Fareston - reviews. The use of Toremifene (Fareston) in strength sports Fareston or Tamoxifen - which is more effective
FARESTON ®
Toremifene(toremifen)
FARESTON- a new anti-estrogenic drug. It is a non-steroidal derivative of triphenylethylene with an attached chlorine atom in the ethylene side chain, which distinguishes it from tamoxifen and determines a better safety profile. Acting indirectly through endogenous estrogens, FARESTON effectively blocks the growth of breast tumors. In tumor tissue, FARESTON binds competitively to the estrogen receptor. In addition, toremifene has the ability to reduce prolactin production, which can also play a positive role in the treatment of patients with breast cancer.
When taken orally, FARESTON is completely absorbed and reaches peak plasma concentrations after 4 hours. At a dose of 60 mg per day, steady-state concentrations of the drug are achieved within 3-4 weeks. The metabolism of FARESTONA occurs in the liver. It is excreted mainly in bile and faeces. The half-life of FARESTON is approximately 5 days, which allows the drug to be administered once a day.
FARESTON has excellent safety performance. The chlorine atom stabilizes the electronic structure of the molecule and prevents the formation of metabolites that damage DNA. Due to this, toremifene does not have mutagenic and teratogenic properties and does not lead to the development of hepatocellular cancer and endometrial cancer.
Toremifene specifically binds to cellular estrogen receptors and inhibits DNA synthesis and cell division.
Fareston is also effective in estrogen-independent cancers.
FARESTON is effective and well tolerated in the treatment of breast cancer in postmenopausal women. For primary tumors, the remission rate is 50%. In high doses, FARESTON is also effective in cases where side endocrine and/or cytostatic treatment does not bring results.
Indications: breast cancer in postmenopausal women.
Release form:
Tablets 20 mg, 30 pcs. packaged;
tablets 60 mg, 60 pcs. packaged.
Indications for use:
1. Young women who have a long theoretical life expectancy when contracting breast cancer.
2. Women with hyperplastic processes in the uterus, fibroids, polyps.
3. Women with a history of cancer (uterine cancer in close relatives).
4. Women with liver pathology (with an increased risk of hepatocellular cancer).
5. Women with a mutation in the BRCA gene - 1, 2.
6. Fibrocystic mastopathy with a high risk of developing cancer, for example, proliferative forms of mastopathy.
7. Prevention of breast cancer in women at high risk of developing cancer.
The undeniable advantages of long-term use of tamoxifen as hormone therapy for patients with breast cancer have been proven in large-scale studies. However, this drug exhibits estrogenic activity to a certain extent, being a partial agonist of estradiol. Therefore, there is a high probability of developing endometrial cancer and liver cancer as a result of tamoxifen therapy.
The oncogenic effect of this drug is associated with stimulation hyperplastic processes in the endometrium, oxidation of the drug in the liver, as well as its unstable structure.
Antiestrogen Fareston(torimifene) produced by the Orion company, having a chlorine atom in its chemical structure, is more sustainable than tamoxifen - this drug is a derivative of triphenylethylene, which blocks receptors for estradiol.
In our study, 27 patients with metastatic breast cancer received torimifene as the first line of endocrine therapy at a dose of 60 mg daily until the end of the therapeutic effect, due to the fact that initially they had concomitant pathology - dysplastic processes in the endometrium, a history of metrorrhagia, disorders liver functions.
The drug was well tolerated by all patients: no unwanted side effects typical of tamoxifen were recorded. Adverse reactions from the gastrointestinal tract (nausea, anorexia, gastric discomfort) were less pronounced.
Thus, in terms of hormonal therapy for metastatic breast cancer, the use of fareston seems more promising in comparison with tamoxifen, since this drug can be prescribed in higher doses.
This drug is available in the following pharmacies:
Pharmacy: Minsk, st. Rosa Luxemburg, 143, tel. 207-32-56
Pharmacy: Minsk, Zvezda Avenue, 16 (Moscow market)
Pharmacy: Minsk, st. Yesenina, 35
Pharmacy: Minsk, st. Sukharevskaya, 16 (supermarket "Vester")
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Date of:
2014-01-29
Views: 21 643 Grade: 5.0
Important! The “Your Trainer” website does not sell or encourage the use of anabolic steroids and other potent substances. The information is provided so that those who decide to take them do so as competently as possible and with minimal risk to health.
Fareston is the commercial name for the substance toremifene citrate. A very expensive medicine, which has already become firmly established in the diet of advanced chemists and constantly raises questions among those new to chemotherapy. This article is intended to dispel all misunderstandings regarding Fareston. What it is?
