Dimephosphone, 1 piece, 100 ml, 15%, solution for oral and external use
Inside
, after meals, with water.
The course of treatment depends on the nature of the disease and lasts from 3 days to 2 months.
In complex therapy of the following diseases and conditions:
For acute and chronic cerebrovascular accidents, consequences of ischemic and hemorrhagic strokes, traumatic brain injury
- adults 15 ml (1 tablespoon) 3-4 times a day. The duration of the course is 2–3 weeks, in some cases up to 6 weeks.
During planned neurosurgical operations
- 15 ml (1 tablespoon) for 5 days before and 2 months after surgery.
For osteochondrosis
— adults, 10 ml (1 tablespoon) 3–4 times a day for 2–3 weeks, improvement is observed on the 8–10th day of treatment.
For multiple sclerosis
- adults 100 mg/kg (45 ml) per day (15 ml (1 tablespoon) 3 times a day) for 10 days in the autumn-spring period monthly.
For chronic nonspecific lung diseases with signs of respiratory and pulmonary-heart failure
- adults 15 ml (1 tablespoon) 3-4 times a day. Course - 7–10 days. The use of Dimephosphone® does not relieve asthma attacks and does not affect the frequency of use of beta-agonist aerosols.
For vegetative-vascular dystonia of the parasympathetic type
— adults 15 ml (1 tablespoon) 3 times a day for 2–3 weeks, children over 12 years old — 50 mg/kg (10–15 ml) 3 times a day for 3 weeks.
For chronic cerebrovascular insufficiency due to atherosclerosis and hypertension
— 15 ml (1 tablespoon) 3 times a day for 2–3 weeks.
For migraine
— 15 ml (1 tablespoon) 3 times a day for 2–3 weeks.
For Meniere's disease
- 15 ml (1 tablespoon) 3 times a day for 3 weeks.
For respiratory diseases, acidosis, atopic bronchial asthma and hay fever
- adults are prescribed 15-25 ml, children are prescribed at a dose of 75-100 mg/kg: up to 3 years - 5 ml (1 teaspoon), 3-8 years - 10 ml (1 teaspoon), over 8 years - 15 ml (1 tablespoon) 3 times a day, in severe cases - 4 times a day for 4-5 weeks. For atopic bronchial asthma in combination with hay fever, it is prescribed 2-3 weeks before the onset of deterioration and taken throughout the entire flowering period.
Externally.
For infectious-inflammatory-allergic diseases of the skin and mucous membranes
- in the form of bandages, turundas and lotions with a solution daily for 3–14 days.
For complex treatment of acne
wipe the skin 3-4 times a day, apply lotions in the evening.
For erysipelas
lubricate the inflammation area 3 times a day for 3–5 days.
To the area of sutures and exit points of Ilizarov wires
Apply gauze pads soaked with Dimephosphone® daily for 7–14 days.
For the prevention of radiation mucositis
gauze wipes moistened with Dimephosphon® are placed in the projection of the radiation beams 20 minutes before dose exposure.
Dimephosphone concentrate for the preparation of intravenous solution 1g amp N 5
Dimephosphone concentrate d/pig solution iv 1g amp N 5
Dosage form
concentrate for the preparation of solution for intravenous administration.
Description
Colorless or yellowish transparent liquid with a peculiar odor.
Compound:
1 ampoule contains:
Active ingredient: dimethyloxobutylphosphonyl dimethylate (Dimephosphon®) – 1.0 g.
Pharmacological properties
Pharmacodynamics
Dimephosphone exhibits anti-acidotic, membrane-stabilizing, anti-inflammatory and antioxidant properties, normalizes blood flow and metabolism of brain tissue, reduces heart and pulmonary failure, improves the regulation of blood circulation, including cerebral circulation.
The anti-acidotic effect is realized due to the intensification of the renal and pulmonary mechanisms of regulation of the acid-base state, increased intraorgan blood flow and tissue metabolism, and dimephosphone also reduces the content of lactic and pyruvic acids in brain tissue.
Dimephosphone stabilizes cell membranes, restoring the reactivity of cerebral vessels, improving the functions of the cerebral hemispheres and the brain stem, reduces the depth of disturbances of consciousness, restores the sleep-wake cycle, reflexes, the arcs of which close through the brainstem, reduces the severity of the pyramidal, cerebellar, vestibular, visual and auditory disorders.
The antioxidant effect is achieved by preventing the activation of lipid peroxidation and increasing the activity of antioxidant enzymes in brain tissue.
Dimephosphone enhances energy processes in the brain both directly, acting directly on mitochondria, and indirectly, stimulating the pituitary-thyroid system, increasing tissue consumption of thyroid hormones, which is accompanied by activation of energy and catabolic processes in cell mitochondria. Shows the properties of some neurotransmitters (GABA-positive, N-cholinergic and dopaminergic activity).
Dimephosphone reduces heart and pulmonary failure by restoring the resistance of peripheral vessels (arterial and venous).
Dimephosphone improves the regulation of cerebral circulation without having a pronounced vasodilator effect, but has a positive effect on the metabolism of brain tissue during ischemia and improves venous outflow. The effectiveness of the clinical use of the drug in various forms of cerebrovascular insufficiency is associated with its ability to increase the resistance of nerve cells to ischemia, reduce edema and, therefore, improve microcirculation.
Pharmacokinetics
Easily passes through histohematic barriers and is distributed to various organs and tissues. The highest concentrations are created in the brain, heart and spleen. Three days after a single administration of dimephosphone, only trace concentrations remain in the body.
Dimephosphone is excreted unchanged mainly in the urine in an amount of 11-15% of the drug (up to 70% of the excreted amount of the drug is excreted during the first 12 hours).
Indications for use
As part of complex therapy:
Chronic cerebrovascular accidents, in the intermediate and long-term period of traumatic brain and neurosurgical injuries, consequences of ischemic and hemorrhagic strokes, Meniere's disease.
Contraindications
Epilepsy, chronic renal failure grade 2 - 3 (creatinine clearance less than 40 ml/min), individual intolerance, children under 18 years of age.
Directions for use and doses
In complex therapy:
Chronic cerebrovascular accidents, in the intermediate and long-term period of traumatic brain and neurosurgical injuries:
intravenous injection - 1 g (1 ampoule) of the drug, diluted in 10 - 20 ml of sterile water for injection or 0.9% sodium chloride solution 1 - 4 times a day for 10 - 14 days;
or intravenous drip - 1 g (1 ampoule) of the drug, diluted in 200 - 400 ml of sterile water for injection or 0.9% sodium chloride solution 1 - 4 times a day for 10 - 14 days.
Consequences of ischemic and hemorrhagic strokes:
intravenously in a stream - 1-2 g (1-2 ampoules) of the drug, diluted in 10 - 20 ml of sterile water for injection or 0.9% sodium chloride solution 1 - 4 times a day for 10 - 15 days;
or intravenous drip - 1-2 g (1-2 ampoules) of the drug, diluted in 200 - 400 ml of sterile water for injection or 0.9% sodium chloride solution 1 - 4 times a day for 10 - 15 days.
Meniere's disease:
intravenously in a stream - 1 g (1 ampoule) of the drug, diluted in 10 ml of 0.9% sodium chloride solution 1 - 3 times a day for 10 days, then it is recommended to continue the course of treatment with the drug Dimephosphon®, solution for oral and external use application, in accordance with the instructions for use.
Side effect
Drowsiness and deterioration in concentration (dissipate by 3–4 days after the first administration of the drug).
Overdose
Symptoms: increased severity of side effects.
special instructions
If drowsiness occurs in the first days of taking the drug, you should refrain from driving vehicles and activities that require increased attention and a high speed of psychomotor reactions.
There have been no strictly controlled clinical studies of the safety of Dimephosphon® in children.
