Dimetrose

Quick links to important sections

Medically reviewed

Marina Burgos

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 Dimetrose

This section provides a foundational overview of Dimetrose, defining its identity, chemical composition, pharmacological class, and general intended purpose.

Property Description
Active ingredient Gestrinone (INN)
Form Oral capsule
Pharmacological class Antigonadotropin, Synthetic steroid hormone
Common purpose Management of hormone-sensitive conditions
Origin Synthetic 19-norsteroid

What is Dimetrose and Its Chemical Origin?

Dimetrose is a prescription medication whose single active ingredient is Gestrinone (INN), typically supplied as an oral capsule. Gestrinone is a highly specialized, synthetic steroid hormone derivative, specifically classified as a 19-norsteroid and related to the 19-nortestosterone group. This structure is fundamental to its unique, multifaceted hormonal action. The drug is utilized as a single-entity product, focusing its therapeutic effect entirely on the properties of Gestrinone following systemic absorption via the oral route of administration.

Pharmacological Classification and General Purpose

Dimetrose is formally classified as an Antigonadotropin, a category within the broader group of Synthetic steroid hormones. The core general purpose of this medication is to achieve hormonal quietude by suppressing the central hormone signals (gonadotropins) that stimulate the ovaries. This antigonadotropic action is clinically recognized for its ability to create a hypoestrogenic environment. This means the medication is fundamentally designed to reduce the activity and proliferation associated with abnormal tissue growths driven by reproductive hormones.

How Gestrinone Differs from Simple Progestins

Gestrinone's functional profile differs from simple progestins due to its distinct, dual mechanism: it functions as an antiprogestin while simultaneously exerting a potent functional antiestrogen effect. This multi-receptor hormonal modulation is what confers its specialized ability to promote endometrial atrophy—the quieting and reduction of activity in hormone-sensitive tissues—providing a targeted approach to managing hormone-driven discomfort.

What side effects are possible with Dimetrose?

Possible Side Effects and Safety Information

The safety profile of Dimetrose (Gestrinone) is primarily characterized by adverse reactions stemming from its antiestrogenic and androgenic hormonal activity, as documented in regulatory sources.

Frequency and System-Organ Effects

Adverse reactions that are frequently encountered, often classified as Very Common or Common, include those related to hormonal shifts. These include amenorrhea (absence of menstruation), seborrhea (oily skin), and acne. Other effects commonly documented include weight gain, hot flushes (hot flashes), and a reduction in breast size (breast hypoplasia).

Adverse effects are documented across several System-Organ Classes, notably Skin and Subcutaneous Tissue Disorders (acne, hirsutism, alopecia) and Metabolism and Nutrition Disorders (weight gain, changes in lipid profile, specifically a decrease in HDL cholesterol).

Serious Safety Considerations and Regulatory Constraints

Regulatory documentation highlights the potential for a few significant, sometimes irreversible physical changes, such as voice deepening and clitoral enlargement. Additionally, the medication is associated with Hepatobiliary Disorders, including documented elevations in liver transaminases (ALT/AST), which necessitates monitoring.

Strict contraindications for Dimetrose are specified in regulatory labels. The medication is not to be used during pregnancy due to the risk of fetal harm, including the potential for fetal masculinization. It is also contraindicated in individuals with severe liver disease, severe cardiac disease, or chronic kidney disease. Its use is restricted in patients who have experienced certain metabolic or vascular disorders during prior hormonal therapies.

Overdose and Emergency Response

Dimetrose Overdose and when to seek help

The official regulatory documents define the overdose profile of Dimetrose (Gestrinone) based on a low acute toxicity risk, meaning that acute ingestion is generally unlikely to produce serious or life-threatening reactions.

Category Official Regulatory Statement
Documented overdose presentations Symptoms are typically restricted to an exaggeration of known pharmacological effects, primarily manifested as menstrual disturbances (e.g., irregular bleeding, amenorrhea).
Physiological systems affected Primarily the hormonal and reproductive systems. Acute serious systemic effects are not anticipated by regulators.
When immediate medical help is required Seek immediate medical attention for any suspected or confirmed substantial acute ingestion.

Official overdose statements:

  • No specific antidote is known for Gestrinone overdose.
  • Management is specified as symptomatic and supportive treatment.
  • Gastric decontamination procedures (e.g., activated charcoal) may be considered in the event of recent, large-volume ingestion.
  • Hospital monitoring and observation for an appropriate period may be required following substantial ingestion.
  • No specific increased severity or management adjustments for overdose are explicitly documented for unique populations.

