Loading...
Loading...
Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Gonadotropin [EPC]
Androsterone is an endogenous steroid hormone and an unmasked metabolite of testosterone, classified within the androgen and gonadotropin pharmacological classes. It functions primarily as a weak androgen receptor agonist and a potent modulator of the GABA-A receptor complex.
Name
Androsterone
Raw Name
ANDROSTERONE
Category
Gonadotropin [EPC]
Drug Count
3
Variant Count
3
Last Verified
February 17, 2026
About Androsterone
Androsterone is an endogenous steroid hormone and an unmasked metabolite of testosterone, classified within the androgen and gonadotropin pharmacological classes. It functions primarily as a weak androgen receptor agonist and a potent modulator of the GABA-A receptor complex.
Detailed information about Androsterone
This page is for informational purposes only and does not replace medical advice. Consult a qualified healthcare professional before using any medication containing Androsterone.
Androsterone (3α-hydroxy-5α-androstan-17-one) is an endogenous steroid hormone, a neurosteroid, and a pheromone that belongs to the pharmacological class of Androgens [EPC] and is closely associated with Gonadotropin [EPC] and Progesterone [EPC] pathways. Historically, androsterone holds a significant place in endocrinology as the first mammalian steroid hormone to be isolated in pure crystalline form by Adolf Butenandt in 1931. While it is naturally produced in the human body as a metabolite of testosterone and dihydrotestosterone (DHT), its clinical application involves its role as a biomarker for androgenic activity and its potential therapeutic implications in hormonal replacement and neurological modulation.
Androsterone belongs to a class of drugs called androgens, which are essential for the development and maintenance of male secondary sexual characteristics. In the context of the FDA (U.S. Food and Drug Administration) and international regulatory bodies, androsterone is primarily recognized as a metabolite, though its parent compounds (like testosterone) are widely approved for clinical use. It is important to note that androsterone itself is often studied for its 'backdoor pathway' in steroidogenesis—a process where androgens are synthesized without the intermediate step of testosterone. This pathway is particularly relevant in certain clinical conditions like congenital adrenal hyperplasia (CAH) and polycystic ovary syndrome (PCOS).
Androsterone functions through a dual mechanism of action that distinguishes it from more potent androgens like DHT. At the molecular level, it acts as a weak Androgen Receptor Agonist [MoA]. When androsterone binds to the androgen receptor (AR) in the cytoplasm, it triggers the translocation of the receptor into the nucleus, where it modulates the transcription of specific genes involved in protein synthesis and cellular growth. However, its binding affinity is significantly lower than that of testosterone, making its systemic androgenic effects relatively mild.
Beyond the androgen receptor, androsterone is a potent positive allosteric modulator of the gamma-aminobutyric acid type A (GABA-A) receptor. This neurosteroid activity is a critical component of its pharmacological profile. By enhancing the inhibitory effects of GABA, the primary inhibitory neurotransmitter in the central nervous system, androsterone may exert anxiolytic (anti-anxiety), sedative, and anticonvulsant effects. This dual role—acting as both a traditional steroid hormone and a neuroactive steroid—makes it a subject of intense research in both endocrinology and psychiatry.
Understanding the pharmacokinetics of androsterone is essential for evaluating its clinical impact and potential for therapeutic monitoring.
While androsterone is not typically prescribed as a standalone primary therapy in the same manner as testosterone cypionate, its clinical relevance is found in several areas:
Androsterone is available in several forms, primarily for research and specialized clinical use:
> Important: Only your healthcare provider can determine if Androsterone or related androgenic therapies are right for your specific condition. Never attempt to self-administer hormonal treatments without professional medical supervision.
Dosage for androsterone varies significantly based on the clinical objective (e.g., diagnostic testing vs. experimental therapeutic use). Because it is a weak androgen, doses are often higher than those of more potent steroids when used for systemic effects.
Androsterone is generally NOT approved for pediatric use. The introduction of exogenous androgens in children can lead to severe developmental issues, including:
If a child is accidentally exposed to androsterone (e.g., through secondary contact with a caregiver's topical gel), a pediatric endocrinologist must be consulted immediately.
