History
Insulin was isolated by Frederick Banting and Charles Best at the University of Toronto in summer 1921 (with collaborators James Collip and J.J.R. Macleod), and the discovery was announced publicly in November 1921. The first human treatment came in January 1922: 14-year-old Leonard Thompson received the first Banting/Best extract on 11 Jan 1922, and Collip's purified extract on 23 Jan 1922 effectively stabilized his blood glucose — transforming type 1 diabetes from a death sentence into a manageable disease. Banting and Macleod received the 1923 Nobel Prize in Physiology or Medicine (sharing the prize money with Best and Collip), and the patent was sold to the University of Toronto for $1. Recombinant human insulin (Humulin, Genentech/Eli Lilly, produced in E. coli) received FDA marketing approval on 30 October 1982 — the first recombinant-DNA pharmaceutical ever approved for human use, cleared in roughly 5 months versus a then-average ~30 months.
Insulin lives a double life. It is at once one of the most important, best-proven, life-saving drugs in all of medicine — and one of the most acutely dangerous things misused in strength sports. For people with diabetes, it is essential and impossible to replace. But used as a performance or “anabolic” (muscle-building) tool by healthy people, the human track record is mostly a track record of harm — dangerously low blood sugar, brain injury, and death — with no solid evidence that it actually builds meaningful muscle. This page is here to educate and reduce harm. It contains no doses, cycles, stacks, or sourcing information.
What it is
Insulin is a small protein — a 51-amino-acid peptide hormone — made of two chains (A and B) held together by disulfide bonds (sulfur-to-sulfur links), with a molecular weight of about 5.8 kDa. Your pancreas makes it, in clusters of cells called the islets of Langerhans (specifically the beta cells). It is the body’s main hormone for both lowering blood sugar and building tissue.
Here is how it works, step by step. Insulin latches onto the insulin receptor on the surface of your cells (a receptor tyrosine kinase, meaning a docking protein that switches on a chemical signal once insulin attaches). That switch sets off a chain of signals inside the cell (the IRS/PI3K/Akt cascade), which does four things: (1) it moves glucose transporters called GLUT4 to the cell surface in muscle and fat, so those cells soak up more sugar; (2) it tells the body to store sugar as glycogen (its storage form); (3) it pushes the body to make and hold onto fat; and (4) it pulls amino acids (the building blocks of protein) into cells, ramps up protein-building, and slows protein breakdown — which is exactly why it has an “anabolic” reputation. It also fires a second signal route (the MAPK pathway) tied to growth. The bottom line: blood sugar drops, and the body flips into a store-fuel, build-tissue mode.
The medical versions include recombinant human insulin (made in the lab to match human insulin) plus engineered “analogs” tweaked to start working and last for different lengths of time: rapid-acting (lispro, aspart, glulisine), short-acting (regular), intermediate (NPH), and long-acting “basal” types that work slowly in the background (glargine, detemir, degludec).
The claims
In strength sports — bodybuilding and powerlifting especially — people misuse insulin for its muscle-building effects. The thinking behind it is rooted in real biology: insulin drives glucose, amino acids, and creatine into muscle, packs muscle with glycogen (the “fullness” or “pump” look), and slows the breakdown of protein. Users often combine it with anabolic-androgenic steroids and growth hormone, on the (mostly word-of-mouth) idea that insulin and GH/IGF-1 work together to boost tissue growth.
One published study tracked 41 non-diabetic insulin users (Ip et al., 2012). It found they averaged about 30.7 years old, were 97.6% male, 95.1% also used anabolic steroids, and used roughly 16 different performance-enhancing drugs per year. About 81% said insulin was “easy” to get, from pharmacies and local or gym sources.
What the evidence actually shows
The evidence falls neatly into two very different stories.
Medical (overwhelming). For type 1 diabetes, insulin clearly works and saves lives, and it is a mainstay for advanced type 2 diabetes too. It is among the most solidly proven treatments in all of medicine, with a century of use behind it.
Performance/anabolic (essentially absent). There is no strong, controlled human evidence that injected insulin meaningfully adds lean muscle or strength in healthy, well-fed athletes. The “evidence” for this use is basically case reports and one survey-based study — not proper trials that test whether it works. The documented human record on insulin in athletes is dominated by harm — severe low blood sugar, coma, permanent brain injury (neuroglycopenia, meaning the brain is starved of glucose), and death. Ip et al. (2012) found that 56.8% of users reported episodes of low blood sugar, including one person who lost consciousness, and individual case reports describe non-diabetic bodybuilders showing up in a coma after injecting themselves. In short: the practice runs on biology and anecdote, and it carries the highest acute risk of death among common PEDs.
