Nafarelin

• Gonadotropin-releasing hormones
• Antiendometriotic agent
• ATC:H01CA02

• Moexipril HCL
• Moexiprilum [INN-Latin]
• Univasc

• No information avaliable

C₆₆H₈₃N₁₇O₁₃

http://www.rxlist.com/cgi/generic2/nafarelin.htm

Nafarelin MSDS

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1321.6344 g/mol

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Solid

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Liquid; Metered-dose (aerosol)

For treatment of gonadotropin-dependent precocious puberty in children of both sexes and for the treatment of endometriosis.

Nafarelin is a potent agonistic analog of gonadotropin-releasing hormone (GnRH). At the onset of administration, nafarelin stimulates the release of the pituitary gonadotropins, LH and FSH, resulting in a temporary increase of gonadal steroidogenesis. Repeated dosing abolishes the stimulatory effect on the pituitary gland. Twice daily administration leads to decreased secretion of gonadal steroids by about 4 weeks; consequently, tissues and functions that depend on gonadal steroids for their maintenance become quiescent. After nafarelin therapy is discontinued, pituitary and ovarian function normalize and estradiol serum concentrations increase to pretreatment levels. Recurrences of endometriosis are frequent after cessation of any hormonal therapy and after surgery that leaves the ovaries and/or uterus intact.

Rapidly absorbed into the systemic circulation after intranasal administration. Bioavailability from a 400 µg dose averaged 2.8% (range 1.2 to 5.6%). Not absorbed after oral administration.

In experimental animals, a single subcutaneous administration of up to 60 times the recommended human dose (on a µg/kg basis, not adjusted for bioavailability) had no adverse effects. At present, there is no clinical evidence of adverse effects following overdosage of GnRH analogs.

Humans and other mammals