Fareston - reviews. The use of Toremifene (Fareston) in power 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 gives it a better safety profile. Acting indirectly through endogenous estrogens, FARESTON effectively blocks the growth of a breast tumor. 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, a stable concentration of the drug is 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 binds specifically 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. With a primary tumor, the remission rate is 50%. In high doses, FARESTON is also effective in cases where side endocrine and / or cytostatic treatment does not work.
Indications: breast cancer in postmenopausal women.
Release form:
Tablets 20 mg, 30 pcs. packaged;
tablets 60 mg, 60 pcs. packaged.
Indications for appointment:
1. Young women who have a longer theoretical life expectancy with 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 disease (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 a hormone therapy for breast cancer patients have been proven in large-scale studies. However, this drug exhibits estrogenic activity to a certain extent, being a partial agonist of estradiol. In this connection, 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 with its unstable structure.
Antiestrogen Fareston(torimifen) produced by the Orion company, having a chlorine atom in the chemical structure, is more sustainable than tamoxifen - this drug is a triphenylethylene derivative that blocks estradiol receptors.
In our study, 27 patients with metastatic breast cancer received tormifene at a dose of 60 mg daily as the first line of endocrine therapy for a long time until the end of the therapeutic effect, due to the fact that initially they had comorbidities - dysplastic processes in the endometrium, a history of metrorrhagia, disorders liver function.
The drug was well tolerated by all patients: no undesirable side effects characteristic of tamoxifen were registered. To a lesser extent, adverse reactions from the gastrointestinal tract (nausea, anorexia, gastric discomfort) were expressed.
Thus, in terms of hormone therapy for metastatic breast cancer, the use of fareston appears to be more promising than tamoxifen, since this drug can be prescribed in higher doses.
This drug is available in the following pharmacies:
Pharmacy: Minsk, st. Rosa Luxembourg, 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 site "Your Trainer" does not sell or encourage the use of anabolic steroids and other potent substances. The information is provided so that those who nevertheless decide to take them do it as competently as possible and with minimal risk to health.
Fareston is the commercial name for the substance toremifene citrate. A very expensive drug that has already firmly entered the diet of advanced chemists and constantly raises questions from beginners in chemotherapy. This article is intended to dispel all misunderstandings regarding the fareston. What it is?
Fareston is the closest relative of tamoxifen and Clomid. That is, a selective (selective) modulator of estrogen receptors. Simply put, 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-estrogen drugs to fight estrogen-dependent breast cancer in women. It is designed to help in cases where the good old tamoxifen refuses to work.Why is it needed?
What is the practical value of Fareston in power sports? In principle, it can serve as a full-fledged 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 clarify right away that Clomid makes sense to eat only in the period after course therapy. It perfectly starts the work of the genital arc, but as a means of preventing the phenomena of feminization, 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 expensive, but indispensable in this case, toremifene. It will allow you to fight the estrogenic side effects of these steroids and will not aggravate their progestogenic activity. 2. But toremifene does not cope with the progestogenic activity of these three. are 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 concomitant and post cycle use with progestins. It can greatly exacerbate the progestogenic side effects of these steroids. This does not happen to everyone, but by trying 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 actually the whole situation. As you can see, there are no secrets here. If it is difficult for you to digest and assimilate the information in this article, ask questions in the comments below it. I will definitely answer. Quite simply, writing in this case does not work.The composition of Tamoxifen includes 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 pieces.
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 derived from them.
As a result, a complex tamoxifen receptor transfer cofactor”, which, translocating to cell nucleus , prevents hypertrophy of estrogen-dependent cells.
The Sports Wiki states that the substance was first synthesized in 1971 and became the first antiestrogen among members of the class of selective estrogen receptor modulators (EMREs).
Renders antigonadotropic effect and suppress 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 women in her absence. At oligospermia increases serum concentration in men 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 exactly.
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 4 to 7 hours after oral administration of the tablet. Steady-state plasma concentration is observed 4 weeks after the start of treatment with a dosage of 40 mg / day.
WITH blood plasma albumin the substance binds to 99%. Metabolism 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 is 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 anticancer antiestrogen non-steroidal agent , which is based on the substance . The main features of the drug:
- the presence of a chlorine atom in its chemical structure (which makes the drug more stable in comparison with Tamoxifen);
- absence oncogenic effect ;
- the ability to induce apoptosis;
- effectiveness at RE-negative tumors .
According to clinical observations conducted within six months, it was found that when taking Fareston:
- changes in hormonal homeostasis are much more favorable than when taking Tamoxifen;
- changes that are less dangerous for the patient in terms of oncorisk develop;
- an order of magnitude less often there are undesirable side effects.
The studies also led to the conclusion that, as part of complex treatment, the influence of Fareston on tumor process with progressive breast cancer more effective than the effect of its analogue: when it was used, patients had a complete remission much more often, and the progression of the disease began 1.2 months later.
Besides, antitumor effect during treatment Fareston observed in more patients.
Hello, Dmitry Andreevich! I turn to 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 biopsy of the sentinel lymph node were performed. Histological conclusion: grade 1 invasive ductal carcinoma with a maximum diameter of 0.9. Outside the invasive tumor, numerous ducts are observed with ductal carcinoma in situ. Tumor lesions of two lymph nodes were not found. Further treatment took place in Russia according to the issued protocol. She 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 breast irradiation of 50 Gy in 25 fractions, followed by additional targeted irradiation (“boost”) at a dose of 10 Gy per 5 factions. According to the protocol, after the end of radiotherapy, I was recommended hormone therapy with Tamoxifen for a period of 2.5 years, followed by a switch to an aromatase inhibitor drug (such as Letrozole) for an additional 2.5 years. I finished radiotherapy at the beginning of March of this year, but the oncologist advised me to wait a while to take Tamoxifen hormonal pills. Reason:: gynecologists found endometrial hyperplasia in me. 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), Tamoxifen should not be taken. However, yesterday at the appointment with the chemotherapist, I was told that I should start taking Tamoxifen right 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 be 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 appeal to you with a big request to advise: which drug should I start taking anyway: Tamoxifen or Fareston? Because I already missed three months (after all, I had to start taking hormonal drugs as soon as the radiotherapy ended in March). And further. My periods stopped in August 2014 after the very first course of chemotherapy and started only 7 months later, after the end of irradiation. 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 artificial menopause, in which I was 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 passed tests for the presence of human papillomavirus. HPV type 56 was found. 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 (total 20 tablets), "Imunofan" 2.0 cubes / m 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-Intim Spray. Now I'm taking Indinol-forte, 3 months left. In this regard, one more question: is it possible to take hormonal pills along with Indinol-forte? Perhaps I have confusedly stated my problem. But I need to figure out which drug is preferable in my case: Tamoxifen or Fareston. I will look forward to your reply. Thank you very much in advance.
In your case, I would appoint Zoladex - to turn off the function of the ovaries. It is believed that tamoxifen does not work with her2neu 3+, although not everyone agrees with this. Hormonal drugs (duphaston or others based on progesterone, as well as containing estrogens) are contraindicated for you. In any case, you should be guided by the opinion of the attending physician.
