Pantocalcin®

Nosological classification (ICD-10)

• E63 Physical and mental overload
• F03 Dementia, unspecified
• F06.7 Mild cognitive impairment
• F20 Schizophrenia
• F79 Mental retardation, unspecified
• F80 Specific developmental disorders of speech and language
• F81 Specific developmental disorders of learning skills
• F82 Specific developmental disorders of motor function
• F84 General disorders of psychological development
• F90 Hyperkinetic disorders
• F95 Tiki
• F98.5 Stuttering [stammering]
• G09 Consequences of inflammatory diseases of the central nervous system
• G10 Huntington's disease
• G20 Parkinson's disease
• G40 Epilepsy
• G46 Vascular cerebrovascular syndromes in cerebrovascular diseases
• G80 Cerebral palsy
• G93.9 Brain damage, unspecified
• R25.8.0* Hyperkinesis
• R32 Urinary incontinence, unspecified
• R39.1 Other urinary difficulties
• R41.8.0* Intellectual-mnestic disorders
• T43.3 Poisoning with antipsychotic and antipsychotic drugs
• T90.5 Consequences of intracranial injury

Pharmacodynamics

The spectrum of action is associated with the presence of GABA in the structure. The mechanism of action is due to the direct effect of the drug Pantocalcin® on the GABAB receptor-channel complex. It has neurometabolic, neuroprotective and neurotrophic properties. Increases the brain's resistance to hypoxia and the effects of toxic substances, stimulates anabolic processes in neurons. It has an anticonvulsant effect, reduces motor excitability while regulating behavior. Increases mental and physical performance. Helps normalize GABA content during chronic alcohol intoxication and subsequent ethanol withdrawal. Shows analgesic effect. It is capable of inhibiting acetylation reactions involved in the mechanisms of inactivation of novocaine and sulfonamides, thereby prolonging the action of the latter. Causes inhibition of the pathologically increased bladder reflex and detrusor tone.

The proportion of psychoorganic pathology is growing among both children and adults. Comprehensive rehabilitation is usually complemented by drug therapy, which creates a favorable background for non-drug treatment methods and enhances their effect by activating metabolic processes in the nervous system. Unfortunately, neurometabolites have a number of limitations - many stimulant-type medications are characterized by side effects in the form of irritability, agitation, aggressiveness, and sometimes the threat of seizures. Their use is also limited by time intervals and gradual adaptation of the body with a decrease in the expected effectiveness of treatment [1].

The relevance of including drugs with nootropic and neurotrophic effects in the treatment regimen for various psychoneurological pathologies of childhood is associated with the high plasticity of the child’s brain, the possibility of age-dependent compensation and, consequently, reducing the severity of neurological deficits [2]. However, there are a number of features of therapy and rehabilitation of children associated with both objective and subjective reasons. The first include age-related, idiopathic and dose-dependent restrictions. The second includes the peculiarities of the parents’ psychology: reluctance to “feed the child pills at all,” “frightening” side effects and discussion of possible “horrors” of treatment on Internet forums with people far from medicine. In such conditions, minimizing drug therapy with the widest possible positive effects and relative harmlessness of the drug used guarantees the patient’s adherence to treatment and, accordingly, the quality of rehabilitation.

The choice and use of certain drugs are determined by the nature of the existing disorders, the degree of their severity, the age and individual reaction of the child. Since diseases of the nervous system in children in the first years of life are characterized by impaired maturation of individual functional systems, drug therapy should be aimed primarily at stimulating normal brain development. For this purpose, medications are used that improve metabolism in the nervous system. Over the past decades, studies by many domestic and foreign scientists have been devoted to studying the effectiveness of the use of various nootropic drugs.

In particular, various works are devoted to the study of the mechanisms of action of hopantenic acid as a derivative of one of the main neurotransmitters of the human brain. L.S. Chutko [3] (2012) describes the problem of school maladjustment and the possibility of neurotrophic correction of this condition with the help of Pantocalcin (hopatenic acid). Review by K.V. Voronkova (2011) [4] modern literature on cognitive impairments of various origins confirms the effectiveness and safety of the use of Pantocalcin in solving this problem. Articles by N.N. Zavadenko (2006) [5], V.B. Sosina (2006) [6], N.A. Korovina (2006) [7], A.F. Tumashenko (2006) [8], N.M. Musatova (2006) [9], N.V. Muratova (2007) [10], T.A. Lazebnik (2010) [11], E.A. Morozova (2011) [12] are devoted to the use of Pantocalcin in psychoneurological pathology in children and adults, in particular with attention deficit hyperactivity disorder, vegetative-vascular dystonia, extrapyramidal disorders, speech disorders and senile dementia. The problem of enuresis and the possibility of using Pantocalcin for this disorder is highlighted in the works of V.I. Borodina (2006) [13] and T.V. Otpuskova (2009) [14].

