ANABOLIC STEROIDS, BODYBUILDING AND THE LAW
STEROIDS 101





What are Steroids?

Steroids are a class of hormones synthesized from cholesterol. All steroids share the same basic four-ring carbon Steroids structure, but differ in the number of carbon atoms attached to the number 17 carbon atom in the structure, and in the manner in which hydrogen (H), oxygen (O), and the hydroxyl (OH) groups are attached to the carbon atoms. There are various types of steroids. For example, corticosteroids, such as prednisone or cortisone, are anti-inflammatory, catabolic compounds that break tissue down. They are completely different from the substances known as anabolic steroids. The term "anabolic steroids" commonly refers to steroids which are synthetically produced, molecularly altered derivatives (or "analogs") of testosterone. Naturally occurring testosterone is the primary sex hormone found in men, produced primarily by the Leydig cells of the testes. The adrenal glands are the primary source of testosterone in women, where testosterone is produced in a much lesser (10 to 15 times lesser) amount.

A Brief History of Testosterone

Ancient cultures believed that strength and manliness were regulated in some unknown way by the testes. In modern times, experiments into this area attempted to learn how the testes affected male characteristics. In 1771, a Scotsman transplanted the testes from a rooster to a hen and confirmed his hypothesis that the hen would display characteristics more like the rooster. A German scientist furthered the research in 1849 by examining the effects of castration upon the secondary sex characteristics of roosters and proving the existence of a masculinizing substance produced in the testes and released through the bloodstream. In 1935, scientists working in Amsterdam succeeded in collecting ten milligrams of a chemical from one hundred kilograms of bull testes and identified this chemical as testosterone. K. David, "Ueber des Testosteron, des Kristallisierte Manniche Hormon aus Steerentestes," 5 Acta Brev. Neerland Physiol. Pharmacol. Microbiol. (1935), pp. 85-86. It is believed that by the late 1940s, Russian weightlifters had discovered testosterone and were using it as a means of augmenting strength and muscular development. (For further information, see C.D. Kochakian, "Anabolic-Androgenic Steroids: A Historical Perspective and Definition," in C.E. Yesalis [Ed.], Anabolic Steroids in Sport and Exercise [Champaign, IL; Human Kinetics, 1993], pp. 3-33.)

The Development of Anabolic Steroids

Testosterone has both anabolic (tissue building) and androgenic (masculinizing) qualities. The anabolic effects are primarily muscle growth. The androgenic effects are the development of secondary male sex characteristics, such as growth of facial and body hair and deepening tone of the voice. Obviously, the anabolic effects are desirable for sports performance and cosmetic appearance. In fully developed adults, especially women, the androgenic effects are not so desirable at all. By the early 1950's, scientists were trying to isolate testosterone's muscle building properties without the masculinizing effects. Synthetic anabolic steroids were developed in this pursuit. Researchers discovered that by making certain modifications to testosterone, such as by adding or removing certain elements at specific locations on the molecule, the resulting compound had high anabolic effects with a substantially reduced androgenic effect. The term "anabolic" instead of "androgenic" steroid connotes the modification of the molecular structure to enhance tissue building and minimize masculinizing effects. (However, because the anabolic and androgenic qualities of these substances cannot be completely separated, some experts prefer the term "anabolic/androgenic steroids.") It is also quite common to see both testosterone and anabolic steroids generically referred to as androgens. One of the pioneers in the history of anabolics was John Ziegler, M.D., who in collaboration with the pharmaceutical manufacturer CIBA, introduced the oral steroid Dianabol to weightlifters in 1956. By the mid 1960's, scientists had created many different anabolic steroids and thousands of strength athletes were using them.

Types of Anabolic Steroids

Some steroids were designed to be taken orally, and usually have short half-lives, generally on the order of several hours. Other variations were developed for parenteral administration (by intramuscular injection, commonly in the buttocks), and tend to have longer half-lives than orals, usually around one to three days.

Anabolic steroids were also chemically modified to prevent rapid breakdown by the liver and thereby enable better utilization. Orally ingested compounds are absorbed from the gastrointestinal tract and must first pass through the liver before entering the blood to be distributed throughout the body. Accordingly, many oral anabolic steroids were modified by the addition of a side chain or group of molecules at the alpha position of the number 17 carbon atom through a process called alkylation in order to withstand inactivation on this first pass. The modification of these C-17 alkylated steroids to survive liver degradation makes them unusually harsh upon the liver.

Injectable steroids are slowly absorbed into the blood stream without a first pass through the liver. Consequently, the liver experiences a much lower concentration than with oral anabolics. For this reason, most injectable steroids have little effect upon liver function. [However, a few C-17 alkylated steroids that are usually used orally in humans are available as injectable veterinary compounds (examples are stanozolol and methandrostenelone), and these have similar hepatic profiles to their oral counterparts.] Most injectable steroids undergo a process called esterification to slow quick breakdown by the liver. Most of the common injectable androgens are oil-based preparations containing a mixture of sesame seed oil and alcohol. Enhanced forms of injectable testosterone are often collectively referred to as testosterone esters. A few injectable steroids are not oil-based, but shorter-lasting, water-based suspensions (examples are the testosterone and stanozolol suspensions).

How Anabolic Steroids Work in the Body

Steroids taken orally proceed through the gastrointestinal tract to the liver, where they are processed before going into the blood; steroids taken parenterally go directly into the blood stream. Eventually, however, all anabolic steroids wind up in the blood stream, carried along with thousands of other types of molecules. How anabolic steroids work to increase muscular size and strength is best explained on a cellular level. The cells within the tissues of our bodies have certain areas that are receptive to some free-floating molecules within the blood. These areas are called receptor sites. There are receptor sites with an affinity for steroid molecules in our skeletal muscle cells, for example. A steroid molecule being carried along in the blood enters the muscle cell by diffusion and binds to one of these receptor sites. The connection that is formed permits the steroid molecule to deliver a cellular message or command to the receptor site to effect certain metabolic changes within the cell. One of these primary metabolic changes is increased protein synthesis and nitrogen retention, leading to increased size and strength of the skeletal muscle cell. The connection of a steroid molecule and receptor site is fleeting: once the steroid molecule delivers its cellular command, it moves on to other receptor sites, delivering its message over and over until it is converted into another compound or is excreted in the urine. This capacity of androgens to be converted into other substances by chemical reactions and enzymes within certain tissues of the body will be extremely significant later when we discuss potential side effects (see Health Risks section).

Anabolics also enhance size and strength through a different mechanism. Intense training causes the body to produce increased levels of cortisol, a catabolic substance that causes muscle tissue breakdown. Anabolics have an anticatabolic effect; that is, they prevent the breakdown of muscle tissue by displacing cortisol from its receptors. Consequently, recovery processes are speeded up and injuries, including the microscopic muscle damage incurred from heavy training, heal faster. Some authorities believe that the anticatabolic properties of steroids may be of equal significance to the anabolic properties.

Medical Uses of Anabolic Steroids

The public is most familiar with anabolic steroids as used by competitive (professional and amateur) athletes to improve performance through increased muscular size or strength, and by noncompetitive weight trainers for purely cosmetic physique enhancement. However, androgens have legitimate medical uses, such as in the treatment of hypogonadal men (men with damaged or undescended testes) to compensate for the lack of endogenous production. Anabolic steroids are also helpful for the treatment of certain adolescent diseases, some types of anemias, and for a relatively rare form of edema. Other clinical uses focus on the tissue building and anti-catabolic effects, such as in the treatment of burn victims, AIDS or HIV positive patients, or patients malnourished from disease or advanced age. Testosterone supplementation has also been extensively tested as a means of male contraception. Further, as endogenous testosterone production decreases with age, recent research has begun to explore the use of androgen replacement as a safe and effective anti-aging therapy for middle-aged men. The judicious use of androgens could improve age-related decreases in sexual desire and sexual arousal in many men, and would seem to have a positive effect toward lowering serum cholesterol when used in appropriate dosages.

COPYRIGHT (c) 1999 by Rick Collins. www.steroidlaw.com All rights reserved. No commercial reproduction of any portion of this material is permitted without the express written permission of the author.