Triptorelin is a synthetic decapeptide analogue of Gonadotropin-Releasing Hormone (GnRH). The 22.5mg formulation is a long-acting, sustained-release depot injection, typically administered intramuscularly every 3 months (12 weeks). It acts as a potent GnRH agonist, initially stimulating then profoundly suppressing the pituitary-gonadal axis, leading to a chemical castration effect. It is a cornerstone in the management of hormone-sensitive cancers and central precocious puberty in the Indian context.
Adult: 22.5 mg as a single intramuscular injection every 12 weeks (3 months). For prostate cancer, treatment is usually continuous.
Note: For intramuscular use ONLY. Reconstitute the microsphere powder with the provided sterile diluent (typically 2ml of water for injection). Shake the suspension well until it appears milky and uniform. Administer immediately via deep intramuscular injection into the gluteal region. Do not inject intravenously. Rotate injection sites.
Triptorelin is a superagonist analogue of endogenous GnRH. Upon continuous administration, it binds with high affinity to GnRH receptors on pituitary gonadotroph cells. Initial agonistic action causes a surge in Luteinizing Hormone (LH) and Follicle-Stimulating Hormone (FSH) release ('flare effect'). With sustained receptor stimulation, it leads to profound down-regulation and desensitization of GnRH receptors, resulting in a sustained suppression of LH and FSH secretion. This, in turn, drastically reduces gonadal production of sex steroids (testosterone in males, estradiol in females).
Pregnancy: CONTRANDICATED - Category X. May cause fetal loss or teratogenic effects based on mechanism. Exclude pregnancy before starting. Advise use of non-hormonal contraception during and for some time after treatment.
Driving: May cause fatigue, dizziness, or visual disturbances. Patients should be cautioned about operating machinery or driving until they know how the drug affects them.
| Other Androgen-blocking therapies (e.g., Bicalutamide, Flutamide) | Additive therapeutic effect in prostate cancer. Often used initially to block 'flare'. | Moderate |
| Drugs that prolong QT interval (e.g., Class IA/III antiarrhythmics, certain antipsychotics, antibiotics) | Increased risk of life-threatening cardiac arrhythmias (Torsades de Pointes). | Major |
| Corticosteroids (e.g., Dexamethasone) | May suppress the pituitary-adrenal axis and potentially interfere with the action of GnRH agonists. | Moderate |
| Hormonal Contraceptives | Not reliable during triptorelin therapy for endometriosis/fibroids. Use non-hormonal barrier methods. | Moderate |
Same composition (Triptorelin (22.5mg)), different brands: