CELLIV

METADOXINE
Metadoxine, also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol abuse.[1]Metadoxine improved the clinical signs of acute alcohol intoxication and accelerated alcohol clearance from the blood [2]It is in human clinical trials as an attention-deficit/hyperactivity disorder predominantly inattentive treatment.[3] Pyridoxine is an ion pair salt of a vitamin B6 form and of a precursor to the metabolically active pyridoxal phosphate. Pyridoxal phosphate is a coenzyme to many enzymes: see vitamin B6 metabolic functions. Pyrrolidone carboxylate is involved in amino acid metabolism through the glutathione pathway.[4] Glutathione is an important antioxidant and combats redox imbalance. It also supports de novo ATP synthesis.

History

Metadoxine is predominantly used in developing nations for acute alcohol intoxication. Alternate names include: Abrixone (Eurodrug, Mexico), Alcotel (Il Yang, South Korea), Ganxin (Qidu Pharmaceutical, China), Metadoxil (Baldacci, Georgia; Baldacci, Italy; Baldacci, Lithuania; CSC, Russian Federation; Eurodrug, Colombia; Eurodrug, Hungary; Eurodrug, Thailand; Micro HC, India), Viboliv (Dr. Reddy's, India), and Xin Li De (Zhenyuan Pharm, China).

Pharmacology

Treatment for acute alcohol abuse In an animal model, metadoxine treatment increased the clearance of alcohol and acetaldehyde, reduced the damaging effect of free radicals, and enabled cells to restore cellular ATP and glutathione levels. [7][8] It increases the urinary elimination of ketones, which are formed when the oxidation rate of acetaldehyde into acetate is exceeded on massive alcohol intoxication.[8][4] As a medical treatment, it is typically given intravenously.

Treatment for AD/HD-PI

Metadoxine is a selective antagonist to the 5-HT2B receptor, a member of the serotonin receptor family.[3] Electrophysiological studies also showed that Metadoxine caused a dose-dependent, reversible reduction in glutamatergic excitatory transmission and enhancement of GABAergic inhibitory transmission, changes that may be associated with cognitive regulation.[3] It is given orally in an extended release pill, which differs from the instant release alcohol treatment.

Treatment for liver disease

Metadoxine may block the differentiation step of preadipocytes by inhibiting CREB phosphorylation and binding to the cAMP response element, thereby repressing CCAAT/enhancer-binding protein b during hormone-induced adipogenesis.

Treatment for Fragile X Syndrome

Metadoxine treatment led to significant improvement in blood and brain biological markers (AKT and ERK), which may have a role in learning and memory.[3] The study also demonstrated a reduction in the amount of immature neurons and abnormally increased protein levels.

SILYMARIN

Silymarin: A Potent Antioxidant, Liver Protector, and Anti-Cancer Agent Silymarin is a unique flavonoid complex—containing silybin, silydianin, and silychrisin—that is derived from the milk thistle plant. These unique phytochemicals from the milk thistle have been the subject of decades of research into their beneficial properties. Milk thistle's common name comes from the white markings on the leaves, its milky white sap, and its traditional use by nursing mothers to increase milk. But it is best known for its use as a liver protectant and decongestant, which can be traced to the Greeks and Pliny the Elder (23-79AD), who wrote that it was excellent for "carrying off bile." The famous English herbalist Culpepper (1616-1654) used milk thistle to cleanse the liver and spleen, and to treat jaundice and gallstones.1 In the U.S., the Eclectics—a prominent group of American doctors who practiced during the 20th century—used it for liver problems, and to treat varicose veins, menstrual problems, and kidney disorders. The plant was also cultivated as a food, providing leaves for salad, seeds for a coffee-like drink, and flowers, which were eaten as artichokes are today. In 1968, a group of German scientists discovered the active flavonoid complex silymarin, which provides milk thistle's medicinal benefits. Since then, hundreds of studies have been done on silymarin, and it is approved in the German Commission E Monographs (the most accurate information available on the safety and efficacy of herbs) as a supportive treatment for inflammatory liver conditions such as cirrhosis, hepatitis, and fatty infiltration caused by alcohol and other toxins.

Silymarin is used to:

Regenerate liver cells damaged by alcohol or drugs Decongest the liver (A liver decongestant stimulates bile flow through the liver and gallbladder, thus reducing stagnation and preventing gallstone formation and bile-induced liver damage.) Increase the survival rate of patients with cirrhosis Complement the treatment of viral hepatiti Protect against industrial poisons, such as carbon tetracholoride (a colorless gas that leaks into air, water and soil near manufacturing and waste sites Protect the liver against pharmaceuticals that stress the liver, such as acetaminophen and tetracycline1 Antidote and prevent poisoning from the death cap mushroom, Amanita phalloides, How does silymarin work? As an antioxidant, silymarin scavenges for free radicals that can damage cells exposed to toxins. Silymarin has been said to be at least ten times more potent in antioxidant activity than vitamin E It increases glutathione in the liver by more than 35% in healthy subjects and by more than 50% in rats. Glutathione is responsible for detoxifying a wide range of hormones, drugs, and chemicals. High levels of glutathione in the liver increases its capacity for detoxification. Silymarin also increases the level of the important antioxidant enzyme superoxide dismutase in cell cultures. It stimulates protein synthesis in the liver, which results in an increase in the production of new liver cells to replace the damaged ones. Silymarin inhibits the synthesis of leukotrienes (mediators of inflammation, which can result in psoriasis, among other things). Scientific studies has seen, silymarin has proved to be successful in treating alcohol-related liver disease. In one study, researchers assessed the benefits of milk thistle extract on 170 patients, 91 of them alcoholics with liver cirrhosis. Subjects received 140 mg silymarin three times a day for 41 months. The four-year survival rate was 58 percent in the silymarin group and 39 percent in the placebo group. The reduced death rate among those taking silymarin was most pronounced in the alcoholic cirrhosis subgroup. There were no side effects from silymarin.

Treatment for liver disease

Metadoxine may block the differentiation step of preadipocytes by inhibiting CREB phosphorylation and binding to the cAMP response element, thereby repressing CCAAT/enhancer-binding protein b during hormone-induced adipogenesis.

Treatment for liver disease

Metadoxine may block the differentiation step of preadipocytes by inhibiting CREB phosphorylation and binding to the cAMP response element, thereby repressing CCAAT/enhancer-binding protein b during hormone-induced adipogenesis.

Treatment for liver disease

Metadoxine may block the differentiation step of preadipocytes by inhibiting CREB phosphorylation and binding to the cAMP response element, thereby repressing CCAAT/enhancer-binding protein b during hormone-induced adipogenesis.