Drug reference

Buserelin

GnRH Analogue · Endocrine System Agent

Also known as Suprefact

GnRH AnalogueEndocrine System AgentATC null

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

—

none in our sources

PREGNANCY

Avoid in confirmed pregnancy.

FDA category + note

Mechanism

Buserelin is a gonadorelin analogue. Its continued administration leads to down-regulation of gonadotrophin-releasing hormone receptors, thereby reducing the release of gonadotrophins (follicle stimulating hormone and luteinising hormone). This reduction in gonadotrophin release in turn inhibits androgen and oestrogen production.

Indications

EndometriosisPituitary desensitisation before induction of ovulation by gonadotrophins for in vitro fertilisation (under expert supervision)Advanced prostate cancerAndrogen deprivation therapy (ADT) for all forms of advanced prostate cancer

Dosing

Adult: Endometriosis: By intranasal administration, 300 micrograms 3 times a day (one 150 microgram spray into each nostril), maximum duration 6 months (do not repeat), to be started on days 1 or 2 of menstruation. Pituitary desensitisation for IVF: By intranasal administration, 150–300 micrograms 4 times a day (150 micrograms equivalent to one spray) during waking hours.…
Renal adjustment: Avoid in moderate to severe renal impairment.
Hepatic adjustment: Manufacturer advises avoid in moderate to severe impairment (no information available).
Max dose: For endometriosis, maximum duration of treatment 6 months (do not repeat). For advanced prostate cancer, intranasal dose of 200 micrograms 6 times a day. For pituitary desensitisation, subcutaneous dose up to 500 micrograms twice daily.

Pharmacokinetics

Onset

Initial rise in LH and FSH levels, followed by sustained decrease in serum testosterone after 14 to 21 days. Castrate testosterone levels achieved within 3 to 4 weeks.

Contraindications

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

Side effects

Common

Depressionmood alteredHot flashesDecreased bone densityVaginal dryness (women)Vaginal atrophy (women)Erectile dysfunction (men)Vasomotor instabilityLoss of libidoImpotenceGynecomastiaFatigueAnemiaWeight gainDecreased insulin sensitivityAltered lipid profilesOsteoporosisFracturesLoss of muscle mass

Serious

Auditory disorder
hypotension
leucopenia
pituitary tumour benign
thrombocytopenia
tinnitus
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