Anabolic-androgene steroids(AAS)

Anabolic-androgene steroids(AAS) are synthetic derivats of male sex chormone testosterone. These compositions were created as a try to synthetize chormones with potentiated anabolic effect in organism. Fact that anabolic steroids manifest their effects by connecting to specific testosterone receptor in the cell, disabled separation of androgenic from anabolic effects. So all anabolic steroids manifest androgene effects in organism, especially if they are intaked in big doses, as it is done by athletes that use this group of substances for doping.

Chemical structure and anabolic steroids features

Anabolic-androgene steroids are divided into 4 groups according to their chemical structure:

1)      5-α androstane derivates

17-β hydroxi-5alfa-androstan-3-on doesn’t have anabolic activity, but through chemical transformation on the ring A(alciling in position 1 and 2) following anabolics are made:

• Mesterolone(short use, appliance per os)
• Metenolone
• Drostanolone(used also as antineoplastic)

2)      17 α-alkil-5 α androstane derivates

By alkalizing of position 17 derivates that are substrates for enzyme 17- β dehydrogenase to have longer effect from testosterone. Chemically, these are tertiary alcohols, that are more stabile in acid surround in gastric, so they are given per os. Typical representors are:

·         Stanozolol

·         Oxandrolone

·         Oxymetholone

3)      17α- metal testosterone derivates

·         Metandrostenolone

·         Oxymethrone

·         Bolasterone

4)      19-nor testosterone derivates(19-nor testosterone nandrolone):

·         Metandrolone

·         Etandrolone

·         Norboletone

Ratio of anabolic and androgene activity at this group is 22:1.

Clinical appliance of testosterone and anabolic steroids

There are some pathology conditions when anabolic steroids are applied:

• Hypogonadism
• Delayed puberty
• Older males, for climax and impotence
• Appliance in male contraception
• HIV/AIDS therapy
• Earlier used as antidepresives

Goals and ways of anabolic steroids use in sport

Goals of anabolic steroids users vary from their sports activities. Mutual goal of all sport competitors or recreatives is to increase lean body mass, and to reduct fat component. These are primary goals of bodybuilders. In strength sports, it is expected that increased mass will enable increase of strength and power in muscles. Athletes into the activites like swimming and running think that use of anabolic steroids will enable high intensity trainings in longer period of time. Special group are the people that want to look physically great.

Anabolic steroids are mostly taken in cycles that last 6-12 weeks or more. There are athletes that use these chormones continuosly, and increase dose in the period of preparations for competitions.

Very often more rimifon is combined, according to the schema. Users think that synergic effect will be done that way, or more receptors, through which chormones manifest their appliance. Often pyramid model is used, when dose is increased progressively, and then decreases in the end of the cycle.

There are AAS that can be taken into the organism in different ways: sublingually, through skin, nose sprays or through special flasters.

In endurance sports like in sprint it is needed to create anticatabolic effect. “Threshold” effect is common for this – under effective doses cannot cause body mass increase that is wished. There are no determined doses in power or mass for any anabolic steroid.

There is often situation that other substances are used along with anabolic steroids.

It is sure that there is coincidence of harmful effects caused by same time use of various things.

Changes in body mass and composition made under the influence of anabolic steroids

The most attention is excited by changes created in skeletal muscles, or clear muscle mass or lean body mass(LBM).

Stimulation of protein synthesis, water retention, increase of glycogen level in muscles, increase of mineral percent in bones and non-bone matherials, that are thought to be the key factors for body mass increase.

Influence of anabolic steroids on the condition of fat matheries in organism is not clear enough. Relative fat percentage drops with increase of LBM, and increase of RMR(rest metabolic rate) leads to increased fat burning. In the researches on rats AAS intake was followed by lipase activity increase in adipose tissue.

In the most of short-term researches(3-10 weeks) increase of body mass was 3-5kg.

Increase of muscle mass and muscle power that are created under the influence of anabolic steroids are primarily related to upper parts of the body. Increase of lower parts is also spotted, which was followed by increase of success in squat.

Results in muscles power has to be judged according to training level and sport experience.

Other AAS effects important for sport success

Psychological changes like increase of aggression, self-confidence and training motivation represent very important factors that lead to sport success at anabolic steroids users. Users of steroids justify use by fact that in some phases of training drop of testosterone level in blood is spotted.

It is thought that insufficient energy intake that follows the syndrome of overtrainness and restriction of groceries intake in periods of reduction(or keeping) TM (fat) is the most significant factor that leads to drop of testosterone in athletes’  organism. Similar explanation can be used also in endurance sports(testosterone level drop in plasma).

Pathology conditions related to AAS use

These are following conditions:

• Cerebrovascular and peripheral trombosis
• Adenocarcinome of the prostate
• Miocard infarct, heart stop, myocarditis and cardiomyoempathy
• Liver tumor, hepatitis, liver peliose with bleeding, serious choleostasis and jaundice
• Haemoralgic shock
• Aterosclerosis and hypercholesterolemia
• Wilms’ tumor and renal adenocarcinome
• Colone adenocarcinome
• Infertility
• Musculo-skeletal injuries
• Cosmetic effects
• HIV/AIDS
• Lethal outcome.

Psychological changes in users of anabolic steroids

The most often manifests or AAS use are:

• Aggression increase
• Irritability increase
• Increase in libido
• Feeling of good basic condition
• Feeling of faster recovery from work

The most often changes of behaviour that are spotted in contact with surround are hostility and increase of aggression towards women.

Dissatisfaction with body composition, primarily excited wish to achieve maximally big body mass and goal of drastic body fat reduction dominate in the answers of steroids users.

