Cerebrolysin

Nootropic drug used for dementia

Cerebrolysin was discovered by Gerhart Harrer, who worked at the University of Innsbruck. He discovered that during the fermentative hydrolysis of the brain tissues forms substances that have a stimulating effect on nerve cells and are able to regulate vegetative disorders.

After the technological development of the drug, cerebrolysin was first registered in Austria on August 1, 1954. G. Harrer, later a professor at the University of Salzburg and chairman of the Society of Neurologists and Psychiatrists of the Austrian Republic, made a great contribution to the further successful advancement of cerebrolysin in clinical practice. The first publications on the clinical use of cerebrolysin dated back to 1954-1955, when it was found that cerebrolysin might contribute to waking up the patient from hypoglycemic coma.

In a series of studies in 45 patients, half of the patients wake up immediately after the administration of the drug, evaluation of the parameters of the electroencephalogram (EEG) showed the disappearance of pathological changes typical for hypoglycemia. At the same time, another study was published about the positive effect of the “amino acid mixture” (cerebrolysin) in the treatment of Petit mal epilepsy and narcolepsy.

In subsequent years, the number of publications on the clinical use of cerebrolysin in the treatment of mental disorders of various nature, cerebrovascular disorders, chronic brain trauma and cerebral atherosclerosis increased. Cerebrolysin was used in the numerous clinical trials on patients with dementia and other mental disorders. It was also found that cerebrolysin may potentiate the therapeutic effect of tricyclic antidepressants.

The drug has a unique neuron-specific multimodal effect on the brain, which is manifested in the ability of cerebrolysin to regulate metabolic functions, neuroprotective action, functional neuromodulation and neurotrophic activity.

Cerebrolysin provides protection of nerve cells from lactic acidosis and the damage from free radicals increases the number of viable neurons and promote their survival during hypoxia.

The main mechanisms of action of cerebrolysin in its effect on energy metabolism (the decrease in the level of lactate in the nervous tissue and the optimization of mitochondrial processes), the neurotrophic effect and modulation of the activity of endogenous growth factors, as well as the interaction with neuropeptide and neurotransmitter systems. Besides, according to studies Cerebrolysin injections has the immunomodulating effect.

It is known that cerebrolysin contains biologically active amino acids and peptides, which, after penetrating the blood-brain barrier, regulate intracellular metabolism and improve synaptic transmission. As the result of their action, aerobic energy metabolism gets enhanced, intracellular protein synthesis is improved, which reduces the effect of lactic acidosis.

As shown in the studies, the peptide fraction of cerebrolysin exhibits neuron-specific neurotrophic activity. Neurotrophic factors as secretory proteins, acting on neurons, regulating their long-term experience, causing differentiation, protecting neurons from the consequences of various types of damage and supporting their regeneration. One of those neurotrophic factors is Nerve growth factor (NGF) – the first discovered protein that is able to stimulate the growth of cholinergic neurons in the basal forebrain.

According to experimental studies, cerebrolysin reduces the need of the brain in oxygen, promoting an increased resistance to ischemic and hypoxic conditions, enhances aerobic metabolism, significantly lowers the level of lactate in the neuronal tissue, and also provides an optimal level of ATP in the neurons, which allows them to respond adequately to energy-dependent problems.

The first information about the cerebrolysin side effects began to accumulate in the system of pharmacological control since 1974. A couple cases were described, which constitute an insignificant percentage of the total number of adverse reactions in cerebrolysin-treated patients that are not directly related to treatment. Some of those side effects include:

  • Dizziness
  • Anxiety
  • Irritability
  • Tachycardia
  • Nausea
  • Loose stools
  • Local allergic reactions on skin

Local reactions might be caused by a rapid intravenous introduction of cerebrolysin, which causes a slight soreness at the injection site, and insignificant hyperthermia after a rapid IV infusion.