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Antò Antò Non in Linea
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Predefinito Andriol (testosterone undecanoate) - 26-06-2007, 04:13 AM

Andriol (testosterone undecanoate)


Active Life: Less than 8 hours
Drug Class: Anabolic/Androgenic Steroid (Oral)
Average Dose: Men 240-320 mg/day
Acne: Low
Water Retention: Yes, in higher doses - 280-400 mg/day
High Blood Pressure: Yes - Dosage related
Liver Toxic: Low
Aromatization: Low to moderate
DHT Conversion: Yes in higher dosage
Decrease HPTA function: Low, except in higher dosages
Andriol is a unique oral testosterone product, developed by the international drug firm Organon. One of the more recently developed anabolic steroids, Andriol first became available in the early 1980's. This compound contains 40 mg of testosterone undecanoate, based in oil (oleic acid) and sealed inside a capsule. Subtracting the ester weight, this equates to a dosage of approximately 25mg of raw testosterone per cap. The design of this steroid is quite different from that of most oral steroids. Drugs administered orally generally enter the blood stream through the liver. When a steroid compound is given this way without some form of structural protection, it will be quickly broken down during the "first pass". This process leaves very little steroid intact, basically deactivating the drug. Adding a methyl group (c-17 AA) to the structure is one way to protect it from this process, however stress is also placed on the liver as a result. In some instances this stress can lead to actual damage to liver tissues, so the designers of this steroid sought another way to protect the testosterone molecule. With Andriol, this was accomplished by making a form of testosterone that would be absorbed through the lymphatic system. This is due to its high fat solubility brought about by the ester, and its suspension in oil. Having the compound absorbed this way was thought to be very advantageous, as it allows the steroid to bypass the destructive first-pass through liver. This should permit the compound to enter the blood stream intact, without the need for a harsh chemical alteration. The ester breaks off once it is in circulation of course, yielding free active Pharmacokinetics of Oral Testosterone. In design this steroid appears to be undecanoate that of a completely liver safe and orally active form of testosterone.
On paper this drug seems like a great oral testosterone product. Clean, safe and worlds apart from other oral testosterone derivatives like the crude methyltestosterone. But as we always hear in life, if it looks to good to be true, it probably is. There are definitely some issues with Andriol. The first problem is that bioavailability, although clearly worlds apart from trying to take straight testosterone orally, is probably not significant next to c17alpha alkylated orals. Athletes typically find that in doses of less than 240mg per day (6 capsules) effects are generally not seen at all. 240mg of testosterone ester daily, the primary male androgen, and only a meager effect. When doses go higher, maybe 8-10 capsules (320-400mg), new muscle growth is slight to moderate at best, but no incredible bulky gains are ever reported. Logic leads one to believe that only a little testosterone is making its way into circulation. Testosterone is a powerful hormone no matter what the ester or form of administration. If it were active in the blood stream, the results would have to be pronounced. When one injects an oil based testosterone ester like cypionate, a dosage of 400mg per week is more than sufficient to see results. 400mg Andriol per day should be packing on an incredible amount of mass. Where does it all go? Individual problems with absorption may play a role into things here. Clearly there is little to be said except that this drug is unpredictable in its ability to be absorbed and utilized by the body. While one day you might be getting great absorption, perhaps the next day you are getting very little. Studies with men were no better than with women, where again this drug was shown to be unpredictably absorbed and utilized with blood levels ranging from 11.5 to 60.1 nmol/L with 80mg twice daily.
One might also pay interest to the "mildness" of this compound as described by other bodybuilding materials. Andriol is often spoken about as some type of magic product, which to spite being a form of regular testosterone somehow allows for only minimal estrogen conversion. You should know that the way a drug is administered includes a number of factors that can slightly alter its effect, the most predominant being the speed of release. This effects the time it takes for a peak blood level to be reached, and likely the length it takes to see results. The primary reason Testosterone suspension seems more powerful than enanthate is because more drug is active on day one. At the same time estrogen builds up faster and side effects become pronounced very quickly. The ester is also part of the total weight, and 100mg testosterone contains a much larger quantity of testosterone molecules that testosterone plus ester, another reason for varying effect. But these changes do not amount to all that much. The structure of testosterone is what allows it to break down into estrogen. The only way we can really prevent an androgen from converting to estrogen is to change the base molecule, not the ester. Once free in the blood stream we cannot prevent testosterone from being aromatized without interfering with the aromatase enzyme itself. The lack of results and side effects often reported with Andriol must be going hand in hand with poor absorption.
Most athletes today consider Andriol a very poor buy. I know other references do find use for this drug, which is defendable because some amount of steroid clearly does enter the blood stream in tact. Technically it is still an oral testosterone, and definitely does not carry the same liver-toxicity risks associated with most steroids designed for this type of administration. Those specifically looking for a mild oral at times do purchase this product, and occasionally are even satisfied with their results. But for most its high price and required high daily dosages usually causes them to avoided it when crossing it on the black market. Besides, if we want a mild steroid the last thing we really should shop for is a testosterone.


