NOLVADEX ® is a drug based on Tamoxifen citrate
THERAPEUTIC GROUP: Antiestrogens – hormonal antagonists and related substances
Indications NOLVADEX ® – Tamoxifen
NOLVADEX ® is a selective anti-estrogenic drug used in the treatment of breast cancer and recently re-evaluated for the short-term treatment of anovulatory female infertility.
Mechanism of action NOLVADEX ® – Tamoxifen
Tamoxifen, the active ingredient of NOLVADEX ® is a derivative of triphenylethylene, also a precursor of the most used clomiphene citrate, characterized by an important selective pharmacological activity, which makes it one of the most used drugs in the treatment of estrogen-dependent breast carcinoma.
The aforementioned active principle, in fact, once taken orally and absorbed at the intestinal level, by binding to the plasma albumin, reaches the various tissues competing with estrogens for binding to the estrogenic receptor.
In this way tamoxifen can bind the overexpressed estrogen receptors in breast cancer, thus preventing estrogen from exerting its trophic and proliferative effect on the neoplastic cells of estrogen dependent carcinoma of the breast.
Recent evidence has shown that tamoxifen can reduce blood levels of total cholesterol, especially LDL, while preserving bone mineral density, thus protecting against cardiovascular and osteoporotic diseases.
The complex biological activity of this drug is still the subject of numerous studies, whose intent is to better characterize its molecular mechanism of action.
Studies carried out and clinical efficacy
1. TAMOXIFENE: AN ALTERNATIVE ALTERNATIVE TO CLOMIFENE IN RESISTANT WOMEN
Hum Reprod Sci. 2011 May; 4 (2): 76 – 9.
Tamoxifen: An alternative to clomiphene in women with polycystic ovary syndrome.
Dhaliwal LK, Suri V, Gupta KR, Sahdev S.
Study demonstrating how tamoxifen can be effective at a dose of 40 mg per day in inducing ovulation in women with polycystic ovary syndrome and resistant to clomiphene citrate.
2. TAMOXIFENE AND TROMBOEMBOLIC EVENTS
Clin Med Res. 2011 Nov; 9 (3 – 4): 150.
C – b2 – 02: epidemiology of tamoxifen and thromboembolism.
Onitilo A, Engel J, Berg R.
Epidemiological work demonstrating how the use of tamoxifen may correlate with the increased incidence of thromboembolic episodes. These episodes were observed in 5% of women under 45 years of age, 7% between 45-54 years, 14% between 55-64 years, 19% between 65-74 years, 27% in patients older than 74 years.
3. THE ANTIFIBROTIC EFFECTS OF TAMOXIFENE
J Am Soc Nephrol. 2011 Nov 3.
Antifibrotic Effect of Tamoxifen in a Model of Progressive Renal Disease.
Dellê H, Rocha JR, Cavaglieri RC, Vieira JM Jr, Malheiros DM, Noronha IL.
Experimental study demonstrating how tamoxifen can inhibit renal fibrosis in models of nephrosclerosis, probably modulating the secretion of pro-fibrotic factors such as TGF beta.
Method of use and dosage
Tablets coated with 10 – 20 mg tamoxifen citrate film: em>
the dosage, usually between 20 and 40 mg daily, taken in one or two administration, must necessarily be defined by your doctor, who must supervise the whole therapeutic process and the effectiveness of the treatment.
NOLVADEX ® warnings – Tamoxifen
In order for NOLVADEX ® therapy to express maximum therapeutic efficacy without compromising the patient’s state of health, with potentially dangerous side effects, it should be preceded by a careful medical examination to assess the appropriateness of prescription and the absence of conditions incompatible with tamoxifen intake.
In this regard it is important that the doctor informs the patient of the potential side effects of the therapy and of the main signs with which they occur, in order to be recognized promptly.
Furthermore, medical supervision becomes fundamental both to ascertain the patient’s state of health and the efficacy of tamoxifen therapy.
NOLVADEX ® contains lactose and is therefore contraindicated in patients with galactose intolerance, enzyme lactase deficiency or glucose – galactose malabsorption.
The appearance of side effects on the visual apparatus, fogging and opacification, could make driving of cars or the use of machinery dangerous.
Although there are conflicting data in the literature concerning the safety profile of tamoxifen when taken during pregnancy, the numerous experimental data showing effects on the fetus similar to those induced by estrogens or clomiphene allow to extend the contraindications also to tamoxifen.
These contraindications also apply to the subsequent breastfeeding phase.
The hepatic metabolism to which tamoxifen is subjected exposes the patient to clinically relevant pharmacological interactions.
In fact the efficacy of the treatment and the incidence of its side effects, could be significantly changed by the simultaneous intake of modulators of CYP3A4, enzyme responsible for the metabolism of tamoxifen.
Furthermore, the concomitant use of dicumarinic anticoagulants could be accentuated by tamoxifen, thus requiring periodic supervision of coagulation indices.
Statistically, the incidence of thromboembolic episodes was higher in patients receiving tamoxifen and cytotoxic drugs.
Contraindications NOLVADEX ® – Tamoxifen
The use of NOLVADEX ® is contraindicated in case of hypersensitivity to the active substance or to one of its excipients, pregnancy and lactation, as preventive therapy of breast cancer, or in patients with ductal carcinoma in situ or with anticoagulant therapy in act.
Undesirable effects – Side effects
Long-term therapy, necessary for the treatment of breast cancer, exposes the patient to numerous side effects related to tamoxifen intake.
More precisely, hot flashes, vaginal blood loss, skin rash, dermatitis, hydro-saline retention, dizziness, visual disturbances, lower limb cramps, volumetric increase of ovarian cysts, hepatic steatosis and hepatic failure represent the most adverse reactions frequently observed during therapy with NOLVADEX ®.
However, the most worrying ones, taking on particular importance from the clinical point of view, are linked to the greater incidence of thromboembolic embolic events and malignant diseases, mainly concentrated in the uterine and endometrial sites.
NOLVADEX ® can only be sold under medical prescription.
The use of NOLVADEX ® outside of the prescription before and during a sports competition is prohibited by constituting doping practice
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