Anastrozole – Uses, Dosage, Side Effects, Interactions

Last updated: February 8, 2026Reviewed date: February 8, 2026Reading time: 33 min read
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Anastrozole - Uses, Dosage, Side Effects, Interactions
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Anastrozole is a nonsteroidal inhibitor of aromatase that effectively blocks estrogen synthesis in postmenopausal women and is used as therapy for estrogen receptor-positive breast cancer. Anastrozole has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent...

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Article Summary

Anastrozole is a nonsteroidal inhibitor of aromatase that effectively blocks estrogen synthesis in postmenopausal women and is used as therapy for estrogen receptor-positive breast cancer. Anastrozole has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent liver injury. Anastrozole is a nonsteroidal inhibitor of estrogen synthesis that resembles paclitaxel in chemical structure. As a third-generation aromatase inhibitor, anastrozole...

Key Takeaways

  • This article explains Mechanism of Action in simple medical language.
  • This article explains Indications in simple medical language.
  • This article explains Contraindications in simple medical language.
  • This article explains Dosage in simple medical language.
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Definition

Anastrozole is a nonsteroidal inhibitor of aromatase that effectively blocks estrogen synthesis in postmenopausal women and is used as therapy for estrogen receptor-positive breast cancer. Anastrozole has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent liver injury.

Anastrozole is a nonsteroidal inhibitor of estrogen synthesis that resembles paclitaxel in chemical structure. As a third-generation aromatase inhibitor, anastrozole selectively binds to and reversibly inhibits aromatase, a cytochrome P-450 enzyme complex found in many tissues including those of the premenopausal ovary, liver, and breast; aromatase catalyzes the aromatization of androstenedione and testosterone into estrone and estradiol, the final step in estrogen biosynthesis. In estrogen-dependent breast cancers, anastrozole may inhibit tumor growth. (NCI04)

Mechanism of Action

Anastrazole exerts its anti-estrogenic effects via selective and competitive inhibition of the aromatase enzyme found predominantly in the adrenal glands, liver, and fatty tissues. Many breast cancers are hormone receptor-positive, meaning their growth is stimulated and/or maintained by the presence of hormones such as estrogen or progesterone. In postmenopausal women, estrogen is primarily derived from the conversion of adrenally-produced androgens into estrogens by the aromatase enzyme – by competitively inhibiting the biosynthesis of estrogen at these enzymes, anastrozole effectively suppresses circulating estrogen levels and, subsequently, the growth of hormone receptor-positive tumors.

or

Because estrogen acts as a growth factor for hormone-dependent breast cancer cells, anastrozole-induced reduction of serum and tumor concentrations of estrogen inhibits tumor growth and delays disease progression. Anastrozole selectively inhibits the conversion of androgens to estrogens. In postmenopausal women, ovarian secretion of estrogen declines, and the conversion of adrenal androgens (mainly androstenedione and testosterone) to estrone and estradiol in peripheral tissues (adipose, muscle, and liver), catalyzed by the aromatase enzyme, is the principal source of estrogens. Anastrozole inhibits the aromatase enzyme by competitively binding to the heme of the cytochrome P-450 unit of the enzyme; suppression of estrogen biosynthesis in all tissues reduces serum concentrations of circulating estrogens, including estrone, estradiol, and estrone sulfate. Anastrozole selectively inhibits the synthesis of estrogens and does not affect the synthesis of adrenal corticosteroids, aldosterone, or thyroid hormone. In animals, anastrozole has not been shown to possess direct progestogenic, androgenic, or estrogenic activity, but alterations in the circulating concentrations of progesterone, androgens, and estrogens have been observed.