Interaction with other drugs
No interactions with other drugs have been identified.
Use during pregnancy and breastfeeding
Strictly controlled clinical studies of the safety of the use of Dimephosphon® during pregnancy and breastfeeding have not been conducted.
Currently, there is insufficient data on the use of Dimephosphone® concentrate for the preparation of a solution for intravenous administration during pregnancy to assess the teratogenic effect of Dimephosphone.
Taking this into account, the drug Dimephosphon® concentrate for the preparation of a solution for intravenous administration should be prescribed during pregnancy and breastfeeding only if the expected benefit from its use outweighs the potential risk to the fetus or infant.
Animal studies have not revealed any harmful effects on the embryo or its development.
Impact on the ability to drive vehicles and machinery
When using the drug, you should refrain from driving vehicles and activities that require increased attention and reaction speed.
Release form
Concentrate for the preparation of solution for intravenous administration 1.0 g.
1 g of the drug in colorless glass ampoules.
5 ampoules are placed in a blister pack.
1 or 2 strip packaging along with instructions for use are placed in a cardboard box
Storage conditions
In a place protected from light, at a temperature not exceeding 250 C.
Keep out of the reach of children.
Best before date
3 years.
Do not use after the expiration date stated on the package.
Conditions for dispensing from pharmacies
Available with prescription
Introduction
Autonomic dysfunction is a common syndrome characterized by a wide range of multisystem autonomic disorders, often combined with anxiety. In these cases, patient complaints of decreased memory, attention, and thought processes, which impede professional and social activities, are obligatory. In this regard, when choosing a drug for the treatment of anxiety-associated autonomic dysfunction, it is necessary to take into account, in particular, its effect on cognitive functions.
Many of the psychotropic drugs used to treat anxiety relieve vegetative symptoms well, but can aggravate cognitive impairment, which reduces the patient’s satisfaction with the treatment effect, increasing his maladjustment. In this regard, it is important to use drugs that do not have anticholinergic and muscle relaxant effects. These requirements are met by the drug mebicar, a synthetic compound (a derivative of bicyclic biureas) with tranquilizing ability [1]. Mebicar reduces feelings of anxiety, restlessness, reduces irritability, and has a mild sedative effect. The targets for the action of mebikar are the structures included in the limbic-reticular complex and the emotional zones of the hypothalamus. The wide range of pharmacological effects of mebicar is explained by its integrative effect on the serotonin, adrenergic, cholinergic and GABAergic systems. Along with the main stress-protective and anxiolytic effect, the drug has a pronounced nootropic effect: improves memory, mental functions, increases logic, coherence and speed of thinking, improves attention and mental performance, helps normalize mental functions in general under conditions of stress and overload. Mebicar does not have a muscle relaxant effect and does not impair coordination, which significantly distinguishes it from benzodiazepine tranquilizers [1-5]. Mebicar improves the quality of sleep, facilitating the process of falling asleep, normalizes sleep structure and reduces the frequency of anxious dreams, without having a direct hypnotic effect and without causing daytime drowsiness, which allowed the drug to be classified as a “daytime” tranquilizer. In combination with other psychotropic and hypnotic drugs, Mebicar enhances the hypnotic effect. Additional effects of mebicar are its modulating effect on lipid metabolism, due to the ability to change the ratio of high and low density lipoproteins, which helps reduce the concentration of cholesterol in the blood [6], as well as the ability to improve myocardial trophism by increasing coronary blood flow, reducing blood viscosity and intravascular aggregation erythrocytes [7, 8]. Mebicar does not cause euphoria or addiction. All this justifies the possibility of its use in various fields of medicine, including neurology.
The purpose of the study was to study the effectiveness of Mebikar in patients with autonomic dysfunction combined with anxiety disorder.
Hypothesis: Mebicar, while effectively eliminating symptoms of mild to moderate anxiety and autonomic disorders in patients with autonomic dysfunction, should not have a negative effect on cognitive function.
