Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “DIAZEPAM”

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 793 records · Page 44Linked to original sources
PubMed1997

[Effects of rifampin and isoniazid on the pharmacokinetics of diazepam in rabbits].

The pharmacokinetics of diazepam (3 mg.kg-1, i.v.) in rabbits was studied after pretreatment with rifampin (RFP, 100 mg.kg-1.d-1 x 4), isoniazid (INH, 50 mg.kg-1.d-1 x 4) and RFP + INH. The results showed that RFP significantly increased cytochrome P-450 content, but the T 1/2 and AUC of diazepam were significantly decreased. The plasma clearance (CL) was increased in the RFP group. In the INH group the T 1/2 and AUC of diazepam were significantly increased and the CL was significantly decreased. However, cytochrome P-450 content and the pharmacokinetic parameters of diazepam were not changed in the RFP + INH group. Our results indicate that RFP induces the activity of hepatic microsomal enzymes and increases the metabolism of diazepam, INH inhibits the activity of hepatic microsomal enzymes and decreases the metabolism of diazepam in rabbits.

Animals↗
PubMedDate not supplied

Plasma levels of diazepam and mood ratings.

Ten subjects received 10 and 20-mg. doses of diazepam intravenously. The plasma levels of the drug and its major metabolite, desmethyl-diazepam were measured and coordinated with answers to a subjective questionnaire. After initial rapid decline of the diazepam level, the level and shape of the remaining part of individual plasma curves showed considerable variance. Increases in diazepam levels were minute (0.04 plus or minus 0.03 mcg./ml.). Desmethyl-diazepam levels continued to build up until the end of sampling. Contrary to some previous reports, no recurrent drowsiness was evident after initial recovery. Correlation between plasma levels of diazepam and some of the subject's moods was significant. Nevertheless, further studies are needed to determine whether plasma levels can be meaningfully related to various cerebral effects of the drug.

Adult↗
PubMed1976

Limitations of compounding diazepam suspensions from tablets.

The concentration of diazepam in two types of suspension vehicles, as prepared from 10-mg tablets was tested over a 14-day period. The suspensions (1 mg/ml) were stored at room temperature in amber glass bottles. In one suspension, consisting of eight triturated tablets, 4.0 ml ethanol, 24.0 ml propylene glycol, 20.0 ml Syrup, USP, and 32.0 ml chocolate syrup, 90% of the diazepam was dissolved. This suspension demonstrated consistently acceptable concentrations of diazepam. In the other suspension, consisting of triturated tablets and Syrup, USP, only 25% of the diazepam was dissolved, and less consistent, subpotent concentrations of diazepam were found. The variation of diazepam concentrations between the suspensions was unrelated to the chemical stability of the drug.

Diazepam↗
PubMed2003

Effects of diazepam on facial emotion recognition.

OBJECTIVE: There have been few studies of the pharmacologic modulation of facial emotion recognition. The present study aimed to replicate and extend the finding that recognition of facial anger was selectively impaired by diazepam. The hypothesis was that, in comparison with placebo, diazepam would impair the recognition of facial anger in healthy volunteers, but not the recognition of 5 other basic emotions: happiness, surprise, fear, sadness and disgust. DESIGN: A randomized, counterbalanced, double-blind, placebo-controlled, within-subjects comparison of diazepam with placebo. SETTING: A university psychopharmacology research unit. PARTICIPANTS: Healthy male (n = 6) and female (n = 22) volunteers, aged 18-45 years. PROCEDURES: Subjects were tested on 2 tasks following the administration of diazepam, 15 mg, and placebo on separate occasions. In the first "multimorph" task, images of facial expressions were morphed to produce continua between the neutral and full expressions of 6 basic emotions. Accuracy and identification thresholds were assessed for stimuli in which the intensity of expression gradually increased. In the second "emotional hexagon" task, facial expressions were morphed between pairs of emotions. Single images were presented, and accuracy and speed of response were assessed. RESULTS: Diazepam produced broad impairments in response accuracy, recognition thresholds and response speed on the facial emotion tasks that were not limited to angry expressions. CONCLUSIONS: The present study found that diazepam, 15 mg, impaired facial emotion recognition, but not selectively. In the emotional hexagon task, a reaction-time analysis suggested that the identification of facial anger might be differentially sensitive to variations in stimulus duration, complicating the interpretation of this paradigm.

