Substance: Anastrozole Manufactured by: Axiolabs Packaging: 1 x 25 tabs (1mg/ tab) Average Dose: .25mg - 1mg per day Half Life: 5 - 7 days Water Retention: none Aromatization: no DHT Conversion: no
GENERAL INFORMATION:
Arimiplex (Anastrozole) is a novel, potent aromatase inhibitor belonging to the triazole class. In vitro and in vivo animal studies have revealed the drug to be a potent inhibitor of the aromatase enzyme with no inhibitory activity versus other enzymes involved in steroid synthesis. The drug is a potent suppressor of plasma estrogens in healthy male and postmenopausal female volunteers as well as postmenopausal breast cancer patients, and Arimiplex administered as 1 mg or 10 mg daily has been shown to inhibit in vivo aromatization by 96.7 and 98.1%, respectively. Two large, randomized studies revealed Arimiplex to cause objective response rates and stable disease comparable to what was achieved with megestrol acetate but with a lower incidence of side effects. While follow-up results have not revealed any significant difference in time to relapse between the drug regimens, they have revealed an improved survival among patients treated with Arimiplex 1 mg compared to megestrol acetate 160 mg daily. Further follow-up is required to finally decide whether there may be a survival benefit also among patients treated with Arimiplex 10 mg daily and to evaluate whether the improvement in survival is associated with an improved disease-free survival as would be anticipated.
The compound Arimiplex is indeed a revolution in the treatment of breast cancers. It's a new generation of aromatase blocker. Up until recently the main product for this purpose was the androgenic steroid Proviraplex (Mesterolone). But the problem here was that Proviraplex was not particularly strong and in the required doses of 50 to 100 mg per day, androgenic side-effects were not uncommon. Proviraplex is after all a DHT derivative. It could also never be used longer than the cycle lasted, because to some extent (despite readily being deactivated) it was suppressive of natural testosterone production. Arimiplex seems to do the job more efficiently. In clinical trials a single tab daily proved to have a profound effect. In steroid circles, mostly due to the high cost, experimentation with half and quarter tabs proved it to be almost unbelievably strong. So much, that really half a tab per day suffices for most users.
Things one needs to note while using Arimiplex is that the benefits of estrogen become non-existent as well. First of all that means gains can be drastically reduced. They will be leaner and more qualitative, but they will nonetheless be seriously reduced. A second problem is that estrogen seems to have a positive effect on cholesterol levels. Since estrogen is reduced, the use of Arimiplex may have a profound impact on HDL to LDL ratio's in your cholesterol profile. In this aspect the use of Tamoxiplex (Tamoxifen Citrate) is more user-friendly, because despite its anti-estrogenic effects in most tissues, it seems to exert positive estrogenic effects in the liver and promote a better cholesterol profile.
A significant proportion of breast cancers are estrogen-dependent and are therefore amenable to endocrine therapy. Although tamoxifen has been the mainstream of endocrine treatment for over 20 years, new agents have entered the clinic that have potentially superior activity and an improved safety profile. The development of orally-active, potent and selective third-line aromatase inhibitors represents a major advantage in the management of hormone-sensitive breast cancer. Arimiplex was the first of these agents to become available and is currently widely indicated for both first- and second-line treatment for postmenopausal women with breast cancer. This review focuses on the biochemical properties and clinical efficacy of Arimiplex, providing an overview of the current clinical status and possible future applications.
HOW DOES IT WORK:
Arimiplex operates by blocking the aromatase enzyme, the primary enzyme for the conversion of testosterone to estrogen. A steroid that is altered by this enzyme is referred to as an aromatizing steroid, and such steroids can bring to estrogen build-up. This has several potential side-effects such as water retention, fat gain and lets not forget gynocomastia (the growth of breast tissue in men).
To prevent such effects anti-aromatase products such as Arimiplex can be used. Often times during a cycle most will want to allow for some estrogen, since it heavily promotes strength and gains as well (increases GH, upgrades the androgen receptor, improves glucose utilization). These people will generally opt for an estrogen receptor antagonist such as Tamoxiplex (Tamoxifen Citrate) or Clomiplex (Clomiphene Citrate). These products do not stop the formation of estrogen, but stop the estrogen from exerting its effects by competitively taking up the receptors for this hormone. This allows them to stop any problems dead in their tracks, acting very fast, but upon discontinuation allowing for immediate influx of estrogen again as well. This has the benefit that they can be used as soon as problems arise, and discontinued when they subside, thereby only reducing estrogen-mediated gains for the time-span of the occurring problem (mostly gyno).
Aromatase blockers like Arimiplex and Proviraplex (Mesterolone) on the other hand are more useful for those seeking to eliminate estrogen from a cycle of aromatizable steroids all together. People who are willing to settle for slower gains, in an attempt to stay lean throughout, or for those who are truly sensitive to estrogen and do not want to take the risk of problems occurring. And Arimiplex is the clear weapon of choice here, at least to those who can afford it.
SIDE EFFECTS:
Treatment with Arimiplex (pronounced a-RIM-ih-dex) may cause side effects. In the early breast cancer clinical trial, the most common side effects seen with Arimiplex include hot flashes, joint symptoms, weakness, mood changes, pain, sore throat, nausea and vomiting, depression, high blood pressure, osteoporosis, swelling of arms/legs, and headache. Fractures (including fractures of the spine, hip, and wrist) occurred more frequently with Arimiplex than with tamoxifen (10% vs 7%).
But can you use it for the entire duration of a cycle? Is it dangerous? Well, certainly reducing estrogen levels in your body is good from a body building point of view, as it reduces water-retention and the potential for gynocomastia (if there´s no estrogen in your body, you can´t get gyno, regardless of how much progesterone is floating around)(5). Luckily this stuff is very mild on blood lipids (cholesterol) and doesn´t affect them adversely (2), in the studies ever seen.
STACKING AND USAGE:
Things one needs to note while using Arimiplex is that the benefits of estrogen become non-existent as well. First of all that means gains can be drastically reduced. They will be leaner and more qualitative, but they will nonetheless be seriously reduced. A second problem is that estrogen seems to have a positive effect on cholesterol levels. Since estrogen is reduced, the use of Arimiplex may have a profound impact on HDL to LDL ratio's in your cholesterol profile. In this aspect the use of Tamoxiplex (Tamoxifen Citrate) is more user-friendly, because despite its anti-estrogenic effects in most tissues, it seems to exert positive estrogenic effects in the liver and promote a better cholesterol profile.
As mentioned, Arimiplex is an ancillary that is supposed to be stacked with aromatizing steroids in order to stop all formation of estrogen. Its seemingly very potent, so doses of 0.5 to 1 mg are enough. Some claim that 0.25 mg is enough, but for anyone doing any sort of serious cycle, I would not advise less than 0.5. These steroids are, without exception testosterone, nandrolone, norethandrolone, boldenone and methandrostenolone. And all of their derivatives as well.
The drug Oxyplex (Oxymetholone) has estrogenic effects as well, but they seem to be the result of oxymetholone's acidic A-ring activating the estrogen receptor by itself, rather than by conversion to estrogen. So Tamoxiplex (Nolvadex) would be more advisable in that case.
Although it does block gains, aromatase blockers are generally used for the extent or a certain duration on a cycle, whereas receptor antagonists are used mostly to solve problems. Because it takes some time for an aromatase blocker to take effect (even when aromatase is blocked, there is still a level of circulating estrogen) and again some time to bring estrogen back upon discontinuation (new estrogen needs to be made again), acute problems are best solved with Tamoxiplex (Tamoxifen Citrate) or Clomiplex (Clomiphene Citrate). When an aromatase blocker is used, Arimiplex is the best choice by far. Proviraplex (Mesterolone) may be more apt when using with testosterone, due to its other characteristics and positive benefits on testosterone, but for all other intents and purpose Arimiplex should be preferred in these instances. Literature provided by the original maker of Arimiplex states that stable blood plasma concentrations of the compound are achieved after a mere 7 consecutive 1mg daily doses. Also, Arimiplex is just over 80% effective at inhibiting aromatase (3). Thus, if you want to take it for the entire duration of a cycle of anabolic steroids, you can simply start taking it on the same day you begin your cycle.