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Autor Tema: Winstrol: Bad News and More Bad News  (Pročitano 24168 puta)

Van mreže Polomac

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Winstrol: Bad News and More Bad News
« poslato: Januar 10, 2010, 01:18:21 pre podne »
Winstrol: Bad News and More Bad News      
Written by Dan Gwartney, MD   
Wednesday, 06 January 2010

In 1988, the sporting world was rocked by the announcement proclaiming that Ben Johnson, a Canadian sprinter who’d just shamed Carl Lewis in the Olympic 100-meter race, tested positive for anabolic steroid use. Johnson, who tested positive for stanozolol, was banned for several years from competition, losing his gold medal and an estimated $8.2 million in endorsements.1 Then, the Steroid Control Act of 1990 was passed and steroids became classified as a controlled substance.

Little Potency, Lots of Danger
Stanozolol, known classically by the trade name Winstrol, is a relatively mild steroid in terms of mass or strength gains, yet is extremely popular, particularly with bodybuilders and performance athletes.2  Winstrol (now sold under a variety of brand names and varying tablet strengths and concentrations) was originally available either as a low-strength tablet of two milligrams or as an aqueous suspension containing 50 milligrams per milliliter (mg/ml). Its use was commonly reserved for pre-competition phases for bodybuilders, as it aided in imparting a hardened appearance. In an audiotape series released in 1995 by the magazine Muscle Media 2000, one speaker suggested that a number of runners, particularly endurance runners, used a comparatively low dose of Winstrol to prevent muscle loss secondary to the catabolism experienced during long-distance training and competitions.
Stanozolol is the generic name for the chemical 17-Methyl-5alpha-androstano(3,2-c)pyrazol-17beta-ol, identified as CAS registry number 302-96-5.3 Considered to be a highly anabolic steroid due to its impressive anabolic/androgenic ratio, it’s in fact a very mild steroid in terms of muscle or strength gains. The surprising lack of potency is explained by the fact that stanozolol is a very weak androgen and as an anabolic agent, is less effective than a comparable dose of testosterone.4
Despite its relatively low potency, stanozolol is still commonly abused, in part due to its reputation for being a “safe” steroid. While stanozolol does not have the more dramatic or obvious side effects seen with many of the highly androgenic steroids, it’s by no means safe. In fact, the published record of medical reports suggests stanozolol may be one of the most dangerous forms of steroids to use.

    State of Confusion
The confusion surrounding stanozolol is understandable as its actions are complex and poorly understood. Stanozolol, based upon the highly androgenic, reduced form of testosterone, DHT, would seemingly be a potent androgen, responsible for increased aggression, hair loss and acne. In fact, stanozolol is a very weak androgen4 and rather than promoting aggression, it’s been found to suppress aggression in animals such that they will not even respond to physical provocation or the presence of a male intruder.5,6 Further, the male sex glands, specifically the seminal vesicles, do not respond to stanozolol as a testosterone substitute and rats maintained on stanozolol lose the ability to ejaculate,6,7 eventually eliminating all sexual behavior.8 A similar response is seen in female rats failing to become sexually receptive under the influence of estrogen.9 Thus, in terms of behavior, stanozolol appears to act more as an anti-androgen, rather than an androgen. If these results are applicable to humans, it would make an athlete less competitive and interfere with normal sexual relations.
Complicating the social and psychological effects of stanozolol are the numerous reports demonstrating that stanozolol actively blocks normal brain function in a variety of receptor systems, and may interfere with anti-depressants and anxiety medications.10-12  Many steroid users describe a period of “depression” after completing a cycle of steroids and the findings from these studies suggest stanozolol may be exceptionally problematic for those who are subject to the psychological effects of steroid withdrawal. While stanozolol may be a less likely candidate to cause events described as “roid rage,” it may be a dangerous drug for anyone predisposed to suicide or other psychological trauma.

