Trade name: Arimidex®.
Anastrozole is the generic name for the drug Arimidex®. In some cases, healthcare professionals may use the trade name Arimidex® when referring to the generic drug name Anastrozole.
Type of drug:
Anastrozole is an anti-cancer hormone therapy. This drug is classified as a "non-steroidal aromatase inhibitor" (see "How anastrozole works" below for more information).
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.
Anastrozole
If there is doubt about the patient's hormonal status, menopause should be confirmed by determining the concentration of sex hormones in the blood serum. In case of persistent uterine bleeding while taking anastrozole, consultation and observation of a gynecologist is necessary. There are no data on the use of anastrozole in patients with severe liver dysfunction.
In patients with osteoporosis or an increased risk of developing osteoporosis, bone mineral density should be assessed by densitometry, such as a DEXA scan (dual energy x-ray absorptiometry), at the beginning of treatment and regularly throughout it. If necessary, treatment or prevention of osteoporosis should be prescribed and the patient's condition should be carefully monitored. Because anastrozole decreases circulating concentrations of estradiol, it may result in decreased bone mineral density. There is currently insufficient data regarding the beneficial effects of bisphosphonates on anastrozole-induced bone loss or their benefit when used prophylactically.
There is no data on the simultaneous use of anastrozole and GnRH analogue drugs.
In women with estrogen receptor-negative tumors, the effectiveness of anastrozole has not been demonstrated unless there has been a previous positive clinical response to tamoxifen.
Preparations containing estrogens should not be prescribed concomitantly with anastrozole, because they will neutralize the pharmacological effect of anastrozole.
The effectiveness and safety of anastrozole and tamoxifen when used simultaneously, regardless of hormonal receptor status, are comparable to those when using tamoxifen alone. The exact mechanism of this phenomenon is not yet known.
It is not known whether anastrozole improves treatment outcomes when used in conjunction with chemotherapy.
Influence on the ability to drive a car and operate machinery. Some side effects of anastrozole, such as asthenia and drowsiness, may adversely affect the ability to perform potentially hazardous activities that require increased concentration and speed of psychomotor reactions. In this regard, it is recommended to exercise caution when operating vehicles and machinery when these symptoms appear.
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.
How Anastrozole works:
Hormones are chemicals produced by glands in the body that enter the bloodstream and can affect other parts of the body. For example, the hormone testosterone is produced in the testicles and is responsible for masculine characteristics such as a deeper voice and increased body hair. The use of hormone therapy to treat cancer is based on the observation that the growth of cancer cells may depend in part on the binding of hormones to receptors on the surface of cancer cells.
Hormone therapy can work through methods such as stopping the production of a particular hormone or disrupting the hormone's binding to a cancer cell receptor. Different types of hormone therapy are classified based on their function and/or the type of hormone affected.
Anastrozole is an aromatase inhibitor. This means that it blocks the enzyme aromatase (found in muscle, skin, breasts and fat), which is used to convert androgens (hormones produced by the adrenal glands) into estrogens. Estrogen-dependent tumor cells grow less when estrogen is absent.
Note. We strongly encourage you to talk with your healthcare provider about your specific condition and treatment options. The information contained on this website is useful and educational in nature and is not a substitute for medical advice.
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.
Precautionary measures:
- Before starting treatment with anastrozole, be sure to tell your doctor about any other medications you take (including over-the-counter medications, vitamins, or herbal remedies).
- Anastrozole interacts with some medications. Be sure to tell your doctor if you are taking these medications:
- Tamoxifen
- Estrogen
- Warfarin
- Medicines containing estrogen/estradiol (commonly used for menopause and birth control)
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.
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.
Self-care tips:
- If you experience hot flashes, wearing light clothing, staying in a cool environment, and placing a cool cloth on your head may help reduce symptoms. Check with your doctor if they get worse or become intolerable.
- Acetaminophen or ibuprofen may help relieve discomfort from general pain. However, be sure to consult your doctor before taking it.
- Anastrozole causes slight nausea. However, to reduce nausea, take anti-nausea medications as prescribed by your doctor before taking them.
- Proper treatment methods such as plenty of rest and a healthy diet along with regular exercise are recommended.
- If you experience symptoms or side effects, be sure to discuss them with your doctor. They may prescribe medications and/or suggest other effective solutions to resolve such problems.
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.
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.”
How is anastrozole administered:
- Anastrozole is a tablet that is taken orally.
- You should take anastrozole at approximately the same time every day.
- You can take anastrozole with or without food.
- If you miss a dose of anastrozole, take it as soon as you remember, unless it is time for your next dose. Do not take a double dose to make up for a missed dose.
- You should not stop taking Anastozole without talking to your doctor, even if you feel well.
The amount of anastrozole you receive depends on many factors, including your general health or other health problems, and the type of cancer or condition being treated. Your doctor will determine your dose and how long you will take anastrozole.
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.
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