Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2020 Publisher: Neon Healthcare Limited, Mill Studio Business Centre, Crane Mead, Ware, Hertfordshire, SG12 9PY, United Kingdom
Buserelin is a synthetic peptide. It is a superactive analogue of natural gonadotrophin releasing hormone (gonadorelin, LHRH or GNRH). After an initial stimulation of gonadotrophin release, it down-regulates the hypothalamic-pituitary-gonadal (HPO) axis such that a decrease in ovarian steroid secretion into the post-menopausal range occurs. The time taken to achieve these levels varies between individuals and with the regimen of administration, so that close monitoring of circulating levels of oestradiol and progesterone should be performed during treatment. This effect provides an appropriate setting for the administration of follicle-stimulating therapy and reduces the incidence of premature ovulation by inhibition of surges in LH.
The bioavailability of buserelin after subcutaneous injection is 100%. Cmax occurs at about 1 hour post-injection. The half-life after injection is about 80 minutes.
Buserelin accumulates preferentially in the liver, kidneys and in the anterior pituitary lobe, the biological target organ. Buserelin circulates in serum predominantly in the intact, active form. Protein binding is about 15%.
Buserelin is inactivated by peptidases (pyrogutamyl peptidase and chymotrypsin-like endopeptidases) in the liver and kidneys. In the pituitary gland, receptor-bound buserelin is inactivated by membrane-located enzymes. Buserelin and inactive buserelin metabolites are excreted via the renal and the biliary route.
No signs of toxicity or histopathological changes were detected in long-term pharmacology and toxicology studies with buserelin in rats, dogs, and monkeys; the endocrine effects observed were restricted to the gonads.
Pituitary adenoma occurred during long-term treatment in rats, this phenomenon has not been found in dogs and monkeys. There are no indications of a mutagenic or carcinogenic potential.
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