Connection to the overall overdose profile

Regulatory authorities define the overdose profile primarily by stating that no specific antidote is available, which constrains management to supportive measures and clinical observation. Due to the low acute toxicity profile, manifestations are typically confined to hormonal disruptions. Authorities mandate that immediate medical attention must be sought for any substantial acute ingestion to ensure professional observation and implementation of supportive procedural steps.

Therapeutic Uses of Dimetrose

What Dimetrose Treats: Main Uses and Benefits

The primary therapeutic goal of Dimetrose (Gestrinone) is to provide supportive symptomatic relief in conditions where symptoms may intensify temporarily. The medication is applied across domains where additional symptomatic support is needed.

Dimetrose may be part of symptomatic management in conditions characterized by periods of heightened symptoms, such as Endometriosis, Uterine Fibroids (Leiomyomas), and Fibrocystic Breast Disease. It is used for managing symptoms related to physical discomfort, including menstrual pain (dysmenorrhea), pelvic pain, and symptoms related to systemic imbalance (such as heavy bleeding). By supporting the management of these distressing manifestations, the therapy contributes to improved comfort and assists with maintaining functional stability during symptomatic periods.

This treatment is relevant in contexts marked by increased discomfort or tension associated with hormone-driven pathologies. It is an approach that plays a role in managing symptoms that interfere with daily functioning by easing the physical burden of disease.

“The therapy is designed to address symptom clusters that may become intense or disruptive, offering a period of greater clinical stability.”

Quick Fact: Relief for Chronic Pelvic Pain
This medication is commonly used to help with symptoms that create noticeable physiological strain and interfere with daily functioning.

Regulatory References

  1. Gestrinone Overview in the NIH MeSH Database

Eligibility and Restrictions for Use

Who can and cannot use Dimetrose? — Official Regulatory Information

Dimetrose (a synthetic steroid related to Gestrinone) is subject to strict eligibility rules documented in regulatory labeling. The medicine is primarily intended for use only in adult women who are not subject to any contraindications.


Contraindications (Must Not Use)

The medicine is absolutely contraindicated for specific populations due to significant safety concerns or lack of established data:

  • Physiological Status: Individuals who are pregnant or breastfeeding must not use this medicine.
  • Age: Use is contraindicated in children and adolescents under 18 years of age.
  • Hypersensitivity: Patients with a known allergy or hypersensitivity to Dimetrose or its components.
  • Pre-existing Conditions: Individuals with severe, active liver disease, chronic kidney disease, or a history of severe cardiovascular/arterial thromboembolic disorders (e.g., recent myocardial infarction) are excluded from use.

Restricted/Limited Use

Regulatory documents specify that use may be limited or require special consideration for patients with moderate renal impairment or those with a history of metabolic/vascular disorders linked to prior hormonal therapy. The treating physician must assess eligibility against these documented restrictions.

What should I know about interactions with other medicines?

Interactions with other medicines and products

This section describes the formally documented interaction patterns for Dimetrose (Gestrinone) as defined in government regulatory sources, focusing on pharmacokinetic alterations and pharmacodynamic conflicts.

Classification Interacting Entity / Class Official Regulatory Statement Focus
Pharmacokinetic Strong Hepatic Enzyme Inducers (e.g., Rifampin, Oxcarbazepine, Phenytoin) Co-administration enhances the metabolism of Gestrinone, leading to a reduction in Dimetrose plasma concentration and decreased clinical exposure.
Strong Hepatic Enzyme Inhibitors (e.g., Atazanavir, Amprenavir) These agents decrease Gestrinone clearance, resulting in an increase in Dimetrose serum concentration and systemic exposure.
Pharmacodynamic Other Hormonal Preparations (e.g., Estrogens, Progestins, Oral Contraceptives) Gestrinone’s strong anti-hormonal activity (antiprogestin, antiestrogen) may antagonize the therapeutic effects of co-administered hormonal agents.
Herbal Products St. John's Wort Due to its enzyme-inducing properties, St. John's Wort may similarly reduce Gestrinone plasma concentrations, consistent with the risk posed by prescription enzyme inducers.

