Mexidol sparkled my intrest a bit altough it doesnt seem to show the same nootropic potential as some of the other russian things, here's a list of the most interesting abstracts regarding this compound, i'm alot more interested in semax, cerebrolysin and cortexin tough, still this one is worth discussing.
[Antihypoxic and antiamnesic effects of mexidol and semax]
Upon single administration, mexidol and semax only in doses of 100 and 0.05 mg/kg, respectively, produced an antihypoxic effect on mice in the altitude chamber and hermetic chamber tests. Preventive course administration of mexidol and semax for 6 days gave significant antihypoxic effect on the model of acute hypobaric hypoxia in mice in doses of 75 and 0.1 mg/kg per day, respectively, in which the same preparations upon single administration were ineffective. Neither mexidol nor semax upon single administration were effective on the models of acute hemic and histotoxic hypoxia. On various models of amnesia (except that induced by the maximal electroshock) in mice, both mexidol and semax exhibited marked antiamnesic effects comparable with that of the reference nootrope drugs piracetam and oxyracetam. Mexidol showed a linear, while semax exhibited a bell-shaped reversible dose-effect relationships. Mexidol and semax inhibited the ortho- and antidromic population response spikes of CA1 pyramidal neurons of survival hippocampal slices in rats. It was estimated that mexidol (in contrast to semax) increased oxygen consumption in rat brain mitochondria and had a linear dose-effect relationship in a concentration range of 1-5 mM. It is concluded that mexidol should be used in high doses (for both single and course administration) for obtaining antihypoxic and antiamnesic effects, while semax requires a thoroughly controlled choice of dosage.
[Effect of semax and mexidol on brain ischemia models in rats]
It was established that semax and mexidol significantly reduced neurological deficiency and increased the survival in rats with model brain ischemia induced by the bilateral ligation of common carotid arteries. Mexidol exhibited a linear dose-effect relationship (in a range of doses from 30 to 120 mg/kg per day), while the effect of semax decreased with increasing dose (in a dose range from 0.3 to 1.2 mg/kg per day). Preventive course administration of semax and mexidol considerably reduced neurologic deficiency and amnesia in a step-down passive avoidance situation in rats with model brain ischemia caused by gravitation overload.
[Metabolic effects of mexidol in complex treatment of chronic brain ischemia]
Patients with a chronic brain ischemia of stages I-II on the background of hypertension and/or cerebral atherosclerosis are characterized by energy insufficiency of the metabolism, as estimated by the activity of succinate dehydrogenase in peripheral blood lymphocytes. Within the framework of randomized comparative investigation of the efficiency of actovegin and mexidol in the complex therapy of a chronic brain ischemia, positive dynamics in reduction of the clinical semiology, restoration of cognitive processes in the brain, and reduction of the expression of subjective manifestations of the disease is established. On this background, the administration of mexidol led to restoration of the energy exchange due to substrate effects of the Krebs cycle intermediates present in its structure.
[Mexidol effects in extreme conditions (experiments with animals)]
In extreme conditions like a new situation, bright light, open space, immobilization, height (the open field and lifted cruciform labyrinth test) and a conflict between an unavoidable action and fear of painful mexidol at the doses of 50 and 100 mg/kg of a body weight eliminates anxiety and fear in rats, recovers adequate reactions and the orientative-trying behavior, and lessens aggressiveness. Mexidol extends life span of mice in acute hypoxic conditions. Mexidol is highly competitive with diazepam as an anti-stress agent and excels it as an anti-hypoxic agent; in contrast to diazepam, mexidol does not cause sedation and myorelaxation. Based on these findings, mexidol can be prescribed to humans to maintain efficiency in all kinds of extreme situations.
[The experimental study of peculiarities and mechanism of neuroprotective action of mexidol in hemorrhagic stroke]
An efficacy of mexidol, a Russian drug of the new generation, used in 100 mkg during 7 days has been demonstrated in rats in the model of experimentally caused intracerebral posttraumatic hematoma (hemorrhagic stroke). The drug significantly reduced the number of neurological impairments (paresis, riding-arena movements) and increased the animal's survival rate. Mexidol improved learning and memory in rats with hemorrhagic stroke in the passive avoidance test and exerted influence on the locomotor activity in the open field test.
[The regulatory effect of mexidol on the hemoglobin level under acute stress conditions]
Experiments on a group of 39 Wistar albino male rats showed that, 2 and 5 days after a model acute stress procedure, the total amount of erythrocytes is increased. This process is accompanied by a hypochromia of red cells and by a decrease in the concentration of serum iron. Single administration of mexidol (100 mg/kg) before stress induction prevents changes in the amount of blood erythrocytes, as well as in their saturation with hemoglobin. Mexidol also prevents a decrease in the level of serum iron. The drug does not influence the hematological parameters and iron concentration in blood serum of intact animals 2 and 5 days after injection.
