Androgens (Anabolic Steroids)
include testosterone, testosterone esters (propio-nate, enanthoate, and cypionate), danazol,
fluoxymesterone, methyltestosterone, oxandrolone, nandrolone, stanozolol,
ethylestrenol, oxymetholone, methandrostenolone, mester-olone, and boldenone.
Testosterone is secreted by the testis and is the main androgen in the plasma
of men. In women, testosterone (in small amounts) is secreted by the ovary and
adrenal glands. Many of the androgens are modified forms of testosterone (to
circumvent rapid degradation in the body) or synthetic testosterone-like drugs.
Anabolic steroids cause a retention
of nitrogen which may result in weight gain and a feeling of well-being. There
is also retention of potassium, sodium, phosphorus and chloride asso-ciated
with a gain in weight, which could be accounted for by the water held in
association with the retained salts and protein. Anabolic steroids are thought
to promote the improved use of proteins by contributing to the reversal of
catabolic processes. Increased protein synthesis has been noted in skeletal
muscle cells. They have been used in the treatment of hypogonadism, hereditary
angioneurotic oedema, osteoporosis due to androgen deficiency, and also for
enhancement of athletic performance, for stimulation of erythropoiesis in
refractory anaemias, and enhancement of stature (controversial).
Testosterone is readily absorbed on
oral administration, but is virtually ineffective since it is absorbed into the
portal circulation and metabolised by the liver before reaching the systemic
circulation. Injected testosterone also is metabolised and excreted too quickly
for the androgenic effect to manifest. In order to retard the rate of
absorption, testosterone esters in oil are used which are less polar than the free
steroid, and when injected intramuscularly are slowly absorbed. Testosterone is
metabolised mainly in the liver, at first to androstenedione, and later to
androsterone or etiocholanolone. Dihydrotestosterone is metabolised to
androsterone, androstenedione and andro-stanediol. Esters of testosterone are
hydrolysed to free testos-terone and subsequently metabolised in the manner described.
Excretion occurs principally in the urine and minimally in the faeces.
Virilising effects—Results in masculinisation
when taken by women, characterised by hirsutism, acne, deepening of the voice,
menstrual irregularities, male pattern baldness,prominent musculature, and
hypertrophy of clitoris.
Feminising effects—Seen in men who
receive androgens,* and is characterised by gynaecomastia. This is because of
conversion (by aromatisation) of the androgen to oestrogen in extraglandular
Administration of anabolic steroids
during gestation may result in masculinisation of the urogenital sinus and
clitoral hypertrophy. Premature bone maturation and decreased birthweight have
Growing children may develop
pre-mature fusion of the epiphyses of long bones, leading to permanent short
Cystic acne, sebaceous cysts,
furunculosis, and seborrheic dermatitis have occurred in persons using anabolic
Oedema—Retention of water and sodium
chloride leads to
weight gain and oedema.
Jaundice—Results from stasis and
accumulation of bile inbiliary capillaries of the central portion of hepatic
lobuleswithout obstruction in the larger ducts. Peliosis hepatis is
common: formation of blood-filled
sacks in the peripheral zones of hepatic lobules. There is elevation of plasma
levels of bilirubin, aspartate aminotransferase, and alkaline phos- phatase. An
increased predisposition to hepatic carcinoma has been reported. Hepatotoxicity
is however rare with testosterone esters.
CVS effects—Hypertension and
thrombotic complications (stroke, myocardial infarction).
Endocrine effects—Testicular atrophy,
low sperm count, sterility, gynaecomastia. In women, masculinising effects
occur (vide supra). Decreased testicular size is a common complaint among
users, and a common finding in chronic users at autopsy.
aggressiveness, iritability, psychosis. Increased aggression known as “roid
rage”, delusional grandiosity, and acts of violent crime including homicide
have been described as a result of anabolic steroid abuse by athletes.
Psychotic symptoms have been described in bodybuilders and football players
during periods of anabolic steroid abuse. Patients who chronically misuse
anabolic steroids may experience a withdrawal reaction. Anorexia, depression,
fatigue, insomnia, decreased sex drive, and dissatisfaction with body image
have all been reported.
Anabolic steroid use parallel with
exercise may lead to dysplasia of collagen fibrils, decreased tendon strength,
and increased likelihood of rupture under stress. Several cases of unusual
tendon rupture have been reported among steroid users, including that of
triceps, extensor pollicis longus, and rectus femoris.
Blood anabolic steroid levels are not clinically useful.
Withdrawal of androgen. Steroid withdrawal needs to be
treated as other drug withdrawals, including detoxification, support in denial
phase, short-term rehabilitation/recovery therapy, and long-term aftercare
Natriuresis for treatment of oedema.
Supportive and symptomatic measures. In acute single
overdosage, toxicity is unlikely. Gastrointestinal decon- tamination is
generally not needed after acute ingestion unless another toxic coingestant is
Liver-specific isoenzymes (alkaline phosphatase, lactate
dehydrogenase) should be used to monitor liver function in athletes.
Some of the effects resulting from long-term administration
Forensic Issues: Abuse of anabolic steroids by
athletesto enhance performance has attained epidemic proportions in recent
times. Athletes often take doses of androgens in 100 to 1000-fold excess over
physiologic doses. In spite of such widespread conviction about the
“beneficial” effects of anabolic steroids in relation to athletic performance,
it is not yet clear as to whether these agents really do work (except for
increasing muscle mass). The tragic part is that several athletes have died in
their prime due to the adverse effects of such abuse. Testing for anabolic
steroids in athletes is now mandatory during the course of competitive athletic
events. Testosterone abuse may be detected by checking the ratio of
testosterone to epitestos-terone. If this ratio exceeds 6 to 1, it is an
indication of exog-enous testosterone use. The International Olympic Committee
has issued strict guidelines in this regard, and suggests that gas
chromatography-mass spectrometry (GC-MS) is the best method for drug testing in
urine samples. Oral products can be detected for 2 to 14 days after the last
use, and injectables for up to a month. Nandrolone decanoate injections can be
detected up to 12 months.