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Buserelin

Also known as: Buserelin Acetate

Pharmacodynamic Properties

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 hypothalanic-pituitary-gonadal axis.

Pharmacokinetic Properties

Subcutaneous administration

Metabolic inactivation by peptidases occurs in the liver and kidney. The drug is also inactivated by pituitary membrane enzymes.

Intra-nasal administration

The intra-nasal absorption rate of buserelin is about 3%. Metabolic inactivation by peptidases occurs in the liver and kidney. The drug is also inactivated by pituitary membrane enzymes. After intra-nasal administration to humans, buserelin is excreted for more than 8 hours in the urine. Virtually all the serum fraction, and half the urine fraction of buserelin, are present as the parent drug.

The bioavailability of buserelin after nasal administration is not adversely influenced by the presence of rhinitis.

Preclinical Safety Data

None stated.

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