Sublingual Liquid Vitamin B12 (methylcobalamin) 4 ounce

Methylcobalamin - Vitamin B-12 - Sublingual Liquid 120 ml, 4 fl. oz.

Recommended Dosage:  One or more times per day, place 1 ml (1 dropper which is 1/4 tsp [or 1 mg] as indicated on dropper) under tongue, hold for 30 seconds and then swallow.  Or, see below.  120 day supply at 1/4 tsp [or 1 mg or 1000 mcg] per day.

Other Ingredients:  Purified water, glycerin, polysorbate 80 cinnamon and cranberry flavoring, sodium benzoate and benzoic acid.  Contains no added starch, salt, wheat, gluten, corn, coloring, or dairy products. 

B12 -- The Vital Vitamin -- Oral B12 Equivalent to Injections
Reprinted by permission from Bill Faloon of The Life Extension Foundation

by Terri Mitchell

Methylcobalamin is the form of vitamin B 12 active in the central nervous system.  It is an active coenzyme of the vitamin B12 analogs, that are essential for cell growth and replication.  The liver may not convert cyanocobalamin, the common supplemental form of vitamin B 12, into adequate amounts of methylcobalamin the body may need for proper neuronal functioning.  Methylcobalamin may exert its neuroprotective effects through enhanced methylation, acceleration of nerve cell growth or its ability to promote healthy homocysteine levels.  For methylcobalamin to be available to the brain, it should be allowed to dissolve under the tongue in order to bypass the liver during first pass through the blood stream.

For decades, people have been injecting themselves with vitamin B12 because they thought oral supplements were not adequately absorbed.  New research indicates that oral B12 supplements may be as good or better than injections.

Those who have low levels of vitamin B12 in the blood have long resorted to injections of this essential B vitamin, an uncomfortable delivery method at best.  New evidence suggests that oral B12 works as well as injections, according to a study published in the journal Blood but high doses must be taken.  This verifies reports from Sweden dating from the 1970s.  Resolving the debate over oral-versus-injections is very timely, given that vitamin B12 is a homocysteine-lowering factor.

According to the recent data, 2,000 micrograms (2 mg) / day of oral B12 is necessary.  The oral version works as well as injections, with the added feature of maintaining high levels in the blood over time.  The study showed that after a month, the blood levels of the vitamin in people receiving injections dropped and stayed at a plateau, whereas blood levels of those receiving oral B12 continued to rise.

B12 Lowers Homocysteine
Although oral B 12 did not reduce homocysteine (high levels is a marker of poor health) in every case, when it did, the results were dramatic.  Some of the people in the study had homocysteine levels as high as 175 micromoles per liter (the optimal safe range for homocysteine is under 6).  In the case of one patient, 2,000 micrograms of oral B12 for four months reduced their homocysteine from 113.4 micromoles per liter to 8.2.  Injected B 12 also significantly reduced homocysteine - the main difference being that the injected version worked faster.

Interestingly, some of the patients did not respond to supplemental vitamin B12.  It was discovered that they were also deficient in folate (folic acid), and until folate was replaced, their homocysteine remained elevated.  Vitamin B12 and folate work synergistically in the chemical reactions that recycle homocysteine back to methionine in the methylation cycle.  It is also interesting to note that participants in the study with both B12 and folate deficiencies had several health problems including those related to alcohol consumption.  This is probably due to the vitamin's role in methylation.

Intrinsic factor is secreted by the stomach to help the body absorb B12.  Older people produce less intrinsic factor, and are thus more vulnerable to B 12 deficiency.  In the study mentioned at the beginning of this article, high-dose oral B12 was absorbed as well as injectable.  No supplemental intrinsic factor was given.  Insufficient stomach acid can be the result of low intrinsic factor.  Injected B12 has traditionally been used because it bypasses the absorption problem.

Different Forms of Vitamin B12
Cyanocobalamin is the usual form of B 12 sold in this country.  Hydroxocobalamin and adenosylcobalamin are two other forms.  For the past 20 years, English doctor Anthony G. Freeman has been attempting to get the cyano form of B12 removed from the market and replaced with the hydroxocobalamin.  He points out that the cyano form is not effective for certain eye problems caused by smoking and alcohol.  But another form, methylcobalamin, may be the best of all.  Research shows that this active form of B 12 has the unique ability without adverse side effects.

It has been documented that the level of B12 decreases every year with age.  They also have less SAM-e (s-adenosylmethionine) - the substance required to methylate cobalamin (B12) to methylcobalamin, the active form.  Methylcobalamin is already methylated: it doesn't require SAMe.

The Elderly
B12 deficiency is a fairly common deficiency in elderly people.  It is crucial for the retention of folate (folic acid) in cells.  Diet, age, and drugs are the prime culprits behind B12 deficiency.  Meat is the primary source of vitamin B12. Strict vegetarians (people who eat no animal products whatsoever) are at risk for vitamin B12 deficiency. (Vegetarians who eat eggs and fish will get B12 in their diet. In addition, some seaweeds contain the vitamin, and the gut may manufacture a certain amount.) However, a meat diet doesn't guarantee that a person won't be B12 deficient. Some elderly people, for example, can eat high quantities of meat but still be B12 deficient because they don't have enough hydrochloric acid in their stomach to maintain intrinsic factor. Meat-eaters taking certain drugs are also at risk for B12 deficiency.  Drugs that inhibit gastric secretion can cause B12 deficiency. Anyone who chronically takes drugs for stomach ulcers, "heartburn" or gastroesophageal reflux may be creating B12 deficiency in themselves.

