Side effects of hcl

Dear Dr. Roach: I started taking betaine hydrochloride for my digestive health.

I have had some ongoing issues, and my sister, the wellness guru, has been sharing some things she has learned and suggested this to me. In the first week, I have noticed a difference. My wonderful partner, who is always skeptical, is wondering if there is true value with this supplement, so we are turning to you for some insight.

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J.Y.

Betaine hydrochloride has several purported uses. One is to improve athletic performance; however, the data are mixed about whether it is effective at improving muscle strength and endurance.

It also is used to relieve symptoms of gastroesophageal reflux disease and “functional dyspepsia,” a nonspecific term encompassing several types of stomach upset.

Betaine temporarily increases acid levels in the stomach (that’s the same thing as a lower pH). This effect lasts a few hours, at least in one study of volunteers taking acid-suppressing drugs. Because of this, betaine hydrochloride has been used to help absorption of some medications.

However, there is no convincing evidence that this helps with symptoms. I am always concerned that an individual person’s response could be due to the placebo effect, meaning that the difference you noted could be due to expecting to find some benefit from taking the supplement.

Betaine hydrochloride does not have many side-effects in most people. Nausea, stomach upset, diarrhea and a body odour all have been reported.

I don’t recommend betaine hydrochloride, but if it is helping and is not causing side-effects, it is not likely to harm you.

Dear Dr. Roach: I have a question about your recent column on colloidal silver. Are you saying you do not advocate using OTC antimicrobial silver (55 PPM) for topical wound care? Is that what the U.S. Food and Drug Administration says is neither safe nor effective for any condition?

When I had shingles 15 years ago, I was told to get some silver salve to use. Can’t really say if it did anything or not.

E.C.

Topical silver is an effective antimicrobial, and even at small doses can improve the effectiveness of other antibiotics.

Prescription-strength silver ointments usually are 0.5 to one per cent, which is 50,000-100,000 parts per million concentration. The effectiveness of 55 ppm silver is doubtful: For a difficult bug such as Staphylococcus aureus, the minimum concentration of silver needed to effectively kill bacteria is about 500-1,000 ppm. I’m not sure why you would have been recommended it for shingles, which is a reactivation of the chickenpox virus. The only thought I had was that perhaps your rash got secondarily infected by bacteria, but that should have been treated by a more effective method. An OTC antibiotic such as triple antibiotic (neomycin, polymyxin and bacitracin) is a reasonable first-line treatment for superficial wounds with mild infection.

While topical silver (in the correct dose) is effective for treatment of infected wounds, colloidal silver, which is taken internally, is neither safe nor effective.

Dear Dr. Roach: I heard that taking L-lysine when you have shingles helps to relieve the symptoms. What is your opinion regarding this treatment? I take it for three or four days whenever I get fever blisters, and it does help to clear my lips.

J.B.

L-lysine, an amino acid, has some effectiveness at reducing recurrences and speeding healing in herpes simplex infection of the mouth or genitals. However, even though varicella-zoster virus is related to herpes simplex, L-lysine has not been effective for treatment or prevention of shingles. The vaccine is the best protection, but early treatment with antivirals, such as valacyclovir, also is helpful.

Dr. Roach regrets that he is unable to answer individual letters, but will incorporate them in the column whenever possible. Readers may email questions to [email protected]

Betaine Anhydrous

1.What Is It?

Betaine Anhydrous is a natural compound that is found in the body. Betaine is also known as and referred to as Trimethylglycine or TMG for short. From a structural point of view, Betaine is a small trimethylated amino acid with the amino acid element being glycine and therefore giving us the name of ‘Trimethyl-glycine’. As mentioned it can be found in the body but also found in sugar beets which is how it got the name of Betaine.

Just to be clear with the naming of this ingredient; Betaine Anhydrous, Trimethylglycine and TMG are the exact same ingredient. Whichever name they choose to use on the nutritional panel, you are getting the same ingredient. Sometimes you may see products use ‘Betaine Nitrate’ which is Betaine Anhydrous paired with a Nitrate for additional benefits.

2.What Does It Do?

Betaine plays a few roles in the body but is most known in the sports supplements industry for providing similar benefits to Creatine. Without going to scienctific; Betaine works as an osmolyte in the body just like Creatine. Osmolytes are molecules that are moved in and out of cells in order to maintain cell volume and fluid balance. A better-hydrated cell is more resilient to stressors such as training and exercise.

Betaine serves a vital role in methylation in the body. It does this through two possible mechanisms: either being used as a methyl donor to reduce homocysteine into the amino acid L-methionine or by increasing levels of active folate molecules which then go on to donate methyl groups and reduce homocysteine levels through the methylation process.

So why is all this improved methylation important? It’s all about this amino acid called homocysteine. Homocysteine is an amino acid that is produced in the body from the breakdown of proteins as part of the methylation process. High levels of homocysteine are increasingly being recognised as an important risk factor for disease and seen as an indicator of potential health problems such as cardiovascular disease and Alzheimer’s.

Patients that are diagnosed with methylation issues or high homocysteine levels are prescribed Betaine supplements as it can directly reduce homocysteine levels through methylation.

From a performance point of view; Betaine supplementation has been studied to have positive effects on muscular power, muscular endurance & body composition. There have even been 2 studies that have specifically looked at these effects; 1 study on just males and 1 study on just females. Additionally, there have been numerous studies on Betaine supplementation that have shown improvements in power, strength and muscular endurance.