Interaction-Related Restrictions and Constraints

The primary interaction structure is defined by its susceptibility to liver enzyme modulation. The regulatory profile classifies interactions with strong enzyme inducers as potentially hazardous due to the risk of decreased efficacy. No specific drug-drug combinations are universally documented as a formal interaction-based contraindication, nor are there mandatory timing separation rules (e.g., “administer X hours apart”) explicitly stated in the regulatory documentation. No specific interaction cautions are explicitly noted for elderly or renally impaired populations.

Mechanism of Action

Dimetrose functions as a non-ATP-competitive allosteric inhibitor of the mammalian Target of Rapamycin (mTOR), primarily targeting the mTOR Complex 1 (mTORC1).

This interaction is mediated by the binding of Dimetrose to its intracellular receptor, the immunophilin FK506-binding protein 12 (FKBP12), forming a drug-protein complex that then engages mTORC1. The binding event at an allosteric site disrupts the kinase activity of mTORC1. Intracellularly, this inhibition suppresses the phosphorylation and activation of key downstream effectors, including S6 kinase (S6K) and eukaryotic initiation factor 4E-binding protein 1 (4E-BP1). The reduced phosphorylation of these substrates results in the repression of protein synthesis and the inhibition of ribosome biogenesis. Downstream signaling also impacts the transcription factor HIF-1 alpha (Hypoxia-Inducible Factor 1 alpha). System-level physiological consequences involve the modulation of cellular proliferation, cell cycle progression, and cellular metabolism across affected tissues.

Dosage and Administration Information

How to Use Dimetrose

Dimetrose (Gestrinone) is administered according to a specific, non-daily, time-bound protocol. Administration typically follows parameters regarding route, dose, frequency, and duration.


Administration Scope

Feature Usage Parameters
Route of administration: Primarily Oral (Capsule/Tablet). Vaginal and Subcutaneous (Implant) routes are also documented in clinical use.
Dosing schedule: The standardized oral dose is 2.5 mg of Gestrinone per administration. Alternative doses, such as 1.25 mg and 5.0 mg, have also been utilized.
Frequency pattern: The medication is taken Twice Weekly (biweekly), often on non-consecutive days, to maintain consistent systemic concentrations.
Special conditions: Administration is typically initiated at the beginning of the menstrual cycle. No dose adjustments for organ-impaired or older adult populations are explicitly specified.

Use Protocol and Duration

The entire course of therapy is structured as a fixed, short-term duration. The treatment is generally limited to a single, continuous course of 6 months (or 24 weeks), after which the administration is discontinued. This fixed duration and twice-weekly frequency establish a precise, intermittent usage framework.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Dimetrose

This section describes what has been studied regarding Gestrinone (Dimetrose) and what remains uncertain, without providing any medical or clinical guidance.


Evidence for Use in Endometriosis

Research for endometriosis includes randomized controlled trials (RCTs) and systematic reviews that were designed to explore outcomes related to physical discomfort, specifically measuring pelvic pain and menstrual pain. Studies generally enrolled adult pre-menopausal women and also monitored objective markers like the size of endometriotic lesions.

Research describes patterns observed in the studies where pain scores were monitored to assess changes during the typical 6-to-9-month treatment periods. Some trials documented measurements of volume or number of endometriotic lesions. However, certainty remains low for long-term outcomes, and long-term effects are not fully established regarding how measured changes evolve years after study discontinuation. The evidence base is limited by a smaller number of recent, large-scale comparative RCTs.


Evidence for Use in Uterine Fibroids (Leiomyomas)

The available research includes open-label clinical trials and imaging studies that tracked physiological measurements such as uterine volume and instances of heavy uterine bleeding. The studies observed measurements showing a reduction in the volume of the uterus and the lesions during the treatment period. Comparative evidence is lacking against many current standard medical options, and follow-up durations were typically limited when assessing the persistence of observed changes post-treatment.


Research Gaps and Remaining Uncertainties

The evidence base has more evidence available for short-term symptom changes than for long-term maintenance. Data for certain groups remain insufficient, particularly adolescents, post-menopausal individuals, or patients with other complex health conditions. Evidence quality varies across studies, with older trials often lacking contemporary, rigorous design, which contributes to the finding that the certainty remains low regarding long-term recurrence rates. This research provides context but not individual predictions.

Key Studies & References

  1. Safety Profile of Gestrinone: A Systematic Review

Frequently Asked Questions (FAQ)

Common questions about Dimetrose (FAQ)


Q: How quickly does Dimetrose usually start working for the intended condition?

Clinical studies have examined the timeline for symptom changes following the start of treatment. Official information indicates that painful symptoms associated with the condition being managed were observed to be alleviated in the monitored patient population within eight weeks from the start of therapy.


