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Androgens

Anabolic steroids can have both anabolic (muscle-building) and androgenic (masculinizing) effects. Common medical uses include treating hypogonadism and wasting diseases, but recreational users believe they improve performance and physique. However, adverse effects include acne, hair loss, cardiovascular and liver problems. Education is needed on safer alternatives for athletes seeking performance enhancement.

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150 views42 pages

Androgens

Anabolic steroids can have both anabolic (muscle-building) and androgenic (masculinizing) effects. Common medical uses include treating hypogonadism and wasting diseases, but recreational users believe they improve performance and physique. However, adverse effects include acne, hair loss, cardiovascular and liver problems. Education is needed on safer alternatives for athletes seeking performance enhancement.

Uploaded by

theintrov
Copyright
© Attribution Non-Commercial (BY-NC)
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PPT, PDF, TXT or read online on Scribd
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Anabolic-Androgenic Steroids Dr keli

Effects of steroids
Androgenic Male characteristics
Hair growth Penile enlargement Voice change

Anabolic Protein synthesis


Increased muscle mass Increased strength Increased performance

Testosterone actions in Males


Produced mainly in the testis
Small amount produced in the adrenal gland Synthesized from cholesterol Hypothalamus produces Gonadotrophin releasing hormone (GnRH) Acts on the anterior pituitary to increase the production of luteinizing hormone (LH) and follicle stimulating hormone (FSH)

LH acts on the Leydig cells in the testis, causing them to produce testosterone. FSH & testosterone act on the Sertoli cells in the testis to regulate the production and maturation of spermatozoa. Testosterone in turn acts on the hypothalamus and anterior pituitary to suppress the production of GnRH, FSH and LH, producing a negativefeedback mechanism which keeps everything well-regulated. The small amount produced in the adrenal (in both sexes) is regulated by secretion of adrenal corticotrophin hormone (ACTH), also secreted by the pituitary.

introduction
Sertoli cells synthesize and secrete inhibin and activin Activin stimulates FSH release and is structuarally similar to Transforming growth Factor B Inhibin with testosterone and dihydrotestosterone are responsible for inhibition of pituitary FSH secretion A

Pharmacologic preparations Synthetic androgens (no non-steroidal androgens presently available) a. Testosterone esters (parenteral use) a) testeosterone propionate b) testosterone ethanthate b. Orally Active Androgens a) methyltestosterone b) fluoxymesterone c. Orally active protein anabolic agents a) norethandrolone b) oxandrolone c) bolasterone

Testosterone
Normal production of testosterone in the testis
Adult male is 4 to 8 mg.day-1
Normal plasma concentration is 700 ng.dl-1 of which 97% is protein bound. Most is excreted in the urine as 17-keto steroids
Small amount is converted to estrogens

Adult female is approximately .3 mg.day-1 produced in the ovary and adrenals and perioheral conversion
Normal plasma concentration is 38-40 ng.dl-1

Types of annabolic Androgenic steroids


Oil based injectable
Fewer side effects More active Long term presence

Oral forms
Water soluble Less active Short term presence Liver & kidney strain

Testosterone forms

Commonly Abused Steroids


More than 100 different steroids available Oral Oxymethalone (Anadrol) Oxandrolone (Oxandrin) Methandrostenolone (Dianabol) Stanozolol (Winstrol) Injectable Nandrolone decanoate (Deca-Durabolin) Nandrolone phenpropionate (Durabolin) Testosterone cypionate (Depo-Testosterone) Boldenone undecylenate (Equipoise)

Testosterone Met
Met to dihydrotestesterone by 5 a reductase and to estradiol by P 450 in the liver adipose and hypothalamus for gonadol regulation Degraded in the liver Excreted in urine

Mechanism of Action

MOA- Androgens
Testosterone / dihydrotestosterone binds with intracellular androgen receptor & their complex combines with DNA Initiating a series of events such as enhanced DNA transcription is & effects are expressed through modification of protein synthesis

Growth, differentiation, synthesis of enzymes & other functional proteins

Pharmacologic effects of testosterone


Its converted to its active metabolite in the skin, prostrate, seminal vescicles, and epididymis Testosterone and the metabolite bind on to receptors and initiate growth differentiation synthesis of enzymes

Physiologic effects in men


Testosterone and its metabolite dihydrotestosterone is responsible for Pubertal growth Penile and scrotal growth Male sex chararacteristics, voice change, maintaining sexual function in men Hair growth face and body and sebum secretion Large doses inhibit gonadotrophic secretion and cause testicles to atrophy

Physiologic effects in women


Development of secondary sexual characteristics Clitoral enlargement

REGULATION OF SECRETION

Regulation of secretion

4) Mechanism of action (1) Plasma protein binding - 98% of circulating androgen bound to sex hormone binding globulin (2) Receptors a. Gene activation

Perrett et al. 1998, Nature

Feminised

Masculinised

Testosterone and Marriage


750 700

650

600 Married Once Never Married Remarried Married and divorced

Physiological Effects
Positive Protein synthesis Increase Lean body mass/prominet masculature Decreased body fat % Force production Power Speed Shortens Recovery time

Negative Hypertension Atherogenic effect Hirsutism (excessive hair growth) Liver function Liver tenderness Clitoral enlargement Edema Glucose tolerance

Psychological Effects
Positive
Euphoria Motivational energy Aggression Libido

Negative
Depression Anxiety Irritability Suicidal Paranoia Hallucinations Dependence

Synthetic steroids with androgenic and anabolic effects


Oral adminstartion only 1/6 is available Parenteral forms esters of Propionate, enthate, undecanoate, cypionate

Primary Medical Uses of AAS


Hypogonadism
Replacement therapy

Wasting diseases
Tuberculosis Cancer AIDS

Male infertility Breast carcinoma Refractory anemias Stunted child growth*

Catabolic conditions
Osteoporosis Burn patients Severe infections

Steroidal Supplements
Often taken because user believes they have anabolic effects Common supplements
Dehydroepiandrosterone (DHEA) Androstenedione (street name Andro)

Can be converted to testosterone (or estrogen)

Clinical uses
Androgen replace or augment endogenous androgens In men In young male patients with hypopitutarism to achieve puberty Gynae disorders; with estrogen to reduce breast engorgement in post partum For endometriosis With ostrogen to Rx post menopausal low libido CXR of breast tumours in premenopausal women Rx of age related changes

Clinical uses
Adrogens and anabolic steroid have been used in trauma surgery and prolonged illness to concerve proteins Rx of anaplastic Ax, Fanconis Ax, Sickle cell Ax, Myelofibrosis Haem Ax replaced by rErythropoetin Rx Osteoporosis oestrogen replaced by biphosphonates In boys with delayed puberty caveat early epiphyseal closure

Scope of Steroid Abuse


Use is increasing in adolescents (8th grade and higher) Steroid abuse is highest in males but use in young women is increasing at a faster rate than in young males

Reasons for Steroid Abuse


Thought to Improve performance in sports Increase muscle size/reduce body fat
Muscle dysmorphia
Behavioral syndrome of distorted body image ;
Men think they look small and weak Women think they look fat and flabby

Adverse Effects & Steroids


Most data on long-term effects comes from case studies
Incidence of life threatening effects appears to be low Serious side effects may be under-recognized and under-reported

Animal studies
In one study, exposing male mice to steroid doses comparable to those abused in human athletes for onefifth of their life span resulted in a high percentage of premature deaths

Adverse Effects
Males Infertility Gynecomastia Atrophy of testicles Male pattern baldness Acne Erythrocytosis Sleep apnea azoospermia

Females 200-300 mg Enlargement of the clitoris Deep voice Excessive growth of body hair Male pattern baldness Acne Atherogenesis Bleeding on withdrawal

AE androgens
Na retention especially in HF and renal dx Elevated liver enzymes Cholestatic Jaundice In the aged prostrate hyperplasia

C/I androgens
Pregnancy or planning to be Tumours of the prostrate, breast Infants Renal or cardiac dx ? Hepatocellular ca

Adverse Effects
Musculoskeletal system
Short stature Tendon rupture

Cardiovascular system
Myocardial infarction Left ventricular hypertrophy

Adverse Effects
Liver
? Cancer Peliosis hepatitis (blood filled cysts)

Skin
Acne Cysts Oily skin and hair

Steroids: Adverse Effects in abuse


Infections Nonsterile injection techniques Contaminated steroid products from clandestine labs Increased risk for
HIV, hepatitis B and C Infective endocarditis Infections/abscess formation at injection site

Samuel Wilson Fussell


When faced with the syringe, even my own worst fears didnt matter, I couldnt stop. Seventeen-inch arms were not enough, I wanted 20. And when I got to 20, I was sure that Id want 22. My retreat to the weight room was a retreat into the simple world of numbers. Numerical gradations were the only thing left in my life that made sense. Twenty was better than 17, but worse than 22. Bench pressing 315 was better than bench pressing 275, but worse than 365. I was reduced to a world where such thinking ruled, and it was only by embracing it that I could sleep at night. Muscle: Confessions of an Unlikely Bodybuilder, 1991

Real Life Example


21 year old male using for four weeks 1 cc testosterone cypionate (injectable) 1 Anadrol tablet
Body weight 180 pounds to 210 pounds 1 RM Bench press 225 pounds to 290 pounds

Conclusions
Criminal offense
Distribution is a felony
5 years imprisonment and/or $250,000

Possession without a legal prescription


Misdemeanor

Educate people on side-effects Long-term studies Blood testing Ethical alternatives for athletes

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