The female study gave the subjects either 2.5g of Betaine Anhydrous each day or a placebo with the results being:

  • 250% more weight loss with Betaine supplementation
  • 50% more body fat loss with Betaine supplementation

The male study gave the subjects either 2.5 of Betaine Anhydrous (1.25g twice a day) or a placebo for only 6 weeks and the results of the Betaine group were:

  • 3.2% decrease in Body Fat vs. 0.2% increase in the placebo group
  • 2.4 kg increase in Lean Body Mass vs. 0.3 kg increase in the placebo group
  • 2.9 kg decrease in Fat Mass vs. 0.3 kg increase in the placebo group
  • Larger arm size (cross-sectional measurement) growth over the placebo group
  • High training volume over the placebo group

The exact mechanism for these body composition & performance changes hasn’t been identified. Some argue it is the osmolyte properties of Betaine while others argue that it is the improved methylation ability of the body. Personally, we feel it’s a mixture of a both working together to allow the body to function at a higher level and all aspects of training, recovery and vital bodily processes.

3.How Much Do I Need To Take?

A minimum of 2.5 grams per day has been to yield the body composition changing results from the studies above. The studies supplemented Betaine, in both a single 2.5 gram dose per day and also a 1.25 gram dose, taken twice per day. It’s not clear if there is any benefit to how you ingest the 2.5 gram serve.

In regards to having a reducing effect on homocysteine levels; dosages as low as 1 gram can be effective with upper dosages being at 5+ grams per day. There is some relation to the reduction in homocysteine levels and the amound of Betaine supplemented, the higher the dose of Betaine, the lower homocysteine levels were.

4.When Do I Take It?

Betaine does not need to be supplemented at any particular time of day to utilise its benefits. The key to supplementing with Betaine is consistency day after day, much like creatine. Ensuring you are getting your daily dose of at least 2.5 grams each day is all you need to worry about when supplementing with Betaine.

Often you will find Betaine in pre-workouts, with the intention of providing muscular power and endurance. You will often see it in post-workout formulas, with the intention of supporting muscle growth and recovery.

5.How Long Does It Take To Work?

The specific results we mentioned above were from studies that had subjects supplementing and training for both 6 and 8 weeks. We can say that body composition results showed show after 6 weeks of consistent supplementation of Betaine in conjunction with a training and nutritional plan that is tailored towards these goals. In regards to the effects on homocysteine levels in the body, positive results have been shown in as little as 4 weeks of consistent Betaine supplementation. This is dependant on the dose being supplemented and also the levels of homocysteine in the individual wanting to reduce them.

6.What Are The Top Products?

The top products containing Betaine Anhydrous / Trimethylglycine / TMG are:

Jim Stoppani’s Expert Guide To Betaine

Every once in a while, a hot new supplement comes along and generates a buzz based on a single study that sounds—and often is—too good to be true. And then there are the supplements that gradually build up a solid body of research without much hype. Then, years later, they finally get the recognition they deserve. Betaine is one of these.

In recent years, betaine has become a common ingredient in new pre-workout and post-workout products. But it’s actually not a new supplement. People have been taking it for health reasons for many years. Only now, researchers are showing how powerful of an ally it can be for athletic performance and body composition.

If you like to be ahead of the curve, then it’s time you get behind the label of your favorite pre-workout and see what this promising supplement can do for you.

Stoppani Expert Guide Betaine
Watch The Video – 09:21

What is betaine?

Betaine (pronounced “BEET-uh-een”) is also sometimes sold under its technical name of trimethylglycine, or as TMG, for short. The names are pretty much interchangeable; no matter what you call it, it’s made of the amino acid glycine with three methyl groups attached to it.

In the human body, betaine is naturally derived from the breakdown of choline, and it’s also found in a number of food sources. One of these, you probably guessed, is beets.

Betaine got its name because it was originally isolated from sugar beets, known by their Latin name of Beta vulgaris. But ironically, a number of other foods are far richer sources. For example, 3 oz. of wheat germ contains more than 1,000 mg, which is more than four times the betaine in the same amount of beets. Spinach and quinoa both provide more than twice the amount of betaine as beets. But the name has still stuck.

In all of these plants, betaine serves the same crucial function: protecting the cells from stress, like what happens during droughts or extreme temperatures. It has also been used as a supplement in animal feeds for decades, in order to make pigs, chickens, and salmon healthier and more resilient.

In human health circles, betaine has also been revered for its health promoting effects. People have taken it to support joint and liver health and promote healthy inflammation levels.* In some studies, betaine was even been found to support healthy cholesterol levels, already in normal range.*

What does it do?

In humans, most of betaine’s purported benefits derive from its role as a methyl donor. A methyl donor is any molecule that can transfer a methyl group, which is a carbon atom attached to three hydrogen atoms, to another molecule. Many important biochemical processes in the body rely on methylation.

The most critical reaction where betaine performs this function is in the methylation of the amino acid homocysteine to form methionine. Methionine is important in the body’s internal synthesis of creatine. So one way that betaine may boost muscle strength and size is by increasing creatine production in the body.*

Methionine also plays an important role in muscle protein synthesis, and specifically the process known as “translation.” By having more methionine available for this process, protein synthesis is ramped up, and therefore so is the potential for muscle growth and strength gains.

Betaine may also has the beneficial effect of supporting healthy homocysteine levels.* High homocysteine levels have been shown to impair insulin signaling, which can interfere with muscle growth and fat loss.

And finally, betaine supplementation has also been suggested to raise levels of S-adenosylmethionine, also known as SAMe. Having healthy levels of SAMe may support positive mood, promote liver health, and aid joint recovery.*

Betaine supplementation may support positive mood, promote liver health, and aid joint recovery.*

What are the Performance and Physique Applications?

In the last few years, clinical studies have looked at betaine supplementation in a number of modalities, from strength, to muscle growth, to endurance and sprinting performance. What do they all have in common? Betaine left the placebo in the dust.

One of the first studies to look into betaine’s performance-supporting effects was done in my old lab at the University of Connecticut in 2010. The UCONN researchers found that weight-trained athletes taking 1.25 grams of betaine twice per day increased their muscle strength by 25 percent, and their muscle power by 20 percent.* They also determined that betaine significantly increased markers for muscle protein synthesis following a workout as compared to the placebo.*

Since this initial study, other researchers have found that betaine supplementation helped lifters complete more total reps in bench press workouts, pedal with more power in cycling workouts, and sprint for almost 40 seconds longer than subjects drinking just water. Like the similar-sounding beta-alanine, it has also been suggested to significantly lower levels of lactate, which can delay muscular fatigue and allow athletes to train harder, for longer.*

Researchers have found that betaine supplementation helped lifters complete more total reps in bench press workouts.

And then there’s the latest study on betaine, which comes from the College of Springfield in Massachusetts. Weight-trained males followed an undulating periodized weight-training program for six weeks. One group supplemented with 1.25 grams of betaine twice per day and one group supplemented with a placebo twice per day. They reported that the subjects supplementing with betaine increased muscle mass by 4 pounds and arm size by 10 percent, all while decreasing body fat by 7 pounds.* The placebo group experienced no increase in muscle mass or arm size and no loss of body fat.

What’s to explain these incredible results? A recent study from UCONN indicated that these increases in muscle strength, power, and endurance may be due to betaine’s ability to increase levels of important anabolic substances while supporting a healthy balance of the catabolic hormone cortisol.*

Previous research also suggests that betaine supplementation increases nitric oxide and helps regulate cellular fluid volume, which could further promote muscle pump and overall muscle size.*

Are there any side effects?

There are no known serious side effects of betaine supplementation. However, it can cause nausea, upset stomach, and/or diarrhea in some people. This is one good reason to split your intake into two smaller daily doses, as several of the recent studies have done.

How should I stack it?

It’s no coincidence that betaine is in pre-workout supplement blends alongside ingredients like creatine, L-citrulline, and beta-alanine. Its effects are definitely complementary to these tried-and-true performance supports, and it indirectly helps your body produce and process creatine to boot.*

Several of the most promising recent studies focusing on betaine have included it as a pre-workout, either on its own in water or mixed into a drink with elecrolytes and carbs. Then, the subjects took a second dose later in the day.

That seems like a solid approach to me. Either add betaine to your current pre- and post-workout stack, or look for a blend that includes it.

Should I cycle it?

At this time, there doesn’t appear to be any reason to cycle betaine. It can be taken continuously.

When should I take it?

It is estimated that most people consume about 1-2 grams of betaine in their daily diet. However, research does confirm that supplementing with extra betaine provides distinct health and performance benefits. Plus, research confirms that a good deal of betaine is lost in the sweat during exercise. This further supports the notion that you should supplement with betaine daily, and not only before working out.

Given that betaine has been suggested to boost greater levels of muscle protein synthesis and can decrease cortisol levels, it makes sense to put those doses on both ends of your intense training. This is when you work hardest to create an anabolic environment.

So look for products which supply betaine in the form of betaine monohydrate, betaine anhydrous, or simply listed as trimethylglycine (TMG). Take 1.25-1.5 grams of betaine twice per day, preferably pre- and post-workout.

It makes sense to put doses of betaine on both ends of your intense training.

What’s the Bottom Line?

The bottom line is that betaine can help to take your strength gains and lean mass gains to new levels. It may not have the name-recognition of a classic supplement like creatine yet, but its star is definitely is on the rise.

It appears to be safe and effective, is easily stacked with other supplements, and has the potential to support your general health and well-being outside of the gym to boot.*

For a stack that can’t be beat, don’t forget to include betaine.

These statements have not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure, or prevent any disease.

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  9. Barak AJ, et al. Dietary betaine promotes generation of hepatic S-adenosylmethionine and protects the liver from ethanol-induced fatty infiltration. Alcohol Clin Exp Res. 1993 Jun;17(3):552-5.
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Cautions, Safety and Techniques for the Use of Betaine Hydrochloride

This article is not intended to diagnose or treat any diseases.

Due diligence is a necessary part of the healing process. If you believe you are worth the effort, then seek the knowledge you need to reveal the truth.

In the world of functional medicine and nutrition we use a large array of herbs, vitamins, minerals, amino acids and other biological substances to restore function and support healing. Most of the supplements we use are fairly safe. Even when the diagnosis is incorrect or if a side effect occurs, most reactions will resolve quickly with no permanent harm. However, there is a handful of supplements that can cause, at best, a setback and, on occasion, significant side effects. Betaine hydrochloride (HCl) is one of them. When used appropriately and under the correct diagnosis, Betaine HCl can have seemingly magical effects on conditions like acne, eczema, asthma, idiopathic malnutrition, GERD and other digestive issues. However, a visit to most mainstream medical websites will advise you, “Do not take Betaine HCL”. This is with good reason. Betaine HCL can exacerbate several underlying health conditions and, in rare instances, can cause life-threatening health issues.

Betaine HCL is used to treat a condition called hypochlorhydria (insufficiently strong stomach acid). Although it hasn’t been subject to rigorous clinical trials, here is the simplified hypothesis; when acid is the stomach is not strong enough (pH between 1.5 and 3.5) animal protein cannot be effectively digested into amino acids and smaller protein fragments. As a result, the stomach somehow detects this problem and continues to produce weak acid. The weak acid fills up past the stomach and into the esophagus. Unlike the iron-clad lining of the stomach, the esophagus is easily damaged by acid. The thinking is that Betaine HCl works by restoring the correct pH (increasing the acidity) of stomach acid. When the correct dosage achieved, the excess production of weak acid stops and normal digestion of protein and minerals resumes. If the correct dose is not achieved, supplementing with Betaine HCl has little value. Practitioners, here is a link to a method that was originally presented by Jonathan Wright M.D. on how to figure out the correct dose of Betaine HCl. As the author describes, most cases require no more than 2500mg for reestablishing adequate acid levels. I have seen a few cases where the replacement dose was over 6000mg per meal.

