I. Drug History
Insulin is a proteinaceous hormone which is manufactured in the pancreas and which has a number of important physiological actions in the body. It's a polypeptide made from 51 amino acids, separated in an A and B chain by a sulfide bridge (Covalent bond). It is an essential hormone in maintaining the body's blood glucose level so that the brain, muscles, heart and other tissues are adequately supplied with the fuel they require for normal cellular metabolism and normal function. Insulin also plays an essential role in fat and protein metabolism. For example, it promotes transport of amino acids from the bloodstream into muscle and other cells. Within these cells, insulin increases the rate of incorporation of amino acids into protein (amino acids are the building blocks of protein) and reduces protein break down in the body ("catabolism"). These physiological actions probably form the basis regarding the additional anabolic gains which might be made through the use of exogenously administered insulin.
Normally, blood glucose and blood insulin levels are not both elevated for any extended period of time as these two chemicals influence each other through a feedback system in the body. In the post-absorptive state, the blood insulin concentration tends to decrease during exercise, allowing the blood glucose to be maintained at or above resting levels and to provide increased energy supplies (fuel) to muscle cells. Following a meal, the blood glucose and amino acid levels rise (the absorptive state) and this triggers an increase in insulin release from the pancreas, driving glucose and amino acids from the blood into cells and maintaining the blood glucose level within a certain physiological (operating) range.
Medically, Insulin is typically used in the treatment of diabetes. Diabetes is a disease that affects the body's ability to produce or respond to insulin, a hormone that allows blood sugar to enter the cells of the body and be stored or used for energy. Type 1 diabetes occurs when a person no longer is capable of making any insulin. This type of diabetes usually begins in childhood, adolescence, or young adulthood and requires insulin injections for treatment. Type 2 diabetes occurs when a person becomes resistant to his or her own insulin, thereby creating a need for greater amounts of insulin. This type usually happens after age 45. Type 2 diabetes is closely linked with obesity.
Bodybuilders use insulin due to the anabolic effect it can offer. With well-timed injections, insulin will help to bring glycogen and other nutrients to the muscle. Insulin can also help athletes' stamina by providing then with "fuel" - glycogen, which stores carbohydrate energy - by taking insulin and glucose.
At one time, all insulin was produced by laboratory animals, most often cows and pigs. In the last decade, however, American insulin manufacturers have almost completely shifted to use of "recombinant DNA" technology, enabling laboratory production of a close analog to real human insulin. This "human" insulin is said to more closely match our endogenous (pancreatic) insulin.
Although labeled much like "animal source" insulin’s, recombinant DNA insulin’s are not quite the same, either in time-of-onset or in amount of insulin required. Experience shows that any switch between the one and the other must be done with care, and under your doctor's supervision. Use human insulin rather than an animal insulin preparation if possible (there is little animal insulin available now).
There are three types of non-prescription insulin. Short-acting, “regular” insulin which is mostly used, commonly known as Humulin-R, also Actrapid, Insulin Neutral, Humulin R, Hypurin Neutral). These slower acting insulins effect Blood Glucose levels to a lesser degree and are generally considered to be safer than longer acting insulin. Then there is an intermediate form (Humulin-N or Humulin-L) which can last almost three times as long, which means up to a day. And lastly there is the Humulin-U, which stays active for longer. Particularly useful for diabetics who may forget their shots, as it stays active longer than a day. There is the fast-acting form called Humalog, this type is only available via prescription in the US. Most bodybuilders prefer the fast acting insulin such as Humalog because of the rapid onset. The quick action of the insulin is important because muscles posses a short window of recovery, and in regards to muscle growth - rapid nutrient disbursement is crucial. There are also mixtures of short and fast acting insulin but for non-diabetics the mixed types are not recommended.
• Substance name
US Manufacturers
Eli Lilly and Company and Novo Nordisk Pharmaceuticals Inc.
In America, regular human insulin is available without a prescription by the name of Humulin R by Eli Lilly and Company, the company also produces 5 other insulin formulations, but none of these should be used by bodybuilders.