Following effects of break in anabolic steroids intake

Psychological manifestations that are mostly mentioned in literature after the stop of intake are:

• Depression and suicidal tendencies
• Feeling of energy loss for work, decreased concentration and insomnia
• Loss of apettite followed by loss in body mass

Symptoms of depression and following appears are treated by antidepresives, and in some cases electroconvulsive.

Effects of AAS use on female organism

It is thought that the level of intaked anabolic steroids at athletes is 30 times bigger than normal female, and 2 times bigger than normal healthy males.

Unwished effects are:

• Increase of hair in the region of face
• Male type alopecia on head apex
• Intensive acne growth
• Clitoris increase
• Decrease in the size of breasts
• Deeper voice
• Menstrual cycle disorders
• Increased psychical functions, aggressivity and libido.

Detection

Technic gas chromatography – mass spectrometry is the key factor for detection.

These procedure started with use on Olympic Games in Montreal,1976.The radioimmunoassay screening technology had a lot of failures related to steroid metabolits.

In the goal of doping detection it is needed to determine ratio of testosterone and its epimere – epitestosterone. In normal conditions this relation is T/E = 1:1. It is thought that recommendation of value T/E 6:1 is very suspicious to abuse of synthetic testosterone(but physical variations are possible), while T/E ratio of 10:1 is treated as confirmed doping. 

Anabolic steroids and testosterone level can be changed as a consequence of: animal meat intake that is treated by anabolic steroids, presence of “normal” metabolites contraceptives, chormonal changes in pregnancy.

It is thought that physiological variations are possible, in the levels of epitestosterone and other natural chormones, which is conditioned by gender, growth, weight, nutrition, diet supplements intake and other legal medication.

Variables that influent onto the concentration and detectability of anabolic-androgene steroids in urine:

• The volume of urine excreted
• Urinar pH
• Urine volume that is used for testing in laboratory
• Dose of intaked AAS, time of last consumption and way of use
• Short term or long term AAS intake
• Simultaneous use of others AAS
• Variability in AAS detection
• Differences in various laboratory techniques sensitivity and other laboratory variabilities
• Other agences(various substances and medicaments) that can influent to the way of AAS excretion
• Genetically determined athlete metabolism variations
• Fat component intake in total body composition
• Various habits influences in athletes nutrition during test
• Trauma/shock in the previous period.

Use of testosterone in the shape of skin-patches gels decreases the possibility to create bigger ratio than 6:1, and disables detection. Chormone is released easily, continuously, not causing big oscillations in plasma, by making it “safe”.

Theoretic possibilities of manipulations in order to prevent positive anabolic steroids test:

• AAS user can cause dilution(diuretics)
• User can block excretion through urine(probenecid)
• User can mask the presence of AAS in urine by use of substances that inerferate with AAS during GH-MS detection
• User can use low doses that are not treated as doping
• Doses in ratio of relation T/E = 6:1 can be intaked
• Same time use of testosterone and its epimere creates relation between these two substances 6:1.

Egzogene AAS(list not limited):

Androstenedion, bolasterone, boldenone, boldione, clostebol, danazol, dehydrochlorometyltestosterone, delta 1-androstene-3, 17-dione, drostanolone, drostanediol, fluoxymesterone, formebolone, gestrinine, 4-hydroxytestosterone, 4-hydroxy-19-nortestosterone, mestnolone, mesterolone, methandienone, metenolone, methandriol, methyltestosterone, mibolerone, nandroline, 19-norandrostenediol, 19-norandrostenedione, norbolethone, norethandrolone, oxabolone, oxandrolone, oxymesterone, oxymetholone, quinbolone, stanozolol, stenbolone, 1-testosterone(delta 1-diydro-testosterone), trenbolone and its analogues.

Endogene AAS(list not limited):

Androstenediol, androstenedione, dehydroepiandrosterone(DHEA), dihydrotestosterone, testosterone and its analogues.

Names and synonims of anabolic steroids:

Dianabol(Methandienone), Fluoxymesterone(Halotestine), Metandren(Numan, Oreton-M), Nortestosterone(Nandrolone), Oxandrolone(Anavar), Oxymetholone, Stanozolol(Stromba, Winstrol), Clostebol(4-Chlorate-stosterone Acetate, Steranabol Propionate, Yonchlon Caproate, Macrobin-Depot), Drostanolone(Methalone), Methenolone(Primobo-lan), Norethandrolone(Nilevar, Ethylnortestosterone), Oral-Turinabol(Chlorodianabol, Chlorodehyomethyltestosterone), Oxymesterone(Balnimax, Theranabol, Oranabol), Stenbolone(Anatrofin), Anroisoxazole(Neoponden), Allytrenbolone, Bolandiol(Anabiol), Bolasterone, Boldenone(Boldene, 1-Dehydrotestosterone), Bolenol, Bolmantalate, Calusterone(Methosarb), Chlordrolone, Chloroxydienone, Chloroxymesterolone, Dihydrotestosterone(Stanolone, Anaprotin), Enestebol, Formebolone(Hubernol Formyl-nolone), Furazabol( Androfuranazol), Mebolazine(Dimethazine, Roxilon), Metribolone, Mestanolone(Androstalone), Methandriol, Probolin, Anbolin, Proto-sbolin, Notandrondepot, Mibolerone, Norbolethone(Genabol), Norclostebol, Normethandrolone(Organon), Oxabolone(Steranabol Depot), Penmesterol(Pandrocine), Roxibolone(Dodecylster), Silandrone, Thiomeste-rone(Embadol, Protabol), Tibolane( Livial), Trenbolone( Parabolan, Hexabolan), Trestolone.

“Doping in sport”, Marina Djordjevic Nikic