Adolescent↗
PubMed1992

Comparison of diazepam with progestin for effectiveness in suppression of urine spraying behavior in cats.

The most common treatment for urine spraying and marking in cats has been administration of long-acting progestins. Treatment with diazepam has recently been gaining favor, particularly because of reported adverse effects of progestins. Results of a clinical trial involving 20 cats indicated that diazepam was effective in eliminating or markedly reducing spraying in 11 (55%) of them. However, most cats required continuous treatment, or at least intermittent treatment, when spraying recurred. The physiologic and behavioral dependency of cats on diazepam, which presumably develops over the course of administration, may contribute to the tendency for spraying to recur once diazepam treatment is discontinued. Using data from previously published findings on progestin administration, plus additional cases, it was documented that a significantly (P less than 0.05) higher percentage of males than females responded favorably. Although the number of cases was not sufficient for a statistical comparison of diazepam vs progestin treatment with regard to male vs female, possible gender difference in the effectiveness of diazepam was not indicated.

Animals↗
PubMedDate not supplied

[Combined effect of diazepam and GABAA-ergic ligands on the activity of Cl(-)-ATPase from plasma membrane of bream brain (Abramis brama L.)].

We studied the combined effect of diazepam and GABAA-ergic ligands on the activity of Cl- -ATPase from plasma membrane of bream brain. of The membranes were preincubated and incubated with diazepam as well as with other GABAA-ergic ligands at physiological pH (7.4), i.e. under the conditions when Cl- -ATPase activity is undetectable. GABA (0.1-100 microM) induced Cl- -ATPase activity with the maximum effect at 10 microM. Diazepam (0.1 microM) enhanced the effect of low GABA concentrations (0.1-1 microM) on Cl- -ATPase activity but had no effect on the enzyme in the presence of high GABA concentrations (10-100 microM). At the same time, GABA (1 microM) enhanced the effect of low diazepam concentrations (0.1-1 microM) on the enzyme activity but had no effect on it in the presence of high concentrations of the ligand. Blockers of GABAA-ergic receptors, picrotoxin (50 microM) and bicuculline (5 microM), canceled the combined effect of diazepam and GABA on the enzyme activity. The obtained data demonstrate that the combined effect of diazepam and GABAA-ergic ligands on Cl- -ATPase activity at physiological pH is similar to the effect of these ligands on GABAA/benzodiazepine/Cl- channel.

Adenosine Triphosphatases↗
PubMed2004

[Validation of an HPLC method for the analysis of decomposition products in injectable diazepam].

Diazepam is an important drug from the group of benzodiazepines, used in clinical practice for its sedative, hypnotic, anticonvulsive, myorelaxant, and primarily anxiolytic effects. Several kinetic studies have been published which show that diazepam is a drug sensitive to hydrolysis both in acid and alkaline media. The present study aimed to elaborate and validate a simple and rapid HPLC/UV method for simultaneous analysis of three decomposition products of diazepam in the presence of diazepam and to apply it also on the control of stability of the injectional solution of diazepam. The optimization of chromatographic conditions resulted in the use of the high-performance chromatographic column Zorbax ODS, the mobile phase represented by a mixture of acetonitrile/water in a ratio of 60/40 (w/w, %), flow rate 1.5 ml/min, and spectrophotometric detection at 242 nm. The elaborated method and the employed chromatographic system were successfully validated and they can be used in practice in the control of stability of injection solution of diazepam.

Chromatography, High Pressure Liquid↗
PubMed2004

The effect of ketamine and fentanyl in reducing the pain of diazepam injection.

