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Nolvadex is a means to block the action of female sex hormones – estrogen. This preparation belongs to a non-steroidal estrogen antagonist. It can manifest itself as a complete or partial estrogen agonist (depending on the target tissue). Antiestrogenic activity is explained by binding to the hormone-binding domain of estrogen receptors.
- Mammary gland cancer;
- Breast cancer in men;
- Prostate cancer;
- Skin cancer;
- Ovarian cancer;
- Female infertility.
Dosage and administration
Usually, the dose is set individually depending on the indications. Oral administration. If breast and kidney cancer diagnosed, 20-40 mg 1-2 times a day (morning and evening), endometrium 20-30 mg 1-2 times a day. The course dosage is 2.4-9.6 g. Treatment is carried out for a long time (until symptoms of disease progression appear) because the effect is preserved only on the background of continuous use. If necessary, this drug can be used in combination with radiation and cytostatic therapy.
Tablets should be taken as a whole, washed down with a small amount of water. Take one dose in the morning or divide the required dose into 2 doses (in the morning and evening).
Mechanism of action
Generic Nolvadex is an antitumor antiestrogenic agent. It competitively inhibits estrogen receptors in target organs and tumors. The result is a complex, which, after translocation to the cell nucleus, prevents hypertrophy of cells dependent on estrogen regulation. It has antigonadotropic properties, inhibits the synthesis of Pg in tumor tissue. It inhibits the progression of the tumor process stimulated by estrogen.
The ability to block estrogens may persist for several weeks after a single dose.
In addition, it can cause ovulation in women in its absence, stimulating the release of the hypothalamus, stimulating the release of the pituitary gonadotropin hormones. In men with oligospermia, it increases the concentration of LH and FSH, testosterone and estrogen in the blood serum. The drug and some of its metabolites are strong oxidase inhibitors of the mixed-function of the liver cytochrome P450 system. However, the clinical significance of these effects has not been determined.
- Pregnancy and lactation;
- Idiosyncrasy to the drug components.
- Sexual disorders: abnormal vaginal bleeding, hot flashes, menstrual irregularities, genital itching, vaginal discharge, reversible cystic ovarian edema, loss of libido, impotence, cessation of menstruation in premenopausal women, proliferative changes in the endometrium (endometrial hyperplasia, endometriosis, polyps, endometrial cancer).
- Metabolic disorders: anorexia, fluid retention in the body, hypercalcemia (with bone metastases), hypertriglyceridemia.
- Hematological disorders: leukopenia, thrombocytopenia, neutropenia, pancytopenia, thrombosis, pulmonary thromboembolism.Ophthalmic disorders: decreased visual acuity, cataract development, corneal opacity, retinopathy.
- Immune disorders: hypersensitivity reactions, incl. rash, polymorphic erythema, bullous pemphigoid, angioedema, Stevens-Johnson syndrome.
- Digestive disorders: nausea, constipation, vomiting, diarrhea, pancreatitis, elevated liver enzymes, fatty liver, hepatitis, cholestasis.
- Dermatological disorders: skin rash, intense hair growth or alopecia, the spread of erythema around skin lesions, an exacerbation in existing skin lesions, or the appearance of new ones.
- Other: transient acceleration of tumor growth, dizziness, fatigue, headache, taste disturbance, depression, leg muscle cramps, increased pain in bones, tumors.
Do not exceed the recommended dose. Excessive use of the drug will not alleviate your condition, and can also cause poisoning and severe side effects. If you observe an overdose of Nolvadex, contact the emergency services. Be sure to bring along the packaging, container or name of the drug to facilitate diagnosis.
- Taking the drug enhances the effect of indirect anticoagulants (requires careful monitoring to adjust the dose of anticoagulants).
- Cytostatics increase the risk of thrombosis.
- Allopurinol promotes the development of hepatotoxic effects.
- The combined use of the drug and tegafur can cause active chronic hepatitis and cirrhosis.
- The simultaneous use of other hormonal drugs (especially estrogen-containing contraceptives) results in a weakening of the specific effect of both drugs.
- Drugs that reduce Ca2 + excretion (e.g. thiazide-type diuretics) may increase the risk of hypercalcemia.
- Antacids, H2-histamine receptor blockers, and other drugs that reduce the acidity of gastric juice can cause premature dissolution and loss of the protective effect of enteric tablets. The interval between taking Nolvadex and these drugs should be 1-2 hours.
Pregnancy and lactation
- The drug should not be used during pregnancy. In pregnant women treated with tamoxifen, there have been underlined cases of spontaneous miscarriage, birth defects, fetal death, but the relationship of these phenomena with tamoxifen has not been established. A study of reproductive toxicity in animals did not reveal teratogenic effects.
- A study of intrauterine development in animals showed that drug therapy is associated with changes similar to the effects of estradiol, ethinyl estradiol, clomiphene, diethylstilbestrol.
- Before starting therapy, you must make sure that the patient is not pregnant. During the entire period of therapy and at least 3 months after its completion, contraceptive agents must be used.
- Do not use oral contraceptives.
- It is not known whether the drug is excreted in breast milk, so breastfeeding is stopped during the treatment period.
During treatment, Nolvadex should regularly monitor the level of platelets and calcium in the blood. Prolonged use of the drug should be accompanied by a consultation with an oculist. During treatment, it is not recommended to perform work requiring an increased concentration of attention. It should not be combined with drugs containing hormones, especially estrogens. When administered concomitantly with drugs that affect the blood coagulation system, dose adjustment of Nolvadex is necessary. When combined with other oncological drugs, the risk of thrombosis increases.