Dimethofosfon 15% Solution for Oral Administration 100 ml

Indications

Orally, as part of combination therapy:
Acute and chronic cerebrovascular disorders, consequences of ischemic and hemorrhagic strokes, cranial and neurosurgical injuries, planned neurosurgical operations, vegetative-vascular dystonia of the parasympathetic type, migraine, Meniere's disease, osteochondrosis, multiple sclerosis, acidosis, chronic nonspecific lung diseases with signs of respiratory and pulmonary heart failure, respiratory diseases, atopic bronchial asthma, and pollinosis.
The use of Dimethosphone® does not relieve asthma attacks and does not affect the frequency of beta-adrenergic aerosol use.
Externally:
Infectious-inflammatory-allergic skin and mucous membrane diseases: wounds, suture areas, and sites of pin exit from the Ilizarov apparatus; erysipelas; in dermatology, comprehensive treatment of skin diseases (acne, seborrheic dermatitis, rosacea); prevention of radiation mucositis.

Section: Method of Use and Doses

Dimefosfon® is taken orally after meals, with water. The duration of treatment depends on the nature of the disease and lasts from 3 days to 2 months. In combination therapy for the following diseases and conditions: For acute and chronic cerebrovascular disorders, consequences of ischemic and hemorrhagic strokes, traumatic brain injury, adults take 15 ml (1 tablespoon) 3 to 4 times a day. The duration of the course is 2 to 3 weeks, in some cases up to 6 weeks. For planned neurosurgical operations, 15 ml (1 tablespoon) for 5 days before and 2 months after the operation. For vegetative-vascular dystonia of the parasympathetic type, adults take 15 ml (1 tablespoon) 3 times a day for 2 to 3 weeks, children over 12 years take 50 mg/kg (10 to 15 ml) 3 times a day for 3 weeks. For migraines, 15 ml (1 tablespoon) 3 times a day for 2 to 3 weeks. For Meniere's disease, 15 ml (1 tablespoon) 3 times a day for 3 weeks. For osteochondrosis, adults take 10 ml (1 dessert spoon) 3 to 4 times a day for 2 to 3 weeks, improvement is observed on the 8th to 10th day of treatment. For multiple sclerosis, adults take 100 mg/kg (45 ml) daily, 15 ml (1 tablespoon) 3 times a day for 10 days during the autumn-spring period monthly. For chronic nonspecific lung diseases with signs of respiratory and pulmonary heart failure, adults take 15 ml (1 tablespoon) 3 to 4 times a day. The course is 7 to 10 days. For respiratory diseases, acidosis, atopic bronchial asthma, and pollinosis, adults are prescribed 15 to 25 ml, children are prescribed at a dose of 75 to 100 mg/kg: children under 3 years take 5 ml (1 teaspoon), 3 to 8 years 10 ml (1 dessert spoon), over 8 years 15 ml (1 tablespoon) 3 times a day, in severe cases 4 times a day for 4 to 5 weeks. For atopic bronchial asthma combined with pollinosis, it is prescribed 2 to 3 weeks before the onset of exacerbations and taken throughout the flowering period. The use of Dimefosfon® does not relieve asthma attacks and does not affect the frequency of using beta-adrenergic aerosol medications. A measuring cup included in the package (if available) can be used for dosing.

For external use: In case of infectious-inflammatory-allergic skin and mucous membrane diseases, apply as dressings, turundas, and compresses with the solution daily for 3 to 14 days. On the area of sutures and points of exit of the Ilizarov apparatus pins, daily apply gauze napkins soaked in Dimefosfon® for 7 to 14 days. In case of erysipelas, lubricate the inflamed area 3 times a day for 3 to 5 days. In the complex treatment of skin diseases (acne, seborrheic dermatitis, rosacea), wipe the skin 3 to 4 times a day, in the evening apply compresses. To prevent radiation mucositis, gauze napkins soaked in Dimefosfon® are placed in the projection of the radiation beams 20 minutes before exposure to the dose.

Section: Composition

1 L of solution contains:
Active ingredient: dimethyloxobutylphosphonildimethylate (dimefosfon®) 150 g.
Excipients: purified water.

Description of the dosage form

Colorless or yellowish, transparent or opalescent liquid with a distinctive odor.

• Hypersensitivity to the components of the drug;

• Pregnancy and breastfeeding;

• Epilepsy.

