In the late 1980s and early 1990s a number of non-selective partial agonists, exemplified by bretazenil, pazinaclone and abecarnil, were described.
However, despite their proven clinical anxiolytic efficacy, such compounds possess a relatively narrow window between doses that produce anxiolysis and those that cause sedation, and are also associated with physical dependence and a potential for abuse. Non-selective benzodiazepine (BZ) binding-site full agonists, exemplified by diazepam, act by enhancing the inhibitory effects of GABA at GABA(A) receptors containing either an alpha1, -2, -3 or -5 subunit. Product label Diazepam Auto-injector Last revised: September 1997 by a syringe (operated manually) indicates that the mean percent availability of the drug from the autoinjector is 100% of that obtained from the syringe. Injection of 10 mg of diazepam in the mid-anterior/lateral thigh by the autoinjector versus 10 mg I.M. A study performed in 24 healthy male subjects comparing the I.M. Injections into animals have produced localized irritation of tissue surrounding injection sites and some thickening of veins after intravenous use. Diazepam was found to have transient cardiovascular depressor effects in dogs, Long-term experiments in rats revealed no disturbances of endocrine function. However, animals treated with diazepam do have a transient ataxia at higher doses. Diazepam, unlike chlorpromazine and reserpine, has no demonstrable peripheral autonomic blocking action, nor does it produce extrapyramidal side effects. In animals, diazepam appears to act on parts of the limbic system, the thalamus and hypothalamus, and induces calming effects.
Evidence-based medicine for Chemical Defense - including efficacy and safety A. The anticonvulsant diazepam has been used therapeutically in the treatment of both convulsant (e.g., picrotoxin, hydrazine, strychnine, tetramethylenedisulfotetramine) and cholinergic (e.g., sarin (GB), soman (GD), cyclosarin (GF), tabun (GA), VX, and organophosphorus pesticides) agents to enhance the inhibitory effect of gamma-aminobutyric acid at GABA(a) receptors and limit excess central nervous system excitation and seizures. Chemical Defense therapeutic area(s) - including key possible uses Name of Chemical Defense therapeutic agent/deviceĭiazepam 2.
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