Humulin R is the considered the safest because it takes effect in a fairly short amount of time but does not stay in the body for a long time period. The slow acting insulin formulations remain active for a longer time period thus the user has to monitor BGL for a longer period of time, the fast acting insulins onset is very quick so carb/sugar consumption has to occur immediatley following the injection - both of the latter can put an inexperienced user in an unexpected state of hypoglycemia.
• Date created
Eli Lilly and Company was the first to isolate and purify insulin for the treatment of diabetes, then a fatal disease with no effective treatment options. The work resulted in Lilly's introduction of Iletin, the world's first commercially available insulin product, in 1923.
• Medical Use / dosing
Injections are the most common delivery system.
Insulin pens are very convenient - look like a pen with a cartridge which holds 100 to 200 units of insulin.
Be aware that 1.0 ml of insulin contains one hundred International Units (100 IU), 0.1 ml of insulin contains ten (10) IU and 0.01 ml contains one (1.0) IU.
Note that 0.01 ml is the volume contained in the space between the smallest graduated markings on a 1.0 ml Terumo diabetic syringe.
All insulins sold in the United States today are of U-100 strength, 100 units of insulin per cc of fluid. But there are other dilutions in other countries, and if you were to encounter one of these (all perfectly usable), and inject your usual volume of insulin, you would get a higher dosage of insulin. Insulin manufactured outside the US and in higher units of cc per fluid is for use in Insulin pumps and should not be injected.
Inject about 1 IU per 10-20 pounds of lean bodyweight of insulin immediately following a workout when GH is surging. Manipulation of GH/insulin synergy is an effort to both dramatically enhance the anabolism of muscle tissue and reduce the fat accumulation that insulin would cause if used alone. It seems that post-workout timing is the key to maximum potential.
First-time users should start at a low dosage and gradually work up. For example, first begin with 2 IU and then increase the dosage by 1 IU every consecutive workout. It is unadvisable to exceed 10 IUs for your first Insulin cycle. This will allow you to safely determine a dosage. Insulin dosages can vary significantly and are dependent upon insulin sensitivity and the use of other drugs. First time users should inject only once a day for the first cycle.
Humilin R should be injected by the subcutaneous route (injecting just under the skin and preferably in the abdominal area or outer part of the upper thigh), (with a U-100 insulin syringe) not intramuscularly or intravenously as using the latter routes can lead to a rapid rise in blood insulin level and a sudden hypoglycemic episode.
• Androgenic-Anabolic Ratio/Aromatization
Insulin is not Androgenic but Anabolic, nor is it a sex hormone. It is not related in any way to testosterone, or to estrogen for that matter. It is a product of the pancreas as opposed to testosterone which is a product of the HPTA, pituitary, gonadal, leydig, mishmash of interconnected glands...
So how is insulin anabolic? Insulin is a partitioning agent. If blood sugar levels are too high insulin is released, which stores more glucose in the cells as the polysaccharide glycogen, the prime energy source in the human body. This alone makes it a valuable hormone. But it also increases the uptake of other compounds into the cell. This includes protein. Since anabolic steroids increase protein synthesis, and we eat lots of protein, the only thing missing in that system is a way to get the amino acids to where the protein is synthesized. Insulin can do that.
In laymens terms....picture insulin as a transport system. Insulin aids in transporting nutrients where they need to go, it enables anabolism and is therefore it is anabolic.
Its interesting to note that insulin does not have a direct negative feedback system like steroids do. When blood sugar levels drop, cells simply become more resistant to the insulin and don't receive as much of an impulse to store glycogen as they would at first. This is important, as it will have certain implications. If not used properly.
