Ephedrine and its parent herb, mahuang, are two of the most popular and effective thermogenic food supplements available—but perhaps not for long. Reports concerning the alleged dangers of ephedrine use are appearing regularly in mainstream media, and the deaths of several high-profile professional athletes who used ephedrine supplements have added to the impetus to remove ephedrine and mahuang from over-the-counter sales due to their inherent “toxicity.”
Those reports imply that ephedrine is a dangerous and unpredictable substance for everyone, but that simply doesn’t jibe with most available scientific evidence on ephedrine. In fact, as I’ve said in this column before, most cases of serious health problems involving ephedrine or mahuang are due to idiosyncratic reactions. In short, many of the people who experience serious side effects from using ephedrine or related compounds do so because of either existing health problems that contraindicated the use of ephedrine or from using too high a dose.
Ephedrine is a sympathomimetic drug, meaning that it acts similarly to or promotes the release of sympathetic hormones in the body, such as epinephrine and norepinephrine. Those hormones are also known as “fight-or-flight” hormones because of the reactions they promote during stress, including higher blood pressure due to vascular constriction, release of glucose and release of fat into the blood. A healthy person can easily tolerate those effects, but for someone who already has cardiovascular disease, such reactions could prove dangerous, particularly if he or she used too high a dose.
Since ephedrine shares some properties of other substances known to affect brain function, such as cocaine and amphetamine, it’s reasonable to assume that ephedrine affects behavior. Higher doses of ephedrine produce mental effects that in a broad sense mimic the effects of amphetamines, although published research shows that ephedrine doesn’t share the addictive potential or the immediate cardiac and brain toxicity linked to amphetamines.
People who are unaffected by mental illness experience a slight sense of euphoria coupled with a feeling of heightened energy when they use ephedrine. That effect is amplified in the mentally ill, who often overdose on ephedrine-containing supplements, since they’re more readily available than cocaine or amphetamines. In fact, ephedrine is so close in structure to amphetamines that if a person takes it before a drug test, he or she will test positive for speed. A follow-up test can distinguish the two drugs.
Recent reports in the medical literature cite adverse mental effects supposedly induced by ephedrine. One report described a 19-year-old man who suffered from decreased sleep, increased aggression and disorganized behavior after using two of the most popular ephedrine-containing food supplements.1 He was using so much of the supplements that he decided to open up the capsules and snort them like cocaine. Yet he was described as having no previous psychiatric history.
In another case a 21-year-old man took increasing doses of a popular thermogenic supplement and soon developed mania and psychosis, along with delusions. No dosages were mentioned, other than that he increased the dose regularly. A brain scan showed cerebral atrophy—not a usual finding in someone his age—a condition that could cause adverse mental symptoms.
Previous reports linking ephedrine to mental problems show that the typical dose used before symptoms occurred was 510 milligrams daily. Contrast that with the maximum suggested safe dose of 90 milligrams a day or the typical 25 milligrams found in a single capsule of most ephedrine supplements. The symptom most commonly linked to ephedrine use appears to be mania, and again, in nearly all cases the people had the condition before they took any ephedrine or mahuang supplement. In most cases they overdosed, which could cause similar problems in anyone. As the saying goes, “Only the dose determines the poison.”
Another recent case study documented a rare possible side effect of using ephedrine: priapism.2 That’s an extended, involuntary penile erection. It sounds good initially, until you realize that erections are the result of trapped blood that, if not released within a certain time, can cause serious damage and, paradoxically, lead to loss of sexual function.
Those case studies involved the use of cocaine and ephedrine supplements, though not at the same time. Cocaine causes priapism by inhibiting the reuptake of norepinephrine, which extends the vasoconstrictive activity of sympathetic nerves. Interestingly, using cocaine often leads to temporary impotence because an erection depends on an orderly balance between the parasympathetic and sympathetic nervous systems. Initially, the parasympathetic system is dominant, promoting erection by dilating blood vessels in penile tissues. Once the penile tissues are engorged with blood, the sympathetic system takes over to constrict the blood vessels, in effect trapping the blood in penile tissues to maintain the erection. Under normal circumstances the vasoconstriction is abated by the muscular pelvic contractions and rapid release of trapped blood that are linked to orgasm. But coke and ephedrine can block that effect, keeping the tissues engorged and causing the uncomfortable effect of being sexually aroused yet unable to perform. (I’ve always wondered why they refer to sex as a “performance.” Perhaps it’s connected to the reason gonorrhea is called “the clap.”)
In the cases described in the study, men who used OTC ephedrine supplements experienced erections that lasted seven and nine hours. Ouch, that ain’t no Viagra!
Nevertheless, the cases must be considered idiosyncratic, since many men use the same ephedrine supplements with no evidence of prolonged, painful erections. The men involved in the studies may have had hidden health or circulatory problems that made them particularly susceptible to that effect. After all, if this were a common occurrence, it would have no doubt received a great deal of publicity.
