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At least 19 recordsLinked to original sources
PubMed1995

[Comparison of the effectiveness of orally administered clorazepate dipotassium and nordiazepam on preoperative anxiety].

Clorazepate dipotassium (Tranxilium) is one of the benzodiazepines which is widely used for oral premedication. After oral administration it is decarboxylated to its active metabolite nordiazepam (desmethyldiazepam). Nordiazepam is also commercially available in the form of drops (Tranxilium N). The aim of the present study was to compare the effect of these drugs on preoperative anxiety. One hundred and eight patients scheduled for orthopaedic surgery (ASA I-II) were studied. Medication was administered at 10 p.m. the evening before surgery (E) and at 7 a.m. on the morning of surgery (M). There were four groups: 1) E no medication; M clorazepate dipotassium; 2) E no medication; M nordiazepam; 3) E clorazepate dipotassium; M clorazepate dipotassium, 4) E clorazepate dipotassium; M nordiazepam. Dosages were: clorazepate dipotassium: body weight < 55 kg: 10 mg; body weight > 55 kg: 20 mg; nordiazepam: 1 gtt/kg; 5 mg = 24 gtt). Anxiety was measured by using the self-evaluating Erlangen anxiety scales, which measure both background and situational anxiety. Background anxiety (EAS-H) was evaluated during the evening before surgery; situational anxiety (EAS-S) was evaluated at the same time and also on the day of surgery before premedication and immediately before surgery. Pulse rate was measured each time the test was administered. There were no differences between the groups in sex, age, weight or the intervals between premedication and anaesthesia induction (p > 0.05). There were no statistically significant differences between the groups with respect to background anxiety. Situational anxiety did not significantly increase or decrease at any of the testing times, nor were there any differences between the groups (p > 0.05). Heart rate did not vary between the groups or with time (p > 0.05). In this group of patients undergoing elective orthopaedic procedures, clorazepate prevented a rise in anxiety in the immediate preoperative period. Since clorazepate is rapidly metabolized to nordiazepam when administered orally it might be predicted that the two drugs have similar properties. This hypothesis is confirmed by the results of the present study. We conclude that orally administered clorazepate dipotassium and nordiazepam have a similar effect on preoperative anxiety.

Administration, Oral↗
PubMed1996

[Anxiolysis, sedation, and stress reduction following oral premedication with midazolam in adults. A comparison with dipotassium clorazepate and placebo].

Benzodiazepines are the most commonly used anxiolytic agents. Among the benzodiazepines, midazolam has the advantage of a short elimination half-life, which is especially useful in outpatient surgery. However, in contrast to other commonly prescribed benzodiazepines, such as chlorazepate dipotassium, oral premedication with midazolam has not been thoroughly investigated. Therefore, the present study was performed to compare anxiolysis, sedation and stress reduction with midazolam and clorazepate dipotassium in adults. METHODS. After IRB approval and informed consent had been obtained, 85 patients scheduled for breast biopsy were studied. The patients were chosen at random to receive either 7.5 mg midazolam (n = 29), 20 mg clorazepate dipotassium (n = 28) or placebo (n = 28) preoperatively. Before premedication, immediately prior to surgery and postoperatively in the recovery room, the following parameters were determined with visual analogue scales (VAS): "asthenia," "depression," oral salivation, muscle tension, motoric restlessness and sweating of the palms. In addition, anxiety (STAI-G-X-1, Spielberger), heart rate and arterial blood pressure were measured. Before patients underwent surgery, the degree of sedation was evaluated by the anaesthesiologist. RESULTS. Clorazepate dipotassium and midazolam both caused a reduction in anxiety as compared with the placebo (P < 0.05). Only clorazepate dipotassium reduced anxiety postoperatively (P < 0.05). Neither midazolam nor clorazepate dipotassium caused a reduction in "asthenia" and "depression." Midazolam was more effective in preventing increased blood pressure than clorazepate dipotassium and the placebo (P < 0.05). Furthermore, after premedication with midazolam, salivation, muscle tension, motoric restlessness and sweating of the palms remained stable, in contrast to the results after premedication using clorazepate dipotassium or placebo (P < 0.05). CONCLUSIONS. The anxiolytic effects of 7.5 mg midazolam and 20 mg clorazepate dipotassium were similar after oral application. However, the anxiolytic effect of midazolam is shorter-lived than that of clorazepate dipotassium. In contrast to clorazepate dipotassium, midazolam produced no increase in arterial blood pressure and stabilized oral salivation, production in the palms, muscle tension and motoric restlessness.