This page contains only the text of the article. The full article with pictures and tables is here. Adobe Reader is required to view.A.A. Wiesel, MD, Chief Expert Pulmonologist of the Republic of Tatarstan DIMEPHOSPHONE Application in pulmonology Dimephosphone is an original domestic drug obtained through a targeted search in a series of non-anticholinesterase organophosphorus compounds. The drug was developed in Kazan. The novelty and originality of this medicine are confirmed by patents from Russia, Great Britain, Germany, Switzerland, Japan and Hungary. Dimephosphone is the dimethyl ester of 1,1-dimethyl-3-oxobutylphosphonic acid.
The dosage form of Dimephos-fon is a 15% aqueous solution for oral and external use. It is a colorless, transparent liquid with a peculiar odor and bitter taste. Over more than thirty years of research on Dimephosphone in many research and clinical institutions in Russia, and primarily by Kazan scientists - employees of KSMU, anti-acidotic, vasoactive, membrane stabilizing, neuroprotective, cardio- and neurotropic, antiplatelet, antiallergic, immunocorrosive properties were discovered. -rigging, antihypoxic, antioxidant, bacteriostatic, wound-healing and radioprotective properties of the drug. Dimephosphone is widely used in neurosurgery and neurology (Danilov V.I., Polyclinic No. 2, 2008). Acid-base imbalance (ABS) is an important drug that is administered intravenously in a hospital setting and requires constant monitoring of ABS parameters to avoid a shift towards alkalosis. They do not eliminate intracellular pH shifts and do not affect the metabolic processes in tissues that caused acidosis (Studentsova I.A. et al., 1989). The effect of Dimephosphone is achieved through intervention in metabolic processes: it normalizes carbohydrate metabolism in the Krebs cycle and intensifies the breakdown of glucose through the pentose cycle (Zaikonnikova I.V. et al., 1977), intensifies the renal and pulmonary mechanism of regulation of AOS, enhances intraorgan blood flow and tissue metabolism (I.A. Studentsova et al. 1987). The advantage of Dimephos-fon is the rapid manifestation of the anti-acidotic effect, and the possibility of long-term use of the drug outside the hospital without fear of causing alkalosis.
Including it in the complex therapy of various diseases alleviates the course of the disease and speeds up recovery. Dimephosphone is effective in the complex treatment of acute and chronic respiratory diseases with subcompensated pulmonary hypertension, and in bronchospastic variants of bronchial obstruction (chronic bronchitis, bronchial asthma, pulmonary tuberculosis). The use of Dime-phosphon in phthisiopulmonology is due to the fact that it normalizes blood CBS, improves liver metabolism, optimizes central and regional blood flow, and is a mild immunomodulator, which was shown by research by employees of the department of phthisiopulmonology of KSMU (Kazan) for more than ten years, as well as numerous experimental and clinical studies of Kazan scientists and scientists from Moscow, St. Petersburg, Tashkent, Saransk and other cities. It combines well with traditional bronchodilators and, unlike other vasodilators, reduces the level of hypoxemia. A comparative assessment of the effect of bronchodilators on the oxygen composition and acid-base state (ABS) of blood in patients with obstructive respiratory failure was carried out at the Central Institute for Advanced Training of Physicians (Moscow). At the same time, with the help of radioactive xenon, a clear connection was established between the shift in the state of ventilation/blood flow in certain areas of the lungs and changes in the oxygen composition of the blood. When treating patients with an increased pO value with Dime-phosphone, there was a selective 2
significant movement of blood flow into hyperventilated areas of the lungs, and in patients with reduced pO observed - 2
