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Anastrozole

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A hormone treatment used after the menopause to treat breast cancer and prevent it from returning.


Ingredient
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In Stock
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Airmail (14-21 days) | EMS trackable (5-9 days)
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Product Sheet

Alternative/Local Brand
Arimidex
Active Ingredient(s)
Anastrozole
Primary Category
Breast cancer treatment
Therapeutic Class
Endocrine therapy, Enzyme inhibitors
Pharmacological Class
Aromatase inhibitors
Indications
Postmenopausal breast cancer, Hormone receptor-positive early breast cancer
Contraindications
Premenopausal status, Pregnancy and breastfeeding, Severe kidney disease
Minor Side Effects
Hot flushes, Nausea, Stiffness
Moderate Side Effects
Joint pain (arthralgia), Vaginal dryness, Thinning hair
Serious Side Effects
Osteoporosis/fractures, Liver inflammation, Severe skin reactions
Dosage Forms
Tablets
Administration Route
Oral
Mechanism of Action
In postmenopausal women, oestrogen is primarily made by converting other hormones via the 'aromatase' enzyme. Anastrozole blocks this enzyme, significantly lowering oestrogen levels to starve hormone-dependent cancer cells of their growth signal.
Prescription Status
Rx
Patient Summary
A hormone treatment used after the menopause to treat breast cancer and prevent it from returning.
Onset Time
Within 24-48 hours (hormone reduction)
Duration
Long-term (usually 5 years)
Storage Instructions
Store at room temperature.
Drug Interactions
Tamoxifen, Oestrogen-containing therapies
Age Restrictions
Adult postmenopausal women
Pregnancy Use
Contraindicated; strictly for postmenopausal use.
Alternative Drugs
Letrozole, Exemestane

Anastrozole: Generic Medication Overview

Anastrozole is an oral aromatase inhibitor available as a 1 mg pill. It belongs to the class of medications used in women's health and oncology support, primarily to reduce estrogen production in post-menopausal women with hormone-responsive breast cancer. In Hong Kong, anastrozole is a prescription-only medicine regulated by the Department of Health’s Drug Office. Commercially, the same active ingredient is marketed under brand names such as Arimidex.

How Anastrozole Works in the Body

Anastrozole blocks the enzyme aromatase, which converts androgens (e.g., testosterone) into estrogen. By inhibiting this enzyme, anastrozole markedly lowers circulating estrogen levels.

  • Target enzyme: Aromatase (CYP19A1) found mainly in adipose tissue, ovarian stroma, and peripheral sites.
  • Physiologic effect: Reduced estrogen diminishes stimulation of estrogen-dependent tumor cells, slowing their growth.
  • Onset & duration: Serum estrogen levels decline within 24 hours of the first dose; steady-state inhibition is achieved after several days of daily dosing.
  • Pharmacokinetics: Oral absorption is high; peak plasma concentrations occur 2-3 hours after ingestion. The drug is metabolised in the liver (primarily via CYP3A4) and excreted in urine and feces, with a half-life of approximately 50 hours, supporting once-daily dosing.

Conditions Treated by Anastrozole

  • Adjuvant treatment of early-stage hormone-receptor-positive breast cancer in post-menopausal women (FDA-approved; recognized by Hong Kong’s Drug Office).
  • Metastatic breast cancer that is estrogen-dependent, when other endocrine therapies are unsuitable.

These indications are based on large clinical trials that demonstrated improved disease-free survival when anastrozole is used as part of adjuvant therapy.

Evidence-Based Off-Label Uses

  • Fertility preservation in certain assisted-reproductive protocols. Some studies have explored short-term anastrozole to modulate estrogen levels during ovulation induction, but it remains off-label in Hong Kong.
  • Gynecomastia in men receiving androgen therapy. Limited case series suggest benefit, yet formal approval is absent.

Off-label use requires medical supervision and individualized risk assessment.

Who Should Not Use Anastrozole?

Absolute contraindications

  • Known hypersensitivity to anastrozole or any excipients in the pill.
  • Pregnancy (estrogen suppression can harm the fetus).

Relative contraindications

  • Severe hepatic impairment (metabolism is hepatic).
  • Pre-menopausal women with an active menstrual cycle, as estrogen suppression may be inadequate.

Special populations

  • Pregnancy & lactation: Contraindicated.
  • Pediatric patients: Not indicated.
  • Elderly: No dose adjustment required solely for age, but comorbidities should be reviewed.

Common Side Effects

  • Hot flashes - often described as a sudden feeling of warmth.
  • Joint or muscle pain (arthralgia, myalgia).
  • Fatigue or mild dizziness.
  • Nausea or mild gastrointestinal upset.

These effects are usually mild and may lessen with continued therapy.

Serious Adverse Events

  • Severe bone loss leading to osteoporotic fractures. Bone mineral density should be monitored, especially in long-term use.
  • Cardiovascular events (rare) such as myocardial infarction.
  • Allergic reactions (rash, swelling, difficulty breathing) require immediate medical attention.

Drug Interactions

  • Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) can increase anastrozole plasma levels; dose adjustment or alternative therapy may be needed.
  • CYP3A4 inducers (e.g., rifampicin, carbamazepine, St. John’s wort) may lower anastrozole concentrations, potentially reducing efficacy.
  • Anticoagulants (warfarin) - monitor INR more closely as estrogen reduction can affect clotting factors.