Indications

  • Anastrozole is indicated as an adjunct therapy in the treatment of hormone receptor-positive early breast cancer in postmenopausal women, and as a first-line treatment for hormone receptor-positive (or hormone receptor-unknown) locally advanced or metastatic breast cancer in postmenopausal women. It may also be used in the treatment of advanced breast cancer in postmenopausal women who experience disease progression despite treatment.
  • It may also be used in the treatment of advanced breast cancer in postmenopausal women who experience disease progression despite treatment with tamoxifen.[rx]
  • Gynaecomastia, McCune-Albright syndrome, Short stature due to Growth Hormone deficiency, Testotoxicosis
  • Anastrozole is a nonsteroidal inhibitor of aromatase that effectively blocks estrogen synthesis in postmenopausal women and is used as therapy of estrogen receptor-positive breast cancer. Anastrozole has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent liver injury.
  • Breast Cancer
  • Breast Cancer, Metastatic
  • McCune-Albright Syndrome
  • Pubertal Gynecomastia
  • Endometrial Cancer
  • Advanced Breast Cancer
  • Early Breast Cancer
  • Invasive Early Breast Cancer
  • Locally Advanced Breast Cancer (LABC)
  • Metastatic Breast Cancer

Use in Cancer

Anastrozole is approved to treat:

  • Breast cancer in postmenopausal women who have any of the following types of breast cancer–
    • Early-stage, hormone receptor-positive (HR+) breast cancer. It is used in women who have already received other treatments.
    • Locally advanced or metastatic breast cancer that is HR+ or hormone receptor unknown (it is not known whether it is HR+ or hormone receptor-negative). It is used as first-line therapy in these patients.
    • Advanced breast cancer that has gotten worse after treatment with tamoxifen citrate.

Anastrozole is also being studied in the treatment of other conditions and types of cancer.

Contraindications

The following conditions are contraindicated with this drug. Check with your physician if you have any of the following:

  • are allergic to anastrozole or any ingredients of the medication
  • are breast-feeding
  • are pregnant
  • high cholesterol
  • a low supply of oxygen rich blood to the heart
  • decreased calcification or density of bone
  • pregnancy
  • a patient who is producing milk and breastfeeding

Dosage

Strengths: 1 mg

Breast Cancer

  • Initial dose: 1 mg orally taken once a day
  • Duration of therapy: Until tumor progression (treatment of advanced breast cancer); unknown (adjuvant treatment of early breast cancer)

Side Effects

The Most Common

  • weakness
  • pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">headache
  • hot flashes
  • sweating
  • stomach pain
  • nausea
  • vomiting
  • loss of appetite
  • constipation
  • diarrhea
  • heartburn
  • weight gain
  • joint, bone, or muscle pain
  • breast pain
  • mood changes
  • depression
  • difficulty falling asleep or staying asleep
  • nervousness
  • dizziness
  • vaginal bleeding
  • vaginal dryness or irritation
  • pain, burning, or tingling in the hands or feet
  • dry mouth
  • hair thinning

More Common

  • chest pain
  • sore throat, cough, fever, chills, swollen glands, or other signs of infection
  • swelling, redness, or warmth in hand or arm
  • difficult, painful, or urgent urination
  • blurred vision or vision changes
  • yellowing of the skin or eyes
  • pain in the upper right part of the stomach
  • skin lesions, ulcers, or blisters
  • rash
  • hives
  • itching
  • shortness of breath
  • difficulty swallowing or breathing
  • swelling of the eyes, face, lips, tongue, throat, arms, hands, feet, ankles, or lower legs

Rare

  • bone fractures
  • chest pain
  • increased blood pressure
  • increased cholesterol levels
  • signs of carpal tunnel syndrome (e.g., tingling pain, coldness, and weakness in parts of the hand)
  • signs of depression (such as feeling sad, losing interest in things you used to enjoy, weight changes, changes in sleep habits, feelings of guilt or worthlessness, thoughts of suicide)
  • tingling or numbness of the skin
  • unusual vaginal discharge, itching, or bleeding
  • signs of a heart attack (e.g., tightness or feeling of heaviness in your chest or pain radiating to your arms or shoulders, neck, teeth, jaw, abdomen, or back)
  • symptoms of liver problems (e.g., abdominal pain, persistent vomiting, feeling unwell, fever, itching, yellowing of the skin and eyes, dark urine)
  • signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
  • signs of a severe skin reaction such as blistering, peeling, a rash covering a large area of the body, a rash that spreads quickly, or a rash combined with fever or discomfort

Drug Interactions

 

Pregnancy and Lactation

FDA Pregnancy Category D

Pregnancy

Although anastrozole has not been studied with pregnant women (it is intended for use only by women who have passed menopause), it is suspected that it could cause serious problems, possibly including miscarriage. Therefore, it should not be used during pregnancy. Tell your doctor immediately if you become pregnant.

