Citicoline is a nutritional supplement and source of choline and cytidine with potential neuroprotective and nootropic activity. Citicoline, also known as cytidine-5-phosphocholine or CDP-choline, is hydrolyzed into cytidine and choline in the intestine. Following absorption, both cytidine and choline are dispersed, utilized in various biosynthesis pathways, and cross the blood-brain barrier for resynthesis into citicoline in the brain, which is the rate-limiting product in synthesizing phosphatidylcholine. This agent also increases acetylcholine (Ach), norepinephrine (NE), and dopamine levels in the central nervous system (CNS). In addition, citicoline is involved in preserving sphingomyelin and cardiolipin and restoring Na+/K+-ATPase activity. Citicoline also increases glutathione synthesis and glutathione reductase activity and exerts antiapoptotic effects.
Citicoline is a donor of choline in the biosynthesis of choline-containing phosphoglycerides. It has been investigated for the treatment, supportive care, and diagnosis of Mania, Stroke, Hypomania, Cocaine Abuse, and Bipolar Disorder, among others.
CDP-choline is a member of the phosphocholines class, the chlorine ester of CDP. It is an intermediate obtained in the biosynthetic pathway of structural phospholipids in cell membranes. It is a human metabolite, a psychotropic drug, a neuroprotective agent, a Saccharomyces cerevisiae metabolite, and a mouse metabolite. It is a member of phosphocholines and a member of nucleotide-(amino alcohol)s. It derives from a CDP. It is a conjugate base of a CDP-choline(1+).
A nutritional supplement and source of choline and cytidine with potential neuroprotective and nootropic activity.
Mechanism of action
Citicoline is a phospholipid composed of ribose, pyrophosphate, cytosine, and choline. It is water-soluble and highly bioavailable.3 Citicoline is produced endogenously as an intermediate in the production of phosphatidylcholine from choline and is then hydrolyzed in the small intestine to make choline and cytidine available for further biosynthesis.[rx]
Citicoline, also known as cytidine-5-diphosphocholine or CDP-choline, is hydrolyzed into cytidine and choline in the intestine. Following absorption, both cytidine and choline are dispersed, utilized in various biosynthesis pathways, and cross the blood-brain barrier for resynthesis into citicoline in the brain, which is the rate-limiting product in synthesizing phosphatidylcholine. This agent also increases acetylcholine (Ach), norepinephrine (NE) and dopamine levels in the central nervous system (CNS). In addition, citicoline is involved in the preservation of sphingomyelin and cardiolipin and the restoration of Na+/K+-ATPase activity. Citicoline also increases glutathione synthesis and glutathione reductase activity, and exerts antiapoptotic effects.
Supplementation with citicoline increases choline stores available for other biosynthetic pathways. Citicoline appears to decrease glutamate levels in the brain and increase adenosine triphosphate, which in turn offers protection against ischemic neurotoxicity. Increased glucose metabolism in the brain and cerebral blood flow has also been demonstrated, as well as increased availability of the neurotransmitters acetylcholine, norepinephrine, and dopamine.[rx, rx]
Indications
- Drugs are specifically used to facilitate learning or memory, mainly to prevent the cognitive deficits associated with dementias. These drugs act by a variety of mechanisms.
- Citicoline is a donor of choline in the biosynthesis of choline-containing phosphoglycerides. It has been investigated for the treatment, supportive care, and diagnosis of Mania, Stroke, Hypomania, Cocaine Abuse, and Bipolar Disorder, among others.
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- Acute ischemic stroke
Acute ischemic stroke occurs due to blockage of a blood vessel by a clot causing limited blood flow to your brain. If the injectable form of Citicoline is given within 12 hours of having a stroke and then daily for seven days after having a stroke, it can help in a speedy recovery.
- Alzheimer’s disease
Alzheimer’s disease is a condition that occurs due to the destruction of brain cells. It may lead to loss of memory ability to think, communicate or handle daily activities. Citicoline protects your brain cells from damage and also repairs the damaged cells. Therefore, Citicoline is used to improve your brain function in such conditions.
- Cerebral insufficiency
Cerebral insufficiency is a lack of proper blood flow to your brain due to brain injury or blood clots. It can result in memory loss, poor concentration, and lack of orientation. Citicoline is used to prevent further decline in your brain functions.
- Parkinsonism
Parkinson’s disease is a brain disorder that affects movement. It causes muscle weakness, leading to stiffness and shakiness in your hands and legs. It slows down the voluntary indication of your body like sitting, standing, and walking. Citicoline is used with other medicines to improve your condition.
- Acute ischemic stroke
Contraindication
- Data not available
Dosing
- Citicoline is available as an oral form to be taken by mouth and as an injection to be administered into the vein or muscle. Take Citicoline oral forms with or without food. The dose and duration depend on the severity of your health condition.
- Citicoline is water-soluble and highly bioavailable, with minimal drug excreted in the feces.[rx] Citicoline exhibits biphasic plasma peak concentrations at 1 and 24 hours and biphasic elimination.[rx]
- In clinical trials, oral dosages of 250 to 2,000 mg daily have been evaluated in adolescents and adults. Citicoline 100 mg every 12 hours was used in combination with citalopram (20 mg/day for seven days, then 40 mg/day) for six weeks in patients with major depressive disorder.[rx]
Side Effects
The Most common
- Citicoline may cause side effects like stomach discomfort, restlessness, diarrhea, and headache. However, these side effects may subside as your body adjusts to the medicine.
- Headache
- Dizziness
- Shaking of hands or feet
- Sleeplessness
Common
- Irregular heartbeat
- Low blood pressure
- Diarrhoea
- Nausea
- Stomach pain
- Injection site pain
- Blurred vision
Drug Interaction
- Citicoline was well tolerated in clinical trials. Adverse effects may include GI disturbances, transient headaches, hypotension, tachycardia, bradycardia, and restlessness.[rx]
- Citicoline may exacerbate adrenocorticotropic hormone– or cortisol hypersecretion–related disorders, including type 2 diabetes and major depressive disorder.[rx]
Pregnancy and Lactation
FDA Pregnancy Category : D
- Information regarding safety and efficacy in pregnancy and lactation is lacking at dosages above those usually taken nutritionally. The effects of citicoline have been studied in rats during pregnancy for a potential role in the protection of dendrites in the cortex and fetal lung development, as well as in pregnant women in their third trimesters. However, information is limited on the safety of supplemental citicoline.[rx, rx]
References
