Nolvadex for women
Nolvadex is a non-steroidal drug from the triphenylethylene group that has a combined spectrum of pharmacological action as an estrogen antagonist and agonist in different tissues. In breast cancer patients, tamoxifen primarily exhibits an anti-estrogenic effect in tumor cells, preventing estrogen from binding to estrogen receptors. Nolvadex and some of its metabolites compete with estradiol for cytoplasmic estrogen receptor binding sites in tumors of the breast, uterus, vagina, pituitary gland, and estrogen receptor-rich tumors. Unlike the estrogen receptor complex, the Nolvadex receptor complex does not stimulate DNA synthesis in the nucleus, but inhibits cell division, leading to tumor cell regression and death.
In women with estrogen-positive / unspecified breast tumors, adjuvant treatment with Nolvadex significantly reduces disease recurrence and increases life expectancy by up to 10 years. A more pronounced effect is obtained with five years of treatment than with 1 or 2 years of treatment and does not depend on age, menopausal status, tamoxifen dose or adjuvant chemotherapy.
In about 10-20% of postmenopausal women, Nolvadex causes a decrease in the concentration of total cholesterol and low density lipoproteins in the blood plasma. In addition, reports show that in postmenopausal women, Nolvadex retains bone mineral density.
The variation in the clinical response to Nolvadex use may be associated with polymorphism of the CYP2D6 isoenzyme. A low metabolic rate may be associated with a reduced therapeutic response. No recommendations have been developed for the treatment of “poor” metabolizers of the CYP2D6 isoenzyme with Nolvadex .
Elimination of Nolvadex from the body is biphasic with an initial half-life of 7-14 hours followed by a slow terminal half-life of 7 days. It is excreted mainly in the form of conjugates, mainly by the intestines, and only small amounts are excreted by the kidneys.
Indications of Nolvadex for women
Indications:
- Adjuvant treatment of estrogen-positive early breast cancer;
- The treatment of locally advanced or metastatic estrogen receptor positive breast cancer;
- Breast cancer;
- The drug can also be used in other solid tumors that are resistant to standard therapies in the presence of estrogen receptor overexpression.
The drug may reduce the risk of breast cancer in women. It should be taken:
- Women who are at high risk of developing breast cancer due to a family history of the disease or mutations (changes) in the breast cancer genes (BRCA).
- Women who have already been diagnosed with breast cancer to prevent the cancer from coming back (return), including: Development of breast cancer in the untreated opposite breast.
How effective is Nolvadex ?
Millions of people have used Nolvadex to prevent or treat breast cancer. The drug can reduce the risk of developing:
- breast cancer in the opposite breast by 50%;
- recurrence of breast cancer in premenopausal women ranges from 30% to 50%;
- recurrence of breast cancer in postmenopausal women varies from 40% to 50%;
- primary diagnosis of breast cancer – up to 40%;
- invasive breast cancer after diagnosis of non-invasive early stage breast cancer (ductal carcinoma in situ or DCIS) up to 50%.
In addition to reducing the risk of breast cancer and cancer recurrence, Nolvadex:
- prevents bone loss after menopause;
- lowers cholesterol levels.
Pregnancy and lactation:
The use of Nolvadex Geksal during pregnancy is contraindicated. Spontaneous abortions, birth defects and fetal deaths have been reported in women taking tamoxifen during pregnancy, although a causal relationship has not been established.
Breast-feeding is not possible during treatment with Nolvadex as it inhibits breast-feeding at 20 mg twice a week. When Nolvadex is stopped, milk production does not begin for several months due to the preservation of the therapeutic effect of the drug. It is not known whether tamoxifen is excreted in human milk. Therefore, if treatment with Nolvadex Geksal is necessary during breast-feeding, the question of stopping breast-feeding should be considered.
Dosage of Nolvadex for women
The dosing regimen is usually set individually depending on the indications. The maximum daily dose is 40 mg. The standard dose is 20 mg Nolvadex . With the appearance of signs of disease progression, the drug is canceled. The duration of treatment depends on the severity of the disease, usually long-term treatment is required. As an adjuvant treatment in women with breast cancer, the recommended duration of treatment with tamoxifen is approx. 5 years.
The standard dose for adults is 20 mg. In the case of a common form of the disease, the dose may be increased to 30-40 mg / day.
The maximum daily dose is 40 mg. An objective response is usually observed after 4-10 weeks of treatment, but in the case of detection of bone metastases, the therapeutic effect can only be observed after several months of ingestion of the drug.
The tablets should be taken without chewing, with a small amount of liquid, in a single dose in the morning or, by dividing the required dose into two doses, in the morning and in the evening.
Most people take Nolvadex or other hormone therapy for at least five years, and sometimes up to 10 years. The duration of treatment depends on the individual characteristics of the cancer.
The duration of treatment is determined by the severity and course of the disease. As a rule, the treatment is long, lasts until remission is achieved.No dose adjustment is required in elderly patients, patients with renal or hepatic impairment.