The mechanism of action of the drug is based on the similarity of the chemical formula with gamma-aminobutyric acid (GABA), which is one of the natural mediators of the central nervous system (CNS). Pharmacological effectiveness is associated with a direct effect on the GABAb receptor-channel complex and an activating effect on the formation of acetylcholine. Hopanthenic acid, unlike GABA (due to the presence of a pantoyl radical in its molecule), penetrates the blood-brain barrier and has a pronounced effect on the functional activity of the central nervous system. The entry of the drug into the brain reaches a maximum after 60 minutes, after which it accumulates mainly in the cells of the cerebral cortex, subcortical structures, and the cerebellum. Pantocalcin is excreted from the body unchanged, which also reduces the risk of developing dose-dependent and cumulative complications of therapy.

Hopanthenic acid has many points of application in cellular metabolism, which determines a wide range of pharmacological actions. Thus, the drug improves glucose utilization, nucleic acid metabolism, activates the synthesis of ATP, protein and RNA, i.e. stimulates anabolic processes in brain neurons. The indirect neurometabolic effect of the drug is associated with improved microcirculation in the brain by optimizing the passage of red blood cells through the microvasculature and inhibiting platelet aggregation. Along with the neurometabolic effect, the drug has antihypoxic and antioxidant effects. By restoring GABA-dependent neurotransmission, hopantenic acid leads to improved bioelectrical activity and integrative activity of the brain, improved memory, perception, attention, thinking, increased learning ability, activation of intellectual functions and for the same reason is not contraindicated in epilepsy, which is its great advantage compared to other neurotrophic drugs. Side effects of the drug are extremely rare and are expressed in the form of allergic reactions (skin itching, urticaria and allergic rhinitis).

Pantocalcin has no age-related contraindications, which makes it popular in pediatric practice. Taking into account all the positive properties of the drug, its use is possible for almost any psychoneurological pathology of childhood.

Own experience of using Pantocalcin in various psychoneurological pathologies of childhood

The number of children in the dispensary group with pathology of the nervous system (Voronezh) over the past 6 years is presented in the figure.

As can be seen from the diagram above, over the past few years there has been a positive trend in the number of patients being observed for neurological pathology, but the number of patients remains quite large.

Delayed speech development

One of the most common reasons for visiting a neurologist is speech delay in children aged from one to 5 years. The peak of this disease occurs at the age of 2.5–3.5 years. Often, delayed speech development is an integral part of a general psychoneurological deficit, but in most cases it is in the nature of a partial developmental deviation. Neuroprotective therapy is relevant in most cases, excluding such rare conditions as epileptic encephalopathy (in particular, Landau-Kleffner syndrome), true autism and orphan diseases associated with regression of mental development (for example, Rett's disease). According to our data, the share of such diseases in the structure of speech development delays does not exceed 3%. In other cases, nootropic therapy is needed to stimulate and support the child’s nervous system during critical periods of development.

We analyzed 120 cases of delayed speech development in children aged 3 to 5 years. The ratio of partial speech delay (92) and speech delay in the structure of general psychoneurological deficit (28) in the study group was 3.2: 1.0. In 98% (118) of cases, neuroprotective therapy with Pantocalcin was used at a dose of 30–40 mg/kg body weight per day. In two cases, the examination revealed violations that resulted in the exclusion of patients from the study group (1 – high index of epileptic activity on the electroencephalogram, 1 – autistic behavior). In addition, in a third (39; 33.1%) of children, speech delay was combined with hyperactive behavior, so additional light sedative therapy was required (Tenoten for children, Persen, Magne B6).

Due to the fact that this type of disorder is impossible without developmental exercises, fine motor skills, psychological variations and socio-psychological conditions for speech development, the use of nootropics has the character of a “stimulating cushion”, on the basis of which it is necessary to build a dominant speech development. This process is quite lengthy and ideally requires systematic daily combined work of the child, parents, psychologist, neurologist and speech therapist. Therefore, the course of Pantocalcin averaged 2.5 months (from 2 to 3 months).

In 83.1% (98 out of 118) of cases, parents fully complied with the doctor’s recommendations and in 74.5% (73 out of 98) noted significant changes in the development of speech in children along with improved behavior and sleep. The remaining 25 patients showed less pronounced results after 3 months, but positive dynamics were observed in all cases. Lack of adherence to therapy on the part of parents of 20 (out of 118) patients did not allow us to reliably assess the results of treatment.

