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Megestrol Acetate Tablets

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Megestrol Acetate Tablets

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Treatment option:

Medically reviewed

Marina Burgos

Last updated on 10/01/2026

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.

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Overview of Megestrol Acetate Tablets

Quick Facts

Property Description
Active ingredient Megestrol acetate (INN)
Form Tablets (for oral administration)
Pharmacological class Progestin, Antineoplastic agent
Origin Synthetic steroid derivative
Single/Combination Single-ingredient product

What is Megestrol Acetate Tablets?

What is the Pharmacological Classification of Megestrol Acetate Tablets?

Megestrol Acetate Tablets are a prescription-only medicine whose active ingredient, Megestrol acetate, is formally classified as a progestin. Specifically, it is a synthetic progestational agent chemically derived from progesterone, a naturally occurring steroid hormone. This hormone derivative and synthetic steroid is recognized in medical guidelines for its capacity to serve as an anti-hormonal agent. The medicine also carries the official classification of an antineoplastic agent, differentiating it from simpler progestins used solely for hormonal birth control.

Composition and Available Forms of the Drug Entity

The tablets represent a specific pharmaceutical preparation and are a single-ingredient product intended for oral administration, containing Megestrol acetate (INN) as the exclusive active ingredient alongside solid pharmaceutical excipients. This composition ensures a consistent, measured dose of the compound. The same Megestrol acetate compound is also commonly supplied as an oral suspension, which provides an alternate liquid option for systemic absorption, a feature clinically useful for patients who may require it. Both preparation forms deliver the identical synthetic steroid compound.

What is the General Therapeutic Purpose of this Synthetic Progestin?

The general therapeutic purpose of this synthetic progestin is linked to two primary and distinct physiological actions: hormonal regulation and appetite modulation. The anti-hormonal agent is primarily utilized to exert an anti-estrogenic effect in specific tissues where cell activity is hormone-dependent. Separately, the drug has a pronounced effect on metabolic function, influencing central pathways to promote an increase in hunger and food intake. The literature consistently notes that Megestrol acetate is clinically recognized for its ability to promote body weight maintenance in patients experiencing involuntary weight loss. This established dual mechanism provides its overall utility in different therapeutic settings.

Regulatory References

  1. Megestrol Acetate - MeSH - NCBI
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What side effects are possible with Megestrol Acetate Tablets?

Possible Side Effects and Safety Information

The regulatory information for Megestrol Acetate Tablets documents the spectrum of possible side effects by frequency and the organ systems involved, with specific emphasis on serious adverse reactions and safety considerations for certain patient populations. Risk classifications are based on official Summary of Product Characteristics (SmPC) data.


Very Common and Common Adverse Reactions

Adverse reactions classified as Very Common (occurring in 10% or more of patients) predominantly affect Metabolism and nutrition, resulting in weight increased and increased appetite. Effects on the Endocrine system include adrenal insufficiency and manifestations of a Cushing's syndrome presentation. Other Very Common effects reported are thrombophlebitis, pulmonary embolism, hypertension, hot flush, and constipation.

Reactions listed as Common (occurring in 1% to less than 10% of patients) involve several body systems, including Gastrointestinal disorders such as nausea, vomiting, diarrhoea, and flatulence. Other Common effects noted are rash, alopecia (hair loss), menorrhagia, and erectile dysfunction.


Serious Adverse Reactions and Systemic Safety Patterns

The official labeling identifies several serious and otherwise important adverse reactions. These include a risk of Thromboembolic Phenomena, comprising thrombophlebitis and pulmonary embolism.

Metabolic and endocrine safety concerns include the reported association of adrenal insufficiency and clinical cases of Overt Cushing's Syndrome with the chronic use of the medicine. Furthermore, cases of new onset diabetes mellitus and the exacerbation of pre-existing diabetes mellitus have been reported.

