Fat Loss Supplements

This is another excerpt from the forthcoming book on women’s physiology, training and fat loss (which is past the halfway mark on editing so please just be patient).   It is part of a longer chapter looking at general use supplements with sections on luteal phase specific supplements (including PMS), and supplements specifically for women entering menopause.  No joke.  So here’s an excerpt on fat loss supplements.

Fat Loss Supplements

Perhaps the single most popular, lucrative and marketed type of supplement is those aimed at fat and weight loss. It’s an industry filled mostly with nonsense and false claims with hundreds if not thousands of products having come and gone with little to no effect. This has led many to conclude, at least partially correctly, that there is no product that any impact on fat loss. But this is a little bit too extreme of a conclusion.

There are absolutely compounds that have been shown to have some effect on one or another component of fat loss. Some increase energy expenditure, some help to blunt appetite, some do both. None of them can or will ever make up for a proper diet and exercise program and at most they add only a small amount to the overall results. Absolutely none of them are required for fat loss but they may be useful.

With one exception, all of the products that I’m going to talk about in this section fall under the general heading of thermogenics (24). This term refers to any compound or product that increases the body’s calorie expenditure, typically generating heat as a result. The overall impact of thermogenics is not enormous, potentially increasing energy expenditure by 5-10% depending on the product. Without any change in diet or exercise, the impacts are fairly meaningless.

But added to a proper diet and exercise program, this increase can not only enhance the overall results but help to offset some of the normal diet related reduction in metabolic rate. These compounds have also been shown to improve long-term weight maintenance, once again by helping to offset the normal drop in energy expenditure. This can allow more food to be eaten when the diet is over without fat gain occurring.

Most of these compounds also help to control hunger to one degree or another, through various mechanisms. Most raise DA levels in the brain and part of their effect may be through an impact on NEAT; people move around more on stimulants and that’s part of the extra calorie burn.

Most thermogenics are stimulants which means that they all can cause some slight side effects, typically an increased heart rate or blood pressure. Taken late at night, many will interrupt sleep as well. They also make some people simply feel jittery. These effects typically go away fairly rapidly, however.

But the potential risk is there. When you add to that the general attitude that more is better when it comes to fat loss, there can be problems. A number of highly publicized deaths from one of the compounds I’ll talk about below, for example, came from people taking three times the recommended dose and it’s the abuse that causes the problems.

Because of this, in many cases, I will recommend starting with a lower dose than is considered optimal initially. This is to assess individual tolerance to the compounds as this can vary wildly. Some people get incredibly jittery and uncomfortable from certain compounds while others feel nothing. But it’s always going to be better to err on the side of too little to begin with. If the lower dose is tolerated, the optimal dose can be approached gradually. But it should never be exceeded. More is not better and when you are dealing with products with any potential risk, that holds even more.

Caffeine

Caffeine is probably the most used compound in the world and even by itself can have a number of positive metabolic effects. By itself caffeine increases energy expenditure and 600 mg/day will burn about 100 extra calories per. This isn’t a huge amount but it does add up over time. Coffee also has it’s own health benefits, due to the other non-caffeine compounds, but realize that there are only about 60 mg of caffeine in the average cup of coffee (25). So it takes quite a lot to get 600 mg of caffeine.

A problem with coffee is the common tendency for people to add all kinds of high-calorie toppings such as whip cream, chocolate, etc. at gourmet coffee shops. This turns and effectively zero calorie drink into one containing hundreds of calories. Going back to my comments about food mis-reporting, most have no idea of the actual calorie counts of these types of drinks. Even the small amounts of cream and/or sugar that are added can add up across a large amount of coffee per day; this easily overwhelms any metabolic effects

Unless someone has never taken caffeine before, it is unlikely to cause any real side effects. However, caffeine metabolism does change in women over the course of the menstrual cycle as I mentioned. During the luteal phase, while women are less sensitive to caffeine is stays in the body longer. To ensure proper sleep, caffeine may have to be stopped earlier in the day. Due to their high progestin content, birth control appears to have the same effect on overall caffeine metabolism (26) and the same comments apply. Caffeine may also increase the cortisol response to stress so overuse should be avoided.

