Cerebrolysin^® Instruction

International Non-Proprietary Name (INN): none
Dosage form: solution for intramuscular and intravenous injections in ampoules/vials (2, 5, 10 ml)
Structure
In 1 ml:
Active substance: 215.2 mg of Cerebrolysin^® concentrate (complex of peptides derived from the pig brain tissue) in aqueous solution. The active fraction of Cerebrolysin^® is represented by peptides, whose molecular weight does not exceed 10,000 daltons.
Excipients: sodium hydroxide and water for injection.
Description
Transparent solution of amber color.
Pharmacological classification: nootropics
ATC code: N06BX

• Pharmacodynamics
• Pharmacokinetics
• Intended Uses
• Contraindications
• Dosage and Administration
• Side Effects, Overdose
• Drug Interaction
• Special instructions
• Pregnancy and Lactation
• Influence on the Ability to Drive Vehicles
• Storage Conditions & Shelf Life
• Manufacturer

Pharmacodynamics

Cerebrolysin^® contains low molecular weight biologically active neuropeptides that penetrate the BBB (blood-brain barrier) and directly enter the nerve cells. The drug has an organ-specific multimodal effect on the brain, i.e., provides metabolic regulation, neuroprotection, functional neuromodulation, and neurotrophic activity.

Metabolic regulation: Cerebrolysin^® improves the effectiveness of aerobic energy metabolism of the brain and improves intracellular protein synthesis in both the developing brain and the aging brain.

Neuroprotection: Cerebrolysin^® protects neurons from the damaging effects of lactic acidosis, prevents the formation of free radicals, improves survival and prevents the death of neurons under conditions of hypoxia and ischemia, and reduces the damaging neurotoxic effect of excitatory amino acids (glutamate).

Neurotrophic activity: Cerebrolysin^® is the only nootropic peptidergic drug with proven neurotrophic activity similar to that of natural neuronal growth factors (NGF), but manifested under peripheral administration.

Functional neuromodulation: Cerebrolysin^® has a positive effect on violations of cognitive functions and memorization processes.

Pharmacokinetics

The complexity of the drug’s composition does not allow for the conducting of the usual pharmacokinetic analysis of individual components, since the Cerebrolysin^® active fraction consists of a balanced and stable mixture of biologically active oligopeptides with a total polyfunctional action.

Intended uses

• Alzheimer’s disease, dementia of various genesis;
• chronic cerebrovascular insufficiency;
• ischemic stroke;
• traumatic brain and spinal cord injuries;
• mental retardation in children;
• attention deficit hyperactivity disorder (ADHD) in children;
• complex therapy of endogenous depression resistant to antidepressants.

Contraindications

Hypersensitivity to one of the components of the drug, epilepsy, and severe renal impairment.

Dosage and administration

Intramuscularly (up to 5 ml), intravenously (up to 10 ml), intravenously by slow infusion (10 to 50 ml). Important: inject slowly over 3 minutes!

Dosages and duration of treatment depend on the nature and severity of the disease, as well as on the patient’s age. It is possible to prescribe single dosages up to 50 ml, but still, it is preferable to conduct a course of treatment. The recommended optimal course of treatment is 10–20 days of daily injections.

Acute states (ischemic stroke, traumatic brain injury, complications after neurosurgical operations)
From 10 to 50 ml.

Residual period (cerebral stroke and traumatic damage of the brain and spinal cord)
From 5 to 50 ml.

Psycho-organic syndrome and depression
From 5 to 30 ml.

Alzheimer’s disease, dementia of vascular and combined Alzheimer’s-vascular genesis
From 5 to 30 ml (1 cycle: 5 days weekly/4 weeks (2–4 cycles per year)).

In neuropediatric practice
0.1–0.2 ml/kg.

Treatment courses can be repeated to enhance effectiveness as long as there is an improvement in the patient’s condition due to treatment. After the first course, the periodicity of dosage administration can be reduced to 2 or 3 times a week.

Dosages of 10 to 50 ml are recommended only through slow intravenous infusions after dilution with the proposed standard solutions for infusion (do not mix with balanced amino acid solutions, vitamins, and cardiovascular medicinal products!). The duration of the infusion is 15 to 60 minutes.

Side effects

The side effects of Cerebrolysin^® are rare and of mild intensity.

If the injection is made too fast, in rare cases, there can be a feeling of heat, sweating, dizziness; in some cases, there can be heart palpitations or arrhythmia. Therefore, the drug should be injected slowly.

Rarely: loss of appetite, indigestion, nausea, and allergic reactions.

Very rarely: hyperexcitability, confused state, insomnia, headache, pain in the neck, extremities, and lower back, dyspnea, chills and collaptoid state.

Exceptionally: hyperventilation, arterial hypertension, arterial hypotension, fatigue, tremor, depression, apathy, dizziness, and flu-like symptoms.

It should be noted that some undesirable effects (excitation, arterial hypertension, arterial hypotension, fatigue, tremors, depression, apathy, dizziness, headache, dyspnea, diarrhea, nausea) were detected during clinical trials and occurred in the same way both in patients who received Cerebrolysin^® and in patients of the placebo group.

Overdose

No cases of drug overdose have been reported.

Interaction with other drugs

Given the pharmacological profile of the drug Cerebrolysin^®, special attention should be given to possible additive effects when co-prescribing with antidepressants, including MAOIs. In such cases, it is recommended to reduce the dosage of antidepressant.

Do not mix Cerebrolysin^® and balanced amino acid solutions in a single solution for infusions.

Cerebrolysin^® is incompatible with solutions containing lipids or modifying the pH of the medium (5–8).

Special instructions

The compatibility of the preparation with the following standard infusion solutions was checked and confirmed (for 24 hours at room temperature and with illumination):

• 0.9% solution of sodium chloride (NaCl – 9 mg/ml);
• Ringer’s solution (Na+ – 153.98 mmol/l, Ca2+ – 2.74 mmol/l, K+ – 4.02 mmol/l, Cl- –163.48 mmol/l);
• 5% glucose solution.

It is permissible to use Cerebrolysin^® simultaneously with vitamins and preparations for cardiac circulation improvement, but these preparations should not be mixed in the same syringe with Cerebrolysin^®. Use only a clear solution and only once.

Pregnancy and lactation

The drug may be prescribed with caution in the first trimester of pregnancy and during lactation.

During pregnancy and during breastfeeding Cerebrolysin^® should only be used after a thorough analysis of the impact of the positive effect of the treatment and the risk associated with its administration. The results of experimental studies do not give reasons to believe that Cerebrolysin^® has a teratogenic or a toxic effect on the fetus. However, similar clinical studies in humans have not been conducted.

Influence on the ability to drive vehicles and operate machines

Clinical trials have shown that Cerebrolysin^® does not affect the ability to drive vehicles and operate machines.

Terms of release from pharmacy

On prescription.

Storage conditions

Store at room temperature not exceeding 25°C, do not freeze, protect from light (in the carton). Keep in a safe place out of reach of children.

Shelf life

5 years. Do not use beyond the expiration date printed on the package.

Manufacturer

EVER Pharma, Austria. https://www.everpharma.com/