Fareston is the closest relative of tamoxifen and Clomid. That is, a selective (selective) modulator of estrogen receptors. To put it simply, this is a group of drugs whose molecules, when they enter the body, find estrogen receptors and attach to them in various parts of our body. But in some tissues they prevent estrogens from activating their receptors, while in others they activate these receptors better than estrogens themselves. Toremifene is a new generation of anti-estrogenic drugs to combat estrogen-dependent breast cancer in women. It is designed to help in cases where good old tamoxifen refuses to work.Why is it needed?
What is the practical value of Fareston in strength sports? In principle, it can serve as a complete replacement for tamoxifen and Clomid during the PCT period (). But this is unreasonable due to the high cost of toremifene. Why pay more? Let's immediately clarify that it makes sense to eat Clomid only in the period after course therapy. It perfectly starts the functioning of the genital arch, but as a means of preventing feminization phenomena, it is too weak. Especially given the now generally accepted dosages of steroids. So let's leave Clomid alone. And tamoxifen has one VERY unpleasant feature. In some cases, used in parallel with progestins (,), it can significantly enhance their side effects associated with progestogenic activity:- Excessive fluid retention
- Gynecomastia,
- Accumulation of fat in unexpected places
- The strongest oppression of the reproductive system.
conclusions
1. In parallel with nandrolone, oxymetholone and trenbolone, we use toremifene, an expensive but irreplaceable drug in this case. It will combat the estrogenic side effects of these steroids and will not exacerbate their progestogenic activity. 2. But toremifene does not cope with the progestogenic activity of these three. Needed here. 3. On PCT after these steroids, we use ONLY Clomid. Toremifene is also suitable, but why pay a lot of money? No need. 4. Tamoxifen is NOT SUITABLE for parallel and post-cycle use with progestins. It can greatly exacerbate the progestogenic side effects of these steroids. This doesn’t happen to everyone, but if you try to save on your health, you risk global changes, both in the reproductive system and in appearance. Miser pays twice. 5. The working dose of toremifene is in the range of 20-60 mg per day. It all depends on the dosages of drugs - progestins. That's the whole situation. As you can see, there are no secrets here. If you find it difficult to digest and assimilate the information in this article, ask questions in the comments below. I will definitely answer. It’s not possible to write anything very simply in this case.Tamoxifen contains 15.2; 30.4 or 45.6 mg tamoxifen citrate , which, respectively, is equivalent to 10, 20 or 30 mg of tamoxifen.
Tablets are packaged in blisters, containers or polyethylene bottles of 10, 20, 30, 40, 50, 60, 90, 100, 120, 150 or 300 pcs.
Release form
Pills.
pharmachologic effect
It has antiestrogenic and antitumor properties.
Pharmacodynamics and pharmacokinetics
Tamoxifen is non-steroidal anticancer antiestrogen drug , characterized by the ability to competitively inhibit peripheral estrogen receptors in target organs and tumors arising from them.
As a result, the complex “ tamoxifen receptor-transfer cofactor”, which, translocating into cell nucleus , prevents hypertrophy of estrogen-dependent cells.
Sports Wiki states that the substance was first synthesized in 1971 and became the first antiestrogenic agent among representatives of the class of selective estrogen receptor modulators (SREs).
Renders antigonadotropic effect and suppresses education prostaglandins in tumor tissue , slows down the development of the tumor process, which is stimulated.
After taking a single dose of the drug, the ability to block estrogens persists for several weeks.
Promotes release pituitary gonadotropic hormones , thereby causing ovulation in women in its absence. At oligospermia in men increases serum concentration estrogen , luteotropin And follitropin .
Tamoxifen and some of its metabolites exhibit the properties of powerful inhibitors (oxidases) with mixed functions (monooxygenases) of the liver cytochrome P450 system. However, how clinically significant these effects are is not known.
In some cases, Tamoxifen is effective in estrogen-independent tumors . The substance has a partial estrogen-like effect on the lipid spectrum, and bone tissue .
Absorption of Tamoxifen is high, TCmax is from 4 to 7 hours after oral administration of the tablet. Steady-state plasma concentrations are observed 4 weeks after the start of treatment using a dosage of 40 mg/day.
WITH blood plasma albumin the substance is 99% bound. Metabolization occurs in the liver by demethylation, hydroxylation and conjugation and with the participation of the CYP2C9 isoenzyme.
Metabolites are excreted mainly with the contents intestines and partly kidneys (minor amount). The extraction is carried out in two stages. The initial half-life of the main metabolite circulating in the systemic circulation ranges from 7 to 14 hours, the final slow half-life is 7 days.
Indications for use
The use of Tamoxifen is advisable for:
- estrogen sensitive tumors ;
- malignant damage to breast tissue (especially during the period in women);
- breast cancer , including in men after surgical removal of the genitals;
- ductal breast cancer (ductal carcinoma in situ);
- endometrial cancer .
Fareston or Tamoxifen - which is more effective?
