29.11.2020

Phenotropil: pharmacological action of the drug and analogues medicines

Phenotropil the original drug was registered in practical healthcare of Russia in 2003 as a stimulant with nootropic activity. Medicines of this group of students ‘ cognitive (cognitive) function, strengthen memory, improve learning ability.

Phenotropil, was developed in the Institute of biomedical problems as a means of enhancing physical and mental performance of astronauts in various stages of space flight. The drug was given the opportunity to overcome the heavy load. Reiterating their high efficiency, the drug moved into civilian clinical practice.

In the history of medicine there have been occasions when some of the substance had initially opened up some properties, and others are optional or even drastically alter the view of him as the drug. A large number of experimental and clinical studies Phenotropil showed an extremely wide range of pharmacological and therapeutic effects of the drug.

Pharmacological effects of Phenotropil

Clinical activity of Phenotropil manifested in the following effects:

  1. Nootropic effect – affects the disorder of higher functions of the cerebral cortex, the degree of critical judgment, improves the control of subcortical centers, attention, thinking, speech.
  2. Mnemotropic action – affects memory, learning ability.
  3. The increased activity levels, clarity of consciousness affect the state of the oppressed and dizziness.
  4. Adaptogenic effect – affects resistance to various external factors, including drugs, increases the overall resistance of an organism to influence of extreme factors.
  5. Antiasteniceski action affects the emaciation, weakness, lethargy, mental and physical fatigue.
  6. Stimulating effect – affects apathy, reduced volitional activity, unwillingness to act, a mental inertia, psychomotor retardation.
  7. Antidepressant effects.
  8. Sedative (tranquilizing) action – reduces irritability and emotional excitability.
  9. Vegetative action affects headache, dizziness, zerebrasteniceskie syndrome.
  10. Antiparkinsonian effect.
  11. Antiepileptic action affects epileptic paroxysmal activity.

When applied topically Phenotropil has anti-inflammatory, rejuvenating effect by restoring the vascular tone, joint mobility, softening and repairing the skin changes associated with age.

Counterparts Phenotropil

A number of substances belonging to the group of nootropic drugs, has a broad spectrum of pharmacological activity. The Russian market presents a wide range of drugs of this group. Most of them are medicines of domestic production. Table 1 shows the analogues of Phenotropil, which are the nootropic drugs.
Table 1

International non-proprietary name, active ingredient of the drug Trade name drugs
Vinpocetine Cavinton, Vinpocetine, Telekol, Brevicon, Vincentin
Glycine Glycine
Gopantenova acid Pantogram, Pantokaltsin, Garantam, Gopantenova acid
Idebenone Noben, Idebenone, Neyromet, Celesta
Meclofenoxate Ceruti, Meclofenoxate hydrochloride
Have nicotinoyl –gamma-aminobutyric acid Pikamilon, Pikogan, Amelanosis, Aminalon
Piracetam Nootropil, Piracetam, Lucetam, Memotropil
Pyritinol Encephabol, Piriditol, Averbol
The hydrolysate brain of cattle Cerebrolysin
Polypeptides from the brain of embryos of pigs Cellex
The polypeptides of the cerebral cortex Cortexin
Cerebrolysin Cerebrolysin
Citicoline Ceraxon, Lira, Citicoline sodium, Napilap, Recogne, Pronare, Quinell
Ethyl ether N-phenylacetyl-L-polyglycine Noopept
D,L-Gopantenova acid Pantogam-Aktiv, rat-gopantenova acid
Kaviton

Kaviton – original medication pharmaceutical company Gedeon Richter (Hungary). It is anti-inflammatory medication for the prevention of diseases of small vessels. With the 60-ies of XX century Cavinton is widely used for the treatment of diseases of the brain caused by pathological changes of cerebral vessels with cerebrovascular disease – cerebrovascular disease. The drug increases cerebral blood flow and has a neuroprotective effect.
The mechanism of action of Kaviton:

  • improves cerebral blood flow and metabolism;
  • has a beneficial effect on the properties of blood.

Proven neuroprotective effect of Cavinton can be recommended for long term treatment of prophylactic in the early stages of cerebrovascular diseases that do not manifest significant symptoms.

A decade of large-scale observational study 967 patients with different cerebrovascular disorders have shown that Cavinton is most effective when the appointment early, at the stage of first manifestations of the disease.

Glycine

Glycine eliminates depressive disorders, irritability, normalizes sleep, reduces pathological attraction to alcohol. Having antiepileptic, anti-stress, sedative effect. Restores the metabolism.

The effectiveness of glycine in various pathological conditions associated with anoxia, due to the influence of amino acids on the receptors of cell membranes of various organs and tissues.

The introduction of glycine to animals promotes their survival by 67 %, restores the indices of electrocardiography in a short time after the injection, significantly improved the ejection volume of the left ventricle.

Cortexin

Cortexin is used to treat diseases of the Central nervous system. The drug increases brain resistance to adverse effects, has anticonvulsant effect, reduces the toxic effects of substances that affect the Central nervous system, improves the processes of learning and memory, accelerates the restoration of the cerebral cortex.

Cortexin gives a powerful neurotrophic effect. The drug is used in neurology in critical pathological conditions involving edema-swelling of brain neurotrauma, epileptic status, meningoencephalitis, coma, a vegetative state.

Cortexin has found wide application in pediatric neurology. Its positive therapeutic effect observed in the prenatal damage to the Central nervous system, cerebral palsy, residual-organic pathology, delayed psychomotor and speech development, syndromes of attention disorders and autonomic dysfunction.

Ceraxon

Ceraxon (international nonproprietary name – citicoline) developed by a Spanish pharmaceutical group Ferrer International S. A. Pharmacological properties are investigated citicoline for more than 40 years. The drug has membrane-stabilizing, anti-edema effect, reduces the level of memory loss, cognitive manifestations, sensitive and motor disorders.

The drug has been used successfully to protect and restore the nervous tissue when ischemia – cerebrovascular disorders after strokes, after head injuries, discirculatory encephalopathy.

Ceraxon is included in the standard treatment of ischemic stroke in several countries in Europe with proven effects in reducing the area of non-functioning and partly corrupt, but preserving the viability of the cells surrounding the lesion of primary damage in ischemic stroke.
Ceraxon has a complex effect on the Central nervous system:

  • provides structural support and restorative effect;
  • optimizes the metabolic and energy processes, neurotransmitter metabolism;
  • improves synaptic transmission;
  • inhibits cascade processes and reduces the formation of free radical compounds.

Ceraxon is recommended for use at all stages of treatment including the acute phase, when brain injury and stroke.

Cerebrolysin

Cerebrolysin – a neurotrophic drug action. This is one of the most popular in everyday clinical practice medication in the treatment of acute stroke and chronic forms of vascular brain pathology.

Due to the multifactorial action of Cerebrolysin is regarded as potential therapeutic tool in the following diseases: dementia (dementia), stroke, Alzheimer’s disease, traumatic brain injury, perinatal pathology, mental retardation.

Contained in the Cerebrolysin low-molecular biologically active neuropeptides have a specific effect on the brain, providing the regulation of metabolic processes, slowing the processes of brain damage, functional stimulation, the activity of growth and development of cells of the nervous tissue. This increases the efficiency of energy metabolism of the brain, increasing intracellular protein synthesis.

The drug protects neurons from the damaging effect of lactic acidosis, prevents the formation of free radicals, increases survival and prevents neuronal death in conditions of hypoxia and ischemia, reduces the damaging neurotoxic effects of excitatory amino acids (glutamate).

In disorders of cognitive functions Cerebrolysin positively influences the processes of memorization and reproduction of information, stimulates mental activity, improves mood, promotes the formation of positive emotions.

Pikamilon

Pikamilon has a regulating influence on the Central nervous system, increases cerebral blood flow and reduces the tonus of the arteries. Experimentally proved that Pikamilon influence on an emotional sphere, substantially affecting the level of depression.

Pikamilon administered as vasoactive (affecting blood vessels) and neuroprotective agent in acute cerebral blood circulation of mild and moderate severity, as well as in chronic cerebrovascular insufficiency and syndrome of vegetative dystonia, particularly with signs of high blood pressure, and if the leading is dominated by the increasing manifestations of migraine, tachycardia. Medicine contributes to the reduction of systemic blood pressure and slowing heart rate.
Picamilon is recommended for asthenic disorders of various etiology, depressive disorders in old age, senile psychosis, as well as in the complex therapy for relieving asthenic and asthenic-neurotic manifestations.

Among the analogues Phenotropil medication with the best evidence base are Ceraxon and Cerebrolysin. Drugs have in the Arsenal more than five high quality research evidence – a placebo-controlled randomized study, involving more than 1000 patients with various cerebrovascular diseases.

To a lesser extent tested the efficacy and safety of the drug Cortexin – two randomized placebo controlled trials involving 332 patients with stroke and chronic brain ischemia.

According to the analysis of the Russian market of neuroprotectant in 2017 on the effectiveness of the drug Phenotropil, there was one placebo-controlled randomized study in a single centre, which was attended by 75 patients with chronic brain ischemia. Phenotropil have no study with high level of evidence that puts them on a lower step of the pyramid of evidence-based medicine. However the drug enters into the three of leaders of sales among nootropic drugs.
Phenotropil, its analogs Cortexin, Ceraxon, Cerebrolysin are expensive. Much cheaper than analogues of Glycine, Pikamilon.

International nonproprietary name The trade name of the drug Price Release form Manufacturer
Phenotropil (N-carbamoylmethyl-4-phenyl-2-pyrrolidone) Phenotropil 535 RUB Tablets 100 mg, 10 pieces Russia
glycine Glycine 28 RUB. Tablets under the tongue 100 mg, 50 pieces Russia
Cortexin Cortexin 734 RUB. Lifelist for preparation of solution for injections 5 mg, 10 vials Russia
citicoline Ceraxon 680,50 RUB. Ampoules 500 mg, 4 ml, 5 pieces Spain
Cerebrolysin Cerebrolysin 992 RUB. Solution for injections 2 ml, 10 vials Austria
N-nicotinoyl-gamma-aminobutyric acid sodium salt Pikamilon 95 RUB. Tablets 20 mg, 30 pieces Russia

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