Safety Considerations for Special Populations

  • Fetal Toxicity: Megestrol Acetate may cause fetal harm, and its use is formally contraindicated during pregnancy.
  • Renal Impairment: The risk of toxic reactions may be greater in individuals with impaired renal function.
  • Older Adults: Dose selection for older adults may require caution due to the greater frequency of decreased organ function in this population.
  • Thromboembolic History: Use of this medicine requires caution in patients with a history of thromboembolic disease.
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Overdose and Emergency Response

Overdose and when to seek help

The official regulatory prescribing information for Megestrol Acetate Tablets details the approach to managing a suspected overdose and specifies when emergency medical care is required. In the event of known or suspected overdosage, the mandatory regulatory action is to seek immediate medical attention.

Documented Manifestations and Management

Official studies have documented the absence of serious unexpected side effects following the administration of megestrol acetate at high daily dosages, specifically up to 1600 mg. Based on this data, a severe acute toxicity profile is not formally established at these high doses.

Management Component Regulatory Statement
Antidote No specific antidote is known for megestrol acetate overdosage.
Treatment Management is restricted to symptomatic and supportive treatment.
Procedural Caveat Due to the compound's low solubility, dialyzability is not an effective means of treating overdose.

Population Considerations

The prescribing information notes that monitoring of the patient's clinical status is required during supportive care. Furthermore, a risk of toxic reactions may be greater in patients with impaired renal function. Specific caution is mentioned for elderly patients, who are noted as being more likely to have decreased renal function, which can increase the potential for adverse outcomes following drug overexposure.

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Therapeutic Uses of Megestrol Acetate Tablets

What Megestrol Acetate Tablets Treats: Main Uses and Benefits

Megestrol Acetate Tablets are commonly used to help manage two distinct therapeutic areas.


Symptomatic Support for Wasting and Malignancy

This medication is applied across domains where additional symptomatic support is needed to address the critical symptom cluster of severe involuntary weight loss and pronounced loss of appetite (anorexia), especially in patients with AIDS or cancer-related cachexia. The therapeutic benefit provided is the support of body weight maintenance and enhanced food consumption, which generally contributes to easing the overall symptom load and helps improve nutritional status. In a separate clinical context, the medication is also commonly used for the palliative treatment of certain hormone-sensitive malignant neoplasms, specifically advanced breast carcinoma or endometrial carcinoma. In these situations, it assists in managing cell activity associated with these conditions.

“The medication is considered relevant for managing distressing symptoms that interfere with daily comfort and stability during advanced illness.”


Quick Fact: Relief for Nutritional Decline

Category Description
Main Symptom Cluster Severe involuntary weight loss and anorexia (loss of appetite).
Primary Benefit Support for body weight maintenance and increased food intake.
Common Scenarios Palliative care setting for advanced malignancy and AIDS-related wasting syndrome.
Therapeutic Role Hormonal support in specific advanced breast and endometrial cancers.

Regulatory References

  1. U.S. National Library of Medicine DailyMed data
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Eligibility and Restrictions for Use

Who Can and Cannot Use Megestrol Acetate Tablets?

This information details the officially documented population eligibility and non-eligibility for Megestrol Acetate Tablets, based on governmental regulatory sources. Eligibility is defined by a patient's physiological status, medical history, and age.


Absolute Contraindications (Must Not Use)

Status or Condition Regulatory Constraint
Pregnancy Contraindicated in patients with known or suspected pregnancy. Females of reproductive potential must use effective contraception.
Allergy Contraindicated in patients with a history of hypersensitivity to megestrol acetate or any component.
Genetic/Metabolic Not recommended for patients with rare hereditary problems like galactose intolerance or lactose deficiency (tablet formulation).

Population Restrictions and Cautions

Population Group Regulatory Constraint
Pediatric Patients Safety and effectiveness have not been established; use is not recommended.
Elderly Patients Dose selection should be cautious, reflecting the greater frequency of decreased organ function.
Lactation Nursing should be discontinued if treatment is required. HIV-1-infected women must not breastfeed.
Organ Function Caution is required for patients with impaired renal function or impaired liver function.
Comorbidities Caution is advised for patients with a history of thromboembolic disease or pre-existing diabetes.
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What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory information for Megestrol Acetate Tablets documents specific interaction patterns with other medicines, primarily categorized as pharmacokinetic modification or pharmacodynamic interference.


