The Most Dangerous Drugs, Part 2

Pharmaceutical diuretics are often classified by which kidney function they affect. All, however, work by purging the body of (mainly) sodium. Since a teaspoon of sodium holds more than two quarts of water in the body, eliminating it helps release a huge volume of water—but that approach is a biochemical shotgun, as other essential minerals also wash away, including magnesium, chloride and potassium. Loss of those vital electrolytes, as they’re called, leads to potentially serious problems, besides the excessive loss of water, which can rapidly induce dehydration. The effect is even more pronounced in bodybuilders because they are often dehydrated to begin with due to water restriction and certain dieting methods that lead to water loss, such as low-carb diets.

The most common diuretic drugs used in bodybuilding and other sports are thiazide diuretics, such as Diuril; loop diuretics, such as Lasix; and potassium-sparing diuretics, such as spironolactone, or Aldactone. Bodybuilders often use combination diuretics, such as Aldactazide, which combines a potent thiazide diuretic with the potassium-sparing Aldactone. That type of combination lets you use lower doses of the drug and partially prevents the potassium loss that would otherwise ensue. The loop diuretics, so named because they work in a section of the kidneys called the loop of Henle, are the most potent. Lasix, besides helping release all those minerals, also brings on calcium loss, making it a prime cause of severe muscle cramps, unless it’s taken with supplemental minerals.

Lasix and other diuretics have a few other quirks. For example, Lasix works very rapidly, and it’s out of your body in about four to six hours. Your body, however, quickly senses the extreme loss of water induced by Lasix. That, in turn, leads to a rapid water rebound as soon as the Lasix is gone. The body often compensates for the loss of water by retaining water. Many bodybuilders who’ve been told to use Lasix the day prior to a contest have found out the hard way about the Lasix rebound effect, as they appeared waterlogged onstage. Injectable Lasix should be strictly reserved for a hospital setting. It’s simply too potent and unpredictable. Just ask Paul Dillett.

Bumetanide, trade name Bumex, is a second-generation loop diuretic. While Lasix is only 60 percent absorbed in the small intestine, Bumex features an 80 percent absorption rate and can be taken with food. It’s 40 times more potent in its diuretic activity than Lasix, making it even more dangerous if misused. Bumex turned out to be the secret ingredient in a popular weight-loss supplement called StarCaps. Of course, weight lost with that supplement consisted entirely of water. Bumex is excreted even faster than Lasix is, thus increasing the chances of a rapid water rebound.

Thiazide diuretics can cause insulin insensitivity and raise blood glucose. They make your body photosensitive, which means if you use them before lying in the sun or using a sun bed, the UV rays will be concentrated on your skin and can result in a severe burn or rash. Taking supplemental potassium with potassium-sparing diuretics can elevate blood potassium. Consider that in executions, potassium is injected into the heart, causing it to stop immediately—so you see what high concentrations of blood potassium can do. Potassium-containing foods are okay, just no concentrated supplemental potassium with any potassium-sparing drug, including the combination drugs such as aldac-tizide. Non-steroidal anti-inflammatory drugs, often used to treat joint and muscle pain, block the diuretic effects of Lasix and other loop diuretics.

The loss of potassium caused by diuretics can lead to muscle weakness, fatigue, pain and muscle destruction. If you replace potassium, you also need to take magnesium, which is lost through diuretic use. Without magnesium you don’t retain potassium in the cells. Women who use anabolic steroids often use Aldactone, as it can block androgen cell receptors, leading to fewer androgenic side effects, such as facial and body hair growth. In men anabolic steroid use can result in gynecomastia, or male breast formation.

