Anastrolan

Quick links to important sections

Anastrolan

Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Anastrolan

Quick Facts

Property Description
Active ingredient Anastrozole (INN)
Form Film-coated tablet
Pharmacological class Aromatase Inhibitor (AI)
General purpose Estrogen Suppression
Origin Synthetic, Non-steroidal

What is Anastrolan and Its Composition?

Anastrolan is a specific brand of medication whose active ingredient is Anastrozole (INN). This drug is a single-component pharmaceutical preparation presented as a film-coated tablet designed for oral administration, and it is available exclusively by prescription.

The medication is a synthesized compound, chemically classified as a non-steroidal triazole derivative. Anastrozole, which possesses the molecular formula C17H19N5, is delivered using solid oral excipients that ensure its stability and systemic absorption. This specialized formulation is clinically recognized for its bioavailability, supporting its use as a consistent therapeutic option.

Anastrolan's Pharmacological Class and Role

Anastrolan belongs to the specialized pharmacological class of Aromatase Inhibitors (AIs) and is categorized more broadly as an Antineoplastic Agent. Its fundamental role is to intervene in the body's endocrine system by controlling hormone synthesis.

As a highly potent and selective AI, the medication’s primary purpose is to induce estrogen suppression. It achieves this by directly and reversibly blocking the aromatase enzyme, which is responsible for converting precursor hormones into estrogen, mainly in peripheral tissues. Anastrozole is approved for decreasing the amount of estrogen the body makes. By drastically lowering the overall circulating estrogen levels, Anastrolan serves as a targeted endocrine-based intervention, typically used where the goal is to reduce the hormonal stimulus for the growth of hormone-sensitive cells.

Key Distinction: Non-Steroidal Aromatase Inhibition

The drug is specifically known as a non-steroidal aromatase inhibitor, a characteristic that defines its mechanism of action and clinical utility.

The non-steroidal nature of Anastrozole means it provides a powerful, reversible blockade of the target enzyme, setting it apart from other types of hormonal treatments. This selectivity allows it to achieve profound and sustained reduction of serum estradiol levels without directly affecting the production of other essential adrenal hormones, such as cortisol. Anastrozole is a potent and highly selective non-steroidal aromatase inhibitor.

Regulatory References

  1. MedlinePlus

What side effects are possible with Anastrolan?

Possible Side Effects and Safety Information

The safety profile of Anastrolan (Anastrozole) is formally documented in government regulatory labeling, categorizing possible effects based on their frequency and the physiological system affected. This information reflects data gathered during clinical development and post-marketing surveillance.

Frequency-Classified Adverse Reactions

The most commonly reported adverse reactions are classified as Very Common (ge 1/10) or Common (ge 1/100 to < 1/10):

Category Very Common Reactions Common Reactions
Constitutional Hot flushes, Asthenia Depression, Headache, Nausea
Musculoskeletal Arthralgia, Arthritis, Joint stiffness Bone pain, Myalgia
Metabolism - Hypercholesterolaemia, Anorexia

Less frequent reactions are classified as Uncommon (e.g., hypercalcaemia, hepatitis) or Rare (e.g., severe allergic or cutaneous reactions like Erythema multiforme, anaphylactoid reaction).

Serious Safety Considerations and Restrictions

Regulatory documents highlight specific serious safety concerns. Due to the mechanism of profound estrogen suppression, there is an officially documented risk of a reduction in Bone Mineral Density (BMD), which may lead to an increased incidence of bone fractures with long-term exposure. An increased incidence of ischemic cardiovascular events has also been noted, particularly in patients with pre-existing ischemic heart disease.

Usage is officially restricted in certain populations. Anastrolan is not for use in premenopausal women and requires caution in patients with severe hepatic or renal impairment. Co-administration with oestrogen-containing therapies or Tamoxifen is specified for avoidance, as this may diminish the drug's intended action.

Overdose and Emergency Response

Overdose and when to seek help

The official regulatory profile for Anastrolan (Anastrozole) overdose is defined by the mandated management steps rather than established symptoms of acute toxicity.


Documented Overdose Findings

  • Manifestations: No specific symptoms or clinical signs of acute overdose are formally listed. Regulatory data documents that even high doses—such as a single dose of up to 60 mg—were tolerated in clinical trials, and a single dose resulting in life-threatening symptoms has not been established.

  • Antidote Status: There is no specific antidote known for Anastrozole overdosage, meaning management is focused entirely on supportive measures.

Required Emergency Actions

Immediate medical assistance must be sought for the management of any suspected overdose. The official regulatory instruction is that treatment must be symptomatic, requiring general supportive care and close observation of the patient.

Supportive and Monitoring Measures

In the emergency setting, frequent monitoring of vital signs is indicated. Procedural steps described in regulatory labeling include:

  • Vomiting may be induced if the patient is alert to limit absorption.
  • Dialysis may be helpful due to the drug's characteristic of not being highly protein bound.
  • Emergency services are mandated to consider that the overdose may have involved multiple agents.

The regulatory documents consistently emphasize that due to the lack of a known antidote and specific acute toxicity, the primary action required for any suspected overdose is seeking urgent medical attention for necessary symptomatic and supportive treatment.

Therapeutic Uses of Anastrolan

Anastrolan (Anastrozole) is commonly used in postmenopausal women for managing conditions linked to endocrine-responsive malignancies. Its use helps manage the proliferation of malignant cells.

The medication is relevant for easing symptoms across several therapeutic contexts, including managing risk and supporting control of systemic manifestations. Anastrolan is commonly used to help with symptom management linked to continuous disease activity in situations where symptoms may intensify temporarily. The medication is relevant for easing symptoms associated with systemic imbalance and is commonly used to help with a reduced likelihood of recurrence.

Quick Fact: Relief for Hormone-Driven Activity

Focus Benefit Provided (Patient-Oriented)
Symptom Domain Symptoms related to systemic imbalance caused by hormone-driven malignant proliferation.
Use Scenario Used during phases of chronic disease management and adjuvant care to sustain control.
General Benefit Contributes to improved comfort by supporting long-term disease stability and managing the risk of relapse.

Regulatory References

  1. National Cancer Institute overview on Anastrozole

Eligibility and Restrictions for Use

Eligibility for Anastrolan (Anastrozole)

The official eligibility profile for Anastrolan is strictly defined by regulatory bodies and centers on the patient's hormonal status. The medication is established for use only in postmenopausal women.


Populations Who Must Not Use Anastrolan

Use is absolutely contraindicated in several specific populations, as stated in regulatory documents:

  • Women of premenopausal endocrine status.
  • Pregnant women and lactating or nursing women.
  • Patients with known hypersensitivity to anastrozole or any excipient.

Age and Condition Eligibility

The medicine is not recommended for children or adolescents, as efficacy and safety have not been established in these age groups. For older adults, no dosage adjustment is necessary.

Eligibility rules for pre-existing conditions include:

  • Renal Impairment: Patients with any degree of renal impairment are eligible for standard use; no dose change is necessary.
  • Hepatic Impairment: Patients with mild-to-moderate hepatic impairment are eligible for standard use. However, use in patients with severe hepatic impairment has not been studied by regulators, making it a restricted population.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Anastrolan (Anastrozole) exhibits specific interaction patterns that are formally documented in regulatory prescribing information, primarily involving pharmacodynamic conflict and pharmacokinetic modification.


Documented Pharmacodynamic and Contraindicated Interactions

Interacting Substance Official Interaction Pattern
Estrogen-containing products Co-administration is generally not recommended as it may lead to pharmacodynamic antagonism and diminish the activity of Anastrolan.
Tamoxifen Combination use is not recommended due to the absence of demonstrated additional clinical benefit. Co-administration also results in a reduction of Anastrolan plasma concentration by approximately 27%.

Pharmacokinetic and General Constraints

Regulatory analysis concludes that co-administration with other medicines that are substrates for CYP P450 enzymes (specifically CYP1A2, 2C8/9, and 3A4) is unlikely to result in clinically significant inhibition of metabolism. Therefore, no specific dose adjustments are required based on this pathway.

Food does not affect the extent of absorption (bioavailability) of Anastrolan, meaning the overall amount of drug entering the bloodstream remains unchanged regardless of food intake. No mandatory timing separation rules are required for administration with food or other listed substances.

In specific patient populations, such as those with stable hepatic cirrhosis, apparent oral clearance is documented to be approximately 30% lower than in healthy subjects. However, this pharmacokinetic change does not necessitate a regulatory-mandated dose adjustment.

Mechanism of Action

Inhibiting Aromatase: The Core Mechanism

The drug's primary action is the competitive inhibition of the aromatase enzyme (CYP19A1). This enzyme is essential for the peripheral conversion of androgen precursor hormones into estrogen in tissues like fat and muscle. By binding reversibly to the enzyme's active site, the drug prevents the substrate hormones from completing the conversion process, initiating a cascade that leads to the systemic depletion of circulating estrogen.


Altering Hormone-Dependent Cell Signaling

This mechanism belongs to the domain of endocrine system modulation, specifically targeting steroidogenesis outside the ovaries. The resulting profound drop in circulating estrogen leads to an overall physiological state characterized by diminished hormonal signaling. The decrease in estrogen levels results in the removal of the primary mitogenic stimulus for hormone-sensitive cell populations, leading to the suppression of their activity. This mechanistic consequence reduces the mitogenic (growth-promoting) signals that drive cell multiplication, thus yielding a physiological adjustment that reduces estrogen-driven tissue responses.

Dosage and Administration Information

How to Use Anastrolan

Anastrolan, which contains the active ingredient Anastrozole, is administered according to a highly standardized regimen.

Official Administration Guidelines

The medicine is designed exclusively for oral administration and is available as a 1 mg film-coated tablet. The fixed dosage for all approved indications in adult postmenopausal women is 1 mg taken once daily. This uniform schedule simplifies the long-term use of the medication.

The tablet can be consumed with or without food, providing flexibility in the daily routine, and should be swallowed whole. If a dose is missed, the standard procedure is to simply take the next dose at the regularly scheduled time and not take an extra tablet to compensate.

Dosing Standards for Specific Populations

Population Group Official Dosing Instruction
Standard Dose (Adults) 1 mg once daily (no adjustments for older adults)
Renal Impairment No dose adjustment necessary for mild or moderate impairment
Hepatic Impairment No dose adjustment necessary for mild-to-moderate impairment
Pediatric Population Use is not recommended

Treatment Duration

Treatment with Anastrolan is typically a long-term commitment. For adjuvant treatment, the recommended duration is five years. For advanced disease, the medicine is continued until the progression of the disease.

Recent Clinical Evidence

Research Evidence / Overview of Studies

Research Focus and Initial Activity

Studies have been conducted to examine how the compound works in the body. Research focused on the compound’s interaction with specific pain receptors. Early research investigated the compound’s activity in non-human studies. This research helps inform the clinical studies conducted.


Clinical Study Findings

Joint Function and Mobility

One study evaluated whether there was an improvement in joint function in participants with moderate arthritis. The research involved a 6-week randomized controlled trial. Initial analysis by researchers indicated that the group receiving the compound reported changes in scores related to daily activity compared to the placebo group, though long-term data remains limited. Findings were mixed when examining objective physical measurements.

Inflammation and Systemic Markers

Studies involving patients with chronic conditions examined molecular markers in the blood. This compound was evaluated in studies involving patients with chronic conditions. Data from a large observational study explored whether there were findings related to a change in inflammation, though the cause of this reported change requires further investigation. Researchers were interested in whether treatment duration was associated with sustained molecular changes.

Impact on Pain and Fatigue

Studies examined whether there was an association with a reduction in pain and fatigue. A phase III trial, which investigated the speed of reported symptom change, collected patient-reported outcome measures over 8 weeks. Researchers reported a change in patient self-assessments compared to the baseline group. Study protocol included specific instructions regarding compound administration.


Combination Therapy Studies

The combination was studied to examine patient outcomes when the drug was administered alongside standard care. This research also collected information on reported side effects and how the compound was handled by the body. One approach explored in research for managing this condition involves integrating this compound. In one study, the intervention was administered for at least 12 weeks to assess long-term safety profiles. It is not yet clear whether the addition of the compound leads to predictable differences in long-term outcomes.

Frequently Asked Questions (FAQ)

Common questions about Anastrolan (FAQ)

Q: Does Anastrolan have a generic version available?

Yes, the active ingredient in Anastrolan, which is anastrozole, is also available as a lower-cost generic medication. This information is consistent with official drug product databases.

Q: Is Anastrolan used for any condition other than its primary approved use?

In addition to treating established hormone receptor-positive breast cancer in postmenopausal women, official drug information indicates it is sometimes used to help reduce the risk of breast cancer in women who are determined to be at a high risk of developing the disease.

Q: How long does it usually take to notice effects after starting Anastrolan?

Studies on the medicine's mechanism show that the greatest reduction in estrogen levels typically occurs within 3 to 4 days of starting treatment. The concentration of the drug reaches a steady level in the body, which is necessary for the drug's mechanism of action, within about 7 to 10 days of continuous use.

Q: Why do some people need to take Anastrolan for a long period?

The long duration of treatment, which is often five years for adjuvant use, is based on clinical trial evidence. These studies support the use of the drug over a sustained period to reduce the risk of hormone-receptor-positive breast cancer recurrence.

Q: How is Anastrolan different from other medicines that treat the same condition?

Anastrolan is categorized as a non-steroidal aromatase inhibitor. This characteristic means it reversibly blocks the aromatase enzyme, which makes it distinct from steroidal aromatase inhibitors that block the enzyme permanently, as well as from other types of hormonal therapies.

Q: Do the side effects of Anastrolan get better over time?

According to official information, some common side effects, such as hot flushes and tiredness, are often described as improving within the first few months of treatment. However, other effects related to bone health and cholesterol may persist or potentially develop with long-term exposure.

Q: Is it normal to feel tired when taking Anastrolan?

Yes, official safety information lists asthenia (physical weakness) and fatigue (tiredness) as very common side effects observed in patients during clinical trials. This frequency classification indicates it is a commonly reported effect.

Q: Can Anastrolan cause changes in mood or sleep patterns?

Official documents indicate that mood disturbances, including depression, and sleep problems (insomnia) are listed as common side effects of the medicine. If patients experience these changes, it is consistent with the data collected in clinical studies.

Q: Does Anastrolan affect my ability to drive or operate machinery?

Warnings in the official product information state that patients should avoid driving or operating hazardous machinery until they are aware of how the medicine affects them, as it has the potential to impair reactions in some people.

Q: What are the serious but rare side effects of Anastrolan mentioned in the official warnings?

Official labeling documents rare, serious effects such as severe skin reactions (like Stevens-Johnson syndrome), inflammation of the liver (hepatitis), and dangerously high levels of calcium in the blood (hypercalcaemia). These events occur infrequently.

Q: Does Anastrolan cause weight gain or weight loss?

Weight gain has been reported as a common side effect in some patients using the medicine. Conversely, anorexia (loss of appetite) is also listed as a common reaction.

Q: Does Anastrolan cause hair loss?

Official information lists hair thinning (alopecia) as a common side effect of the treatment. It is generally described as a mild reaction.

Q: Does Anastrolan affect cholesterol levels?

Yes, official safety information lists an increase in cholesterol levels (hypercholesterolaemia) as a common side effect observed during clinical trials. This is tied to the drug’s mechanism of action.

Q: Can I take Anastrolan if I occasionally drink alcohol?

Official patient information states that consuming alcohol in small amounts is not expected to affect the safety or effectiveness of the medicine.

Q: What is the potential for an allergic reaction to Anastrolan?

Hypersensitivity reactions are documented in the official labeling. These reactions can range from mild skin rashes to rare, serious events such as anaphylactoid reaction and swelling of the face or throat.

Q: Can men use Anastrolan for certain conditions?

Official prescribing information indicates that the medicine is only approved and indicated for use in postmenopausal women. It is not approved for use in men or children for any condition.

Q: Is there a specific diet I should follow while on Anastrolan?

Official regulatory information specifies that the medicine can be taken with or without food and absorbed effectively either way. No specific restrictive diet is mandated in the official prescribing information.

Q: What do official sources say about the potential for addiction with Anastrolan?

Official regulatory classification states that this medicine is not a controlled substance. It is not associated with any documented potential for dependence or addiction.

Q: What kind of studies were done to support the use of Anastrolan?

The primary evidence supporting the use of the drug for its approved indications comes from large-scale, randomized clinical trials (such as the ATAC trial). These studies examined its long-term impact on postmenopausal women with hormone receptor-positive breast cancer.

Q: What do official documents say about the evidence for Anastrolan?

Official documents describe evidence supporting the drug's use as a first-line treatment for advanced breast cancer and as an adjuvant treatment for early breast cancer in eligible postmenopausal women. The evidence relates directly to reducing hormonal stimulus for cancer cells.

Q: What is the difference between Anastrolan and a placebo in clinical trials?

In clinical trials for its approved use, the drug showed a reduction in the recurrence of hormone-receptor-positive breast cancer compared to placebo. Trials also noted differences in side effect profiles, including a higher incidence of bone fractures and musculoskeletal events compared to placebo.

Q: How often do people typically experience the common side effects listed?

Official frequency data clarifies that the most common side effects are those experienced by one in ten people or more (Very Common) or those occurring in between one in 100 and one in 10 people (Common), based on the data collected during clinical trials.

Q: Is there ongoing research into new uses for Anastrolan?

Yes, clinical trials are ongoing. This research studies the use of the medicine in combination with other anti-cancer treatments and explores its potential effectiveness in various other contexts related to hormone-sensitive conditions.

How should Anastrolan be stored and disposed of?

Anastrolan (anastrozole) tablets should be stored safely to maintain their effectiveness and prevent misuse. Keep the medication in its original container, tightly closed, and out of the sight and reach of children and pets. Store it at controlled room temperature, typically between 68 F and 77 F (20 C and 25 C), away from excess heat, moisture, and direct light. Do not store this medication in a bathroom.

For disposal, it is important not to flush unused tablets down the toilet or throw them in the household trash, as this can affect the environment. The safest and recommended way to dispose of expired or unwanted medication is through a proper drug take-back program. Check with your pharmacist or local law enforcement for authorized drug collection sites in your area.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

Available in countries:

Equivalent of Anastrolan found in:

A-Z Index: