Aromasin y tamoxifeno… Bajar un ciclo de esteroides

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Coming off a steroid cycle is a bitch. Nothing new about that. When you're on the juice, you look great, siento muy bien, you're strong as an ox, and you're usually horny as a mother-f#cker! Sino, alas, all good things eventually must come to an end and a steroid cycle is no different.

Sino, bodybuilders have known for a long time that a good post-cycle protocol can make the transition back to being natural a lot easier. And it can help you keep your muscle gains and bring your natural testosterone levels back to where they were before your cycle. Good post cycle therapy can also be used to keep cycle related estrogen levels in check and prevent all the nasty estrogen related side effects.

In this week's EliteFitness.com news we share some of the benefits of an often overlooked post-cycle drug and powerful anti-estrogen - Aromasin. We'll also share with you how to combine it with the old favorite Nolvadex for even better gains-keeping results!

Rationale for the Use of Aromasin with Tamoxifen (Nolvadex) During Post Cycle Therapy

Aromasin (Exemestane) is one of those weird compounds that nobody really knows what to do with. What we generally hear about it makes it very uninteresting… Es una inhibidor de la aromatasa de tercera generación (A) just like Anastrozole and Femera (Letrozol). Both of those two drugs are very efficient at stopping the conversion of androgens into estrogen, y puesto que tenemos, por qué molestarse con Aromasin? It’s a little harder to get than the other two commonly used aromatase inhibitors, porque no está en alta demanda, and there’s never been a readily apparent advantage to using it.

Y me refiero a… permite enfrentarlo: Es torpe-sonando. Aromasin no tiene mucho de un anillo que, y exemestane es aún peor. Anastrozole has a bunch of cool abbreviations ("A-dex" or just ‘dex) and even Letrozole is just "Letro" a la mayoría de las personas. Where’s the cool nickname for Aromasin (exemestane)? A-Sin? E-Stane? Simplemente no funciona. It’s the black sheep of AIs. Y por qué aún necesitamos cuando tenemos Letrozole, which is by far the most efficient AI for stopping aromatization (the process by which your body converts testosterone into estrogen)? Letro can reduce estrogen levels by 98% o mayor; clinically a dose as low as 100mcgs has been shown to provide maximum aromatase inhibition (2)!

So why would we need any other AIs? Bien, En primer lugar, estrogen is necessary for healthy joints (3) así como un sistema inmunológico saludable (4). Así que deshacerse de 98% of the estrogen in your body for an extended period of time may not be the best of ideas. This may be useful on an extreme cutting cycle, conduce a un concurso de culturismo, or if you are particularly prone to gyno, but certainly can’t be used safely for extended periods of time without compromising your joints and immune system.

That leaves us with Anastrozole, which isn’t as potent as Letrozole, pero a 5mgs/day será aún deshacerse de alrededor de la mitad (50%) of the estrogen in your body. Problema resuelto, derecho? Use Anastrozole on your typical cycles, and if you are very prone to gyno or are getting ready for a contest, Utilice Letro.

Pero qué pasa con terapia Post ciclo (PCT)?

Creo que en este momento se vende la mayoría de la gente sobre el uso de Nolvadex (Citrato de tamoxifeno) en vez de Clomid para post ciclo de terapia (PCT), Dado que ambos compiten estrógeno en el sitio del receptor, both increase serum test levels, and both drugs may also alter blood lipid profiles favorably (6). But since 20mgs of Tamoxifen is equal to 150mgs of clomid for purposes of testosterone elevation, FSH y LH, but Tamoxifen doesn’t decrease the LH response to LHRH (6) I think most people agree to Nolvadex’s superiority for PCT.

Aromasin con Nolvadex

Siempre he estado a favor del uso de Nolvadex durante el PCT, junto con un AI, because reducing estrogen levels has been positively correlated with an increase in testosterone (7) so in my mind, it’s be beneficial to increase testosterone by as many mechanisms as possible while trying to recover your endogenous testosterone levels after a cycle. ASÍ que AI utilizamos? Letro o A-dex? Bien, why don’t we just keep using whichever one we used during the cycle, y añadir en algunos Nolvadex? Desafortunadamente, Nolvadex will significantly reduce the blood plasma levels of both Letrozole as well as Anastrozole (8). Así que si decide utilizar uno de ellos con el Nolvadex sobre PCT, nos estamos tirando un poco de dinero como el Nolvadex se reduce su efectividad.

