Goserelin

About Goserelin

• Goserelin acetate received its first U.S. Food and Drug Administration (FDA) approval on December 21, 1989. 
• Goserelin, a Gonadotropin Releasing Hormone (GnRH) agonist, is indicated for multiple medical conditions. It is used in combination with flutamide for managing locally confined prostate carcinoma and for palliative treatment of advanced prostate carcinoma. 
• Additionally, it is prescribed for the management of endometriosis and as an endometrial-thinning agent before endometrial ablation for dysfunctional uterine bleeding. 
• Furthermore, it serves as a palliative treatment option for advanced breast cancer in pre and perimenopausal women. 
• With its diverse range of indications, It plays a crucial role in addressing various health concerns effectively.
• Goserelin operates as a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH), exerting its effects as a partial agonist at the GnRH receptor. 
• By stimulating sex hormone production, including testosterone and estrogen, in a non-pulsatile manner, it disrupts natural hormonal feedback systems. Initially, this stimulation boosts the production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). 
• However, prolonged exposure prompts a down-regulation of LH and FSH production, leading to reduced levels of testosterone and estrogen. 
• This mechanism is harnessed in the treatment of hormone-sensitive cancers like breast and prostate cancer, as well as in benign gynecological conditions such as endometriosis and uterine fibroids.

Strength: 

Goserelin injection is available in strength of  3.6 mg. 

Recommended Dosage:

Prepare the patient comfortably, sterilize the area, inspect the implant, insert the needle at an angle, depress the plunger fully, withdraw the needle, and dispose of it safely. Goserelin acetate injection can be localized by ultrasound if surgical removal is needed.

• Goserelin, administered subcutaneously at a 3.6 mg dose, should be given every 28 days into the anterior abdominal wall below the navel line, following sterile techniques under a physician’s supervision. While a slight delay of a few days is acceptable, efforts should be made to adhere to the 28-day regimen.
• For Stage B2-C Prostatic Carcinoma, the treatment begins 8 weeks before radiotherapy initiation and continues during radiation therapy. Options include a Goserelin 3.6 mg depot followed by a Goserelin 10.8 mg depot, or four 3.6 mg depot injections every 28 days, with two before and two during radiotherapy.
• In advanced prostate cancer management, this medicine is typically administered long-term unless clinically unsuitable.
• For endometriosis, treatment duration is generally 6 months, with no established data supporting extended use. Retreatment isn’t recommended due to insufficient safety data, but hormone replacement therapy (estrogens and/or progestins) may help alleviate symptoms and mitigate bone mineral loss.
• As a pre-endometrial ablation agent, it is given as one or two depots, with surgery scheduled within four weeks after a single depot or within two to four weeks following the second depot.
• In advanced breast cancer management, it is generally used long-term unless clinically contraindicated.

Important:

Before initiating treatment, it is essential to inform your doctor if you are pregnant, planning to become pregnant or suspect you may be pregnant. Additionally, disclose all existing medical conditions to your doctor. Inform your doctor about all medications, including over-the-counter medicines, you are currently taking to avoid any potential adverse effects.

Warnings & Precaution:

• Do not undergo this treatment if you are hypersensitive to it or if you are pregnant unless it is being used for the treatment of advanced breast cancer.
• In considering the administration, several warnings and precautions should be heeded. Firstly, for women of childbearing potential and those considering pregnancy, it’s imperative to exclude pregnancy before using the medication for benign gynecological conditions. 
• Additionally, women are advised to avoid pregnancy during treatment. Patients may experience a transient worsening of tumor symptoms, such as ureteral obstruction and spinal cord compression, within the initial weeks of the therapy, necessitating close monitoring for complications. 
• Furthermore, men receiving GnRH analogs like Goserelin acetate may face an elevated risk of hyperglycemia and diabetes, emphasizing the importance of regular blood glucose monitoring and appropriate management. 
• The use of GnRH analogs in men has also been linked to an increased risk of cardiovascular diseases, including myocardial infarction, sudden cardiac death, and stroke, necessitating careful monitoring and management. 
• Other potential concerns include hypercalcemia, systemic hypersensitivity reactions, increased cervical resistance, and the effect on QT/QTc interval. 
• Lastly, instances of injection site and vascular injuries have been reported during the administration, highlighting the need for cautious and meticulous administration techniques.

Common Goserelin Side Effects:

The most common, clinically significant adverse reactions occurring in men include:

• Hot flashes
• Sexual dysfunction
• Decreased erections
• Lower urinary tract symptoms

Similarly, in women treated for breast cancer, dysfunctional uterine bleeding, or endometriosis, adverse events reported in over 20% of cases include:

• Hot flushes
• Headache
• Sweating
• Acne
• Emotional lability
• Depression
• Decreased libido
• Vaginitis
• Breast atrophy
• Seborrhea
• Peripheral edema

Use in Specific Population

• Goserelin acetate implant is contraindicated during pregnancy except for its use in the palliative treatment of advanced breast cancer. 
• Limited data from animal studies suggest potential fetal harm due to administration during pregnancy. It is unclear whether the drug is excreted in human milk, but it has been observed in the milk of lactating rats. 
• Considering the possibility of adverse reactions in nursing infants, a decision should be made regarding the continuation of nursing or the treatment, weighing the benefits against the risks for the mother. 
• The safety and efficacy of the drug have not been established in pediatric patients, and its use in geriatric populations, particularly in women over 65 years, has not been studied extensively. 
• While no dosage adjustments are necessary for male geriatric patients, the effects of reduced drug clearance due to renal impairment on drug efficacy and toxicity remain uncertain in females. 
• Pharmacokinetic studies in patients with renal impairment indicate no need for dose adjustment with depot formulation use. 
• Additionally, pharmacokinetic data in patients with moderate liver impairment suggest no requirement for dose adjustment, although there is limited information on patients with severe hepatic insufficiency.

Storage and Handling 

• Store at room temperature (do not exceed 25°C [77°F]).
• Keep the medicine away from pets and children.