Anxiolytic of benzodiazepines group chlordiazepoxide, has anxiolytic, sedative, myorelaxing, anticonvulsant action. Anxiolytic action is associated with increased GABAergic inhibition in the central nervous system. The GABAA-receptor-C1~-channel complex contains a benzodiazepine receptor, the stimulation of which leads to conformational changes of the GABA-receptor, resulting in increased sensitivity to GABA. This leads to increased permeability of the GABA-receptor channel for chlorine ions. Ingestion of negatively charged chlorine ions into the neuron leads to hyperpolarization of the membrane and inhibition of neuronal activity.
Anticonvulsant effect is associated with suppression of epileptogenic activity by strengthening inhibitory GABAergic processes in the central nervous system. Miorelaxing effect is associated with suppression of spinal polysynaptic reflexes and disturbance of their supraspinal regulation.In small doses it has sedative effect, in case of increase – sleeping pills.With prolonged use, a drug dependence is formed. After taking the drug, withdrawal symptoms are possible.
After taking inside on an empty stomach up to 75% is absorbed in the gastrointestinal tract. The maximum concentration in plasma is reached after 0.5-4 hours. The binding with plasma proteins is 96%. https://pubchem.ncbi.nlm.nih.gov/compound/Chlordiazepoxide. It is deposited in the adipose tissue. It penetrates through hematoencephalic and placental barrier and enters breast milk.
Metabolism in liver with formation of 4 active metabolites with periods of semi elimination: oxazepam – 5-15 hours, desmethylchlordiasepoxide – 8-24 hours, demoxepam – 14-95 hours, desmethyldiasepam – 40-250 hours.
It is use in neurosis-like and neurotic conditions accompanied by fear and anxiety. It is used for premedication before surgical intervention and for injection into anesthesia. It is uCsed to relieve withdrawal syndrome in chronic alcoholism, substance abuse, drug addiction, as well as for the treatment of diseases manifested by increased muscle tone: epilepsy, schizophrenia, psychopathic agitation, specific personality disorders, insomnia.
Liver and kidney failure, closed-angle glaucoma, myasthenia, pregnancy and lactation, children under 4 years of age, individual intolerance.
Kidney and liver diseases, chronic respiratory failure, sleep apnea syndrome.