Arimidex: Advanced Aromatase Inhibition for Breast Cancer Treatment
Arimidex
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Synonyms | |||
Arimidex (anastrozole) represents a significant advancement in endocrine therapy for hormone receptor-positive breast cancer in postmenopausal women. As a third-generation aromatase inhibitor, it specifically targets the aromatase enzyme system responsible for estrogen production. This medication has demonstrated superior efficacy compared to traditional anti-estrogen therapies in multiple clinical trials, establishing itself as a cornerstone in both adjuvant and metastatic treatment settings. The selective mechanism of action minimizes estrogen synthesis without affecting other steroid hormone pathways, offering a targeted approach to hormone-sensitive malignancies.
Features
- Contains 1 mg of anastrozole per tablet
- Non-steroidal aromatase inhibitor classification
- High specificity for aromatase cytochrome P450 enzyme
- Oral administration with once-daily dosing
- Bioavailability of approximately 80% when taken fasting
- Plasma protein binding of approximately 40%
- Hepatic metabolism via N-dealkylation, hydroxylation, and glucuronidation
- Mean elimination half-life of approximately 50 hours in postmenopausal women
Benefits
- Significantly reduces circulating estrogen levels by up to 97% in postmenopausal women
- Demonstrates superior disease-free survival rates compared to tamoxifen in adjuvant therapy
- Reduces contralateral breast cancer incidence by approximately 42%
- Lower risk of thromboembolic events and endometrial cancer compared to tamoxifen
- Maintains bone mineral density better than other aromatase inhibitors when properly managed
- Improves overall survival in hormone receptor-positive early breast cancer
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 first-line treatment of advanced or metastatic breast cancer in postmenopausal women. Additionally, it finds application in extended adjuvant therapy following initial tamoxifen treatment and as a switching strategy after 2-3 years of tamoxifen therapy. The medication may be used in combination with ovarian suppression in premenopausal women undergoing goserelin therapy, though this represents an off-label application requiring careful endocrine monitoring.
Dosage and direction
The recommended dosage of Arimidex is one 1 mg tablet taken orally once daily, with or without food. For adjuvant treatment, therapy should continue for 5 years unless disease recurrence or unacceptable toxicity occurs. Patients should swallow the tablet whole with water and maintain consistent dosing times. No dosage adjustment is necessary for elderly patients or those with mild to moderate hepatic impairment. In cases of severe hepatic impairment, careful monitoring is advised, though formal dosage recommendations have not been established. Renal impairment does not significantly affect anastrozole clearance, making dosage adjustments unnecessary.
Precautions
Patients should undergo comprehensive bone mineral density assessment before initiating therapy and at regular intervals during treatment due to the increased risk of osteoporosis. Regular monitoring of lipid profiles is recommended, as aromatase inhibitors may affect cholesterol metabolism. Hepatic function should be assessed periodically, particularly in patients with pre-existing liver conditions. Patients with pre-existing ischemic heart disease require careful cardiovascular monitoring. Caution is advised when prescribing to patients with strong CYP3A4 inducers or inhibitors due to potential drug interactions. Vitamin D and calcium supplementation should be considered as prophylactic measures against bone mineral density loss.
Contraindications
Arimidex is contraindicated in premenopausal women, pregnant women, and nursing mothers due to the potential for hormonal disruption and fetal harm. Patients with demonstrated hypersensitivity to anastrozole or any components of the formulation should not receive this medication. Those with severe hepatic impairment (Child-Pugh Class C) should generally avoid use unless potential benefits outweigh risks under close supervision. The medication is not indicated for estrogen receptor-negative breast cancer unless being used in combination with other targeted therapies in clinical trial settings.
Possible side effects
The most frequently reported adverse reactions include hot flashes (35%), arthralgia (30%), asthenia (20%), pain (18%), and nausea (16%). Musculoskeletal events such as arthritis and carpal tunnel syndrome occur in approximately 10% of patients. Vasodilatation affects approximately 25% of patients, while mood disturbances and depression are reported in 15% of cases. Less common but serious side effects include cardiovascular events (2-3%), osteoporosis and fractures (10-11% over 5 years), and elevated cholesterol levels (9%). Rare cases of hepatitis and hypersensitivity reactions including angioedema and urticaria have been reported.
Drug interaction
Arimidex demonstrates interactions with estrogen-containing therapies, which may diminish its pharmacological effect. Tamoxifen co-administration reduces anastrozole plasma concentrations by 27% and should be avoided. Strong CYP3A4 inducers such as rifampicin may decrease anastrozole exposure, while inhibitors like ketoconazole may increase plasma levels. The medication does not significantly interact with warfarin, but monitoring of International Normalized Ratio (INR) is recommended during concomitant therapy. No clinically significant interactions have been observed with commonly used medications including diuretics, calcium channel blockers, or beta-blockers.
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 never take two doses simultaneously to make up for a missed dose. Consistency in dosing is important for maintaining stable estrogen suppression, but occasional missed doses are unlikely to significantly impact overall treatment efficacy. Patients should maintain a medication diary or use pill organizers to improve adherence.
Overdose
There is limited experience with Arimidex overdose. Single doses up to 60 mg have been administered without serious clinical consequences. Expected effects would include increased incidence and severity of adverse reactions such as hot flashes, nausea, and dizziness. No specific antidote exists, and treatment should be symptomatic and supportive. Gastric lavage may be considered if ingestion occurred within 2 hours. Dialysis is unlikely to be beneficial due to high protein binding. Patients should seek immediate medical attention and bring the medication container for identification.
Storage
Store Arimidex tablets at room temperature between 15-30°C (59-86°F) in their original container. Protect from light and moisture, and keep the bottle tightly closed. Do not store in bathroom cabinets where humidity levels fluctuate. Keep out of reach of children and pets. Do not use tablets that show signs of discoloration, cracking, or other physical deterioration. Proper disposal of unused medication should follow local regulations, typically through medication take-back programs rather than flushing or household trash disposal.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient characteristics and current clinical guidelines. The prescribing physician should be consulted for specific dosage recommendations and management of adverse effects. Actual clinical outcomes may vary based on individual patient factors, disease characteristics, and adherence to therapy. Regular monitoring and follow-up are essential components of safe and effective treatment.
Reviews
Clinical trials demonstrate Arimidex’s superior efficacy compared to tamoxifen, with the ATAC trial showing a 24% reduction in recurrence risk and 16% reduction in distant recurrence. The BIG 1-98 trial confirmed these findings with improved disease-free survival rates. Patient-reported outcomes indicate generally good tolerability, though musculoskeletal symptoms remain a significant concern affecting quality of life. Long-term follow-up data from multiple studies support the sustained benefit of 5-year adjuvant therapy, with ongoing research investigating extended treatment durations. Real-world evidence correlates with clinical trial data, confirming the established efficacy and safety profile in diverse patient populations.