Mexidol® [Emoxypine succinate]
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Mexidol® has antihypoxic, membrane-protective, nootropic, anticonvulsant, anxiolytic effect, increases the body's resistance to stress. The drug increases the body's resistance to the effects of major damaging factors, to oxygen-dependent pathological conditions (shock, hypoxia and ischemia, impaired cerebral circulation, intoxication with alcohol and antipsychotics (neuroleptics)).
Mexidol® improves brain metabolism and blood supply to the brain, improves microcirculation and blood rheological properties, and reduces platelet aggregation. Stabilizes the membrane structure of blood cells (erythrocytes and platelets) during hemolysis. It has a hypolipidemic effect, reduces the level of total cholesterol and LDL. Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.
The mechanism of action of Mexidol® is due to its antihypoxant, antioxidant and membrane-protective action. It inhibits lipid peroxidation, increases the activity of superoxide dismutase, increases the ratio of lipid-protein, reduces the viscosity of the membrane, increases its fluidity. Modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which enhances their ability to bind to ligands, helps to preserve the structural and functional organization of biomembrane as a picture of a new mode of amateur synthesis of the same as a picture of a new mode for a day. Mexidol® increases the dopamine content in the brain. It causes an increase in the compensatory activity of aerobic glycolysis and a decrease in the degree of inhibition of oxidative processes in the Krebs cycle under hypoxic conditions, with an increase in ATP, creatine phosphate and activation of energy-synthesizing functions of mitochondria, stabilization of cell membranes.
Mexidol® normalizes metabolic processes in ischemic myocardium, reduces the area of necrosis, restores and improves electrical activity and myocardial contractility, and also increases coronary blood flow in the ischemic area, reduces the effects of reperfusion syndrome in acute coronary insufficiency. Increases the antianginal activity of nitropreparatov.
Mexidol® contributes to the preservation of retinal ganglion cells and optic nerve fibers with progressive neuropathy, the causes of which are chronic ischemia and hypoxia. It improves the functional activity of the retina and optic nerve, increasing visual acuity.
With the introduction of Mexidol® in doses of 400-500 mg Cmax in plasma is 3.5-4.0 mcg / ml and is achieved within 0.45-0.5 h.
After i / m administration, the drug is determined in the blood plasma for 4 hours. The average retention time of the drug in the body is 0.7-1.3 h.
Excreted from the body with urine mainly in glucurono-conjugated form and in small quantities in unchanged form.
- acute disorders of cerebral circulation;
- traumatic brain injury, the consequences of traumatic brain injury;
- vegetative dystonia syndrome;
- mild cognitive impairment of atherosclerotic genesis;
- anxiety disorders in neurotic and neurosis-like conditions;
- acute myocardial infarction (from the first day) as part of complex therapy;
- primary open-angle glaucoma of various stages, as part of complex therapy;
- relief of withdrawal syndrome in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders;
- acute intoxication with antipsychotics;
- acute purulent-inflammatory processes of the abdominal cavity (acute necrotic pancreatitis, peritonitis) as part of complex therapy.
Mexidol is marketed under different brands and generic names, and comes in different dosage forms:
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Dosage and Administration
In the treatment of acute myocardial infarction Medixol® administered IV or IM within 14 days on the background of traditional therapy, including nitrates, beta-blockers, ACE inhibitors, thrombolytics, anticoagulants and antiplatelet agents, as well as symptomatic means for indications.
In the first 5 days to achieve maximum effect, it is desirable to introduce the drug IV the next 9 days - the drug can be administered IM.
IV the introduction of the drug is carried out by drip infusion, slowly (in order to avoid side effects), on a physiological solution or 5% dextrose solution (glucose) in a volume of 100-150 ml for 30-90 minutes. If necessary, a slow jet injection of the drug for at least 5 minutes is possible.
Drug administration (intravenously or intramuscularly) is carried out 3 times / day, every 8 hours. The daily therapeutic dose is 6–9 mg / kg body weight, a single dose - 2-3 mg / kg body weight. The maximum daily dose should not exceed 800 mg, single - 250 mg.
In acute disorders of cerebral circulation (ischemic stroke) Medixol® used as part of complex therapy in the first 2-4 days intravenous drip, 200-300 mg 2-3 times / day, then intramuscular dose, 100 mg 3 times / day. The duration of treatment is 10-14 days. In the future, the drug is administered orally in the form of capsules 100 mg 2 times / day for 14 days and 100 mg 3 times / day for the next 7 days. The frequency and duration of repeated courses of therapy is determined by the doctor.
When dyscirculatory encephalopathy in the phase of decompensation Medixol® should be applied IV the jet or drip at a dose of 100 mg 2-3 times / day for 14 days. Then the drug is administered intramuscularly at 100 mg / day for the next 2 weeks. In the future, the drug is prescribed in the form of capsules 100 mg 2-4 times / day, the frequency and duration of courses of therapy determined by the doctor.