Amid the reports in the scientific literature of ephedrine’s adverse effects, a positive study emerges.3 Thirteen male subjects took in caffeine (four milligrams per kilogram of bodyweight), ephedrine (0.8 milligrams per kilogram of bodyweight), a combination of ephedrine and caffeine or a placebo. Ninety minutes later they did three sets each of leg presses and bench presses.
Those on either the caffeine-and-ephedrine combo or the ephedrine alone showed increased muscular endurance, but only during the first set of each exercise. The subjects on the supplements lifted more weight than those on the placebo on all three sets, and the blood pressure of those using the ephedrine increased before training. They showed a 48 percent improvement on the leg press and a 16 percent improvement on the bench press that would normally have taken four to 12 weeks of training to achieve. The researchers noted that caffeine plus ephedrine didn’t do anything for the subjects that ephedrine didn’t accomplish by itself, which contradicts recent statements that ephedrine doesn’t provide any ergogenic benefits.
Insulin Abuse
If you’d asked competitive bodybuilders 20 years ago about the possibility of injecting insulin as an anabolic drug, most of them would have said that insulin is for diabetics only. Indeed, insulin does treat diabetes, which comes in two forms. Type 1 diabetes is characterized by a complete failure of the beta cells of the pancreas to synthesize insulin. That’s why people who have that form of the disease must use insulin injections. Type 2, or adult-onset, diabetes, so named because it most often becomes apparent after age 40, may be controlled with other drugs, along with weight loss and proper diet, although in some cases insulin is required for maintaining normal blood glucose levels.
Insulin is vital for several aspects of nutrient storage and processing. It’s required for glucose uptake into cells and aids in amino acid entry into muscles. Insulin promotes the activity of glycogen synthetase, the rate-limiting enzyme for glycogen synthesis. On the dark side, insulin is the most potent fat-promoting hormone in the body.
Bodybuilders and other athletes use insulin for several purposes. It promotes rapid muscle glycogen storage, thus increasing energy stores and muscle fullness. Its role in amino acid uptake is key because the aminos are used for muscle protein synthesis reactions, and it provides an anticatabolic effect in muscle, preventing excessive muscle tissue breakdown.
Insulin also is synergistic with other anabolic hormones, such as testosterone and growth hormone. In fact, the combination of those three hormones is chiefly responsible for the massive appearance of today’s professional bodybuilders. All three hormones amplify one another’s anabolic effects. Unfortunately, that same combination is also responsible for the bloated abdomens that are so frequently seen on bodybuilders today. The combination of insulin and IGF-1 (from GH use) appears to foster internal organ growth and a thickening of the abdominal wall musculature.
Various forms of insulin are available without a prescription, to make it convenient for diabetics to obtain required medication. Athletes favor two types of synthetic insulin, both which are produced with recombinant DNA technology: Humalog, a quick-acting form that peaks in two hours and is out of the body by the four-hour mark, and Humulin-R, which also acts rapidly and is out of the body in six to eight hours. As a polypeptide composed of long chains of amino acids, insulin is always injected; taking it orally would lead to rapid inactivation. Insulin must also be injected subcutaneously, or right under the skin. Users rotate injection sites.
A full cc of insulin equals 100 I.U., and the doses used by bodybuilders average 1 I.U. per 15 pounds of bodyweight. The usual suggested protocol involves taking a minimum of 10 grams of simple, or rapidly acting, carbohydrates within 20 to 30 minutes of the insulin injection. Not following the carb protocol can lead to rapid hypoglycemia, or a drop in blood glucose levels. Symptoms include sleepiness, drowsiness, hunger, blurred vision, dizziness, sweating, slurred speech, inability to concentrate, tingling in hands and feet and other effects. If a simple sugar isn’t immediately ingested when those symptoms arise, the brain is deprived of its primary fuel—glucose—and coma can ensue.
Several bodybuilders have fallen into comas through injudicious use of insulin. In the most recently reported case in the medical literature, a 31-year-old bodybuilder went into a coma after switching to a rapidly acting insulin injection.4 He had previously used longer-acting forms of insulin and was apparently unaware that he needed a timely and correctly proportioned infusion of simple carbs. In another case a 21-year-old bodybuilder suffered severe brain damage after using insulin.5
“Incorrectly administered, insulin can kill you stone dead or leave you as a vegetable,” notes Peter Sonksen, a British medical researcher.
As for when to use insulin, for those of you intrepid or foolish enough to consider it, the best suggested times are first thing in the morning and following an intense training session. During those periods levels of cortisol, the primary catabolic hormone in the body, are high, and insulin opposes its effects.
You should also be aware that a hyperinsulinemic environment, or elevated insulin levels, has serious long-term health consequences, besides the considerable immediate dangers already cited. Elevated insulin promotes a process in the body known as glycation, or sugar deposition in tissues, thought to be one of the primary causes of aging. Diabetics, whether on insulin therapy or not, are known to age at an accelerated rate. Recent animal-based studies show that lifelong insulin control may be a key factor for healthy aging and maintenance of vigor with passing years.