Epilepsy and non-epileptic paroxysmal conditions

Unprovoked paroxysms are observed annually in 56.8 people per 100 thousand per year, in 23.5 per 100 thousand per year - this is the only unprovoked attack. During their lifetime, 5% of the population suffers at least one paroxysm [15]. Paroxysms that occur in childhood are clinically more diverse; a significant part of them are epileptic seizures. Other, non-epileptic, include fainting, affective-respiratory seizures, syncope, metabolic convulsions, parasomnias, etc. Depending on the etiology of these conditions, various groups of drugs are used to treat children - psychostimulants, tricyclic antidepressants, neuroleptics, combination drugs, antiepileptic drugs, etc. .d. Most treatment regimens include neuroprotective drugs, which is directly related to the age-related characteristics of the nervous system of children [16–19].

As was shown in our study [20] (E.A. Balakireva, 2010), which included 363 patients with paroxysmal conditions of various origins, 76% (276) after three days allotted for establishing a clinical diagnosis in accordance with the standards, it was necessary to start therapy with the use of injectable drugs without definitively establishing the etiology of the attacks. In addition, 47% (171) of treatment had to be carried out during the initial hospital stay without final verification of the diagnosis. Thus, during the first inpatient course, there is a need to prescribe drugs that are not contraindicated for any type of paroxysmal conditions; accordingly, they can be used regardless of the etiology and clinical picture of paroxysms. The algorithm we developed (E.A. Balakireva, 2012) [21] included a course of Cortexin injections followed by maintenance therapy with Pantocalcin at a dose of 30–40 mg/kg body weight/day for a month. A marked decrease in the frequency of paroxysmal states of non-epileptic origin, improvement in behavioral and dyssomnic disorders was noted among 76% (189 out of 248) of patients. Positive dynamics in behavior and sleep disorders in children with epileptic seizures were noted by 48% (28 out of 59) of parents.

In 42% (152) of cases, the course of Pantocalcin was repeated after 3 months for children with both epileptic and non-epileptic paroxysmal conditions. The positive effect of the applied scheme was noted in 100% of cases.

Tiki

The prevalence of tic hyperkinesis, according to various literature data, varies within a fairly large reference range – from 5 to 25% [22–24].

Summarizing the literature data, we can say that the etiopathogenetic factors of tics necessarily include genetic (tic disorder is inherited in an autosomal dominant manner with low penetrance), socio-psychological (environmental) and neurochemical.

Following the principle of selecting the smallest effective and safe dose of drug therapy, we gradually tested various mild and moderate sedative drugs in a group of 138 patients aged 3 to 12 years (M: F – 1.3: 1.0), suffering from acute and chronic tic disorder in the form of a local tic (facial muscles, isolated choking, blinking tic). Initial monotherapy with Pantocalcin for 1–3 months was effective in a group of children with acute tic disorders – 21% (29).

Improvement occurred from the first days of use, which can be explained by the moderate sedative effect of the drug. Complete relief of hyperkinesis occurred in all children by the end of the second week of use, when, obviously, the cumulative nootropic effect of the drug came into effect. In 27% (37) of cases, the full effect could not be achieved, but positive dynamics were noted by the majority (27) of patients. In other cases, polytherapy could not be avoided. Thus, in almost half (48%) of cases in children with tic disorder of predominantly mild severity, Pantocalcin was effective in monotherapy.

Conclusion

Our experience in using Panto-calcin in children with various disorders of the nervous system has shown that the drug is well tolerated by patients and is effective for correcting psychoneurological symptoms even in monotherapy.

Indications for the drug Pantocalcin®

cognitive impairment in organic brain lesions and neurotic disorders;

as part of complex therapy for cerebrovascular insufficiency caused by atherosclerotic changes in cerebral vessels; senile dementia (initial form), residual organic brain damage in mature and elderly people;

cerebral organic failure in patients with schizophrenia (in combination with antipsychotics, antidepressants);

extrapyramidal hyperkinesis in patients with hereditary diseases of the nervous system (including Huntington's chorea, hepatocerebral dystrophy, Parkinson's disease);

consequences of neuroinfections and traumatic brain injuries (as part of complex therapy);

correction and prevention (cover-up therapy with simultaneous prescription) of side effects of antipsychotics; extrapyramidal neuroleptic syndrome (hyperkinetic and akinetic);

epilepsy with slowing of mental processes (in combination with anticonvulsants);

psycho-emotional overload, decreased mental and physical performance; to improve concentration and memory;

urinary disorders: enuresis, daytime urinary incontinence, pollakiuria, urgency;

Children:

mental retardation (delayed mental, speech, motor development or a combination thereof);

cerebral palsy;

stuttering (mainly clonic form);

epilepsy (as part of combination therapy with anticonvulsants, especially for polymorphic seizures and petit mal seizures).