• Chronic renal failure of stages 2 and 3 (creatinine clearance less than 40 ml/min).
The drug is contraindicated in children and adolescents under 18 years of age (due to insufficient clinical data on its use in this category of patients) acute and chronic cerebrovascular disorders, consequences of ischemic and hemorrhagic strokes, traumatic brain injuries and neurosurgical injuries, planned neurosurgical operations, migraine, Meniere's disease, osteochondrosis, multiple sclerosis, chronic nonspecific lung diseases with signs of respiratory and pulmonary heart failure.
The drug is contraindicated in children under 12 years of age (due to insufficient clinical data on its use in this category of patients) in vegetative-vascular dystonia of the parasympathetic type.
With caution
Dimethyldiphosphonate® is well tolerated by patients. When applied to mucous membranes, it may cause irritation; in this case, it is necessary to dilute the Dimethyldiphosphonate® solution by half.

Special instructions

Has a bitter taste. It is recommended for children to take it with milk, fruit juice, or sweet tea.

Section: Side Effects

According to the World Health Organization (WHO), side effects are classified according to their frequency of occurrence as follows: very common (> 1/10); common (from > 1/100 to 1/1000 to 1/10000 to < 1/1000); very rare (< 1/10000); frequency unknown - it was not possible to establish the frequency of occurrence based on available data. Nervous system disorders: frequency unknown drowsiness and decreased concentration (these symptoms usually resolve by the 3rd or 4th day of taking the medication). Gastrointestinal disorders: frequency unknown dyspepsia. If any of the side effects listed in the instructions worsen, or if you notice any other side effects not mentioned in the instructions, inform your doctor.Section: OverdoseWhen the drug is used in doses exceeding the recommended amounts, it is possible to enhance the severity of dose-dependent side effects. Treatment: gastric lavage, activated charcoal, symptomatic therapy.InteractionDuring the period of release of Dimethofone®, no interactions with other drugs have been identified.

Pharmacodynamics

Dimethosfon® exhibits anti-acidotic, membrane-stabilizing, anti-inflammatory, and antioxidant properties, normalizes blood flow and tissue metabolism in the brain, reduces heart and lung failure, and improves circulation regulation, including cerebral circulation.
The anti-acidotic effect is realized through the intensification of renal and pulmonary mechanisms of acid-base regulation, enhancement of intra-organ blood flow and tissue metabolism; Dimethosfon® also reduces the content of lactic and pyruvic acids in the tissues of the brain.
Dimethosfon® stabilizes cell membranes, restoring the reactivity of cerebral vessels, improving the functions of the cerebral hemispheres and the brainstem, reduces the depth of consciousness disturbances, restores the sleep-wake cycle, and reflexes, the arcs of which close through the brainstem sections, and decreases the severity of 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 the tissues of the brain.
Dimethosfon® enhances energy processes in the brain both directly, by acting on the mitochondria, and indirectly, by stimulating the pituitary-thyroid system, increasing the consumption of thyroid hormones by tissues, which is accompanied by the activation of energy and catabolic processes in the mitochondria of cells. It exhibits properties of certain neurotransmitters (GABA-positive, N-cholinergic, and dopaminergic activity).
Dimethosfon® reduces heart and lung failure by restoring the resistance of peripheral vessels (arterial and venous).
Dimethosfon® improves the regulation of cerebral blood circulation without having a pronounced vasodilating effect; however, it positively influences the metabolism of brain tissues during ischemia and improves venous outflow. The effectiveness of the clinical application 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 thereby improve microcirculation.
When applied locally, Dimethosfon® has anti-inflammatory and antiseptic effects, enhancing the protective functions of the skin and mucous membranes.

Pharmacokinetics

Dimethylphosphonate® is sufficiently absorbed after a single dose, easily penetrates histohematological barriers, and is distributed across various organs and tissues. The maximum concentration (Cmax) in the blood is observed within the first hour after administration of the drug; three hours after administration, maximum concentrations are determined in the brain, heart, and spleen. Three days after a single administration of Dimethylphosphonate®, only trace concentrations remain in the body.
Dimethylphosphonate® is excreted unchanged primarily in the urine, accounting for 11-15% of the drug (up to 70% of the excreted amount is eliminated within the first 12 hours). No more than 0.5% is excreted in feces.