Picamilon

Picamilon is an analogue of the neurotransmitter γ-aminobutyric acid (GABA), which is marketed as a nootropic claiming to enhance cognition. There is a lack of in silico, in vitro and in vivo data on the safety of picamilon. Therefore, to ascertain potential physiological effects of picamilon, it was screened against 50 safety-related biological targets (receptors, ion channels, enzymes, and transporters) by in silico and in vitro methods. Using two in silico tools, picamilon was not predicted to bind to the targets...

OBJECTIVE: To compare the clinical efficacy and safety of Picamilon Ginkgo and ginkgo biloba in patients with cognitive impairment in vascular diseases of the brain (chronic cerebral ischemia). MATERIAL AND METHODS: An open multicenter randomized comparative study involved 278 patients over 45 years of age with a diagnosis of chronic cerebral ischemia and cognitive impairment. 139 of them received Picamilon Ginkgo and 139 received monotherapy with ginkgo biloba extract for 90 days...

Glutamate is an excitatory neurotransmitter in the nervous system. Excessive glutamate transmission can lead to increased calcium ion expression, related to increased neurotoxicity. Memantine is used for treating patients with Alzheimer's disease (AD) due to its protective action on the neurons against toxicity caused by over activation of N-methyl-D-aspartate receptors. Nootropics, also called "smart drugs", are used for the treatment of cognitive deficits. In this work, we evaluate the neuroprotective action of four memantine analogues of glycine derivatives, including glycyl-glycine, glycyl-glycyl-glycine, sarcosine, dimethylglycine and three conjugates with nootropics, modafinil, piracetam and picamilon...

OBJECTIVE: To identify the presence of unapproved pharmaceutical drugs in over-the-counter dietary supplements marketed to improve memory and cognitive function. METHODS: Supplements were identified by searching 2 supplement databases for products labeled as containing omberacetam, aniracetam, phenylpiracetam, or oxiracetam, 4 drugs not approved for human use in the United States. Products were purchased online and analyzed using nontargeted liquid chromatography-quadrupole time-of-flight mass spectrometry methods...

Vinpocetine and picamilon are drugs prescribed in many countries to treat a variety of cerebrovascular disorders. In the United States, vinpocetine and picamilon have never been approved by the US Food and Drug Administration, but they are both available for sale directly to consumers as dietary supplements. We designed our study to determine the accuracy of supplement labels with regard to the presence and quantity of vinpocetine and picamilon. A validated ultra-high performance liquid chromatography-photodiode-array method was developed for the quantification of vinpocetine and picamilon...

During examination of 165 children aged 5 to 15 years (primarily identified during planned monitoring in Petrozavodsk children's institutions) with dysfunctional urination and encopresis without organic lesion of the central nervous system, autonomic dysfunction syndrome (ADS) was revealed. According to the results of urological examination, which was supplemented with the registration of spontaneous voiding rate and counting the radial pulse, overactive bladder syndrome and insufficient relaxation of the pelvic floor muscles during urination and defecation were detected; relationship between the number of heart rate (as a marker of sympathetic nervous system activity) and the effective volume was identified...

17 patients (mean age, 61 +/- 1.7 years) with an benign prostate hyperplasia (BPH) and urination disorders were under observation. After examination by ultrasound, urodynamic and laboratory studies, patients received conservative combined therapy, including alpha1-adrenoblocker silodosin, L-carnitine, B vitamins and picamilon. As a result of the 4,5-month treatment, most of the symptoms were eliminated as evidenced by the decrease in IPSS score from 17 to 3; urodynamic parameters have improved that was recorded by the home uroflowmetry...

Purpose was to study efficiency and safety of mexidol in combined therapy in patients with primary open-angle glaucoma (POAG). 94 patients (185 eyes) at the age of 18-75 years old with POAG I-III stages were divided into 3 groups: 50 patients received combined therapy of mexidol 100 mg and picamilon 150 mg, 22 patients received combined therapy of mexidol 300 mg and picamilon 150 mg, 22 patients received only picamilon 150 mg. All medicine was administered qd during 14 or 21 days. Examination included standard ophthalmologic methods, perimetry, electroretinography, retinal and optic nerve heard arterial blood flow...

The results of comparative study of efficacy and safety of vision correcting system "Focus" and Picamilon in patients with dry form of age macular degeneration are presented. 60 patients were enrolled into the study, follow-up was 3 months. Routine examination revealed positive impact of "Focus" on dynamics of main visual functions (visual acuity and field). In terms of impact on dynamics of main visual functions "Focus" is comparable with Picamilon, though it is better tolerated. Intake of vision correcting system "Focus" promotes visual functions improvement and prevents progressing of retinal degenerations...

The influence of picamilon and piracetam on the quantitative changes in the central GABA(A) macromolecular receptor complexes in the rat brain has been investigated under the experimental conditions of hypokinesia. It was found that the injection of these nootropes under the conditions of 7-day hypokinesia and 4-day recovery period did not show visible changes in the amount of active GABA(A) receptors. However, the injection of picamilon under the conditions of 15-day hypokinesia and 8-day recovery period showed a tendency to restoration of the number of active GABA(A) receptors...

A rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the determination of picamilon concentration in human plasma. Picamilon was extracted from human plasma by protein precipitation. High performance liquid chromatography separation was performed on a Venusil ASB C(18) column with a mobile phase consisting of methanol -10mM ammonium acetate-formic acid (55:45:01, v/v/v) at a flow rate of 0.65ml/min. Acquisition of mass spectrometric data was performed in selected reaction monitoring mode, using the transitions of m/z 209...

The administration of aminalon (0.25 g), fenibut (0.25 g) and picamilon (0.10 g) during 4 weeks as a means of recovery for swimmers with disadaptation syndrome helped to optimize the biochemical status and cerebral circulation 20-min after warm-up. The reaction to the warm-up load under test conditions was characterized by increasing total blood filling of the brain and difficulty of venous outflow. Under the action of drugs, a decrease in blood filling of the brain and increase in venous blood outflow from the cerebral basin was observed 20 min after load in all test groups (except the hypokinetic group taking picamilon)...

The influence of a 15-day hypokinesia on the development of anxiety-depression state and quantitative changes in the central GABA-A macromolecular receptor complexes in the rat brain has been investigated under conditions of the despair (forced swim) test. Simultaneously, the effects of well-known nootropic drugs picamilon and piracetam on the dynamics of state parameters in the experimental animals have been evaluated. It was found that hypokinesia led to the development of anxiety and depression accompanied by reduction in the amount of active GABA-A receptors...

A total of 43 infants under 3 years of age with organic, functional and reflux obstructive megaureter were studied. The function of the upper urinary tract was examined with dynamic pyeloureterosonography with diuretic load. Contractility of isolated fragments of megaureters and possibility of its pharmacological regulation were studied in patients after surgery in vitro. Different urodynamic variants of the response of refluxing and obstructive megaureters and those with functional obstruction on stimulation of diuresis were established at dynamic pyeloureterosonography with diuretic load...

The role of GABAergic mechanisms in realization of the effects of afobazole and picamilon on the cerebral circulation was studied in rats. It is found that the cerebrovascular effect of afobazole significantly decreases on the background of the GABA receptor antagonists bicuculline and picrotoxin. This is evidence of an important role of the GABA system in the its cerebrovascular and neuroprotective activity of afobazole. The results of experiments with picamilon showed that the cerebrovascular effect of this drug is not affected by receptor blocking with bicucullin...

A comparative acute toxicity test of the nootropic drugs piracetam and picamilon was performed on rats. The study was based on the principles of integral evaluation of the drug effect upon the functional and behavioral state of animals. It was found that the conventional therapeutic index does not coincide with the actual therapeutic activity range. Piracetam and picamilon, while exhibiting significantly different toxicity, are characterized by approximately equal ranges of the therapeutic activity.

The paper is devoted to the role of GABA system in the pharmacotherapy of ischemic brain injuries. In an analysis of the neuroprotector activity of GABA-mimetics, both their involvement in the maintenance of a balance between exciting and inhibiting processes and participation of the GABAergic mechanisms in regulation of the cerebrovascular tone are considered because proper blood supply is an important factor in the successful therapy of patients with ischemic brain injuries. Data available in the literature and the results of original investigations are summarized to assess the cerebrovascular and neuroprotector properties of GABA, as well as agonists and modulators of GABA receptors (muscimol, picamilon, phelbamate, clomethiazole, etc...

Absorption by the bovine retina of physiological concentration of PLP-GABA increase clearing 2-32 minutes of incubation in difference of GABA and its non metabolic preparations, which store up as much as possible in first minutes: picamilon > PLP-GABA > GABA > panthogam > biotinil-GABA. Kinetics of transport of GABA and its preparations into retina has a complex character. By the growth of concentration from 33 mM to 528 mM, it is linear for picamilion, showing diffusion, and not linear for GABA, PLP-GABA and panthogam, showing differently systems of its transport...

Picamilon was used in the treatment of 48 patients with central chorioretinal dystrophies. In group 1 (34 eyes) the drug was delivered to the posterior pole of the eye through an infusion collagen system, which was followed by He-Ne laser exposure. In group 2 (46 eyes) the patients were given picamilon tablets. The following examinations were carried out in all patients before and immediately after treatment: evaluation of visual acuity, borders of peripheral visual field, critical frequency of fusion of flashes, visocontrastometry, electroretinography with consideration for pathological changes in the retina, rheography, direct and indirect ophthalmoscopy...

Electric impedance measurements on awake rabbits with electrodes implanted into cortex, thalamus, and hypothalamus showed that modeling of the noise and general (wide-band) vibration, as well as their combination with sea-sickness action, leads to disturbances in the aqueous-electrolyte balance in brain. This is manifested by extracellular and (less pronounced) intracellular edema development. Picamilon administration (10 mg/kg, i.v.) completely prevented development of the vibration-induced intracellular edema and markedly reduced the development of damage in all other cases studied...