Nolvadex is a drug used to treat breast cancer, breast cancer, kidney cancer, melanoma and soft tissue sarcoma.
Pharmacological properties
Nolvadex (tamoxifen) is a non-steroidal anti-estrogen. Nolvadex acts as an antiestrogen that inhibits the effects of endogenous estrogen, probably through binding to estrogen receptors.
It is recognized that tamoxifen has estrogen-like effects on a number of body systems, including endometrium, bone and blood lipids.
After oral administration, Nolvadex is rapidly absorbed and peak serum concentrations are reached within 4-7 hours.
Steady-state concentrations (approximately 300 ng / ml) are achieved after four weeks of treatment with a daily dose of 40 mg. This drug binds well to serum albumin (> 99%). As a result of metabolism, in the process of hydroxylation, demethylation and conjugation, a number of metabolites are formed having pharmacological profile characteristics similar to the original chemical compound, which thus contributes to the therapeutic effect. Excretion occurs mainly through the feces. The half-life was approximately seven days for the drug itself and 14 days for X-desmethyltamoxifen, the major circulating metabolite.
Indications for use
Indications for taking Nolvadex include breast cancer in women and men, ovarian and prostate cancer, soft tissue cancer (melanoma, sarcoma), kidney cancer. In some cases, the drug is also prescribed for female infertility.
Side effects
With long-term treatment, side effects are less common or less severe with Nolvadex than with androgens and estrogens, which are also used to treat breast cancer.
These side effects can be classified as either due to antiastrogenic effects of the drug, such as hot flashes, vaginal bleeding, vaginal discharge and itching in the genital area, or as side effects of a more general nature, such as gastrointestinal intolerance, recurrence, tumor recurrence , skin rash, and in some cases, fluid retention and alopecia.
In the event of serious side effects, they can be controlled by simply reducing the dose while maintaining control over the course of the disease. Hypercalcaemia has been reported in a small number of patients with bone metastases during therapy.
Patients using Nolvadex for breast cancer have usually had a decrease in platelet count to 80,000 to 90,000 per cubic mm, and sometimes lower. Vision disorders, including rare cases of corneal changes, cataracts, and retinopathy, have been reported in a number of patients taking Nolvadex.
Interaction with other means
Enhances the effect of anticoagulants of indirect action (requires careful monitoring to adjust the dose of anticoagulants). Cytostatics increase the risk of thrombosis. Allopurinol promotes the development of hepatotoxic effects. Co-administration of tamoxifen and tegafur may cause active chronic hepatitis and liver cirrhosis. Concomitant use of tamoxifen with other hormonal drugs (especially estrogen-containing contraceptives) leads to a weakening of the specific action of both drugs. Drugs that reduce Ca2 + excretion (eg, thiazide diuretics) may increase the risk of developing hypercalcaemia.
Antacids, blockers of H2-histamine receptors, etc. 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 tamoxifen and these drugs should be 1-2 hours.