There appears to be something else causing B12 deficiency in older people that researchers don't yet understand.  In a Dutch study, researchers found that about 25% of the participants had low vitamin B 12.  But gut problems only accounted for 28% of those cases.  The cause in the remaining 72% is a mystery.  Researchers do know that more people may be deficient than currently appreciated.  When researchers at the Veterans Administration Hospital in Oklahoma used modified criteria for B12 deficiency (elevations in homocysteine and methylmalonic acid, plus serum B 12 up to 300 pg/mL -- the norm is usually 200), they uncovered twice as many people with B12 deficiency than would have been detected by serum values alone.

Elevated homocysteine levels (a marker of poor health) is found in many people with compromised health.  When treated with 1000 micrograms (1mg) of vitamin B 12 (methylcobalamin) daily for three weeks, homocysteine levels dropped significantly.  Although the study didn't follow the patients long enough to see the effects of long-term treatment, the condition of the patients' blood vessels will likely improve as the levels of homocysteine are reduced, as homocysteine is extremely toxic.

B12 and Sleep Support
Those who have a hard time sleeping may need vitamin B 12.  Studies show that B12 causes an earlier release of melatonin at night which supports the sleep-wake cycle.  B12 acts directly on the pineal gland to provoke a faster release of melatonin.  At the tail end, B12 causes melatonin to drop off faster.  B12 helps you get to sleep earlier, and may help you wake up earlier if you leave a curtain open to the morning sun.  B12 sensitizes you to morning light, which helps you wake up.  However, it may not work for everyone.  Unfortunately, the vitamin doesn't help people who want to cut down on their sleep time altogether.

Testing for B12 Deficiency
There are several tests geared towards diagnosing B12 deficiency.  Homocysteine is an indirect test.  A more direct method is to measure methylmalonic acid which becomes elevated in B12 deficiency.  There are other tests which measure gut secretions or antibodies to gut secretions. The Schilling Test can help ferret out what is causing the deficiency, and a simple blood test can show blood levels.

Dosage
The dose of oral B12 supplements for sleep support is 3000 mcg (3mg) a day, while 2000 mcg (2mg) a day has proven useful in lowering homocysteine and correcting B12 deficiency.  In published studies, it took four weeks for sleep support, and four months for the homocysteine-lowering effect -- so, be patient.  People with more serious issues should take very high doses in the range of 3000-5000mcg, supplemented with SAM-e (s-adenosylmethionine).

The neurologically active form of vitamin B 12 (methylcobalamin), is the recommended form to consume. The potential benefits are well-worth the modest price.  It is the methylcobalamin form of B12 that has been used in most European and Japanese studies showing efficacy. The liver converts about 1% of ingested cyanocobalamin into methylcobalamin, but it is far more efficient to dissolve good tasting methylcobalamin liquid in the mouth for immediate assimilation into the brain.

References

• Berlin R, et al. 1978. Vitamin B12 body stores during oral and parenteral treatment. Acta Med Scand 204(1-2):81-4.
• Bernard MA, et al. 1998. The effect of vitamin B12 deficiency on older veterans and its relationship to health [see comments]. J Am Geriatr Soc 46(10):1199-206.
• Freeman AG. 1992. Cyanocobalamin - a case for withdrawal: discussion paper. J R Soc Med 85:686-7.
• Honma K, et al. 1992. Effects of vitamin B12 on plasma melatonin rhythm in humans: increased light sensitivity phase-advances the circadian clock? Experientia 48:716-20.
• Houston DK, et al. Age-related loss, vitamin B-12, and folate in elderly women. Am J Clin Nutr 69:564-71.
• Kaji R, et al. 1998. Effect of ultra high-dose methylcobalamin on compound muscle action potentials: a double-blind controlled study. Muscle Nerve 21:1775-8.
• Kamgar-Parsi B, et al. 1983. Successful treatment of human non-24-hour syndrome. Sleep 6:257-64.
• Kuzminski AM, et al. 1998. Effective treatment of cobalamin deficiency with oral cobalamin. Blood 92:1191-98.
• Mayer G, et al. 1996. Effects of vitamin B12 on performance and circadian rhythm in normal subjects. Neuropsychopharm 15:456-464.
• Parnetti L, et al. 1992. Platelet MAO-B activity and vitamin B12 in old age. Mol Chem Neuropathol 16(1-2):23-32.
• Salom IL, et al. Effect of drugson the absorption of vitamin B12. 1982. Scand J Gastroenterol 17(1):129-31.
• Shane B, et al. 1985. Vitamin B12--folate interrelationships. Ann Rev Nutr 5:115-41.
• van Asselt DZ, et al. 1998. Role of cobalamin intake in mild cobalamin deficiency in older Dutch subjects [see comments]. Am J Clin Nutr 68(2):328-34.
• Watanabe T, et al. 1994. Ultra-high dose methylcobalamin promotes regeneration in experimental models. J Neurol Sci 122:140-3
• Yamazaki K, et al. 1994. Methylcobalamin (vitamin-B 12) promotes regeneration anterior gracile muscle of gracile axonal (GAD) mutant mouse. Neurosci Lett 170:195-7.

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