Diazepam is an effective drug that is used widely in modern anesthesia. Venous irritation is one of its major side effects attributed to its acqueous insolubility and requisite solvents. There is some evidence that ketamine may acts as a local anesthetic drug, because of its effect on N-methyl-D-aspartate receptors. Fentanyl also may reduce the pain of diazepam injection by blocking the opiate receptors in vessels walls. To determine the effectiveness of ketamine and fentanyl in reducing the pain of diazepam injection, 150 patients (ASA I, II) were randomly assigned to one of three Groups and before intravenous diazepam injection. 2 ml normal saline, 2 ml fentanyl or 10 mg ketamine were administered for Groups 1, 2, 3 respectively. The pain of diazepam injection was then evaluated at 30 minutes intervals. Our results showed that ketamine and fentanyl reduce the pain of diazepam dramaticaly (p < 0.001) in comparison with placebo. Ketamine is more effective than fentanyl in reducing such pain (p < 0.001).

Adolescent↗
PubMed1992

Therapeutic effects and effects on actual driving performance of chronically administered buspirone and diazepam in anxious outpatients.

Two groups of 12 outpatients each (six men and six women) with generalized anxiety disorder, participated in this study. Each patient was treated single-blind with placebo during the first 7 days (baseline), followed by a double-blind drug treatment period of 4 consecutive weeks (active) and ending again with 7 days single-blind placebo treatment (washout). One group received buspirone 5 mg three times a day in the first week and continued with 10 mg in the morning, 5 mg in the afternoon, and 5 mg in the evening during the second, third, and fourth weeks. The other group received diazepam 5 mg three times a day in all 4 weeks. On the evening of the seventh day of each treatment week the Hamilton Rating Scale for Anxiety and the Symptom Check List (90 items) were applied to assess the therapeutic effects, followed by an on-the-road driving test that started 1.5 hours after the last drug or placebo intake. The test consisted of operating an instrumented vehicle over a 100 kilometer highway circuit while attempting to maintain a constant speed and a steady lateral position within the right traffic lane. Two patients in the diazepam group were unable to complete their test after the first and second treatment week, respectively, because of serious sedative reactions. Both buspirone and diazepam were equally effective in reducing overall anxiety symptoms. The specific profiles showed that buspirone also reduced concomitant depressive symptoms and symptoms of interpersonal sensitivity and anger-hostility. In contrast, diazepam was found to be slightly more effective in reducing somatic symptoms and to positively affect sleep disturbances. Moreover, abrupt discontinuation of diazepam resulted in a relapse of psychic anxiety symptoms comparable with the placebo-baseline level and a partial relapse of somatic anxiety symptoms. Chronic treatment with buspirone had no significant effects on lateral position and speed control. In contrast, diazepam significantly impaired control of lateral position in the first 3 weeks of treatment. There was no significant impairment in the fourth treatment week and the placebo-washout week. Speed control was significantly impaired only in the first week. The relevance of the trend toward decreasing performance impairment during chronic treatment remains to be established.

Adolescent↗
PubMedDate not supplied

Comparison of the effectiveness of oral diazepam and midazolam for the sedation of autistic patients during dental treatment.

PURPOSE: This study was undertaken to compare the effectiveness of oral diazepam and midazolam in sedating autistic patients during dental treatment. METHODS: The treatment regimen consisted of nitrous oxide/oxygen inhalation in conjunction with oral administration of either diazepam 0.3 mg/kg or midazolam 0.5 mg/kg in a cross-over design study of 13 subjects aged 5.8 to 14.7 years. A drug was classified as being effective when over 70% of the patients taking the drug were judged as "success" in all 3 behavioral criteria: (1) sleeping; (2) body movement; and (3) crying behaviors. The study was observed by an independent clinician with an intraexaminer reliability of 88%. RESULTS: For sleeping behavior, midazolam was found to be significantly more effective than diazepam as the duration of stimulation increased (P<.05). For the movement and crying behaviors, midazolam also proved to be significantly more effective from the start of treatment through the 35- and 40-min markers, respectively (P<.05). For the remainder of treatment, however, there was no statistically significant difference in these behaviors between the trials (P>.05). Diazepam and midazolam were rated as 77% and 100% successful, according to the overall behavior evaluation criteria (P=.02). CONCLUSIONS: Both diazepam and midazolam were shown to be effective sedative agents, successfully and safely used to sedate autistic patients for dental treatment. Midazolam was significantly more effective than diazepam in those portions of the procedure with increased stimulation.

