Stefania gladkaya – Stephania glabra Miers
Herbaceous tropical plant family lunosemyanikovyh (Menispermaceae) with large tubers and roots off of it. Tuber weight reaches 30-50 kg. For medical purposes, they prepare the roots of plants.
Chemical Stephanie smooth structure
The roots and rhizomes contain alkaloids Stephanie smooth: cikleanin, stefarin (stephaglabrin), tsalmatyn, koridin, gindarin etc.. Gindarin stefarin and chemical structure are derivatives of isoquinoline.
Pharmacological properties Stephanie smooth
The biological activity of Stephanie smooth depends mainly on the content of alkaloids in the plant and gindarina stephaglabrine, the pharmacological properties of which determine its therapeutic value. Experimental research has shown gindarina, that when administered intraperitoneally in doses of 5-25 mg / kg significantly suppresses alkaloid as a spontaneous, and induced locomotor activity fenaminom, It is a central phenomenon in animals miorelaxation, It has an inhibitory effect on conditioned reflexes, reduces the aggressiveness of the animals, It lowers the body temperature. In high doses, the alkaloid has anticonvulsant effect in convulsions, caused Corazol, electroshock, strychnine and nicotine, It has analgesic properties.
As shown by experiments on the interaction gindarina serotonin and noradrenaline, gindarin reduces the content of biogenic amines in the brain and intestine, which indicates a selective sensitivity of certain parts of the regulation of neurotransmitters in the mechanism of action alkaloid.
In studying the effect gindarina on bioelectric activity of the brain, conducted experiments on rabbits with implanted electrodes, found, that the drug causes a change in the background electrical activity, accompanied by the appearance of high-amplitude low-frequency EEG activity, as well as the deterioration of the assimilation reaction rate of light flashes, raising the threshold of the activation in the cortex and subcortical structures in response to the pain and irritation of thermal, an increase in seizure threshold hippocampus and midbrain reticular formation by direct electrical stimulation. Analysis gindarinom caused changes in EEG evidence of possible subcortical localization of its braking effect on the CNS.
On M- and H-holinoreaktivnye drug did not significantly affect. In the study of the impact on the adrenergic system gindarina noted, that eliminates the effect of the drug epinephrine on blood pressure, warns the death of mice from a lethal dose of adrenaline, lowers "group toxicity" of amphetamine. These data indicate the presence of an alkaloid from Adrainoliticaskie properties.
Stephaglabrine sulfate in experiments on various kinds of animals by subcutaneous and intraperitoneal routes of administration in small doses did not significantly affect the general condition and behavior of animals, except for a slight increase in motor activity. However, with the increase to sub-toxic doses of the drug there is a strong motor stimulation, accompanied by twitching, tremor, loss of coordination, and in more severe cases, the appearance of clonic-tonic seizures.
The main feature of the pharmacological action stephaglabrine is its ability to inhibit the activity of true and false cholinesterase and increase sensitivity of acetylcholine. For Example, in experiments with the rectus abdominis of the frog has been found, seems to be built alkaloid, since quite low concentrations, actively increases the sensitivity of muscle to acetylcholine. Besides, alkaloid has a tonic effect on the smooth muscles, where the action is removed by atropine. Stephaglabrine in acute experiments on cats in small doses increases, and in large decreases blood pressure.
Application Stephanie smooth medicine
Clinical trials have shown a significant therapeutic efficacy gindarina functional disorders of the central nervous system (neurasthenia, obsessive-compulsive disorder), residual effects of traumatic lesions and vascular diseases of the brain, Schizophrenia, epilepsy (epileptic seizures and psychosis), alcoholism. In the treatment of the vast majority of patients have expressed sedative effect of the drug. Favorable results have been obtained in the treatment of children, suffering from neurotic conditions: in 97 % We have noted a significant improvement and recovery. Gindarin mild and well tolerated. Many children after unsuccessful treatment bromides, When- ksinom, chlorpromazine and other drugs gindarin gave good results.
Unlike drugs phenothiazine series and other antipsychotics gindarin does not cause a feeling of heaviness in the head and general oppression upon awakening. Sedative effect on the CNS gindarina confirmed by studies of the electrical activity of the brain, if in reflex activity, Data hronorefleksometrii, alphabetic text and associative experiment.
Contraindications gindarina not revealed. Early treatment may slight restlessness, Eliminates reception correctors (tsiklodol and others.).
Study stephaglabrine sulfate in the clinic was performed in patients with various neurological diseases (siringomielija, amyotrophic lateral sclerosis, progressive muscular dystrophy, myasthenia, consequences of cerebral circulatory disorders, neuritis of the facial nerve, polyneuritis and others.).
Application at stephaglabrine siringomielii It was effective in 2/3 patients. Stephaglabrine administered intramuscularly, 1-2 ml 0,25 % solution 2 once a day. The course of treatment was 20-30 days. As a result, the treatment of decreased precipitation area of pain and temperature sensitivity, restore sensitivity to face with the appearance of corneal reflexes, as well as significantly reduce the symptoms of swallowing disorders at siringobulbii. The most effective treatment was in a group of patients, which stephaglabrine injected intramuscularly 2 ml 2 once a day (100-120 Ampoules). Along with stephaglabrine All patients received massage, LFK, electrophoresis of potassium iodide on the spine, vitamins B1 and in12.
Therapeutic efficacy stephaglabrine also studied in patients with progressive muscular dystrophy. The drug is administered intramuscularly 2 ml 2 twice a day in combination with LFK, massage, Vitamins. Positive results were characterized by increase of muscle strength, increasing range of motion and appearance of some reflexes, most knee. A comparative study was carried out with galantamine and neostigmine methylsulfate. In patients with severe generalized form of the disease drugs are not allowed to improve. In mild to moderate disease after injection stephaglabrine torque figures have improved by 2-6 kg, and in some patients - 10-12 kg. Similar results were also observed in the appointment of galantamine.
Stephaglabrine with positive results when used Bokova amiotrofičeskom sclerosis, traumatic plexitis, poliradikulonevritah, neuritis of the facial nerve, polyneuritis. In this group of patients the drug was administered intramuscularly in combination with physical therapy for 1 - 1,5 Months. A number of patients has been a full recovery of sensory and motor disorders. Besides, there was a marked decrease in paresis of mimic muscles in some patients with neuritis of the facial nerve.
Stephaglabrine well tolerated in children older. Compared with neostigmine methylsulfate no side effects.
Formulations, Dosage and administration of drugs Stephanie smooth
Gindarin (The horse) administered orally at a dose of 0,05-0,075 g per reception 2-3 times a day, or injected under the skin. The highest single dose 0,1 g. Children designate smaller doses. Under the skin is introduced 1-2 ml 1 % gindarina solution 2-3 times a day. The course of treatment depends on the nature of the disease and individual patient tolerability and may continue until 3 Months.
Is available in tablets and ampoules (1-2 ML 1 % solution). Keep it in a dark place with caution.
Stephaglabrine sulfate (Stephaglabrini sulfas) used intramuscular injection of 1-2 ml 0,25 % solution 2 once a day. The course of treatment is 20-30 days.
Available in ampoules 1 ml 0,25 % solution. Store in a dark place. Available on prescription.