androstenedione

Action and Spectrum

Actions and spectrum: 

androstenedione is an androgen hormone that is produced primarily in the adrenal glands, but also in the gonads and brain. It is a prohormone that can be converted into other androgenic hormones, such as testosterone and estrone, in various tissues of the body. 

androstenedione has anabolic properties and has been used as a dietary supplement by athletes to enhance athletic performance and increase muscle mass. It has also been used in hormone replacement therapy in women with low androgen levels, and in the treatment of men with hypogonadism.

Drug Interaction

Adverse Reaction

Frequency not defined 

Men: acne, testicular atrophy, prostate cancer risk, decreased testosterone, gynecomastia 

Women:  hirsutism, amenorrhea, clitoral hypertrophy, acne 

Adolescents: decreased adult height, early closure of growth plates 

Black Box Warning

none

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

androstenedione is not approved for any therapeutic use by the FDA, and therefore there are no official contraindications for it. However, it is classified as a Schedule III controlled substance by the United States Controlled Substances Act, which means that its use without a prescription or for non-medical purposes is illegal. Its use as a performance-enhancing drug is also prohibited by various sports organizations. 

Caution: 

androstenedione is a hormone precursor that is naturally produced in the body. While it is not associated with any black box warnings or contraindications, there are some cautions that should be considered. 

Individuals with hormone-sensitive conditions, such as breast cancer or prostate cancer, should use caution when taking androstenedione as it may increase levels of estrogen or testosterone in the body. androstenedione may also interact with medications that affect hormone levels, such as hormone replacement therapy, birth control pills, or drugs used to treat prostate cancer. 

Comorbidities: 

androstenedione is not indicated for any medical condition and is classified as a controlled substance due to its potential for abuse. Its use is not recommended in individuals with a history of substance abuse or dependence. Additionally, individuals with liver, kidney, or heart disease should use androstenedione with caution, as the effects of the supplement on these conditions are not well-established. 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: N/A 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women. 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

androstenedione is a steroid hormone precursor to testosterone and estrone. It is produced mainly in the adrenal glands, gonads, and brain. androstenedione is converted to testosterone and other androgens by the enzyme 17β-hydroxysteroid dehydrogenase (17β-HSD) in the gonads and peripheral tissues. It can also be converted to estrone by aromatase enzyme in adipose tissue, liver, and breast cancer tissue. 

The biological activity of androstenedione is mediated by binding to androgen receptors and estrogen receptors. It also has weak binding affinity for progesterone receptors. 

androstenedione has been shown to have anabolic effects, enhancing muscle mass and strength, and promoting bone growth. It also has androgenic effects, such as the development of secondary sexual characteristics, increased body hair growth, and acne. 

Pharmacodynamics: 

androstenedione is a steroid hormone that is a precursor to both testosterone and estrogen. Once absorbed, it is converted to testosterone or estrogen depending on the needs of the body.  

androstenedione also has anabolic properties and is sometimes used as a performance-enhancing drug. It increases the muscle mass, strength, and endurance in athletes.  

Pharmacokinetics: 

Absorption 

When taken orally, androstenedione is well absorbed from the gastrointestinal tract and reaches peak plasma levels within 2 hours. 

Distribution 

androstenedione is rapidly distributed into tissues, including muscle, liver, and adipose tissue. It is also converted to testosterone and estrogen, which can bind to and activate their respective receptors. 

Metabolism 

androstenedione is metabolized in the liver, where it is converted to testosterone and estrone by the enzymes 17β-hydroxysteroid dehydrogenase and aromatase, respectively. Testosterone can be further metabolized to dihydrotestosterone or estradiol. 

Elimination and excretion 

androstenedione and its metabolites are excreted in the urine and feces. The major metabolites are testosterone, androstenediol, and etiocholanolone. 

Adminstartion

Administration: 

androstenedione is available in the form of dietary supplements, and there is no recommended dosage for it. However, the typical dosage for athletic performance enhancement ranges from 100 mg to 300 mg per day, taken orally. The administration of androstenedione should always be done under medical supervision. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: androstenedione 

Pronounced: (an-druh-steen-die-own) 

Why do we use androstenedione? 

androstenedione is used to increase testosterone and estrogen levels in the body. Some athletes and bodybuilders use androstenedione as a performance-enhancing drug to build muscle mass, increase strength, and improve endurance. However, the effectiveness of androstenedione as a performance enhancer is questionable, and its use is banned by most sports organizations. androstenedione has also been studied for its potential use in the treatment of breast cancer, osteoporosis, and other conditions, but more research is needed to confirm its effectiveness.