Administration, Oral↗
PubMed1992

Effects of diazepam (Valium) on aortic atherogenesis and plasma lecithin: cholesterol acyltransferase activity in cockerels fed an atherogenic diet.

Blood plasma LCAT (lecithin: cholesterol acyltransferase, EC 2.3.1.43) was studied in cockerels fed an atherogenic diet to determine if attenuation of aortic atherogenesis, as a result of simultaneous treatment of the birds with diazepam, might be related to modulation of enzyme activity by the drug. Administration of diazepam (0.6 mg/kg) did not influence LCAT. It was observed that no relationship could be established between enzyme activity and the extent of aortic atherogenesis. In contrast, addition of diazepam in vitro to cockerel plasma caused a concentration-dependent inhibition of LCAT activity. The effect was most pronounced when diazepam was present at a concentration of 50-200 microM, where inhibition of enzyme activity was 25-65%. Thus, pharmacologic doses of diazepam do not appear to affect LCAT in vivo. It is concluded that diazepam attenuates aortic atherogenesis in cockerels fed an atherogenic diet by a mechanism independent of LCAT.

Animals↗
PubMed1991

Effects of diazepam on cerebral metabolism and mood in normal volunteers.

The effects of diazepam on regional cerebral metabolism were examined in eight healthy volunteers using positron emission tomography with 18-fluorodeoxyglucose as the tracer. Each subject was tested three times, at 1-week intervals, with placebo, a low oral dose of diazepam (0.07 mg/kg), and a moderate dose of diazepam (0.14 mg/kg). Subjects completed mood questionnaires before and at regular intervals after taking the drug, and performed a vigilance task during the 60-minute period of tracer uptake. The effects of the drug on cerebral metabolism were examined alone and in relation to the subjective and behavioral effects of the drug. Both doses of diazepam decreased global (whole brain) metabolic rate but did not affect specific regions differentially. Subjects experienced sedative like effects during all three scans (placebo as well as drug). Compared to placebo, both doses of diazepam decreased anxiety, and neither dose produced significant impairment of task performance. Neither the subjective nor behavioral drug effects were correlated with the changes in metabolic rate. Thus, diazepam decreased whole brain metabolic rate at doses that produced only modest subjective or behavioral effects. The changes in metabolic rate were not clearly related to other observable drug effects.

Adult↗
PubMed1991

Comparison of adinazolam, amitriptyline, and diazepam in endogenous depressive inpatients exhibiting DST nonsuppression or abnormal contingent negative variation.

Adinazolam, a triazolobenzodiazepine that has an action similar to antidepressants in several pharmacological tests, was compared with amitriptyline and diazepam in endogenous depressive inpatients exhibiting dexamethasone suppression test non-suppression and/or abnormal contingent negative variation. Three parallel groups of 22 patients received in double-blind conditions either adinazolam (60-90 mg/day), amitriptyline (150-225 mg/day), or diazepam (30-45 mg/day) over a 4-week period, with weekly assessments by the Hamilton Rating Scale for Depression. Results showed significant superiority of amitriptyline over diazepam on total Hamilton depression scores. On the endogenomorphy subscale, amitriptyline induced significantly better improvement than both diazepam and adinazolam, whereas both amitriptyline and adinazolam exhibited significantly better antidepressant efficacy on the core symptoms of depression. Moreover, the dropout rate for inefficacy after 2 weeks of treatment was higher in the diazepam group. Taken together, these findings suggest that adinazolam has an antidepressant efficacy intermediate between amitriptyline and diazepam. Adinazolam was, however, much better tolerated than amitriptyline, and produced significantly fewer anticholinergic side effects.

Adult↗
PubMed1990

A comparison of chloral hydrate and diazepam sedation in young children.

The purpose of this study was to compare a high and low dose of diazepam with chloral hydrate in the sedation of young children. Thirty healthy children between the ages of 20 and 48 months, with a mean age of 33.5 months, participated in the study. All children exhibited negative behavior during a screening visit and required at least two restorative appointments with the use of sedation. A dose of either 0.3 mg/kg or 0.6 mg/kg of diazepam at one visit and 50 mg/kg of chloral hydrate at another visit was administered in a double-blind manner. All children were restrained in a Papoose Board with auxiliary head restraint and received 50% nitrous oxide/oxygen during treatment. The degree of sleep, body movement, crying, pulse rate, respiratory rate, and blood oxygen saturation were monitored before and during the operative procedures. Vital signs remained essentially unchanged during treatment, except for transitory elevations of the pulse during periods of stimulation. There were no statistically significant differences among the three drug regimens with regard to movement and crying. Significantly more patients who received chloral hydrate were asleep than when either dose of diazepam was given during the first 60 min of treatment. The only side effect found was vomiting in one patient with both chloral hydrate and diazepam. It is concluded that the sedative effects of chloral hydrate and diazepam are similar when young children are sedated for dental treatment. The use of diazepam might be more advantageous because chloral hydrate produces more sleep during the first hour of treatment.

Anesthesia, Dental↗
PubMed1989

Effects of diazepam and flumazenil on sedation and hypoxic ventilatory response.

We evaluated the effects of a benzodiazepine antagonist, flumazenil (Ro 15-1788), 1 mg intravenous, on the hypoxic ventilatory response in 10 healthy patients who had received diazepam 0.97 +/- 0.34 mg/minute (mean +/- SD) for sedation during minor operative procedures. When assessed using a sedation analog scale, flumazenil significantly decreased diazepam-induced sedation. In only two of the five patients with evidence of diazepam-induced depression of the ventilatory response to hypoxia was there significant reversal of this depression after flumazenil administration. Finally, patients in whom the duration of sedation with diazepam was shorter (78 +/- 14 minutes) had a significantly greater decrease in the slope of their hypoxic ventilatory response curve (1.3 +/- 0.8 L.min-1.%sat-1 [-43% from baseline]) than did patients with longer sedation times (145 +/- 37 minutes duration; 2.0 +/- 0.8 L.min-1.%sat-1 [-5% from baseline]). These data suggest that flumazenil, 1 mg intravenous, is only partially effective in reversing diazepam-induced depression of hypoxic ventilatory drive and that tolerance may develop to the respiratory depressant effects of diazepam.

Adult↗
PubMedDate not supplied

Interaction of intravenous diazepam and bupivacaine in conscious dogs.

The cardiac and hemodynamic effects of bupivacaine, diazepam and their coadministration were evaluated in six mongrel dogs chronically instrumented for recording of mean arterial pressure (MAP), left ventricular (LV) pressure, and cardiac output (CO, electromagnetic flow probe around the ascending aorta). LVdP/dt was derived from the LV pressure signal, and its positive peak was used as an index of myocardial contractility. Heart rate (HR), RR, PR and QT intervals were measured from ECG. At weekly intervals, each dog received in a random order one of the following treatments: (1) saline as control, (2) diazepam (0.2 mg/kg, intravenous, bolus), (3) bupivacaine (0.4 mg/kg intravenous bolus, followed by 15 micrograms/kg/minute, during 30 minutes), and (4) a combination of diazepam and bupivacaine, as in (2) and (3), respectively. Despite its intrinsic cardiodepressant effects, bupivacaine induced a delayed (30-minute) compensatory increase in HR (+ 11%, p less than 0.05) and LVdP/dt (+ 10%, p less than 0.05). Diazepam decreased systemic vascular resistance (SVR; -16%, p less than 0.05) with concomitant increases in HR and CO. After diazepam pretreatment, LVdP/dt did not rise after bupivacaine administration, whereas SVR decreased (-14%, p less than 0.05) and HR increased (+19%, p less than 0.05). The QT-RR relationship remained unchanged regardless of the treatment administered. Thus, diazepam might blunt the compensatory effects of bupivacaine on cardiac function and may decrease the margin of safety of this local anesthetic agent during major neural blockade procedure.

