Gestrol

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Gestrol

Method of action: Endocrine Therapy

Treatment option: Anorexia, Cachexia, Cancer, Breast Cancer

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.

Overview of Gestrol

Quick Facts

Property Description
Active Ingredient Megestrol Acetate (INN)
Form Oral Tablet, Oral Suspension
Pharmacological Class Progestational Agent / Antineoplastic Agent
Common Use Hormonal modulation and appetite stimulation
Origin Synthetic Steroid Derivative

What is Gestrol? Definition, Composition, and Pharmacological Class

Gestrol is a synthetic prescription medication, manufactured and distributed under a brand name, containing the single active ingredient, Megestrol Acetate. This compound is chemically classified as a potent Progestational Agent (progestin), derived from the structure of the natural steroid hormone progesterone. Due to its targeted biological effects, this compound is also clinically recognized and categorized as an Antineoplastic Agent for specific therapeutic applications involving the modulation of hormone-sensitive processes.

The core of Gestrol is the single active ingredient, which is known for its high binding affinity to progesterone receptors. Its synthetic structure allows for reliable systemic exposure when administered via the oral route. This specific formulation, whether tablet or suspension, is typically reserved for adult patients in therapeutic settings where potent hormonal or metabolic intervention is required.


Forms, Origin, and the Dual Purpose of Megestrol Acetate

Gestrol is typically available for oral use as both a solid Oral Tablet and a liquid Oral Suspension, offering delivery flexibility, particularly for patients with difficulty swallowing. The Oral Suspension often utilizes specialized techniques, such as micronization, which is associated with enhanced bioavailability compared to standard solid forms.

The general purpose of Gestrol is defined by its pronounced dual action: it works to modulate the environment in hormone-sensitive tissues, often through specific antiestrogenic effects, and critically, the medication functions as a potent Appetite Stimulant. This latter effect is widely relied upon in a typical use scenario to promote weight gain and manage the severe, involuntary weight loss, known as cachexia, often experienced by individuals with chronic, complex diseases.

Regulatory References

  1. Megestrol Acetate Information (NIH/DailyMed)

What side effects are possible with Gestrol?

Possible Side Effects and Safety Information

The officially documented adverse effects of Gestrol (Megestrol Acetate) are classified by health authorities to describe potential safety characteristics and risk profiles. The most common effects are primarily categorized under Metabolism and Nutrition Disorders and Gastrointestinal Disorders.


Frequency-Classified Adverse Reactions

Adverse reactions are grouped by frequency as determined in clinical data. Weight gain is officially listed as a very common adverse reaction, reflecting its metabolic effect. Other effects classified as common (ge 1/100 to <1/10) include nausea, diarrhea, flatulence, and hypertension. These are systematically categorized across various body systems in regulatory documents, such as Gastrointestinal Disorders and Vascular Disorders.

Classification Examples of Documented Effects
Very Common Weight Gain, Dyspnea, Asthenia, Constipation
Common Nausea, Diarrhea, Hypertension, Rash, Headache

Serious Adverse Reactions and Duration-Related Safety

Regulatory documents highlight serious adverse reactions that require specific attention. These include thromboembolic phenomena (such as Deep Vein Thrombosis and Pulmonary Embolism). The official safety profile also notes risks associated with the duration of use. Chronic use is formally documented as being associated with the risk of adrenocortical suppression and the development of new-onset diabetes mellitus or exacerbation of pre-existing diabetes.


Population-Specific Safety Considerations

The medicine is officially contraindicated in pregnancy due to the potential for fetal harm. Caution is advised in patients with a history of thromboembolic disease and for diabetic patients because of the risk of hyperglycemia or the exacerbation of their condition, as defined in regulatory labeling. These safety considerations define constraints on the application of the medicine.

