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Methylcobalamin
Methylcobalamin is the most potent form of Vitamin B12 found in nature. We need methylcobalamin for the healthy development and sustenance of our circulatory, immune and nervous systems. Eggs, dairy products, fish and meat, especially organ meat like liver, are good sources of Vitamin B-12. In fact, meals incorporating large amounts of liver represented the main treatment for Vitamin B-12 deficiency in the past. Methylcobalamin is the only active form of Vitamin B-12 in the brain outside the mitochondrion. The liver must convert cyanocobalamin to methylcobalamin in order for Vitamin B-12 to do its biochemical work in the brain. When the complex conversion of cyanocobalamin is not completed, the brain is robbed of the benefits of methylcobalamin. Cyanocobalamin is a by-product of Vitamin B-12 charcoal extraction. Scientific methods led people to believe that cyanocobalamin, not methylcobalamin was the naturally occurring form of Vitamin B-12. Cyanide in the charcoal replaces the methyl group in much the same way as it does in the body of a cigarette smoker. Vitamin B-12 requires the assistance of Intrinsic Factor to enter the body from the small intestine. Without Intrinsic Factor, dietary Vitamin B-12 or B-12-containing supplements go unabsorbed. Autoimmune reactions and diseases sometimes destroy the stomach's parietal cells that produce Intrinsic Factor. Pernicious anemia results from this destructive process. More rarely, pernicious anemia develops when the body makes antibodies against the binding site of Intrinsic Factor. The antibodies rob Vitamin B-12 of the binding spot on Intrinsic Factor as it tries to make its way into the small intestine. Monthly injections of Vitamin B-12 can correct the anemia, immune and neurological problems that sneak up on people with pernicious anemia. Surveys of depressed patients indicate nearly one-third of them do not receive enough folate or Vitamin B-12. It is extremely important to take Vitamin B-12 when taking folate supplements. Without Vitamin B-12 supplementation, worse physical problems might develop during folate supplementation. Small amounts of Vitamin B-12 are absorbed directly through the mucosal tissue of the mouth. This discovery led to the development of Vitamin B12 lozenges and sprays. When Vitamin B-12 is absorbed in the mouth, it goes into the blood and then to the enzymes that require Vitamin B-12 as a coenzyme. With other forms of Vitamin B-12, the liver must use its enzyme systems to produce methylcobalamin. With increased availability of methylcobalamin, medical research has shown that methylcobalamin has important benefits not seen with cyanocobalamin. It acts to reverse nerve damage and promote nerve cell regeneration. Methylcobalamin plays a key role in sleep. It helps the brain fill up its neurotransmitter "gas tank" when neurotransmitters are produced from amino acids. Similarly, depression also improves more quickly and completely when patients take methylcobalamin. Depression also can worsen even while using antidepressants if a restrictive diet is started to lose weight. A diet can run the neurotransmitter "gas tank" dry. Homocysteine has emerged on center-stage as a biochemical culprit associated with vascular and brain disease. Methylcobalamin and 5-methyl-tetrahydrofolate are crucial to the elimination of homocysteine. Vitamin supplementation reduces the chances of building up levels of homocysteine associated with stress. Clinical experience and scientific research have clearly established the importance of Vitamin B-12. The discovery of Vitamin B-12 was considered so monumental that the responsible researchers were honored with the Nobel Prize. Recent discoveries have demonstrated the value of using methylcobalamin for improvement in the cardiovascular, immune and nervous systems.*
Methylcobalamin
Introduction

Methylcobalamin is one of the two coenzyme forms of vitamin B12 (the other being adenosylcobalamin). It is a cofactor in the enzyme methionine synthase which functions to transfer methyl groups for the regeneration of methionine from homocysteine.

Pharmacokinetics

Evidence indicates methylcobalamin is utilized more efficiently than cyanocobalamin to increase levels of one of the coenzyme forms of vitamin B12. Experiments have demonstrated similar absorption of methylcobalamin following oral administration. The quantity of cobalamin detected following a small oral dose of methylcobalamin is similar to the amount following administration of cyanocobalamin; but significantly more cobalamin accumulates in liver tissue following administration of methylcobalamin. Human urinary excretion of methylcobalamin is about one-third that of a similar dose of cyanocobalamin, indicating substantially greater tissue retention.