II. Performance Uses and Effects
Insulin is often referred to as “the most anabolic hormone”. Unfortunately, this means it builds adipose tissue as well as muscle. Endogenous (naturally-produced) insulin production is reduced during and immediately after exercise. This is mostly due to the effects of increased circulating catecholamine (epinephrine and norepinephrine). These “fight or flight” hormones put the damper on one’s pancreas. This is too bad for bodybuilders since GH may really be flowing at this time (depending on meal timing, age, etc.) and it seems to have very, synergistic anabolic effects when present at the same time as insulin.
Research has shown that GH or insulin alone has little effect on weight gains, but when injected together there is evidence of a dramatic effect. It’s speculated that GH stimulates uptake of about half of the 9 or so essential amino acids into muscle, while insulin stimulates the uptake (or prevents the loss) of the complimentary half. All must be present for protein synthesis, since this does not occur naturally the two should be “injected together”. (GH and insulin are largely counter-regulatory (and not naturally present together).
• General Information
To further increase the effects of this powerful combination, a relatively mild aerobic or weight workout at least 4-5 hours apart from the “main” training session, can be used to get another GH surge and thus a second chance during the day to use insulin when it’s most effective. This second workout of the day need only be about 10-20 minutes in duration and at a moderate intensity to elicit a GH surge that lasts 15-40 minutes after exercise. This will up the anabolic drive, generally speaking you will lose existing fat because this minimal cardio workout won’t do much from a (fat) calorie-burning point of view. (Using a beta-2 adrenergic agonist like clenbuterol or an ephedra/yohimbe blend would only serve to suppress GH release as well.) This “two-a-day” approach is primarily for anabolic purposes.
• Effects on Body Composition
Growth Hormone in regards to muscle growth has shown to do very little without testosterone and/or insulin. The anabolism GH induces alone is largely organ mass and insulin is not only acutely dangerous if used improperly, it’s also likely to induce some serious fat gain if used alone. Together, however, there is the potential for enhanced muscle recovery and growth without tremendous fat accumulation.
• Goal-Orientated Cycling (examples)
6-8 week cycles
It is important to note, if you use the long acting insulin rather than the short or regular, you will have to monitor your glucose levels for atleast 24 hours and keep glucose (dextrose) on hand for the entire duration. This is the reason that Humulin R or Humalog are the preferred sources, and not a long acting insulin!
Start with no more than 5 IU (0.05 ml) of this short acting/ regular insulin preparation and increase the dose gradually over a period of one week, to a dose no higher than 20 IU (0.20 ml) per day. Doses above this will expose you to progressively greater risk and most bodybuilders who use insulin believe there is no advantage in taking doses higher than this. Anecdotal evidence amongst bodybuilders suggests increased doses leads to excess body fat accumulation.
For optimal results, use immediately after training (Post Work Out) because that is when your body is most depleted of Glycogen stores and is primed to overcompensate for the influx of nutrients. Insulin hits in 5-15 minutes so you must immediately ingest 10 grams of simple carbohydrates for every IU of insulin you inject. Taking in additional nutrients help contribute to muscle growth, such as amino acids whey isolate. Also have 5 grams of creatine at this time will aid in cell volumizing.
The best case scenario would be to do this twice a day (the more you deplete your Glycogen stores, the more of an opportunity you have to use insulin.) If you choose to inject twice daily you increase the risk of entering a hypoclycemic state. The General information section above gives detail on a two-a-day injection routine.
Immediately after, you should have a carbohydrate drink, again you should consume at least 10 grams of carbohydrates for every 1 IU of insulin injected. You can also take creatine monohydrate with the carbohydrate drink since the insulin will help to force the creatine into the muscles. An hour or so after injecting insulin eat a meal or consume a protein shake. The carbohydrate drink and meal/protein shake are necessary. Without them, blood sugar levels will drop dangerously low and you will most likely go into a state of hypoglycemia. Note: Sugar water will absorb the fastest, minimizing the risk as opposed to other carbs. Mix 150 grams of sugar in water and consume within 20 minutes of the injection and keep a glass with another 150 grams handy. If you finish the glass, immediately prepare another until the insulin has cleared the blood.
