Triptorelin Acetate/GnRH Triptorelin

Triptorelin Acetate is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH or LHRH). It is used primarily in medicine to regulate hormone production and manage hormone-sensitive conditions.

Mechanism of Action

Triptorelin works by initially stimulating the pituitary gland to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH). However, with continuous use, it leads to downregulation of GnRH receptors, which eventually suppresses LH and FSH secretion — reducing testosterone in men and estrogen in women. This hormonal suppression mimics a chemical castration effect.

Medical Uses

1. Prostate Cancer (advanced or metastatic)

   • Triptorelin reduces testosterone, which helps slow or stop cancer growth.

2. Endometriosis

   • Reduces estrogen levels to relieve pain and inflammation.

3. Uterine Fibroids

   • Helps shrink fibroids and reduce related symptoms.

4. Precocious Puberty

   • Delays early onset of puberty by suppressing hormone release.

5. Fertility Treatment (Assisted Reproduction)

   • Used to control hormonal cycles and prevent premature ovulation.

Dosage Forms

Triptorelin is available as:

• Injectable powder (Triptorelin Acetate)

• Sustained-release depot injections (monthly, 3-month, or 6-month formulations)

Common Brand Names

• Decapeptyl®

• Trelstar®

• Gonapeptyl®

Dosage Guidelines

• Varies depending on the condition.

• Typically administered intramuscularly or subcutaneously.

• For prostate cancer: 3.75 mg every 4 weeks or 11.25 mg every 3 months (depot form).

Side Effects

Initial “flare” effects:

• Temporary increase in testosterone or estrogen before suppression.

• Can cause a temporary worsening of symptoms (e.g., bone pain in prostate cancer).

Common Side Effects:

• Hot flashes

• Decreased libido

• Erectile dysfunction (men)

• Vaginal dryness (women)

• Mood changes

• Headaches

• Injection site irritation

Long-Term Use Risks:

• Bone density loss (osteoporosis)

• Hormonal imbalances

• Fatigue or metabolic changes

Bodybuilding & Off-Label Use

While Triptorelin is not approved for bodybuilding, it has been explored off-label in post-cycle therapy (PCT) to restart natural testosterone production after anabolic steroid use. However, this use is not medically recommended and carries risks due to its potent hormonal effects.

Precautions & Contraindications

• Not for use during pregnancy or breastfeeding.

• Caution in patients with cardiovascular disease, depression, or bone density issues.

• Should only be administered under medical supervision.

Legal Status

Triptorelin is a prescription-only medication in most countries and regulated due to its strong hormonal effects.