Goserelin


Generic Medicine Info
Indications and Dosage
Subcutaneous
Localised prostate cancer, Locally advanced prostate cancer
Adult: As an alternative to surgical castration (in locally advanced cases), adjuvant treatment to radical prostatectomy or radiotherapy, or neoadjuvant treatment prior to radiotherapy in high-risk patients: 3.6 mg every 28 days or 10.8 mg every 12 weeks. Doses to be injected into the anterior abdominal wall.

Subcutaneous
Metastatic prostate cancer
Adult: As palliative treatment in patients suitable for hormonal manipulation: 3.6 mg every 28 days or 10.8 mg every 12 weeks. Doses to be injected into the anterior abdominal wall.

Subcutaneous
Advanced breast cancer in pre- and perimenopausal women
Adult: In patients suitable for hormonal manipulation: 3.6 mg every 28 days, to be injected into the anterior abdominal wall.

Subcutaneous
Estrogen receptor positive early breast cancer in pre- and perimenopausal women
Adult: As an alternative to chemotherapy in standard care: 3.6 mg every 28 days, to be injected into the anterior abdominal wall.

Subcutaneous
Endometrial thinning
Adult: 3.6 mg as a single dose to be injected into the anterior abdominal wall 4 weeks before surgery. Alternatively, 3.6 mg for 2 doses given 4 weeks apart, followed by surgery within 2-4 weeks after the administration of the 2nd dose.

Subcutaneous
Endometriosis
Adult: 3.6 mg every 28 days, to be injected into the anterior abdominal wall. Max treatment duration: 6 months.

Subcutaneous
Pituitary desensitisation for assisted reproduction in infertility
Adult: In preparation for superovulation: 3.6 mg to be injected into the anterior abdominal wall. Monitor serum estradiol levels until they decline to levels similar to those in early follicular phase (approx 150 pmol/L) which usually takes 7-21 days.