It is a good idea to invest in a Blood Glucose Monitor. It is a battery operated device that quickly and easily test Blood Glucose Levels. Monitors can be purchased at drug stores for about $15.00.
The Glycemic Index Factor:
Scientists have discovered that carbohydrate containing foods can be measured and ranked on the basis of the rate and level of blood glucose increase they cause when eaten. This measurement is called the "Glycemic Index" or "G.I. factor". The rate at which glucose enters the bloodstream affects the insulin response to that food and ultimately affects the rate at which this glucose (fuel) is made available to exercising muscles. Review the Glycemic Index to understand the G.I. factor to determine what foods are best to consume following an insulin injection.
III. Side Effects and Precautions
Insulin has one of the highest potentials for danger of all bodybuilding drugs. Use requires complete discipline and control. Insulin misuse should not be taken lightly because death can occur.
Repeated Insulin use in a non diabetic can cause you to become Insulin dependent. Misuse can also contribute to obesity.
The major risk associated with insulin is a physical state known as hypoglycemia or "low blood sugar". This occurs when the level of glucose in the blood falls below a certain level required for normal body function. If the blood glucose level is substantially reduced below this normal level and if this is not quickly corrected, there is a risk of disorientation, collapse, coma, permanent brain damage and even death. Exercise and reduced food intake decreases the body's need for insulin and increases the risk of hypoglycemia associated with non-medical use of insulin.
Hypoglycemia occurs when blood glucose levels are too low. It is a common and before you begin taking insulin, it is critical that you understand the warning signs and symptoms of hypoglycemia. The following is a list of symptoms which may indicate a mild to moderate hypoglycemia: hunger, drowsiness, blurred vision, depressive mood, dizziness, sweating, palpitation, tremor, restlessness, tingling in the hands, feet, lips, or tongue, lightheadedness, inability to concentrate, headache, sleep disturbances, anxiety, slurred speech, irritability, abnormal behavior, unsteady movement, and personality changes. If any of these warning signs should occur, you should immediately consume a food or drink containing sugar such as a candy bar or carbohydrate drink. This will treat a mild to moderate hypoglycemia and prevent a severe state of hypoglycemia. Severe hypoglycemia is a serious condition that may require medical attention. Symptoms include disorientation, seizure, unconsciousness, and death.
It is possible to become sleepy after injecting insulin. This may be a symptom of hypoglycemia, and you should consume more carbohydrates. Avoid the temptation to go to bed since the insulin may take its peak effect during sleep and significantly drop glucose levels. Being unaware of the warning signs during his slumber, you are at a high risk of going into a state of severe hypoglycemia without anyone realizing it. Humulin R usually remains active for only 4 hours with a peak at about two hours after injecting. An athlete would be wise to stay up for the 4 hours after injecting.
Rather than waiting to the end of a workout, you may prefer to inject the insulin dosage 30 minutes before the training session is over and then consume a carbohydrate drink immediately following the workout. This will make the insulin more efficient at bringing glycogen to the muscles, but it will also increase the danger of hypoglycemia. You may inject a few IUs before lifting to improve a pump, but this practice is extremely risky and best left to experienced insulin users. Finally, you may inject insulin upon waking in the morning. After the injection, consume a carbohydrate drink and then have breakfast within the next hour. Some find this application of insulin very beneficial for putting on mass, while others will tend to put on excess fat using insulin in this way.
However, before you attempt to use insulin, you should educate yourself and make yourself aware of the consequences. One mistake in dosage or diet can be potentially fatal.
It is difficult to provide a quantitative estimate of risk for any drug but on a scale of risk in relation to other non-medical and unsanctioned drug use, the use of insulin in this manner would rank towards the higher end of the scale. If zero equals "no risk" of harm to a person's health and ten equals "extreme risk", the use of anabolic steroids in a non-medical context might rate towards the middle of the scale of risk (particularly in the medium to long term) whilst insulin would rate higher.