Accurate Diagnosis is Crucial

There are many downstream health issues that can arise from inadequate digestion of protein. These include IBS, excessive flatulence, leaky gut syndrome, asthma, acne, allergies, eczema, acid reflux, idiopathic malnutrition, premature osteoporosis etc. There are scientifically sound explanations for each of these that we will discuss another time. However, any of these conditions can be caused by other factors and, none of them is a defining symptom of low stomach acid (hypochlorhydria).

Most importantly, acid reflux, often diagnosed as GERD, is NOT a pathognomonic symptom of hypochlorhydria. The exact same symptoms can be caused by overgrowth of bacteria and in small intestine, excess production of acid, stagnation of the motor migrating complex and, more commonly, by excess histamine. This is why decades of research produced two classes of drugs to treat GERD. These are the proton pump inhibitors (PPI’s) and H2 blockers (Histamine receptor blockers). It can be implied that the effectiveness of these two categories of drugs in treating symptoms can shed some clarity on the root of the problem. In more complex cases, hypochlorhydria and excess histamine will occur simultaneously.

The Big Cautions With Betaine HCl

Esophageal Damage and Strictures

Pills of Betaine HCl can get lodged in areas where the esophagus has narrowed from scar tissue or has shrunk from old age. This usually causes a strong, sharp pain. If the pill remains for more than a couple of minutes, it can literally burn the area. If this happens, the irritation can last several days and it is best to discontinue the course of Betaine HCl therapy until it is completely healed. To prevent damage to the esophagus in cases like these, it is crucial to flush the area until the pill is small enough to move on. This can be done by sipping a weak solution of baking soda in warm water (1/4 tsp per 12 oz of water) OR by diluting a full dose of a liquid antacid in warm water. DO NOT use baking soda if the patient has high blood pressure. This scenario is more common in elderly patients and it is better to break up the Betaine HCl capsules before swallowing them. As a general rule, if this happens, don’t hesitate to seek medical attention.

Exacerbation of Gastritis

Gastritis is inflammation of the stomach lining. It has many causes but ultimately occurs because the cells lining the stomach cannot replace themselves quickly enough to maintain the integrity of the tissue. When this happens, any small amount of acid can quickly damage the lining. This is a potentially dangerous situation as ulcers can form. Possible causes include excessive alcohol consumption, use of corticosteroids and NSAIDS, stress, excess acid production, nutritional deficiencies, excess levels of histamine and infection.

Combine a stomach that is severely irritated by excess histamine and add Betaine HCl and you have yourself a new condition that can take several weeks to fully heal.

Symptoms of gastritis can easily go unnoticed. This is especially true for people who are busy, overwhelmed and/or highly driven. I meet people all the time in my practice who have had low to mid-grade symptoms of gastritis for years without giving it a single consideration that something could be wrong. This can also happen because some people have an altered perception of pain in their digestive tract. Nerve blocks and cauterizations as well as medications, like antidepressants, narcotics and opioids, can reduce pain sensations. Practitioners! Confirm your diagnosis before prescribing Betaine HCl and proceed cautiously with the dose. DO NOT assume that patients will notice side effects immediately.

A True Story of a Gastritis Nightmare

More than a decade ago, I had a nutrition consultation with a gentleman who had clear signs of gastritis. Although he didn’t think so, his lifestyle was extremely stressful. He was founder and CEO of a very successful chain of stores. He worked long hours and traveled frequently. Drinking too much alcohol was one way he compensated for the stress. His symptoms manifested as a dull ache (fairly mild) above his naval that was worse on an empty stomach, with water, with spicy food and about 20 minutes after eating (food usually absorbs acid for a few minutes before the stomach makes more). He denied any sign of dark, tarry pieces in his stool (a sign of bleeding in the digestive system). At the time of our meeting, he was preparing to leave for a big game hunting trip in east Africa. I insisted that he consult a physician before departing. His first week in the African bush he developed anemia as a result of a bleeding ulcer. It took several days for him to reach a facility with adequate medical care. He ended up having to have surgery and, more unfortunately, a blood transfusion that left him with a lifelong disease.

by

Digestive System Health Center

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29. Francis HW. Achlorhydria as an etiological factor in vitiligo, with report of four cases. Nebraska State Med J 1931;16(1):25–6.

30. Kokkonen J, Simila S, Herva R. Impaired gastric function in children with cow’s milk intolerance. Eur J Pediatr 1979;132:1–6.

31. Gillespie M. Hypochlorhydria in asthma with specific reference to the age incidence. Q J Med 1935;4:397–405.

32. Fravel RC. The occurrence of hypochlorhydria in gall-bladder disease. Am J Med Sci 1920;159:512–7.

33. Murray MJ, Stein N. A gastric factor promoting iron absorption. Lancet 1968;1:614.

34. Russell RM, Krasinski SD, Samloff IM, et al. Correction of impaired folic acid (Pte Glu) absorption by orally administered HCl in subjects with gastric atrophy. Am J Clin Nutr 1984;39:656.

If you made it out to our seminar with Bruce Topping about digestive health, you’ll know he talked a lot about Betaine Hydrochloride, or HCl, and how it can help to level out stomach acid production.

Bruce was kind enough to find this article for us, perfectly articulating the protocol of using HCl and how it can help to rebuild your gut.

Here are some important excerpts from this article:

How to Figure Out Your Betaine HCL Dose
Each person will have a specific supplementary HCL dosage. Unfortunately, there isn’t a special formula I can give you to figure it out. This is a case of trial and error until you get to the correct dosage. Failing to get to your correct dosage can remove the benefits of supplementing.

You must find the right dosage for you situation. If you fail to do the trial and error you’re wasting your time and money.

This is a very common problem we see with our readers. Remember, the stomach is purposely built to handle extreme acid environments. If your correct dosage is 2400mg and you’re only taking 1200mg, you’re not really doing your stomach any favors. You must follow the process below to figure out the right dosage to get the maximum benefit.

  1. Eat a meal that contains at least 15-20grams of protein (about 4-6ounces of meat).
  2. Start by taking 1 pill (650mg or less) of Betaine HCL during the beginning of the meal.
  3. Finish the meal as normal and observe your body for any changes in feeling associated with the stomach and belly button area. Things to look for: heaviness, hotness, burning, or other GI distress.
  4. Stay at this dosage of 1 pill for another day of meals with protein and if you don’t notice anything on the 3rd day, try 2 pills.
  5. Stay there for another day and then try 3 pills.
  6. Keep increasing the number of pills taken with each meal until you notice some GI discomfort described in step #3.
  7. When this happens, you will know your ideal Betaine HCL dosage is 1 pill less. For example, if you felt the discomfort going from 5 pills to 6 pills, then 5 pills is your proper dosage for a normal meal.

A Couple Points to Clarify:

  1. – If you eat a snack or a meal without much protein, you won’t need as much Betaine HCL (for a small snack like a piece of fruit you won’t need any at all)
  2. – When you experience the GI discomfort finding your correct dosage, you can mix ½ teaspoon of baking soda in 8oz of water and drink it to help lessen the pain.
  3. – Dr. Wright notes in his book that “paradoxically adverse symptoms are most likely to occur in individuals with the lowest levels of stomach acid. This is because these people are most likely to have atrophic gastritis (a thinned-out stomach lining), which makes them much more sensitive to even small quantities of HCL than a normal, thicker stomach lining.” This makes sense because a super inflamed stomach lining won’t have its normal protective barrier intact to contain the strong acids. In this case, it is wise to start with digestive bitters or get smaller dose Betaine HCL pills (think 350mg or less).
  4. – If you have low stomach acid and you can’t supplement with Betaine HCL, there’s a few natural methods to help with symptoms. Start by taking a shot of lemon juice or vinegar before a meal to help the symptoms of indigestion. But know that these don’t actually help the digestion of food only the symptoms. A supplement that can help the digestion is digestive bitters.

I Need to Take How Many Betaine HCL Pills
It’s very common for people to stop short of their needed Betaine HCL dosage. In fact, in the beginning I was nervous about taking 6 pills at a meal. But trust me. there is nothing to worry about.

Dr. Wright reports that the common Betaine HCL dosage range in his clinical practice is 3,250-4,550mg per meal.

That means there are also plenty of people who need above 5,000mg for an effective dosage.
Remember, a normal functioning stomach is capable of producing and handling extreme acid ranges. If your dosage starts getting extremely high without any GI distress (step #3), you must use your GI symptoms as a guide instead. These include burping, bloating, farting, and stool consistency. Keep everything else the same in your diet as you wait for these indicators to change for the better. Just because you can take 20 pills, doesn’t mean you should. It could be that at 11 pills all of your problems disappear. For this group of people try to find the minimum dose needed to help your GI symptoms and for Pete’s sake go get more testing to figure out what is going on!

Unlocking Health Benefits With Betaine

Our continued evolution into an increasingly health-conscious society has catapulted the natural health industry to heights never before seen. In our quest to combat the toxic byproducts and effects of our modernized society, we have turned back to nature and its remedies. This repositioning has spurred unprecedented research into how our body works and the components therein that ensure proper functioning. We are looking back to nature to aid in fighting off the effects of the unnatural things we have introduced into our environment and consequently, into our bodies.
We know more now than we ever have, and we’re still at just the tip of the iceberg. There are many compounds that we are just beginning to thoroughly research, study and understand. One of those is betaine. Although betaine was first discovered in the 19th century, we are now beginning to delve deeply into the critical and multi-faceted role it plays in our bodies.

Betaine has long been studied for its positive impact on heart health, but now we are thoroughly exploring ever expanding benefits, such as digestive support and the improvement of exercise performance and body composition. Betaine is on the cusp of a breakthrough into the mainstream natural health channel.

What is Betaine?

Betaine is a naturally occurring amino acid compound also known as trimethylglycine, or TMG. Betaine is a nonessential nutrient found in numerous food sources, including sugar beets, wheat bran, rye grain, bulgar grain, spinach, quinoa, brown rice, sweet potato, turkey breast, beef, veal and some seafood, such as shrimp. It was originally discovered in beets, which is where the name betaine is derived from.
Betaine is composed of the amino acid glycine which is attached to three methyl groups. There are two major functions that betaine undertakes in the body. It acts as a methyl donor and also as an osmolyte. Betaine is rich in methyl groups. A methyl group is a special kind of hydrogen and carbon molecule that can be transferred around the body via a process known as methylation. This process is a critical component of numerous physiological processes, including protein function and genetic activities. Betaine is known as a “methyl donor,” because it has so many of these methyl groups to distribute around the body. Additionally, betaine is an osmolyte. An osmolyte is a compound that affects the process of osmosis by creating fluid level balance outside and inside of cells. The consequence of imbalanced fluid levels can be cellular rupture or cellular shrinkage, dependent upon whether there’s excess fluid on the inside or the outside of the cell. Severe imbalance can ultimately cause the cell to die.

