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Anabolic Steroids. What are they?. Hormones synthesized from cholesterol Produced by interaction of hypothalmic, pituitary & gonadal glands Male production=5-10 mg./day Female production = 1-2 mg./day Stored in blood – not the glands Effects on body anabolic androgenic.
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What are they? • Hormones synthesized from cholesterol • Produced by interaction of hypothalmic, pituitary & gonadal glands • Male production=5-10 mg./day • Female production = 1-2 mg./day • Stored in blood – not the glands • Effects on body • anabolic • androgenic
Effects of Anabolic Steroids • Mimics Testosterone • Androgenic Effects • male sex characteristics • want to limit these effects • Anabolic Effects • increase protein & creatine phosphate synthesis • increase muscle mass • increase aggressiveness **increase oxygen carrying capacity - not proven
Anabolic Steroids • Usage began in the 1940’s • Synthetic substance developed in 1953 • IOC banned steroids in late 1960’s • IOC instituted testing at 1976 Summer Olympics • 21 FB players banned from bowl games in 1987 • Recent increase in usage
History • Developed in early 1950s for the anabolic effects • 1954 Olympic games first reported use when syringes were found in Soviet Union locker room • Introduced to US in 1960’s • Banned by IOC in 1968 • First urine tests done in 1976 at Olympic games • First confirmed use by women at 1976 Olympics after + tests of E. German swimmers
History cont. • NCAA instituted drug testing in 1986 at national competitions. 21 FB tested + that year at bowl games. • Federal Anabolic Steroid Act of 1990 classified them as controlled substances • Schedule III of Controlled Substances Act • Use has been on decline since 1980s • Probably due to increased use of prohormones • Exception is women
Types of Anabolic Steroids • Exogenous, synthetic steroids developed to decrease androgenic effects without affecting anabolic effects • Also modified to prevent 1st pass breakdown in liver • Oral (short ½ life) • Injectable (bypass liver)
Modified oral compounds have additional carbon molecule, C-17 alkylated steroids which withstand liver degradation. These are very hard on the liver. • Most injectable steroids are oil based, lipid soluble.
How do they work? • Bind to receptors in skeletal muscle, prostate, heart, testes, & brain • Cause increased protein synthesis & nitrogen retention which causes increased muscle size and strength • Prevent catabolic effects of cortisol by controlling it’s release during intense training
Anabolic Steroids - Sources • Prescription • anemia, replacement therapy, increase appetite, abnormal protein synthesis • NORMAL dose = 5-10 mg/day • Veterinarian • Blackmarket
Legitimate Medical Use • Hypogonadal men • Burn victims, AIDS patients, severe osteoporosis, breast cancer, malnourishment, adolescent disease • ?? Uses being tested • Injury treatment • Male contraception • Anti-aging • Lowering serum cholesterol
How are they taken? • Cycling • Take for a period of time and then cycle off before beginning again. • Method used to beat drug testing • Stacking • Take more than one at a time trying to achieve synergistic effect • Pyramiding • Gradually increase number and amount of compounds to maximize effects and decrease side effects
Health Risks of Steroid Use • Not well tested or documented • History of misinformation by medical community • Unethical to administer doses equal to abuse levels • Funding • Retrospective studies are unreliable
Abuse Effects on Women • Hirsutism - facial • Skin coarsening ** • Deepening of voice ** • Breast tissue reduction • Alteration of menstrual cycles • Facial masculization ** • Clitoral enlargement • ** irreversible after prolonged use
Abuse Effects on Men • Decreased endogenous serum testosterone (as little as 3 weeks) (12 weeks = problems) • Testicular atrophy • Impaired sperm production • Impotence • Male pattern baldness ** • Prostate enlargement ** • Gynecomastia (aromatization) ** • ** irreversible after prolonged use
Abuse Effects on Teenagers • Same sex effects • Premature epiphyseal growth plate closure
Abuse Effects on Both Sexes • Severe acne • Weakened tendons • Jaundice • Fluid retention • Cardiovascular effects
Effects on liver • Liver toxicity • Cancer • Formation of blood filled sacs • Pre-existing conditions could lead to more serious problems
Cardiovascular Effects • Reduction of HDL levels • High BP • Enlargement of heart
Psychiatric Symptoms • “Roid rage” • Not well documented, anecdotal evidence • Reported after high dosage levels, sustained use • Athletes could be predisposed to anger • Psychological dependence • “bigger biceps” mindset • Sociological pressure • Suppressed endogenous testosterone production after abuse
Other Adverse Effects • Connective tissue injuries • Musculotendinous areas • Needle contamination • Blood borne pathogens • Counterfeit steroids • Contamination
Drugs used to counter effects • Cytadren & Arimidex (s) • Counters aromatization • Tamoxifen • Reduce gynecomastia • Clomid (s) • Restore natural testosterone production • Nolvadex • Anti-bloating • HCG (Human chorionic gonadotropin) • Avoiding testicular atrophy
Legal Implications • Anabolic Steroid Act 1990 classified them as controlled substances • Use • 1st offense = 1 yr. jail & $1000 fine • 2nd offense = up to 2 yrs. jail & minimum of $2500 fine • Selling & distribution • Federal offense • 1st offense = up to 5 yrs. jail and $250,000 fine • 2nd offense = up to 10 yrs. jail & higher fine
Anadrol oxymetholone Arimidex anastrozole Deca Durabolin Nandrolone deconaoate Dianabol methandrostenolone Equipoise boldenone Parlodel bromocriptine Primobolan Depot Methenolone enanthate Trenbolone acetate Winstrol Depot stanozolol Oxandrin oxandrolone Common Brands, Names
Anabolic Steroids - Administration • Oral – Dianabol, Android, Anadrol, Oxandrin • EXCESSIVE dose = >25-50 mg/day (200 mg/day) • Injection – Deca-Durabolin, DEPO-Testosterone • EXCESSIVE dose = >100-200 mg/week • Programs • stacking - use of oral & injectable • pyramiding - then usage • cycling - on/off (6-12 wks)
Drug Testing • Urine test • Test 1 hr. after announcing test • Masking agents – Benemid, Corticosteroids, DHEA, other substances • T/E Ratio • also measure concentration of testosterone and specific gravity
Drug Testing Problems • Detection of substances that occur naturally in the body is difficult. Also must set standards of sensitivity to accommodate these levels. • Testosterone / epitestosterone ratio of 6:1 is standard guide but higher ration can occur naturally in 2-3% of population. • Baseball, NHL, NBA do not ban their use. • IOC, NCAA, NFL do ban use.
History • Through 1980’s the medical establishment concluded “use of these agents (androgens) does not cause an increase in muscle bulk, strength, or athletic performance”. • Athletes “knew better” • Bhasin (1996) study found 600 mg. / week of testosterone ethanthate increased triceps and quadriceps size in non-exercising group as well as exercise group. No changes in mood, behavior or cardiac indicators (HDL, LDL, triglycerides)
Prohormones • Anabolic Steroid Control Act of 1990 made use of agents a federal offense.. however.. • DSHEA labeled prohormones as a nutritional supplement. • Compounds that are precursors to testosterone and readily convert, based on their proximity in the metabolic pathway.
Testosterone ^^ Androstenedione / Androstenediol ^^ DHEA ^^ 17-OH-pregnenolone ^^ Pregnenolone ^^ cholesterol
Questions That Need Answers • Does compound survive digestion? • Does compound appearing in blood convert to the active compound? • Are there downstream effects? • Do metabolic byproducts appear in the urine in a form identical to banned substances? • Does supplement have the claimed effects?
Androstenedione / Androstenediol • Made famous by Mark McGuire • Earnest (2000), Ziegenfuss (1998, 1999) found androgens converted to higher levels of serum testosterone in males. Effects on body composition only seen after 450 mg. sublinqual dose, 3-4 weeks. • Mahesh & Greenblat found 100 mg. androgens increased testosterone levels in women. • Also found elevated estradiol & estrone levels & decreased HDL levels in untrained males.
Androstenedione • Natural substance – produced in adrenal glands • Nutritional supplement • Anabolic effects, increase energy, enhance recovery
19-Norandrostenedione19-Norandrostenediol • Gammeren, et. Al, found 100 mg. Of N-dione and 56 mg. Of N-diol had no effects on body composition or strength. • Studies have shown 10 micrograms will cause + urine tests (intense training can increase concentration in urine so there can be combined effect in athletes). • 50 mg. Dose can be detected for 7-10 days after ingestion
DHEA • Brown, et. al, found 50 mg dose increased androstenedione concentrations by 150% within 60 minutes of ingestion. • 150 mg./day for 8 weeks increased serum androstenedione but had no effect on serum levels of testosterone. No difference in strength gains between groups
DHEA (Dehydroepiandrosterone) • Natural steroid hormone produced in the adrenal glands • converted to testosterone – anabolic effects • Medicinal uses – heart disease, obesity, diabetes, amount in body decreases w/age • Masking agent – normalizes T/E ratio • Available as a supplement
Delta 5 Metabolites • All studies probe these metabolites double or triple urinary testosterone & epitestosterone ratio a few hours after ingestion.
Human Growth Hormone(Somatotropin) • Hormone secreted from pituitary gland • Effects • stimulate protein synthesis • stimulate growth • increase muscle mass • increase strength of muscles, tendons, etc
Human Growth Hormone • Adverse effects • acromegaly - large hands & feet • abnormal shaped head • increase size of heart, liver, kidneys • increase cholesterol • Alternative to steroids • cheaper • harder to detect
Growth Hormone Enhancers • Amino acids (Aa) have been used to increase circulating growth hormone (GH) concentrations. • Strength training increases GH serum concentrations so looking for synergistic effect. • Most common Aa used are arginine, lysine & ornithine
Studies of Aa effects • Many studies confirm increased GH concentrations after ingestion of arginine & lysine. • Effects are modified by training level, sex, diet and age. • High levels produce stomach cramps & diarrhea • Women have greater response. • People on high protein levels (1.7-2.2 g/kg day) have less effects • Ingestion right before exercise blunts absorption
Peptide Secretagogues • Being developed and studied as compounds that stimulate secretion of endogenous GH. • Studies have all been done on GH deficient patients. • No reports of athletes using them but doesn’t mean there isn’t illegal use.
Other GH Releasing Agents • Clonidine, L-dopa & methylphenidate have been shown to induce GH release. • L-dopa most commonly used by athletes but no studies have been done on effectiveness but does induce nausea & vomiting.