Q: Does Dimetrose interact with any herbal supplements, such as St. John's Wort?

The official regulatory profile explicitly notes a concern about an interaction with the herbal product St. John's Wort. This is due to its enzyme-inducing properties, which can lead to a reduction in the concentration of the medication.


Q: Can taking Dimetrose lead to changes in cholesterol or blood pressure levels?

Regulatory safety reports indicate that the medication is described as being associated with effects on the body's lipid profile. This includes a decrease in high-density lipoprotein (HDL) cholesterol and an increase in low-density lipoprotein (LDL) cholesterol. Changes in blood pressure are also noted as a possible cardiovascular effect in regulatory reports.


Q: Is Dimetrose available in a generic form?

The active ingredient is Gestrinone, which is available globally from various suppliers. The final marketed oral capsule (Dimetrose) is available in countries including Europe, Australia, and Latin America, but official information states it is not currently marketed in the United States or Canada.


Q: What should be done if I experience mild, common side effects that are bothersome but not severe?

Official information states that these effects are typically monitored by a healthcare provider. A healthcare provider usually monitors for these side effects and may consider adjustments to the treatment plan as appropriate.


Q: What kind of monitoring or follow-up tests (e.g., blood work, check-ups) are usually recommended while on Dimetrose?

Official monitoring protocols typically include checks for liver function (transaminases) and the body's lipid profile (cholesterol and related fats). Additionally, levels of steroid hormones and related proteins, such as SHBG, are often monitored to assess the medication’s effect.


Q: Are there specific instructions for avoiding the sun or using sunscreen while using Dimetrose?

The risk of developing melasma (dark patches of skin on the face) is noted as a potential adverse effect. While specific instructions for sun avoidance or sunscreen use are often not detailed in public regulatory summaries, managing sun exposure is generally relevant when taking medications associated with melasma.


Q: Is Dimetrose considered a form of hormone therapy?

Yes, Dimetrose is formally classified as a synthetic steroid hormone that functions as an antigonadotropin, meaning it helps quiet the central hormone signals. Its action is described as involving androgenic, anti-estrogenic, and progestational properties.


Q: Can Dimetrose cause changes to my menstrual cycle, like spotting or the absence of periods?

Yes, changes to the menstrual cycle are frequently documented side effects. The complete absence of menstruation (amenorrhea) is a commonly reported event. Clinical trials also monitor for changes in the uterine bleeding pattern, including spotting.


Q: Is it common for Dimetrose to cause mood changes, nervousness, or depression?

Studies cited in regulatory reports have recorded psychiatric effects associated with the medication’s use. These reports include instances of emotional lability (mood swings), depression, and nervousness.


Q: How does Dimetrose compare to other medicines used for the same purpose (without making a superiority claim)?

Research explores its use relative to other hormonal treatments like Danazol and GnRH agonists. The descriptive rationale for its use is tied to its unique combination of multi-receptor hormonal modulation in managing hormone-sensitive tissues.


Q: What are the potential long-term concerns, such as effects on bone density, that are associated with taking Dimetrose?

While evidence quality varies, abnormalities in bone mineral density have been reported in some studies. Official documentation indicates that the long-term safety regarding effects after stopping the treatment are not fully established.


Q: Can Dimetrose affect the results of certain laboratory tests?

Yes, official documents indicate that the medication is known to interfere with some lab tests. Specifically, it can decrease the concentration of thyroid-binding globulin, which often leads to a decrease in serum total thyroxine (T4) levels.


Q: Does Dimetrose have any potential effects on hair growth or hair loss?

As a result of its androgenic activity, effects on hair are commonly reported side effects. These include increased hair growth (hirsutism) and scalp hair loss (alopecia).


Q: Is Dimetrose suitable for women who are close to menopause or who are postmenopausal?

The primary evidence base and initial studies for this medication focused on pre-menopausal women. Official documents note that the current evidence base is insufficient to provide general guidance on its suitability for perimenopausal or postmenopausal individuals.


Q: Is Dimetrose available in a dosage form other than a tablet or capsule?

Yes, while the oral capsule/tablet is the most common form, official documents and clinical use reports show the medication is also documented as a subdermal implant or pellet.


Q: What are the common research themes or findings associated with Dimetrose in clinical studies?

Common research themes include the relief of pelvic pain and dysmenorrhea, monitoring of androgenization side effects, effects on lipid profiles, and the consistent finding that long-term safety and efficacy remain uncertain.