Adult↗
PubMed1998

Anticonvulsant effects of dipotassium clorazepate on hippocampal kindled seizures in rats.

We examined the anticonvulsant properties of dipotassium clorazepate (DC) against hippocampal kindled seizures in rats. Adult male Wistar rats were subjected to kindling 1 week after the implantation of electrodes. After five stage 5 seizures were induced, the generalized convulsion triggering threshold (GST) was determined. Dipotassium clorazepate was administered intraperitoneally in rats that showed two stable stage 5 seizures induced at the GST current intensity. Dipotassium clorazepate at doses of 1 mg/kg or more produced an anticonvulsant effect, but did not readily suppress limbic seizures. Dipotassium clorazepate did not completely suppress after-discharges (AD) even at the highest dose, which was 5 mg/kg. Moreover, raised stimulus intensity failed to affect its efficacy as an anticonvulsant. The results of the present study suggest that DC has a modest anticonvulsant potency. It is reasonable to assume that its anticonvulsant efficacy is primarily due to attenuation of AD propagation rather than the raising of the seizure triggering threshold at the kindling focus.

Animals↗
PubMed2000

Stability of the powdered dosage form prepared by unsealing the capsules: water vapor sorption and discoloration of the powdery contents of clorazepate dipotassium capsules.

The hygroscopicity of the contents of clorazepate dipotassium (Mendon) capsules (CM) was investigated by storage at various relative humidities (RHs). The CM adsorbed water vapor significantly at more than 75% RH. At the same time, a marked discoloration of CM from white to yellow was also observed during storage. On the basis of differential scanning calorimetry (DSC) and Fourier transform (FT) Raman spectroscopy, the discoloration seemed to be due to the change in clorazepate dipotassium to nordiazepam and other substances. It was found that, when opening of the Mendon capsule is necessary to prepare the powdered dosage form, the CM should be stored below 60% RH to avoid the adsorption of water vapor and discoloration.

Anti-Anxiety Agents↗
PubMed1997

[Optimizing anesthesiologic premedication with reference to biopsychological theories. Exemplified by the effect of dipotassium clorazepate and zolpidem in combination with promethazine].

UNLABELLED: The following double-blind randomized placebo-controlled study dealt with three questions: 1. Are differentiated psychometric test systems suitable measuring emotions before anaesthesia? 2. What are the effects of different doses of zolpidem (8.03 mg vs. 16.06 mg) compared with dipotassiumclorazepat (10 mg vs. 20 mg) on emotions in premedication? 3. Is the combination with Promethazin suggestive? METHOD: 320 patients were randomly assigned to different regimes of preanaesthetic medication. As primary premedication they received either zolpidem 8.03 mg or zolpidem 16.06 mg or dipotassium clorazepate 10 mg or dipotassium clorazepate 20 mg or placebo. The secondary premedication was either promethazine 50 mg or placebo. The tablets/dragees were given in the evening before surgery (09.00 p.m.-10.00 p.m.). Every cell of the 5 x 2-factorial design contained 16 men and 16 women. Emotions were measured by a multidimensional rating scale, comprising the aspects elated mood, anxiety, hostility, deactivation, vigilance and introversion. In addition, somatic symptoms and the quality of sleep were measured. Statistics were performed using multivariate analysis of variance. RESULTS: No differing effects of zolpidem and dipotassium clorazepate on preoperative mood were found. There was also no difference compared with placebo. Compared with placebo, promethazin leads to greater deactivation. Specific emotions were not affected. In somatic aspects there was a greater amount of cholinergic effects under promethazine, which was mainly expressed by a higher intensity of a dry mouth and weakness in general. Compared with placebo all of the tested drugs led to a better quality of sleep. CONCLUSIONS: Using multidimensional rating scales and considering emotions as a multifactorial construct, the study shows no different effects of benzodiazepines or benzodiazepin-like drugs on preoperative mood. No differences were also found on comparing these drugs with placebo. However, a better quality of sleep was seen under zolpidem and dipotassium clorazepate compared with placebo. The study shows that a combination with promethazine is recommended, because promethazine has a selective deactivating effect. The study stresses the significance of multidimensional rating scales for the measurement of emotions before anaesthesia.

