Arimidex: Advanced Aromatase Inhibition for Hormone Therapy
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Synonyms | |||
Arimidex (anastrozole) is a potent, nonsteroidal aromatase inhibitor indicated for the treatment of hormone receptor-positive early and advanced breast cancer in postmenopausal women. It functions by significantly reducing estrogen production, a key driver in certain breast cancer types. This targeted approach helps inhibit cancer cell proliferation and is a cornerstone of adjuvant and metastatic hormonal therapy regimens. Its well-established efficacy and favorable tolerability profile make it a first-line choice for endocrine treatment.
Features
- Active ingredient: Anastrozole 1 mg
- Pharmaceutical form: Film-coated tablets
- Mechanism: Selective, nonsteroidal aromatase inhibition
- Bioavailability: Well-absorbed orally with minimal food interaction
- Half-life: Approximately 50 hours in postmenopausal women
- Metabolism: Hepatic, primarily via N-dealkylation, hydroxylation, and glucuronidation
- Excretion: Primarily hepatic (85%), with renal elimination of metabolites
Benefits
- Effectively reduces estrogen levels by up to 97% in postmenopausal women
- Demonstrates superior disease-free survival compared to tamoxifen in hormone receptor-positive early breast cancer
- Reduces contralateral breast cancer incidence in adjuvant settings
- Generally well-tolerated with manageable side effect profile
- Oral administration allows convenient once-daily dosing
- No associated cumulative toxicity with long-term use
Common use
Arimidex is primarily prescribed for the adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer, typically following initial therapy such as surgery or radiation. It is also indicated for the first-line treatment of hormone receptor-positive or hormone receptor-unknown locally advanced or metastatic breast cancer in postmenopausal women. Additionally, it may be used as extended adjuvant therapy following initial tamoxifen treatment and for advanced breast cancer that has progressed following tamoxifen therapy.
Dosage and direction
The recommended dosage is one 1 mg tablet taken orally once daily, with or without food. Tablets should be swallowed whole with water. For adjuvant treatment of early breast cancer, the recommended treatment duration is five years. For advanced breast cancer, treatment should continue until tumor progression is evident. No dosage adjustment is necessary for elderly patients or those with mild-to-moderate hepatic impairment. Patients with severe hepatic impairment have not been studied and should be monitored closely.
Precautions
Patients should undergo bone mineral density assessment before initiating treatment and at regular intervals thereafter due to the increased risk of osteoporosis. Regular monitoring of lipid profiles is recommended. Caution should be exercised in patients with pre-existing ischemic heart disease. Patients should be advised about potential effects on driving and operating machinery due to possible fatigue and dizziness. Regular liver function tests are advised during treatment. Patients should be monitored for signs and symptoms of carpal tunnel syndrome.
Contraindications
Arimidex is contraindicated in premenopausal women, pregnant women, women of childbearing potential not using effective contraception, patients with hypersensitivity to anastrozole or any excipients, and patients with severe hepatic impairment. It should not be co-administered with estrogen-containing therapies as this would counteract its pharmacological action. Concomitant use with drugs that contain estrogen, including hormone replacement therapy, is contraindicated.
Possible side effects
Most common adverse reactions (≥10%) include:
- Hot flashes (35%)
- Asthenia/fatigue (16%)
- Arthritis/arthralgia (15%)
- Pain (11%)
- Headache (9%)
- Nausea (8%)
- Rash (6%)
- Back pain (6%)
- Osteoporosis (11% after 2 years of treatment)
- Fractures (10% after 2 years of treatment)
Less common but serious side effects may include ischemic cardiovascular events, hepatic enzyme alterations, and hypercholesterolemia.
Drug interaction
Anastrozole does not inhibit major CYP450 enzymes at therapeutic concentrations. However, co-administration with tamoxifen reduces anastrozole plasma concentrations by 27% and should be avoided. Estrogen-containing medications may diminish its pharmacological effect. Medications that induce CYP3A4 may potentially decrease anastrozole concentrations. No clinically significant interactions have been observed with warfarin or other common medications, though monitoring is advised when used with drugs having a narrow therapeutic index.
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 take a double dose to make up for a missed dose. Maintaining consistent daily dosing is important for optimal therapeutic effect.
Overdose
There is no specific antidote for anastrozole overdose. Single doses up to 60 mg have been tolerated without severe effects. Expected symptoms would be an exaggeration of known adverse effects, particularly nausea, vomiting, and dizziness. Treatment should be symptomatic and supportive. Gastric lavage may be considered if ingestion was recent. Dialysis is unlikely to be beneficial due to high protein binding.
Storage
Store at room temperature (15-30°C/59-86°F) in the original container to protect from light and moisture. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging. Tablets should be protected from high humidity and excessive heat. Do not transfer tablets to other containers as this may affect stability.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Treatment decisions should be made by qualified healthcare professionals based on individual patient circumstances. Always follow the prescribing information provided with the medication and consult with a healthcare provider regarding any questions about medical conditions or treatment. Dosage and administration may vary based on individual patient needs and clinical context.
Reviews
Clinical studies demonstrate Arimidex’s superior efficacy compared to tamoxifen in hormone receptor-positive early breast cancer, with a 26% reduction in recurrence risk (ATAC trial). The BIG 1-98 trial confirmed improved disease-free survival rates. Patient-reported outcomes indicate generally good tolerability, though musculoskeletal symptoms and vasomotor symptoms are commonly reported. Long-term follow-up data support its safety profile over extended treatment periods, with appropriate monitoring and management of bone health.