Documented Interaction Patterns

Interacting Substance Official Regulatory Outcome
Indinavir Co-administration results in a significant decrease in Indinavir exposure (AUC and Cmax), requiring consideration of a higher Indinavir dose.
Antidiabetic Agents (e.g., Insulin) Decreased therapeutic efficacy of these agents due to pharmacodynamic antagonism.
Warfarin May cause an increase in the International Normalized Ratio (INR), requiring close monitoring of coagulation parameters.
Immunosuppressants (Etrasimod, Siponimod) Co-administration can lead to additive immunosuppressive effects.

Interaction-Related Constraints and Notes

The product label notes that administration of the oral suspension formulation with food may increase its bioavailability and resulting plasma concentrations, though specific timing separation rules for other medicines are not documented. Regarding population-specific interaction notes, official labeling indicates that the risk of toxic reactions may be greater in patients with impaired renal function. Furthermore, use in patients with pre-existing diabetes mellitus requires special consideration due to reports of its exacerbation and new-onset diabetes.

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Mechanism of Action

Megestrol acetate functions as a synthetic derivative of progesterone and is classified as a progestin. Its primary molecular action involves serving as an agonist for the nuclear progesterone receptor (PR). Upon binding, the ligand-receptor complex translocates to the cell nucleus.

Within the nucleus, the complex interacts with specific Hormone Response Elements (HREs) in the regulatory regions of target genes, thereby modulating the rate of gene transcription. This alteration in genetic expression leads to subsequent changes in the synthesis of various cellular proteins, influencing cell growth and differentiation in progesterone-sensitive tissues.

Downstream, activation of the PR also exerts antigonadotropic effects by disrupting the hypothalamic-pituitary-gonadal (HPG) axis. Specifically, it inhibits the release of luteinizing hormone (LH) from the anterior pituitary gland, which systemically reduces ovarian estrogen synthesis. Additionally, megestrol acetate exhibits agonist activity at the glucocorticoid receptor (GR) and is hypothesized to modulate the effects of catabolic cytokines, influencing systemic metabolic pathways.

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Dosage and Administration Information

Official Administration Guidelines

Megestrol Acetate Tablets are intended for oral administration and are supplied in strengths such as 20 mg and 40 mg. Proper use is defined by specific daily dose totals and administration schedules, which vary by the official indication.


Field Official Administration Instruction
Route of Administration Oral administration only.
Dosing Schedule Breast Carcinoma: 160 mg per day. Endometrial Carcinoma: 40 mg to 320 mg per day.
Frequency Pattern The total daily dose is administered either in divided doses or, in some regional labels for breast carcinoma, as a single 160 mg dose.
Minimum Duration At least 2 months of continuous treatment is considered the adequate period for determining the efficacy of the drug.
Formulation Constraint The tablet form is not substitutable on a milligram-for-milligram basis with the high-concentration oral suspension.
Older Adult Patients Dose selection for older adults should be cautious, typically starting at the low end of the dosing range.
Procedural Condition Females of reproductive potential must have a negative pregnancy test prior to initiation of therapy.

The regulatory instructions establish that the standard approach involves calculating the specific daily dose for the condition, ensuring it is taken according to the daily frequency pattern documented in the prescribing information, and continuing the treatment for the officially mandated minimum duration to assess effect. The label specifies that its use is not established for children.

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Recent Clinical Evidence

Megestrol Acetate Tablets: Recent Clinical Evidence

Clinical research has historically focused on Megestrol Acetate (MA) for two primary indications: managing anorexia/cachexia (weight loss and wasting) in patients with AIDS and, at higher doses, for treating advanced breast and endometrial cancers.


Evidence for Weight Loss and Cachexia

Studies have assessed the impact of MA on appetite and body weight in individuals experiencing significant involuntary weight loss, such as those with HIV-related cachexia. Research consistently showed that MA, compared to placebo, was associated with an increase in appetite and body weight, primarily due to an increase in fat mass, rather than lean muscle mass. This finding suggests MA may play a role in nutritional support rather than preventing muscle wasting.


Evidence in Oncology

In oncology, MA has been explored as a hormonal therapy for hormone-sensitive tumors:

  • Endometrial Cancer: Research has evaluated MA as a treatment for advanced, recurrent, or metastatic endometrial carcinoma. Findings indicate that MA may induce a clinical response, particularly in tumors that express progesterone receptors.
  • Breast Cancer: Studies assessed MA use in postmenopausal women with advanced or metastatic breast cancer that has progressed despite treatment with other hormone therapies (e.g., tamoxifen). Clinical trials examined whether MA could offer a palliative option for these patients.

Safety and Tolerability

Across clinical studies, the most common serious adverse event observed with MA was an increased risk of thromboembolic events (blood clots). Due to this recognized risk, participants are often monitored for signs of deep vein thrombosis or pulmonary embolism during treatment. Other frequently observed adverse effects included weight gain and breakthrough vaginal bleeding.

Key Studies & References

  1. MEGESTROL ACETATE TABLETS, USP (Prescribing Information / DailyMed)
  2. Hormone Therapy for Endometrial Cancer (American Cancer Society Guideline/Information)
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Frequently Asked Questions (FAQ)

Common questions about Megestrol Acetate Tablets (FAQ)


Q: How quickly does Megestrol Acetate Tablets start working for its main uses?

Regulatory documents indicate that at least 2 months of continuous treatment is considered the adequate period for assessing the efficacy of the drug. For its use in stimulating appetite, clinical studies observed improvement in appetite and weight over a 12-week period.


Q: What is the biggest difference between Megestrol Acetate and Progesterone?

Megestrol Acetate is a synthetic derivative of progesterone, classified as a progestin. Its approved therapeutic uses are distinct, including the palliative treatment of certain advanced cancers and the treatment of significant involuntary weight loss or anorexia. It is formally recognized as an antineoplastic agent.


Q: What are the most serious side effects of Megestrol Acetate Tablets that I should be aware of?

Official labeling highlights several serious risks, including thromboembolic phenomena (the formation of blood clots, such as in the legs or lungs). The medication can also affect the body's natural hormones, leading to issues like adrenal insufficiency or manifestations of Cushing’s syndrome. The drug also has the potential to cause fetal harm and is contraindicated during pregnancy.


Q: What are the general expectations for benefits when starting Megestrol Acetate Tablets?

Clinical studies supporting its use for anorexia and cachexia reported quantified outcomes. Official data indicates that, at the highest doses used in clinical studies, approximately 64 percent of trial patients were associated with a weight gain of ge 5 pounds after 12 weeks of treatment.


Q: Is it common to feel tired while taking this medication?

The official product information notes adverse reactions related to general physical weakness. These effects include terms such as asthenia (weakness) and lethargy (sluggishness) among other possible effects.


Q: Are there different forms of Megestrol Acetate besides the tablet?

Yes, in addition to the tablet, the active ingredient Megestrol acetate is also commonly supplied as an oral liquid suspension. The official label notes that the different formulations are not considered interchangeable on a milligram-for-milligram basis.


Q: Why is this medication sometimes used for conditions other than cancer?

The medication has a dual purpose. Official regulatory bodies have approved the drug not only for treating certain advanced cancers but also for the treatment of anorexia, cachexia (wasting syndrome), or significant unexplained weight loss in patients with AIDS, due to its metabolic effects on appetite.


Q: Is Megestrol Acetate Tablets considered a chemotherapy drug?

