Pharmacological properties

The tranquilizer of the benzodiazepine group, has an anxiolytic, sedative, miorelaxing and anticonvulsant effect, potentiating the effects of the GABAergic system by stimulating the central action of GABA, the main inhibitory mediator of the brain. Benzodiazepine derivatives act in the same way as benzodiazepine receptor agonists that form a component of a functional supramolecular unit known as the benzodiazepine receptor complex-GABA-chloro-ionophore located on the neuron membrane.

Due to the selective stimulating effect on the GABA receptors in the ascending reticular formation of the brainstem, it reduces the excitation of the cortex, limbic region, thalamus and hypothalamus and exerts an anxiolytic and sedative-hypnotic effect. Due to the inhibitory effect on polysynaptic spinal reflexes, it has a miorelaxing effect.

Diazepam is rapidly and completely absorbed in the digestive tract; the maximum concentration in the blood plasma is reached after 30-90 minutes after ingestion diazepam and zopiclone. After the / m injection also occurs its full absorption, although this process is not always faster than after oral administration. The diazepam elimination curve has a two-phase character: after the initial phase of rapid and extensive distribution with a half-life of up to 3 hours, a prolonged terminal elimination phase follows (with a half-life of up to 48 hours). Diazepam is metabolized to pharmacologically active nordiazepam (half-life – 96 h), hydroxydiazepam and oxazepam. Diazepam and zopiclone and its metabolites bind to plasma proteins (diazepam 98%); are mainly excreted in the urine (about 70%) in the form of free or conjugated metabolites.

The half-life may increase in newborns, elderly and senile patients and in patients with liver or kidney disease; in order to achieve an equilibrium concentration in the blood plasma may take a longer time. Diazepam and its metabolites pass through the BBB and placental barrier. They are also detected in breast milk at a concentration of approximately 1/10 of the concentration in the mother’s blood plasma.

Indications

Inside for symptomatic therapy of patients in an anxiety state (may manifest as a worrisome mood, behavior and / or functional, vegetative or motor equivalent – palpitation, excessive sweating, insomnia, tremors, anxiety, etc.), agitation and stress in neuroses and transient reactive states; as an auxiliary tool in the expressed mental and organic disorders.

Parenterally applied diazepam and zopiclone to provide sedative effect before stressful medical or diagnostic procedures, such as electroimpulse therapy, cardiac catheterization, endoscopy, some radiological examinations, small volume operations, dislocation and bone repositioning in fractures, biopsy, bandaging of burn wounds, etc .; to eliminate anxiety, fear, prevent acute stress; for premedication before surgical intervention in patients experiencing a sense of fear or tension; in psychiatry to eliminate the state of excitement associated with acute anxiety and panic, as well as motor excitation, paranoid-hallucinatory states, alcoholic delirium; for emergency treatment of epileptic status and other convulsive conditions (tetanus, eclampsia); with the aim of facilitating the flow of the first period of labor.

Both ways of administration are used to eliminate reflex muscle spasms with local damage (trauma, wound, inflammation); as an effective adjuvant to relieve spastic conditions caused by damage to spinal and supraspinal intermediate neurons (for example, in cerebral palsy and paraplegia, diazepam and zopiclone with athetosis and rigor mortis).