[Effect of mexidol on hemopoietic system in conditions of an emotional stress after exposure to ionizing radiation]
The emotional stress after an irradiation can complicate the current of radiative defeats. At an emotional stress developing in early terms after an irradiation in low doses, are reduced adaptive and compensator capabilities of hemopoietic system. The emotional stress after a lethal dose irradiation inhibits the post-radiation recovery of haemopoiesis, aggravates the course of acute radiation disease and decreases the efficiency of the radioprotector--indralin. These disorders are especially pronounced under a prolonged and intensive stress. The use of the mexidol, having anxiolytic and antistress by activity, made it possible to arrest completely disturbances in the development of adaptive reactions to stress in the blood system and to normalize its compensatory potentialities in animals under conditions of combined influence of intensive long-term emotional stress and of low-dose irradiation. In the case of lethally irraiated animals, the treatment of stressed animals with mexidol favorably influenced the course of acute radiation disease, enhanced recovery processes in the blood system. Under these conditions, the use of mexidol completely removes the negative effect of emotional stress in indralin-protected animals. The pharmacological correction by mexidol from displays of an intensive emotional stress, developing after an irradiation in various doses, can be a part in system of medical measures.
[The efficacy of oxynicotinic acid a nd its derivatives in respect of functional activity of hepatocytes during acute toxic hepatopathy]
Hepatoprotective activity of oxynicotinic acid and its derivatives XC-2, XC-2, XC-4, XC-9 in destructive processes in the liver induced by CCl4 injection has been studied. It was found in that injection of oxynicotinic acid derivatives in toxic lesion of the liver decreases cytolysis, cholestasis, hepatodepressive and mesenchymal-inflammatory syndromes. Membrane-stabilizing and antioxidant effects of oxynicotinic acid derivatives increase in the following sequence: XC-1 --> XC-2, XC-3 --> XC-4, mexidol --> XC-9.
[The use of mexidol in urgent treatment of drug addiction]
Results of the clinical study of efficacy and tolerability of mexidol administered in intravenous drop-by-drop introduction during 5-7 days in the therapy of 50 cases of complicated alcoholic delirium are presented. The patient condition and changes in device test data were assessed in comparison with those of a control group of patients receiving a basic therapy without mexidol. It is shown that mexidol has stopped psychosis in shortest terms thus decreasing secondary complications and lethality.
[Antioxidants in complex treatment of Parkinson's disease]
Experimental and clinical study of mexidol efficacy in the complex therapy of Parkinson's disease has been carried out. It is shown that in a Parkinsonian animal model using oxotremorine, mexidol reduces Parkinsonian symptoms and decreases expression of neurophysiological changes caused by oxotremorine. Neurohistological study of substantia nigra neurons in a Parkinsonian model using MPTP revealed a neuroprotective effect of mexidol. An assignment of mexidol (4,0 ml intravenous in drops during 10 days) to patients with Parkinson's disease, receiving the basic therapy with antiparkinsonic drugs, reduced tremor, rigidity and bradykinesia. The most marked effect was observed in patients with prevalence of trembling symptoms at early stages of the disease. The results of clinical study have been confirmed by electromyographic and electroneuromyographic data.
[Antistressor and analgesic effects of mexidol, diazepam, paracetamol, and their combinations]
Mexidol (100 and 200 mg/kg) and diazepam (1 and 2 mg/kg) exhibit a dose-dependent antistressor effect in the pain expectation stress test in rats (conditional emotional reflex). The effect is manifested by the normalization of both motor and somatovegetative characteristics. Paracetamol in a dose of 50 and 100 mg/kg does not possess antistressor properties. Both mexidol and paracetamol increase the threshold of pain sensitivity in the test with electric stimulation of tail in rats. Diazepam does not reduce the pain threshold in this test. The combined administration of mexidol or diazepam with paracetamol does not change the antistressor effect as compared to that of each drug alone. Mexidol, but not diazepam, enhances the effect of paracetamol on the pain threshold.
[The use of mexidol in psychiatric practice]
Mexidol has been used in combination with basic therapy in 65 patients with mental disorders of organic genesis. The patients were treated during 56 days in accordance with a special scheme including the drug intake and intramuscular and intravenous injections. Mexidol exerted a positive effect on affective sphere, normalized the sleep-wake cycle, promoted rehabilitation of cognitive function thus improving the global clinical state of patients. Marked and significant improvement was found in 40,0% and 33,8% of cases, respectively. No severe side-effects were noticed.