Legal and regulatory status
US — prescription drug, not a controlled substance. All insulins are legitimate prescription (Rx) drugs regulated by the FDA. They are NOT controlled substances and are not scheduled under the Controlled Substances Act. You can legally have and use them with a prescription. FDA-approved uses include type 1 diabetes (where insulin keeps people alive and is required), type 2 diabetes when other treatments aren’t enough, gestational diabetes (diabetes during pregnancy), and treating diabetic ketoacidosis and other high-blood-sugar emergencies. Worth knowing: the older “human” insulins — Regular, NPH, and 70/30 mixes (such as Novolin/ReliOn) — can still be bought without a prescription through the pharmacist in nearly all US states (Indiana is the one noted exception); the newer analogs (lispro, aspart, glargine, and the rest) need an Rx. Getting or using insulin for non-medical performance enhancement is off-label, illicit misuse — but it does not break drug-scheduling law.
For contrast within the wider PED picture:
- DNP (2,4-dinitrophenol) kills people. It is NOT approved for people to consume. The FDA declared it unfit and extremely dangerous for human use in 1938 after a wave of cataracts (“dinitro-cataracts,” clouding of the eye’s lens), agranulocytosis (a dangerous drop in infection-fighting white blood cells), overheating, and hundreds of deaths. Today it is sold illegally online as a “fat burner” and still causes fatal poisonings. It works by uncoupling mitochondrial oxidative phosphorylation (short-circuiting the way cells turn food into energy, so the energy escapes as heat), has almost no gap between a dose that “works” and a dose that kills, and has no specific antidote.
- Mesterolone and fluoxymesterone are anabolic-androgenic steroids and are Schedule III controlled substances under the US Controlled Substances Act (Anabolic Steroids Control Act of 1990).
Anti-doping (WADA). Insulins (and insulin-mimetics, meaning substances that copy insulin’s action) are banned under S4.4.2 (“Insulins and Insulin-Mimetics”) within the S4 Hormone and Metabolic Modulators class. S4 substances are banned at all times — both in and out of competition. Athletes with diabetes who medically need insulin must hold a Therapeutic Use Exemption (TUE, official permission to use a banned drug for a genuine medical reason). For related context, aromatase inhibitors and anti-estrogens/SERMs (e.g., tamoxifen, clomifene) also sit under S4 (S4.1–S4.3), and other metabolic modulators under S4.4 include AMPK activators/PPARδ agonists (S4.4.1), meldonium (S4.4.3), and trimetazidine (S4.4.4). DNP and anabolic steroids sit outside S4 — anabolic agents are class S1, and non-approved substances such as DNP can fall under S0 (Non-Approved Substances). All are likewise banned at all times.
Safety
Insulin is the most acutely dangerous of all the PED-adjacent agents discussed here, because its main danger comes on fast, hits hard, and can kill within minutes to hours.
- Hypoglycemia (the lethal risk). “Hypoglycemia” means dangerously low blood sugar. In a non-diabetic person — or with any insulin overdose — insulin drops blood sugar to dangerous levels. Early warning signs are sweating, shakiness, a pounding heart, hunger, and anxiety. As the brain runs out of glucose (neuroglycopenia), it gets worse: confusion, slurred speech, seizures, coma, permanent brain damage, and death. Long-acting analogs are especially dangerous because they keep working long after a single meal, so they can cause delayed, drawn-out, repeating crashes. Hard exercise, fasting, and alcohol all make it worse. There is no room for error: the gap between an “effect” and a fatal event can be tiny, and injecting it without checking blood sugar can be deadly. People who survive a severe crash can be left with lasting problems with thinking and the nervous system.
- Other risks. Hypokalemia (low blood potassium — insulin pushes potassium into cells, which can trigger dangerous heart rhythms), lipohypertrophy (lumpy fatty buildup at injection sites), fat gain, and rare allergic reactions. Counterfeit or shared “gym” insulin adds the risk of contamination and not knowing the real dose.