There was a movement of blood flow to hypo-ventilated areas of the lungs, i.e. increase in parenchymal shunting. (Zamotaev I.P. et al., 1981). The drug has a clear oxygenating effect, normalizes blood pH, so Dimephosphon is advisable to use in a pulmonology clinic in the presence of hypercapnia and a decrease in blood oxygen saturation (Alekseeva N.V., 1982). Dimephosphone suppresses high kininogenase activity in the blood in the acute period of acute respiratory viral infections with broncho-obstructive syndrome (BOS). Infant children with ARVI and BOS, along with conventional therapy, received dimephosphone in the form of a 15% solution orally at the rate of 100 mg/kg per day for 5 days (the reference drug Kontrikal daily, intravenously, by drip for the first 3 –5 days of illness). It has been established that Dimephos-fon has the ability to increase anti-kallikrein activity and reduce the level of blood kallikrein after 2 days of treatment with the drug. After completing the five-day course of treatment, the indicators of kininogenesis activity returned to normal. Iieeeeeeeea .5 2008 tel./fax editorial office: (495) 6727029\92, 3684703
IoeuiiiieiaeyThe advantage of Dimephos-fon is oral administration and the absence of adverse reactions. The use of Dimephosphone led to a significant reduction in the duration of signs of respiratory failure, shortness of breath, and physical changes in the respiratory system compared to the control group of patients who received only conventional therapy, and led to a decrease in the length of stay of patients in the hospital for 2 bed days. The positive therapeutic effect of Dimephosphone is also associated with a decrease in the increased level of blood histamine recorded in the acute period of the disease, which is explained by the membrane-stabilizing properties of Dimephosphone. As a result of the study, Dimephosphone was recommended for inclusion in the complex therapy of patients with ARVI with BOS (Anokhin V.A., 1985). The effect of using Dimephosphone (at a dose of 100 mg/kg 4 times a day for 10 days) in patients with chronic nonspecific lung diseases was assessed. All patients had symptoms of respiratory failure of varying degrees of severity, metabolic and respiratory acidosis of varying degrees of compensation. In all patients, rheograms of the brain, lungs, liver and polycardiogram were recorded before the start of treatment or control observation and, respectively, 5 and 10 days after. In patients receiving Dimephosphone, there was a positive dynamics of volumetric blood flow in the brain, lungs, and liver, normalization of venous tone with a decrease in arterial inflow resistance compared to the control group of patients who did not receive it. Dimephos-fon had a normalizing effect on the contractility of the left ventricular myocardium, improved the general condition of patients, which was manifested by a decrease in shortness of breath,
Iieeeeeeeea .5 2008 tel./fax editorial office: (495) 6727029\92, 3684703
increasing tolerance to physical activity, reducing cyanosis of the lips. In the control group of patients, no such changes occurred by the tenth day of traditional therapy. Clinical improvement in general condition is associated with a decrease in hypercapnia, confirmed by CBS studies, as well as an improvement in diffusion and aeration conditions due to an increase in the intensity of pulmonary blood flow. The data obtained allow us to consider it appropriate to include Dimephosphone in the course of treatment of patients with chronic nonspecific lung diseases (Pankova V.P., 1978). A comparative clinical analysis of the results of treatment of acute purulent destructive pneumonia (APDP), mainly with the pulmonary-pleural form of the disease, was carried out in 46 children aged 8 months to 3 years; half of the patients, in addition to conventional therapy, received Dimephosphone and Essentiale. In children of the second group, relief of the main manifestations of the disease (respiratory failure, symptoms of intoxication, weakness), restoration of the composition and stability of cell membranes, the composition of lung surfactants, as well as normalization of pulmonary ventilation, occurred within the time period was one and a half times shorter than in children who received only conventional therapy. These results are associated with the presence of Dimephosphone's oxygenating effect, as well as antiphospholipase activity, so it is advisable to include Dimephosphone in the complex therapy of OGDP in children (Weinberg M.M., 1987). A similar effect of Dimephosphone was observed in young children in the treatment of acute destructive pneumonia and it was noted that Dimephosphone promotes the activation of reparative processes in damaged lung tissue (Ismailova M.A. et al., 1989). ... The advantage of Dimephosphone is oral administration and the absence of adverse reactions. The use of Dimephosphone led to a significant reduction in the duration of signs