Buserelin
| Buserelin | ||
|---|---|---|
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| Structural formula | ||
| Mass / length primary structure | 9 amino acids, 1239 daltons | |
| Identifier | ||
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| Drug information | ||
| ATC code | L02 AE01 | |
| Drug class | Antiandrogens | |
Buserelin is the abbreviation for Bu tyl se ryl relin and describes a hormonally active drug that acts as a GnRH analogue .
structure
Buserelin is a synthetic non- peptide with the primary structure : Pyr-His-Trp-Ser-Tyr- D -Ser (tBu) -Leu-Arg-Pro-NH-Et, which acts analogously to the gonadotropin-releasing hormone (GnRH) .
Compared to the GnRH, the amino acid glycine at position 6 was exchanged for O - tert- butyl- D -serine, the C -terminal amino acid glycine was removed and the C -terminal was protected as ethylamide. The chemical modification leads to an increased resistance to the enzymatic degradation by peptidases and to a long-lasting release of gonadotropins with a significantly reduced dose of active ingredient against GnRH. Buserelin is a hundred to two hundred times more effective than natural GnRH.
effect
The active ingredient binds agonistically to the GnRH receptor in the pituitary gland and thus leads to the secretion of another hormone, the luteinizing hormone (LH), and, to a lesser extent, the follicle-stimulating hormone (FSH). Ultimately, pulsatile administration of buserelin causes the ovarian follicles to mature in the ovary and cause ovulation . This is used in the treatment of ovarian cysts and in artificial insemination , in veterinary medicine also for the ovarian stimulation test .
If the receptor is continuously stimulated for more than 24 hours, a paradoxical inhibition occurs , since receptor desensitization occurs, whereupon LH secretion is suppressed despite the binding of the promoting hormone. As a result, the production of the male sex hormone testosterone is suppressed at the castration level in the testes . This mechanism is used to treat testosterone-dependent tumors, especially in advanced prostate cancer . Buserelin is also used in breast cancer treatment.
Trade names
Metrelef (D), Profact (D), Suprecor (A), Suprefact (CH)
In veterinary medicine it is sold as a receptal or as a veterinarian.
Individual evidence
- ↑ Red List online, as of September 2009.
- ↑ AM comp. d. Switzerland, as of September 2009.
- ↑ a b AGES-PharmMed, as of September 2009.
- ↑ Veterelin 0.004 mg / ml solution for injection for cattle, pigs, horses and rabbits. (pdf; 51 kB) pharmazie.com, March 19, 2012, accessed on April 2, 2012 : "Active ingredient: Buserelin 0.004 mg" .
Web links
- Entry on Buserelin at Vetpharm, accessed on August 11, 2012.
