Drug reference

Goserelin

GnRH Analogue · Antineoplastic agent, Endocrine therapy

Also known as ZOLADEX

GnRH AnalogueAntineoplastic agent, Endocrine therapyATC null

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Avoid in confirmed pregnancy—toxicity in animal studies; potential for teratogenesis.

FDA category + note

Top interactionssee all 12 →

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Mechanism

Goserelin, a GnRH agonist, signals through GPCRs on gonadotropes, initially increasing LH and FSH synthesis and secretion. However, continuous nonpulsatile administration causes desensitization and down-regulation of pituitary GnRH receptors. This results in the inhibition of FSH and LH secretion, ultimately leading to the suppression of gonadal function and a fall in testosterone or estradiol levels to castration levels.

Indications

Carcinoma prostateEndometriosisPituitary desensitization before ovulation induction with exogenous gonadotrophinsGonadal suppression in women undergoing assisted reproductive technology proceduresGonadal suppression in women with gynecologic problems benefited by ovarian suppressionEndometrial-thinning agent prior to endometrial ablation for dysfunctional uterine bleedingAdvanced prostate cancerAdvanced breast cancerAndrogen deprivation therapy (ADT) for all forms of advanced prostate cancerProstate cancer in conjunction with radiation therapy or in some cases following surgical removal of the prostate gland (for localized intermediate- to high-risk)Adjuvant treatment of breast cancer or metastatic disease for premenopausal women (in combination with tamoxifen or AIs)Suppression of ovarian estrogen and progesterone production in pre- and perimenopausal womenEndogenous Gn suppression before ovulation inductionOvarian suppression for premenopausal women with higher risk tumors (in combination with tamoxifen or AI for 5 years)For premenopausal women with ER-positive metastatic breast cancer (with aromatase inhibitor and CDK4/6 inhibitor)For male breast cancer where an AI is indicated (concomitant administration with AI)Concurrent administration with adjuvant chemotherapy for fertility preservation

Dosing

Adult: For pituitary desensitization before ovulation induction: 3.6 mg of the depot injection given once in the anterior abdominal wall 1–3 weeks earlier. For endometriosis and carcinoma prostate: 3.6 mg injected in the same way every 4 weeks.
Renal adjustment: Avoid in moderate to severe renal impairment.
Hepatic adjustment: Manufacturer advises avoid in moderate to severe impairment (no information available).

Pharmacokinetics

Onset

Initial increase in Gn secretion for 1–2 weeks, followed by desensitization and down-regulation.

Duration

Approximately 4 weeks (for 3.6 mg depot injection)

Half-life

2–6 hours (for superactive/long-acting GnRH agonists)

Contraindications

Hypersensitivity
Undiagnosed vaginal bleeding (when used for endometriosis or pituitary desensitisation)
Use longer than 6 months for endometriosis (do not repeat)
Confirmed pregnancy
Pregnant women

Side effects

Common

DepressionMood alteredHot flushLoss of libidoVaginal drynessOsteoporosisEmotional labilityEdemaHeadacheWeight changesHot flashesDecreased bone densityVaginal dryness (women)Vaginal atrophy (women)Erectile dysfunction (men)Vasomotor symptoms (hot flashes)Decreased libidoAmenorrheaDyspareuniaVasomotor instabilityImpotenceGynecomastiaFatigueAnemiaWeight gainDecreased insulin sensitivityAltered lipid profilesFracturesLoss of muscle massPostmenopausal symptoms

Serious

Auditory disorder
Hypotension
Leucopenia
Pituitary tumour benign
Thrombocytopenia
Tinnitus
Ovarian hyperstimulation syndrome
Pelvic pain
Embolism and thrombosis
Increased risk of fracture
QT interval prolongation
Shock
Tumour activation temporary (e.g., progression of prostate cancer during initial 1–2 weeks)
Allergic reactions
risk of osteoporosis (with long-term use)
estrogen withdrawal symptoms (e.g., hot flashes)
Testosterone flare (transient rise in testosterone leading to acute stimulation of prostate cancer growth and symptoms, typically lasting 2 to 3 weeks)
Increased risk of diabetes
Increased risk of coronary heart disease
Bone loss