NOLVADEX ® is a Tamoxifen citrate based drug
THERAPEUTIC GROUP: Antiestrogens - hormonal antagonists and related substances
Indications NOLVADEX ® - Tamoxifen
NOLVADEX ® is a selective antiestrogenic drug used in the treatment of breast cancer and recently re-evaluated also 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, a precursor of the more widely 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 cancer.
In fact, the aforesaid active principle, once taken orally and absorbed in the intestine, by binding to plasma albumin, reaches the various tissues competing with estrogens for binding to the estrogen receptor.
In this way, tamoxifen can bind overexpressed estrogen receptors in breast cancer, thus preventing estrogen from exerting its trophic and proliferative effect on the neoplastic cells of estrogen-dependent breast cancer.
Recent evidence has shown how tamoxifen can reduce blood levels of total cholesterol, and in particular LDL, while preserving the maintenance of bone mineral density, thus being protective against cardiovascular and osteoporotic diseases.
The complex biological activity of this drug is still the subject of numerous studies, the aim of which is to better characterize its molecular mechanism of action.
Studies carried out and clinical efficacy
1. TAMOXIFEN: A VALID ALTERNATIVE TO CLOMIPHENE IN RESISTANT WOMEN
Hum Reprod Sci. 2011 May; 4: 76-9.
Tamoxifen: An alternative to clomiphene in women with polycystic ovary syndrome.
Dhaliwal LK, Suri V, Gupta KR, Sahdev S.
Study showing 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. TAMOXIFEN AND THROMBOEMBOLIC 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 that demonstrates how the use of tamoxifen can be correlated with the increased incidence of thromboembolic episodes. These episodes were observed in 5% of women undergoing treatment under the age of 45, 7% between 45 - 54 years, 14% between 55 - 64 years, 19% between 65 - 74 years, 27% in patients over the age of 74 years old.
3. THE ANTIFIBROTIC EFFECTS OF TAMOXIFEN
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 nephrosclerosis models, probably by modulating the secretion of pro-fibrotic factors such as TGF beta.
Method of use and dosage
NOLVADEX ®
Tamoxifen citrate 10 - 20 mg film-coated tablets:
the dosage, usually between 20 and 40 mg per day, taken in one or two administrations, must necessarily be defined by your doctor, who must supervise the entire therapeutic process and the effectiveness of the treatment.
Warnings NOLVADEX ® - Tamoxifen
In order for the therapy with NOLVADEX ® to express the 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 useful to evaluate the prescribing appropriateness and the absence of conditions incompatible with taking tamoxifen.
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, so that they can be recognized promptly.
In addition, medical supervision becomes essential both to ascertain the patient's state of health and the efficacy of tamoxifen therapy.
NOLVADEX ® contains lactose therefore it is contraindicated in patients with galactose intolerance, lactase enzyme deficiency or glucose-galactose malabsorption.
The appearance of side effects on the visual apparatus, clouding and opacification, could make driving vehicles or using machines dangerous.
PREGNANCY AND BREASTFEEDING
Although there are conflicting data in the literature regarding the safety profile of tamoxifen when taken during pregnancy, the numerous experimental data showing effects on the fetus similar to those induced by estrogen or clomiphene allow to extend the contraindications to tamoxifen as well.
These contraindications also apply to the subsequent breastfeeding phase.
Interactions
The hepatic metabolism to which tamoxifen is subjected exposes the patient to clinically relevant drug 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, an enzyme responsible for the metabolism of tamoxifen.
Furthermore, the concomitant intake of dicumarin anticoagulants could be accentuated by tamoxifen, thus requiring periodic supervision of coagulation indices.
Statistically, the incidence of thrombo-embolic episodes was higher in patients undergoing therapy with 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 a preventive therapy for breast cancer, or in patients with ductal carcinoma in situ or with anticoagulant therapy in progress.
Undesirable Effects - Side Effects
Long-term therapy, necessary for the treatment of breast cancer, exposes the patient to numerous side effects related to taking tamoxifen.
More precisely, hot flashes, vaginal bleeding, skin rash, dermatitis, hydro-saline retention, dizziness, visual disturbances, cramps in the lower limbs, volumetric increase in ovarian cysts, fatty liver and liver failure are the most frequently observed adverse reactions in progress. of therapy with NOLVADEX ®.
However, those of greatest concern, assuming particular importance from a clinical point of view, are linked to the higher incidence of developing thrombo-embolic events and malignant diseases concentrated above all in the uterine and endometrial areas.
Note
NOLVADEX ® can only be sold under medical prescription.
The use of NOLVADEX ® outside the medical prescription, before and during a sports competition is prohibited as it constitutes a doping practice
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