One study shows that insulin use promotes the oxidation of low-density lipoprotein (LDL), the bad kind of cholesterol.6 That would promote atherosclerosis and subsequent cardiovascular disease. Another study shows that using large doses of insulin can cause a vasospasm in the coronary arteries, resulting in a heart attack.7
A study published earlier this year points to the possibility that high insulin levels are related to the onset of Alzheimer’s disease.8 The mechanism involves increased release of and inhibited degradation of beta-amyloid protein, which builds up in the brains of people afflicted with the disease and is thought to be a root cause of Alzheimer’s. Oddly enough, insulin appears to increase memory function in younger people, but a researcher involved in the study said that “high insulin levels are bad for your brain as well as your body.” By the way, the doses of insulin used in that study were higher than diabetics use but comparable to what’s suggested for “anabolic” effects in bodybuilders.
The one aspect of insulin use that I find curious is that in the usual protocols suggested for athletes, there’s never any mention of amino acid use with the drug. Yet evidence clearly shows that insulin promotes muscle protein synthesis only in the presence of elevated amino acid levels. So it would appear prudent to take amino acids—not a whole-protein source—with simple carbs shortly after a rapidly acting insulin injection, since the insulin will “push” those aminos directly into muscle, producing a pronounced muscle protein synthesis effect.
You should also be aware that if you’re already insulin-insensitive from carrying too much bodyfat, the insulin-and-simple-carb protocol will make you appear about as muscularly defined as John Goodman. Using insulin and high simple carbs under that condition is tantamount to attempting to put out a fire with gasoline. Recall that insulin promotes bodyfat synthesis by turning on every system in the body for that purpose while simultaneously turning off fat-oxidizing systems. The lesson here is to avoid even considering using insulin—unless you are diabetic—until you diet and train away that excess bodyfat. Insulin is also a potent water- and sodium-retaining hormone, which may increase blood pressure in some people.
For those who—wisely—prefer to avoid using a drug as potentially dangerous as insulin, you can get a similar, if less dramatic, muscle protein synthesis effect simply by taking in a rapid-acting protein source (such as whey) with simple carbs immediately following a workout. That combination maximizes your own output of insulin, leading to increased amino acid uptake into muscle, coupled with quicker muscle glycogen replenishment. And the great part about it is that you don’t have to worry about falling into a coma.
References
1 Walton, R., et al. (2003). Psychosis related to ephedra-containing herbal supplement use. Southern Med J. 96:718-20.
2 Munarriz, R., et al. (2003). Cocaine and ephedrine-induced priapism: case reports and investigation of potential adrenergic mechanisms. Urology. 62:187-92.
3 Jacobs, I., et al. (2003). Effects of ephedrine, caffeine, and their combination on muscular endurance. Med Sci Sports Exer. 35:987-94.
4 Evans, P.J., et al. (2003). Insulin as a drug of abuse in bodybuilding. Brit J Sports Med. 37:356-7.
5 Elkin, S., et al. (1997). Bodybuilders find it easy to obtain insulin to help them in training. Brit Med J. 314:1280.
6 Quinones, A., et al. (1999). Evidence that acute insulin administration enhances LDL cholesterol susceptibility to oxidation in healthy humans. Aterioscler Thromb Vasc Biol. 19:2928-2932.
7 Kamijo, Y., et al. (2000). Myocardial infarction with acute insulin poisoning. Angiology. 51:689-693.
8 Watson, G.S., et al. (2003). Insulin increases CSF Ab42 levels in normal older adults. Neurology. 60:1899-1903.
©,2013 Jerry Brainum. Any reprinting in any type of media, including electronic and foreign is expressly prohibited.
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has recently emerged as the superstar amino acid, displacing such previous favorites as glutamine
and leucine
. That’s particularly interesting because L-arginine 
meaning one that must be provided in food. Like glutamine
: one that’s required in greater amounts during times of growth and stress.
. NO is both a gas and a free radical that is short-lived in the body but that performs myriad vital functions.
and obesity as humans—elevated blood glucose; elevated blood lipids, such as cholesterol
andtriglycerides
; elevated resting insulin levels; and dysfunction of the lining of blood vessels that leads to atherosclerosis, high blood pressure and cardiovascular disease.1 Researchers gave the fat, diabetic rats arginine because of the relationship between NO and fat metabolism
.
NO
rats, blood arginine
, but it doesn’t affect muscle protein breakdown, or catabolism.
, which is a primary inhibitor of fat oxidation in the mitochondria. That substance increases in the presence of carbohydrates, which explains why eating carbs just before training blunts fat burning during the workout. Specifically, malonyl coenzyme-A
blocks the enzyme that works with L-carnitine in shuttling fat into the mitochondria for oxidation purposes.
in the body.2 CRP is a general measure of inflammation in the body, and inflammation is the cornerstone of most serious diseases, including cancer and cardiovascular disease. Most supplements, even potent antioxidants such as vitamins C and E, have little or no effect on CRP. The effect on CRP may explain why eating nuts and fish protects the cardiovascular system; both foods are rich sources of arginine. Eating 3.6 ounces, or 100 grams, of walnuts provides 2.5 grams of arginine
.
is comparable to a health terrorist.