Cerebrolysin

Cerebrolysin

Manufacturer:

Ever Pharma

Distributor:

Globo Asiatico
Full Prescribing Info
Contents
Neuropeptide.
Description
Each ml contains: 215.2 mg of porcine brain-derived peptide preparation (Cerebrolysin concentrate) in aqueous solution.
Excipients/Inactive Ingredients: Sodium hydroxide and water for injections.
Action
Pharmacology: Pharmacodynamics: The porcine brain-derived proteolytic peptide fraction stimulates cell differentiation, bolsters nerve cell function, and induces mechanisms of protection and repair. In animal experiments, Cerebrolysin directly influences neuronal and synaptic plasticity, thus improving learning. This has been shown in young, adult, and aged animals with reduced cognitive abilities. In models of cerebral ischaemia, Cerebrolysin reduced the infarct volume, inhibited oedema formation, stabilized microcirculation, doubled the survival rate, and normalised lesion-related neurological failure and learning deficits. Positive results were also obtained using models of Alzheimer’s disease. In addition to its direct effects on neurons, Cerebrolysin appears to significantly increase the number of glucose transport molecules in the blood-brain barrier, thereby balancing out the critical energy deficit associated with this disease.
Quantitative EEG studies of healthy volunteers and patients suffering from vascular dementia have shown dose-dependent acute effects of elevated neuronal activity (increase in alpha and beta frequencies) after 4 weeks of treatment. Regardless of the cause of the disease, be it neurodegenerative dementia of Alzheimer’s type or vascular dementia, Cerebrolysin therapy results in improvements in the objective cognitive abilities and in the activities of daily living. After only two weeks, there are improvements in the clinical global impression, which increase with continuation of the therapy. Also independent of the type of dementia, approximately 60–70 % of patients respond positively to Cerebrolysin therapy. In the case of senile dementia of Alzheimer's type, the improved clinical state of the patient is maintained after the end of active treatment. In particular, the activities of daily living are improved and stabilised over the long term, which in general leads to a reduced need for patient care and supervision. On the basis of its neurotrophic (nerve growth factor-like) activity, Cerebrolysin can achieve a significant reduction, or in some cases even the cessation of progression, of neurodegenerative processes.
Pharmacokinetics: The porcine brain-derived proteolytic peptide fraction consists of short biological peptides similar or identical to those produced endogenously. Direct measurement of pharmacokinetic properties has not been performed successfully. Indirect pharmacokinetic data have been established on the basis of Cerebrolysin's pharmacodynamic profile. The neurotrophic activity of Cerebrolysin can be detected in blood plasma up to 24h after a single application. Furthermore, components of the drug can cross the blood-brain barrier. Preclinical in vivo experiments revealed identical pharmacodynamic actions on the central nervous system following intra-cerebroventricular or peripheral application. Thus, indirect evidence for the passage of components of the drug across the blood-brain barrier has been established.
Toxicology: Preclinical Safety Data: Acute Toxicity/LD50: Rat male 68 ml/kg BW IV, rat female 74 ml/kg BW IV, dog male/female >52.2 ml/kg BW IV.
Chronic Toxicity: Rat: Above 5 mL/kg body weight/day for 26 weeks: Moderate changes in blood counts.
Dog: The highest applied dose of 9 mL/kg body weight/day for 28 days (corresponding to approximately 10 times the human therapeutic dose) and the highest applied dose of 4.5 mL/kg body weight/day (corresponding to approximately 5 times the human therapeutic dose) for 26 weeks showed no substance-related systemic intolerability.
Reproductive Toxicity: Intravenous administration of Cerebrolysin at doses toxic to the mother, or of the highest possible volume, showed no evidence of teratogenic effects in any phase of reproduction in rats or rabbits, no influence on fertility, breeding capacity, posterity, and no embryotoxic or fetotoxic effects.
Sensitizing Potential: Larger molecular weight peptides with antigenic potential are excluded from the infusion solution during the manufacturing and quality control processes.
No influence on the immune system has been detected during testing. Tests revealed that Cerebrolysin does not result in the formation of antibodies or in cutaneous anaphylaxis. Cerebrolysin shows no histamine-stimulating potential and no hemagglutinating effects.
Carcinogenicity: None of the studies of chronic toxicity or clinical experience have given any indication of carcinogenic effects.
Mutagenicity: Cerebrolysin has shown no genotoxic or mutagenic potential, in vitro or in vivo.
Indications/Uses
Patients with acute ischemic stroke, dementia and traumatic brain injury.
Dosage/Direction for Use
Single doses of up to 50 mL can be administered, but a course of therapy is the preferred option.
A recommended optimum course of therapy comprises daily application over a total of 10-20 days.