Females trying to put themselves through extreme dieting with excessive calorie reductions or enormous amounts of activity often end up living on diet sodas to try and keep their energy up during the day. Given that cortisol is already elevated in this situation, this type of caffeine abuse may be making the problem worse in the long run. There is also some indication that caffeine can make symptoms of PMS worse (certainly the suggestion to reduce intake during the final days of the luteal phase have been made) and women with more severe symptoms may wish to reduce their intake until menstruation.

It’s difficult to give an actual recommendation for daily caffeine intake. Given what I’ll discuss regarding some of the other thermogenics, most of which work better with caffeine, an upper limit of 400-600 mg/day or less might be considered an upper limit with less than this being allowed during PMS. A typical cup of coffee is about 60 mg, a diet soda is about 30mg of caffeine and some of the extreme energy drinks can contain up to 400 mg of caffeine. The typical caffeine pill is 200 mg. So a 400-600 mg/day limit could be 2-3 pure caffeine pills, up to 10 cups of coffee per day and nearly double that much diet soda (which I think most would consider excessive).

Capsicum/Hot Pepper

Capsicum is the active compound in hot peppers and has small effects on energy expenditure, fat mobilization and fat burning. Taken before exercise is can increase the use of fat for fuel and may even be able to activate the beige/brown fat I mentioned in a previous chapter. It’s effects are very short-lived however, at most a few hours. Unlike the other compounds in this section, capsicum has no stimulant effects although it makes people feel warm.

Since it is part of food preparation, it’s not uncommon for capsicum to be eaten with food although how much is actually used is highly cultural. In India, for example, the intake of capsicum is as high as 25-100 mg/day while it may be as low at 1.5 mg/day in other countries. There also appears to be ethnic differences in the maximum tolerable amount of capsicum that can be taken per dose. Simply, people raised on hot peppers can more easily eat them than those who are not.

The potency of capsicum is measured in Scoville Heat Units (SHU) which can range from 0 (for a bell pepper) up to 1,600,00 (for something called a Carolina Reaper). Cayenne pepper is between 30,000-40,000 SHU and commercial supplements are typically in this range. Amounts used in studies are in the 2.5-10 mg/day range which would equate to roughly 3-10 grams of whole peppers.

For those not culturally acclimated to eating hot peppers, isolated supplements would be a better choice since. One note of warning: anyone who has problems swallowing pills needs to be very careful with cayenne supplements. The a pill gets stuck in your throat and dissolves, you will have a very bad time when the powder is released.

Green Tea/Caffeine

Green tea, or rather it’s active ingredient EGCG (don’t ask what this stands for) is another mild thermogenic compound. and may be a better choice for people compared to the next two supplements. The effects of EGCG, and it works far better with caffeine, are mild, raising energy expenditure by about 5%. It also doesn’t seem to have a huge stimulant effect overall.

Theoretically it is possible to consume enough EGCG in brewed tea but it takes and absolutely enormous amount to get effective amounts. An isolated green tea/EGCG supplement is usually superior for this reason. The recommended dose is 130-160 mg of EGCG . with 100 mg of caffeine taken up to three times per day (a typical dosing schedule would be 8am, 12pm and perhaps 4pm).

That means that a total of 390-480 mg EGCG and 300 mg caffeine total could be taken per day and would be taken. Different herbal supplements are standardized differently so you’ll have to read the label to see how much active EGCG is actually present.

Nicotine/Caffeine

I suspect that many readers will have a fairly strong response to my inclusion of nicotine in this book as a fat loss aid due to it’s association with smoking (and those associated health risks). But it’s important to realize that isolated nicotine, in patch or gum for, is far different than smoking itself. The other hundreds or thousands of chemicals found in cigarettes (which are what cause the major problems) aren’t present.

