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Chapter 9

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CHAPTER 9 - Evolutionary Anabolic Factor Ebook - Oral PCT Items, Injectable PCT, Legal PCT Items

PCT Drug Profiles

So this is basically the scenario at the end of a steroid cycle. Testosterone levels are bottom low while estrogen is still abundant in the bloodstream. The HPTA is almost inert, the body's homeostasis is threatened, and then those hard earned gains made during the cycle have a strong probability of just going down the drain if the right precautions are not taken.

Ancillary drugs are necessary when on an Anabolic-Androgenic Steroid (AAS) cycle, where there is the attendant buildup of estrogen in the body, especially in cases of highly aromatizing AAS. Post cycle, estrogen control is also a problem when re-normalizing HPTA function. Also, as mentioned in Chapter 8, there is the problem of low or no production of testosterone after discontinuance. Below are some of the products that can help you plan your PCT.

Oral PCT Drugs

  • Arimidex (anastrozole)

    Arimidex is an oral aromatase inhibitor manufactured by Zeneca Pharmaceuticals and which was approved for use in 1995 in the United States. It is a prescription drug in most countries, which means it is a licensed medicine and one needs a written prescription from a medical practitioner in order to obtain one. It was developed to treat advanced breast cancer in women. As an aromatase inhibitor, it blocks the aromatase enzyme, thereby preventing the conversion of testosterone or other androgen hormones to estrogen and other female hormones.

    This drug is ideal in bodybuilding because it produces effective radblock against estrogenic side effects of steroids use, such as gynecomastia and water retention.

    Key Points for Arimidex Users

    • Aromatase inhibitors like Arimidex have the tendency to completely suppress estrogen activity, including the beneficial sides of this hormone. If used with steroids like testosterone, Arimidex is known to decrease HDL (good) cholesterol. Estrogen positively affects cholesterol levels in the body. In clinical studies, it has been observed that a daily dose of 1 mg results to more than 80% of estrogen suppression.

    • Side effects with this ancillary drug include hot flashes and hair thinning, especially in sensitive individuals.

    • Daily dosage for males is from 0.5 to 3 mg. For women, a maximum dosage of 1 mg per day is enough to combat estrogenic side effects. Because Arimidex has a short active life, dosages are usually taken two to six times a day at equal intervals. During PCT, athletes normally start with higher dosage then implement a progressive decrease in dosage. The PCT protocol typically runs for seven to 14 days.

    • The principal downside of this drug is its high cost.

  • Nolvadex (tamoxifen citrate)

    This is an oral anti-estrogen/estrogen antagonist prescription drug. Nolvadex is commonly referred to as an anti-estrogen, but technically it is more of an estrogen antagonist. An estrogen antagonist has a unique way of preventing estrogen activity. What it does is to compete with estrogen at the estrogen receptor sites, occupying them so that estrogen cannot bind with these receptors. Take note that Nolvadex does not directly prevent estrogen production, for it only blocks estrogen receptors from binding with estrogen. During Nolvadex use, there would still be elevated levels of estrogen in the system, it just can't get to the receptors since Nolvadex does a good job of docking there first and keeping Estrogen out. Nolvadex itself does not send a signal when it is on the receptor, it just sits there and keeps Estrogen out.

    Key Points for Nolvadex Users

    • High dosage can prevent natural testosterone production by the testes. Further, high dosage can be counter-productive; instead of lowering estrogenic levels, it increases the levels. This is a consequence of the adrenal glands being overly stimulated to produce the prohormone dehydroepiandrosterone or DHEA. DHEA can convert to estrogen.

    • It does not directly prevent estrogen production; it is only capable of blocking estrogen from binding with the receptors.

    • Dosage ranges from 10 to 60 mg daily.

    • It is recommended to be stacked with highly aromatizable steroids like Dianabol and testosterone

    • It is NOT recommended to be used in conjunction with highly anabolic/moderate to low androgenic (with the absence of highly aromatizable compounds), and when the desired aim is to gain mass.

