Halotestin® (fluxymesterone)

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Quick overview: Active Life: 6-8 hours
Drug Class: Highly Anabolic/Androgenic Steroid (Oral)
Average Dose: Men 20-40 mg/day
Acne: Yes
Water Retention: No
High Blood Pressure: Rare
Liver Toxic: Yes, very high
Aromatization: Debatable
DHT Conversion: No
Decrease HPTA function: Yes, moderate
Halotestin is the Upjohn brand name for the steroid fluoxymesterone. Structurally fluoxymesterone is a derivative of testosterone, differing from our base androgen by three structural alterations (specifically l7alpha-methyl, 11 beta-hydroxy and 9-fluoro group additions). The result is a potent oral steroid that exhibits extremely strong androgenic properties. This has a lot to due with the fact that it is derived from testosterone, and as such shares important similarities to this hormone. Most importantly, like testosterone, Halotestin appears to be a good substrate for the 5-alpha reductase enzyme. This is evidenced by the fact that a large number of its metabolites are found to be 5-alpha reduced androgens, which coupled with its outward androgenic nature, suggests it is converting to a much more active steroid in androgen responsive target tissues such as the skin, scalp and prostate.
The 11 beta-hydroxyl group also inhibits aromatization, making estrogen production impossible with this steroid. Estrogenic side effects such as water retention, fat fain and gynecomastia are therefore not a concern when taking this compound. Strong androgenic side effects are to be expected though, and in many cases are unavoidable. Oily skin and acne a very common for instance, at times requiring sensitive individuals to seek some form of topical or even prescription drug treatment to keep it under control. Hair loss is an additional worry, making Halotestin a poor choice for those with an existing condition. Aggression may also become very pronounced with this drug. This effect is often desired by users looking to "harness" this in order to increase the intensity of workouts or a competition. Clearly Halotestin is a strong androgen, and definitely one female athletes should stay away from. Masculinizing side effects can be intense, and may occur very rapidly with this substance. Even women daring enough to take Dianabol should think twice about this compound, as virilization symptoms are most often permanent.
Although Halotestin appears to be more androgenic than testosterone, the anabolic effect of it is not very strong. This makes it a great strength drug, but not the best for gaining serious muscle mass. The predominant effect seen when taking Halotestin is a harder, more dense look to the muscles without a notable size increase. It is therefore very useful for athletes in weight-restricted sports like wrestling, powerlifting and boxing. The strength gained from each cycle will not be accompanied by a great weight increase, allowing most competitors to stay within a specified weight range. Halotestin also makes an excellent drug for bodybuilding contest preparation. When the competitor has an acceptably low body fat percentage, the strong androgen level (in absence of excess estrogen) can elicit an extremely hard and defined ("ripped") look to the muscles. The shift in androgen/estrogen ratio additionally seems to bring about a state in which the body may be more inclined to burn off excess fat and prevent new fat storage. The "hardening" effect of Halotestin would therefore be somewhat similar to that seen with trenbolone, although it will be without the same level of mass gain. Clearly non-aromatizing androgens such as Halotestin and trenbolone can play an important role during contest preparations.
The main concern with this steroid is that it can be a very toxic drug. This is due to the fact that fluoxymesterone is a 17 alpha alkylated compound, its structure altered to survive oral administration. l7alpha alkylation can be very harsh to the liver. The possibility of damage is therefore a legitimate concern with Halotestin, especially when used at higher doses or for prolonged periods of time. The total daily dosage is likewise best kept in the range of 20-40mg, used for no longer than 8 weeks. After which an equally long break (at a minimum) should be taken from all c17-AA orals. One should also resist the temptation to stack this drug with other alkylated orals if possible, and instead opt for orals without this alteration or esterified injectable compounds (which will not add to the strain on the liver).
In cutting phases a mild anabolic such as Deca-Durabolin or Equipoise might prove to be a good addition, as both provide good anabolic effect without excessive estrogen buildup. Here Halotestin will provide a well needed androgenic component, helping to promote a more solid and defined gain in muscle mass than obtained with an anabolic alone. Perhaps Primobolan Depot would even be a better choice, as with such a combination there is no buildup of estrogen (and likewise even less worry of water and fat retention). For mass we could alternately use an injectable testosterone. A mix of 400-800mg Testosterone enanthate and 20-30mg Halotestin for example, should prove to be an exceptional stack for strength and muscle gain. This however would be accompanied by a more significant level of side effects, both compounds exhibiting strong androgenic activity in the body.
Fluoxymesterone also seem to depress endogenous testosterone levels rather quickly with use, despite its complete lack of estrogen conversion. One therefore should consider ancillary drug use at the conclusion of each cycle in order to help restore the normal release of androgens in the body. Using a combination of HCG and clomid/nolvadex is of course the best option, the two drugs working well together to restore normal hormonal functioning. Although estrogen is not a problem with Halotestin, the use of an anti-estrogen such as nolvadex or Clomid is still indicated when discontinuing a cycle. Since HCG stimulates aromatase activity in the Leydig's cells, here nolvadex/Clomid help by blocking the activity of any excess estrogen that may be produced. Afterward they will also block the inhibitory effect of endogenous estrogens on the hypothalamus, stimulating the enhanced release of gonadotropins and supporting the normal biosynthesis of testosterone.
Since Halotestin is only used for a few specific purposes, it is not in high demand among athletes. Likewise it is not a very popular item on the black market. Investing in the manufacture of a counterfeit version would probably not pay off well, no doubt the reason we haven't seen any yet. All of the various forms of Halotestin could therefore be assumed legitimate when found in circulation. Currently the most popular item found on the black market is the Stenox brand from Mexico, sold in boxes of 20 tablets. Although the dosage of these tablets is only 2.5mg, the low price usually asked for this preparation more than compensates. Overall, Halotestin is an effective steroid for a narrow range of uses, and is probably not the most ideal product for the recreational user.