And isolated nicotine with caffeine has been studied for it’s thermogenic and fat loss effects. Like green tea the effect of nicotine and caffeine is fairly small with an increase of perhaps 5% in metabolic rate. As importantly, the combination of nicotine and caffeine has been reported to have a profound impact on blunting hunger and appetite.

The effects of nicotine and caffeine are fairly short lived, perhaps 2 hours. But this, in addition to being less stimulatory than other compounds, makes the combination of nicotine and caffeine potentially useful at night when hunger can be a problem. A dose can be taken during the trouble times but will stop having an effect in time for sleep. The effective dose is 1 mg of nicotine with 100 mg of caffeine.

Ephedrine/Caffeine

The final thermogenic compound I want to discuss is the ephedrine and caffeine (or EC) stack and this is another topic I suspect many readers will have somewhat of a reaction to. EC was insanely popular in the 90’s and, due to misuse there were a handful of deaths attributed to it. But this was always associated with overdosing of some sort or combining it with something else (raver kids combined it with alcohol and other drugs). For this reason, herbal products containing ephedra or mahuang, were pulled from the market.

At the same time, EC has been extensively studied for over two decades and no problems were ever encountered except for the small increase in heart rate and blood pressure, both of which go away quickly. The problem was invariably, mis-use. But used intelligently, EC has a stunning number of potential benefits for both weight/fat loss and maintenance.

Of all of the compounds I’ve discussed, EC has the most potent effect, raising energy expenditure by 5-10% over normal. This helps to offset the drop that occurs with dieting or will increase the total amount of fat loss that occurs in the beginning stages of the diet. EC blunts appetite, increases fat burning and improves many types of exercise performance (27). Athletes do need to be aware of the potential for cramping and EC will raise body temperature. Female endurance athletes, especially during the luteal phase, need to be aware of the potential for overheating. EC is also banned in many sports federations.

Getting back to fat loss, ephedrine is unique among fat loss treatments in that regular use appears to increase rather than decrease it’s effects (28). Almost all other fat loss drugs lose effect with chronic use but EC does not, it works better. The mechanisms behind this are currently unknown but may have to do with EC increasing the amount or activity of the beige/brite fat I mentioned earlier in this book. EC may also help with long-term weight maintenance; by helping to offset the normal decrease in metabolic rate that occurs with weight loss, the risk of weight/fat regain is at least lessened.

Like other stimulants, EC will raise DA levels in the brain and this would be expected to not only help with cravings but might also help to increase NEAT. Many people get a little bit hyped up on EC and move around more and that alone probably contributes to it’s calorie burning effects.

The biggest potential drawback to the EC stack is that it is a potent stimulant, raising both heart rate and blood pressure. As I mentioned, this goes away fairly quickly but women in Category 3 are often starting off with elevated blood pressure and raising it more could be problematic. Unless someone has used the EC stack and knows their personal response to it, I will always recommend starting with a lower dose to assess tolerance before moving up. I’ll provide specific recommendations below.

Recommendations

It was determined fairly early on that the optimal dose of ephedrine and caffeine were 20 mg ephedrine and 200 mg of caffeine and this was generally given three times per day in research. Typically EC is used at perhaps 8am, 12pm and again at 4pm. Taking it much later than this tends to interrupt sleep and some can’t even take the 4pm dose at all. This is potentially a problem during the luteal phase or for women on BC due to the slower clearance of caffeine but is highly individual.

While the above might represent an optimal dosing schedule, I recommend that anyone who has never used EC before start with a single half dose in the beginning. So 10 mg of ephedrine and 100 mg of caffeine would be taken in the morning to assess tolerance (and ensure that it doesn’t interrupt sleep). Being jittery with a racing heart are common here and these are the major side effects to watch for.

If any major side effects are noticed, the combination should be discontinued immediately. If not, either a second half dose can be added at lunchtime or the morning dose can be moved up to the full 20 mg/200 mg dose of ephedrine and caffeine. If that is well tolerated, after a few days, the dose and frequency can be increased further.