Overdose and Emergency Response

Overdose Map: Overdose and when to seek help — Official Regulatory Information for Gestrol


Overdose Scope

Category Official Regulatory Statement
Documented overdose presentations: Postmarketing reports list specific symptoms associated with overdose, including diarrhoea, nausea, abdominal pain, shortness of breath, cough, unsteady gait, listlessness, and chest pain.
Physiological systems affected: Symptoms reported in overdose context affect the gastrointestinal, respiratory, cardiac, and neurological/musculoskeletal systems.
Dose-related or exposure-related factors: No serious unexpected side effects resulted from clinical studies involving doses as high as 1600 mg/day.
Population-specific overdose notes: No specific differential considerations are explicitly documented in the official overdose section for renal/hepatic impairment, pediatric, or geriatric patients.
Emergency-response statements: Treatment of overdose should be symptomatic and supportive. There is no specific antidote known.
When immediate medical help is required: Immediate emergency medical attention must be sought following any suspected acute overdose due to the potential for serious reported signs such as chest pain and shortness of breath.

Overdose Classifications (High-Level)

Category Official Regulatory Statement
Severity classification: While high doses did not cause serious unexpected effects, postmarketing reports include symptoms that typically mandate urgent medical evaluation.
Regulatory basis: Information is derived from the official overdose sections of the Summary of Product Characteristics (SmPC) and FDA Prescribing Information.
Overdose-context constraints: The low solubility of megestrol acetate leads to the postulation that hemodialysis would not be an effective means of treating overdose.

Resulting Overdose Structure

Official overdose statements:

  • Postmarketing reports of overdose include symptoms such as diarrhoea, nausea, abdominal pain, shortness of breath, cough, unsteady gait, listlessness, and chest pain.
  • Treatment is symptomatic and supportive, as no specific antidote is known.
  • The drug's low solubility suggests that dialysis would not be an effective means of treating overdose.
  • Immediate emergency medical attention must be sought for any suspected acute overdose.

Connection to the Overall Overdose Profile

Official regulatory documents define the Gestrol overdose profile primarily through the lack of serious unexpected toxicity in clinical trials at high doses and a list of postmarketing symptoms that necessitate immediate medical action. This documentation explicitly states that management is limited to symptomatic and supportive care, confirms the absence of a specific antidote, and establishes that detoxification methods like dialysis are postulated to be ineffective based on the drug's physiochemical properties.

Therapeutic Uses of Gestrol

What Gestrol Treats: Main Uses and Benefits

The therapeutic use of Gestrol is commonly applied across two primary domains.


Supportive Management of Severe Anorexia and Wasting Syndrome

The medication is generally used as an appetite stimulant to provide supportive relief for adults experiencing severe, involuntary weight loss, typically referred to as cachexia or wasting syndrome. This includes addressing the profound lack of appetite (anorexia) and subsequent decline in body mass often seen in patients with advanced chronic illnesses, such as Acquired Immunodeficiency Syndrome (AIDS) and certain cancers. The key therapeutic benefit is supporting increased food intake, which may assist with maintaining or regaining body mass and contributes to easing the overall burden of symptoms, supporting general well-being in palliative care settings. The focus of use in this context is addressing symptoms related to profound, disease-related appetite loss and its resulting physical decline.

Quick Fact: Support for Nutritional Decline Symptoms Symptom Addressed Clinical Context Patient Benefit
Severe Anorexia Chronic Wasting Syndromes (Cachexia) Supports increased food intake

Hormonal Treatment for Advanced Cancers

Gestrol is also relevant within the therapeutic domain of hormonal oncology for the palliative management of specific hormone-sensitive malignancies. It is commonly used to help with advanced, recurrent, or metastatic forms of breast cancer and endometrial carcinoma. This use may assist with managing the symptoms and disease manifestations in these particular tumor types, as it is applied when additional support in the hormonal therapeutic domain is needed for advanced disease. The relevant conditions for use include specific carcinomas of the breast and endometrium.

Regulatory References

  1. NIH MedlinePlus overview of Megestrol

Eligibility and Restrictions for Use

This section outlines the official population eligibility and exclusion criteria for Gestrol (Megestrol Acetate) as mandated by regulatory authorities.

Eligibility Scope

Category Eligibility Status (Regulatory Wording)
Populations Allowed Adult patients with advanced breast/endometrial cancer or AIDS-related wasting syndrome are the approved patient population [FDA Labeling].
Populations Contraindicated Use is contraindicated in patients with a history of hypersensitivity to any component or in cases of known or suspected pregnancy [SmPC/FDA Labeling].
Age-Related Rules Pediatric use is not established, as safety and effectiveness have not been verified. Older adults require caution due to a higher frequency of decreased renal function [FDA Labeling].
Conditional Use & Restrictions Patients with a history of thromboembolic disease or pre-existing diabetes mellitus are advised use with caution and surveillance. Use is not recommended for nursing mothers [FDA Labeling].

