Prof. Dr. Amani S. Awaad

Professor of Pharmacognosy

Pharmacognosy Department,

College of Pharmacy Salman Bin Abdulaziz University,

Al-Kharj. KSA.

Email: amaniawaad@hotmail.com

Substance Abuse

PHG 414

Welcome Back

Dears

Anabolic Steroids

You should be able to :

Discuss the source and synthesis of anabolic hormones

•Explain the abuse of anabolic hormones in view of its actions in male and female.

•Identify the consequences of abusing anabolic hormones.

Performance enhancing drugs What is performance? Physical , Mental, & sexual

Performance enhancing drugs

Anabolic Steroids , Clenbuterol, Gamma Hydroxybutyrate, Natural Products and

Nutritional Supplements & Prescription Medications

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. 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.

Actions of anabolic hormones

*Increase skeletal muscle

mass

• Increase bone density

• Increase hemoglobin

concentration

• Increase red blood cell mass

• Enhancement of immune

system

• promote cell growth.

Increase nitrogen retention,

Increase protein synthesis,

appetite

• Increase retention of several

electrolytes

Anabolic Steroids

*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.

Steroid abuse has become so widespread in athletics that it can

affect the outcome of sports contests.

*Anabolic Steroids are a group of synthetic

hormones that promote the storage of protein

and the growth of tissue. They are synthetic

drugs similar to the male hormone,

testosterone.

*The proper term for these compounds is

"anabolic-androgenic steroids.“

- The full name for this class of drugs is

androgenic (promoting masculine

characteristics) anabolic (tissue building)

steroids (the class of drugs).

Anabolic Steroids as Abused Drugs

What are anabolic steroids?

Anabolic Steroids as Abused 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.

*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.

Anabolic Steroids as Abused Drugs

Routes of Administration:

Administration patterns

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).

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

• 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

Adults who take anabolic steroids can be affected

psychologically; their livers may be damaged, and may

suffer heart disorders.

Anabolic Steroids as Abused Drugs

Medical use of anabolic steroids

Oral Steroids :Anadrol (oxymetholone), Oxandrin

(oxandrolone),Dianabol (methandrostenolone), Winstrol

(stanozolol)

Injectable Steroids: Deca-Durabolin (nandrolone decanoate),

Durabolin (nandrolone phenpropionate), Depo-Testosterone

(testosterone cypionate), Equipoise (boldenone und

Testosterone

Nandrolone

Oxandrolone

Stanozol

1) Liver damage 2) Weak tendons (injuries) 3) Kidney damage

4) Immunosuppression 5) Water & salt retention

6) Heart damage (arteriosclerosis, hypertension, hypertrophy of

left ventricle)

7) Psychological: Aggressiveness, paranoid jealousy, extreme

irritability, confusion, anxiety, sleep disorders, euphoria,

depression, hallucination.

Anabolic Steroids as Abused Drugs The side effects of anabolic steroids ♀ ♂

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.

In Women ♀

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.

Anabolic steroids and sports

Anabolic Steroids as Abused Drugs

**In sports, doping refers to the use of Performance-enhancing drugs,.

*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.

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

*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.

Anabolic Steroids as Abused Drugs

Epitestosterone (E) is biologically inactive with stable level

*Administration 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)

Anabolic Steroids as Abused Drugs

Tests for doping:

*Random selection of athletes in 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 samples (no ET) 2) Extraction by

buffer solution 3) Deconjugation by enzyme 4) 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 de-conjugation with beta-

glucuronidase, solid-phase extraction, and semi preparative HPLC.

Anabolic Steroids as Abused Drugs

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 administration of

LH or human chorionic gonadotropin.

Why anabolic hormones abused

*Most common reason: improve

athletic performance.

•Also, to gain rapid and

substantial muscle size and/or

reduce body fat in an effort to

attain a desired physical

appearance

•Reinforcement issues: in

addition to initial physical

gains, androgen receptors in the

brain stimulate feelings of

euphoria and increased

aggressiveness.

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GOOD LUCK