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Halotestin

(fluoxymesterone)

Halotestin (Fluoxymesteron) is legendary among powerlifters and strength athletes. The mere word conjures up images of little mint colored pills that turn Dr. Jeckyl instantly into Mr.Hyde. Since I´m generally Mr.Hyde 24/7 this isn´t of much concern to me.. but lets see what else Halotestin can do for us.
If you´re anything like me, the first thing you´ll notice is Halotestin´s absurd Anabolic and Androgenic rating. This stuff is 19x as anabolic as testosterone and 8.5x as androgenic! Whoa! I have to admit, those numbers are a bit deceiving, and through personal experience, I can say that Halotestin will not put anywhere near as much muscle on you as testosterone. Let´s take a closer look at Halo and see what kind of realistic effects we can expect from it, and what kind of side effects we´ll be dealing with.
Firstly, I have to admit that I love this stuff, and generally its use in athletics and powerlifting is far more pronounced than it´s use in bodybuilding, where it is basically a one-trick-wonder used in the final weeks before a contest to harden up an already lean physique and give the user some added aggression during the final calorie depleted workouts before a contest. Halo has no estrogenic activity, and thus will not cause any kind of water retention or most of the bad effects associated with estrogen. It is however hepatoxic (liver toxic) (13) and I recommend keeping doses at or around 40mgs/day for a maximum of 4-6 weeks. If you are using it for it´s pronounced effect on aggression, you can simply use 10mgs prior to a workout, I personally prefer 10mgs upon rising and 10mgs prior to a workout, during the most intense weeks of a bulking or cutting cycle. This does (as you will see later) can be used with minimum HPTA inhibition.
Effects of Halotestin

Halotestin also has a volumizing effect on the physique, and for those with low a body fat percentage, this will cause an immediately more contest ready appearance. This is due, at least in part, to Halo´s ability to increase mean hematocrit with and hemoglobin level as well as red cell mass (4)(5)(6). Halotestin also appears to act through cells already committed to respond to erythropoietin (11), which is good news for athletes, of course. As you can see, Halo has quite a profound effect on red blood cell production, and this action is clearly one of the most obvious mechanisms by which it is thought to exert its effects with regards to increasing strength and energy levels. It also points to the possibility of using it for athletics and sports where a high VO2 max is needed, such as Rugby, Mixed Martial Arts, etc..
It also exerts its effects on strength and fat loss by both regulation of fatty acid oxidation in the liver and fast-twitch muscle mitochondria (2). Oddly, for a drug which exerts such a nice anabolic effect, and promotes such good strength gains, it has a pretty low Androgen Receptor Binding affinity (14).. I suppose, in this respect it can be compared to Winstrol (Stanozolol).
As far as strength and agression goes, Halo is a great drug. It is especially useful on a cutting or strength cycle. It´s use for mass and weight gains have been pretty disappointing for most users, however.
Fluoxymesterone administration is (unfortunately) accompanied by a reduction in thyroid binding globulin which causes associated decreases in T3, while the free T4 index remained totally unaltered; thus implying that thyroid function was unchanged. Remember, many anabolic steroids (notably Trenbolone) lower your T3 levels. In addition, during fluoxymesterone administration, there was a reduction in testosterone, gonadotropins and LH response to LHRH. Basal TSH did not vary, but there was a reduction in the peak and integrated TSH response to TRH. PRL levels tend to remain unchanged during fluoxymesterone use (8). Halo is of course suppressive to your HPTA, but I´ve found that in some studies where measurements were made of serum FSH, LH, testosterone, up to 20mgs per day of Halo did not suppress them measurably (9). This could possibly indicate the use of up to 20mgs/day of Halotestin without being in any great danger of suppressing endogenous hormones.
Halotestin as Steroid