- Deliberate harm. Insulin is also a well-known tool for deliberate self-harm, faked illness, and even murder — precisely because it can be hard to detect after death. That alone shows how powerful and silent its lethality is.
For comparison only: DNP causes uncontrolled overheating, multi-organ failure, has no antidote, and is often fatal. T3/liothyronine (a thyroid hormone) can cause irregular or racing heartbeat, bone loss, and shutdown of the body’s own thyroid function. Aromatase inhibitors carry harms to bone density and to lipids/cardiovascular health. SERMs carry a risk of venous thromboembolism (dangerous blood clots in the veins). Insulin’s defining danger is fatal low blood sugar. None of this is medical advice.
Bottom line
Insulin is a 51-amino-acid peptide hormone and one of the true triumphs of modern medicine — essential and life-saving for type 1 diabetes and a mainstay for advanced type 2, with a century of evidence behind it. Used as a performance compound in healthy people, the story flips: the human record is one of harm — low-blood-sugar coma, irreversible brain injury, and death — with no good controlled evidence that it builds meaningful muscle. It is a prescription drug (older human insulins are available over the counter through the pharmacist in nearly all states), it is not a controlled substance, and it is banned in sport at all times under WADA S4.4.2. This is not a “manageable side-effect” situation: a sudden blood-sugar crash can kill before help arrives.
Evidence grade: 10/10 · Established. Strong (overwhelming) for its medical indications in diabetes; the performance/anabolic use is not supported by efficacy evidence and is dominated by documented harm.
Sources
- Ip EJ, Barnett MJ, Tenerowicz MJ, Perry PJ. “Weightlifting’s risky new trend: a case series of 41 insulin users.” Curr Sports Med Rep. 2012;11(4):176-9. PMID 22777326
- Heidet M, et al. “Severe Hypoglycemia Due to Cryptic Insulin Use in a Bodybuilder.” J Emerg Med. 2019;56(3):279-281. PMID 30527564
- Evans PJ, Lynch RM. “Insulin as a drug of abuse in body building.” Br J Sports Med. 2003;37(4):356-7. PMID 12893725; PMCID PMC1724679
- Konrad C, Schüpfer G, Wietlisbach M, Gerber H. “[Insulin as an anabolic: hypoglycemia in the bodybuilding world].” Anasthesiol Intensivmed Notfallmed Schmerzther. 1998;33(7):461-3. PMID 9728265
- Thomas A, Benzenberg L, Bally L, Thevis M. “Facilitated Qualitative Determination of Insulin, Its Synthetic Analogs, and C-Peptide in Human Urine by Means of LC–HRMS.” Metabolites. 2021;11(5):309. PMCID PMC8151387
- NobelPrize.org — “The ‘miracle’ discovery that reversed the diabetes death sentence” (insulin discovery and the 1923 Nobel Prize)
- UMass Chan Medical School — Leonard Thompson, first human insulin injection (Jan 1922)
- UMass Chan Medical School — Banting & Best isolate insulin (1921)
- American Council on Science and Health — record-time 1982 FDA approval of recombinant human insulin (Humulin)
- BioSpace — first recombinant insulin (Humulin), Genentech/Eli Lilly
- WADA — The Prohibited List (official)
- Drugs.com — WADA S4 Hormone and Metabolic Modulators (insulins/insulin-mimetics under S4.4.2; prohibited at all times)
Checking ClinicalTrials.gov…
- What is Insulin?
- A 51-amino-acid peptide hormone (two disulfide-linked chains, ~5.8 kDa) — the body's primary anabolic and glucose-lowering hormone, secreted by pancreatic beta cells.
- What is Insulin used for?
- Insulin is mainly studied for type 1 and advanced type 2 diabetes, gestational diabetes, diabetic ketoacidosis/hyperglycemic emergencies (medical); misused off-label for 'anabolic' muscle effects.
- Is Insulin FDA-approved or legal?
- Prescription drug (older human insulins OTC via pharmacist in nearly all US states); NOT a controlled substance; prohibited at all times in sport under WADA S4.4.2.
- How strong is the evidence for Insulin?
- On the Codex Scale, Insulin grades 10/10 — Established. FDA-approved for this exact use, confirmed by large randomized trials and meta-analyses.
- What else is Insulin called?
- Recombinant human insulin (Humulin, Novolin, ReliOn); analogs lispro, aspart, glulisine, glargine, detemir, degludec; forms regular, NPH, 70/30.
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