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Alpha-GPC
(L-alpha glycerylphosphorylcholine, Choline alfoscerate)


 General Info  

Active Forms
Chemically, alpha-GPC is known as L-Alpha Glycerylphosphorylcholine.

Absorption
Studies report that alpha-GPC is well absorbed in the intestinal mucosa after oral ingestion.(1)

Dietary Sources
Small amounts of alpha-GPC are present in cow's milk and the brassica vegetables, which include cabbage, cauliflower, and Brussels sprouts. Mother's milk contains substantial amounts of alpha-GPC.

 Dosage Info
Dosage Range
200 mg to 1,500 mg daily.

Most Common Dosage
400 mg, 3 times daily.

Dosage Forms
Tablets, capsules, powder, and intravenous.
Adult RDI
None established

Adult ODA
None established

 
 Overview
Alpha-GPC, which is also known as L-alpha glycerylphosphorylcholine and choline alfoscerate, is an intermediate in phospholipid metabolism that naturally occurs in humans. Structurally, it is made up of choline, glycerol, and phosphate. It is a primary storage form of choline and occurs in cells throughout the human body. In addition to being a recognized source of choline, it can stimulate the synthesis of phosphatidylcholine and the neurotransmitter acetylcholine. Numerous studies report that its ability to increase the synthesis and release of acetylcholine make it a promising candidate as a cognitive enhancing agent in the treatment of the elderly as well as patients with senility and Alzheimer's disease.

Alpha-GPC is a product of catabolic phospholipid degradation as well as a precursor for the production of phospholipids. Thus, alpha-GPC plays a key role in both the synthesis and the catabolic recycling of phospholipids.

Alpha-GPC has also been shown to be a natural human growth hormone (hGH) secretagogue. Studies report that it increases growth hormone releasing hormone (GHRH)-induced secretion of human growth hormone (hGH) in both normal elderly and young subjects as well as in elderly patients with dementia and Alzheimer's disease.

Because alpha-GPC influences phospholipid metabolism, the production of acetylcholine, and human growth hormone secretion, researchers are suggesting that it may be therapeutically useful in a wide range of conditions related to aging, long-term stress, chronic or acute disease states, and various anti-aging applications.

 Toxicities & Precautions

Studies report that alpha-GPC is well absorbed in the intestinal mucosa after oral ingestion.(1)

General
No serious side effects or toxicities have been reported with alpha-GPC.

Side Effects
Approximately 1% of patients taking orally administered alpha-GPC experience side effects such as heartburn, nausea and vomiting, insomnia, restlessness, and headache.(2) These problems are almost always considered mild and usually resolve by lowering the dosage or discontinuing the product.

 Functions in the Body
Uses
Clinical Applications

Alzheimer's Disease

Cerebral Ischemic Attacks

Cognitive Enhancement

Dementia

Head Injuries

Acetylcholine
Alpha-GPC is a precursor of acetylcholine and administration of alpha-GPC has been shown to increase the synthesis and release of acetylcholine from the hippocampus.(3)

Choline
Alpha-GPC is a source of choline, which can be used in the body for the production of phosphatidylcholine and acetylcholine.(4)

GABAnergic neuronal system
There is some indication that alpha-GPC may also play a role in the activation of the GABAnergic neuronal system. In animal studies, administration of alpha-GPC caused increased GABA release.(5)

Human growth hormone
Administration of alpha-GPC results in small increases in human growth hormone (hGH) and a potentiation of the effects of growth hormone releasing hormone (GHRH) in both young and elderly individuals, with effects in the elderly being more pronounced.(6, 7)