Health Benefits

The health benefits of betaine are numerous. Evidence increasingly shows that betaine is a critical nutrient in protecting and enhancing the function of internal organs and improving vascular risk metrics. It may also aid with digestive function, heart health, liver function and detoxification, fat loss, and muscle mass improvement.

Digestive Aid

In order to digest food, your stomach must have adequate acid levels. Without sufficient acid levels, the food you eat will not be entirely broken down, which means that you will be unable to absorb all the nutrients provided by your food. Consequently, insufficient acid levels (called Hypochlorhydria) can lead to nutritional deficiencies which, in turn, may put you at an increased risk of developing a variety of health and hormone issues.
The acid that carries the biggest workload in the digestive process is hydrochloric acid or HCl. Without enough HCl in your stomach, you will suffer from digestive dysfunction. If you are over 50, the chance that you are not producing enough hydrochloric acid stands at around 50%. Luckily, there is a compound of betaine that is frequently used to aid this digestive issue. Betaine hydrochloride is a compound that consists of betaine and hydrochloride and is naturally found in beets. The most popular composition of betaine supplements is betaine HCl. When taken as a digestive supplement, betaine HCl (hydrochloride) promotes production of additional hydrochloric acid in the stomach, which aids digestion. It assists in the absorption of B12, calcium, iron and proteins. It is also thought to prevent fungi and bacteria from overproducing by ensuring that you have adequate levels of acid to kill them. People who suffer from candida (yeast overgrowth) often have a low level of stomach acid.
The symptoms of low stomach acid often mirror those of high stomach acid, so it’s important to be tested in order to determine if betaine HCl supplementation could be helpful for you. Betaine HCl supplementation should be avoided by people who have peptic ulcers. Hydrochloric acid could also be detrimental to a person with severe atrophic gastritis or inflammation along the stomach wall.

Heart Health

The most extensively researched health benefit of betaine is its cardiovascular affect. The primary way in which betaine may safeguard heart health is by reducing levels of the amino acid homocysteine within the bloodstream. It does this by providing the homocysteine molecule with one of its methyl groups; this, in turn, transforms it into an innocuous substance called methionine. Elevated levels of homocysteine in the blood (known as Homocystinuria) can clog and harden arteries by creating arterial plaque, which can contribute to cardiovascular health issues. Betaine’s effectiveness has warranted FDA approval for use as a treatment for high homocysteine levels.

Liver Function Support and Detoxification

Betaine may also support healthy liver function and liver detoxification. There are many conditions that can result in excessive fatty acid build up in the liver. Some of these conditions include obesity, a diet rich in fatty, sugary foods, diabetes and alcohol abuse. It is difficult for your liver to function properly when you have too much fat in the liver cells. A liver burdened with too much fat can result in scarring of the liver, fluid retention, muscle waste, cardiovascular issues and abdominal pain. Research has indicated that betaine can help break down fatty acids in the liver, and it has also been shown to aid people in recovering from damage to the liver. Additionally, there is evidence to suggest that betaine may protect the liver from hepatotoxins like carbon tetrachloride and ethanol. These dangerous toxic chemicals have been found to access the body through certain prescription medications and also via herbicides and pesticides used on crops that we end up consuming. It is possible that betaine aids the liver in processing these harmful chemicals and eliminating them from the body.

Muscle Mass Improvement and Fat Loss

Betaine is also a popular newcomer to the physical fitness and exercise supplements category, because it plays a critical role in fat reduction and the metabolizing of protein. You’ll likely find betaine in many pre-workout and “muscle building” supplements on the market today. In clinical trials, it has been shown to increase muscular power, strength and endurance, in conjunction with fat loss. The overall result is improved body composition. You may have heard of another popular osmolyte in the health and fitness supplement segment called creatine. Like creatine, it is possible that betaine may hasten muscle and strength gains. Through protein synthesis, betaine is able to increase the growth of muscle. The digestive and cardiovascular benefits are much more established and understood than the body composition benefits; however, much research is underway in this area.

Effective Doses

A recommended daily intake amount of betaine for adults is yet to officially be established. The suggested dose depends on the particular condition that is being addressed. Additional research is underway to establish a universal standard, although recommendations do exist for certain conditions. For example, for those afflicted with liver issues induced by alcohol consumption, between 1,000 to 2,000 milligrams taken three times daily is the advised dosage level. This is quite an aggressive dose, but it is required in order to repair the damage done to the liver in recovering alcoholics.
For nutritional support in otherwise heathy people, a less aggressive dose is suggested. If you’re looking to take a supplement as a digestive aid (in the form of betaine HCl), there are offerings on the market ranging from 650 to 2500 milligrams. We recommend supplementing with Betaine HCL with Pepsin and Mucosave® by Enzymedica to acidify the stomach, activate the digestive process, and soothe the stomach lining.
For those looking to support their exercise performance with betaine and improve their body composition, they should consider taking a daily dose of between 1500 to 2000 milligrams. This suggestion is provided while acknowledging that there is no official recommendation at present.

Conditions Requiring Caution

Please note: It is not recommended that women who are pregnant or breastfeeding supplement with betaine. More testing needs to be completed in this area to ensure safety. Unless specifically prescribed by a physician to treat certain conditions, such as genetic diseases related to liver malfunction, children and infants should not be given betaine supplementation.

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Indications

for improved protein digestion*
• enhances stomach acidity*
• promotes protein breakdown and absorption*
• benefits individuals with occasional indigestion*
• made without lactose, preservatives, magnesium stearate, or other lubricants and diluents

Ingredients

Two Capsules Contain:
Betaine Hydrochloride* 1.04 g.
Pepsin (Porcine)** 40 mg.
*Equivalent to 16 grains
**Equivalent to 3.2 grains (208 mg.) of Pepsin 1:3,000 potency
Other Ingredients: Hypromellose (derived from cellulose) capsule, Leucine, Silicon Dioxide.
Note: Betaine Hydrochloride derived from a non-plant source. This product is not diluted with lactose. Individuals with porcine allergies should not take this product.

Description

Indigestion affects millions of people every day. For some, eating fatty foods can bring on heartburn. For others, simple carbohydrates (like bread and pasta) may cause gas and bloating. And for other individuals, spicy foods can cause them grief. Although what we eat greatly influences the frequency and severity of indigestion, this discomfort could be related to an underlying problem – poor digestive enzyme activity.
Situations such as illness, gall bladder removal, overuse of antacids, and normal aging can contribute to insufficient secretion of stomach acid, pancreatic enzymes, and bile, and can adversely affect digestive enzyme activity and lead to occasional heartburn, gas, bloating, and other forms of gastrointestinal discomfort.*
Maldigestion can lead to digestive problems and poor absorption of nutrients, resulting in vitamin deficiencies (particularly fat-soluble vitamins like vitamins A, D, E, and K). Food allergies can develop when inadequately digested proteins are absorbed through the gut. As large proteins are absorbed intact, the body might recognize them as foreign and create antibodies to them, resulting in an allergic response to the food. An individual who has frequent indigestion should make sure to have adequate enzyme support.*
Hydrochloric acid secretion in the stomach does several positive things. It assists protein digestion by activating pepsinogen to pepsin, it renders the stomach sterile against ingested pathogens, it inhibits undesirable overgrowth in the small intestine, and it encourages the flow of bile and pancreatic enzymes.* Hydrochloric acid also facilitates the absorption of a number of nutrients, including folate, vitamin B12, ascorbic acid, beta-carotene, iron, and some forms of calcium, magnesium, and zinc.* Numerous studies have shown hydrochloric acid secretion in the stomach declines with advancing age. Overuse of antacids can also lead to low levels of hydrochloric acid in the stomach, which can result in poor protein digestion.* Thorne offers hydrochloric acid and pure pepsin from a porcine source. Unlike many supplement companies, the pepsin utilized in Thorne’s product is pure, undiluted, and lactose-free.

Quantity

225 Vegetarian Capsules
Servings Per Container: 112

Dose

Take 1-2 capsules with each meal or as recommended by a health-care practitioner.

Potential side effects/Safety

ALLERGY WARNINGSThis product is contraindicated in an individual with a history of hypersensitivity to any of its ingredients.Betaine HCl & Pepsin contains an ingredient derived from a porcine (pork) source.EXCIPIENT FREEThis product does not contain wheat, gluten, corn, yeast, soy, egg, dairy products, or artificial colors, sweeteners, or flavors. This product also does not contain lactose, palmitic acid, or magnesium, calcium, or vegetable stearates.PREGNANCY WARNINGIf pregnant, consult your health-care practitioner before using this product.INTERACTIONS/CONTRAINDICATIONSBetaine HCL & Pepsin should not be used concurrently with H2-blocking drugs and proton pump inhibitors, because these drugs are intended to block the production of stomach HCl.OTHER WARNINGSBetaine HCL & Pepsin should be used with caution in an individual with a history of a peptic or duodenal ulcer.It is not recommended to remove the Betaine HCL & Pepsin powder from the capsule, as it can be irritating to the oral mucosa.

PMC

Discussion

In this pilot study, we demonstrated that 1500 mg of BHCl significantly (P <0.001) and safely reduced gastric pH in healthy subjects with pharmacologically-induced hypochlorhydria by over 4 pH units (Figure 2), lowering gastric pH from above pH 5 to below pH 1 for more than an hour. These findings support the further investigation of BHCl as a solid oral dosage form of HCl that can potentially aid in the absorption of orally administered weakly basic drugs with pH-dependent solubility given under hypochlorhydric conditions.

Hypochlorhydria (or achlorhydria) is defined as a lack (or absence) of acid in the gastric fluid, and can be caused by medical conditions such as Helicobacter pylori infection13 or autoimmune metaplastic atrophic gastritis.14 Hypochlorhydria can also be induced through the repeated administration of acid-reducing agents, such as proton-pump inhibitors (PPIs) or H2-receptor antagonists (H2-RAs), commonly used to manage symptoms of gastroesophageal reflux disesase (GERD) or peptic ulcer disease (PUD). Individuals on daily drug regimens of acid-reducing agents therefore will have high gastric pH. From a pharmacologic perspective, gastric acid is important for the dissolution and solubilization of many solid oral dosage form medications and therefore is critical in oral drug absorption. Thus, conditions in which gastric acid levels are lowered or suppressed can lead to drug-drug interactions (DDIs) resulting in altered systemic concentrations and drug exposures. For example, for weakly basic drugs that exhibit pH-dependent solubility over a pH range of 1 to 4, the fraction of the dose available to the body for absorption will be severely reduced when gastric pH is > 4, limiting drug absorption and systemic exposure during acid-reducing agent therapy. In this scenario, temporary gastric re-acidification during drug administration may be helpful.

