- July 3, 2019
- Other drugs
- Smirnova Alexandra
The drug "Anastrozole" is an anti-estrogen drug available in tablet form. It was originally developed as a drug intended for breast cancer. But besides this, it is also used in sports. It is used by athletes and fans of strength training. This medicine helps patients avoid gynecomastia, that is, enlargement of the mammary glands, eliminating swelling and other negative side effects that often accompany treatment with anabolic steroids. Next, we will consider in detail the instructions for using this medication. And at the end of the article there are reviews from patients who happened to drink it during treatment.
About the drug
In addition to modern use in sports, it is primarily an antitumor agent. It acts as a non-steroidal selective aromatase inhibitor. During postmenopause, estradiol is predominantly formed from estrone, produced in peripheral tissue through conversion from androstenedione (subject to the participation of the aromatase enzyme).
Decreasing circulating estradiol may have a therapeutic effect in women with breast cancer. It is worth mentioning that it does not have androgenic and estrogenic activity, and also does not affect the secretion of aldosterone and cortisol in therapeutic doses.
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.
What effects can the medication have?
This medication has the following pronounced effect: just 1 milligram of its active substance helps reduce the content of estradiol in the bloodstream by eighty percent. Even Tamoxifen, which is quite popular, cannot compare with this medicine in terms of strength of action. Among other things, Anastrozole can produce the following effect on the body:
- Reduced aromatization level (by about eighty percent).
- Has inhibitor properties.
- Decrease in estrogen levels in the blood.
One of the main properties of Anastrozole tablets is their fairly rapid effectiveness. Just two hours after administration, the maximum concentration of the active substance is observed in patients’ blood. Against this background, suppression of aromatization processes occurs as quickly as possible. In this regard, Anastrozole is considered one of the most effective remedies for athletes who have a tendency to aromatize.
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.
Pharmacokinetics
In accordance with the instructions for use of Anastrozole, after ingestion the drug can be quickly absorbed from the digestive system. Its maximum concentration in plasma is usually achieved within two hours (on an empty stomach). The speed decreases somewhat, but not the degree of suction. Plasma protein binding is forty percent. There is no information about cumulation.
The metabolism of this drug is carried out by dealkylation, glucuronidation and hydroxylation. Triazole, the main metabolite detected in plasma and urine, does not inhibit aromatase. "Anastrozole" with its metabolites are excreted primarily in urine (less than ten percent unchanged) within seventy-two hours after administration of a single dosage.
As the instructions for use of Anastrozole indicate, the clearance of the drug in question after oral administration in patients with stable cirrhosis of the liver or failure of kidney function does not differ from the indicator determined in healthy people. The pharmacokinetics of this drug in postmenopausal women does not change.
What is the main purpose of the presented medication?
Indications for use
It is advisable to take Anastrozole in the following cases:
- Presence of early hormone-positive breast cancer among postmenopausal women (as part of adjuvant therapy).
- The occurrence of common breast cancer in postmenopausal women.
- The presence of early hormone-positive breast cancer among postmenopausal women after treatment with Tamoxifen for two to three years (adjuvant therapy).
Indications for the drug are described in detail in the instructions.
Dosage
How to take Anastrozole for oncology? The medicine is taken orally. The recommended dose is 1 milligram (that is, one tablet) once a day. For early stage invasive breast cancer (hormone receptor positive) among postmenopausal patients, the standard duration of endocrine adjuvant therapy is five years.
For patients suffering from mild or moderate renal dysfunction, no dosage adjustment of Anastrozole is required. The use of the drug in this group of women requires caution. Patients with liver dysfunction also do not require adjustment of the volume of medication.
Instructions for the use of Anastrozole by athletes
This drug is recommended only for experienced athletes, and it is advisable for beginners not to take it. Pills are used immediately after the course of anabolic steroids is completed. This medication should be taken in the following two cases:
- against the background of the appearance of severe adverse reactions after using steroids;
- before the start of the course as a prophylactic drug.
After steroids, they usually take from 0.25 to 1 milligram per day. But it will be better if the dosage is determined by a specialist.
According to indications, Anastrozole can be taken for two weeks. It is during this period of time that this drug will have time to fully demonstrate all its properties. In order for the active component to enter the bloodstream as quickly as possible, it is necessary to drink the medicine before meals and wash it down with a large volume of liquid. Experts do not recommend that athletes use Anastrozole. The fact is that this drug can provoke a sharp change in hormonal levels, which can lead to unpredictable consequences for the health of the female body.
Next, we will figure out when this medication is not suitable for use during treatment.
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.
Contraindications for Anastrozole
The presented pharmaceutical product may not always be used as part of treatment; for example, it is not prescribed to patients in a number of the following cases:
- Against the background of the premenopausal period.
- In case of severe liver failure (since safety, as well as effectiveness, have not been established).
- Concomitant treatment with Tamoxifen or medications that contain estrogens.
- Pregnancy and lactation period (i.e. breastfeeding).
- In childhood (since safety and effectiveness in this category of patients have not been established).
- The presence of hypersensitivity to anastrozole or other components of the drug.
With great caution, it is necessary to prescribe the drug in question if people have osteoporosis, hypercholesterolemia, coronary heart disease, liver dysfunction, severe renal failure, lactase deficiency and lactose intolerance. You should also beware of it against the background of galactose malabsorption (the fact is that the dosage form of the drug described contains lactose).
Side effects
General hormonal influences may cause adverse reactions. Other side effects are possible. Some patients experience sensitivity of the immune system to the substances contained in the tablets. Before therapy, the doctor must rule out allergies and intolerances.
Main adverse reactions:
- Nervous system: cephalgia, daytime sleepiness, carpal tunnel syndrome in patients with a predisposition to the disease.
- Digestive system: lack of appetite, exhaustion of the body, urge to vomit, abdominal discomfort, loose stools.
- Reproductive system: dryness of the vaginal mucosa, vaginal hemorrhage (often after stopping therapy or changing the drug).
- Skin: rashes, itching, hair loss, erythema reactions, Stevens-Johnson syndrome.
- Metabolism: increased cholesterol levels in the blood, imbalance of mineral components of bone tissue with decreased bone density, bone fractures.
- Liver and biliary tract: increased levels of liver enzymes, increased bilirubin levels, inflammation of the liver tissue.
- Allergic manifestations: anaphylactoid effects, Quincke's edema, anaphylactic shock, urticaria, other reactions.
- Others: joint pain, stenosing thromsynovitis, flushing of the facial area, general weakness, fatigue.
The doctor monitors the patient’s condition at all stages of treatment. If adverse reactions occur, you should seek advice.
Drug interactions
Anastrozole reduces the effectiveness of estrogens. Clinical studies have shown that with the simultaneous combination of this medication with Antipyrin or Cimetidine, drug interaction, which is caused by the induction of microsomal liver enzymes, is unlikely.
What should you expect from using these tablets? What are the main consequences of taking the drug?
What side effects can the drug cause in patients?
Side effects of Anastrozole occur relatively rarely. Usually they are associated with intolerance to the active components or exceeding the recommended dosages. Among the most common undesirable manifestations, it is worth highlighting fatigue along with drowsiness, redness of the skin, headache, as well as various negative manifestations from the digestive system (nausea, vomiting, diarrhea, and so on).
You should stop taking Anastrozole if you have chronic pathologies of the cardiovascular system. This is due, first of all, to the fact that the medication actively counteracts the side effects of taking steroids, but at the same time it blocks the production of good cholesterol, which can lead to certain heart problems. For these reasons, patients with heart disease should consult a doctor before taking Anastrozole or prefer medications with a similar effect, but a distinctive mechanism of action on the body.
Composition and release form
Anastrozole is an active component with antitumor properties. The concentration and composition of additional components depend on the manufacturer. Typically, milk sugar, polyvinylpyrrolidone K25, sodium dodecyl sulfate, sodium starch glycolate A, calcium salt of stearic acid are present in tablet form. The special shell facilitates the absorption of the substance in the digestive tract.
Package
It is produced in the form of tablets.
special instructions
Against the background of doubts about the hormonal status, menopause must be confirmed biochemically. If metrorrhagia persists during therapy, a consultation with a gynecologist will be required. If patients have concomitant osteoporosis or are at risk of its occurrence, it is recommended to evaluate bone mineral density using densitometry at the beginning and during therapy. If necessary, osteoporosis is prevented under the supervision of a doctor.
In case of moderately severe renal impairment, no dosage adjustment is required. Efficiency, as well as safety, when used simultaneously with Tamoxifen, regardless of the general status of hormonal receptors, is comparable to that when using this medicine alone. During the period of therapy, you will need to be careful when driving vehicles and engaging in other dangerous types of activities that require special attention and speed of psychomotor reaction.
Overdose of the drug in question
Over the entire period, isolated clinical cases of accidental overdose of this drug have been described. A single dose of medication that could lead to life-threatening symptoms has not been established.
According to the instructions for use of Anastrozole, there is currently no specific antidote; in case of overdose, symptomatic therapy is carried out. You can independently induce vomiting if the patient is conscious. Dialysis may be performed. General supportive treatment is recommended; patient monitoring will also be required along with monitoring the functions of important systems and organs.
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
Reviews about this drug
Women who have used this medicine in the setting of early hormone-positive postmenopausal breast cancer write that this medicine is well suited for adjuvant therapy. Since the medication lowers circulating estradiol, it may have a therapeutic effect in this cancer.
According to reviews, Anastrozole is also very popular among athletes, which is directly related to its pronounced anti-estrogenic properties. As people write, the results of use can be noticed a couple of hours after consuming the tablet. The most positive comments come from professional bodybuilders who believe that such a drug can cope well with the excessive production of estrogen observed after a long course of anabolic steroid use.
But it is worth noting that this product must be used with great caution. And just before you start using it, you need to consult a doctor. In addition, it is important to strictly follow the recommended dosages of Anastrozole. It is better to read the reviews in advance.
Reviews and prices
It is not recommended to evaluate the effectiveness of serious drugs based on patient reviews, since antitumor drugs are prescribed only by oncologists as part of life-saving drug therapy. Experts speak well of the properties of the medicine. There is a lower risk of serious complications while taking the tablets compared to other anticancer drugs.
The average price of thirty tablets is 1200 rubles.