There are some natural ways to dump water from the body. A few years ago sodium loading was popular. As the name implies, you take in large amounts of sodium a few days prior to a contest. A day before the contest, you curtail sodium intake. The technique was thought to work because large doses of sodium blunt the release of the adrenal hormone aldosterone, which retains sodium in your body. If you timed it right, the body would react by releasing large volumes of water but allow enough water retention to prevent a flat appearance and promote vascularity. If you either timed it wrong or ate a bit too much sodium on the minimal day, however, you wound up appearing bloated. (Incidentally, carbohydrate loading is also a popular precontest technique, involving first limiting, then loading up on carbs the week prior to a contest. The high-carb intake, however, also leads to insulin release, which results in aldosterone release. So if you also take in a lot of sodium during the carb-loading phase, you end up looking quite bloated by contest time.)

Some bodybuilders use diuretics to offset the water-retaining effects of anabolic steroids. Many such drugs inhibit the enzymes that cause the adrenal glands to produce more water-retaining hormones. In other cases the steroids may convert into estrogens, which typically help push intracellular water into the extravascular space—such as just under the skin. A high estrogen environment also leads to aldosterone release and water retention, as any woman who suffers the notorious monthly bloat can readily attest.

Growth hormone is a potent water-retaining hormone because it directly brings on aldosterone release. Using GH too close to a contest can cause bloating that is often blamed on something else. Taking high-dose steroid combinations can displace estrogen from its protein carrier in the blood, resulting in higher levels of free, or active, estrogen. Using drugs that block aromatization will do nothing to prevent that, but using a receptor blocker, such as Nolvadex, will.

There are natural methods that can help reduce excess water retention. They include the following:

• Low-carb dieting. Low-carb diets cause the loss of glycogen, which is stored with nearly three grams of water per gram of glycogen. Most of the initial weight loss with low-carb diets results from glycogen depletion and water loss.

• Drinking water. As paradoxical as it may seem, withholding fluids leads to water retention. In contrast, drinking copious amounts of water inhibits the release of antidiuretic hormone, resulting in water loss.

• Aerobic exercise. It’s not only sweating that causes water loss. Doing aerobics leads to the release of atrial naturetic peptides, which are heart proteins that cause water loss as well as fat oxidation during exercise. More on that in a future column.

• Water-soluble vitamins. They include vitamin C and the B-complex vitamins. Large doses induce rapid excretion of water.

• Potassium-magnesium. These minerals not only prevent diuretic-related side effects but also bring on sodium loss. Taking half the dose of potassium in relation to sodium prevents sodium water retention and blood pressure effects.

• Sauna. Leads to a temporary water loss that can quickly be replenished with normal fluid intake.

• Coffee/tea/alcohol. In small doses, all help you lose fluid through various mechanisms.

• Plant-based diuretics. Often sold as over-the-cover supplements, they’re far milder in their effect than drug versions. One recent study showed the effectiveness of a common ingredient in such natural diuretics, namely dandelion.¹ The French refer to dandelion as pissenlit, a wry reference to its diuretic activity. A notable advantage of dandelion is that it provides antioxidant effects and naturally contains such minerals as magnesium and potassium.

Rumors abound about pro bodybuilders clandestinely using designer diuretics that don’t show up in standard drug-testing procedures. If a bodybuilder appears to have noticeably shed water weight between the prejudging and finals of a contest, which can involve anything from a few hours to a day, odds are good that he or she used a diuretic. Considering the danger inherent in these drugs, it’s only a matter of time before some competitor experiences side effects that could range from mildly annoying, such as onstage muscle cramps, to more serious, including cardiovascular collapse. I’d wager that’s already happened a few times, despite the “ironclad” drug tests currently in use.

¹ Clare, B.A., et al. (2009). The diuretic effect in human subjects of an extract of Taraxacum officinale Folium over a single day. J Alt Comp Med. 15:929-34.

Editor’s note: Jerry Brainum has been an exercise and nutrition researcher and journalist for more than 25 years. He’s worked with pro bodybuilders as well as many Olympic and professional athletes. To get his new e-book, Natural Anabolics—Nutrients, Compounds and Supplements That Can Accelerate Muscle Growth Without Drugs, visit www.JerryBrainum.com. IM