Anyway, Halotestin is a testosterone derived steroid, and has an 11-beta group attached to it to inhibit aromatization, although it is particularly prone to being 5-alpha-reduced and may thus cause DHT related side effects, such as acne and hair loss. It is metabolized primarily by 6 beta-hydroxylation, 4-ene-reduction, 3-keto-reduction, and 11-hydroxy-oxidation. We know this by the identification of 4 particular metabolites and the tentative identification of at least 3 other metabolites. Detection of Halo in urine is possible for at least 5 days after a single 10 mg oral dose to previously untreated adult males, by monitoring the presence of 2 metabolites, since the parent drug is not detectable more than 1 day after the dose(12). However, the moral-compass of the athletic world, the IOC, has developed a test for fluoxymesterone metabolites that will detect them for up to 2 months after cessation of use.
This item is not in high demand in bodybuilding except for as a pre-contest drug, and would more likely be found circulating in Athletic and Powerlifting circles, where it is more commonly used in a cycle.
Halotestin (Fluoxymesteron) Profile

[9-alpha-fluoro-11-beta-hydroxy-17-alpha-methyl-4-androstene-3-one,17b-ol]
Molecular Weight: 336.4457
Formula: C20 H29 F O3
Melting Point: 240C
Manufacturer: Upjohn, Various
Date Released: 1957
Effective Dose:10-40mgs/day
Active life:6-8 hours
Detection Time: 2 months
Anabolic/Androgenic ratio:1,900/850
References:

1. Treatment with anabolic steroids increases the activity of the mitochondrial outer carnitine palmitoyltransferase in rat liver and fast-twitch muscle. Biochem Pharmacol. 1991 Mar 1;41(5):833-5.
2. Effects of synthetic androgen fluoxymesterone on triglyceride secretion rates in the rat.Proc Soc Exp Biol Med. 1975 Jun;149(2):452-4.
3. Metabolism of anabolic steroids in humans: synthesis of 6 beta-hydroxy metabolites of 4-chloro-1,2-dehydro-17 alpha-methyltestosterone, fluoxymesterone, and metandienone. Steroids. 1995 Apr;60(4):353-66.
4. Influence of fluoxymesterone on in vitro erythropoiesis affected by leukemic cells.Exp Hematol. 1984 Mar;12(3):171-6.
5. [Erythropoietin in serum and urine in healthy persons and patients with chronic renal disease upon hypoxic stimulation and hypoxic stimulation after pretreatment with fluoxymesterone (author´s transl)]
6. Fluoxymesterone therapy in anemia of patients on maintenance hemodialysis: comparison between patients with kidneys and anephric patients. J Dial. 1977;1(4):357-66
7. Combination hormonal therapy with tamoxifen plus fluoxymesterone versus tamoxifen alone in postmenopausal women with metastatic breast cancer. An updated analysis.Cancer. 1991 Feb 15;67(4):886-91.
8. Effect of non aromatizable androgens on LHRH and TRH responses in primary testicular failure.Horm Metab Res. 1984 Sep;16(9):492-7.
9. The effect of synthetic androgens on the hypothalamic-pituitary-gonadal axis in boys with constitutionally delayed growth. J Pediatr. 1979 Apr;94(4):657-62.
10. The effect of synthetic androgens on the hypothalamic-pituitary-gonadal axis in boys with constitutionally delayed growth. J Pediatr. 1979 Apr;94(4):657-62.
11. Steroids and hematopoiesis. II. The effect of steroids on in vitro erythroid colony growth: evidence for different target cells for different classes of steroids. J Cell Physiol. 1976 Jun;88(2):135-43.
12. Testing for fluoxymesterone (Halotestin) administration to man: identification of urinary metabolites by gas chromatography-mass spectrometry. J Steroid Biochem. 1990 Aug 28;36(6):659-66.
13. Toxic effects of anabolic-androgenic steroids in primary rat hepatic cell cultures. J Pharmacol Toxicol Methods. 1995 Aug;33(4):187-95.
14. 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.
15. The relationship of androgen to the thyrotropin and prolactin responses to thyrotropin-releasing hormone in hypogonadal and normal men. J Clin Endocrinol Metab. 1981 Feb;52(2):173-6.