Disease relevance of Chlorazepate

• Five pregnant Long-Evans rats were given 32 mg/kg of body weight of clorazepate dipotassium (Tranxene) intramuscularly on gestational days 8.5, 9.5, and 10 [1].
• We report a woman who developed a generalized exanthem 1 day after receiving chlorazepate and four other drugs related to anaesthesia for surgery of the larynx [2].
• OBJECTIVES: The purpose of this study was to detect drug allergy to chlorazepate or a metabolite in vitro by means of the lymphocyte transformation test (LTT), and to determine the concentrations of the T-helper (Th) 2-type cytokine interleukin (IL)-5 and the Th1-type cytokine interferon (IFN) -gamma in the culture supernatants [2].
• Hypersensitivity to chlorazepate dipotassium [3].
• 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 [4].

Psychiatry related information on Chlorazepate

• 1. Repeated nocturnal doses of 30 mg clobazam and dipotassium chlorazepate 15 mg showed no significant effects compared to matching placebo on tests of psychomotor performance and serial subtraction of numbers given in the morning and afternoon of the day following treatment [5].
• 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 [6].
• Although the treatment of panic disorder and agoraphobia has been best studied with the benzodiazepine alprazolam, it now appears likely that other benzodiazepines, for example diazepam, lorazepam and chlorazepam, may also be effective when correctly used [7].
• Clorazepate dipotassium produced statistically significant impairment in attention and simple reaction time compared with placebo [8].

High impact information on Chlorazepate

• Chlorazepate in temporal lobe epilepsy [9].
• Cytochrome P450 2E1 activity was significantly increased in alcoholic patients treated with chlorazepate (1.16 +/- 0.40 vs. 0.27 +/- 0.03, P < .05) [10].
• Clorazepate dipotassium (Tranxene), an anticonvulsant benzodiazepine, was tested for teratogenicity by injecting ten pregnant Long-Evans rats with 32 mg/kg of body weight intramuscularly on days 8.5, 9.5, and 10.5 of gestation [11].
• Pharmacokinetics of chlorazepate after intravenous and intramuscular administration [12].
• Pharmacokinetics of N-desmethyldiazepam in healthy volunteers after single daily doses of dipotassium chlorazepate [13].

Chemical compound and disease context of Chlorazepate

• The effects of repeated nocturnal doses of clobazam, dipotassium chlorazepate and placebo on subjective ratings of sleep and early morning behaviour and objective measures of arousal, psychomotor performance and anxiety [5].

Biological context of Chlorazepate

• An analysis of the main target symptom revealed better effects of chlorazepate on the following items: anxiety, feeling of muscular tension and gastro-intestinal disturbances [14].
• Steady-state bioavailability of two clorazepate dipotassium dosage forms [15].
• To apply this method, a competitive binding of L-tryptophan and one benzodiazepin (dipotassium chlorazepate) for human serum albumin is perfectly demonstrated [16].
• The hygroscopicity of the contents of clorazepate dipotassium (Mendon) capsules (CM) was investigated by storage at various relative humidities (RHs) [17].

Anatomical context of Chlorazepate

• In vitro drug allergy detection system incorporating human liver microsomes in chlorazepate-induced skin rash: drug-specific proliferation associated with interleukin-5 secretion [2].
• Blisters of the skin in coma induced by amitriptyline and clorazepate dipotassium. Report of a case with underlying sweat gland necrosis [18].
• RESULTS: In the LTT, no T-cell reactivity was observed to the parent compound chlorazepate, whereas coincubation of the drug with human liver microsomes yielded proliferative T-cell reactivity, which was associated with secretion of IL-5 but not of IFN-gamma [2].

Associations of Chlorazepate with other chemical compounds

• 1. Behavioural activity (delayed differentiation and spatial delayed alternation) and pharmacokinetics of diazepam and its metabolites, N-desmethyldiazepam (nordiazepam), 3-hydroxydiazepam (temazepam) and 3-hydroxy-N-desmethyldiazepam (oxazepam), and of dipotassium clorazepate (clorazepate), were studied in the monkey (Macaca mulatta) [19].
• After oral premedication with 20 mg clorazepate dipotassium, anesthesia was induced with etomidate (0.2 mg/kg intravenously [IV]) [20].
• 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 [6].
• Intramuscular bioavailability of chlorazepate as compared to diazepam [21].
• Clinical trials have demonstrated that buspirone (BuSpar) is effective in the treatment of anxiety with efficacy and dosage comparable to diazepam or chlorazepate [22].

Gene context of Chlorazepate

• The association constants and the enthalpy variations are equal to 14 000 +/- 2000 M-1 and --6.6 +/- 0.2 kcal/mol for human serum albumin . tryptophan complex and 13 000 +/- 1000 M-1 and --10.0 +/- 0.2 kcal/mol for human serum albumin . chlorazepate complex [16].

Analytical, diagnostic and therapeutic context of Chlorazepate

• Chlorazepate for premedication [23].
• After oral administration of DMDZ in tablet form (10 mg), or of clorazepate dipotassium in capsule form (15 mg), systemic availability of DMDZ from each of the oral dosage forms was not significantly different from 100% [24].
• Patch tests pointed to chlorazepate as the culprit drug for the skin rash [2].
• The validity of the WARS was determined by correlation with the Hamilton Anxiety Rating Scale (HARS) in a single-blind study in which 20 chronically anxious patients consecutively received placebo (three days), 15 mg clorazepate dipotassium (two weeks), and 22.5 mg clorazepate dipotassium (two weeks) [25].
• 5 patients with chronic renal failure on maintenance hemodialysis and 5 healthy matched controls received single 20-mg intravenous doses of clorazepate dipotassium [26].

References