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Indications/Uses
Cerebrovascular Diseases (eg, From Ischemia Due to Stroke): Citicoline accelerates the recovery of consciousness and overcoming motor deficit. The clinical testing of citicoline has challenged the historical concept that one can do nothing for a stroke patient after a certain period of time has transpired after the onset of symptoms. The practicality of a drug that can be administered up to 24 hrs after stroke is a key factor in evaluating the potential of citicoline.
The potential of citicoline as stroke therapy is underscored by other key attributes: Its oral dosage for a 24-hr window of therapeutic opportunity following stroke and an apparent absence of significant side effects. Preliminary evidence suggests that in a small subgroup of patients, citicoline may reduce the size of the impact caused by stroke.
Treatment of citicoline within the first 24 hrs after onset in patients with moderate to severe stroke increase the probability of complete recovery in 3 months.
Head Trauma of Varying Severity: In a clinical trial, citicoline accelerated the recovery from posttraumatic coma and the recuperation of walking ability, achieved a better final functional result and reduced hospital stay.
Cognitive Disorders of Diverse Etiology [eg, Senile Cognitive Impairment which is Secondary to Degenerative Diseases (eg, Alzheimer's Disease) and to Chronic Cerebral Vascular Disease]: Citicoline improves scores on cognitive evaluation scales and slowed the progression of Alzheimer's disease.
Parkinson's Disease: Citicoline has also been shown to be effective as co-therapy for Parkinson's disease. Beneficial neuroendocrine, neuroimmunomodulatory and neurophysiological effects have been described. Considerable experimental evidence of effects of citicoline on CNS dopaminergic system has accumulated. After treatment with citicoline, regeneration of cells in rats with substantia nigra lesions has been demonstrated. Citicoline increases striatal dopamine and tyrosine hydroxylase synthesis.
The potential of citicoline as stroke therapy is underscored by other key attributes: Its oral dosage for a 24-hr window of therapeutic opportunity following stroke and an apparent absence of significant side effects. Preliminary evidence suggests that in a small subgroup of patients, citicoline may reduce the size of the impact caused by stroke.
Treatment of citicoline within the first 24 hrs after onset in patients with moderate to severe stroke increase the probability of complete recovery in 3 months.
Head Trauma of Varying Severity: In a clinical trial, citicoline accelerated the recovery from posttraumatic coma and the recuperation of walking ability, achieved a better final functional result and reduced hospital stay.
Cognitive Disorders of Diverse Etiology [eg, Senile Cognitive Impairment which is Secondary to Degenerative Diseases (eg, Alzheimer's Disease) and to Chronic Cerebral Vascular Disease]: Citicoline improves scores on cognitive evaluation scales and slowed the progression of Alzheimer's disease.
Parkinson's Disease: Citicoline has also been shown to be effective as co-therapy for Parkinson's disease. Beneficial neuroendocrine, neuroimmunomodulatory and neurophysiological effects have been described. Considerable experimental evidence of effects of citicoline on CNS dopaminergic system has accumulated. After treatment with citicoline, regeneration of cells in rats with substantia nigra lesions has been demonstrated. Citicoline increases striatal dopamine and tyrosine hydroxylase synthesis.
Dosage/Direction for Use
Capsule: 1 cap once or twice daily. Adult Oral Drops: 1-2 mL twice or thrice daily.
Administration
May be taken with or without food.
Contraindications
Patients with hypertonia of the parasympathetic.
Special Precautions
In case of persistent intracranial hemorrhage, the very slow administration (30 drops/min) is recommended, the administration of larger doses could provoke an increase of the cerebral blood flow.
Use in pregnancy & lactation: There is inadequate evidence of safe use of Zynapse in human pregnancy. Zynapse should be used in pregnancy and lactation only if the potential benefits justify the potential risks.
Use in pregnancy & lactation: There is inadequate evidence of safe use of Zynapse in human pregnancy. Zynapse should be used in pregnancy and lactation only if the potential benefits justify the potential risks.
Adverse Reactions
Occasionally, citicoline may exert a stimulating action of the parasympathetic, as well as a fleeting and discrete hypotensor effect.
Drug Interactions
Zynapse potentiates the effects of L-dopa.
Incompatibilities: Zynapse must not be administered in conjunction with medicaments containing meclofenoxate (also known as clophenoxate).
Incompatibilities: Zynapse must not be administered in conjunction with medicaments containing meclofenoxate (also known as clophenoxate).
Storage
Store below 25°C.
Action
Pharmacology: Citicoline, a naturally occurring endogenous nucleoside, is an intermediate compound in the major pathway for the biosynthesis of the structural phospholipids of cell membranes, including neurons.
Citicoline activates the biosynthesis of structural phospholipids in the neuronal membrane, increases cerebral metabolism and the level of various neurotransmitters, including acetylcholine and dopamine. Citicoline has shown neuroprotective effects in situations of hypoxia and ischemia, as well as improved learning and memory performance in animal models of brain aging. Furthermore, it has been demonstrated that citicoline restores the activity of mitochondrial ATPase and of membranal Na+/K+ ATPase, inhibits the activation of phospholipase A2 and accelerates the reabsorption of cerebral edema in various experimental models.
Pharmacodynamics: When administered orally, it is absorbed almost completely and its bioavailability is approximately the same when administered IV.
Once absorbed, cytidine and choline disperse widely throughout the body, cross the blood-brain barrier and reach the central nervous system (CNS), where they are incorporated into the phospholipid fraction of the cellular membrane and microsomes.
The concept that administration of exogenous citicoline can augment the synthesis of neural membrane phospholipid is attractive, because accelerated replacement or repair plays a critical role in maintaining the healthy function of numerous physiological processes. It has shown therapeutic efficacy in a variety of diseases in which membrane disorder, dysfunction or degeneration result in cellular and tissue ischemia and necrosis.
Citicoline activates the biosynthesis of structural phospholipids in the neuronal membrane, increases cerebral metabolism and the level of various neurotransmitters, including acetylcholine and dopamine. Citicoline has shown neuroprotective effects in situations of hypoxia and ischemia, as well as improved learning and memory performance in animal models of brain aging. Furthermore, it has been demonstrated that citicoline restores the activity of mitochondrial ATPase and of membranal Na+/K+ ATPase, inhibits the activation of phospholipase A2 and accelerates the reabsorption of cerebral edema in various experimental models.
Pharmacodynamics: When administered orally, it is absorbed almost completely and its bioavailability is approximately the same when administered IV.
Once absorbed, cytidine and choline disperse widely throughout the body, cross the blood-brain barrier and reach the central nervous system (CNS), where they are incorporated into the phospholipid fraction of the cellular membrane and microsomes.
The concept that administration of exogenous citicoline can augment the synthesis of neural membrane phospholipid is attractive, because accelerated replacement or repair plays a critical role in maintaining the healthy function of numerous physiological processes. It has shown therapeutic efficacy in a variety of diseases in which membrane disorder, dysfunction or degeneration result in cellular and tissue ischemia and necrosis.
MedsGo Class
Other CNS Drugs & Agents for ADHD / Peripheral Vasodilators & Cerebral Activators
Features
Brand
Zynapse
Full Details
Dosage Strength
1g
Drug Ingredients
- Citicoline
Drug Packaging
Tablet 1's
Generic Name
Citicoline
Dosage Form
Tablet
Registration Number
DR-XY34865
Drug Classification
Prescription Drug (RX)