Animals↗
PubMed1989

On acute effects of some drugs on the higher nervous activity in man. Ethanol (0.5 g/kg) and its interaction with diazepam (5 mg) and meclophenoxate (100 mg). Part LVIII.

1. Acute effects of ethanol (0.5 g/kg of body weight) and its interactions with diazepam (5 mg) and meclophenoxate (100 mg) and placebo on the higher nervous activity were tested on a group of 16 healthy and unfatigued volunteers-university students (8 females, 8 males, aged 21 years). The experimental subjects were given the following combinations of the studied drugs: (a) Ethanol plus meclophenoxate, (b) Ethanol plus placebo, (c) Ethanol plus diazepam, (d) Placebo solution plus placebo. The method of artificial conditioned speech connections was made use of. Three statistically balanced trials were always carried out: before, and one and two hours after the administration of the tested drug combinations during the early and late forenoon hours. The investigation-sets consisted of two optic, two complex tactile, and two acoustic associations. The criteria for the evaluation of the results were the number of repetitions necessary for mastering the given task, then the number of correct responses and the frequencies of responses in the first eight repetitions of the sets when the active knowledge of the persons under investigation was tested. 2. One hour after the application, there appeared a statistically significant impairment in NNR and NCR, both after ethanol alone and ethanol in combinations with diazepam and meclophenoxate. The frequency of responses was impaired only after the combination of ethanol plus diazepam. 3. Two hours after the administration, the combinations of ethanol plus diazepam and ethanol plus meclophenoxate impaired significantly the number of necessary repetitions. NCR impairment was observed only after application of ethanol with diazepam. Ethanol administered separately did not impair the followed up characteristics of learning. 4. The most marked effect appeared during the formation of artificial conditioned speech connections with acoustic stimuli.

Adult↗
PubMed1989

Kinetic and dynamic study of intravenous lorazepam: comparison with intravenous diazepam.

Six healthy volunteers received a single i.v. dose of 'low dose' lorazepam (0.0225 mg/kg), 'high dose' lorazepam (0.045 mg/kg) and placebo by 1-min infusion in a double-blind three-way crossover study. Plasma concentrations were measured 24 hr after dosage, and the EEG power spectrum was simultaneously computed by fast-Fourier transform to determine the percentage of total EEG amplitude occurring in the 13-30-Hz range. Low and high dose lorazepam did not differ significantly in distribution volume (1.89 versus 1.81 l/kg) or elimination half-life (11.5 versus 12.2 hr); clearance was slightly although significantly reduced at the higher dose (2.08 versus 1.88 ml/min/kg, P less than .005). EEG effects were of relatively slow onset, reaching their maximum change over baseline 30 min after infusion. The duration of action was prolonged, with the fraction of EEG activity in the 13-30-Hz range still significantly above baseline 8 hr after the 0.045 mg/kg dose. Five of these subjects received 0.15 mg/kg of i.v. diazepam in a companion study of identical design. EEG effects of diazepam were shorter than those of lorazepam, probably because of the more rapid and extensive decline in plasma diazepam concentrations in the postinfusion distribution phase. In addition, the onset of diazepam's effect was immediate. In male CD-1 mice that received i.v. diazepam (8.3 mg/kg) or lorazepam (3.3 mg/kg), the brain:plasma concentration ratio was maximal 2.5 min after dosage for diazepam, but equilibration was delayed at least 30 min after dosage for lorazepam. Thus the slow onset of action of lorazepam is probably attributable to slow entry into brain.

Adult↗