[Estimating the potential of antioxidant therapy for patients with Parkinson's disease diagnosis]
The efficiency of using the natural antioxidant mexidol in a combined therapy of Parkinson's disease has been evaluated in a group of 65 patients including 29 females and 36 males. The drug was administered in the form of infusions (4-ml of a 5% solution per 200 - 250 ml of physiological solution) over a period of 10 days. The clinical dynamics was evaluated in terms of the universal parkinsonism disease rate scale (UPDRS) and using the data of electromyography and electroneuromyography. The 10-day treatment led to a reliable decrease in the level of postural tremor and static tremor, a decrease in the muscle tone, and an increase in the mobility and locomotor activity of patients. The maximum positive effect of mexidol was observed for patients in the initial stage of disease with tremor as predominant clinical syndrome. Neurophysiological evidence of the efficacy of mexidol therapy included a decrease in the level of volley activity manifested in the electromyograms and a decrease in the velocity of conduction over peripheral motor nerve fibers.
[A comparative study of the development of drug differentiation between mexidol and phenazepam]
Interceptive stimulus properties of mexidol (50 and 100 mg/kg, i.p.) and phenazepam (2 mg/kg, i.p.) were compared using the standard operant model of liquid-reinforced drug discrimination (DD) procedure in male albino rats. Successful DD development has been shown in 100% of phenazepam-pretreated rats, while only 10% of mexidol-treated animals demonstrated DD. In the case of a high stimulus control, both mexidol and phenazepam DD manifestations showed high reproducibility (not less than 80% adequate reactions) and stability. The results suggest that mexidol, while possessing interceptive stimulus properties, belongs to the group of moderately discriminated psychotropic drugs.
[Mexidol corrects model post-reanimation changes in cerebral lipid metabolism]
The lipid spectrum of brain tissues in various stages of post-reanimation period was studied in rats upon clinical death modeled by cardiovascular fascicle ligation according to V. G. Korpachev. Reproduction of same model on the background of mexidol was characterized by (i) an increase in phosphatidylserine, (ii) normalization of the relative content of phosphatidylethanolamine and cholesterol, (iii) stabilization of the content of phosphatidylcholine, sphyngomyelin, lysophosphatidylethanolamine, and free fatty acids, and (iv) the absence of lysophosphatidylserine in late post-reanimation period (30 days) upon mexidol reperfusion. Mexidol also favored the development of protective and adaptive reactions on the level of lipid components of cerebral cell membranes in the early period upon reperfusion and prevented from the development of irreversible changes in cerebral phospholipid metabolism in the late post-reanimation period.
[Effect of mexidol on status of conditioned reflex activity after traumatic brain damage]
Even partial hippocampal lesions in rats resulted in a disturbance of time interval determination over the course of several months (1200-1500 presentations) other complex conditioned reactions being preserved. As distinct from the control animals, the long period of failure of time interval counting was absent in rats receiving Mexidol. Continuous time conditioning took place in these animals. Due to substantial improvement of autonomic processes and emotional reactions, it was possible to present a higher number of conditioned stimuli in experiments. Mexidol seems to improve the compensatory and recovery processes after brain injuries: the impaired functions recover faster, the rate of the retrograde degeneration in the lesioned brain structures decreases, phenomena like Monakov's diaschis are not observed etc.
[Mexidol potentiates antiparkinsonian effect of L-DOPA in MPTP-induced parkinsonism model]
Preliminary peroral administration of mexidol into mice with (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine)-induced parkinsonism model prevented the formation of malonaldehyde in striatum. In combination with small doses of L-DOPA (2-mg/kg), mexidol decreased oligokinesia and muscular rigidity manifestations and increased the levels of dopamine and its metabolites--dioxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in striatum. The combined (mexidol + L-DOPA) drug administration produced a 3-5 h increase in the time of the parkinsonism syndrome inhibition as compared to that upon the administration of a greater L-DOPA dose (100 mg/kg) without mexidol. It is suggested that mexidol, possessing antioxidant properties, is capable of preventing the damage and loss of the nigrostriatial dopaminergic neurons.
[Pharmacological treatment of memory disorders caused by hypoxia and cerebral ischemia in rats]
Experiments with white mongrel rats (both females and males) showed that nootropic substances, i.e. sodium hydroxybutyrate, pyracetam, oxyracetam, aniracetam, centrophinoxine, nooglutyl, mexydol, semax, amide L-pyroglutamyl-D-alanine, and MK-801, a specific noncontesting antagonist of the NMDA-receptor complex, significantly increased survivability of the animals following bilateral occlusion of the common carotid arteries. The nootrops prevented, partly or completely, mnestic disorders in the experimental rats. In contrast, MK-801 profoundly aggravated these disorders. Similar results were obtained with a model of hypoxic amnesia. Except for N-acetylglycine amide and amide L-pyroglutamyl-D-alanine, the nootrops fully or to a considerable extent blocked the development of mnestic disorders in hypoxic rats. The authors recommend novel nootrops (nooglutyl, mexidol, semax and GVS-111) for the pharmacological correction of mnestic disorders consequent to hypoxia or cerebral ischemia.
Edited by medievil, 04 September 2010 - 02:02 AM.