of respiratory failure, shortness of breath, and physical changes in the respiratory system compared to the control group of patients who received only conventional therapy, and led to a decrease in the length of stay of patients in a hospital for 2 bed days... Studying the effectiveness of Dimephosphone in the complex therapy of chronic pneumonia and recurrent bronchitis in children (in the form of a 15% solution, at a rate of 30 mg/kg, 3 times a day, for 10 days), showed that the drug increases the number of T- and B-lymphocytes in the peripheral blood, reduces the degree of disimmunoglobulinemia, improves the well-being of patients, there is a pronounced positive dynamics of percussion and auscultation data, and reduces the “bed-day” stay of patients in hospital. In some cases, the use of Dimephosphone allows one to exclude antibacterial drugs from therapy. The author recommends the inclusion of Dimephosphon as an immunocorrector in the complex therapy of chronic pneumonia and recurrent bronchitis in the acute stage (Osintsev A.N., 1986). Dimephosphone was used in the complex therapy of pneumonia in newborns, which was accompanied by shifts in the gas composition of the blood and disturbances in the functional state of all organs and systems. Under observation were 50 children aged from 5 to 28 days, with small focal and confluent pneumonia. In 20 newborns, the disease was severe with manifestations of respiratory failure and symptoms of severe intoxication. Dimephosphone was prescribed in the acute period of pneumonia in the form of a 15% solution at the rate of 50 mg/kg body weight per day for 4–9 days (1 teaspoon 3 times a day before feeding the child). In children receiving Dimephosphone, there was a more rapid disappearance of symptoms of respiratory failure, intoxication and physical changes in the lungs. Normalization of CBS indicators occurred in most children already on days 2–3 after taking the drug, whereas in control
In the role group receiving traditional treatment, these indicators were restored only on days 4–6. Dimephosphone had a positive effect on myocardial function. This was expressed in a decrease in the number of children in whom pathological changes were recorded on the ECG, and during treatment it amounted to 53% of newborns treated with Dimephosphone, and 80% in the control group. A positive therapeutic effect of Dimephosphone on peripheral blood circulation parameters was also revealed, clearly manifested in the regulation of vascular tone and blood rheological parameters. All this, apparently, contributes to the healing process. Considering the high therapeutic activity of Dimephosphone, the authors recommend its use in the complex treatment of pneumonia in newborns (Pikuza O.I. et al., 1989). The effect of Dimephosphon on the immunological status and seasonal imbalance of lipids and lipid peroxides in children with bronchial asthma was studied. The use of Dimephosphone contributed to the normalization of the number of complete and incomplete rosettes, a decrease in the percentage of O-ROK, an increase in the number of low-affinity T cells, a decrease in the level of T suppressors and an increase in T helper cells. A positive effect of Dimephosphone on lipid metabolism and lipid peroxidation was noted. The authors believe that Dimephosphon, having a pronounced immuno-corrective effect, can be the drug of choice, because its effects are superior to those of levamisole, and no side effects from the use of Dimephosphone were observed (Gordeev V.V., 1988). It was also found that against the background of traditional therapy for bronchial asthma (aminophylline, intal, as-tmopent or novodrine), the administration of Dimephosphone in the form of a 15% solution for 1–2 weeks (50 mg/kg body weight 3 times a day ) significantly increased vital capacity (VC) by 14.5% and decreased leukocytosis. A bicycle ergometer test after a course of Dimephosphone led to a predominance of the volume response over the pressor response. The results obtained made it possible to positively evaluate the inclusion of Dimephosphone in the complex therapy of bronchial asthma (Vizel A.A., 1991). Dimephosphone is recommended for clinical use in pneumonia, acute respiratory diseases, influenza and other infections, chronic nonspecific lung diseases, tuberculosis, as well as in other pathological processes accompanied by acidosis: diabetes mellitus, rickets-like diseases, postoperative period.