Performance enhancing drugs

What is performance ?• Physical• Mental• sexual

A. Anabolic SteroidsB. ClenbuterolC. Gamma HydroxybutyrateD. Natural Products and Nutritional

SupplementsE. Prescription Medications

Performance enhancing drugs

Anabolic Steroids As Abused Drugs

• "Anabolic steroids" is the familiar name for synthetic substances related to the male sex hormones (e.g., testosterone). They promote the growth of skeletal muscle (anabolic effects) and the development of male sexual characteristics (androgenic effects) in both males and females. So the proper term for these compounds is "anabolic-androgenic steroids.“

• Anabolic steroids were developed in the late 1930s primarily to treat hypogonadism, a condition in which the testes do not produce sufficient testosterone for normal growth, development, and sexual functioning. The primary medical uses of these compounds are to treat delayed puberty, some types of impotence, and wasting of the body caused by HIV infection or other diseases.

• During the 1930s, scientists discovered that anabolic steroids could facilitate the growth of skeletal muscle in laboratory animals, which led to abuse of the compounds first by bodybuilders and weightlifters and then by athletes in other sports.

Anabolic Steroids are a group of synthetic hormones that promote the storage of protein and the growth of tissue. Anabolic steroids are synthetic drugs similar to the male hormone, testosterone.

- The full name for this class of drugs is androgenic (promoting masculine characteristics) anabolic (tissue building) steroids (the class of drugs).

Examples are, Nandrolone, Oxandrolone, Oxymetholone, and Stanzolol. They can be taken as tablets, in powder form or by intramuscular injection.

- These steroids improve muscle growth, strength and power. In many cases, these steroids are used by athletes.

-Both males and females have testosterone produced in their bodies: males in the testes, and females in the ovaries and adrenal cortex.

- Some of the common street (slang) names for anabolic steroids include arnolds, gym candy, pumpers, roids, stackers, weight trainers, and juice.

Routes of Adminstation:

- Currently, there are more than 100 different types of anabolic steroids that have been developed, and each requires a prescription to be used legally in the United States.

- Anabolic steroids can be taken orally, injected intramuscularly, or rubbed on the skin when in the form of gels or creams.

1) cycling, which involves taking multiple doses of steroids over a specific period of time, stopping for a period, and starting again.

2) stacking Users also frequently combine several different types of steroids in a process known as stacking. By doing this, users believe that the different steroids will interact to produce an effect on muscle size that is greater than the effects of using each drug individually (avoid tolerance, different receptors, decrease side effects).

Adminstration patterns :

3) Pyramiding: This is a process in which users slowly escalate steroid abuse (increasing the

number of steroids or the dose and frequency of one or more steroids used at one time), reaching

a peak amount at mid-cycle and gradually reducing the dose toward the end of the cycle.

Administration (continued)

• P.O. or IM (frequently together)• Testosterone cannot be given

orally (WHY?)• Anabolic steroid injections are

formulated in oil which allows a sustained release of drug from the IM site over a period of weeks or days

• Doses: 10-100 excess of therapeutic doses

Medical use of anabolic steroids

• Bone marrow stimulation: For decades, anabolic steroids were the mainstay of therapy for hypo-plastic anemia due to leukemia or kidney failure, especially aplastic anemia.

•Hormone Replacement Therapy (HRT) e.g. in hypogonadism, infertility, … etc.

•Post-surgical muscle wasting.

•As Performance Enhancing Drugs in some cases.

Commonly Abused SteroidsOral SteroidsAnadrol (oxymetholone)Oxandrin (oxandrolone)Dianabol (methandrostenolone)Winstrol (stanozolol)

Injectable SteroidsDeca-Durabolin (nandrolone decanoate)Durabolin (nandrolone phenpropionate)Depo-Testosterone (testosterone cypionate)Equipoise (boldenone undecylenate)Tetrahydrogestrinone (THG)

Testosterone Nandrolone

Oxandrolone Stanozol

The side effects of anabolic steroids ♀♂

1) Liver damage 2) Heart damage (arteriosclerosis, hypertension, hypertrophy of left ventricle)3) Weak tendons (injuries)4) Immunosuppression5) Psychological: Aggressiveness, paranoid jealousy, extreme irritability, confusion, anxiety, sleep disorders, euphoria, depression, hallucination. 7) Kidney damage8) Water & salt retention

In men ♂

1) Development of breasts (Gynecomastia)♂ 2) Atrophy of the testicles, reduced sperm count, infertility

3) Baldness (male-type M), acne, diarrhea, nausea, bloating

4) Prostate enlargement, cancer

Women will also suffer from: ♀ 1) irregular menstruation

2) Virilization (breast reduction, development of beard, deepening of voice) …………infertility

3) Birth defects: development of male sex organs in female fetus if conception occurs when the mother is taking these anabolics.

In sports, doping refers to the use of Performance-enhancing drugs, particularly those forbidden by organizations that regulate competitions.

The World Anti Doping Agency (WADA) constantly maintains an updated list of performance enhancing substances used around the world as reference. This list includes all anabolic agents and precursors.

Anabolic steroids and sports

Types of doping are:

1) Blood doping, either by blood transfusion or use of the hormone erythropoietin (EPO, is a glycoprotein hormone that controls erythropoiesis, or red blood cell production)

2) Anabolic steroid. Also considered "doping" by many is the use of substances that mask other forms of doping (e.g. Finasteride= Finasteride is a synthetic type II 5α-reductase inhibitor. This enzyme converts testosterone to dihydrotestosterone).

3) Growth hormone

How is growth hormone abused?

People sometimes take GH illegally to stop or reverse the effects of aging or to improve athletic performance. Some

athletes believe taking GH alone will not achieve the desired results, so take it along with anabolic (tissue-

building) steroids in an effort to build muscle, increase strength, and decrease body fat.

Some athletes also use insulin to increase the muscular effects of GH, which is a dangerous practice because it

lowers blood sugar.

Doping is considered unethical by most international sports organizations and especially the International Olympic Committee (IOC).

- The reasons are mainly: 1) The health threat of performance-enhancing drugs, 2) Endanger the equality of opportunity of the athletes.

Some rules for testing for Anabolic, androgenic Steroids (AAS):

The most common method to detect anabolic steroid usage is through urine and blood sample tests. Urine tests today can determine whether a person has (or not) taken any anabolic steroids during the previous 30 days.

Epitestosterone is a natural steroid, an inactive epimer of the hormone testosterone. Structurally, it differs from testosterone only in the configuration at the OH-bearing carbon, C17.

Epitestosterone levels are typically highest in young males; however, by adulthood, most healthy males exhibit a testosterone to epitestosterone ratio (T/E ratio) of about 1:1.

• Epitestosterone (E) is biologically inactive with stable level

• Adminstration of testosterone (T ) does not lead to increase of E (T is not converted to E inside the body)

• Concentration of testosterone in male blood is variable (difference in metabolism).

• It has been shown that exogenous administration of testosterone does not affect levels of epitestosterone in the body. As a result, tests to determine the ratio of testosterone to epitestosterone in urine are used to find athletes who are doping.

• Positive doping should be confirmed by taking other samples and carrying out confirmatory tests.

• All tests are performed (on urine, sometimes blood) in laboratories accredited by the International Olympic Committee (IOC) using GC-MS or HPLC-MS in urine after Deconjugation using beta-glucuronidase enzyme on metabolites (glucuronides).

• T/E > 6 may indicate positive test unless there is evidence that it is due to natural condition or disease.

• T/E ratio is used to test for doping (reliable)

• T/E < 6 is considered normal (Negative test)

Tests for doping:

- Random selection of atheletes in preliminaries in addition to a selection of other finalists are tested.

- Carried out in a handful of facilities that have World Anti-Doping Agency (WADA) accreditation:

Procedure:

1) Collection of urine from random samples (no ET)2) Extraction by buffer solution 3) Deconjugation by enzyme4) Analysis by GC/MS or LC/MS/MS

Epitestosterone is prohibited by sport authorities because its administration will lower the urinary testosterone/epitestosterone ratio, a marker of testosterone administration. A definitive method for detecting epitestosterone administration is needed.

So it is developed a method in which gas chromatography-combustion-isotope ratio mass spectrometry method for measuring the delta(13)C values for urinary epitestosterone.

Sample preparation included deconjugation with beta-glucuronidase, solid-phase extraction, and semi preparative HPLC.

Confirmation of positive test results

-Isotopic ratio mass spectrometry: the method is called Gas Chromatography/Combustion/Isotope Ratio Mass Spectroscopy (GC/C/IRMS) which can measure very small differences in the 13C/12C ratio of testosterone (distinguish).

-Depend on that the carbon source of synthetic testosterone (originally from Yam) with different ration from that of natural testosterone (produced within the body).

-Negative test is uninformative due to possible adminstration of LH or human chorionic gonadotropin.

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