies of [ 3H]TZ binding in the presence or absence of GABA (100uM) showed a GABA-shift. At 0°C the K d values were (K d=0.24±0.03 nM/−GABA; K d=0.16±0.04/+GABA) and at 37°C the K d values were (K d=1.84±0.44 n/M−GABA; K d=0.95±0.29 n/M+GABA). In contrast to reported literature, our findings show that TZ interacts with benzodiazepine receptors with a temperature dependence and GABA-shift consistent with predicted behavior for benzodiazepine agonists.

Triazolam withdrawal

Triazolam withdrawal

Zopiclone: is preferred over triazolam by insomniacs

Zopiclone: is preferred over triazolam by insomniacs

Repeated administration of diazepam and triazolam to subjects with histories of drug abuse

The present study examined the effects of repeated administration of diazepam (DZ) and triazolam (TZ) on psychomotor performance and subject-rated drug liking. Subjects were 11 males (30–41 years) who had documented histories of drug abuse and who resided on a behavioral pharmacology research ward. Six subjects received 80 mg DZ every third day (3 subjects) or every sixth day (3 subjects) for a total of 3–6 dosing occasions and six subjects received TZ (2.0 or 3.0 mg) every second day (4 subjects) or every third day (2 subjects) for a total of 3–5 dosing occasions. The results showed that on the first dose occasion, the two drugs produced generally similar degrees of psychomotor impairment and subject-rated drug liking. Following the first DZ dose, subsequent doses produced less of an effect (i.e. single-dose tolerance). Across at least the first three dose occasions, progressive tolerance development was observed with DZ but no tolerance was observed with TZ. It is hypothesized that pharmacokinetic differences between DZ and TZ may account for the difference in the development of tolerance.

Seizure following withdrawal from triazolam

Seizure following withdrawal from triazolam

Pharmacodynamic evaluation of the benzodiazepine-oral contraceptive interaction.

The sedative, psychomotor, and memory effects of single oral doses of alprazolam (ALP), lorazepam (LOR), temazepam (TMP), and triazolam (TRZ) were evaluated in women taking oral contraceptives (OCs) and a comparable group of control women. Nine women taking OCs and 11 control women took doses of 1 mg ALP and 2 mg LOR and 10 OC users and 10 control women took 30 mg TMP and 0.5 mg TRZ on two occasions separated by 28 days. Minimal psychomotor impairment was noted after TMP. ALP, LOR, and TRZ produced greater performance impairment in the OC users. Correcting the maximum observed performance decrement for plasma concentration did not account for the differences between OC users and controls. After TMP, there was less sedation during the first 2 hours in OC users, who also had higher plasma TMP clearance. There were no differences in sedation between OC users and controls after ALP, LOR, and TRZ; however, there was less than 50% power to detect a 30% difference. Amnestic effects in OC users and controls did not differ after any of the four drugs. The observed patterns of anterograde amnesia were different, with the earliest and most pronounced recognition failure after TRZ (50% at 1.5 hours), while the LOR effect increased to a maximum (30%) 4 hours after dosing. Our data suggest that differences in benzodiazepine pharmacokinetics between OC users and control women do not account for observed differences in psychomotor impairment. Women taking OCs are more sensitive to the psychomotor effects of single oral doses of benzodiazepines.(ABSTRACT TRUNCATED AT 250 WORDS)

Cimetidine Increases Levels of Alprazolam and Triazolam

Cimetidine Increases Levels of Alprazolam and Triazolam

Effect of oral contraceptives on triazolam, temazepam, alprazolam, and lorazepam kinetics.

The effects of low-dose estrogen oral contraceptives (OC) on the elimination of the oxidized benzodiazepines triazolam (TRZ) and alprazolam (ALP) and the conjugated benzodiazepines temazepam (TMZ) and lorazepam (LOR) were studied in two parallel crossover studies of 20 women each. Women taking OC steroids containing low doses of estrogen and women matched for age, weight, and cigarette smoking received single oral doses of TRZ (0.5 mg) and TMZ (30 mg) or ALP (1 mg) and LOR (2 mg). Kinetics were determined as plasma concentrations during 48 hr after dosing. OCs inhibited the metabolism of ALP: The AUC increased and the elimination rate constant was greater in users of OCs. For TRZ, which has an intermediate extraction ratio, the AUC was increased by OCs but not significantly so. In contrast, OCs decreased the AUC for TMZ and the elimination rate constants for LOR and TMZ. The AUC of LOR was not affected by OCs. Low-dose estrogen OCs may therefore inhibit the metabolism of some oxidized benzodiazepines and accelerate the metabolism of some conjugated benzodiazepines.

TRIAZOLAM: Shortacting benzodiazepine hypnotic introduced in the US in January by Upjohn

TRIAZOLAM: Shortacting benzodiazepine hypnotic introduced in the US in January by Upjohn

Hallucinations from Triazolam

Hallucinations from Triazolam

Model insomnia, noise, and methylphenidate, used for the evaluation of hypnotic drugs

Experimental sleep disturbance (model insomnia) was produced by intermittent white noise and the administration of 10 mg of methylphenidate (MPD). The effects of flurazepam (FZP) 15 mg and triazolam (TZM) 0.25 mg on these models was investigated. All night sleep polygraphy was performed on 8 normal male subjects under each of the following 9 conditions: baseline, TZM 0.25 mg, FZP 15 mg, white noise alone, noise and TZM, noise and FZP, MPD alone, MPD and TZM, and MPD and FZP. A reduction in total sleep time and stage were (S-REM) and an increase in the wakening stage were observed with both noise and MPD. Stage 4 sleep was reduced only by MPD. Administration of TZM or EZP did not cause any significant change in sleep parameters. These drugs in combination with noise or MPD resulted in almost complete recovery of the sleep disturbance induced by noise or MPD, except for a reduction in S-REM. These results indicate that model insomnia, particularly MPD insomnia, will assist in the evaluation of hypnotic drugs.