Recommended Dose: Adults: Organic Brain Disorders, Metabolic Disorders and Neurodegenerative Diseases (Dementia): 5-30 mL daily.
Postapoplectic Complications and Craniocerebral Trauma: 10-50 mL daily.
Children: 1-2 mL daily.
The effectiveness of therapy can be increased by repeated courses, until no further benefit results. After the initial course, the frequency of doses may be reduced to 2 or 3 times/week. A treatment-free period, equal in length to the therapy course, should be allowed between successive therapy courses.
Doses of up to 5 ml IM and up to 10 ml undiluted IV may be given. Doses between 10ml up to a maximum of 50ml are recommended only as a slow intravenous infusion after dilution with the suggested standard infusion solutions. The duration of the infusion should be between 15 and 60 mins.
The compatibility over 24 hours at room temperature in the presence of light has been tested with the following standard infusion solutions: 0.9% sodium chloride solution (9 mg NaCl/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 Vitamins and cardiovascular drugs may be given concomitantly with Cerebrolysin but the drugs should not be mixed with Cerebrolysin in the syringe.
Direction for Dilution: 5 to 30 mL Cerebrolysin should be diluted up to 50 mL of 0.9% NaCl, Lactated Ringer's Solution or 5% Dextrose.
Higher volume of Cerebrolysin up to 50 mL should be diluted with 50 mL of 0.9% NaCl, Lactated Ringer's Solution or 5% Dextrose. Not to administer the solution undiluted for concentrated solution. For Single Use Only.
Overdosage
There are no known instances of health-related negative effects due to overdose or intoxication.
Contraindications
Hypersensitivity to one of the components of Cerebrolysin. Epilepsy. Severe renal impairment.
Special Precautions
Special care is indicated in cases of Allergic diathesis, epileptic conditions and grand mal convulsions; Cerebrolysin treatment may result in an increase in the frequency of seizures.
Although there are no data indicating that Cerebrolysin causes renal stress, the product should not be administered in the presence of existing severe renal failure.
Effects on the Ability to Drive or Operate Machinery: Clinical tests of Cerebrolysin have shown no effects on the ability to drive a car or operate machinery.
Use in Pregnancy & Lactation: Animal studies did not show any indication of reproductive toxicity. However, no data are available for humans. Therefore, during pregnancy and lactation, Cerebrolysin should only be used after careful risk/benefit considerations.
Use In Pregnancy & Lactation
Animal studies did not show any indication of reproductive toxicity. However, no data are available for humans. Therefore, during pregnancy and lactation, Cerebrolysin should only be used after careful risk/benefit considerations.
Adverse Reactions
In rare cases, the desired activating effects have also been associated with agitation (aggression, confusion, insomnia).
In one study, rare cases of hyperventilation, hypertension, hypotension, tiredness, tremor, depression, apathy, dizziness and symptoms of influenza (eg, cold, cough, respiratory tract infections) were reported.
Single cases of grand mal attacks and convulsions have been reported after administration of Cerebrolysin.
In rare cases, gastrointestinal disturbances eg, loss of appetite, dyspepsia, diarrhea, constipation, vomiting and nausea, have been observed.
If injected too quickly, feelings of heat or sweating, dizziness, and in isolated instances, palpitations or arrhythmias may result.
Injection site reactions such as erythema, pruritus and burning have been reported.
In very rare cases, hypersensitivity or allergic reactions such as skin reactions, local inflammatory reactions, headache, neck and limb pain, fever, low back pain, dyspnoea, chills and shock-like state have been observed.
As Cerebrolysin is used in the elderly, and the above mentioned undesirable effects are typical of this patient population, they may also be observed without drug use.
Drug Interactions
On the basis of Cerebrolysin's pharmacological profile, special attention should be given to possible additive effects when used in conjunction with antidepressants or MAO inhibitors. In such cases, it is recommended that the dose of the antidepressant is lowered.
Cerebrolysin should not be mixed with balanced amino acid solutions in an infusion.
Caution For Usage
Instructions for Use and Handling: When Cerebrolysin is administered via a long-term intravenous catheter, the catheter has to be rinsed before and after the application with physiological sodium chloride solution.
For single use only.
Incompatibilities: Cerebrolysin is incompatible with solutions which change the pH (5.0-8.0) and with lipid-containing solutions.
Storage
Cerebrolysin must be stored at room temperature not exceeding 25°C and protect from light. Do not freeze.
Remove the solution from the vials/ampoules immediately before use.
Shelf-Life: Ampoules: 4 years.
MIMS Class
Nootropics & Neurotonics/Neurotrophics
ATC Classification
C04A - PERIPHERAL VASODILATORS ; Used as peripheral vasodilators.
Presentation/Packing
Infusion 215.2 mg/mL x 10 mL x 5's.
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