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Wednesday, August 20, 2025

Androgens and anabolic steroids


Androgens and anabolic steroids are synthetic or natural hormones that mimic the effects of testosterone, the primary male sex hormone. These drugs play a central role in male sexual development, secondary sexual characteristics, and the regulation of protein metabolism. They are used both in legitimate medical contexts—such as hormone replacement therapy, delayed puberty, and certain muscle-wasting conditions—and inappropriately in sports and bodybuilding for performance enhancement.

This professional write-up provides an in-depth analysis of androgens and anabolic steroids, covering their mechanisms of action, therapeutic uses, commonly prescribed agents with doses, contraindications, side effects, precautions, and drug interactions.

1. Mechanism of Action

  • Androgenic effects: These hormones bind to intracellular androgen receptors, influencing gene transcription. This results in the development and maintenance of male characteristics, such as deep voice, facial hair, and increased muscle mass.

  • Anabolic effects: They stimulate protein synthesis, nitrogen retention, and bone growth, enhancing muscle development and strength.

  • Feedback suppression: Administration of exogenous androgens or anabolic steroids suppresses the hypothalamic-pituitary-gonadal axis, reducing endogenous testosterone production and spermatogenesis.

2. Therapeutic Uses

  1. Hypogonadism in men

    • Replacement therapy in primary or secondary hypogonadism to restore testosterone levels and sexual function.

  2. Delayed puberty in males

    • Short-term use can induce pubertal changes such as growth of facial hair, voice deepening, and genital development.

  3. Anemia

    • Certain anabolic steroids (e.g., nandrolone) stimulate erythropoiesis and have historically been used in anemia of chronic disease or renal failure, though now largely replaced by erythropoietin.

  4. Cachexia and muscle wasting

    • In conditions such as AIDS or cancer, anabolic steroids may be prescribed to prevent muscle loss and improve weight maintenance.

  5. Hereditary angioedema

    • Some androgens (e.g., danazol, stanozolol) reduce the frequency and severity of attacks.

  6. Breast cancer (palliative use in women)

    • Androgens have been used in certain types of breast carcinoma unresponsive to other therapies.

  7. Osteoporosis (historically)

    • Anabolic steroids were once used to enhance bone density but have been replaced by safer options like bisphosphonates.

3. Commonly Used Androgens and Anabolic Steroids (Generic Names with Doses)

3.1 Testosterone and Derivatives

  • Testosterone enanthate:

    • Intramuscular injection: 50–400 mg every 2–4 weeks for hypogonadism.

  • Testosterone cypionate:

    • Intramuscular injection: 50–400 mg every 2–4 weeks.

  • Testosterone undecanoate:

    • Oral: 120–160 mg daily in divided doses initially, then maintenance at 40–120 mg daily.

    • Intramuscular injection: 750 mg initially, followed by 750 mg after 4 weeks, then every 10 weeks.

  • Testosterone transdermal patch/gel:

    • Gel: 50–100 mg applied once daily.

    • Patch: 4–6 mg/day applied nightly.

3.2 17-Alpha Alkylated Oral Steroids

  • Methyltestosterone:

    • Oral: 10–50 mg/day for hypogonadism.

  • Fluoxymesterone:

    • Oral: 2.5–20 mg/day in divided doses for hypogonadism or delayed puberty.

3.3 Anabolic Steroids

  • Nandrolone decanoate:

    • Intramuscular injection: 50–200 mg every 2–4 weeks for anemia or wasting syndromes.

  • Oxandrolone:

    • Oral: 2.5–20 mg daily for weight gain and muscle wasting.

  • Stanozolol:

    • Oral: 2–6 mg three times daily for hereditary angioedema.

  • Danazol:

    • Oral: 200–800 mg/day in divided doses for endometriosis or hereditary angioedema.

4. Contraindications

  • Prostate or male breast cancer

  • Pregnancy or breastfeeding (teratogenic risk)

  • Severe liver disease

  • Nephrotic syndrome or nephritis

  • Hypercalcemia (risk of worsening calcium imbalance)

  • Known hypersensitivity to the active drug or formulation excipients

5. Side Effects

5.1 In Men

  • Testicular atrophy and infertility (due to suppression of gonadotropins)

  • Gynecomastia (from peripheral aromatization to estrogen)

  • Priapism (painful prolonged erections)

  • Acne, oily skin, male pattern baldness

  • Increased risk of prostate hypertrophy and prostate cancer progression

5.2 In Women

  • Virilization (deepening of voice, hirsutism, clitoral enlargement)

  • Menstrual irregularities

  • Breast atrophy

  • Male pattern baldness

5.3 In Both Sexes

  • Hepatotoxicity (especially with 17-α-alkylated oral steroids)

  • Dyslipidemia (↑ LDL, ↓ HDL) leading to increased cardiovascular risk

  • Edema, fluid retention, and hypertension

  • Polycythemia due to increased erythropoiesis

  • Psychological changes (aggression, mood swings, dependence)

6. Precautions

  • Liver function monitoring: Required in patients on long-term anabolic steroids.

  • Prostate health: Regular PSA testing and digital rectal exams for men >40 years old.

  • Cardiovascular risk assessment: Caution in patients with pre-existing hypertension, ischemic heart disease, or dyslipidemia.

  • Adolescent use: Risk of premature epiphyseal closure leading to stunted growth.

  • Pregnancy and lactation: Contraindicated due to teratogenic and virilizing effects on female fetus.

7. Drug Interactions

  • Anticoagulants (e.g., warfarin): Increased risk of bleeding due to enhanced anticoagulant effect.

  • Insulin and oral hypoglycemics: Androgens may enhance the hypoglycemic effect, requiring dose adjustment.

  • Corticosteroids: Increased risk of fluid retention and edema.

  • Cyclosporine: Potential increase in nephrotoxicity.

  • Hepatotoxic drugs: Enhanced risk of liver injury when combined with other hepatotoxic agents.

8. Clinical Considerations and Misuse

  • Sports and performance enhancement: Non-medical use is common but carries significant risks, including cardiovascular disease, liver tumors, infertility, psychiatric disorders, and dependence.

  • Withdrawal symptoms: Abrupt discontinuation after prolonged misuse can cause depression, fatigue, and hypogonadism.

  • Therapeutic monitoring: Periodic assessment of testosterone levels, hematocrit, liver enzymes, and lipid profiles is essential during treatment.

9. Emerging Alternatives

  • Selective Androgen Receptor Modulators (SARMs): Experimental agents designed to provide anabolic benefits with fewer androgenic side effects. Not yet approved for medical use but under investigation.

  • Safer testosterone formulations: Novel delivery systems (subcutaneous implants, long-acting injectables) are being developed to improve compliance and minimize fluctuations in hormone levels.




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