    • For women: Nolvadex disables birth control drugs.

  • Aromasin (exemestane)

    Aromasin is also considered to be a suicide aromatase inhibitor whose structure and mode of action is similar to those of Lentaron (formestane). Aromasin inhibits the aromatase enzyme that converts pre-estrogen to active estrogen. This enzyme is present in fat tissues, including the breast tissues.

    Among bodybuilders, Aromasin is one of the top choices from this group of drugs. This is because it reportedly works more efficiently than most anti-estrogen compounds.

    Aromasin is a prescription drug and it is available in 25 mg pills. It is used for the treatment of adjutant treatment of postmenopause with estrogen-receptor positive early breast cancer. This drug is also indicated for patients with advanced (metastatic) breast cancer, if Nolvadex (tamoxifen) is unable to prevent the spread of cancer.

  • Key Points for Aromasin Users

    • In postmenopausal women, this drug can lower estrogen level by up to 98%. This is very significant since less estrogen means less risk of estrogen-related tumor growth. Bodybuilders seem to agree with this statistics because of their preference for Aromasin over any other anti-estrogen.

    • It can be a more cost effective drug choice since it can be effective at a relatively lower dosage. Users report that it can significantly suppress estrogen with just 2.5 mg per day, which is considerably lower than the recommended daily dosage of 25 mg.

    • Aromasin is also called an aromatase inactivator, meaning it renders estrogen receptors useless. This drug not only inhibits estrogen production, but completely stops production.

    • Aromasin can also cause androgenic sides, thus its users experience mood changes. It can also cause cardiovascular disorders and osteoporosis, particularly in long term use.

  • Femara (letrozole)

    Femara, manufactured by Novartis, is an oral non-steroidal aromatase inhibitor that has been approved by the FDA for the adjutant treatment of hormonally-responsive breast cancer. Estrogens are produced by the conversion of androgens through the activity of the aromatase enzyme.

    Femara prevents such conversion via competitive, reversible binding to the heme of its cytochrome P450 unit. Thus, its action is considered to be target-specific, as it does not reduce production of mineralo-or corticosteroids. In contrast, the anti-estrogenic action of Nolvadex (tamoxifen), the top medical therapy prior to the arrival of third generation aromatase inhibitors like Femara, is due to its interfering with the estrogen receptor, rather than inhibiting estrogen production.

    Key Points for Femara Users

    • This drug is known to reduce estrogen levels by 98 percent while raising testosterone levels, a characteristic bodybuilders find desirable in an anti-estrogen compound.

    • Its side effects can include signs and symptoms of hypoestrogenism (lower than normal level of estrogen). Osteoporosis may be a concern, especially in long term use. This is why a prescription of Femara is usually accompanied by such drugs as Fosamax, an osteoporosis-fighting medication.

    • According to its product insert, the recommended dosage of Femara is 2.5 mg, sufficient to lower estrogen levels as (observed in clinical trials). However, like Aromasin, Femara's dosage can be lowered and users can still expect ideal estrogen inhibition. In clinical studies, doses of 0.1 mg and 0.5 mg produced 75% and 78% estrogen inhibition, respectively.

  • Proviron (mesterone)

    Proviron is an oral androgenic steroid / anti-aromatizaion prescription drug. It exerts its anti-estrogen activity by preventing production of estrogen and elevating androgen levels. This makes it a better option than Nolvadex in prevention of estrogen buildup.

    Proviron is one of the most popular drug choices in bodybuilding as it is reportedly effective during and after AAS cycle. During cycle, it is noted for its high affinity with SHBG; therefore, heightening the effectiveness of other stacked steroids.

    Key points for Proviron Users:

    • Restores sperm production and sexual functions.

    • It can cause erectile dysfunction (prolonged and frequent erections) among male users.

    • Disruption of menstrual cycles can be experienced by female users.

    • Daily dosage is 25-200 mg daily for males; 25-50 mg for females. It is usually used with Nolvadex.

  • Clomid (clomiphene citrate)

    Clomid is classified as an oral synthetic estrogen/HPTA stimulator. It is a prescribed drug whose clinical application is to aid in women's ovulation. In bodybuilding, is in great demand in PCT because it stimulates the release of gonadotropin from the hypophysis (pituitary gland), which causes a domino-effect reaction in the body – this stimulates the production of FSH and LH, which turn sends a memo (to use an office setting jargon) the Leydig cells in the testes to produce sperm and testosterone.

    Key Points for Clomid Users:

    • The recommended dosage is to start 50 mg twice daily for five consecutive days, then to decrease to 50 mg once a day for another five to 10 days.

    • It is usually used partnered with Nolvadex and HCG.

    • Clomid is generally considered to be inferior when compared with Nolvadex. This requires a deeper comparative study, however, since both of these drugs exhibit similarly desirable actions in the body.

    • To jump-start testosterone production in the body, many opt to use Clomid with HCG as a post-cycle regimen. The typical practice is to administer this PCT after the first or second week of steroid use.

    • Clomid is considered to be a safe buy since there are no reported counterfeit versions of this drug.

Injectable PCT Drugs

  • Human Chorionic Gonadotropin (HCG)

    The clinical application of human chorionic gonadotropin (HCG) is to promote ovulation in females, as it mimics the body's LH. Athletes who use steroids opt for this injectable ancillary drug because it significantly increases endogenous testosterone levels.

    There has been a study showing that the LH suppression is not the only culprit in preventing HPTA function normalization. The occurrence of testicular atrophy and desensitization to LH is the major obstacle in re-establishing normal HPTA function. The testes undergo such alteration because of inactivation during steroid use (remember the take-a-vacation thing in Chapter 9?). When the time comes for them to do some real work, the testes are incapable of providing the necessary output.

    This is when HCG's work is required. HCG administration stimulates production of androgen and sperm by the testes. This solves some of the negative reactions brought about by steroid use, which are mostly reproductive dysfunctions such as loss of libido, testicular atrophy and low sperm count.

  • Key Points for HCG Users

    • Dosage protocol is from 2000 to 5000 I.u. Every fifth day for two to three weeks. This dosage is applied mid-and-post-cycles. It is usually stacked with Clomid and Nolvadex.

    • Injection of HCG can increase plasma testosterone levels up to 200-300%.

    • HCG recommended maximum dosage period is three weeks. This is because a prolonged use can again increase testosterone and estrogen levels, which can result to backlash.

  • Faslodex (fulvestrant)

    Faslodex is one of the newest drugs aimed to counter estrogen negative effects. It was approved by the FDA in 2002 for the treatment of breast cancer. Faslodex is classified as estrogen receptor antagonist/estrogen receptor downregulator. Its mode of action is comparable to that of Clomid and Nolvadex. Like these two drugs, Faslodex also blocks estrogen receptors but does not prevent the production of estrogen.

    Key Points for Faslodex Users

    • Unlike Clomid and Nolvadex, this drug is considered to be a pure estrogen receptor antagonist. Clomid and Nolvadex have both agonist and antagonist properties. This means that they allow estrogenic activity in selective tissues, which can be ideal for HDL biosynthesis. With Faslodex, this beneficial activity is missing; a drawback it shares with aromatase inhibitors.

    • Faslodex is a good alternative in use of ancillary drugs, which are mostly in oral forms. With this drug, users can do away with frequent administration (sometimes several times a day) typical of oral drugs. A once a month injection is enough to achieve desirable levels.

    • Dosage regimen is convenient with this drug as it come in pre-loaded syringes. One version has a single pre-loaded 5 ml syringe while another has two 2.5 ml pre-loaded syringes in a box. Each 5 ml dose contains 50 mg of anti-estrogen.

    • Cost may be a negative point for this drug. A single 5 ml injection can cost to almost a thousand dollars.

  • Lentaron (formestane)

    Lentaron Depot is the injectable version of formestane sold by the Novartis Pharmaceuticals. Formestane is used in breast cancer patients and is very much considered as a 'potent steroidal suicide aromatase inhibitor'. It is derived from the prohormone androstenedione with just the addition of a 4-hydroxyl group. This said group is what makes formestane to bind with the aromatase enzyme.

    The aromatase has both an iron-containing and a steroid-binding site. The substrate, androstenedione, sits in the enzyme's steroid-binding site. This site catalyzes the formation of estrogen. Lentaron works by occupying the steroid – binding. Its oral version is Formastat.

    Key Points for Lentaron Users

    • Lentaron is regarded as the next best option when tomoxifen fails to treat patients with breast cancer.

    • It is an aromatase inhibitor, and therefore can cause negative reactions with the body's cholesterol levels, specifically an increase in bad (LDL) and decrease in good (HDL) levels.

    • Aside from preventing estrogenic side effects, Lentaron is known for providing drier and more defined muscle gains.

    • Dosage is 250-500 mg every two weeks.

    • Lentaron is a nutritional supplement and it can be acquired over the counter. Lentaron Depot is, therefore, a legal PCT item.

    • Lentaron not only stimulates testosterone production, it also increases insulin-like growth factor-1 (IGF1) by more than 25%. Plus, it reportedly decreases SHBG by 34%, and this translates to more free androgens to exert anabolic action.

Legal PCT Products

In the United States, most of PCT items fall under the prescription drug category,. Thus, those who need them for recreational purposes only have to find (illegal) ways to obtain them. The internet is a reliable source for this class of drugs. Others, however, choose to use over-the-counter supplements to prevent post-cycle crash.

  • Tribulus

    Tribulus is a genus of plants found in many warm regions. It is a source of dietary supplement to increase the body's natural testosterone levels. It is also claimed to enhance sexual behavior in animal test subjects as well as stimulate androgen receptors in the brain.

  • 4-Androstene-3,6,17-trione

    4-Androstene-3,6,17-trione, or simply 6-OXO, is a popular PCT item. It is also considered as a 'suicide aromatase inhibitor' and is marketed as a nutritional supplement that reportedly increases the testosterone-estrogen ratio. A recent United States patent application claims that 6-OCO can cause 88% increase in plasma testosterone levels in men, while decreasing estrogen levels by 11%. The subjects took 300 mg orally twice a day for four weeks without taking any other drugs or supplements. Its use can be detected in urine.

  • Phosphatidylserine

    Phosphatidyleserine, or PS, is a naturally occurring, phospholipid nutrient. PS is essential to the functioning of all the cells of the body, but is principally found in the brain. PS is said to improve neural functions and enhances energy metabolism in cells. One of its clinical applications is its treatment of dementia.

    Its major benefit to recreational users is reportedly its ability to reduce adrenocorticotropin (ACTH) and cortisol output by 30-40%. Such reduction improves the ratio of protein synthesis as against protein breakdown.

  • Fadogia Agrestis

    This herb is regarded as a herbal HCG. It has been proven to increase testosterone production in males by up to 200% in a 5 day period. Many steroid users who have tried Fadogia, report an almost immediate reversal of testicular atrophy. By the third day of use, many men report a noticeable increase in size of their testes (during PCT) and an increased semen volumen.

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Lev Butlerov holds a Masters Degree in Biology, he is NASM Certified, ISSA Certified, The National Council on Strength & Fitness (NCSF) certified and is currently working on his American Council on Exercise (ACE) certificate. From Lev: I love bodybuilding and the biology, chemistry of the industry. It's my hobby and my love. I have done multiple bodybuilding shows, 2 in Germany in the past 5 years. I hope everyone enjoys my articles. In 2021 (going into 2022, 2023) I will be working on my PhD thesis in physiotherapy and biochemistry, I hope to have some of the bits published here.

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