Clinical Applications

Bell’s Palsy: Evidence suggests methylcobalamin dramatically increased the recovery time for facial nerve function in Bell’s palsy.

Cancer: Cell culture and in vivo experimental results indicated methylcobalamin inhibited the proliferation of malignant cells. Research indicated that methylcobalamin enhanced survival time and reduced tumor growth following inoculation of mice with Ehrlich ascites tumor cells.Methylcobalamin has been shown to increase survival time of leukemic mice. Under the same experimental conditions, cyanocobalamin was inactive.5 Although more research is required to verify findings, experimental evidence suggested methylcobalamin might enhance the efficacy of methotrexate.

Diabetic Neuropathy: Oral administration of methylcobalamin (500 mcg three times daily for four months) resulted in subjective improvement in burning sensations, numbness, loss of sensation, and muscle cramps. An improvement in reflexes, vibration sense, lower motor neuron weakness, and sensitivity to pain was also observed.

Eye Function: Experiments indicated chronic administration of methylcobalamin protected cultured retinal neurons against N-methyl-D-aspartate-receptor-mediated glutamate neurotoxicity. Deterioration of accommodation following visual work has also been shown to improve in individuals receiving methylcobalamin.

Heart Rate Variability: Heart rate variability is a means of detecting the relative activity and balance of the sympathetic/parasympathetic nervous systems. Methylcobalamin produces improvements in several components of heart rate variability, suggesting a balancing effect on the nervous.

HIV: Under experimental conditions, methylcobalamin inhibited HIV-1 infection of normal human blood monocytes and lymphocytes.

Homocysteinemia: Elevated levels of homocysteine can be a metabolic indication of decreased levels of the methylcobalamin form of vitamin B12. Therefore, it is not surprising that elevated homocysteine levels were reduced from a mean value of 14.7 to 10.2 nmol/ml following parenteral treatment with methylcobalamin.

Male Impotence: In one study, methylcobalamin, at a dose of 6 mg/day for 16 weeks, improved sperm count by 37.5 percent.13 In a separate investigation, methylcobalamin, given at a dose of 1,500 micrograms per day for 4-24 weeks, resulted in sperm concentration increases in 38 percent of cases, total sperm count increases in 54 percent of cases, and sperm motility increases in 50 percent of cases.

Sleep Disturbances: The use of methylcobalamin in the treatment of a variety of sleep-wake disorders is very promising. Although the exact mechanism of action is not yet elucidated, it is possible that methylcobalamin is needed for the synthesis of melatonin, since the biosynthetic formation of melatonin requires the donation of a methyl group. Supplementation appears to have a great deal of ability to modulate melatonin secretion, enhance light-sensitivity, normalize circadian rhythms, and normalize sleep-wake rhythm.

Dosage: The dosage for clinical effect is 1500-6000 mcg per day. No significant therapeutic advantage appears to occur from dosages exceeding this maximum dose. Methylcobalamin has been administered orally, intramuscularly, and intravenously; however, positive clinical results have been reported irrespective of the method of administration. It is not clear whether any therapeutic advantage is gained from the non-oral methods of administration.

Safety, Toxicity, and Side Effects: Methylcobalamin has excellent tolerability and no known toxicity.

Folic Acid

Folic Acid are forms of the water-soluble vitamin B9. Folate is composed of the aromatic pteridine ring linked to para-aminobenzoic acid and one or more glutamate residues. Folic acid is itself not biologically active, but its biological importance is due to tetrahydrofolate and other derivatives after its conversion to dihydrofolic acid in the liver.

Vitamin B9 (folic acid and folate) is essential for numerous bodily functions. Humans cannot synthesize folate de novo; therefore, folate has to be supplied through the diet to meet their daily requirements. The human body needs folate to synthesize DNA, repair DNA, and methylate DNA as well as to act as a cofactor in certain biological reactions. It is especially important in aiding rapid cell division and growth, such as in infancy and pregnancy. Children and adults both require folic acid to produce healthy red blood cells and prevent anemia.

Folate and folic acid derive their names from the Latin word folium (which means "leaf"). Leafy vegetables are principal sources of folic acid, although in Western diets fortified cereals and bread may be a larger dietary source.