Patients with significant renal (kidney) impairment may experience a buildup of androsterone metabolites, particularly androsterone glucuronide. While specific dose-adjustment scales do not exist for this metabolite, healthcare providers typically exercise extreme caution and may reduce doses by 25-50% in patients with a GFR (glomerular filtration rate) below 30 mL/min.
The liver is the primary site for the metabolism and conjugation of androsterone. In patients with cirrhosis or hepatitis, the clearance of the hormone is significantly reduced. This can lead to increased systemic levels and a higher risk of side effects. Treatment is generally avoided in severe hepatic impairment (Child-Pugh Class C).
Older adults may be more sensitive to the effects of androgens. There is an increased risk of prostatic hyperplasia (enlarged prostate) and cardiovascular complications. Healthcare providers often start at the lowest possible dose and monitor prostate-specific antigen (PSA) levels closely.
If prescribed or used under clinical supervision, follow these guidelines:
If you miss a dose, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and resume your regular schedule. Do not double the dose to catch up, as this can cause acute hormonal fluctuations and increase the risk of side effects.
Signs of an acute overdose of androsterone may include:
In the event of a suspected overdose, contact your local poison control center or seek emergency medical attention immediately. While acute toxicity is low, chronic over-administration can lead to serious cardiovascular and hepatic complications.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop taking this medication without medical guidance, as sudden changes can disrupt your endocrine balance.
As an androgenic steroid, androsterone can cause several common side effects, particularly when used at supraphysiological doses. These include:
> Warning: Stop taking Androsterone and call your doctor immediately if you experience any of these serious symptoms:
Prolonged use of androsterone or related androgens can lead to permanent physiological changes:
While androsterone itself may not have a specific standalone black box warning, it falls under the class-wide FDA warnings for Androgens.
Secondary Exposure Warning: Topical androgen products carry a black box warning regarding the risk of virilization in children. Children who come into contact with unwashed or uncovered application sites can develop enlarged genitalia, premature pubic hair, increased libido, and aggressive behavior. Healthcare providers advise strictly covering the application site and washing hands thoroughly after use.
Report any unusual symptoms or persistent side effects to your healthcare provider immediately. Monitoring through regular blood tests is essential for long-term safety.
Androsterone is a potent biological agent that influences multiple organ systems. It should only be used under the strict supervision of a qualified healthcare professional, such as an endocrinologist. Patients must be screened for pre-existing hormonal imbalances, cardiovascular risks, and malignancies before initiating therapy.
No specific FDA black box warning exists exclusively for androsterone, as it is primarily a metabolite. However, as an Androgen [EPC], it is subject to the class-wide warning regarding Secondary Exposure to Testosterone/Androgen Gels. This warning emphasizes that accidental exposure in children can lead to premature puberty and bone growth issues. Patients using topical forms must ensure the application site is covered with clothing and that they wash their hands immediately after application.
To ensure safety, your healthcare provider will require the following tests:
Because androsterone acts as a neurosteroid and modulates GABA-A receptors, it may cause drowsiness, dizziness, or sedation in some individuals. Do not drive or operate heavy machinery until you know how this substance affects you.
Combining alcohol with androsterone is generally discouraged. Alcohol can exacerbate the liver strain caused by steroids and may increase the sedative effects of androsterone's GABAergic activity. Furthermore, chronic alcohol use can lower endogenous testosterone levels, complicating the clinical picture.
Do not stop taking androsterone suddenly if you have been using it long-term. Abrupt discontinuation can lead to Androgen Withdrawal Syndrome, characterized by:
Your doctor will provide a tapering schedule to allow your body's natural hormone production (the HPG axis) to recover.
> Important: Discuss all your medical conditions, especially any history of cancer, heart disease, or liver issues, with your healthcare provider before starting Androsterone.
Certain medications must never be used in conjunction with androsterone due to the risk of severe adverse events:
Androsterone can interfere with several laboratory tests:
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking. A complete medication review is the only way to prevent dangerous interactions.
Androsterone must NEVER be used in the following conditions:
Conditions requiring careful risk-benefit analysis include:
Patients who have demonstrated hypersensitivity to other androgens (such as testosterone, nandrolone, or oxandrolone) are at a high risk of cross-allergic reactions. Furthermore, those with allergies to specific carrier oils (e.g., sesame, peanut, or cottonseed oil) used in injectable formulations must avoid those specific products.
> Important: Your healthcare provider will evaluate your complete medical history, including any history of cancer or organ failure, before prescribing Androsterone.
Androsterone is contraindicated in women who are or may become pregnant. It is categorized as Category X by the FDA. Exposure during pregnancy, especially during the first trimester, can cause the female fetus to develop male physical traits (virilization), including clitoral hypertrophy and labial fusion. If pregnancy occurs while taking this medication, it must be discontinued immediately, and the patient should be counseled on the potential risks to the fetus.
It is not known whether androsterone is excreted in human milk. However, because of the potential for serious adverse reactions in nursing infants—including alterations in growth and development—a decision should be made whether to discontinue nursing or discontinue the drug. Most healthcare providers recommend avoiding androgen therapy entirely while breastfeeding.
Safety and effectiveness in pediatric patients have not been established. The primary concern in children is the acceleration of bone maturation without a corresponding increase in linear growth, resulting in permanent short stature. If used for specific rare conditions (like constitutional delay of growth), it must be monitored by a pediatric endocrinologist with frequent X-rays of the hand and wrist to monitor bone age.
Clinical studies have not included sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, elderly men are at a significantly higher risk for:
Careful dose selection and frequent monitoring are essential in this population.
In patients with renal impairment, the excretion of androsterone conjugates is diminished. While no specific GFR-based dosing guidelines exist, clinicians should monitor for signs of androgen excess and fluid retention. Dialysis does not significantly clear steroid hormones due to their high protein binding.
Androsterone is extensively metabolized by the liver. In patients with hepatic impairment (Child-Pugh Class B or C), the half-life is prolonged, and systemic exposure is increased. Use is generally contraindicated in severe liver disease and should be used with extreme caution in mild-to-moderate cases.
> Important: Special populations require individualized medical assessment. Always inform your specialist about your age, pregnancy status, and any organ-related health issues.
Androsterone acts through two distinct pathways. First, as an Androgen Receptor Agonist, it binds to the nuclear androgen receptor (AR) with a Ki of approximately 100-200 nM (significantly weaker than DHT). This binding initiates gene transcription related to male sexual development. Second, and perhaps more importantly, androsterone is a potent Positive Allosteric Modulator of GABA-A receptors. It binds to a specific site on the transmembrane domain of the GABA-A receptor, increasing the frequency and duration of the chloride channel opening in response to GABA. This results in hyperpolarization of the neuron and an overall inhibitory effect on the central nervous system.
The pharmacodynamic effects of androsterone are dose-dependent. At low doses, its neurosteroid effects predominate, potentially providing calming or sedative effects. At higher doses, its androgenic effects become apparent, including increased protein synthesis and suppression of the hypothalamic-pituitary-gonadal (HPG) axis. Tolerance to the neurosteroid effects may develop with chronic use, though the androgenic effects typically persist.
| Parameter | Value |
|---|---|
| Bioavailability | 10-15% (Oral due to first-pass); >70% (Topical/IM) |
| Protein Binding | 98% (SHBG and Albumin) |
| Half-life | 1.5 - 3 hours (Free form) |
| Tmax | 1 - 2 hours (Oral); 4-8 hours (Topical) |
| Metabolism | Hepatic (5α-reductase, UGT, Sulfation) |
| Excretion | Renal 90%, Fecal <5% |
Androsterone is classified as an Androgen [EPC], a Gonadotropin [EPC] (due to its feedback effects), and a Progesterone [EPC] derivative. It is related to other 5α-reduced androgens like Dihydrotestosterone (DHT) and Etiocholanolone.
Common questions about Androsterone
Androsterone is primarily used as a clinical biomarker to assess a patient's androgenic status and adrenal function. In a diagnostic setting, measuring its levels helps healthcare providers identify conditions such as congenital adrenal hyperplasia or androgen-secreting tumors. While not a first-line treatment for hormone replacement, it is also studied for its neurosteroid properties, which may help regulate mood and anxiety through GABA-A receptor modulation. Some research also explores its role as a human pheromone and its impact on social behavior. Always consult a specialist to understand how androsterone levels relate to your specific health profile.
The most common side effects of androsterone are related to its androgenic activity and include oily skin, acne, and mild fluid retention. Because it also acts as a neurosteroid, some users may experience changes in mood, such as increased irritability or unexpected sedation. In men, it can lead to changes in libido or mild breast tenderness if converted to estrogen. Women may notice changes in their menstrual cycle or increased body hair growth. Most of these effects are dose-dependent and may subside if the dosage is adjusted by a healthcare provider.
