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Buserelin – Uses, Mechanism of Action & Side Effects

Buserelin is a synthetic GnRH analogue used in the treatment of hormone-dependent conditions such as prostate cancer, endometriosis, and as part of assisted reproduction protocols.

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Things worth knowing about "Buserelin"

Buserelin is a synthetic GnRH analogue used in the treatment of hormone-dependent conditions such as prostate cancer, endometriosis, and as part of assisted reproduction protocols.

What is Buserelin?

Buserelin is a synthetically produced analogue of the naturally occurring gonadotropin-releasing hormone (GnRH), also referred to as luteinizing hormone-releasing hormone (LHRH). It belongs to the class of GnRH agonists and is used medically to regulate hormone levels in the body. Buserelin is available as a nasal spray, injection solution, and subcutaneous implant.

Mechanism of Action

Under normal physiological conditions, GnRH stimulates the pituitary gland to release LH (luteinizing hormone) and FSH (follicle-stimulating hormone), which in turn trigger the production of sex hormones in the gonads.

When Buserelin is administered continuously, the pituitary gland is persistently stimulated, which -- after an initial flare phase -- leads to desensitization and downregulation of GnRH receptors. As a result, LH and FSH secretion drops significantly, causing a marked reduction in testosterone and oestrogen production. This state is referred to as medical or chemical castration (hypogonadism).

Indications

Prostate cancer: Reduction of testosterone levels to slow the growth of hormone-dependent prostate tumours.
Endometriosis: Suppression of oestrogen production to reduce the growth of endometrial tissue outside the uterus.
Uterine fibroids: Pre-operative treatment to reduce the size of uterine fibroids.
Assisted reproduction: Used during in vitro fertilisation (IVF) to control ovarian stimulation and prevent premature ovulation.
Precocious puberty: Treatment of premature puberty in children.

Dosage and Administration

The dosage and form of Buserelin depend on the underlying condition being treated. Common forms of administration include:

Nasal spray: Typically used for endometriosis or as part of assisted reproductive protocols. Applied several times daily.
Subcutaneous injection: Frequently used for prostate cancer treatment or ovulation induction.
Implant: Used for long-term therapy; inserted under the skin and releases the active substance over several weeks or months.

The exact dosage must always be determined and monitored by a qualified healthcare professional.

Side Effects

Because Buserelin significantly alters hormone levels, a range of side effects may occur, many of which resemble menopausal symptoms:

Hot flushes and sweating
Decreased libido
Mood swings and depressive episodes
Osteoporosis (bone loss) with long-term use
Erectile dysfunction in men
Vaginal dryness in women
Local reactions at the injection site
Tumour flare: A temporary worsening of prostate cancer symptoms at the start of therapy, caused by an initial surge in testosterone levels

Contraindications and Interactions

Buserelin should not be used in the following situations:

Known hypersensitivity to GnRH analogues
Pregnancy and breastfeeding (unless specifically indicated by a physician)
Hormone-independent prostate cancer

Potential drug interactions may occur with other hormone preparations, certain antidiabetic agents, and medications that affect the QT interval. A thorough review of all concurrent medications by a healthcare provider is therefore essential.

References

European Medicines Agency (EMA): Buserelin - Summary of Product Characteristics. URL: https://www.ema.europa.eu
Waxman J. - Handbook of Urology. Wiley-Blackwell, 3rd edition, 2010.
National Institute for Health and Care Excellence (NICE): Prostate cancer: diagnosis and management. URL: https://www.nice.org.uk

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