Adult↗
PubMed1999

Effect of dipotassium clorazepate on amygdaloid-kindling and comparison between amygdaloid- and hippocampal-kindled seizures in rats.

We examined the effect of dipotassium clorazepate (7-chloro-1, 3-dihydro-2-oxo-5-phenyl-1H-1, 4-benzodiazepine-3-carboxylate potassium hydroxide), an antianxiety drug, on amygdaloid kindling and compared its effects for 7 successive days on amygdaloid- versus hippocampal-kindled seizures, using the rat kindling model of epilepsy. Dipotassium clorazepate at 5 mg/kg significantly delayed amygdaloid kindling. The contralateral cortical after-discharge duration in the dipotassium clorazepate-treated group was significantly shorter than the after-discharge duration in the amygdala in the first seven stimulations, whereas it was significantly shorter only in the first three stimulations in the control group, indicating that dipotassium clorazepate suppressed the spread of seizure activity from focus to contralateral cortex. Dipotassium clorazepate suppressed amygdaloid-kindled seizures at 2 and 5 mg/kg, while 1 mg/kg or more suppressed hippocampal-kindled seizures. Thus, differences in effective dosages in both amygdaloid- and hippocampal-kindled seizures may suggest a difference in the neuronal mechanisms involved in this kindling.

Amygdala↗
PubMed1993

[Oral premedication with clorazepate dipotassium. Comparison with oral premedication with flunitrazepam and intramuscular premedication with promethazine, pethidine and atropine in adults].

UNLABELLED: The purpose of premedication and the best form have been frequent subjects of controversy among anaesthetists in the past few years. Anxiolysis is now accepted as the main purpose. The preferred route of administration is by mouth. The intention of this study was to examine whether clorazepate dipotassium has the same sedative-hypnotic and anxiolytic effects as i.m. premedication with promethazine, pethidine and atropine. METHODS: A total of 100 patients aged 20-65 years and due to undergo arthroscopy took part in this study. Patients in group I were given 1 mg flunitrazepam p.o. on the evening before the operation and the i.m. premedication described above. The premedication for group II consisted in clorazepate dipotassium, 50 mg on the evening before operation and 25 mg on the morning of the day of the operation. The sedative-hypnotic effects were measured on a four-point scale. The Erlangen anxiety scale (EAS) and a visual analogue scale (VAS) were used to evaluate the anxiolytic effects according to the patient's own and the observer's evaluation of mood. In addition to this, we measured amnesia, heart rate and blood pressure. RESULTS: Clorazepate dipotassium or flunitrazepam p.o. significantly reduces anxiety 1 h after administration as measured by the EAS (P < 0.05) on the evening before the operation. This result was not, however, confirmed by the VAS for self-assessment. Patients who received premedication with clorazepate dipotassium are less anxious on the morning of the operation than patients given flunitrazepam the evening before the operation (P < 0.05); this, however, does not correspond to the VAS results. There were no differences in the other parameters compared. DISCUSSION: Oral premedication with clorazepate dipotassium has the same sedative-hypnotic, anxiolytic and amnestic effects as i.m. premedication with promethazine, pethidine and atropine. The results of this study are better than those obtained by Tolksdorf et al., owing to the higher dosage used in our study (50 mg as against 20 mg). Tolksdorf et al. [21] failed to show any improvement on a placebo. Our results correspond to those of Drautz et al. [2] who used 50 mg of clorazepate dipotassium on the evening before and 25 mg on the morning of the day of the operation.