I'm not drunk it's just epylepsy...

Quando i tuoi occhi si illuminano dell' infantile curiosità, quando i "perchè" soffocano il tuo pensiero, quando le sensazioni toccano il tuo bisogno.....adesso, solo adesso puoi definirti "vivo".....
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Predefinito 26-06-2007, 12:43 PM

Andriol

(testosterone undecanoate)

Andriol is testosterone with the undecanoate ester attached, and produced in oral form. It represents the first real attempt to create an oral testosterone since Methyl testosterone. I can only assume that the scientists responsible for this wanted to create a viable alternative to both injectable testosterones (which, at least for Hormone Replacement Therapy, is inconvenient), as well as other oral forms of testosterone (which have traditionally been very harsh on the liver). What they came up with has proven to be a very odd steroid in many ways.
To create Andriol, the scientists involved had to come up with a solution to the problems facing methyltestosterone, namely the fact that it is harsh on the liver and needs to be taken in very high doses to produce decent results. What they did was put 40mgs of Testosterone Undecanoate in oleic acid (an oil), and encapsulate it. Now they use castor oil and propylene glycol laurate instead of oleic acid, but that only increases the shelf life, and doesn´t do anything else. For some of the aspiring chemists reading this, you may be asking yourself the obvious question. And the answer is yes, you can take almost any estrified drug (Nandrolone Decanoate, for example), and dissolve it in castor oil and propelyne glycol laurate, and create your own "Deca Caps" or whatever. The problem is that you´d need to be able to make sealed gel caps, not just the typical 2-part capsules most people throw steroid powder in. Anyway, I´m digressing; lets get back to Andriol. After you put some testosterone undecanoate in caster oil and propelyne glycol laurate, you´ll have a testosterone which is highly fat-soluble due to the (very large) undecanoate ester attached to it, and able to be absorbed through your small intestine via the lymphatic system. What this means is that it avoids the "first pass" through the liver, a process which could destroy much of the active steroid, and place an undue amount of stress on the liver. It also displayed a rapid absorption and turnover in one study(11), which may account for it´s ability to not cause unwanted side effects . It´s not bad for your blood pressure (13), and also has no adverse effects on the prostate and may even improve blood pressure(12)! Thus, Andriol is remarkably light on all side effects, especially those related to liver toxicity and estrogenic sides.
Andriol for Women

In this study, done with women, it even displayed no ability to lower LH and FSH (Leutenizing Hormone and Follicle Stimulating Hormone, respectively), which are the hormones that tell your body to make more testosterone (11). I doubt Andriol could be properly regarded as liver toxic or too damaging to your HPTA (Hypothalamus-Pituitary-Testicular-Axis, the thing that governs your body´s production of testosterone, among other things). at any kind of reasonable (or even excessive) dose. Actually, one study noted no adverse reactions or effects at all with the use of Andriol (10). As for your lipid profile and cholesterol, it has even been shown to have beneficial effects on them (14)!
So, putting some Testosterone Undecanoate in Gel Caps is what the scientists at Organon have done with their Andriol product, and it all looks good so far, right? The active steroid totally bypasses your liver and hence doesn´t get damaged by or damage your liver, and gets a bunch of Testosterone into your body. Great! But what happens next? Well, after the lymphatic system has brought the testosterone undecanoate into circulation in your body, the undecanoate ester begins to be removed. This would leave you with (roughly) 25mgs of testosterone in your blood stream, as the decanoate ester takes up a lot of "space" and the cap only contains a total of 40mgs of testosterone undecanoate (roughly 15mgs of which are ester). The end results from Andriol would be very similar to the end result of injecting almost any form of testosterone (4), once your body removes the ester. But remember, you´d never inject 25mgs of testosterone suspension and call it a day, but that´s exactly what you are doing when you take only one Andriol cap.
So now you have 25mgs of testosterone floating around in your body. That´s not much, so if you´re realistically considering using this product, you´ll need to take quite a few caps of this it. And there´s one of the first problems we encounter with this drug. You see, the method of administration of this drug provides us with a nice liver-safe product, but this stuff will peak your testosterone levels within around 2 hours after administration, and will only remain (at least slightly) elevated for 10 or so hours(1). Ideally, you´d be taking a capsule every 2 hours, which is inconvenient to say the least. Let´s be generous and say you can simply take one every 4 hours. Problem solved? Not really, because we´re going to need to take at least 2 caps with each dose if we want to see any sort of anabolic effect, and if we´re taking it every 4 hours (assuming we´re awake for 16hrs every day), then we´ll be taking around 8 caps per day. Now we´ve shifted the problem away from the effort needed to take an effective does to being a problem with economics.

