Citimax-darnitsa®
Ukraine
Table of Contents
INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT CYTIMAX-DARNITSA® (CITIMAX-DARNITSA)
Composition:
Active substance: citicoline;
1 ml of solution contains 10 mg of citicoline sodium, calculated as citicoline;
Excipients: sodium chloride, water for injections.
Pharmaceutical form. Infusion solution.
Main physicochemical properties: clear, colorless liquid.
Pharmacotherapeutic group. Psychostimulants, drugs used in attention deficit hyperactivity disorder (ADHD), nootropic agents. Other psychostimulant and nootropic agents. ATC code N06BX06.
Pharmacological Properties
Pharmacodynamics
Citicoline stimulates the biosynthesis of structural phospholipids in neuronal membranes, as confirmed by magnetic resonance spectroscopy data. Due to this mechanism of action, citicoline improves the function of membrane mechanisms such as ion-exchange pumps and receptors, the modulation of which is necessary for normal nerve impulse conduction.
Thanks to its membrane-stabilizing effect, citicoline exhibits anti-edematous properties that contribute to a reduction in cerebral edema.
Experimental studies have shown that citicoline inhibits the activation of certain phospholipases (A1, A2, C, and D), reduces the formation of free radicals, prevents the destruction of membrane systems, and preserves antioxidant defense systems such as glutathione.
Citicoline maintains neuronal energy reserves, inhibits apoptosis, and stimulates acetylcholine synthesis.
Experimental evidence has demonstrated that citicoline also exerts a preventive neuroprotective effect in focal cerebral ischemia.
Clinical studies have shown that citicoline significantly enhances functional recovery in patients with acute ischemic stroke, which correlates with a slowed progression of ischemic brain damage as observed in neuroimaging.
In patients with traumatic brain injury, citicoline accelerates recovery and reduces the duration and severity of post-traumatic syndrome.
Citicoline increases levels of attention and consciousness, reduces cognitive and neurological deficits associated with cerebral ischemia, and helps alleviate symptoms of amnesia.
Pharmacokinetics
After administration, a significant increase in plasma choline levels is observed. The drug is metabolized in the intestine and liver, forming choline and cytidine.
Following administration, citicoline is widely distributed into brain structures, with rapid incorporation of the choline fraction into structural phospholipids and the cytidine fraction into cytidine nucleotides and nucleic acids. In the brain, citicoline integrates into cellular, cytoplasmic, and mitochondrial membranes, becoming part of the phospholipid fraction.
Only a negligible amount of the dose is found in urine and feces (less than 3%). Approximately 12% of the dose is excreted as exhaled CO₂. During excretion in urine, two phases are observed: the first phase lasts 36 hours, during which the elimination rate decreases rapidly, and the second phase, in which the elimination rate decreases much more slowly. The same biphasic pattern is observed in excretion via the respiratory tract. The rate of CO₂ elimination decreases rapidly, approximately within 15 hours, and then declines much more slowly.
Clinical characteristics.
Indications.
- Stroke, acute phase of cerebral circulation disorders and treatment of complications and consequences of cerebral circulation disorders.
- Traumatic brain injury and its neurological consequences.
- Cognitive disorders and behavioral disturbances due to chronic cerebrovascular and degenerative cerebral disorders.
Contraindications.
- Hypersensitivity to citicoline or to other components of the medicinal product.
- Increased tone of the parasympathetic nervous system.
Interaction with other medicinal products and other forms of interaction.
Citicoline enhances the effect of levodopa. The medicinal product Citimax-Darnytsia**®** should not be administered simultaneously with medicinal products containing meclofenoxate.
Special precautions for use.
The infusion rate should be 40–60 drops per minute.
In cases of persistent intracranial hemorrhage, the dose should not exceed 1000 mg per day and the intravenous infusion rate should not exceed 30 drops per minute.
This medicinal product contains less than 1 mmol (23 mg)/dose of sodium, i.e. it is practically sodium-free.
Use during pregnancy or breastfeeding.
Adequate data on the use of citicoline in pregnant women are lacking. Data regarding excretion of citicoline in breast milk and its effects on the fetus are unknown.
During pregnancy or breastfeeding, this medicinal product should be administered only if the expected therapeutic benefit to the mother outweighs the potential risk to the fetus.
Ability to affect reaction speed when driving or operating machinery.
In individual cases, certain adverse reactions affecting the central nervous system may impair the ability to drive or operate complex machinery.
Method of Administration and Dosage
The recommended dose for adults is from 500 mg to 2000 mg per day depending on the severity of symptoms.
The medicinal product should be prescribed and administered intravenously by drip infusion at a rate of 40–60 drops per minute.
Maximum daily dose — 2000 mg.
Duration of treatment depends on the course of the disease and is determined by the physician.
Elderly patients do not require dose adjustment.
After stabilization of the patient's condition, a switch to oral administration of the medicinal product is possible.
Method of Administration
Do not insert the needle(s) into areas of the polymer vial not intended for this purpose, but only into sterile ports!
For infusion therapy, the following procedure should be followed:
- Remove the protective plastic cap with tamper-evident feature (if present).
- Tear off protective valve(s) No. 1 as shown in Figures 1 and 2 (the manufacturer may use different types and materials for protective valves).
- Remove the cap from the needle and insert it into any of the special ports No. 2 of the vial containing the infusion medicinal product (see Figures 1 and 2).
- The other sterile port may be used either for introducing other medicinal products into the infusion vial (No. 4, see Figure 3) or, if the flow rate is insufficient, for a venting needle (No. 4, see Figure 3).
- Hang the vial with solution using the special ring No. 3 located at the bottom of the vial (see Figure 3).
Children
Experience with the use of the medicinal product in children is limited.
Overdose
Due to the low toxicity of Citimax-Darnitsa**®**, intoxication is not expected, even if therapeutic doses have been accidentally exceeded.
In case of accidental overdose, symptomatic treatment should be administered.
Side effects.
Side effects occur very rarely (< 1/10,000), including isolated cases.
Respiratory, thoracic and mediastinal disorders: dyspnea.
Gastrointestinal disorders: nausea, vomiting, diarrhea.
Nervous system disorders: severe headache, vertigo.
Psychiatric disorders: hallucinations.
Cardiovascular disorders: arterial hypertension, arterial hypotension, tachycardia.
Skin and subcutaneous tissue disorders: rash, hyperemia, exanthema, purpura.
General disorders and administration site reactions: chills, edema.
Reporting of suspected side effects.
Reporting of suspected side effects after marketing authorization of the medicinal product is important. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and/or lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua
Shelf life. 2 years.
Storage conditions.
Store in the original packaging at a temperature not exceeding 25 °C. Do not freeze.
Keep out of reach of children.
Packaging.
100 ml in a vial; 1 vial in a carton.
Prescription status. Prescription only.
Manufacturer. JSC "Pharmaceutical company "Darnytsia".
Manufacturer's address and location of its business activity.
13, Borysplilska Street, Kyiv, 02093, Ukraine.