    Examined by Science
Referring back to its chemical structure, as a DHT derivative, stanozolol is a reduced steroid, meaning it’s not a substrate for the enzyme aromatase, which is the enzyme responsible for converting most androgens into estrogens (female hormones). Indeed, few bodybuilders report estrogen-related side effects during or following a stanozolol-only cycle. However, the safety of stanozolol in this regard appears to be overstated; drawing upon an animal study, stanozolol was found to accelerate sexual maturation in female, pre-pubescent mice.13 This effect was prevented when an estrogen blocker was given to the mice prior to the stanozolol treatment. Interestingly, though stanozolol caused early changes in the vaginas of these mice, it was not strong enough at the dose studied to cause complete sexual maturation.
While this study is inconclusive, it might suggest that stanozolol may be capable of acting as a partial-agonist for the estrogen receptor, similar to the more familiar Nolvadex (Tamoxifen). Though it may not be a substrate for aromatase, meaning it is resistant to being converted into an estrogenic (female) hormone, stanozolol can modestly stimulate aromatase activity, possibly adding to the potential for other androgens to be converted to estrogens.14
Another study, examining the effects of stanozolol on skin cells in a lab, discovered that some of the results produced by stanozolol were unique, not explained by its chemical relationship to testosterone.15 Stanozolol has been shown to increase collagen production,16 as well as certain prostaglandins and enzymes within the skin. Investigating this phenomenon, researchers discovered that in the skin fibroblast (an early, undeveloped skin cell), stanozolol could not be displaced (removed) by nortestosterone (an androgen), dexamethasone (a cortisol derivative) or estradiol (an estrogen). Rather, it was partially displaced by progesterone, another female hormone.15 Again, it was interesting to note that though progesterone could displace stanozolol from receptors in the skin cells, progesterone failed to cause the same response. The actions of stanozolol are unclear from this study. It may be possible that stanozolol is capable of interacting with many different receptors, either interfering with other hormones or acting as a weak substitute.
None of these studies directly implicate stanozolol as an estrogenic or feminizing compound, and most users’ experiences with stanozolol would confirm that it is non-estrogenic, leading to a hardened appearance with minimal water retention and few reports of gynecomastia. However, the effect of stanozolol, when combined with other agents, may not be as worry free.

    Liver Toxicity
Stanozolol is provided in both oral and injectable forms. The chemical is identical in both preparations, the practical difference being that the injectable suspension allows for a higher concentration, usually at a lower cost.2 Stanozolol may be taken orally due to the presence of a methyl group (a small side chain) added to the steroid structure. This addition of the methyl group makes stanozolol one of the 17-alkylated steroids, which are commonly known for being more toxic to the liver than the injectable steroid esters.
The liver toxicity of stanozolol is often understated, with most users believing stanozolol is among the least toxic of steroids. In fact, the exact opposite may be closer to the truth. Oral stanozolol has been used for many years in the treatment of a variety of medical conditions, and new uses are being investigated.17-28 Even under conditions in which the drug is prescribed by a physician, dispensed from a legitimate pharmacy, and taken as directed, serious liver damage can occur. In some of the long-term studies reported, half or more of the subjects needed to have the dose lowered or even discontinue treatment due to elevations of the liver enzymes, a sign of cellular damage.22,26 However, most studies concluded that in nearly all cases, the signs and symptoms of liver damage went away with proper intervention and that stanozolol was felt to be a safe treatment alternative for certain conditions.18-20,22,25,27,28
The damaging effect of stanozolol upon the liver appears to be very common, and is of greater severity at higher doses. A binding protein has been discovered in rat and human liver specific for stanozolol and danazol, another steroid.29 Studies have proven stanozolol to be hepatotoxic (damaging to the liver).30-32 The effect of an extremely high level of stanozolol (400 times the recommended dose) upon liver cells failed to show any evidence of stanozolol  causing or promoting cancer in those cells, even when exposed to other known carcinogens.33 This does not mean, however, that stanozolol is protective against cancer or risk-free, as these results would have to be confirmed and other chemicals may interact with stanozolol in a way that was not evaluated.
A case report has been published detailing severe liver damage and acute renal failure in a bodybuilder following the use of stanozolol (i.m. 50 mg every other day) stacked with metandienone (10-50 mg/day) for 80 days.34  This 28-year-old man showed up jaundiced (yellow skin and eyes) three weeks after completing his cycle, and deteriorated for seven weeks until time and treatment allowed him to recover (at significant expense).