• Metabolites and Drug Detection Time
Insulin use can not be detected during a drug test. For this reason, along with the fact that it is cheap and readily available, insulin has become a popular drug among the competitive athlete.
• Drug Half life
Humulin R – a short acting insulin that begins to work within an hour but stops working sooner than intermediate or long-acting insulins. Peaks 2 to 4 hours. Duration 6 to 8 hours
Humalog -- rapid acting insulin is an analog of recombinant DNA technology in which two amino acids of the human insulin molecule -- proline and lysine -- have been reversed. It begins to work in 15 to 30 minutes, peaks 1 1/2 to 2 hours, and lasts 4 hours, has a half-life of about one half hour.
• General Concerns
Consider using the natural method listed below to raise your blood insulin level during workouts by consuming glucose containing fluids at intervals during exercise. These fluids may have a protein sparing effect and at the same time, will help maintain keep your blood glucose and blood insulin levels. However, if you decide to use insulin, you should consider the following advice:
Don't use medium or long acting insulin in the middle or latter part of the day, as you may very well experience a hypoglycemic attack whilst you are asleep. If this happens, neither you nor anyone else will be aware of or able to respond to your urgent need for glucose, in order to prevent possible serious harm.
If you are going to use insulin, it is essential that you have a friend or peer observer remain with you in case you experience problems. This person really needs to be with you for the whole time while the insulin preparation used is working.
Be aware that the risk of hypoglycemia occurs not at the time of insulin injection but rather, when the insulin starts to take effect. The risk will be greatest when your insulin blood level nears or reaches its highest level, usually 30-60 minutes afterwards if a short acting insulin preparation is used (by subcutaneous injection) and up to 20 hours later if a long acting insulin is used.
***A Natural Method of Maintaining an Elevated Blood Insulin Level:
Noting the hypothesis that an elevated blood insulin level may be of some advantage to bodybuilders, a liquid meal consisting of 13.0 g protein, 31.9 g carbohydrate and 2.6 g fat per 100 ml and provided 825 kJ of energy.
It is possible with such intermittent feeding during intense weight training to maintain a person's blood glucose at or above resting levels and at the same time, significantly increase insulin levels for the duration of the workout. This suggests a potentially effective and safe non-drug method for achieving a sustained elevation of blood insulin levels.
It is also relevant to note that muscle repair and growth begins in the hours and days following heavy exercise. It is doubtful that the use of insulin just prior to a workout will have any anabolic effects over and above natural processes, at this time. However, use of insulin prior to a workout will certainly expose you to much greater risk of serious harm. If you believe it is beneficial to have a higher insulin blood level during workouts, try the natural method outlined here.
Intending users should also be aware that insulin stimulates lipid (fat) synthesis from carbohydrate ("lipogenesis"), decreases fatty acid release from tissues ("lipolysis") and leads to a net increase in total body lipid stores. The development of such increased body fat stores runs counter to the training goals of most body builders, athletes and those seeking to improve their physical appearance.
IV. Availability
Humulin-R can be bought over-the-counter for around $20 / 10 cc. (10 ml vial with strength of 100 IU per ml) bottle. Humalog for around $30.95.
• Manufactures
Eli Lilly and Company and Novo Nordisk Pharmaceuticals Inc.
• Counterfeits
Since Insulin can be readily purchased over the counter, counterfeiting of Insulin is not common as with steroids or illegal drugs. Check the packaging to be sure to note the manufacturer and brand name of the insulin you purchase.
• Miscellany
Insulin should be refrigerated and kept away from excessive heat.
Experience
Of the Non-Diabetic Anabolic Review users polled
11% preferred regular acting Insulin such as Humulin R
89% preferred fast acting Insulin such as Humalog
0% preferred slow acting Insulin.
91% experiencd positive results and will use it again
9% experienced positive results but felt the risk factor was too high or
there was too much involved and would not consider another cycle
0% experienced negative results
72% experienced positive results when used with a combination of HGH
and Steroids
21% experienced positive results when used with Steroids
7% experienced positive results when used with HGH