Anastrozole is an aromatase inhibitor (AI).
In simple terms, it delays the body's natural production of an enzyme called aromatase, which is responsible for converting testosterone into estradiol. The drug is used in a course with aromatizing anabolic steroids to reduce the negative effects of estrogen on the body. Initially, it is worth considering the positive and negative effects of estrogens on the male body. Estrogens play an important role in various functions of the male and female body. It is on these very functions that the overall health of the athlete and his results depend.
Positive effects of Estrogens:
- play a major role in the immune system;
- necessary for the nutrition of bone tissue;
- have a positive effect on cholesterol levels;
- necessary for the production of growth hormone (GH) and insulin-like growth factor (IGF);
- play an important role in maintaining the “fluid balance” in the body at the proper level;
- help absorb glucose;
- support sexual desire.
Negative aspects of increased estrogen levels:
- retain fluid in the body, swelling;
- fatigue and increased clogging of muscle tissue during training;
- acne (acne), which has not been observed before;
- the risk of prostate cancer increases;
- blood clotting increases;
- the risk of cardiovascular diseases increases;
- the risk of hypertension (high blood pressure) increases;
- the risk of stroke increases;
- cause gynecomastia (swelling and itching in the nipple area, enlarged mammary glands);
- in some cases, sexual desire decreases;
- female type obesity;
- extra sweating;
- possible sleep disturbances;
- may provoke hair loss;
- possible disturbances in the gastrointestinal tract.
With the help of aromatase inhibitors, the level of estrogen is controlled, the growth of which must be restrained in case of excess production. Proper use of anastrozole allows not only to counteract aromatization, but also to simultaneously enhance the growth of free testosterone. If you follow the dosage regimen, the product will be well tolerated by the body, without any negative consequences.
Let's take Anastrozole as an example. The drug was invented at the end of the last century, its original purpose was to treat breast cancer in an operable form. The effectiveness of the drug in this area has been proven, this has contributed to its popularity in sports when athletes use anabolic steroids.
What is this drug and what is it for?
Anastrozole is an inhibitor of aromatase, an enzyme that causes the conversion of testosterone to estradiol.
When using anabolic drugs, Anastrazolos minimizes the side effects of estrogen.
Anastrozole controls the level of this female sex hormone; Anastrozolum also promotes the free growth of testosterone, and with the right dosages, the drug is well tolerated by the body.
The pharmaceutical company Zeneca Pharmaceuticals developed this drug, and in 1995 it was used in the United States. It was developed for women to treat operable breast cancer. Previously, long-term treatment for breast cancer was carried out with Tamoxifen. Studies in more than 9,000 women after menopause showed the high effectiveness of Anastrozole, regression of pathology was observed, and patient survival increased. In 2002, the product gained popularity among athletes due to its anti-estrogenic effect.
Effect of anastrozole
Anastrozole in bodybuilding is used when an athlete begins to use anabolic steroids, which tend to aromatize, such as testosterone and dianabol. In addition to helping muscle growth, they may also have side effects. Often men have to deal with such a problem as gynecomastia. In simple terms, this is the growth of the mammary gland. This happens because the adrenal glands begin to produce aromatase, which converts testosterone into estrogen.
This is why many athletes take anastrozole during a course of anabolic steroids. It inhibits the action of the enzyme, preventing it from destroying testosterone and producing estrogen.
The main effect of anastrozole is:
- prevention of fluid stagnation;
- suppression of the production of excess female hormones;
- stimulation of the production of your own testosterone;
- prevention of testicular atrophy;
- increasing libido in men;
- prevention of gynecomastia;
- improving muscle tone;
- increasing the level of anabolic hormones in the blood;
- prevention of hypertension.
To avoid serious side effects during a cycle of testosterone and dianabol, anastrozole should be started immediately. It is easier to prevent the development of serious diseases than to treat them.
Pharmacokinetics and pharmacodynamics
The non-steroidal active ingredient selectively blocks aromatase. In postmenopausal women, folliculin, androstenedione and aromatase promote the synthesis of estradiol.
When estradiol levels decrease, breast cancer is treated. Estradiol levels are reduced by 80%. The drug has no progestogenic, estro-, and androgenic activity.
When the tablets are taken orally, the active substance is quickly absorbed from the gastrointestinal tract. Its binding to plasma proteins will be 40%, accumulation in the body does not occur. The maximum concentration in the blood will be reached after 2 hours if the drug is taken on an empty stomach. If a person has eaten, the degree of absorption will not change, the rate of absorption will decrease.
Dealkylation, hydroxylation, and glucuronidation ensure the absorption of the drug by the liver. Urine and blood contain the main metabolic product - triazole. The elimination of drug metabolites takes 3 days.
Pharmacological properties of growth hormone
How does growth hormone work on PCT? It is so called because in adolescents, children, and young adults with unclosed growth areas in the bones, it can cause a pronounced acceleration of linear development, mainly due to an increase in the long tubular bones of the extremities. This element has a powerful anti-catabolic and anabolic effect, enhancing protein synthesis and inhibiting its breakdown, as well as helping to reduce subcutaneous fat deposits, and in addition, enhance its combustion and increase muscle mass ratio.
In addition, growth hormone takes part in the processes of regulation of carbohydrate metabolism: it causes a pronounced increase in blood glucose and it acts as one of the counter-insular antagonists of insulin in its effect on carbohydrate metabolism.
In medicine, its effect on pancreatic cells, immunostimulating effectiveness and increased calcium absorption by bone tissues are also described. A significant part of the properties is mediated by insulin-like growth factor, which is produced under the influence of liver elements. This hormone stimulates the growth of most internal organs.
Benefits and harms
This medicine, like any drug, has its pros and cons.
Characteristics of the benefits of Anastrozole with proper dosage:
- Unnecessary volume of fluid and fat is removed from the body, so the muscles become prominent.
- Positively affects blood fats.
- A man's libido increases.
- Prevents arterial hypertension.
- Reduced estrogen inhibition of the pituitary-hypothalamus-testicular axis.
- The product is popular for PCT during the recovery period.
- The medicine helps well with hormone replacement therapy.
Aromatase blockers (Formestan, Proviron) suppress estradiol levels, but the body needs estradiol for normal functioning. Therefore, it is important for an athlete not to allow critically low levels of this hormone in the blood during a course of anabolic steroids.
If there is little estrogen in the blood, then:
- Memory will deteriorate.
- Your mood will change frequently.
- Your joints will begin to ache.
- Depression will begin.
- Libido will disappear.
- Cholesterol levels will increase.
- The bones will become less strong and other side effects will occur.
If you abuse Anastrozole, anabolism will stop completely.
Vitamins and minerals
First of all, these are B vitamins: B1, B6, B9, B12. They are responsible for metabolic processes in the body, and also regulate appetite, normalize the functioning of the central nervous system and strengthen the immune system.
For example, vitamin B6 enhances the bioavailability and transport of proteins, which is important when consuming amino acids and proteins. The recommended dosage per day is 50 mg
Asparkam is a source of potassium and magnesium, without which seizures can occur and problems in the cardiovascular system can develop. Recommended for use during the drying cycle and during the preparation period for functional sports. The use of this drug will help increase endurance and improve well-being during periods of substance deficiency. The permissible dosage is from 350 to 500 mg per day.
Potassium preparations for additional use during a course of anabolic steroids ensure stable conduction of the nerve impulse necessary for myocardial contraction. In addition to all this, potassium promotes the rapid synthesis of proteins in the body, as well as accelerates tissue regeneration and increases appetite. But additional potassium loading will affect increased sweating. It is recommended not to exceed 500 mg per day and taken if there is a deficiency in your diet.
Calcium and vitamin D supplements help strengthen bone structure and may also help slightly lower iron levels if iron levels are elevated and are affecting blood thickness. In addition, calcium strengthens the walls of blood vessels and helps normalize heart contractions. I recommend taking it for osteoporosis, injuries and elevated iron levels, as well as for deficiency of substances. The optimal dosage of calcium is 500 mg, and vitamin D is 200 IU.
Ascorbic acid is responsible for oxidative processes, strengthens the immune system and improves joint elasticity. On the bridges between courses and on pct it helps reduce catabolism. Vitamin C is a transport system for iron, which is very useful if your iron levels are low during a course of steroids. You can safely take from 500-1000 mg per day. For colds, the dosage can be increased 3 times.
Iron supplementation may be needed if you have low hemoglobin and low iron levels. Yes, not everyone on a course of steroids increases the concentration of iron in the blood, but it also happens that, on the contrary, the body has an increased need for this mineral. In such cases, iron is used as a supplement. Select a dosage from 20-100 mg/day for iron deficiency in the blood.
Omega-3, 6, 9 improves metabolism and also strengthens the cardiovascular system. If you don't have enough unsaturated fats in your diet (fish, flaxseed oil, olive oil, sesame oil, mustard oil), then you need to compensate with omega 3-6-9 supplements. But the priority should still be fish, at least half a kilo every other day, and daily consumption of vegetable oils. The daily dosage outside the course of steroids is 3 grams, and during the cycle of steroids I recommend taking up to six grams of omega 3.
Complex vitamins and minerals. The use of a vitamin-mineral complex is necessary when you cannot compensate for the lack of substances through the food you eat. Regardless of whether you use steroids or not, the body always needs vitamins and minerals. If for some reason you cannot give your body most of the vitamins and minerals through food, you need to take supplements.
Attention! Always remember that an excess of vitamins harms your body! The liver is the first to suffer, and then the whole body. Therefore, be careful about what you are going to take and why!
Indications and contraindications
In addition to bodybuilding, the product is used by women for:
- Therapy of common breast cancer in the last phase of menopause.
- Treatment of invasive estrogen-positive breast cancer in the initial stages with positive parameters of hormonal receptors.
- Complex therapy of estrogen-positive malignant neoplasms of the mammary glands in the initial stages after additional use of Tamoxifen for 2 or 3 years.
The drug is contraindicated in:
- The initial stage of menopause.
- Cardiac ischemia.
- Severe kidney and liver dysfunction.
- Intolerance to the components of the drug.
The drug is not recommended for women involved in bodybuilding. Do not take Vera-Anastrozole during pregnancy or breastfeeding. Changes in hormonal levels in a pregnant woman will negatively affect the fetus, otherwise children will experience hormonal imbalance in the future.
Consequences
The consequences of gynecomastia after the course look like this:
- severe fluid retention in the body, resulting in swelling of the entire body or individual parts;
- breast enlargement and its resemblance to a woman’s;
- either glandular tissue or fatty tissue grows inside the breast (due to this, there is an increase in breast volume);
- breast cancer.
This disease can be successfully treated if you consult a specialist in time and do not wait for complications that may lead to the need for surgery.
Possible side effects
If the recommended dose is not followed or the components of the drug are intolerant, side effects will appear in the form of:
- Deteriorated health of the athlete, apathy towards exercise, deterioration of sports parameters.
- Drowsiness, fatigue.
- Headache, dizziness.
- Anxiety, depression.
- Anemia, thrombophlebitis, thromboembolism.
- Impaired breathing, sinusitis, rhinitis, bronchitis, pharyngitis.
- Skin hyperemia, rashes, itching, polymorphic erythema, malignant exudative erythema, angioedema, cutaneous vasculitis.
- Thinning hair, baldness, hyperhidrosis.
- Cataracts.
- Nausea, vomiting, diarrhea, constipation.
- Lack of appetite, spinal, abdominal, chest pain.
- Excess weight, high levels of cholesterol, calcium in the blood, reduced bone density with the development of osteoporosis.
- Pain, joint stiffness.
- Inflammation of the liver, hyperactivity of alkaline phosphatase, AST, ALT.
How to take it correctly
This remedy is not recommended for a beginner in sports. The tablets are indicated for experienced bodybuilders after a course of anabolic steroids in maximum dosages. The medicine is used in two ways: before a course of anabolic steroids for prevention with therapeutic doses, and after the course, if side effects of steroids occur.
Course duration
How to drink correctly? The tablets must be taken on an empty stomach, washed down with plenty of water. In this case, the active component will quickly flow from the digestive organs into the blood.
During the course of Anastrozole you need to take it every other day. The duration of treatment is 2 weeks. During this period, all the positive properties of the drug will appear. The optimal dosage for good athletic performance does not exceed 250 mcg once every 2 days.
To reduce estradiol levels by half, a dose of 0.5-1 mg is recommended.
For preventive measures in bodybuilding, 0.5 mg every other day is sufficient.
Instructions for use indicate that for gynecomastia, use 1 mg until symptoms disappear, then 0.5 mg every other day.
It is important to remember that not all anabolic steroids are aromatized. For example, Anadrol transforms into estrogens insignificantly.
When using anabolics with a short half-life, for example, Methandrostenolone, after 10 days an analysis is made for the concentration of estradiol in the blood; Anastrozole is taken 0.5 mg every other day. Then estradiol is tested again after 10 days and the dose is adjusted.
When using anabolic steroids with long esters, for example, Sustanon, the dosage is 0.5 mg every other day. It is necessary to conduct a study on the level of estradiol 3 or 4 weeks after the start of the use of “chemistry”. A control analysis is carried out approximately 10 or 14 days after the period when Anastrozole was taken.
The bodybuilder evaluates his subjective sensations, based on which the dose is adjusted. If side effects are observed when taking the drug, then it is reduced.
What you can and cannot combine with
Tamoxifen should not be combined with Anastrozole. With such drug interactions, a mutual weakening of these drugs occurs. It is forbidden to drink alcohol with Anastrozole, otherwise, with such compatibility, the pharmacological effect of the drug will not manifest itself, and undesirable consequences will arise.
Letrozole for Men
Letrozole prevents estrogen synthetase from working without affecting the body's corticosteroid cycles or causing abnormalities. It is used in the fight against gynecomastia, to get rid of excess fluid, and normalize blood pressure.
The main focus of the courses is to strengthen muscles and increase muscle tissue density. Alternate with periods of intense training to improve post-workout recovery. Activation of the body to produce its own, endogenous testosterone.
Among the positive side effects, the drug’s ability to stimulate spermatogenesis and its potential use in azoospermia are noted.
This substance is not used in female bodybuilding due to its strong effect on hormonal balance.
Letrozole from the manufacturer “Kaspa” can be purchased at the Testosteron.com.ua store at a special price.
Post cycle therapy
It is important to remember that drugs that inhibit aromatase are not used in post-cycle therapy; they are used during the course and after the use of anabolic steroids (before post-cycle treatment).
During PCT, medications that block estrogen receptors (Clomid, Tamoxifen) are taken after a course of 2-3 weeks. Tamoxifen is required 10-20 mg per day or Clomid 25-50 mg per day is used. The dose is gradually reduced closer to the last week, then the drug is discontinued.
Thanks to human chorionic gonadotropin, testicular atrophy and desensitization of Leutig cells are prevented. Used in heavy courses, the duration of which is more than 6 weeks. It is administered on the second or fourth week or in the last 4-5 weeks of the course and continues until the anabolic steroid is eliminated. Then you need to switch to drugs that block estrogen receptors.
The use of Cabergloline, which inhibits prolactin, is indicated. They are used during courses of progestin drugs, which increase prolactin levels. The dosage is 0.25 mg every 4 days for the entire course.
Additionally shown application:
- Testosterone boosters.
- Hepatoprotectors.
- Omega-3.
- Peptides, hormones responsible for growth.
- Cortisol blockers.
What it is
Among non-steroidal aromatase inhibitors, Letrozole is very popular among athletes. The product is sold in 65 countries. It effectively blocks aromatase enzymes, which is why the medication is actively used by bodybuilders.
You may be interested in: Protein isolate: the best choice, list, manufacturers, dosage, composition, instructions for use, indications and contraindications
Letrozole is widely used in bodybuilding as an adjunct during a course of anabolic steroids. While taking the drug, the concentration of estrogen decreases and the production of the hormone testosterone increases. Among similar drugs, the product is considered one of the most effective. This makes it very popular among bodybuilders.
You may be interested in: Tribulus sports nutrition: purpose, release form, features of administration, dosage, composition, indications and contraindications
Experts talk about the high effectiveness of Letrozole during a course of steroids and during PCT, which has been confirmed by numerous studies. Estrogen levels are reduced by 97%. A similar result can be obtained only when using high dosages. Taking the recommended amount leads to a decrease in estrogen levels by 76 or 79%, which can also be called a good result.
Due to the decrease in estrogen levels, the occurrence of side effects associated with taking anabolic steroids is reduced. In addition, Letrozole in bodybuilding helps to increase the synthesis of globulin, luteinizing and follicle-stimulating hormones, as well as testosterone production.
Feedback from hosts
Evgeniy, bodybuilder: “I work out in the gym, I already have sports records, I posted photos and videos on social networks. I learned from colleagues about the consequences of Estrogen. I don’t take it myself yet, since I’m new to this business. But I know that many people use Anastrozole during drying because it removes water.”
Alexander, bodybuilder: “I was on steroids a little, just playing around. Then I began to notice that my breasts were sagging, and I was turning into a woman. I found out about Anastrozole, I take it under the supervision of a trainer, and I let it go.”
Sergey, sports doctor: “I select the dosage only when monitoring the estradiol test in order to prevent side effects.”
Svetlana, oncologist: “In my practice, I use Anastrozole to treat breast cancer during postmenopause.”
The downside of estradiol, negative functions
- Provokes swelling (retains fluid), risk of increased blood pressure (hypertension)
- the rate of blood clotting increases
- appearance of acne (pimples)
- there is an increased risk of cardiovascular disease
- swelling, itching in the nipples (gynecomastia), in case of transition to the stage of fibrotic changes, surgical intervention will be required
- decreased sexual desire and potency
- profuse sweating, sleep disturbance
- malfunction of the gastrointestinal tract
Thanks to the use of aromatase inhibitors, in this article we are talking about anastrozole, we can control the levels of estradiol, bringing it to normal, reference values. By selecting the correct dosage of AIs, the results from the use of anabolic and androgenic steroids can be significantly improved, while avoiding most of the above side effects.
Analogs
In bodybuilding, in addition to Anastrozole, the use of Letrozole and Exemestane is acceptable. These are effective means, but have a significantly lower cost. But the disadvantages are characterized by strong suppression of estrogen hormones, the effect of these drugs is difficult to control.
Other analogues:
- Arimidex.
- Anastrex.
- Egistrazol.
- Mammozol.
Which Anastrozole is better?
All analogues have the same effect, but may differ in price.
https://www.youtube.com/watch?v=oD4gvScTDhw