For the most part, the herbal forms of ephedrine are not widely available. When they are they always contain ephedra/mahuang with some type of herbal caffeine such as kola nut. The herbal forms tend to have more side effects and I would generally recommend the pure ephedrine HCL form if it is available.

Ephedrine is not legal for sale in all countries but when it is it will be found with the asthma medications. In the US, Bronkaid is a common brand and in the UK, Chesteeze is commonly found. Most modern ephedrine products also contain something called guaifinesin; this is an expectorant (it makes you cough) that is put there so that the product can’t be used to produce methamphetamine.

Doses of ephedrine can vary with 20-25 mg pills being available. Occasionally doses are limited to 8mg per pill which means that either 2 pills (16 mg) or 3 pills (24 mg) should be taken. Caffeine should be sourced separately and caffeine pills are usually the easiest to use here; it would take 3 strong cups of coffee to get enough caffeine.

In the early days of research into EC, it was thought that aspirin had an additional benefit (some readers may remember the ECA stack) but aspirin is rarely used anymore. It has a small extra effect in the obese but there is a potential problem with taking 300 mg of aspirin up to three times per day. I don’t recommend aspirin be used for the EC stack for this reason.

One issue that comes up with the EC stack is when to introduce it into a diet. Some prefer to add it right at the start to increase fat loss but others prefer to save it until later in the diet when hunger is increasing and metabolic rate is slowing and both are potentially useful. For shorter diets, starting EC right at the beginning makes the most sense but dieters (usually in Category 1) who are looking at very extended dieting periods may wish to wait until perhaps halfway into their diet to introduce the stack. This can help to maintain a sufficient deficit without having to cut calories or add even more exercise.

Let me reiterate that, like every other product in in this section, ephedrine and caffeine is by no means required on a diet. It’s impact can be significant and noticeable but the side effects can be very real. Any reader with any hesitation about using the EC stack simply shouldn’t and I’ll mention this again in the diet and training templates.

Yohimbine

The final compound I want to talk about is not a true thermogenic in that it doesn’t raise metabolic rate or energy expenditure. But it does have potential use for Category 1 dieters. It actually doesn’t have any benefit for anybody else and Category 2 and 3 dieters shouldn’t consider it. Earlier in the book, I talked about women’s hip and thigh fat and how part of the reason it is so difficult to mobilize (among other reasons) is the ratio of beta-2 (which mobilize fat) and alpha-2 (which inhibit fat mobilization) receptors.

As it turns out, yohimbine is a natural inhibitor of the alpha-2 receptors (29). This may be a little bit confusing but by inhibiting an inhibitor, the overall effect is to increase fat mobilization. Think of it like a double negative, or taking your foot off the brake in your car. By removing the normal inhibition on fat mobilization, it increases.

has some use for Category 1 dieters. It actually has no benefit for anybody else and anybody in Category 2 or 3 shouldn’t even consider it. I talked earlier in this book about how women’s hip and thigh fat has a large number of alpha-2 receptors which inhibit fat mobilization, making the burning of this fat more difficult. Well yohimbine is a natural blocker of those alpha-2 receptors (21). And by inhibiting the inhibitor, this has the consequence of increasing fat mobilization. It’s a double negative, like taking your foot off the brake in a car.

Since yohimbine is not for everyone for various reasons, I’ll provide some other strategies to work around the normal difficulty in Appendix 2. Some of them are based around diet and there are effective ways to structure cardiovascular exercise go get around this. But yohimbine, combined with caffeine can do this by itself. But only if it is combined with completely fasted aerobic exercise.

Small amounts of insulin completely inhibit the effects of yohimbine and fasted here means fasted. If coffee is being used for a caffeine source, it should be consumed black. No creme, no sugar. Completely fasted. Aerobic activity must be done after taking yohimbine or the mobilized fat will just be stored again. Yohimbine tends to increase heart rate during exercise and it may be higher than normal at the same levels of workout intensity.

For Category 1 dieters who simply can’t do morning fasted cardio for some reason, yohimbine can still be used. So long as it it taken at least 3-4 hours after a meal, the effects will still occur. Many will be performing aerobic activity after weight training. Since it takes about an hour for the effects of yohimbine to be felt, it should be taken so that it is hitting the system when the aerobic training will start. So if an hour weight workout is being done, take the yohimbine at the very beginning of the workout. The combination of yohimbine and weight training tends to make people feel awful which is why I suggest this timing method.

Yohimbine builds up in the body over time and will have a greater effect with regular use. When female category 1 dieters have reached the high teens for BF%, which is usually when the upper body is starting to get very lean but the hips and thighs may not be, adding yohimbine may be useful. I should mention that yohimbine can also cause water retention which can make it looks as if the diet isn’t working like all other types of water retention.

What is often seen, even if weight isn’t changing, is that the fat gets squishy and dimply in contrast to it’s normal hard as a rock texture. Invariably in this case, when the whoosh happens, the area will show a visual improvement in appearance. Dropping yohimbine for even a few days tends to cause this to occur and anyone using yohimbine for a physique contest should drop it a minimum of 7 days before a show.

During cardio, many report feeling a tingling feeling in their lower body fat (men who use yohimbine get this in their abdominal or lower back fat) which I suspect is due to increased blood flow, which yohimibine also impacts. This isn’t universal and a lack of tingle shouldn’t be taken as an indication that it isn’t having an effect.

The recommended dose of yohimbine is 0.2 mg/kg (0.9 mg/pound) so a 150 pound female would use 16 mg taken with 100-200 mg of caffeine. Yohimbine is limited to 2.5 mg per pill and that would mean 5 total pills and the amount would be rounded up if the dose doesn’t work out exactly. There is a herbal form of yohimbine called yohimbe or yohimbe bark but I do not recommend this. It tends to cause enormous side effects where folks get chills and sweats at the same time. Either find a pure yohimbine or don’t use it.

You may see it written on bottles of yohimbine that women should not use the product but this is due to an old misconception which was that yohimbine has hormonal effects. Early on yohimbine was found to help with erectile dysfunction in men and it was simply assumed that this was due to an elevation in testosterone. But this is not true. Yohimbine simply increases blood flow to the genitals; it does the same thing in women so your hip and thigh fat may not be the only place that tingles during exercise.

Finally, high doses of yohimbine are used to trigger anxiety attacks in research and any female with even the slightest propensity towards them should absolutely not use yohimbine. The potential negatives are far too high for the benefits and there are other ways to mobilize stubborn fat without it.

And with that I’ll wrap up thermogenics and other fat loss supplements. Please safely assume that any product that is not included on this list has no effect and is worthless. This would include garcinia cambogia, rasberry ketone and a host of others that are so often sold but do nothing. And once again realize that none of the above is in any way required for fat loss. They can be helpful and useful in conjunction with a properly set up diet and exercise program. But they can’t ever replace it.

References

24. Diepvens K Obesity and thermogenesis related to the consumption of caffeine, ephedrine, capsaicin, and green tea. Am J Physiol Regul Integr Comp Physiol. 2007 Jan;292(1):R77-85.
25. Greenberg JA et. al. Coffee, diabetes, and weight control. Am J Clin Nutr. (2006) 84(4):682-93.
26. Abernethy DR, Todd EL.Impairment of caffeine clearance by chronic use of low-dose oestrogen-containing oral contraceptives. Eur J Clin Pharmacol. 1985;28(4):425-8.
27. Magkos F1, Kavouras SA.Caffeine and ephedrine: physiological, metabolic and performance-enhancing effects. Sports Med. 2004;34(13):871-89.
28. Astrup A Enhanced thermogenic responsiveness during chronic ephedrine treatment in man. Am J Clin Nutr. 1985 Jul;42(1):83-94.
29. Lafontan M et. al. Alpha-2 adrenoceptors in lipolysis: alpha 2 antagonists and lipid-mobilizing strategies.Am J Clin Nutr. 1992 Jan;55(1 Suppl):219S-227S.

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