A lack of dietary folates leads to folate deficiency, which is uncommon in normal Western diets. A complete lack of dietary folate takes months before deficiency develops as normal individuals have about 500–20,000 µg of folate in body stores. This deficiency can result in many health problems, the most notable one being neural tube defects in developing embryos. Common symptoms of folate deficiency include diarrhea, macrocytic anemia with weakness or shortness of breath, nerve damage with weakness and limb numbness (peripheral neuropathy), pregnancy complications, mental confusion, forgetfulness or other cognitive declines, mental depression, sore or swollen tongue, peptic or mouth ulcers, headaches, heart palpitations, irritability, and behavioral disorders. Low levels of folate can also lead to homocysteine accumulation. DNA synthesis and repair are impaired and this could lead to cancer development.

Alpha Lipoic Acid

Alpha Lipoic Acid (also known as lipoic acid, thioctic acid, or ALA) is one of the good fatty acids produced in every one of our cells. One of its main functions is to help convert glucose (blood sugar) into energy. About forty years ago, biologists discovered that ALA is also an antioxidant—a powerful substance that combats potentially harmful chemicals called free radicals which may cause heart and liver disease, cancer, cell aging, and many other conditions.

There are other very effective antioxidants, including vitamins C and E. But what's special about ALA is that it is both water and fat soluble. Scientists believe that ALA operates in conjunction with vitamins C and E, and the antioxidant glutathione, recycling them when they're used up. Many studies have been conducted confirming the health benefits of alpha-lipoic acid, including recent findings that ALA offers neuroprotective and possibly cognitive enhancing effects

Uses

Besides taking ALA for its general benefits as an antioxidant, studies have shown that alpha lipoic acid can help with the following conditions:

  • Hypertension (High Blood Pressure)
  • Coronary Heart Disease
  • Metabolic Syndrome (high blood pressure and elevated cholesterol)
  • Peripheral Neuropathy (caused by diabetes and other conditions, such as Lyme disease, alcoholism, shingles, thyroid disease and kidney failure)
  • Diabetes (improving glucose metabolism and helping diabetics utilize insulin better)
  • Liver Disease Metastatic Pancreatic Cancer (increasing long-term survival)
  • Impaired Brain Function (as a treatment for stroke and other brain disorders involving free radical damage, including Alzheimer's disease)
  • Effects of Aging (improving blood flow and enhancing immune function, restoring levels of glutathione, a protective antioxidant and detoxification compound)
  • Degenerative Diseases (ALA is a strong anti-inflammatory agent)
Vitamin B1

Vitamin B1 (thiamine): A deficiency in this vitamin causes beriberi. A disease of the nervous system, it is characterised by weight loss, emotional disturbance, weakness and pain in the limbs, periods of irregular heartbeat, heart failure and even death.

Pyridoxine Hydrochloride B6

Vitamins are substances that are required by the body in very small amounts to maintain healthy growth and development. They are in involved in numerous biological activities in the body.

The B group of vitamins are involved in the development and maintenance of the nervous system (brain and nerves) and the formation of blood cells. Pyridoxine plays a vital role in the activities of many enzymes. It is essential for the breakdown and use of proteins, carbohydrates and fats from food and for the release of stored carbohydrates for energy. It is involved in the production of red blood cells and antibodies and in the maintenance of a healthy skin and healthy digestion. It is also important for normal function of the nervous system and several hormones.

Vitamin B6 cannot be produced by the body and is therefore obtained solely from the diet. Pyridoxine deficiency is rare because it is found in most foods. However, it can occur during treatment with isoniazid for tuberculosis, or penicillamine for Wilson's disease, and this can result in inflammation of the nerves (neuritis). It may occur as a result of a poor diet in chronic alcoholism or in malnutrition. The female hormone oestrogen can also reduce levels of this vitamin in the body.

Pyridoxine deficiency can cause weakness, depression, anaemia, nerve problems and skin disorders.

Pyridoxine supplements are given to prevent and treat deficiencies of this vitamin and the problems this can cause.

Use

  • Treating vitamin B6 (pyridoxine) deficiency.
  • Treating a condition called idiopathic sideroblastic anaemia, where red blood cells do not form properly.
  • Preventing and treating nerve problems associated with isoniazid treatment for tuberculosis, or penicillamine treatment for Wilson's disease.
  • Treating pre-menstrual syndrome (PMS), where studies have shown pyridoxine supplements can improve symptoms such as irritability, mood swings and depression. (This is an unlicensed use of the medicine).