Arimidex: Advanced Estrogen Control for Breast Cancer Treatment
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Synonyms | |||
Arimidex (anastrozole) is a potent, non-steroidal aromatase inhibitor specifically formulated for the treatment of hormone receptor-positive early and advanced breast cancer in postmenopausal women. By selectively inhibiting the aromatase enzyme, Arimidex significantly reduces estrogen production, creating an unfavorable environment for hormone-sensitive tumor growth. This targeted mechanism offers a sophisticated endocrine therapy option with a well-established efficacy and safety profile, making it a cornerstone in modern breast cancer management protocols.
Features
- Active ingredient: Anastrozole 1 mg
- Pharmaceutical class: Non-steroidal aromatase inhibitor
- Administration: Oral tablet formulation
- Bioavailability: Approximately 80-85% following oral administration
- Half-life: 40-50 hours in postmenopausal women
- Metabolism: Primarily hepatic via N-dealkylation, hydroxylation, and glucuronidation
- Excretion: Primarily hepatic (85%) with renal elimination of metabolites
- Special coating: Film-coated for easier swallowing
Benefits
- Superior disease-free survival rates compared to tamoxifen in early breast cancer
- Significant reduction in contralateral breast cancer incidence
- Avoids estrogen agonist effects associated with tamoxifen therapy
- Favorable long-term safety profile with reduced endometrial cancer risk
- Convenient once-daily dosing regimen
- No requirement for corticosteroid supplementation
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 hormone receptor-positive or hormone receptor-unknown locally advanced or metastatic breast cancer in postmenopausal women. Additionally, Arimidex is used for treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy. The medication may be prescribed as extended adjuvant treatment following the initial 5 years of tamoxifen therapy.
Dosage and direction
The recommended dosage of Arimidex is one 1 mg tablet taken orally once daily, with or without food. 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 duration typically continues for 5 years in the adjuvant setting, though duration may vary based on individual patient response and tolerability. Dosage adjustment is not necessary for elderly patients or those with mild-to-moderate hepatic impairment.
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 Arimidex may elevate cholesterol levels. Caution is advised in patients with pre-existing ischemic heart disease. Patients should be monitored for signs and symptoms of carpal tunnel syndrome. Those with a history of hypercholesterolemia require close lipid monitoring. Vitamin D and calcium supplementation should be considered for bone health maintenance.
Contraindications
Arimidex is contraindicated in premenopausal women, pregnant women, and nursing mothers. It should not be used in patients with known hypersensitivity to anastrozole or any excipients in the formulation. Concomitant use with estrogen-containing therapies is contraindicated. Patients with severe hepatic impairment (Child-Pugh C) should not receive Arimidex therapy. The medication is contraindicated in patients with severe renal impairment (creatinine clearance <30 mL/min).
Possible side effect
Common adverse reactions (>10%) include hot flashes, asthenia, arthritis, pain, arthralgia, pharyngitis, hypertension, depression, nausea and vomiting, rash, osteoporosis, back pain, insomnia, headache, bone pain, and peripheral edema. Less frequent side effects (1-10%) comprise fractures, lymphoedema, increased cholesterol, weight gain, vaginal dryness, vaginal hemorrhage, diarrhea, anorexia, hypercalcemia, trigger finger, carpal tunnel syndrome, and dizziness. Rare events (<1%) may include hepatitis, thrombocytopenia, leukopenia, and allergic reactions.
Drug interaction
Arimidex may interact with estrogen-containing medications, potentially diminishing its therapeutic effect. Tamoxifen co-administration reduces anastrozole plasma concentrations by 27% and should be avoided. CYP3A4 inducers such as rifampicin may decrease anastrozole concentrations. Although formal interaction studies show no clinically significant interactions with warfarin or other CYP2C9 substrates, careful monitoring is recommended when co-administering with medications having a narrow therapeutic index.
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 such cases, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should never take a double dose to make up for a missed one. Maintaining a consistent dosing schedule is important for optimal therapeutic effect, and patients may benefit from using reminder systems or pill organizers.
Overdose
There is no specific antidote for Arimidex overdose. Single doses of up to 60 mg have been administered without serious adverse effects. In case of suspected overdose, symptomatic and supportive treatment should be initiated. Gastric lavage may be considered if ingestion occurred within a short time frame. Vital signs should be monitored regularly, and appropriate medical supervision maintained until the patient’s condition stabilizes. Dialysis is unlikely to be beneficial due to high protein binding.
Storage
Store Arimidex tablets at room temperature (15-30°C or 59-86°F) in the original container to protect from light and moisture. Keep the medication out of reach of children and pets. Do not store in bathrooms or other areas with high humidity. Discard any medication that has expired or shows signs of deterioration. Proper disposal methods should be followed according to local regulations, preferably through medication take-back programs.
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 consider individual patient circumstances. The prescribing physician should be consulted for complete information regarding indications, dosage, warnings, and precautions. Patients should not alter their treatment regimen without medical supervision.
Reviews
Clinical studies demonstrate Arimidex’s superior efficacy compared to tamoxifen in multiple large-scale trials. The ATAC (Arimidex, Tamoxifen Alone or in Combination) trial showed a significant improvement in disease-free survival with a favorable risk-benefit profile. The IBIS-II prevention trial confirmed reduced breast cancer incidence in high-risk postmenopausal women. Patient-reported outcomes indicate generally good tolerability, though management of musculoskeletal symptoms and bone health requires ongoing attention. Long-term follow-up data continue to support its role as first-line endocrine therapy.