Diazapam химические свойства, назначение, производство
Химические свойства
Light Yellow Crystalline Solid
Использование
Anxiolitic; muscle relaxant (skeletal); anticonvulsant.
Controlled substance (depressant)
Общее описание
Off-white to yellow crystalline powder. Practically odorless. Tasteless at first with a bitter aftertaste.
Реакции воздуха и воды
Hydrolysis occurs in aqueous solutions with a maximum stability around pH 5. . Insoluble in water.
Пожароопасность
Flash point data for Diazapam are not available; however, Diazapam is probably combustible.
Биологическая активность
Ligand at the GABA A receptor benzodiazepine modulatory site. Anxiolytic, anticonvulsant and sedative/hypnotic agent.
Фармакокине?тика
The second group of antispastic drugs to be developed were the benzodiazepines, typified by
diazepam. Diazepam exerts its skeletal muscle relaxant effect by binding as an agonist at the
benzodiazepine receptor of the GABAA receptor complex, which enhances GABA potency to increase chloride
conductance. The muscle relaxant properties of classical benzodiazepines,
such as diazepam, appear to be mediated mainly by the GABAA α2 and α3 subunits. The
result is neuronal hyperpolarization, probably at both supraspinal and spinal sites for spasmolytic
activity. Its actions are sufficient to relieve spasticity in patients with lesions affecting the spinal
cord and in some patients with cerebral palsy.
Побочные эффекты
Few high-quality clinical trials have evaluated
diazepam as a muscle relaxant, but these few suggest that diazepam is no more efficacious than,
for example, carisoprodol, cyclobenzaprine, or tizanidine (i.e., efficacy is marginal).
Moreover, diazepam produces drowsiness and fatigue in most patients at doses required to
significantly reduce muscle tone.
Профиль безопасности
Poison by ingestion,
parenteral, subcutaneous, intravenous, and
intraperitoneal routes. Moderately toxic by
skin contact. Questionable carcinogen with
experimental tumorigenic data. Human
systemic effects: dermatitis, effect on
inflammation or mediation of inflammation,
change in cardiac rate, somnolence,
respiratory depression, and other respiratory
changes, visual field changes, diplopia
(double vision), change in motor activity,
muscle contraction or spasticity, ataxia (loss
of muscle coordination), an antipsychotic
and general anesthetic. Human reproductive
effects by ingestion and intravenous routes
causing developmental abnormalities of the
fetal cardiovascular (circulatory) system and
postnatal effects. Experimental teratogenic
and reproductive effects. Human mutation
data reported. An allergen. A drug for the
treatment of anxiety. When heated to
decomposition it emits very toxic fumes of
Cl and NOx.
Метаболизм
Diazepam is rapidly and completely absorbed after oral administration. Maximum peak blood concentration occurs in
2 hours, and elimination is slow, with a half-life of approximately 20 to 50 hours. As with chlordiazepoxide, the major
metabolic product of diazepam is N-desmethyldiazepam, which is pharmacologically active and undergoes even
slower metabolism than its parent compound. Repeated administration of diazepam or chlordiazepoxide leads to
accumulation of N-desmethyldiazepam, which can be detected in the blood for more than 1 week after
discontinuation of the drug. Hydroxylation of N-desmethyldiazepam at the 3-position gives the active metabolite
oxazepam.
Перевозки
UN2811 Toxic solids, organic, n.o.s., Hazard
Class: 6.1; Labels: 6.1-Poisonous materials, Technical
Name Required. UN3249 Medicine, solid, toxic, n.o.s.,
Hazard Class: 6.1; Labels: 6.1-Poisonous materials.
Diazapam препаратная продукция и сырье
сырьё
препарат