Directions for use and doses

Inside.

Take 15–30 minutes after meals.

A single dose for adults is 0.5-1 g, for children - 0.25-0.5 g, daily dose - 1.5-3 g (for adults), 0.75-3 g (for children). The duration of treatment is from 1 to 4 months, in some cases up to 6 months. After 3–6 months, a second course of treatment is possible.

Children. Mental deficiency - 0.5 g 4-6 times a day, daily for 3 months. Delayed speech development - 0.5 g 3-4 times a day for 2-3 months.

Neuroleptic syndrome (as a corrector for the side effects of neuroleptic drugs). Adults - 0.5–1 g 3 times a day; children - 0.25–0.5 g 3–4 times a day. The duration of treatment is 1–3 months.

Epilepsy. Children - 0.25–0.5 g 3–4 times a day; adults - 0.5–1 g 3–4 times a day daily for a long time (up to 6 months).

Hyperkinesis (tics). Children - 0.25–0.5 g 3–6 times a day daily for 1–4 months; adults - 1.5–3 g per day daily for 1–5 months.

Urinary disorders. Adults - 0.5-1 g 2-3 times a day (daily dose - 2-3 g); children - 0.25-0.5 g (daily dose - 25-50 mg/kg). The duration of treatment is from 2 weeks to 3 months (depending on the severity of the disorder and the therapeutic effect).

Consequences of neuroinfections and traumatic brain injuries. 0.25 g 3-4 times a day.

To restore performance under increased loads and asthenic conditions. 0.25 g 3 times a day.

This dosage form is not recommended for children under 3 years of age.

Pantocalcin®

Orally 15-30 minutes after meals. Taking into account the nootropic effect of the drug, it is preferably taken in the morning and afternoon.

Single dose for children

- 250.0-500.0 mg; daily dose for children - 750.0-3000.0 mg.

Single dose for adults

- 250.0-1000.0 mg; daily dose for adults - 1500.0-3000.0 mg.

The course of treatment is 1-4 months, sometimes up to 6 months. After 3-6 months, a second course of treatment is possible.

For children, depending on age and pathology of the nervous system, the following dose range is recommended: children of the first year - 500.0-1000.0 mg per day, up to 3 years - 500.0-1250.0 mg per day, children from 3 to 7 years - 750.0-1500.0 mg, over 7 years - 1000.0-2000.0 mg. Treatment tactics include increasing the dose over 7-12 days, taking the maximum dose for 15-40 days or more, with a gradual dose reduction until discontinuation within 7-8 days. The course of treatment is 30-90 days (for some diseases - up to 6 months or more).

For epilepsy in combination with anticonvulsants - at a dose of 750.0-1000.0 mg per day. The course of therapy is up to 1 year or more.

For neuroleptic syndrome accompanied by extrapyramidal disorders, the daily dose is up to 3000.0 mg, treatment for several months.

For extrapyramidal hyperkinesis in patients with organic diseases of the nervous system - 500.0-3000.0 mg per day. The course of treatment is up to 4 months or more.

For the consequences of neuroinfections and traumatic brain injuries - 500.0-3000.0 mg per day.

For urinary disorders: children - 250.0-500.0 mg, daily dose is 25-50 mg/kg, course of treatment is 1-3 months; adults - 500.0-1000.0 mg 2-3 times a day.

To restore performance under increased loads and asthenic conditions, 250.0-500.0 mg is prescribed 3 times a day.

For precise dosing of the drug, use a measuring syringe included in the package, which has special divisions, the price of which corresponds to the amount of the drug in milligrams (from 0 to 500.0 mg).

Using a measuring syringe:

Firmly insert the measuring syringe into the hole in the adapter installed in the neck of the bottle.

Turn the bottle upside down and smoothly pull the plunger down, drawing the solution into the syringe to the desired mark (Figure 1).

If air bubbles are visible in the solution, press the plunger all the way, then refill the syringe.

Return the bottle to its original position and remove the syringe, gently turning it (Figure 2).

If the drug is being taken by a child under 3 years of age, place the syringe in the child's mouth (cheek area) and slowly press the plunger, releasing the solution smoothly so that the child can swallow the solution properly. While taking the solution, the child should be in an upright position.

When taking the drug by children over 3 years of age and adults, the solution from the syringe can be first poured into a spoon.

After use, rinse the syringe in warm, clean water and dry it. The measuring syringe should be stored in the package along with the drug.