Cortexin^® Instruction

International Non-Proprietary Name (INN): none
Dosage form: lyophilisate for preparation of solution for intramuscular injections
Structure:
In 1 vial:
Active substance: Cortexin^® (complex of water-soluble polypeptide fractions): 5 mg in a 3 ml vial, and 10 mg in a 5 ml vial;
Excipients: glycine (stabilizer) – 6 mg in a 3 ml vial and 12 mg in a 5 ml vial.
Description
Lyophilized powder or porous mass of white or white-yellowish color.
Pharmacological classification: nootropics
ATC code: N06BX
Pharmacological action: neuroprotective, nootropic, antioxidant, tissue-specific

List of Contents:

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

Pharmacodynamics

Cortexin contains a complex of low molecular weight water-soluble polypeptide fractions, with a molecular weight of less than 10,000 Da, which penetrate through the blood-brain barrier directly to the nerve cells. The drug has nootropic, neuroprotective, antioxidant and tissue-specific action.

Nootropic – improves higher brain functions, learning and memory processes, concentration, stability under various stress influences.

Neuroprotective – protects neurons from damage by various endogenous neurotoxic factors (glutamate, calcium ions, free radicals), reduces toxic effects of psychotropic substances.

Antioxidant – inhibits lipid peroxidation in neurons, increases neuronal survival under conditions of oxidative stress and hypoxia.

Tissue-specific – activates neuronal metabolism of the central and peripheral nervous system, reparative processes, contributes to the improvement of functions of the brain cortex and the general tone of the nervous system.

The mechanism of action of Cortexin is determined by the activation of peptides of neurons and neurotrophic factors of the brain; optimization of the balance of metabolism of excitatory and inhibitory amino acids, dopamine, and serotonin; GABAergic effects; reduction of paroxysmal seizure brain activity, the ability to improve its bioelectrical activity; prevention of free radical formation (products of lipid peroxidation).

Pharmacokinetics

Cortexin active substance consists of a complex of polypeptide fractions. The complexity of the drug’s composition does not allow to conduct the usual pharmacokinetic analysis of its individual components.

Intended uses

• cerebral circulation disorders;
• encephalopathy of various genesis;
• acute and chronic encephalitis and encephalomyelitis;
• epilepsy;
• traumatic brain injury and its consequences;
• asthenia (suprasegmental autonomic disturbances);
• infantile cerebral palsy;
• psychomotor and speech retardation in children;
• cognitive disorders (dysfunction of memory and ideation);
• reduced learning ability.

Contraindications

Individual intolerance, pregnancy and lactation (lack of data).

Dosage and administration

The drug goes in packs containing 10 vials. There are two forms of release: 

1. Vials containing 5 mg of the active ingredient (neuropeptides) – for children.
2. Vials containing 10 mg of the active ingredient (neuropeptides) – for adults. 

Before injection dissolve the content of the vial in 1-2 ml of water for injection, 0.5% procaine (novocaine) solution or 0.9% sodium chloride solution.

The route of administration of the drug is intramuscular (IM). 

The medicine is used in the following dosages: 

• Adults – 10 mg once a day for 10 days. The course can be repeated in 3-6 months.
• Adults in the acute and early recovery periods of stroke – 10 mg twice a day (in the morning and afternoon) for 10 days, the course is repeated after 10 days.
• Children whose weight is less than 20 kg – 0.5 mg / kg once a day for 10 days. The course can be repeated in 3-6 months.
• Children whose weight is more than 20 kg – 10 mg once a day for 10 days. The course can be repeated in 3-6 months.

How to prepare the mixture correctly?