For course prophylaxis of dyscirculatory encephalopathy Medixol® administered intramuscularly in a dose of 100 mg 2 times / day for 10-14 days.
For the treatment of mild and moderate cognitive disorders Medixol® appoint a / m dose of 100-300 mg / day for 14 days. If necessary, in the future, the drug is used in an encapsulated form of 100 mg 2-4 times / day (as recommended by the doctor) without limiting the course of treatment for the duration.
With the / in the introduction, especially the jet, it is possible:
From the digestive system: dry and metallic taste in the mouth.
On the part of the respiratory system: sore throat, chest discomfort and lack of air.
Other: sensation of "overflowing" heat throughout the body.
As a rule, these phenomena are due to the high rate of drug administration and are transient in nature.
On the background of long-term administration of the drug, the following side effects may occur:
From the digestive system: nausea, flatulence.
From the side of the central nervous system: sleep disturbances (drowsiness or sleep disturbance).
- acute abnormal liver function;
- acute renal impairment;
- children and adolescents under 18 years of age (efficacy and safety have not been established);
- lactation period (breastfeeding);
- hypersensitivity to the drug.
Medixol® potentiates the effect of nitrates.
Pregnancy and Lactation
Use of the drug during pregnancy and lactation is contraindicated.
In acute myocardial infarction, acute (ischemic stroke) and chronic (circulatory encephalopathy) cerebral circulation disorders after completion of parenteral administration of the drug, to maintain the achieved therapeutic effect, it is recommended to continue the use of the drug Medixol® in the dosage form of a capsule (100 mg 3 times / day). The duration of therapy is determined by the doctor.
Symptoms: sleep disturbance (insomnia), in some cases drowsiness; with a / in the introduction in rare cases, a slight and short-term (up to 1.5-2 h) increase in blood pressure.
Treatment: the development of symptoms of overdose, as a rule, does not require the use of kupirayuschih funds, these symptoms of sleep disturbance disappear independently within a day. In severe cases, it is recommended to use one of the sleeping pills and anxiolytics for oral administration (nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg). With an excessive increase in blood pressure, antihypertensive drugs are used.
- Brand name: Mexidol
- Active ingredient: Emoxypine succinate
- Country of Origin: Russia
- Bioenergetic mechanisms of the antihypoxic effect of mexidol, a succinate-containing derivative of 3-hydroxypyridine
- Effect of mexidol on the content of transmitter monoamines and amino acids in rat brain structures
- Antioxidant and hypolipidemic properties of mexidol and emoxypine during prolonged immobilization stress
- Antihypoxic and Antinecrotic Effect of Mexidol in Skin Ischemia
- Lymphotropic Effect of Mexidol in Reactive Fever
- Effect of mexidol and nitroglycerine on iron-sulfur centers, cytochrome P-450, and nitric oxide formation in liver tissue of experimental animals
- Lymphotropic effect of dimephosphon, mexidol, and ketorolac is realized via activation of the lymphangion and stimulation of lymph formation
- Histo- and Cytoarchitectonics of the Hippocampus in Young Rats Injected with Propofol and Mexidol
- Evaluation of Effects of Histochrome and Mexidol on Structural and Functional Characteristics of the Brain in Senescence-Accelerated OXYS Rats by Magnetic Resonance Imaging
- The effects of Mexidol on the acquisition of food-related conditioned reflexes and synaptic ultrastructure in field Ca1 of the rat hippocampus after single acoustic stimuli with ultrasonic components
- Antioxidants L-tocopherol, emoxypine, and mexidol modify the effect of antidepressants in mice
- Voltammetric Determination of Mexidol
- Synergism of sulfur-containing phenol (SO-4) with mexidol, α-tocopherol, and phospholipids
- The Action of Mexidol on the State of Conditioned Reflex Activity after Traumatic Brain Lesions
- Postresuscitation Recovery of Functional Activity of Central Nervous System in Rats during Combination Treatment with Mexidol and Neuropeptides Delta Sleep-Inducing Peptide and Oxytocin
- Identification and quantitative determination of specific impurity in mexidol and emoxypine by high-performance liquid chromatography
- Features of the antihypoxic action of mexidol associated with its specific effect on energy metabolism
- P.3.001 Discriminative stimulus effects of mexidol in rats
- P.3.022 Antistressory effect of mexidol in inbredC57BL/6 and BALB/C mice
- P.5.007 Perspectives of the use of a new antioxidant mexidol in the treatment of Parkinson's disease
- P.5.016 Stress-protective effect of mexidol on different levels of natural altitudes
- P.5.042 Enhancement of the activity of antiepileptic drugs in combination with mexidol
- P.5.084 Pharmacokinetics and biotransformation of mexidol in C57BL/6 and BALB/C inbred mice
- P.1.015 Cerebrovascular effects of mexidol in conditions of separate and combined vascular pathology of brain and heart