A gastric pH ≤ 2 was thought to be sufficiently acidic to improve the solubility of weakly basic drugs with pH-dependent solubility. Therefore, a 1500 mg dose of BHCl (2–750 mg tablets) was chosen as it provides the equivalent of 9.7 mmol of hydrogen ions (H+), which equates to pH 1.41 in 250 mL of water. Though 1–750 mg tablet will produce over 4.8 mmol of H+ and a pH of 1.71, two tablets were used to guarantee a more consistent gastric re-acidification across patients. An acidic beverage, such as Coca-Cola® for example, was reported to have a pH of 2.5.1 If a drug was administered with 250 mL of the beverage, this would only provide 0.79 mmol of H+, which is much less than a single 750 mg tablet of BHCl that could provide over 4.8 mmol of H+. BHCl provides an additional benefit over acidic beverages as the solid oral dosage form supplies acid directly to the stomach with no contact to the esophageal walls, minimizing potential patient discomfort and poor oral hygiene associated with repeated dosing. Furthermore, betaine is a safe and important human nutrient obtained from the diet from a variety of foods. Intake of betaine from foods is estimated to be 200–400 mg/day,15 and betaine doses of 6 to 20 grams per day are used safely to therapeutically treat homocystinuria.16

Drug absorption can only be improved for weakly basic compounds if there is adequate exposure to a more acidic environment. If a drug was administered following BHCl dosing and the duration of re-acidification was not adequate, gastric pH would recover too quickly and there would be a minimal effect on the drug’s dissolution and solubility. However, BHCl should provide ample time for gastric re-acidification (time of gastric pH < 4 ranged from 42 to 127 minutes), considering that for “rapidly dissolving” drugs, 85% of the labeled amount of drug is dissolved within 30 minutes.17

The onset of the re-acidification was also favorable, with a mean onset of 6.3 minutes, ranging between 1.8 and 12 minutes (Table 1). This rapid onset of gastric re-acidification is important from a practical standpoint, as this minimizes the time between the dosing of BHCl and a theoretical victim drug. Having a short activation time also allows this strategy to be more applicable in a real-life patient scenario, where co-administration of BHCl and a victim drug would be more commonplace. Nonetheless, while this may help improve overall drug absorption, we do recognize the potential risks of having exposure to high gastric acidity in actual patients who are on an acid-reducing agent for gastrointestinal disorders. As a proof-of-concept study, only one dose of BHCl was chosen and only healthy volunteers were enrolled. Thus, further studies are warranted to investigate the dose-response of BHCl on the potency and duration of gastric re-acidification and the tolerability of BHCl in patients on acid-reducing agents for GERD or other gastrointestinal disorders.

While ΔpH and rebound times to pH > 3 and > 4 were used as the primary markers of BHCl activity, the AUCpH’s below pH 3 and pH 4 have also shown to have some value. Significant correlations were found between the AUCpH below pH 3 and pH 4 and their respective rebound times, making it a secondary measure of the duration of gastric re-acidification as opposed to the potency. As each subject received the same dose of BHCl, the observed ΔpHs did not vary significantly, with coefficients of variation less than 10%. Although the pH-time data can directly provide an estimate of the length of the re-acidification period, the method can be flawed if the data are significantly affected by fluctuations in the pH above and below a given threshold. Using the AUCpH can account for these fluctuations because only the parts of pH-time curves that are actually spent below pH 3 and pH 4 are integrated into the AUCpH calculations, thereby limiting the effect that the variability in pH measurements may have.

In addition to the potency and duration parameters, serum gastrin was examined for its ability to be a predictor of gastric re-acidification following BHCl administration. Gastrin is a hormone produced by antral G cells that is a potent inducer of gastric acid secretion18 and can be affected via negative feedback in the presence of gastric acid, where its release is inhibited.19 We found no significant relationships between serum gastrin levels and gastric pH (Figure 3), indicating that while the hormone is actively involved in the regulation of gastric acid, it is not predictive of the presence of gastric acid from BHCl administration.

The results of this pilot study have shown that BHCl can be used as an effective method to rapidly and temporarily lower gastric pH in healthy volunteers with drug-induced hypochlorhydria. This strategy has several advantages over previous methods of gastric re-acidification. It utilizes a commercially available, oral, natural supplement that can be purchased over the counter, making it easy for potential patients to obtain and use, thereby avoiding the harm and discomfort that can arise as a result of the ingestion of a large quantity of acidic fluid. BHCl has a rapid onset of effect, which allows convenient co-administration with a potential victim drug a possible outcome. Additionally, the duration of gastric re-acidification is temporary, yet sufficient, giving ample time for the dissolution of victim drugs that may be formulated as an immediate release dosage form. Lastly, it is possible that the degree of gastric re-acidification may be tailored to specific patients by altering the administered dose of BHCl, though the dose-dependencies of these effects still require further evaluation.

For weakly basic drugs that are administered orally under drug-induced hypochlorhydria, co-administration of BHCl may have a positive impact on the pharmacokinetics of the compound. Small-molecule, molecularly targeted anti-cancer agents are a class of drugs that have pH-dependent solubility and can be negatively affected by the effects of acid-reducing agents.20 Moreover, many cancer patients on a drug regimen consisting of these anti-cancer medications are also on some type of acid-reducing agent to mitigate adverse gastrointestinal side effects as a result of their disease or treatment.21 Furthermore, the potential for DDIs is heightened given the high availability of acid-reducing agents over the counter, combined with the frequency of the practice of poly-pharmacy in any given patient population. Therefore, we hypothesize that the use of BHCl can be a viable strategy to improve the reduced drug absorption of these anti-cancer agents when given under drug-induced hypochlorhydria.

A clinical study in healthy volunteers is currently ongoing in our laboratory, investigating the use of BHCl and its ability to improve dasatinib (Sprycel®) absorption under drug-induced hypochlorhydria (National Clinical Trials ID: #NCT01398046).

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