Peptide Library / Detail
Triptorelin
Half-life
3-5 hours for immediate-release; sustained-release depot formulations provide therapeutic levels for 1-3 months
Delivery
Subcutaneous or intramuscular injection, available as immediate-release solution or long-acting microsphere depot formulations
Dosage
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Description
Triptorelin is a synthetic decapeptide analogue of gonadotropin-releasing hormone (GnRH) that acts as a potent agonist. It is primarily used in clinical settings to suppress sex hormone production through continuous administration, leading to a reversible medical castration effect. The peptide has applications in treating hormone-sensitive conditions including endometriosis, prostate cancer, precocious puberty, and as part of assisted reproductive protocols.
Usage
Triptorelin is administered as a subcutaneous or intramuscular injection, typically in depot formulations providing sustained release over 1-3 months. For endometriosis, doses of 3.75mg monthly are standard. In precocious puberty, dosing is weight-based and administered every 4 weeks. Microsphere formulations offer extended-release profiles for improved patient compliance. Stimulation tests using triptorelin (0.1mg) are used diagnostically to assess gonadotropin response in suspected central precocious puberty.
Mechanism of Action
Triptorelin binds to GnRH receptors in the anterior pituitary gland, initially causing a surge in luteinizing hormone (LH) and follicle-stimulating hormone (FSH). However, continuous exposure leads to receptor downregulation and desensitization, resulting in suppressed gonadotropin secretion and subsequent reduction in sex steroid production (testosterone and estrogen). This creates a reversible hypogonadal state that persists during treatment and reverses after discontinuation.
Benefits(7)
- Effective treatment for endometriosis with demonstrated efficacy in reducing pain and lesions
- Androgen deprivation therapy for hormone-sensitive prostate cancer
- Management of central precocious puberty in children
- Synchronization of ovulation in assisted reproductive technology protocols
- Reversible suppression of sex hormone production
- Available in long-acting microsphere formulations for monthly dosing
- Established safety profile in both adult and pediatric populations
Side Effects(8)
- Hot flashes and vasomotor symptoms due to estrogen/testosterone suppression
- Bone mineral density reduction with prolonged use
- Mood changes, depression, and emotional lability
- Decreased libido and sexual dysfunction
- Cardiovascular effects including potential QT prolongation
- Injection site reactions
- Headaches and dizziness
- Metabolic changes including weight gain and altered lipid profiles