Androsterone: Benefits, Side Effects and Dosage

Androsterone is a naturally occurring steroid hormone and a metabolite of testosterone. Though less well-known than its parent compound, androsterone plays intriguing roles in the body and brain, influencing everything from cognitive function to seizure threshold. This article provides a comprehensive, research-based overview of androsterone’s benefits, possible side effects, and current information on dosing, helping you understand how it works and whether it might have a place in therapeutic or supplemental contexts.

Benefits of Androsterone

Androsterone has attracted scientific interest for its potential physiological and neurological benefits. From influencing mood and cognition to modulating seizure activity, this steroid appears to be more than just a passive testosterone byproduct. Below, we summarize key findings before diving into the science behind them.

Benefit	Mechanism/Effect	Population/Model	Source
Anxiolytic	Reduced anxiety-like behavior	Rodents	1
Cognitive boost	Improved object recognition	Rodents	1
Anticonvulsant	Raised seizure threshold	Mice (epilepsy model)	3 4
Lipid lowering	Decreased serum cholesterol	Humans (IM administration)	6

Table 1: Documented Benefits of Androsterone

Anxiolytic and Cognitive-Enhancing Effects

Animal studies show that androsterone and related androgens can reduce anxiety-like behaviors and enhance cognitive performance, especially in tasks involving object recognition. These effects appear to be mediated, at least in part, by actions on estrogen receptor beta (ERβ) and GABAA/benzodiazepine receptors in the brain. Interestingly, these benefits are not observed in genetically modified mice lacking ERβ, underscoring the importance of this pathway 1.

• Reduced anxiety: In rodent models, androsterone administration led to noticeable reductions in anxiety-like behaviors, especially in the elevated plus maze test.
• Cognitive performance: Enhanced ability to recognize novel objects has been reported following androsterone treatment, suggesting potential nootropic effects 1.

Anticonvulsant Properties

Androsterone is classified as a neurosteroid, acting as a positive allosteric modulator of GABAA receptors. This mechanism is shared by many clinically used anticonvulsants. Experimental studies confirm that androsterone can raise the threshold for convulsions and enhance the protective effects of certain antiepileptic drugs, such as carbamazepine, gabapentin, and phenobarbital, in animal models of seizures 3 4.

• Seizure protection: High doses of androsterone (80 mg/kg) significantly raised the seizure threshold in mice.
• Adjunctive benefit: At lower doses, androsterone enhanced the efficacy of select antiepileptic drugs without increasing their side effects 4.

Metabolic and Lipid Effects

While most research focuses on neurological aspects, some clinical studies have explored androsterone’s impact on lipid metabolism. Intramuscular administration of androsterone in men with coronary heart disease led to significant reductions in serum triglycerides, phospholipids, and total cholesterol. However, these benefits were not observed with oral administration 6.

• Lipid-lowering effect: Only seen with intramuscular delivery, not oral.
• Potential cardiovascular benefit: Decreased β-lipoprotein fraction, though side effects limited clinical use 6.

Other Notable Effects

• Antioxidant and stress resistance in plants: Although not directly applicable to humans, androsterone has shown remarkable capacity to boost antioxidant systems and resistance to chill stress in maize seedlings. This points to its broad bioactivity across species 2.
• No evidence for sexual behavior stimulation: Androsterone did not stimulate sexual behavior or uterine growth in female rodent models, differentiating it from other androgens 11.

Side Effects of Androsterone

Like all steroid hormones, androsterone is not without risks. While some side effects are specific to its administration, others are inferred from its relationship to the broader androgen pathway. Here’s a quick summary.

Side Effect	Description	Severity/Frequency	Source
Local/systemic	Injection site reactions, systemic effects	Moderate; IM use	6
Hormonal	Androgenic/estrogenic side effects (theoretical)	Variable	5 7
No CNS/motor	No motor impairment at effective anticonvulsant doses	None observed	4

Table 2: Key Side Effects of Androsterone

Local and Systemic Side Effects

Clinical trials using intramuscular androsterone reported a high frequency of both local and systemic side effects, which ultimately limited the compound’s clinical viability for lipid lowering or other purposes 6.

• Injection site reactions: Pain, swelling, or irritation were common with IM injections.
• Systemic effects: Though not always specified, users reported enough discomfort to render routine IM use impractical 6.