Esto, Claro, es donde Aromasin, en 20-25mgs/day.

Aromasin, en que la dosis, aumentará sus niveles de testosterona por sobre 60%, and also help out your free to bound testosterone ratio by lowering levels of Sex Hormone Binding Globulin (SHBG), por sobre 20% (12)… SHBG is that nasty enzyme that binds to testosterone and renders it useless for building muscle. Pero por qué usar junto con Nolvadex para el PCT?

Diferencia entre el tipo-I y tipo II los inhibidores de aromatasa

Para entender por qué Aromasin puede ser útil en combinación con el Nolvadex mientras Letro y A-dex sufren reducida efectividad, we’ll need to first understand the differences between a Type-I and Type-II Aromatase Inhibitor. Inhibidores de tipo I (como Aromasin) son en realidad esteroides compuestos, mientras que los inhibidores de tipo II (like Letro and A-dex) son medicamentos no esteroides. Por lo tanto, androgenic side effects are very possible with Type-I AIs, and they should probably be avoided by women. Claro, there are some similarities between the two types of AIs…tanto de tipo I & tipo II AIs mímico sustratos normales (essentially androgens), allowing them to compete with the substrate for access to the binding site on the aromatase enzyme. Después de este enlace, the next step is where things differ greatly for the two different types of AI’s. In the case of a type-I AI, el inhibidor no competitivo se unirá, and the enzyme initiates a sequence of hydroxylation; this hydroxylation produces an unbreakable covalent bond between the inhibitor and the enzyme protein. Ahora, permanentemente se bloquea la actividad de la enzima; even if all unattached inhibitor is removed. Aromatase enzyme activity can only be restored by new enzyme synthesis. Ahora, Por otra parte, competitive inhibitors, tipo llamado II AI, reversibly bind to the active enzyme site, y una de dos cosas puede suceder:

1.) o ninguna actividad de la enzima se activa o .

2.) la enzima se activa de alguna manera sin efecto. The type II inhibitor can now actually disassociate from the binding site, eventually allowing renewed competition between the inhibitor and the substrate for binding to the site. This means that the effectiveness of competitive aromatase inhibitors depends on the relative concentrations and affinities of both the inhibitor and the substrate, while this is not so for noncompetitive inhibitors. Aromasin es un tipo-yo inhibidor, lo que significa que una vez que ha hecho su trabajo, and deactivated the aromatase enzyme, no lo necesitamos ya. Letrozole and Anastrozole actually need to remain present to continue their effects. Esto es posiblemente por Nolvadex no altera la farmacocinética de Aromasin (11).

Conclusión

Antes de que cerremos el libro de Aromasin, Cabe destacar que se puede (y debe) still use one of the non-steroidal AIs during your cycle to reduce estrogen, Si es necesario. Cuando esté listo para el PCT, Usted puede entonces pasar a Aromasin y todavía experimentar los efectos completos de un AI, since there is no cross-over tolerance experienced between steroidal and non-steroidal AIs (9). Puesto que trata de Aromasin 65% eficaz en la supresión de estrógenos (10), it’s certainly a very powerful agent, especially considering you won’t experience reduced effectiveness because of your concurrent use of Nolvadex or from any sort of tolerance developed by using other AIs on your cycle(9). There is also a decent amount of preclinical data suggesting that Aromasin has a beneficial effect on bone mineral metabolism that is not seen with non-steroidal agents, and it may also have beneficial effects on lipid metabolism that are not found in the non-steroidal Letro and A-dex (9).

Finalmente, como vamos a usar Nolvadex para el PCT de todos modos, y debemos utilizar un AI con ella para la máxima recuperación… I think Aromasin- teniendo en cuenta es compatibilidad con Nolvadex y efectos beneficiosos sobre el hueso mineral contenido lipídico perfil, has finally stopped being the black sheep of AIs and found a home in our cycles.

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