Administration, Oral↗
PubMed1992

Sorption studies of dipotassium clorazepate salt (Tranxène) and midazolam hydrochloride (Hypnovel) in polyvinyl chloride and glass infusion containers.

The compatibilities of dipotassium clorazepate and midazolam hydrochloride with polyvinyl chloride (PVC) bags have been studied and compared with those observed with glass flasks. At room temperature, dipotassium clorazepate showed chemical instability which was independent of the container. At 4 degrees C, dipotassium clorazepate showed no decrease in concentration over 12 h, both in 5% dextrose solution and 0.9% sodium chloride solutions. When stored for longer periods of up to 72 h, a slight decrease not exceeding 5% was observed. The compatibility of midazolam with the PVC bags was found to be good at room temperature. It was slightly better in 5% dextrose solution than in 0.9% sodium chloride solution. High sorption of the drug was observed at pH 7.0 when the primary ring structure is maintained. The results make it possible for the hospital pharmacist to prepare dipotassium chlorazepate salt and midazolam admixtures up to 3 days before administration, provided the former are stocked in a refrigerator and the latter are prepared in dextrose isotonic solutions.

Chemistry, Pharmaceutical↗
PubMed2003

Clorazepate dipotassium versus midazolam for premedication in clear corneal cataract surgery.

PURPOSE: To evaluate and compare the efficacy of oral clorazepate dipotassium (Tranxilium) and intravenous midazolam (Dormicum) as premedication agents in retrobulbar anesthesia and clear corneal phacoemulsification with intraocular lens (IOL) implantation. SETTING: Department of Ophthalmology, University of Essen, Essen, Germany. METHODS: In a prospective clinical trial, 97 consecutive patients (97 eyes) having phacoemulsification with implantation of a foldable IOL were randomized to 2 groups. The first group received 10 mg oral clorazepate dipotassium and the second group, 1 mg intravenous midazolam. The surgeon's subjective experience of patients' cooperation during retrobulbar anesthesia and after surgery was measured on a 5-point Likert scale. The duration of surgery and rate of complications were documented. One day after surgery, the patients' subjective comfort during cataract surgery was evaluated using a 5-point Likert scale and the best corrected visual acuity was determined. RESULTS: The level of anterograde amnesia tended to be higher in the midazolam group than in the clorazepate dipotassium group (4% versus 0% for anesthesia administration; 14% versus 4% for surgery), but the difference between groups was not significant. There were no significant differences in patient cooperation or complications during surgery. Patient satisfaction scores were not significantly different between the groups (P<.14); however, patients in the midazolam group expected to have significantly less pain during surgery (P<.04). The rate of potential visual acuity recovery was similar between groups. CONCLUSIONS: Anterograde amnesia occurred more frequently and patients expected less pain before surgery with midazolam. Both anesthetic agents provided safe and effective premedication for retrobulbar anesthesia in clear corneal cataract surgery.

Administration, Oral↗
PubMed1993

A post-marketing surveillance survey on the use of dipotassium clorazepate in clinical practice in the Philippines.

A post-marketing surveillance survey of dipotassium clorazepate usage was carried out in the Philippines between July 1990 and April 1991. Data were analyzed on 562 patients suffering from conditions in which anxiety was a major component. The results suggest that the medication was prescribed in accordance with the generally accepted best practice for benzodiazepines. Overall, 85% of patients were reported to have recovered and only 2% reported minor side-effects. Dipotassium clorazepate was thus confirmed to be a highly effective and relatively safe anxiolytic agent.

Adolescent↗
PubMed1977

Steady-state bioavailability of two clorazepate dipotassium dosage forms.