Subcutaneous
Uterine fibroids
Adult: In combination with Fe therapy in anaemic patients: 3.6 mg every 28 days, to be injected into the anterior abdominal wall, for up to 3 months before surgery.
Contraindications
Undiagnosed vaginal bleeding. Pregnancy and lactation.
Special Precautions
Patient with congenital long QT syndrome, heart failure, frequent electrolyte abnormalities; hypertension, depression, predisposition to osteoporosis (e.g. family history of osteoporosis, chronic alcohol abusers, smokers, undergoing long-term treatment with anticonvulsants or corticosteroids), polycystic ovarian syndrome; diabetes mellitus. Patient receiving anticoagulant drugs. Obese and underweight (low BMI) patients. Male patient at risk of developing spinal cord compression or ureteric obstruction. Use of the 10.8 mg implant is not indicated for female patients.
Adverse Reactions
Significant: Inj site injury including vascular injury, pain, haematoma, haemorrhage, haemorrhagic shock; tumour flare (during initial treatment), hypercalcaemia, hyperglycaemia, loss of glycaemic control, increased cervical resistance, decreased bone mineral density, hypersensitivity reactions, antibody formation; spinal cord compression, ureteric obstruction; MI, cardiac failure, QT/QTc interval prolongation, stroke; depression, vaginal bleeding. Rarely, pituitary apoplexy.
Gastrointestinal disorders: Nausea, abdominal pain.
General disorders and administration site conditions: Asthenia, voice alteration (in females).
Hepatobiliary disorders: Hepatic dysfunction.
Investigations: Abnormal blood pressure, changes in blood count; increased weight, increased serum cholesterol.
Metabolism and nutrition disorders: Peripheral oedema.
Musculoskeletal and connective tissue disorders: Bone pain, arthralgia, myalgia.
Nervous system disorders: Headache, paraesthesia.
Psychiatric disorders: Mood changes, insomnia, nervousness. Rarely, psychotic disorder.
Reproductive system and breast disorders: Erectile dysfunction, vulvovaginal dryness, breast enlargement, gynaecomastia, breast tenderness, decreased libido, vaginitis, breast atrophy.
Respiratory, thoracic and mediastinal disorders: Pulmonary embolism, interstitial pneumonia.
Skin and subcutaneous tissue disorders: Acne, hyperhidrosis, rash, alopecia; dry skin, change of body hair (in females).
Vascular disorders: Hot flush.
SC: X (In patients w/ endometriosis & endometrial thinning), D (In patients w/ advanced breast cancer)
Monitoring Parameters
Assess pregnancy status before use. Monitor blood glucose and HbA1c periodically; bone mineral density, cholesterol/lipids. Consider monitoring of ECG and electrolytes periodically. Monitor for tumour flare, weakness, paraesthesia, urinary tract obstruction, and spinal cord compression in the 1st few weeks of therapy (particularly in prostate cancer patients). Assess for signs and symptoms of abdominal haemorrhage after administration.
Drug Interactions
May increase the risk of QT interval prolongation with drugs known to prolong QT interval or induce torsade de pointes (e.g. class Ia [e.g. quinidine, disopyramide] or class III [e.g. amiodarone, sotalol, dofetilide] antiarrhythmic agents; moxifloxacin, methadone, antipsychotics). Concomitant use with gonadotropins resulted in ovarian hyperstimulation syndrome.
Lab Interference
May cause a false positive result in anti-doping test. May interfere and mislead the results of pituitary-gonadotropic and gonadal function tests during and for up to 12 weeks after treatment.
Action
Description:
Mechanism of Action: Goserelin is a synthetic decapeptide analogue of gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin). Initially, it causes a transient increase of LH, FSH, serum testosterone and estradiol levels. Following chronic administration, a sustained suppression of pituitary gonadotropins is observed and fall in serum testosterone levels in men and serum estradiol levels in women occurs.
Onset: Testosterone suppression reaching castrate level: 2-4 weeks. Estradiol suppression reaching postmenopausal level: Within 3 weeks. FSH and LH suppression to follicular phase levels: Within 4 weeks.
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed. Time to peak plasma concentration: 3.6 mg implant: 12-15 days (male); 8-22 days (female); 10.8 mg implant: Within 24 hours (male).
Distribution: Volume of distribution: 44.1 L (male); 20.3 L (female). Plasma protein binding: Approx 27%.
Metabolism: Metabolised in the liver via hydrolysis of the C-terminal amino acids.
Excretion: Via urine (>90%; 20% as unchanged drug). Elimination half-life: 2-4 hours.
Chemical Structure

Chemical Structure Image
Goserelin

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5311128, Goserelin. https://pubchem.ncbi.nlm.nih.gov/compound/Goserelin. Accessed Nov. 16, 2020.

Storage
Store below 25°C.
MIMS Class
Cancer Hormone Therapy / Trophic Hormones & Related Synthetic Drugs
ATC Classification
L02AE03 - goserelin ; Belongs to the class of gonadotropin releasing hormone analogues. Used in endocrine therapy.
References
Anon. Goserelin. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/11/2020.

Anon. Goserelin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/11/2020.

Buckingham R (ed). Goserelin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/11/2020.

Joint Formulary Committee. Goserelin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/11/2020.

Zoladex 10.8 mg (TerSera Therapeutics LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/11/2020.

Zoladex 3.6 mg (AstraZeneca Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 04/11/2020.

Zoladex 3.6 mg (TerSera Therapeutics LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/11/2020.

Zoladex 3.6 mg Implant (AstraZeneca UK Limited). MHRA. https://products.mhra.gov.uk/. Accessed 04/11/2020.

Zoladex LA 10.8 mg (AstraZeneca Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 04/11/2020.

Zoladex LA 10.8 mg Implant (AstraZeneca UK Limited). MHRA. https://products.mhra.gov.uk/. Accessed 04/11/2020.

Disclaimer: This information is independently developed by MIMS based on Goserelin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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