Q: Is Dimetrose used to treat any other conditions besides its primary approved use?

While primarily approved for endometriosis, the medication has been explored in studies for other conditions. These include uterine fibroids (leiomyomas), hypermenorrhea (heavy menstrual bleeding), and premenstrual dysphoria.


Q: What is the half-life of Dimetrose, or how long does it generally stay in the system after a dose?

Official pharmacokinetic data indicates that the half-life of the active ingredient in plasma is approximately 24 hours. This time frame describes how long it takes for the concentration of the medication in the body to be reduced by half.


Q: How is the liver generally involved in processing or breaking down Dimetrose?

According to pharmacokinetic reports, the medication is actively metabolized and broken down in the liver. This process mainly occurs through hydroxylation, which converts the active ingredient into conjugated metabolites.


Q: What is the risk of developing dark patches of skin on the face (melasma) while using Dimetrose?

Official regulatory documents list melasma as a potential adverse effect associated with the use of the drug. However, the available public regulatory summaries do not state a specific frequency or risk percentage for the development of this condition.


Q: Does taking Dimetrose cause changes in my body's own natural hormone levels?

Yes, its action is described as centrally affecting hormone signaling. It works by suppressing the release of gonadotropins (LH and FSH), which in turn reduces circulating estrogen levels. It also causes a decrease in the level of Sex Hormone-Binding Globulin (SHBG).


Q: What is meant by the drug having both progestogenic and antiprogestogenic activity?

The medication is described as having complex hormonal activity. It is structurally similar to certain hormones and can exhibit progestogenic activity in some systems, but its dominant action is described as an antiprogesterone effect on certain target tissues.


Q: Is Dimetrose used to prevent pregnancy or as an emergency contraceptive?

While the medication was historically studied for potential contraceptive uses, its primary approved clinical use is for the management of hormone-sensitive conditions.


Q: Is Dimetrose a drug that is widely available internationally?

Official documentation confirms that the medication is marketed in a number of countries. It is available in regions including Europe, Australia, and Latin America, but it is not available in the United States or Canada.


Q: Are there any special considerations for taking Dimetrose if a patient has diabetes?

Yes, regulatory sources advise that glucose should be monitored in diabetic patients during use. This is a common precaution because hormonal agents can potentially affect the body's blood sugar regulation.


Q: What happens in the body when Dimetrose is absorbed (pharmacokinetics overview)?

Following oral administration, pharmacokinetic data indicates that the absorption is approximately 30% pm 30%. The medication is then distributed throughout the body with a volume of distribution of approximately 67 L.


Q: Why might a doctor choose Dimetrose over another medication for a patient's condition (descriptive rationale)?

The descriptive rationale is attributed to its distinctive pharmacological profile as a synthetic steroid. It is known to offer a combination of strong anti-estrogen, anti-progestin, and androgenic effects designed to quiet and reduce activity in hormone-sensitive tissue.


Q: Can Dimetrose cause issues with swallowing or stomach upset?

Studies and post-marketing surveillance reports list potential gastrointestinal side effects. These include abdominal pain and bloating. Dysphagia (difficulty swallowing) has also been reported in surveillance.


Q: Is there a maximum time frame for which official sources suggest using Dimetrose?

Yes, official documentation specifies that the course of treatment is typically limited to a fixed, continuous duration, as detailed in the 'How to Use' section.

How should Dimetrose be stored and disposed of?

How to Store and Dispose of Dimetrose

Official regulatory guidelines for Dimetrose (Gestrinone) require the medicine to be stored below 30 C (86 F).


Environmental and Container Conditions

  • Temperature and Light: Store the capsules in a cool, dark, and dry place and keep them in the original pack until administration to maintain stability. Prohibited environments include hot cars, bathrooms, and areas near a sink due to the risk of heat and dampness.
  • Child Safety: The medication must be kept strictly out of reach of children. A locked cupboard positioned at least one-and-a-half metres above the ground is the recommended storage location.

Disposal Instructions

Unused or expired Dimetrose capsules should be disposed of by asking a pharmacist for specific instructions. If a take-back program is unavailable, non-flush list medicines may be disposed of in household trash after mixing them with an undesirable substance (such as dirt) and placing them in a sealed container. All identifying information on the prescription label must be scratched out before discarding the container.

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

Available in countries:

Equivalent of Dimetrose found in:

A-Z Index: