Arimidex: Advanced Estrogen Control for Breast Cancer Treatment
Arimidex
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| 90 | $4.90
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Synonyms | |||
Arimidex (anastrozole) represents a significant advancement in hormonal therapy for postmenopausal women with hormone receptor-positive breast cancer. As a third-generation aromatase inhibitor, it offers targeted estrogen suppression through a well-tolerated oral formulation. This non-steroidal agent demonstrates superior efficacy compared to earlier hormonal therapies while maintaining a favorable safety profile. Clinical evidence supports its use across multiple treatment settings, from adjuvant therapy to metastatic disease management.
Features
- Contains 1 mg anastrozole per tablet
- Non-steroidal aromatase inhibitor classification
- Oral administration with once-daily dosing
- Bioavailability of approximately 80% when taken fasting
- Plasma protein binding of approximately 40%
- Elimination half-life of approximately 50 hours
- Metabolism primarily hepatic via N-dealkylation, hydroxylation, and glucuronidation
Benefits
- Significantly reduces recurrence risk in early breast cancer by suppressing estrogen production
- Demonstrates superior disease-free survival compared to tamoxifen in clinical trials
- Avoids estrogen receptor agonist effects associated with some anti-estrogen therapies
- Reduces risk of thromboembolic events compared to tamoxifen-based regimens
- Maintains bone mineral density better than other aromatase inhibitors through specific mechanism of action
- Offers convenient once-daily dosing that supports treatment adherence
Common use
Arimidex is primarily indicated for the adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer. It is also approved for the first-line treatment of postmenopausal women with hormone receptor-positive or hormone receptor unknown locally advanced or metastatic breast cancer. Additionally, it is used in the treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy. The medication may be prescribed as extended adjuvant therapy following initial tamoxifen treatment.
Dosage and direction
The recommended dosage is one 1 mg tablet taken orally once daily, with or without food. For adjuvant treatment of early breast cancer, the recommended duration of treatment is 5 years. Patients should take the medication at approximately the same time each day to maintain consistent drug levels. Tablets should be swallowed whole with water and not crushed or chewed. Treatment should continue until tumor progression is documented in the metastatic setting. Dosage adjustment is not necessary for patients with mild to moderate hepatic impairment or renal impairment.
Precautions
Patients should undergo comprehensive bone mineral density assessment before initiating therapy and at regular intervals during treatment due to potential bone density loss. Regular monitoring of lipid profiles is recommended as aromatase inhibitors may alter lipid metabolism. Hepatic function should be assessed periodically, although dosage adjustment is not typically required for mild to moderate impairment. Patients should be advised about potential effects on cholesterol levels and cardiovascular health. Caution is advised in patients with pre-existing osteoporosis or risk factors for bone loss. Vitamin D and calcium supplementation should be considered as preventive measures.
Contraindications
Arimidex is contraindicated in women with known hypersensitivity to anastrozole or any components of the formulation. It must not be used in premenopausal women, pregnant women, or during breastfeeding. The medication is contraindicated in patients with severe hepatic impairment (Child-Pugh class C). Concomitant use with estrogen-containing therapies is contraindicated as these agents would counteract the therapeutic effect. Patients with known severe renal impairment (creatinine clearance <30 mL/min) should not receive this medication without careful risk-benefit assessment.
Possible side effects
Common adverse reactions (≥10%) include hot flashes, asthenia, arthritis, pain, arthralgia, hypertension, depression, nausea and vomiting, rash, osteoporosis, bone fractures, back pain, insomnia, headache, and peripheral edema. Less frequent side effects (1-10%) include peripheral thromboembolic events, vaginal dryness, weight increase, hypercholesterolemia, and carpal tunnel syndrome. Rare but serious adverse events (<1%) may include ischemic cardiovascular events, hepatic enzyme abnormalities, and severe cutaneous reactions. Most side effects are mild to moderate in severity and often diminish with continued therapy.
Drug interaction
Arimidex may interact with estrogen-containing medications, which would antagonize its pharmacological effects. Tamoxifen co-administration reduces anastrozole plasma concentrations by approximately 27% and should be avoided. Medications that induce CYP3A4 may decrease anastrozole concentrations, though clinical significance remains uncertain. No clinically significant interactions have been observed with warfarin, cimetidine, or other commonly co-administered medications. Caution is advised with strong CYP3A4 inducers such as rifampicin, phenytoin, and carbamazepine.
Missed dose
If a dose is missed, patients should take it 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 take double doses to make up for a missed dose. The long half-life of anastrozole (approximately 50 hours) provides some buffer against temporary fluctuations in plasma concentrations. Consistently missed doses should be discussed with the healthcare provider to assess potential impact on treatment efficacy.
Overdose
There is no specific antidote for anastrozole overdose. Single doses up to 60 mg have been administered without serious adverse effects. Expected manifestations would likely include an exaggeration of known side effects, particularly hormonal effects and possibly neurological symptoms. Management should involve supportive care and symptomatic treatment. Gastric lavage may be considered if ingestion occurred within a short time frame. Vital signs should be monitored, and appropriate supportive measures implemented based on clinical presentation. Dialysis is unlikely to be beneficial due to high protein binding.
Storage
Store at room temperature between 20°C to 25°C (68°F to 77°F) with excursions permitted between 15°C to 30°C (59°F to 86°F). Keep the medication in its original container with the lid tightly closed to protect from moisture and light. Do not store in bathroom areas where moisture levels fluctuate. Keep out of reach of children and pets. Do not use tablets that appear discolored, damaged, or beyond the expiration date printed on the packaging. 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 familiar with the patient’s complete medical history. The prescribing physician should be consulted regarding specific dosing, duration, and monitoring requirements. Individual responses to therapy may vary, and not all potential side effects or interactions are described here. Patients should report any unusual symptoms or concerns to their healthcare provider promptly.
Reviews
Clinical trials demonstrate Arimidex significantly improves disease-free survival compared to tamoxifen, with a 17% reduction in recurrence risk (ATAC trial). The BIG 1-98 trial confirmed superior efficacy in both disease-free and overall survival metrics. Patients generally report acceptable quality of life during treatment, though management of arthralgia and bone health requires attention. Long-term follow-up data show maintained efficacy benefits with appropriate supportive care. Many oncologists consider it a cornerstone of hormonal therapy for appropriate patient populations based on robust clinical evidence spanning over two decades of use.