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Triptorelin – Uses, Mechanism and Side Effects

Triptorelin is a synthetic GnRH analogue used to treat hormone-dependent conditions such as prostate cancer, endometriosis, and precocious puberty by suppressing sex hormone production.

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Things worth knowing about "Triptorelin"

Triptorelin is a synthetic GnRH analogue used to treat hormone-dependent conditions such as prostate cancer, endometriosis, and precocious puberty by suppressing sex hormone production.

What is Triptorelin?

Triptorelin is a synthetic analogue of gonadotropin-releasing hormone (GnRH), also referred to as luteinizing hormone-releasing hormone (LHRH). It is administered as a depot injection and works by significantly reducing the body's production of sex hormones. Triptorelin is marketed under several brand names, including Decapeptyl and Trelstar.

Mechanism of Action

Triptorelin binds continuously and with high affinity to GnRH receptors in the pituitary gland. Unlike natural GnRH – which is released in pulses – the sustained stimulation caused by triptorelin leads to a process called receptor downregulation. This results in:

Suppression of LH (luteinizing hormone) and FSH (follicle-stimulating hormone) secretion
A sharp reduction of testosterone levels in men (to castration levels)
A significant decrease in estrogen levels in women

At the start of treatment, a short-term temporary increase in hormone levels may occur – known as the flare-up effect – before suppression takes full effect.

Indications

Prostate Cancer

Triptorelin is widely used in androgen deprivation therapy (ADT) for advanced or metastatic prostate cancer. By lowering testosterone levels, it inhibits the growth of hormone-sensitive tumor cells.

Endometriosis

In women with endometriosis – a condition in which tissue similar to the uterine lining grows outside the uterus – triptorelin reduces estrogen levels and slows the growth of ectopic tissue, relieving pain and other symptoms.

Uterine Fibroids

Triptorelin may be used prior to surgery to reduce the size of uterine fibroids (benign muscle tumors of the uterus), making procedures safer and less complex.

Precocious Puberty

In children experiencing precocious puberty (early onset of puberty), triptorelin suppresses sex hormone production and helps restore a normal pace of physical maturation.

Assisted Reproduction

In the context of in vitro fertilization (IVF), triptorelin is used to control ovulation and prevent premature ovulation, improving the chances of successful egg retrieval.

Dosage and Administration

Triptorelin is administered as a depot injection – depending on the formulation, it may be given monthly (1-month depot), every three months (3-month depot), or every six months. The exact dosage depends on the indication and is determined by the treating physician. Self-administration is not intended.

Side Effects

Because triptorelin strongly suppresses sex hormone production, many side effects are related to hormone deprivation:

In men: hot flashes, loss of libido, erectile dysfunction, weight gain, fatigue, and osteoporosis with long-term use
In women: hot flashes, vaginal dryness, mood swings, headaches, and bone density loss
General: injection site reactions, and a temporary worsening of the underlying condition at the start of treatment (flare-up effect)

Contraindications and Precautions

Triptorelin should not be used in patients with known hypersensitivity to GnRH analogues, or during pregnancy and breastfeeding. Patients at increased risk of osteoporosis should be closely monitored during therapy and may require supplementation with calcium and vitamin D.

References

European Medicines Agency (EMA): Summary of Product Characteristics – Decapeptyl / Trelstar, www.ema.europa.eu
EAU Guidelines on Prostate Cancer, European Association of Urology (EAU), 2023.
Barbieri R.L.: Hormone treatment of endometriosis: The estrogen threshold hypothesis. American Journal of Obstetrics and Gynecology, 166(2): 740-745, 1992.

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