Fareston - This antitumor antiestrogenic nonsteroidal drug , the basis of which is the substance. Main features of the medicine:
- the presence of a chlorine atom in its chemical structure (which makes the drug more stable compared to Tamoxifen);
- absence oncogenic effect ;
- ability to induce apoptosis;
- effectiveness at ER-negative tumors .
According to clinical observations conducted over six months, it was found that when taking Fareston:
- changes in hormonal homeostasis are an order of magnitude more favorable than when taking Tamoxifen;
- changes that are less dangerous for the patient in terms of cancer risk develop;
- Undesirable side effects occur an order of magnitude less often.
The studies also led to the conclusion that, as part of complex treatment, the influence Fareston on tumor process with progressive breast cancer more effective than the effect of its analogue: with its use, patients experienced complete remission much more often, and disease progression began 1.2 months later.
Besides, antitumor effect during treatment Fareston was observed in a larger number of patients.
Hello, Dmitry Andreevich! I am asking you for advice: which hormonal drug to choose: Tamoxifen or Fareston? Briefly about my situation: In July 2014, I was diagnosed with T1H0M0 breast cancer. Histological conclusion: invasive breast carcinoma of a nonspecific type of moderate malignancy (G2). IHC: Er Ts=5 Pr Ts=0 Her2-neu-3b. Ki67-35%. Luminal type B, HER2 positive type. I went to the Rambam Medical Center (Haifa, Israel), where a lumpectomy of the right breast and a sentinel lymph node biopsy were performed. Histological conclusion: grade 1 invasive ductal carcinoma with a maximum diameter of 0.9. Outside the invasive tumor, numerous ducts with ductal carcinoma in situ are observed. Tumor lesions of two lymph nodes were not found. Further treatment took place in Russia according to the issued protocol. I underwent six courses of chemotherapy with Taxotere/Carboplatin/Herceptin (I continue therapy with Herceptin every 21 days until 1 year), then there was radiotherapy with irradiation of the mammary gland 50 Gy in 25 fractions, followed by additional targeted radiation (“boost”) at a dose of 10 Gy per 5 factions. According to the protocol, after the end of radiotherapy, I was recommended to undergo hormonal therapy with Tamoxifen for a period of 2.5 years, followed by a transition to an aromatase inhibitor drug (such as Letrozole) for an additional 2.5 years. My radiotherapy ended at the beginning of March this year, but the oncologist advised me to hold off on taking the hormonal tablets Tamoxifen for now. Reason: gynecologists discovered endometrial hyperplasia in me. A diagnostic curettage of the endocervix and endometrium was performed. Therefore, gynecologists advised: until I finish the course of Herceptin (and this will be in August), I should not take Tamoxifen. However, yesterday at an appointment with a chemotherapy doctor I was told that I need to start taking Tamoxifen now. Then I decided to seek advice from an oncologist-gynecologist, who, in turn, categorically forbade taking Tamoxifen, believing that its main “side” is the growth of endometrioid tissue (endometriosis) and assuring me that if I still take it, then inevitably, in a year or two, I will find myself as their patient with uterine (or cervical) cancer. And she advised me to take another hormonal drug - Fareston, which, in her opinion, does not have such side effects as Tamoxifen. In this regard, I would like to ask you for advice: which drug should I start taking: Tamoxifen or Fareston? Because I already missed three months (after all, I should have started taking hormonal medications as soon as radiotherapy ended in March). And further. My periods stopped in August 2014 after the first course of chemotherapy and began only 7 months later, after the end of radiation. Now they go regularly. I had a diagnostic curettage of the endocervix and endometrium at the end of January 2015, a month before the resumption of menstruation. Maybe endometrial hyperplasia was due to the artificial menopause I was in for all these 7 months? The conclusion was: chronic endocervicitis of a high degree of activity. Histological signs of viral infection. On the recommendation of an oncologist-gynecologist, I was tested for the presence of human papillomavirus. HPV type 56 was detected. Treatment was prescribed: "Indinol-Forte" 1 capsule 2 times a day for 6 months, after one month of taking "Indinol-Forte" add: "Lavomax" 1 tablet every other day (20 tablets in total), “Imunofan” 2.0 cc IM daily for 15 days, “Epigen-intim spray” up to 4-6 times/day, 1 dose for 14 days. I have already taken Lavomax, Imunofan and Epigen-intimate spray. Now I’m taking Indinol-Forte, 3 months left. In this regard, one more question: is it possible to take hormonal pills together with Indinol-Forte? Perhaps I presented my problem chaotically. But I need to figure out which drug is preferable in my case: Tamoxifen or Fareston. I will look forward to your response. Thank you very much in advance.
In your case, I would prescribe Zoladex to turn off ovarian function. It is believed that tamoxifen does not work for her2neu 3+, although not everyone agrees. Hormonal drugs (duphaston or others based on progesterone, as well as those containing estrogens) are contraindicated for you. In any case, you need to rely on the opinion of your doctor.