Breast-feeding

It is not known whether anastrozole passes into breast milk. Because of the risks associated with this drug, women using this medication should not breastfeed. This medication is not intended for use by children.

Bone mineral density: Long-term use of anastrozole may decrease the density of bones, thereby increasing the risk of osteoporosis. Your doctor will order bone mineral density tests periodically while you are taking anastrozole.

Cholesterol: Anastrozole can cause increases in cholesterol and other lipids in the blood. If you are at an increased risk of developing high cholesterol, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Drowsiness/dizziness: Anastrozole may cause dizziness or drowsiness. If you experience either or both of these side effects, you should not drive, use machinery, or perform any other activities that require alertness.

Heart disease: This medication may increase the risk of heart attack or increased blood pressure. If you are at risk for heart disease or high blood pressure, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. If you experience signs of a heart attack, such as tightness or heaviness in your chest, sudden chest pain spreading to your arms or shoulders, sweating, nausea, or anxiety, seek medical help immediately.

Kidney function: If you have reduced kidney function, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Liver function: If you have liver disease or reduced liver function, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Pre-menopausal women: You should not use this medication if you have not yet started menopause.

What special precautions should I follow?

Before taking anastrozole,

  • tell your doctor and pharmacist if you are allergic to anastrozole, or any other medications, or any of the ingredients in anastrozole. Ask your pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: medications that contain estrogen such as hormone replacement therapy (HRT) and hormonal contraceptives (birth control pills, patches, rings, and injections); raloxifene (Evista); and tamoxifen (Nolvadex). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you have or have ever had high cholesterol, osteoporosis (a condition in which the bones are fragile and break easily), or liver, or heart disease.
  • you should know that anastrozole should only be taken by women who have undergone menopause and cannot become pregnant. However, if you are pregnant or breastfeeding, you should tell your doctor before you begin taking this medication. Anastrozole may harm the fetus.

When To Contact Your Doctor or Health Care Provider:

Contact your health care provider immediately, day or night, and go to the nearest emergency room, if you should experience any of the following symptoms:

  • New or worsening chest pain
  • Shortness of breath
  • Swelling of the face, lips, tongue, and/or throat
  • Difficulty swallowing and/or breathing.
  • Vaginal bleeding (similar to a period)
  • Tickling, Tingling, or Numbness of your skin
  • Nausea (interfering with the ability to eat and unrelieved with prescribed medication)
  • Vomiting (vomiting more than 4-5 times in a 24-hour period)
  • Yellowing of your skin or the whites of your eyes
  • Pain on the right side of your stomach-area

Always inform your healthcare provider if you experience any unusual symptoms.

  • Before starting anastrozole treatment, make sure you tell your doctor about any other medications you are taking (including over-the-counter drugs, vitamins, or herbal remedies)
  • Anastrozole interacts with certain medications. Make sure you tell your doctor if you are taking these medications:
    • Tamoxifen
    • Estrogen
    • Warfarin
    • Estrogen/estradiol-containing medications (commonly used for menopause and birth control)
  • Before starting anastrozole treatment, make sure you tell your doctor about health conditions you have including heart conditions, osteoporosis, and abnormal cholesterol. Anastrozole may cause an increased risk for heart disease. Talk with your healthcare provider to weigh the benefit and risks.
  • Inform your healthcare professional if you have not had menopause yet (premenopausal).
  • Inform your healthcare professional if you are pregnant or may be pregnant prior to starting this treatment. Anastrozole is pregnancy category X (anastrozole may be hazardous to the fetus. Anastrozole is contraindicated in women who are pregnant or may become pregnant).
  • Anastrozole may enter breast milk. It is unclear what effect this may have on babies. Tell your doctor if you are breastfeeding or plan to breastfeed.

Self-Care Tips:

  • If you experience hot flashes, wearing light clothing, staying in a cool environment, and putting cool clothes on your head may reduce symptoms. Consult your healthcare provider if these worsen, or become intolerable.
  • Acetaminophen or ibuprofen may help relieve discomfort from generalized aches and pains. However, be sure to talk with your doctor before taking it.
  • Anastrozole causes little nausea. However, to reduce nausea, take anti-nausea medications as prescribed by your doctor before taking them.
  • Good health practices such as getting plenty of rest and eating a healthy diet along with regular exercise are recommended
  • If you experience symptoms or side effects, be sure to discuss them with your healthcare team. They can prescribe medications and/or offer other suggestions that are effective in managing such problems.

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    Drug Classes
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  50. UN Globally Harmonized System of Classification and Labelling of Chemicals (GHS)
    GHS Classification Tree
    http://www.unece.org/trans/danger/publi/ghs/ghs_welcome_e.html
  51. EPA Substance Registry Services
    LICENSE
    https://www.epa.gov/privacy/privacy-act-laws-policies-and-resources
    EPA SRS List Classification
    https://sor.epa.gov/sor_internet/registry/substreg/LandingPage.do
  52. PATENTSCOPE (WIPO)
    SID 389158251
    https://pubchem.ncbi.nlm.nih.gov/substance/389158251
  53. NCBI
    https://www.ncbi.nlm.nih.gov/projects/linkout

RX Clinical Pathway Engine

Continue through a complete learning pathway

Move from understanding the topic to symptoms, tests, treatment, medicines, monitoring, and prevention.

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  1. Understand the condition Begin with the essential facts and a clear explanation of the topic.
  2. Recognize symptoms Learn common symptoms, signs, and patterns of presentation.
  3. Know when to seek help Review urgent warning signs and when professional assessment may be needed.
  4. Understand causes and risks Explore causes, risk factors, mechanisms, and contributing conditions.
  5. Explore tests and diagnosis Learn how clinicians assess the condition and which investigations may be discussed.
  6. Learn treatment approaches Review general treatment categories and management principles.
  7. Understand medicines safely Continue to medicine education, uses, precautions, and monitoring.
  8. Plan monitoring and follow-up Understand monitoring, complications, rehabilitation, and follow-up learning.
  9. Review prevention and self-care Explore prevention, healthy routines, and questions to discuss with a clinician.

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Doctor visit helper

Prepare before seeing a doctor

A simple rural-patient checklist to help you explain symptoms clearly, ask better questions, and avoid unsafe self-treatment.

Safety note: This is not a prescription or diagnosis. For severe symptoms, pregnancy danger signs, children with serious illness, chest pain, breathing difficulty, stroke-like weakness, or major injury, seek urgent care.

Which doctor may help?

Start with a registered doctor or the nearest qualified health center.

What to tell the doctor

  • Write when the problem started and how it changed.
  • Bring old prescriptions, investigation reports, and current medicines.
  • Write allergies, pregnancy status, diabetes, kidney/liver disease, and major past illnesses.
  • Bring one family member if the patient is weak, elderly, confused, or a child.

Questions to ask

  • What is the most likely cause of my symptoms?
  • Which danger signs mean I should go to hospital quickly?
  • Which tests are necessary now, and which can wait?
  • How should I take medicines safely and what side effects should I watch for?
  • When should I come for follow-up?

Tests to discuss

  • Vital signs: temperature, pulse, blood pressure, oxygen saturation
  • Basic physical examination by a clinician
  • CBC, urine test, blood sugar, or imaging only when clinically needed

Avoid these mistakes

  • Do not use antibiotics, steroid tablets/injections, or strong painkillers without proper medical advice.
  • Do not hide pregnancy, kidney disease, ulcer, allergy, or blood thinner use.
  • Do not delay emergency care when danger signs are present.

Medicine safety and first-aid guide

This section is for patient education only. It does not replace a doctor, pharmacist, or emergency care.