Hormonal and Metabolic Effects

As a steroid hormone, androsterone may theoretically exert androgenic and/or estrogenic effects, especially at high or prolonged doses. While direct evidence in humans is limited, side effects seen with androgen manipulation (such as with androgen deprivation therapy) include:

• Reduced bone mineral density
• Changes in metabolism (weight gain, muscle loss)
• Sexual dysfunction, reduced libido
• Fatigue, hot flashes, gynecomastia

However, these effects are primarily reported for more potent androgens or anti-androgens, and specific data for androsterone at typical doses is lacking 5 7.

Central Nervous System Effects

Animal studies assessing anticonvulsant properties of androsterone found no impairment of motor coordination at doses that increased seizure threshold or enhanced antiepileptic drugs. This suggests a favorable CNS side effect profile—at least in preclinical settings 4.

• No motor impairment: Even at doses that potentiated anticonvulsant activity, mice showed no deficits in motor performance tasks 4.

Unknowns and Limitations

It is important to note that there is a lack of comprehensive, controlled trials in humans assessing long-term safety and side effect profiles of androsterone, particularly at doses used for neurosteroid effects. Most information is extrapolated from related androgens or limited trials in specific populations.

Dosage of Androsterone

Determining the optimal—and safe—dosage of androsterone is challenging, as clinical research is sparse and animal studies do not always translate directly to humans. Below is a summary of dosing regimens and outcomes from available research.

Route & Dose	Outcome	Population/Model	Source
Oral 100 mg/d	No clinical/lipid effect	Humans (CHD patients)	6
IM 50 mg/d	Lowered serum lipids; side effects	Humans (CHD patients)	6
IP 80 mg/kg	Raised seizure threshold	Mice (epilepsy model)	4
IP 40 mg/kg	Enhanced anticonvulsant drugs	Mice	4
SC (rodent, various)	Reduced anxiety, improved cognition	Mice and rats	1

Table 3: Documented Dosages and Outcomes for Androsterone

Human Dosage Data

• Oral administration: 100 mg daily for one month had minimal clinical effect in men with coronary heart disease.
• Intramuscular administration: 50 mg daily for 1–4 weeks reduced serum lipids but was associated with frequent side effects, making this route unsuitable for routine use 6.

Preclinical (Animal) Dosage

• Anticonvulsant effects: Effective dose for raising seizure threshold in mice was 80 mg/kg intraperitoneally. Lower doses (5–40 mg/kg) did not have a significant effect unless used as adjuncts to established anticonvulsants 4.
• Behavioral/cognitive effects: Doses in rodent studies varied but were generally administered subcutaneously. Positive effects on anxiety and cognition were reported, but specific translation to human dosing is unclear 1.

Considerations for Human Use

• Route of administration matters: IM injection was more effective than oral for lipid effects in humans, but with more side effects 6.
• No established therapeutic dose: There is no officially recognized dose for cognitive or anticonvulsant uses in humans.
• Lack of safety data: Long-term safety and appropriate dosing for desired neuroactive effects remain undetermined.

Conclusion

Androsterone is a fascinating but under-explored steroid hormone with notable effects on the brain and body. Here’s what we’ve learned:

• Benefits:
  • Demonstrates anxiolytic and cognitive-enhancing effects in animal models
  • Acts as a neurosteroid with anticonvulsant activity and can potentiate certain antiepileptic drugs
  • May lower serum lipid levels when given intramuscularly (though side effects limit use)
• Side Effects:
  • IM administration is associated with frequent local and systemic reactions
  • Theoretical androgenic/estrogenic side effects possible, but not well characterized for androsterone
  • No significant CNS or motor side effects observed in animal models
• Dosage:
  • Human studies used 50–100 mg daily, with limited efficacy and tolerability
  • Effective animal doses for neurological effects are much higher and may not translate safely to humans
  • No standardized or recommended dosing exists for cognitive or neuroprotective purposes

Summary:

• Androsterone shows promise as an adjunct in neurological and metabolic contexts, but its clinical use is limited by a lack of robust human data and concerns over side effects and dosing.
• Most benefits are currently demonstrated in animal studies; large-scale human trials are needed.
• Anyone considering androsterone supplementation should proceed with caution and consult healthcare professionals, as the safety profile and optimal dose remain uncertain.