 Clinical Applications
Alzheimer's Disease
65 patients believed to be suffering from Alzheimer's disease were administered 1,200 mg of alpha-GPC orally for 6 months. Their progress was compared to 61 patients who where administered 1,500 of acetyl-L-carnitine daily. Patients taking alpha-GPC achieved greater improvements, especially in neuropsychological measurements.(8) In a larger study involving 261 participants, those who received 400 mg alpha-GPC showed greater improvement in Alzheimer's symptoms than the control group.(9)
Cerebral Ischemic Attacks
In a multicenter, 6-month trial, 2,058 patients who were recovering from ischemic attacks were treated with alpha-GPC. The patients received 1,000 mg intramuscularly for the first 28 days and then 1,200 mg orally each day thereafter. Nearly 70% of the investigators reported “very good” or “good” results in the first phase of the trial (28 days i.v.) and 77.6% of investigators reported “very good” or good” efficacy during the 5 months of oral therapy with minimal side effects.(10)
Cognitive Enhancement
The results of studies in animals(11) and humans(12) indicate that alpha-GPC improves memory and cognitive performance. Also, in healthy young volunteers, alpha-GPC was successful at improving the memory and attention deficits after administration of scopalamine.(13)
Dementia
Several studies report that patients with primary degenerative dementia (PDD) and multi-infarct dementia (MID) taking alpha-GPC make significant improvements on numerous psychometric tests. In some cases the improvements were still present 90 days after cessation of the trial.(14, 15, 16) In other studies, patients with senile organic brain syndrome or mild cognitive deficit of vascular origin gained measurable clinical and neuropsychological improvements when treated with alpha-GPC.(17, 18, 19)
Head Injuries
Comatose patients given intravenous alpha-GPC within 3 to 14 days of receiving a head injury made much faster progress than control patients. Patients receiving alpha-GPC were comatose for shorter periods of time, had fewer speech problems, and had faster improvements in neurological symptoms.(20)
 Symptoms & Causes of Deficiency
Alpha-GPC is not an essential nutrient for humans and a deficiency condition has not been identified.
 Footnotes
1 Abbiati G, Fossati T, Lachmann G, et al. Absorption, tissue distribution and excretion of radiolabelled compounds in rats after administration of [14C]-L-alpha-glycerylphosphorylcholine. Eur J Drug Metab Pharmacokinet. Apr1993;18(2):173-80.
View Abstract
2 Barbagallo Sangiorgi G, Barbagallo M, Giordano M, et al. alpha-Glycerophosphocholine in the mental recovery of cerebral ischemic attacks. An Italian multicenter clinical trial. Ann N Y Acad Sci. Jun1994;717:253-69.
View Abstract
3 Sigala S, Imperato A, Rizzonelli P, et al. L-alpha-glycerylphosphorylcholine antagonizes scopolamine-induced amnesia and enhances hippocampal cholinergic transmission in the rat. Eur J Pharmacol. Feb1992;211(3):351-8.
View Abstract
4 Gatti G, Barzaghi N, Acuto G, et al. A comparative study of free plasma choline levels following intramuscular administration of L-alpha-glycerylphosphorylcholine and citicoline in normal volunteers. Int J Clin Pharmacol Ther Toxicol. Sep1992;30(9):331-5.
View Abstract
5 Ferraro L, Tanganelli S, Marani L, et al. Evidence for an in vivo and in vitro modulation of endogenous cortical GABA release by alpha-glycerylphosphorylcholine. Neurochem Res. May1996;21(5):547-52.
View Abstract
6 Ceda GP, Ceresini G, Denti L, et al. alpha-Glycerylphosphorylcholine administration increases the GH responses to GHRH of young and elderly subjects. Horm Metab Res. Mar1992;24(3):119-21.
View Abstract
7 Ceda GP, et al. GH responses to GHRH in old subjects and in patients with senile dementia of the Alzheimer's type:the effects of an acetylcholine precursor. Advances in the Biosciences. 1993;87:425-428.
8 Parnetti L, Abate G, Bartorelli L, Cucinotta D, et al. Multicentre study of l-alpha-glyceryl-phosphorylcholine vs ST200 among patients with probable senile dementia of Alzheimer's type. Drugs & Aging. Mar1993;3(2):159-64.
View Abstract
9 De Jesus Moreno Moreno M. Cognitive improvement in mild to moderate Alzheimer's dementia after treatment with the acetylcholine precursor choline alfoscerate: a multicenter, double-blind, randomized, placebo-controlled trial. Clin Ther. 2003 Jan;25(1):178-93.
View Abstract
10 Barbagallo Sangiorgi G, Barbagallo M, Giordano M, et al. alpha-Glycerophosphocholine in the mental recovery of cerebral ischemic attacks. An Italian multicenter clinical trial. Ann N Y Acad Sci. Jun1994;30;717:253-69.
View Abstract
11 Drago F, Mauceri F, Nardo L, et al. Behavioral effects of L-alpha-glycerylphosphorylcholine: influence on cognitive mechanisms in the rat. Pharmacol Biochem Behav. Feb1992;41(2):445-8.
View Abstract
12 Barbagallo Sangiorgi G, Barbagallo M, Giordano M, et al. alpha-Glycerophosphocholine in the mental recovery of cerebral ischemic attacks. An Italian multicenter clinical trial. Ann N Y Acad Sci. Jun1994;717:253-69.
View Abstract
13 Canal N, Franceschi M, Alberoni M, et al. Effect of L-alpha-glyceryl-phosphorylcholine on amnesia caused by scopolamine. Int J Clin Pharmacol Ther Toxicol. Mar1991;29(3):103-7.
View Abstract
14 Muratorio A, et al. A neurotropic approach to the treatment of multi-infarct dementia using L-alpha glycerylphosphorylcholine. Current Therapeutic Research. 1992;52(5):741-752.
15 Di Perri R, et al. A multicentre trial to evaluate the efficacy and tolerability of alpha-glycerylphosphorylcholine versus cytosine diphosphocholine in patients with vascular dementia. J Int Med Res. 1991;19(4):330-341.
View Abstract
16 Frattola L, et al. Multicenter clinical comparison of the effects of choline alfoscerate and cytidine diphosphocholine in the treatment of multi-infarct dementia. Current Therapeutic Research. 1991;49(4):683-693.
17 Abbati C, et al. Nootropic therapy of cerebral aging. Advances in Therapy. 1991;8(6):268-276.
18 Paciaroni E, Tomassini PF. Controlled clinical trial of the efficacy and safety of choline alphoscerate (alpha-GPC) versus oxiracetam in patients with mild cognitive deficit of vascular origin. Giornal Italiano di Ricerche Cliniche e Terepeutiche. 1993;14(2):29-34.
19 Amenta F. The cholinergic approach for the treatment of vascular dementia: evidence from pre-clinical and clinical studies. Clin Exp Hypertens. 2002 Oct-Nov;24(7-8):697-713.
View Abstract
20 Sergei M, Valery A. Gliatinä (L-alpha-Glycerylphosphorylcholin – Italfarmaco) in treatment of consciousness disorder after head injury. Neuropshyhopharmacol. 1994;10(3)(Suppl 8S,Pt2):199.
 
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