More Bad News
This is not the only reported case of serious health consequences associated with stanozolol. A brief literature search revealed two deaths due to heart attacks,35 two heart attack survivors,36,37 one dangerous cardiac rhythm38 and a life-threatening blood loss,39 all in young men. Few steroids are so commonly associated with serious events such as these, which suggests stanozolol is not yet fully understood.
There are a number of other side effects and consequences associated with stanozolol use, but these are well known and generally accepted by the professional and athletic community. Briefly, stanozolol negatively affects the risk of heart attack or stroke by lowering the “good cholesterol” and raising the “bad cholesterol.”25,40,41 Women may experience masculinizing effects even at very low doses (2 mg/day).2,22,26,28 Stanozolol also increases the risk of serious bleeding, from the annoyance of nosebleeds to the life-threatening condition known as esophageal varices;23-25,31,39 may make tendons more prone to injury;42,43 is easily detected in hair and urine and remains detectable for several months following discontinuation;44-48 suppresses natural testosterone production;49,50 and dramatically lowers the carrier protein for androgens in the blood, called sex-hormone binding protein (SHBG).51,52
SHBG, which protects androgens from being metabolized and cleared from the body, is decreased by 50 percent with three days’ use of a low dose of stanozolol.51,52 At first glance, this may appear to be a positive effect, making what androgens are injected or swallowed less likely to be “bound” (prevented from stimulating muscle growth), instead allowing the steroid to float in the bloodstream as a “free” steroid, whereby it can interact with the muscle cell and cause hypertrophy. This is not such a benefit in the body, as SHBG protects androgens from rapid degradation and allows for the effect of testosterone or other androgens to persist for a longer period. SHBG lowers as a defense mechanism, allowing the body to shed excess androgens more quickly.

    Summing Up
In conclusion, stanozolol, generally known as Winstrol, is a commonly abused steroid that’s felt by many users to be a very mild and safe anabolic. Though stanozolol doesn’t carry the risk of the more obvious and dramatic androgenic or estrogenic side effects of other drugs, it may be all the more dangerous for its subtle nature. Stanozolol appears to act upon many different systems in the body and brain, affecting many functions beyond androgen-stimulated hypertrophy of the muscle.
It’d been shown to mimic the effects of estrogen and shares a binding site with progesterone (female hormones); decreases sexual drive, sexual function and aggression; may cause or interfere with the treatment of psychological disorders; is highly likely to cause liver damage (fortunately this appears to be reversible in most cases); and may be involved with the development of life-threatening or fatal events, including heart attacks and bleeding. It may cause the body to more rapidly clear androgens and is easily detectable for long periods in both hair and urine.
Bodybuilders report using doses of 50-100 mg/day,2 yet doses as low as six to 10 mg/day have been shown to increase nitrogen retention greater than 200-300 milligrams of testosterone enanthate/week.53 This low dose has been used safely in studies monitored by physicians, though more than half of users, even at this low dose, need to have the dose lowered or discontinued due to liver damage or other side effects. Given that there are other steroids with fewer known risks, and that stanozolol is comparatively weak as both an androgen and an anabolic steroid, greater caution should be used by those considering stanozolol.