It is generally recommended to avoid or strictly limit alcohol consumption while taking androsterone or any androgenic steroid. Alcohol can increase the strain on the liver, which is already responsible for processing the hormone, potentially increasing the risk of hepatotoxicity. Additionally, because androsterone has sedative neurosteroid effects, alcohol can dangerously amplify these effects, leading to excessive drowsiness or impaired coordination. Chronic alcohol use also disrupts the body's natural hormone production, making it difficult for your doctor to accurately monitor your treatment. Discuss your alcohol intake honestly with your healthcare provider.
No, androsterone is absolutely not safe during pregnancy and is classified as FDA Pregnancy Category X. Exposure to this hormone during fetal development can cause permanent birth defects, most notably the virilization of a female fetus, where the baby develops male physical characteristics. Women who are pregnant, planning to become pregnant, or breastfeeding should avoid all contact with androsterone, including secondary contact with topical gels used by a partner. If you suspect you have been exposed while pregnant, seek medical advice immediately. Effective contraception is mandatory for women of childbearing age who are prescribed related androgenic therapies.
The onset of action for androsterone depends on the effect being monitored. Its neurosteroid effects on the central nervous system, such as changes in mood or anxiety levels, can occur relatively quickly, often within hours of administration. However, its androgenic effects, such as changes in muscle mass, skin oiliness, or hair growth, typically take several weeks of consistent use to become apparent. For diagnostic purposes, blood or urine levels will reflect the presence of the hormone within a few hours of a dose. Your doctor will likely wait 3 to 6 months before fully evaluating the clinical success of any long-term hormonal therapy.
You should never stop taking androsterone or any androgenic hormone suddenly without consulting your doctor. Long-term use of exogenous androgens causes the body to decrease its own natural production of hormones through a process called negative feedback. If you stop abruptly, your body may not be able to produce enough natural testosterone or other steroids immediately, leading to withdrawal symptoms like extreme fatigue, depression, and loss of libido. Your healthcare provider will typically implement a 'tapering' schedule to gradually reduce the dose, allowing your endocrine system to safely resume its natural functions.
If you miss a dose of androsterone, take it as soon as you remember, provided it is not too close to your next scheduled dose. If your next dose is only a few hours away, skip the missed dose entirely and return to your regular schedule. Never take two doses at once to make up for a missed one, as this can lead to a sudden spike in hormone levels and increase the risk of side effects like headaches or mood swings. Maintaining a consistent level of the hormone in your system is key to the effectiveness of the treatment. Using a pill organizer or phone alarm can help you stay on track.
Androsterone can cause weight gain through two primary mechanisms: muscle growth and fluid retention. As an androgen, it promotes the retention of nitrogen and the synthesis of protein, which can increase lean muscle mass over time. However, it can also cause the body to hold onto sodium and water, leading to 'water weight' and visible swelling in the extremities. While muscle gain is often seen as a positive effect in certain clinical contexts, sudden or excessive weight gain should be reported to your doctor, as it may indicate a strain on your heart or kidneys. A balanced diet and monitoring of salt intake can help manage these effects.
Androsterone can interact with a wide variety of medications, some of which can be dangerous. It is particularly known to increase the effects of blood thinners like warfarin, which can lead to an increased risk of bleeding. It may also change how your body responds to insulin or oral diabetes medications, requiring a dose adjustment to prevent low blood sugar. Other steroids, like prednisone, can increase the risk of severe swelling when taken with androgens. Always provide your healthcare provider with a full list of your current medications, including over-the-counter supplements, to ensure that androsterone is safe for you to use.
Androsterone is primarily available as a chemical compound for research and diagnostic purposes rather than a widely marketed brand-name prescription drug. Because it is a naturally occurring metabolite, it does not have the same patent status as synthetic pharmaceutical drugs. However, related androgens and the precursors used in hormonal therapy are available in both brand-name and generic forms. The availability of specific androsterone formulations may vary by country and specialized pharmacy. If your doctor prescribes a hormonal treatment, you can ask if a lower-cost generic version of the specific prescribed compound is available.