Andriol Side Effects

Cost not withstanding, lets see what kind of Andriol side effects we can expect (besides the catabolic effect it will have on your wallet). Although it has a reputation for being very mild, you´ll still see some results from Andriol. One study using a very low dose on adolescent boys still showed a reasonable gain in Fat Free Mass(3) even though the boys were not training. And in another study focusing on the elderly, it improved their quality of life considerably (as androgens often do) (6), and also had beneficial effects on erectile dysfunction (7) (again, this is typical of androgens). This is certainly promising, but in a world where first time-ste In fact, it may even be a useful adjunct with Viagra for this purpose (8). However, in a world where first time steroid users expect upwards of 20lbs per cycle, I would suspect many will be disappointed with the 5lbs or so a cycle of Andriol will produce. Granted, that´s a conservative estimate, but I can´t really be confident predicting much more muscle is to be expected from Andriol. Taking a large amount of Andriol is actually pretty safe (except for your bank account), and there was even a 3 month study done in Korea, where a pretty small dose of Andriol ( 160 mg daily for 3 weeks then half that dose for the remainder of the study) resulted in a very nice rise in testosterone. Serum total testosterone increased from 2.13 +/- 1.20 ng/ml at baseline to 6.04 +/- 3.08 ng/ml (p = 0.005) after 12 weeks. In addition, free testosterone was (barely) significantly changed from 8.60 +/- 2.25 pg/ml to 11.40 +/- 3.81 pg/ml (p = 0.13) (10). However, there were no significant changes in liver function tests, red blood cell count or lipid profiles, nor were there any significant adverse reactions that would have led to the cessation of the administration of oral testosterone. So the scientists at Organon have succeeded in making a nice, safe, moderately effective orally available treatment for low androgen levels. But can we (athletes and bodybuilders) use it also?
Truthfully, I can´t be confident predicting more than a 5lbs gain with the use of Andriol, because this product has a very odd property, and that is the widely varying effects it has on test subjects. In one study I read, four test subjects were each given Andriol, and one had a huge surge in testosterone levels going up to 60.1nmol/L and the other only had a 11.5nmol/L level(5)! The remaining 2 test subjects fell in between those levels. I am speculating that the differences experienced by the test subjects were primarily due to the variances inherent in the lymphatic system. But to make matters even more inconsistent, there is no evidence that those variances wouldn´t occur within the same person taking Andriol (i.e. you get a huge surge in testosterone one day, and a very minor one the next day). This may be due to variability associated with whether this stuff is taken with food or not. Since it operates via association with your small intestine and lymphatic pathways, taking it with food greatly enhances it´s bioavailability (9), and this may be a case of "problem solved" but I´m hesitant to close the books on andriol´s absorption problems so quickly, for now, we´ll just say you are spending your money much more wisely if you take your andriol with meals.
Despite all of it´s problems, if I had the money to run 10-15 caps of Andriol/day, and if I were looking for a stand-alone oral compound to safely run for a full cycle (of perhaps 12 weeks), then I have to admit, Andriol would be my #1 choice.
Testosterone undecanoate and may offer an alternative for androgen treatment in women.
Testosterone + Undecanoate ester
[androsta-4-en-3-one,17b-ol]
Molecular weight of base: 288.429
Molecular weight of ester: 186.2936
Formula: C19 H28 O2
Melting Point: 155
Manufacturer: Organon
Effective dose: 600mgs
Active Life: less than 8-12 hours
Detection Time: 4-5 weeks
Anabolic/Androgenic Ratio (Range): 100:100
References:
  1. Which Androgen Replacement Therapy for Women? Journal of Clin Endocrinol and Metab. 83 1998 3920-24
  2. A new oral testosterone undecanoate formulation. World J Urol. 2003 Nov;21(5):311-5. Epub 2003 Oct 25. Review.
  3. Effects of oral testosterone undecanoate on growth, body composition, strength and energy expenditure of adolescent boys. Clin Endocrinol (Oxf). 1992 Sep;37(3):207-13.
  4. Recovery of free androgens in the rat prostate in vivo and in vitro after treatment with orally active testosterone undecanoate (TU). Horm Metab Res. 1980 Oct;12(10):541-5
  5. Which Testosterone Replacement therapy? Clin Endocrinol (oxf) 21 198497-107
  6. Effect of oral testosterone undecanoate on visuospatial cognition, mood and quality of life in elderly men with low-normal gonadal status. Maturitas. 2005 Feb 14;50(2):124-33.
  7. Effect of 12 month oral testosterone on testosterone deficiency symptoms in symptomatic elderly males with low-normal gonadal status. Age Ageing. 2005 Mar;34(2):125-30. Epub 2004 Dec 13.
  8. Oral testosterone undecanoate reverses erectile dysfunction associated with diabetes mellitus in patients failing on sildenafil citrate therapy alone. Aging Male. 2003 Jun;6(2):94-9.
  9. Important effect of food on the bioavailability of oral testosterone undecanoate. Pharmacotherapy. 2003 Mar;23(3):319-25.
  10. Oral testosterone replacement in Korean patients with PADAM. Aging Male. 2002 Mar;5(1):52-6.
  11. Administration of testosterone undecanoate in postmenopausal women: effects on androgens, estradiol, and gonadotrophins. Menopause. 2000 Jul-Aug;7(4):251-6.
  12. Effects of androgen supplementation therapy on partial androgen deficiency in the aging male: a preliminary study. Aging Male. 2002 Mar;5(1):47-51.
  13. Therapeutic effect of andriol on serum lipids and apolipoproteins in elderly male coronary heart disease patients. Chin Med Sci J. 1992 Sep;7(3):137-41.


I'm not drunk it's just epylepsy...

Quando i tuoi occhi si illuminano dell' infantile curiosità, quando i "perchè" soffocano il tuo pensiero, quando le sensazioni toccano il tuo bisogno.....adesso, solo adesso puoi definirti "vivo".....

Ultima Modifica di Antò : 05-12-2007 08:57 PM.
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