1.    Benjamin D. Shame of the Games. Available through Time Magazine online, http://www.time.com/time/daily/newsfiles/olympics/summer88/johnson.html accessed June 28, 2002.
2.    Llewellyn W. Anabolics 2002. Molecular Nutrition Press, Patchogue NY, 2002 pp 177-80.
3.    ChemIDPlus. Provided through the National Library of Medicine. Available at http://www.chem.sis.nlm.nih.gov/chemidplus accessed June 28, 2002.
4.    Saartok T, Dahlberg E, et al. Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin. Endocrinology 1984 Jun;114(6):2100-6.
5.    McGinnis MY, Lumia AR, et al. Physical provocation potentiates aggression in male rats receiving anabolic androgenic steroids. Horm Behav 2002 Feb;41(1):101-10.
6.    Clark AS, Barber DM. Anabolic-androgenic steroids and aggression in castrated male rats. Physiol Behav 1994 Nov;56(5):1107-13.
7.    Clark AS, Harrold EV. Comparison of the effects of stanozolol, oxymetholone, and testosterone cypionate on the sexual behavior of castrated male rats. Behav Neurosci 1997 Dec;111(6):1368-74.
8.    Clark AS, Harrold EV, et al. Anabolic-androgenic steroid effects on the sexual behavior of intact male rats. Horm Behav 1997 Feb;31(1):35-46.
9.    Blasberg ME, Clark AS. Anabolic-androgenic steroid effects on sexual receptivity in ovariectomized rats. Horm Behav 1997 Dec;32(3):201-8.
10.    Masonis AE, McCarthy MP. Direct interactions of the androgenic/anabolic steroids with the peripheral benzodiazepine receptor in rat brain: implications for the psychological and physiological manifestations of androgenic/anabolic steroid abuse. J Steroid Biochem Mol Biol 1996 Aug;58(5-6):551-5.
11.    Masonis AE, McCarthy MP. Effects of the androgenic/anabolic steroid stanozolol on GABAA receptor function: GABA-stimulated 36Cl-influx and [35S] TBPS binding. J Pharmacol Exp Ther 1996 Oct;279(1):186-93.
12.    Masonis AE, McCarthy MP. Direct effects of the anabolic/androgenic steroids, stanozolol and 17 alpha-methyltestosterone, on benzodiazepine binding to the gamma-aminobutyric acid(a) receptor. Neurosci Lett 1995 Apr 7;189(1):35-8.
13.    Whitney AC, Clark AS. Effects of acute stanozolol treatment on puberty in female rats. Biol Reprod 2001 May;64(5):1460-5.
14.    Roselli CE. The effect of anabolic-androgenic steroids on aromatase activity and androgen receptor binding in the rat preoptic area. Brain Res 1998 May 11;792(2):271-6.
15.    Ellis AJ, Cawston TE, et al. The differential effects of stanozolol on human skin and synovial fibroblasts in vitro: DNA synthesis and receptor binding. Agents Actions 1994 Mar;41(1-2):37-43.
16.    Falanga V, Greenberg AS, et al. Stimulation of collagen synthesis by the anabolic steroid stanozolol. J Invest Dermatol 1998 Dec;111(6):1193-7.
17.    Revenga F, Aguilar C, et al. Cryofibrinogenaemia with a good response to stanozolol. Clin Exp Dermatol 2000 Nov;25(8):621-3.
18.    Parsad D, Pandhi R, et al. Stanozolol in chronic urticaria. J Dermatol 2001 Jun;28(6):299-302.
19.    Helfman T, Falanga V. Stanozolol as a novel therapeutic agent in dermatology. J Am Acad Dermatol 1995 Aug;33(2 Pt 1):254-8.
20.    Daniel F, Rao DG, et al. A pilot study of stanozolol for advanced breast carcinoma. Cancer 1991 Jun 15;67(12):2966-8.
21.    Cooper RG, Mitchell WS, et al. Fibrinolytic enhancement with stanozolol fails to improve symptoms and signs in patients with post-surgical back pain. Scand J Rheumatol 1991;20(6):414-8.
22.    Sheffer AL, Fearon DT, et al. Hereditary angioedema: a decade of management with stanozolol. J Allergy Clin Immunol 1987 Dec;80(6):855-60.
23.    Broekmans AW, Conard J, et al. Treatment of hereditary protein C deficiency with stanozolol. Thromb Haemost 1987 Feb 3;57(1):20-4.
24.    Belch JJ, Madhok R, et al. The effect of increasing fibrinolysis in patients with rheumatoid arthritis: a double blind study of stanozolol. Q J Med 1986 Jan;58(225):19-27.
25.    Kluft C, Preston FE, et al. Stanozolol-induced changes in fibrinolysis and coagulation in healthy adults. Thromb Haemost 1984 Apr 30;51(2):157-64.
26.    Chesnut CH, Ivey JL, et al. Stanozolol in postmenopausal osteoporosis: therapeutic efficacy and possible mechanisms of action. Metabolism 1983 Jun;32(6):571-80.
27.    Cicardi M, Bergamaschini L, et al. Morphologic evaluation of the liver in hereditary angioedema patients on long-term treatment with androgen derivatives. J Allergy Clin Immunol 1983 Sep;72(3):294-8.
28.    Cicardi M, Bergamaschini L, et al. Long-term treatment of hereditary angioedema with attenuated androgens: a survey of a 13-year experience. J Allergy Clin Immunol 1991 Apr;87(4):768-73.
