Somazina

Citicoline.

Film-coated tablet: Each tablet contains 500 mg of citicoline (as sodium salt).

Pharmacotherapeutic group: Psychostimulants, agents used for Attention-Deficit Hyperactivity Disorder (ADHD) and nootropics. ATC code: N06BX06.
PHARMACOLOGY: Pharmacodynamics: Citicoline stimulates the biosynthesis of structural phospholipids of the neuronal membrane as it is demonstrated in the magnetic resonance spectroscopy studies. Citicoline, through this action, improves the function of the membrane mechanisms, such as the functioning of the ionic exchange pumps and receptors inserted in the latter, the modulation of which is indispensable in the neurotransmission.
Citicoline due to its membrane stabilising activity has properties which favour brain oedema reabsorption.
Experimental studies have shown that Citicoline inhibits the activation of some phospholipases (A1, A2, C and D), reducing the formation of free radicals, avoiding the destruction of membranous systems and preserving antioxidant defence systems as glutathione.
Citicoline preserves the neuronal energetic reserve, inhibits apoptosis and stimulates acetylcholine synthesis.
It has been experimentally shown that Citicoline also exerts a prophylactic neuroprotective effect in focal brain ischemic models.
Clinical trials have shown that Citicoline significantly increases the functional evolution of patients with acute ischemic cerebrovascular accident, coinciding with a lower growth of the brain ischemic injury in neuroimagen tests.
In patients with craniocerebral traumatisms, citicoline speeds up their recuperation and reduces the duration and intensity of the post-concessional syndrome.
Citicoline improves the level of attention and consciousness and acts favourably over amnesia and cognitive and neurological disorders associated to brain ischemia.
Pharmacokinetics: Citicoline is well absorbed after oral, intramuscular or intravenous administration. Plasma choline levels significantly increase after the aforementioned routes. Oral absorption is nearly complete and its bioavailability is approximately the same as the intravenous route. The drug product is metabolized in the intestine and in the liver to choline and cytidine. The administered citicoline is widely distributed in brain structures, with a quick incorporation of the choline fraction in structural phospholipids and the cytidine fraction in cytidinic nucleotides and nucleic acids. Citicoline reaches the brain and it is actively incorporated to cellular, cytoplasmatic and mitochondrial membranes, taking part of the structural phospholipids fraction.
Only a small amount of the dose appears in urine and faeces (less than 3%). Approximately 12% of the dose is eliminated via expired CO₂. In the urinary excretion of the drug, two phases can be distinguished: a first phase, around 36 hours, where the excretion speed rapidly decreases, and a second phase where excretion speed decreases much slower. The same happens with expired CO_2, the elimination speed rapidly decreases after approximately 15 hours and later it decreases much slower.
Toxicology: Preclinical safety data: Oral and intraperitoneal chronic toxicity studies (1.5 g/kg/day during 6 months in dogs) did not show significant abnormalities related with the administration of this drug. Intravenous administration of 300-500 mg/kg/day of citicoline during 3 months in dogs, only produced toxic signs immediately after the injection, such as occasional vomiting, diarrhoea and hyper-salivation.
800 mg/kg of Citicoline was administered to albino rabbits during the organgenesis phase, from 7th to 18th gestation day. The animals were sacrificed the 29th day and a detailed exam of foetus and their mothers were carried out. No toxicity sign were observed neither maternal nor embryo-foetal. The effects over organogenesis were inappreciable, only 10% of the treated foetus has a slight delay in brain osteogenesis.

Film-coated tablet & Oral solution: Stroke, acute phase and its neurological sequelae.
Traumatic brain injury and its neurological sequelae.
Cognitive and behavioural impairment secondary to chronic vascular and degenerative cerebral disorders.
Injection: Cerebrovascular accident in acute & subacute phase. Recent head trauma & their sequelae.

Film-coated tablet: Adults: The recommended dose is from 500 to 2,000 mg/day (1-4 tablets), depending on the severity of the symptoms to be treated.
These doses can be modified according to the criterion of the physician.
Elderly: SOMAZINA does not need any specific dose adjustment for this age group.
Children: The experience in children is limited, therefore it may only be administered when the expected therapeutical benefit is higher than any possible risk.
Oral solution: Adult: 500-2,000 mg daily administered directly or dissolved in ½ glass (120 mL) of water.
Injection: 1,000-2,000 mg daily IM, slow IV inj or infusion (infusion rate: 40-60 drops/min). Can be administered orally.

Film-coated tablet: No case of overdose has been reported.

In case of allergy to Citicoline or any excipient.
It must not be administered to patients with hypertonia of the parasympathetic.

Film-coated tablet: Not applicable.
Oral solution: May cause asthma in patients w/ hypersensitivity to acetylsalicyclic acid. Fructose intolerance.
Injection: In case of persistent intracranial hemorrhage, it is recommended to administer Somazina very slowly at 30 drops/min.
Use in Children: Film-coated tablet: Caution in children.
Use in Pregnancy & Lactation: Film-coated tablet & Oral solution: Caution in pregnancy & lactation.

There are no adequate data from the use of Citicoline in pregnant women.
SOMAZINA should not be used during pregnancy unless clearly necessary. That is, only when the expected therapeutic benefit is higher than any possible risk.

Film-coated tablet: Very rare (<1/10,000) (include individual notifications): Psychiatric disorders: Hallucinations.
Nervous system disorders: Cephalea, vertigo.
Vascular disorders: Arterial hypertension, arterial hypotension.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Gastrointestinal disorders (for Film-coated tablet & Oral solution): Nausea, vomiting, occasional diarrhoea.
Skin and subcutaneous tissue disorders: Blush, hives, exanthemas, purple.
General disorders and administration site conditions: Shiver, oedema.
Injection: Hypotension & parasympathetic effects.

Film-coated tablet & Oral solution: Citicoline potentiates the effects of L-dopa.
It must not be administered in conjunction with medicaments containing Meclofenoxate.
Injection: Do not administer w/ centrophenoxine.

Film-coated tablet: This medicinal product does not require any special storage conditions.

Other CNS Drugs & Agents for ADHD

N06BX06 - citicoline ; Belongs to the class of other psychostimulants and nootropics.

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