A specially designed tablet dosage form of the benzodiazepine clorazepate dipotassium (Tranxene) was developed for once-a-day administration. The drug was administered at a dose of 22.5 mg as (1) the tablet, (2) three 7.5 mg capsules, or (3) one 7.5-mg capsule given every 6 hours. Peak serum levels from the tablet were intermediate between those of the single- and divided-dose capsule regimens. The desired decrease in magnitude of peak levels was obtained without affecting the extent of absorption. Pharmacokinetic analysis of the data according to a two-compartment open model with first-order absorption indicated that the serum half-life (t0.5beta) of nordiazepam, the major biotransformation product present in serum, was about 48 hours and served as a basis for the design of a multiple-dose steady-state study. Multiple-dose administration of the tablet and divided-capsule regimen to two groups of subjects for ten days indicated each dosage form yielded similar minimum steady-state serum levels of about 0.6 micrograms/ml which plateaued following seven days of drug administration. The dosage forms were crossed over between the groups on day 11 and administered for an additional four days. The minimum serum levels obtained with the tablet and capsule were not statistically different. Additionally, the peak serum level and area under the curve (pi=24 hours) at steady state were equivalent between the dosage forms. Good agreement was obtained between model-predicted and observed serum levels during multiple-dose administration for both the tablet and capsule regimens. The serum half-life of nordiazepam following 14 days of clorazepate dipotassium administration was similar to that found after a single dose. These results indicate that a single daily dose of drug as the tablet produced serum levels equivalent to a divided-capsule regimen.

Adult↗
PubMed1978

[Determination of dipotassium clorazepate in the plasma by gas chromatography (author's transl)].

The authors present a method of estimation of dipotassium clorazepate by gas chromatography with a detector for electron capture. It requires 2 ml of blood. Two separate extractions are necessary, including one immediately after the sampling to determine the nordiazepam present at the time of the blood sample. The second extraction permits one to determine the total nordiazepam obtained by transformation of all the dipotassium clorazepate. This method is simple and rapid and permits one to determine with precision, specificity and good reproducibility (CV -- 3%) the therapeutic concentrations of this drug.

Anti-Anxiety Agents↗
PubMedDate not supplied

[Evaluation of dipotassium clorazepate in pre-anesthetic medication].

The anxiolytic action of clorazepate 15 mg PO on the eve and 1 hour before the surgical procedure was studied in 50 ASA class 1 patients (18-60 years old, 46-86 kg) scheduled for elective non-oncological surgery. Anxiety, assessed by the anaesthetist employing a modified Hamilton Anxiety Scale, was lower after premedication in 46 patients (p less than 0.01) and only few side-effects were noted. As a conclusion we suggested that clorazepate PO as anaesthetic premedication is suitable for anxiety relief.

Adult↗
PubMed1986

[Initial experience with preorally administered dipotassium clorazepate and tilidine-naloxone in extracorporeal shockwave lithotripsy].

After 70 treatments with extracorporeal shock wave lithotripsy (ESWL), using a combination of dipotassiumclorazepate p.o. 12 h before treatment and tilidin-naloxon 45 min before ESWL, 56 patients reported to be painfree or only minor, well-tolerable pain. Informed consent was obtained in all patients for this pilot study, leaving the possibility of further pain medication. 7 patients asked for an additional analgesic (fentanyl) and another 7 patients required a sedative (midazolam). No further anesthesiologic procedures were necessary. Nausea was observed in one patient as a possible side-effect of tilidin. To confirm these preliminary results, a prospective randomized study is currently conducted.

Administration, Oral↗
PubMed1978

[Treatment of general psychovegetative disorders with a single night dose of dipotassium-clorazepate within a multicenter study (author's transl)].

The therapeutical effect of Tranxilium was studied in an open multicenter study by 66 general practitioners and 26 specialists. 1.027 patients were treated with Tranxilium 20, given in a single dose at night, for a period of three weeks. During this time, the patient's psychic status and functional organic disorders were assessed by means of rating scales. A complete medical assessment followed at the end of the study. States of anxiety, restlessness, depressive mood, irritation and insomnia as well as functional organic disorders improved significantly (p is less than 0.001) already after the first week of treatment. At the end of treatment, with the majority of patients the above symptoms had either completely disappeared or were found only to a small extent. In 85% of the patients, all investigators rated the stabilization and brightening effect on psychic conditions as well as the harmonizing effect on disturbed organic functions as "very good" to "good". In 89% of the patients, the overall therapeutic success was judged as "very good" to "good". The overall tolerance was excellent in 96% of the cases.

Anti-Anxiety Agents↗