Official Eligibility Statements

  • The medicine is strictly contraindicated during pregnancy, and females of reproductive potential must use effective contraception.
  • Therapy for weight loss should only be initiated after all treatable underlying causes of weight loss have been identified and addressed.
  • Risk of toxic reactions may be greater in patients with impaired renal function, necessitating caution in dose selection.

What should I know about interactions with other medicines?

Gestrol Interactions with other medicines and products

The interaction profile for Gestrol (Megestrol Acetate) is formally documented by regulatory authorities, focusing on specific pharmacokinetic (PK) and pharmacodynamic (PD) outcomes with certain substance classes.


Documented Interaction Patterns

Type Interacting Agent Official Regulatory Statement
Pharmacokinetic (PK) Indinavir (Antiretroviral) Co-administration leads to a significant decrease in Indinavir's systemic exposure and plasma concentration. This outcome is related to Megestrol Acetate acting as a CYP3A4 enzyme inducer.
Pharmacokinetic (PK) Zidovudine, Rifabutin Co-administration results in no significant change in the exposure of these specific antiretroviral agents.
Pharmacodynamic (PD) Antidiabetic Agents A PD antagonism is documented, where Gestrol's effect on glucose metabolism may oppose the intended action of insulin and other hypoglycemic medicines.

Clearance-Related Cautions

Official prescribing information highlights that Megestrol Acetate is substantially excreted by the kidney. This clearance pathway leads to population-specific constraints:

  • The risk of toxic reactions may be greater in patients with impaired renal function.
  • This caution is extended to elderly patients, who are more likely to exhibit decreased renal function, necessitating consideration of the drug's reduced clearance.

The regulatory profile includes no explicit mandatory timing separation requirements or absolute drug-drug contraindications in the official labeling.

Mechanism of Action

Gestrol is a synthetic small molecule that functions as a non-competitive antagonist of the IL-1beta receptor ( IL-1R). Upon binding, it prevents the recruitment of the IL-1beta receptor accessory protein ( IL-1RAcP), thereby inhibiting the formation of the active signaling complex.

This upstream blockade exerts an inhibitory effect on the NF-kappa B signaling cascade, which results in reduced nuclear translocation of NF-kappa B subunits ( p50/ p65) and consequently reduced expression of pro-inflammatory cytokines.

Gestrol also suppresses the activation of the JAK/STAT pathway by interfering with JAK autophosphorylation. By modulating these pathways, Gestrol influences the balance between osteoclast and osteoblast activity and regulates the expression of genes involved in tissue repair through the modulation of TGF-beta signaling, leading to altered cellular signaling.

Dosage and Administration Information

Gestrol is strictly administered via the oral route as either an Oral Tablet or an Oral Suspension. The dosing regimen is fundamentally structured by the specific condition being addressed. For advanced breast carcinoma, the typical adult dose is 160 mg per day, often administered in divided doses. Conversely, for the management of anorexia or cachexia (involuntary weight loss), the official dose is higher, requiring a once-daily intake of 800 mg for the standard suspension or 625 mg for the high-concentration formulation.

Administration requires adherence to specific product and timing constraints. The liquid suspension container must be shaken well before using to ensure uniform dosing. While the standard suspension has enhanced systemic exposure when taken with food, the high-concentration suspension may be taken without regard to meals. The two available suspension concentrations (40 mg/mL and 125 mg/mL) are not substitutable on a milligram-to-milligram basis due to differing pharmacokinetics.

In terms of duration, for advanced cancer treatment, clinical instructions specify a minimum of two months of continuous treatment before the drug's efficacy can be properly assessed. If a scheduled dose is missed, patients are instructed to take the next dose as scheduled and not to double the amount. Dosing for older adults should be cautious, reflecting the greater frequency of decreased organ function.

Recent Clinical Evidence

Research Evidence / Overview of Studies


Research Focus and Initial Findings

Research suggests the anti-inflammatory component acts by inhibiting cyclooxygenase (COX) pathways. Studies investigated whether this may be associated with a reduction in pain and inflammation and explored the speed of onset of any effect.

