Tamoxifen tumor control. Antiestrogen. Blocks estrogen receptors and thus inhibits the progression of tumor disease stimulated by estrogens. Tamoxifene is a non-steroidal anti-estrogenic agent with weak estrogenic properties. Its action is based on the ability to block estrogen receptors.
Tamoxifene and some of its metabolites compete with estradiol for binding sites with cytoplasmic estrogen receptors in breast, uterus, vagina, anterior pituitary gland and tumors with high estrogen receptor content. In contrast to the estrogen receptor complex, the tamoxifene receptor complex does not stimulate DNA synthesis in the nucleus, but suppresses cell division, which leads to regression.
Tamoxifen is used when breast cancer in women in menopause, breast cancer in men after castration, kidney cancer, melanoma (containing estrogen receptors), ovarian cancer, prostate cancer when resistant to other drugs.
Tamoxifen refers to non-steroidal antitumor and anti-estrogenic agents. It slows down the activity of peripheral estrogenic neurons located in target cells and developing malignant formations in them. Chemical product contributes to the formation of a complex of transfer cofactor, which is transmitted to the nuclear part of the cell and prevents its uncontrolled growth. The material was first obtained in the early 1970s. It became a discovery among antiestrogenic drugs included in the group of selective modulators of estrogen neurons. The antigonadotropic effect of the drug is to suppress the secretion of gonadotropic hormone compounds by the pituitary glanders. As a result, the synthesis of prostaglandins and tumor cells, which are activated by estrogens, is inhibited. A single daily dose of the drug is enough to stop the negative influence of estrogen for several weeks. Due to the secretion of gonadotropic hormonal substances by the pituitary glanders, ovulation begins in women, if it was previously absent. At the reduced density of sperm in the seminal fluid in men, the drug causes an increase in the density of male and female hormones, as well as luteinizing hormone. The drug and some of its decomposition products demonstrate the quality of strong inhibitors - oxidase with mixed hepatobiliary system cytochrome structure. However, the clinical significance of these effects has not been established. Sometimes Tamoxifen is also active in neoplasms that do not depend on estrogen functioning. The chemical material has a weak influence similar to the action of female hormones on the fat spectrum of blood substance plasma, endometrial tissue and bones. Absorption of the substance is sufficiently high and maximum after its introduction through the mouth reaches within 4-7 hours. Stable concentration in plasma is formed after a month of treatment at a daily dose corresponding to 40 mg. The drug binds almost completely to highly concentrated blood proteins. The reaction of metabolism occurs through the formation of two-atomic alcohols, acetylation of N-oxides on the basis of biosynthetic process of conjugation, characterized by the addition of a number of chemical groups to the medicinal material or its decomposition products. Decomposition products are derived in two stages, mainly with faeces and in small amounts through the urinary system. In the first stage the half-life period is 7-14 hours, in the second stage it is about a week.
Tamoxifen's treatment regimen is established for each patient individually, taking into account the data of the tests. In breast cancer, the daily rate is 20-40 mg. The medication is taken immediately, or distributed to two sessions in the morning or evening. The dosage of the pharmacy in case of endometrial tumor should not exceed 30 mg with single or double administration during the day. Treatment with the use of the chemical preparation is long enough and is carried out until the symptoms of the disease disappear. The aim of the therapy is to maintain a positive effect on the condition that the drug is constantly administered. If necessary, the chemical product is prescribed as an additional means of radiation exposure or in combination with cytostatics. The daily dose of the material taken should not exceed 40 mg. Pills are swallowed in their entirety, not chewed. You can drink a small amount of water. If you take the medicine once in the morning, it is advisable to use it. In the case of anabolic androgenic steroids, Tamoxifen is used starting from the second week of the steroid series. This is due to an increase in estrogen levels at the end of the first seven days of anabolic use. Sometimes it is recommended to administer the drug until the next cycle.
As a result of the combination of the drug with indirect anticoagulant medications there is an increase in the effect of the latter. This requires constant monitoring of the patient's health in order to correct the dosage of anticoagulants in time. In the case of Tamoxifen tablets in combination with letrozol there is a decrease in its density in the plasma blood environment. Cytostatic pharmaceuticals used in conjunction with the drug in question increase the likelihood of clogging of blood vessels with blood clots. In combination with tegafur it is possible to form cirrhosis of liver tissue with subsequent formation of hepatitis symptoms. When administered together with chemicals containing female estrogen hormones, such as contraceptives, the efficacy of both drugs is weakened. Pharmaceutical products that reduce the amount of calcium cations removed, such as thiazid diuretics, increase the risk of developing an increased calcium content in the blood substance. Complex administration of Bromocriptine and Tamoxifene leads to an increase in the density of the latter in serum blood. Means used to reduce gastric secretion acidity, which include antacids and antihistamines, provokes the early dissolution of the tread surface of capsules. The membrane should retain its protective function until the drug enters the intestinal tract. For this reason, antiestrogenic pills and antacids should not be used for at least one hour.