The drug is formally classified as an antineoplastic agent (anti-cancer agent) and a progestin (a hormone derivative). It primarily functions as a hormone therapy and is not typically grouped with cytotoxic (cell-killing) chemotherapy drugs.


Q: How long do most people stay on Megestrol Acetate Tablets?

Regulatory guidance specifies a minimum of 2 months of continuous treatment to assess its efficacy. Since the drug is used for the palliative and chronic management of conditions like advanced cancer or wasting syndrome, the overall duration of use is often long-term, guided by the patient's condition.


Q: Can men use Megestrol Acetate Tablets?

Yes, Megestrol Acetate Tablets are used in men for approved indications, such as the treatment of significant weight loss and appetite issues. Clinical studies supporting this use have included adult male patients.


Q: Does Megestrol Acetate Tablets affect bone density?

The drug has a glucocorticoid-like effect that can lead to suppression of the adrenal (HPA) axis, which regulates the body's natural steroid hormones. This mechanism is associated with effects on bone health, and fractures have been reported as a possible adverse reaction.


Q: Can this medication change my mood or cause depression?

Regulatory documents list changes in mood and depression as documented adverse reactions reported in patients using Megestrol Acetate Tablets.


Q: What kind of patient monitoring is typically needed while taking this drug?

Official documentation indicates that close surveillance is warranted for patients receiving this treatment. Specific monitoring considerations include regular checks for those with pre-existing diabetes and monitoring of renal (kidney) function. Observation for signs of adrenal insufficiency is also noted.


Q: What is the difference in side effects between short-term and long-term use?

The regulatory documents specifically associate certain serious effects with chronic use of the drug. These include the development of new onset diabetes mellitus, the worsening of pre-existing diabetes, adrenal insufficiency, and manifestations of Overt Cushing's syndrome.


Q: What is the general success rate described in studies for its approved uses?

Clinical data supporting the use of the drug for anorexia and cachexia reported that, at the highest approved doses, approximately 64 percent of trial patients were associated with a weight gain of ge 5 pounds after 12 weeks.


Q: Is there a link between Megestrol Acetate Tablets and adrenal gland issues?

Yes, regulatory documents list adrenal insufficiency and manifestations of Cushing's syndrome as important adverse reactions. These issues are associated with the drug's effect on the adrenal glands, particularly with chronic use.


Q: What happens if I accidentally take two tablets at once?

Official documentation notes that in clinical studies, the drug was administered in high dosages (up to 1600 mg/day) without resulting in serious unexpected side effects. However, the regulatory text does not provide specific medical instruction for handling a double dose.


Q: Does the tablet contain common allergens like gluten or lactose?

The official list of inactive ingredients for the tablet formulation includes lactose hydrous impalpable. The ingredients do not list gluten.


Q: What happens when you stop taking Megestrol Acetate Tablets?

Official documents indicate a risk of developing adrenal insufficiency in patients being withdrawn from chronic therapy. This is due to the drug’s potential to suppress the body’s adrenal function.


Q: Does taking this tablet at a specific time of day matter?

Administration guidelines focus on taking the correct total daily dose and frequency (whether once a day or in divided doses). The regulatory text does not specify a critical time of day (such as morning versus evening) for the tablet.

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How should Megestrol Acetate Tablets be stored and disposed of?

Megestrol acetate tablets must be stored at Controlled Room Temperature, defined as 20 C to 25 C (68 F to 77 F), and protected from temperatures exceeding 40 C (104 F).

Storage Conditions

Requirement Specific Instruction
Temperature Controlled Room Temperature 20 C to 25 C (68 F to 77 F), protect from heat.
Container Dispense in tight, child-resistant containers and keep tightly closed.
Protection Store in the original container to protect from moisture.

Disposal Requirements

Unused or expired megestrol acetate tablets must be disposed of in accordance with applicable laws and regulations. The medication must be kept out of the sight and reach of children. Disposal should not typically occur via the household trash or down the sink/toilet unless specifically instructed by the medicine label. The preferred method for discarding unused medicine is through an official drug take-back program.

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

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