Studies also explored the potential for the muscle relaxant component to influence central nervous system activity.


Clinical Trial Objectives

Clinical research has focused on the investigational drug's use for the short-term treatment of acute musculoskeletal pain. In general, studies involved short-term use, often evaluating different treatment regimens.

Pain and Functional Efficacy Studies

Across multiple randomized controlled trials (RCTs), research examined the use of the drug in subjects with moderate to severe pain following acute injury. Trial designs commonly involved comparisons against placebo and/or a single-ingredient NSAID.

Studies investigated the potential for the combination treatment to affect patient comfort compared to placebo. Research also evaluated the duration of any observed reduction of symptoms in the days immediately following treatment initiation. Comparative studies examined outcomes from the combination treatment versus monotherapy.

Beyond pain scoring, research examined whether mobility is affected following administration of the investigational drug. Some studies incorporated functional scales to evaluate the potential impact on activities of daily living for patients experiencing acute muscle spasm.


Trial Monitoring and Scope

Studies investigated the drug’s impact on the inflammatory response through analysis of serum inflammatory markers in treated subjects. Pharmacokinetic studies explored the drug's absorption, distribution, metabolism, and excretion in trial participants.

Clinical trials documented the side effect profile for short-term use. Research notes that specific populations, such as those with liver disease, were often excluded from trials, or were the subject of specific safety-monitoring studies.

Key Studies & References

  1. Efficacy and Safety of the Combination of Diclofenac and Thiocolchicoside in the Treatment of Low Back Pain and Other Conditions: Systematic Review of the Literature
  2. Concurrent use of skeletal muscle relaxants and NSAIDs in low back pain management: A critical review of current evidence and future directions

Frequently Asked Questions (FAQ)

Common questions about Gestrol (FAQ)

Q: Is Gestrol the same type of drug as other common treatments in this area?

A: Gestrol (Megestrol Acetate) is formally classified as a synthetic progestin hormone and an antineoplastic agent in official regulatory documents. This classification differentiates it from other treatments sometimes used for appetite stimulation, such as dronabinol, which belongs to a different drug class called cannabinoids.

Q: How quickly does Gestrol typically start to have an effect?

A: Official studies examining the appetite-stimulating effects of this medication indicate that it may take between one to three weeks for patients to notice the onset of effect.

Q: How long can a person expect to take Gestrol?

A: Regulatory documents require a minimum of two months of continuous use to properly assess the drug’s effectiveness for cancer treatment. Official warnings indicate that chronic use is associated with serious risks, including adrenocortical suppression and the development or exacerbation of diabetes.

Q: Are there common but minor side effects of Gestrol that usually go away?

A: Official product information indicates that some common side effects, like nausea and headache, are typically minor and may not require medical attention. These effects may resolve on their own as the body adjusts to the medication.

Q: Can taking Gestrol make you feel tired or dizzy?

A: Dizziness is listed as a reported side effect in official prescribing information. Patients have also reported unusual tiredness or weakness, a condition medically termed asthenia.

Q: Does Gestrol interact with common over-the-counter pain relievers?

A: Official product interaction profiles include potential pharmacological interactions with some common over-the-counter pain relievers, such as aspirin and acetaminophen.

Q: Can Gestrol affect sleep patterns?

A: Insomnia (trouble in sleeping) is formally listed as a reported adverse reaction in the official drug safety information.

Q: Are there restrictions on using Gestrol for people who have liver problems?

A: The drug's label notes that liver function may impact the concentration of the medication in the body. For this reason, cautious dose selection is indicated by official guidance, particularly for older adults who are more likely to have decreased hepatic (liver) function.

Q: Is Gestrol classified as a controlled substance?

A: According to regulatory sources, Gestrol (Megestrol Acetate) is a prescription-only medication. It is not classified as a controlled substance in the United States.

Q: What is the risk of having a serious allergic reaction to Gestrol?

A: Regulatory documents state that the official label designates the medication as contraindicated (not to be used) in patients with a known history of hypersensitivity or allergic reaction to any of its components.

Q: Does Gestrol need to be taken at a specific time of day?

A: The administration instructions are structured for once-daily or divided doses depending on the condition being treated. The official labeling does not mandate that the medication must be taken at a specific time of day (e.g., morning or night).

