Overview
Goserelin is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH) used as a long-acting depot formulation for the treatment of hormone-sensitive cancers and certain gynecological conditions. It acts as a GnRH agonist, initially stimulating then suppressing pituitary gonadotropin secretion, leading to reduced sex hormone production.
Mechanism of Action
Goserelin is a GnRH agonist that binds to pituitary GnRH receptors, initially causing a transient increase in luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion (flare effect). With continuous administration, it downregulates GnRH receptors, leading to sustained suppression of gonadotropin secretion and subsequent reduction in ovarian and testicular steroidogenesis.
Indications
- Advanced prostate cancer (palliative treatment)
- Locally advanced prostate cancer (as an alternative to surgical castration)
- Early-stage prostate cancer (in combination with radiotherapy)
- Advanced breast cancer in pre- and perimenopausal women
- Endometriosis management
- Endometrial thinning prior to endometrial ablation for dysfunctional uterine bleeding
Dosage
3.6 mg subcutaneous implant administered every 28 days into the anterior abdominal wall. For advanced prostate cancer: 10.8 mg implant administered every 12 weeks. Must be administered by healthcare professional.
Contraindications
- Hypersensitivity to GnRH analogs or any component of the implant
- Pregnancy
- Breastfeeding
- Undiagnosed abnormal vaginal bleeding
Side Effects
- Hot flashes
- Decreased libido
- Impotence
- Gynecomastia
- Sweating
- Headache
- Depression
- Insomnia
- Bone pain
- Peripheral edema
- Nausea
- Injection site reactions
- Weight changes
- Arthralgia
- Vaginal dryness
- Amenorrhea
Interactions
- No clinically significant drug interactions identified in pharmacokinetic studies
- Theoretical interactions with other drugs affecting pituitary-gonadal axis