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Nolvadex

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Nolvadex (tamoxifen) is a nonsteroidal antiestrogen used to treat breast cancer and prevent breast cancer in women at high risk of developing it.

Indications

The drug is used in the treatment of hormone-dependent breast tumors in women and mammary glands in men. It is effective in the treatment of cancer of the ovaries, endometrium, kidneys, tissue sarcoma, as well as in the presence of prostate cancer.

How does it work?

Tamoxifen is an antitumor, antiestrogen substance. It competitively binds to estrogen receptors in target organs, translocates together with the receptor into the nucleus of a tumor cell and thus blocks the action of estrogen.

Dosage and administration

Nolvadex is administered orally with water.

The standard dose for adults is 20 mg. With a common form of the disease, the dose can be increased to 30-40 mg/day.

The maximum daily dose is 40 mg. Objective response is usually observed after 4-10 weeks of therapy, however, if metastases in the bones are detected, the therapeutic effect can be observed only after several months of taking the drug.

The duration of treatment is determined by the severity, course of the disease. As a rule, treatment is long, lasting until remission is achieved.

There is no need for dose adjustment in elderly patients, patients with impaired renal or hepatic function.

Side effects

  • Sexual disorders: abnormal vaginal bleeding, hot flashes, menstrual irregularities, genital itching, vaginal discharge, reversible cystic ovarian edema, loss of libido, impotence in men, 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;
  • Hematologic disorders: leukopenia, thrombocytopenia, neutropenia, pancytopenia, thrombosis, pulmonary thromboembolism;
  • Ophthalmic disorders: decreased visual acuity, cataracts, 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 increase in existing skin lesions, or the appearance of new ones;
  • Others: transient acceleration of tumor growth, dizziness, fatigue, headache, taste disturbance, depression, leg muscle cramps, increased pain in bones, tumors.

Contraindications

Do not use Nolvadex if you have any of the following conditions:

  • Pregnancy and lactation;
  • A history of deep vein thrombosis and pulmonary embolism during treatment with indirect coumarin anticoagulants,
  • Thrombocytopenia,
  • Leukopenia,
  • Hypercalcemia,
  • Hyperlipidemia,
  • Cataracts,
  • Visual impairment.

Overdose

Theoretically, an overdose of tamoxifen can cause an increase in antiestrogenic side effects. Observations in animals indicate that excessive overdose (100-200 times higher than the recommended daily dose) can cause estrogenic effects. There is no specific antidote, treatment should be symptomatic.

Pregnancy and lactation

The drug should not be used during pregnancy. In pregnant women treated with tamoxifen, there have been isolated 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, it is important to ensure 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.

Drug interaction

Avoid taking Nolvadex with any of the following drugs:

  • Coumarin derivatives with anticoagulants;
  • Allopurinol;
  • Bromocriptine;
  • Warfarin;
  • Mitomycin;
  • Rifampicin;
  • Estrogens.

Precautions

Before treatment, women should undergo a thorough gynecological examination. Nolvadex causes ovulation, which increases the risk of pregnancy, so women of reproductive age need to use reliable methods of contraception (non-hormonal) during the treatment period and within 3 months after the end of treatment.

Treatment with this drug should be stopped when there are spotting from the vagina or vaginal bleeding, signs of vein thrombosis of the lower extremities (leg pain or swelling), shortness of breath.

In the process of treatment, you should monitor blood coagulation indices, blood patterns (leukocytes, platelets), and liver function indices. Before and periodically during treatment, an ophthalmic examination is recommended.

In patients with bone metastases, it is necessary to monitor the concentration of calcium in the blood serum (in case of severe hypercalcemia, tamoxifen therapy should be temporarily stopped). In patients with hyperlipidemia, it is necessary to control the concentration of cholesterol and TG in the blood serum.

The drug is ineffective in the treatment of patients with metastases (especially in the liver).