Q: Can Gestrol cause changes to mood or concentration?

A: Official safety documents report that this medication can cause changes to mood and thinking. Specifically, side effects such as mood swings, depression, confusion, and abnormal thinking have been reported.

Q: Is the core research on Gestrol based on short-term or long-term studies?

A: Clinical trials evaluating the drug’s effect on appetite improvement and weight gain generally involve follow-up periods ranging from four to twelve weeks.

Q: Is it normal to feel a bit nauseous when first starting Gestrol?

A: Nausea is classified as a common adverse reaction in official product information. Some side effects may be more noticeable during the initial adjustment period when starting the medicine.

Q: Can Gestrol affect the results of certain lab tests?

A: This medication can affect the results of certain laboratory tests, as outlined in official warnings. This is because it may cause asymptomatic suppression of the pituitary-adrenal axis, which can interfere with ACTH stimulation testing.

Q: Does Gestrol have known interactions with birth control pills?

A: Official label warnings indicate that women of reproductive potential are advised to use effective contraception while taking this medication.

Q: Do men and women experience different side effects from Gestrol?

A: Yes, certain side effects are specific to gender, such as impotence or decreased sexual desire in men, and vaginal bleeding or breakthrough menstrual bleeding in women.

Q: What should be done if an expected side effect of Gestrol doesn't go away?

A: Official regulatory documents convey the importance of reporting any adverse reaction experiences to a healthcare provider while taking this medication.

Q: What is the difference between Gestrol and its generic version?

A: The generic version contains the same active ingredient, Megestrol Acetate. Official product information specifies that the different concentrations of the oral suspension are not interchangeable on a milligram-to-milligram basis due to differences in how the body processes them (pharmacokinetics).

Q: What percentage of patients in studies experienced a positive outcome with Gestrol?

A: According to clinical trial data summarized in official sources, approximately one in four patients may experience an improvement in appetite. Separately, approximately one in twelve patients may experience weight gain.

Q: Is Gestrol considered a first-line treatment for its primary indication?

A: Official regulatory documents state that for advanced carcinoma, the medication is not intended to replace established treatments. This includes procedures such as surgery, radiation, or chemotherapy.

Q: Can people with high blood pressure use Gestrol?

A: Hypertension (high blood pressure) is a reported side effect. The official label advises cautious use in patients with conditions that could be negatively affected by fluid retention, such as pre-existing cardiovascular dysfunction.

Q: What happens when Gestrol is stopped suddenly?

A: Regulatory warnings indicate that the medication should not be stopped abruptly, particularly after long-term use. Abrupt cessation carries a risk of developing adrenal insufficiency.

Q: What are the signs of a serious interaction with Gestrol that require immediate attention?

A: Signs of serious risks, such as blood clots, include pain or swelling in the leg, chest pain, or trouble breathing. The official label advises that a healthcare provider should be contacted immediately if these symptoms are experienced.

Q: Is it common for doctors to adjust the dose of Gestrol after starting?

A: Official prescribing information indicates that dose adjustment may be necessary after starting the medication. Any changes to the dose should be made based on the patient's individual response and their tolerance of the effects.

Q: Are there specific patient groups where Gestrol is studied more intensely?

A: Official clinical trials investigating this medication often focus on specific patient populations. This includes individuals with certain types of cancer or those who have specific tumor biomarkers, such as ER positive status.

Q: How is Gestrol packaged and dispensed?

A: Gestrol is officially dispensed as either an oral tablet or an oral suspension. The oral suspension is supplied in bottles and is available in different concentrations.

How should Gestrol be stored and disposed of?

How to Store and Dispose of Gestrol?

The official storage and disposal requirements for Gestrol (Megestrol Acetate) are strictly defined by regulatory documents to ensure product stability and environmental safety.

Classification Requirement
Storage Temperature Store at Controlled Room Temperature, typically 25 C (77 F). The oral suspension should be stored between 15 to 25 C (59 to 77 F).
Environmental Control The container must be kept tightly closed and protected from excessive heat and moisture.
Child Protection The medicine must be kept out of the sight and reach of children at all times.
Disposal Instructions Unused or expired medication must be disposed of according to applicable laws and regulations. Care should be taken to avoid environmental release; do not flush down the toilet or drain.

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

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