1. With a sterile syringe, draw up 1-2 ml of water for injection, saline, or local anesthetic. By injecting the mixture diluted with local anesthetic, the injection will be less painful. But in this case, the risk of developing undesired allergic reactions is higher.
2. Remove the foil from the Cortexin bottle and insert the needle through the stopper. It is recommended to lower it to the middle of the bottle and lean against the wall to reduce foaming. Then slowly push the plunger until the contents of the syringe are inside.
3. Without removing the needle, shake the bottle with the mixture until all the powder is dissolved.
4. Pull the plunger towards you until the contents of the vial are inside the syringe.

It is also recommended to prepare the solution right before an injection.

How to inject Cortexin correctly?

All manipulations are carried out in gloves.

First, you need to choose the site where the injection will be made:

• Hip,
• Deltoid,
• Femoral, front thigh.

It is preferable to choose the gluteal region. The buttock is mentally divided into four squares. The injection is placed in the upper outer square. It is better to alternate the injection sites. For example if yesterday you made an injection in the right buttock, today – do it in the left one.

1. Before injection, treat the selected site with a cotton swab dipped in medical alcohol. Wipe in a circular motion from center to periphery.
2. Before starting the procedure, tap the syringe slightly, lifting it with the needle up. Then press the plunger until all the air is out of the syringe.
3. Stretch the skin at the site of the intended injection with your hand. Take the syringe in another hand, lift it up a little and sharply insert the needle at 2/3 of its length. During injection, insert the needle perpendicular to the surface of the body.
4. The injection should be quick, because if you insert the needle slowly, it will be more painful.
5. Then press down on the plunger to slowly get the medicine into the muscle. The optimal injection rate is 1 ml in 10 seconds.
6. After that, quickly remove the needle and put the cap on it. Only in this form can the syringe be thrown away.
7. It is recommended to massage the injection site so that the drug is better absorbed into the tissue. Re-treat the area into which the injection was made with a cotton swab dipped in an alcohol solution. This is done in order to prevent infection.

The medicine is best taken before lunch, like any nootropic drugs.

Cortexin begins to take effect only a few days after the start of use, so you should not stop injections if you do not see a quick result.

Side effects

The following adverse reactions reported during clinical use, are listed below according to the system-organ classification, in descending order of occurrence: Very common (≥1/10), common (≥1/100, but <1/10), infrequent (≥1/1,000 but <1/100), rare (≥1/10,000 but <1/1,000), very rare (<1/10,000).

(Very rare) Immune system disorders: laryngeal angioneurotic edema, skin rash, skin itching, skin hyperemia (incl. in the place of injection).
(Very rare) Nervous system disorders: psychomotor agitation, motor dysfunction, insomnia.
(Very rare) Cardiac disorders: tachycardia (increased heart rate).
(Very rare) Mental disorders: apprehension.

Overdose

No cases of the drug overdose have been reported.

Interaction with other drugs

No data.

Special instructions

Consult with your doctor before use.

When using 0.5% procaine (novocaine) solution as a solvent for Cortexin, please adhere to the information on contraindications, precautions and age restrictions described in the drug sheet of procaine (novocaine).

The use of the local anesthetic Lidocaine as a solvent for preparing a solution of Cortexin is not recommended.

Do not store/use after storage the dissolved preparation. It is not recommended to mix Cortexin with other solutions.

In case you have missed an injection, it is not recommended to administer a double dose, the course shall be continued as prescribed.

Pregnancy and lactation

There have been no records of undesirable effects when using Cortexin during pregnancy or lactation. However, since the data from clinical trials are insufficient to establish the safety of the drug during these time intervals, these groups of patients are not recommended to use the drug. If it is necessary to prescribe the drug during lactation, breastfeeding shall be discontinued.

Influence on the ability to drive vehicles and operate machines

In case of psychomotor agitation (see “Side Effects”) Cortexin may affect the ability to drive vehicles and operate machines or perform potentially hazardous activities that require special attention and quick reactions.

Storage conditions

Store in a dry dark place at temperatures no higher than 25°C (77°F). Keep in a safe place out of reach of children.

Shelf life

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

Manufacturer

Geropharm, Russia. https://geropharm.com/