Thioderon

The name Thioderon is a brand name for the drug Mepitiostane.

Here is a detailed explanation based on available information:

The Thioderon (Mepitiostane)

• Different Name (Generic Name): Mepitiostane (INN, JAN)

• Active Form: Mepitiostane is an orally active prodrug of the steroid Epitiostanol (which is also sold under the brand name Thiodrol, and is typically administered by intramuscular injection).

• Drug Class: It is an Anabolic–Androgenic Steroid (AAS) of the dihydrotestosterone (DHT) group and an Antiestrogen.

• Medical Use (Original/Primary): It is marketed in Japan as an antineoplastic agent (anti-cancer drug) primarily for the treatment of breast cancer. It has also been used to treat anemia of renal failure and estrogen receptor-dependent meningiomas.

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Side Effects and Benefits

Benefits (Therapeutic Use):

1. Antiestrogenic Action: It acts as an antagonist (blocker) of the Estrogen Receptor (ER), which is the primary mechanism for its use in treating estrogen-dependent breast cancer and gynecomastia.

2. Anabolic Properties: As an AAS, it promotes protein synthesis and muscle growth, which can be beneficial in counteracting muscle-wasting (cachexia) often seen in cancer patients or for treating anemia of renal failure.

Side Effects (Adverse Effects):

As an AAS, it carries risks of androgenic side effects, particularly in women being treated for breast cancer, but also in men who may misuse the drug.

• Androgenic/Virilizing Effects: Acne, hirsutism (excessive hair growth), and voice changes (deepening). These are reported to be frequent with mepitiostane.

• Other Potential AAS-Related Side Effects: Like other anabolic steroids, there are general risks which can include:

  • Cardiovascular: Changes in cholesterol levels (dyslipidemia), potential impact on heart health.

  • Hepatic (Liver): While its active form (epitiostanol, and likely mepitiostane) is not a 17α-alkylated steroid (which are typically hepatotoxic), liver issues are a general concern with steroid use, and caution is advised for patients with severe hepatic impairment.

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Pros and Cons (In Context of General AAS and Antiestrogen Properties)

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Dosage and Frequency

Information on typical dosing and frequency for medical use is scarce in general public summaries. In a clinical setting, it is carefully managed and prescribed by a professional to optimize benefits and minimize side effects, with courses of treatment varying widely.

• Mepitiostane is described as orally administered.

• Its active form, Epitiostanol (Thiodrol), is typically administered via intramuscular injection.

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Half-Life and Detection Time

Half-Life:

Specific scientific data for the plasma elimination half-life of Mepitiostane or its active metabolite Epitiostanol is not readily available in public sources. For reference, most orally active anabolic steroids have half-lives ranging from a few hours to about 1-2 days.

Detection Time (How many days/weeks):

A precise detection time for Mepitiostane/Epitiostanol is not consistently published. However, like all anabolic-androgenic steroids:

• Detection times are highly variable and depend on the dose, duration of use, route of administration, and the sensitivity of the anti-doping test (e.g., in urine or hair).

• Typically, most drugs are effectively eliminated from plasma after 4−5 half-lives, but metabolites of steroids can be detectable in urine for days to several weeks or even months for certain long-ester injectables.

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Sterogenic, Progestronic, Prolactin Effects

• Estrogenic Affects (Sterogenic): Antiestrogen (Estrogen Receptor antagonist). It blocks the effects of estrogen, particularly in breast tissue. It is non-aromatizable (does not convert to estrogen).

• Progestronic Affects: There is no specific information to suggest that Mepitiostane/Epitiostanol acts as a significant progestogen (Progesterone Receptor agonist). DHT derivatives generally do not have progestogenic activity.

• Prolactin Affects: There is no specific data on a direct effect on prolactin. However, some androgen receptor (AR) agonists can indirectly influence the pituitary-gonadal axis.

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Anabolic Androgenic Ratio (AAR)

The Anabolic Androgenic Ratio (AAR) is a relative measure, usually compared to the standard reference steroid, Methyltestosterone or Testosterone propionate, which are assigned a ratio of 100:100 (or 1:1).

The literature describes the active form, Epitiostanol, as:

• Having 11 times the anabolic activity of the reference AAS methyltestosterone.

• Having approximately equal androgenic activity relative to methyltestosterone.

Assuming the reference steroid's AAR is 1:1 (100:100):

Anabolic Androgenic Ratio (AAR) for Epitiostanol:

• 1100:100 (relative to Methyltestosterone)

• 11:1 (Simplified)