29.    Luzardo OP, Machin RP, et al. Photoaffinity labeling identification of a specific binding protein for the anabolic steroids stanozolol and danazol: an oligomeric protein regulated by age, pituitary hormones, and ethyl estradiol. Endocrinology 2000 Sep;141(9):3377-87.
30.    Boada LD, Zumbado M, et al. Evaluation of acute and chronic hepatotoxic effects exerted by anabolic-androgenic steroid stanozolol in adult male rats. Arch Toxicol 1999 Nov;73(8-9):465-72.
31.    Harkin KR, Cowan LA, et al. Hepatotoxicity of stanozolol in cats. J Am Vet Med Assoc 2000 Sep 1;217(5):681-4.
32.    Welder AA, Robertson JW, et al. Toxic effects of anabolic-androgenic steroids in primary rat hepatic cell cultures. J Pharmacol Toxicol Methods 1995 Aug;33(4):187-95.
33.    Ghia M, Mereto E. Assay of stanozolol for tumor initiating and promoting activity in two rat liver foci bioassays. Cancer Lett 1992 Apr 30;63(3):203-9.
34.    Habscheid W, Abele U, et al. Severe cholestasis with kidney failure from anabolic steroids in a bodybuilder. Dtsch Med Wochenschr 1999 Sep 10;124(36):1029-32.
35.    Fineschi V, Baroldi G, et al. Anabolic steroid abuse and cardiac sudden death: a pathologic study. Arch Pathol Lab Med 2001 Feb;125(2):253-5.
36.    Mewis C, Spyridopoulos I, et al. Manifestations of severe coronary heart diease after anabolic drug abuse. Clin Cardiol 1996 Feb;19(2):153-5.
37.    Goldstein DR, Dobbs T, et al. Clenbuterol and anabolic steroids: a previously unreported cause of myocardial infarction with normal coronary angiograms. South Med J 1998 Aug;91(8):780-4.
38.    Sullivan ML, Martinez CM, et al. Atrial fibrillation and steroids. J Emer Med 1999 Sep-Oct;17(5):851-7.
39.    Winwood PJ, Robertson DA, et al. Bleeding oesophageal varices associated with anabolic steroid use in an athlete. Postgrad Med J 1990 Oct;66(780):864-5.
40.    Thompson PD, Cullinane EM, et al. Contrasting effects of testosterone and stanozolol on serum lipoprotein levels. JAMA 1989 Feb 24;261(8):1165-8.
41.    Bausserman LL, Saratelli AL, et al. Effects of short-term stanozolol administration on serum lipoproteins in hepatic lipase deficiency. Metabolism 1997 Sep;46(9):992-6.
42.    Inhofe PD, Grana WA, et al. The effects of anabolic steroids on rat tendon. An ultrastructural, biomechanical, and biochemical analysis. Am J Sports Med 1995 Mar-Apr;23(2):227-32.
43.    Miles JW, Grana WA, et al. The effect of anabolic steroids on the biomechanical and histological properties of rat tendon. J Bone Joint Surg Am 1992 Mar;74(3):411-22.
44.    Cirimele V, Kintz P, et al. Testing of anabolic stanozolol in human hair by gas chromatography-negative ion chemical ionization mass spectrometry. J Chromatogr B Biomed Sci Appl 2000 Apr 14;740(2):265-71.
45.    Schanzer W, Opfermann G, et al. Metabolism of stanozolol: identification and synthesis of urinary metabolites. J Steroid Biochem 1990 Jun;36(1-2)):153-74.
46.    Choo HY, Kwon OS, et al. Quantitative determination of stanozolol and its metabolite in urine by gas chromatography/mass spectrometry. J Anal Toxicol 1990 Mar-Apr;14(2):109-12.
47.    Schanzer W, Delahaut P, et al. Long-term detection and identification of metandienone and stanozolol abuse in athletes by gas chromatography-high-resolution mass spectrometry. J Chromatogr B Biomed Appl 1996 Dec 6;687(1):93-108.
48.    Dumestre-Toulet V, Cirimele V, et al. Hair analysis of seven bodybuilders for anabolic steroids, ephedrine, and clenbuterol [In Process Citation] J Forensic Sci 2002 Jan;47(1):211-4.
49.    Ballarin E, Guglielmini C, et al. Unmodified performance in runners following anabolic steroid administration. Int J Sports Med 1986 Dec;7(6):302-6.
50.    Small M, Beastall GH, et al. Alteration of hormone levels in mormal males given the anabolic steroid stanozolol. Clin Endocrinol (Oxf) 1984 Jul;21(1):49-55.
51.    Sinnecker GH, Hiort O, et al. Functional assessment and clinical classification of androgen sensitivity in patients with mutations of the androgen receptor gene. German Collaborative Intersex Study Group. Eur J Pediatr 1997 Jan;156(1):7-14.
52.    Sinnecker G, Kohler S. Sex hormone-binding globulin response to the anabolic steroid stanozolol: evidence for its suitability as a biological androgen sensitivity test. J Clin Endocrinol Metab 1989 Jun;68(6):1195-200.
53.    Fryburg DA, Weltman A, et al. Short-term modulation of the androgen milieu alters pulsatile, but not exercise- or growth hormone (GH)-releasing hormone-stimulated GH secretion in healthy men: impact of gonadal steroid and GH secretory changes on metabolic outcomes. J Clin Endocrinol Metab 1997 Nov;82(11):3710-9.


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Odg: Winstrol: Bad News and More Bad News
« Odgovor #1 poslato: Januar 11, 2010, 05:30:56 posle podne »
opet neki BS ili ... ???