Food and Lifestyle Interactions

  • Food: Anastrozole may be taken with or without food; consistent intake with regard to meals is advisable.
  • Alcohol: Moderate consumption is generally safe, but excessive intake may worsen liver function and bone health.
  • Driving: No known impairment, but dizziness should be reported.
  • Sun exposure: No direct photosensitivity, but bone health considerations warrant adequate vitamin D and calcium intake.

How to Take Anastrozole

  • Standard dosing: One 1 mg pill taken orally once daily, at the same time each day.
  • Special populations: No routine dose reduction for renal impairment. For severe hepatic dysfunction, clinicians may consider dose reduction or alternative therapy.
  • Administration: Swallow the pill whole with a glass of water. Do not crush or chew unless instructed by a pharmacist.
  • Missed dose: Take the missed tablet as soon as remembered on the same day; do not double the next day's dose.
  • Overdose: Symptoms may include severe nausea, vomiting, and dizziness. Seek emergency medical care; supportive measures are primary, as no specific antidote exists.
  • Discontinuation: Stopping abruptly is generally safe, but clinicians may advise a gradual taper if therapy has been prolonged to monitor for rebound estrogenic effects.

Monitoring and Follow-Up

  • Bone health: Baseline and periodic dual-energy X-ray absorptiometry (DEXA) scans to assess bone mineral density. Calcium (1,000 mg) and vitamin D (800 IU) supplementation are often recommended.
  • Liver function: Baseline hepatic panel; repeat if clinical concern arises.
  • Symptoms: Patients should report new or worsening joint pain, unexpected fatigue, or signs of fracture.
  • Clinical visits: Typically every 3-6 months during adjuvant therapy, aligning with oncology follow-up schedules.

Storage and Handling

  • Store the pill at room temperature (15-30 °C), protected from moisture and direct sunlight.
  • Keep the container tightly closed and out of reach of children.
  • Do not use the medication after the expiration date printed on the label.
  • Dispose of unused pills according to local pharmacy take-back programs or Hong Kong’s hazardous waste guidelines.

Medication-Specific Glossary

Aromatase Inhibitor
A class of drugs that block the aromatase enzyme, preventing the conversion of androgens to estrogen.
Estrogen Receptor
Cellular proteins that bind estrogen; when activated, they can promote the growth of certain breast cancer cells.
Bone Mineral Density (BMD)
A measurement of the amount of mineral (mostly calcium) in a defined area of bone, used to assess osteoporosis risk.
CYP3A4
A liver enzyme that metabolises many medications, including anastrozole; its activity can affect drug levels.

Medical Disclaimer

This article provides educational information about anastrozole and is not a substitute for professional medical advice. Treatment decisions, including use for unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Anastrozole FAQ

Can anastrozole be used for cancer prevention in high-risk women?

Current evidence does not support routine use of anastrozole for primary prevention of breast cancer in women without a known diagnosis. Clinical guidelines reserve aromatase inhibitors for treatment after a cancer diagnosis, and any preventive use would be off-label and require specialist oversight.

How does anastrozole affect bone health, and what can be done to protect it?

Anastrozole lowers estrogen, a hormone that helps maintain bone density. Patients are advised to undergo baseline BMD testing, supplement calcium and vitamin D, and consider bisphosphonate therapy if significant bone loss occurs.

Is it safe to take anastrozole while on hormone replacement therapy (HRT)?

Concurrent use is generally contraindicated because anastrozole suppresses estrogen, directly opposing HRT. If estrogen levels need to be reduced, clinicians will typically discontinue HRT before starting anastrozole.

What are the differences between anastrozole and other aromatase inhibitors like letrozole?

Both drugs inhibit aromatase, but anastrozole is taken at 1 mg daily, whereas letrozole is typically dosed at 2.5 mg daily. Pharmacokinetic profiles, side-effect spectra, and physician preferences may vary; selection depends on individual patient factors and treatment guidelines.

Can anastrozole be taken with dietary supplements such as soy isoflavones?

Soy products contain phytoestrogens that may partially counteract anastrozole’s estrogen-lowering effect. Patients should discuss supplement use with their oncologist to avoid potential interference with therapy.

Will traveling internationally affect my anastrozole supply?

Anastrozole is a prescription-only medication in Hong Kong and most other jurisdictions. Carry a copy of the prescription and the original pharmacy label when traveling; some countries may require a local prescription for refills.

Does anastrozole cause weight gain or loss?

Weight changes are not a common direct effect of anastrozole. However, menopausal symptoms such as hot flashes or fatigue may indirectly influence activity levels and appetite.

Are there any special considerations for patients with liver disease?

Because anastrozole is metabolised hepatically, severe liver impairment may increase drug exposure. Dose adjustment is often considered on a case-by-case basis, and liver function tests should be monitored.

What should I do if I miss a dose while on anastrozole?

Take the missed tablet as soon as you remember, provided it is still the same day. If it is already near the time for the next scheduled dose, skip the missed tablet and continue with the regular dosing schedule. Do not double the dose.

How long will treatment with anastrozole typically continue?

Adjuvant therapy often lasts five years, but duration may be individualized based on tumor characteristics, response, and tolerability. Your oncologist will determine the optimal treatment length for your situation.

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