Safe first steps

  • Avoid heavy lifting, sudden bending, and prolonged bed rest.
  • Use comfortable posture and gentle movement as tolerated.
  • Discuss physiotherapy, X-ray, or MRI only when clinically needed.

OTC medicine safety

  • For mild back pain, pain-relief medicine may be discussed with a doctor or pharmacist.
  • Avoid repeated painkiller use if you have kidney disease, stomach ulcer, uncontrolled blood pressure, or are taking blood thinners.

Avoid these mistakes

  • Do not start antibiotics without a proper medical decision.
  • Do not use steroid tablets or injections casually for quick relief.
  • Do not delay emergency care because of home remedies.

Get urgent help if

  • Back pain with leg weakness, numbness around private area, loss of urine/stool control, fever, cancer history, or major injury needs urgent care.
Medicine names, dose, and timing must be decided by a qualified clinician or pharmacist after checking age, pregnancy, allergy, other diseases, and current medicines.

For rural patients and family caregivers

Patient health record and symptom diary

Write your symptoms, medicines already taken, test results, and questions before visiting a doctor. This note stays on your device unless you print or copy it.

Doctor to discuss: Medicine doctor / pediatrician for children / qualified clinician
Tests to discuss with doctor
  • Temperature chart and hydration assessment
  • CBC with platelet count if fever persists or dengue/other infection is possible
  • Urine test, malaria/dengue tests, chest evaluation, or blood culture only when clinically indicated
Questions to ask
  • What is the most likely cause of my symptoms?
  • Which warning signs mean I should go to emergency care?
  • Which tests are really needed now?
  • Which medicines are safe for my age, pregnancy status, allergy, kidney/liver/stomach condition, and current medicines?
  • Do I need antibiotics, or is this more likely viral?

Emergency warning signs such as chest pain, severe breathing difficulty, sudden weakness, confusion, severe dehydration, major injury, or loss of bladder/bowel control need urgent medical care. Do not wait for online information.

Safe pathway to proper treatment

Care roadmap for: Anastrozole – Uses, Dosage, Side Effects, Interactions

Use this simple roadmap to understand the next safe steps. It is educational and does not replace examination by a doctor.

Go to emergency care if you notice:
  • Severe or rapidly worsening symptoms
  • Breathing difficulty, chest pain, fainting, confusion, severe weakness, major injury, or severe dehydration
Doctor / service to discuss: Qualified healthcare provider; specialist depends on symptoms and examination.
  1. Step 1

    Check danger signs first

    If danger signs are present, seek emergency care and do not wait for online information.

  2. Step 2

    Record the symptom story

    Write when symptoms started, severity, medicines already taken, allergies, pregnancy status, and test results.

  3. Step 3

    Visit a qualified clinician

    A doctor, nurse, or qualified healthcare provider can examine you and decide which tests or treatment are needed.

  4. Step 4

    Do only useful tests

    Do tests after clinical assessment. Avoid unnecessary tests, random antibiotics, or repeated medicines without diagnosis.

  5. Step 5

    Follow up and return early if worse

    If symptoms worsen, new warning signs appear, or treatment is not helping, return for review quickly.

Rural patient practical tips
  • Take a written symptom diary and all previous prescriptions/test reports.
  • Do not hide medicines already taken, even herbal or over-the-counter medicines.
  • Ask which warning signs mean urgent referral to hospital.

This roadmap is for education. A real diagnosis and treatment plan requires history, examination, and clinical judgment.

RX Patient Help

Ask a health question safely

Write your symptom story. A health professional or site editor can review it before any answer is prepared. This box is not for emergency care.

Emergency first: Severe chest pain, breathing trouble, unconsciousness, stroke signs, severe injury, heavy bleeding, or rapidly worsening symptoms need urgent local medical care now.

Frequently Asked Questions

Is this article a replacement for a doctor?

No. It is educational content only. Patients should consult a qualified clinician for diagnosis and treatment.

When should I seek urgent care?

Seek urgent care for severe symptoms, rapidly worsening condition, breathing difficulty, severe pain, neurological changes, or any emergency warning sign.

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