Nolvadex: Advanced Estrogen Receptor Modulation for Breast Health
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Synonyms
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Nolvadex, with its active ingredient tamoxifen citrate, represents a cornerstone in endocrine therapy for hormone receptor-positive breast cancer. As a selective estrogen receptor modulator (SERM), it operates by competitively blocking estrogen receptors in breast tissue, thereby inhibiting the proliferation of cancer cells that are dependent on estrogen for growth. Its well-established efficacy profile and extensive clinical history make it a first-line option for both treatment and risk reduction in appropriate patient populations. This expert guide details the critical medical information required for its informed use.
Features
- Active Ingredient: Tamoxifen citrate
- Therapeutic Class: Selective Estrogen Receptor Modulator (SERM)
- Available Formulations: 10 mg and 20 mg oral tablets
- Bioavailability: High oral bioavailability with peak plasma concentrations reached within 4-7 hours post-administration
- Metabolism: Primarily hepatic, via CYP2D6 and CYP3A4 isoenzymes, into active metabolites such as endoxifen
- Half-life: Approximately 5-7 days for tamoxifen and its active metabolites, allowing for once or twice daily dosing regimens
- Mechanism of Action: Competitively antagonizes estrogen receptors in breast tissue while acting as a partial agonist in other tissues such as bone and endometrium
Benefits
- Significantly reduces the risk of recurrence in early-stage, hormone receptor-positive breast cancer following primary treatment
- Lowers the incidence of contralateral breast cancer in patients treated for primary breast malignancy
- Demonstrated efficacy in reducing the risk of invasive breast cancer in high-risk populations, such as those with BRCA mutations or strong family history
- Provides bone-protective effects in premenopausal women by exhibiting estrogen-agonist activity on bone tissue, helping maintain bone mineral density
- Serves as an effective treatment for metastatic breast cancer in both pre- and post-menopausal women with estrogen receptor-positive disease
- Offers a well-tolerated oral administration option compared to some injectable hormonal therapies
Common use
Nolvadex is primarily indicated for the treatment of hormone receptor-positive breast cancer in women. This includes adjuvant treatment following surgery and radiation for early-stage disease, treatment of advanced or metastatic breast cancer, and as a preventive measure in women at high risk of developing breast cancer. It is also used off-label for the treatment of other conditions such as gynecomastia in men and infertility in women with anovulatory disorders, though these uses require careful specialist supervision.
Dosage and direction
The standard dosage for breast cancer treatment is 20 mg once daily, though doses may range from 20-40 mg daily based on disease stage and individual patient factors. For risk reduction in high-risk patients, the recommended dose is 20 mg daily for 5 years. Tablets should be taken with water, with or without food, at approximately the same time each day to maintain steady state concentrations. Treatment duration typically spans 5-10 years based on individual risk assessment and clinical response. Dosage adjustments may be necessary in patients with hepatic impairment or those experiencing significant side effects.
Precautions
Patients should undergo comprehensive baseline assessment including endometrial evaluation before initiation and regularly during treatment due to increased risk of endometrial changes. Regular ophthalmological examinations are recommended as tamoxifen use has been associated with ocular toxicity including cataracts and retinopathy. Liver function tests should be monitored periodically as hepatotoxicity, though rare, can occur. Blood lipid profiles should be assessed as tamoxifen may alter lipid metabolism. Patients should be advised about the potential for increased risk of thromboembolic events, particularly during periods of immobilization. Pre-menopausal women should use non-hormonal contraception during treatment as tamoxifen may cause fetal harm.
Contraindications
Nolvadex is contraindicated in patients with known hypersensitivity to tamoxifen citrate or any component of the formulation. It should not be used concomitantly with warfarin or other coumarin-derived anticoagulants except under strict monitoring due to potentiation of anticoagulant effect. Contraindicated in patients with history of deep vein thrombosis or pulmonary embolism. Should not be used during pregnancy or in women who may become pregnant due to potential teratogenic effects. Not recommended for use in patients with pre-existing endometrial cancer or atypical endometrial hyperplasia.
Possible side effect
Common side effects (≥10% incidence) include hot flashes, vaginal discharge or dryness, nausea, fatigue, and mood changes. Less frequent effects (1-10%) may include endometrial changes, visual disturbances, skin rash, and headache. Serious but rare (<1%) adverse reactions include venous thromboembolism, stroke, endometrial cancer, hepatic necrosis, and neutropenia. Many side effects are dose-dependent and may diminish with continued therapy or dose adjustment. Patients should report any unusual vaginal bleeding, visual changes, or signs of thromboembolism immediately.
Drug interaction
Nolvadex exhibits significant interactions with medications that affect CYP2D6 metabolism, particularly strong CYP2D6 inhibitors such as paroxetine, fluoxetine, and quinidine, which may reduce conversion to active metabolites and diminish efficacy. Drugs that induce CYP3A4 (rifampin, carbamazepine) may decrease tamoxifen concentrations. Warfarin and other anticoagulants require careful monitoring due to increased anticoagulant effect. Aromatase inhibitors should not be used concomitantly. Tamoxifen may reduce letrozole plasma concentrations when co-administered. Use with other hepatotoxic drugs may increase risk of liver injury.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed dose. Consistent daily administration is important for maintaining therapeutic effect, so patients should be advised to use reminder systems if forgetfulness is an issue.
Overdose
Acute overdose may manifest as tremor, hyperreflexia, unsteady gait, dizziness, and nausea. There is no specific antidote for tamoxifen overdose. Management should include supportive care with monitoring of vital signs and symptomatic treatment. Gastric lavage may be considered if presentation is early after ingestion. Activated charcoal may be administered. Due to the long half-life, extended monitoring may be necessary. Serious complications may include QT prolongation and seizures, requiring appropriate medical management.
Storage
Store at controlled room temperature (20-25°C or 68-77°F) in the original container, protected from light and moisture. Keep tightly closed and out of reach of children. Do not use if tablets show signs of discoloration or deterioration. Proper disposal of unused medication should follow local regulations for pharmaceutical waste.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made in consultation with a qualified healthcare professional who can assess individual patient circumstances. The prescribing physician should be consulted for specific dosage recommendations and treatment duration. Regular monitoring and follow-up are essential during therapy.
Reviews
Clinical studies consistently demonstrate Nolvadex’s efficacy in reducing breast cancer recurrence by approximately 40-50% in hormone receptor-positive disease. The NSABP P-1 trial showed a 49% reduction in invasive breast cancer incidence in high-risk women. Long-term follow-up data confirm sustained benefit with 10 years of therapy in certain populations. Patient-reported outcomes indicate generally good tolerability, though side effect management remains important for adherence. Real-world evidence supports its position as a fundamental component of breast cancer management strategies.