Nafarelin
Brand names,
Nafarelin
Analogs
Nafarelin
Brand Names Mixture
Nafarelin
Chemical_Formula
C66H83N17O13
Nafarelin
RX_link
http://www.rxlist.com/cgi/generic2/nafarelin.htm
Nafarelin
fda sheet
Nafarelin
msds (material safety sheet)
Nafarelin
Synthesis Reference
No information avaliable
Nafarelin
Molecular Weight
1321.6344 g/mol
Nafarelin
Melting Point
No information avaliable
Nafarelin
H2O Solubility
No information avaliable
Nafarelin
State
Solid
Nafarelin
LogP
No information avaliable
Nafarelin
Dosage Forms
Liquid; Metered-dose (aerosol)
Nafarelin
Indication
For treatment of gonadotropin-dependent precocious puberty in children of both sexes and for the treatment of endometriosis.
Nafarelin
Pharmacology
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.
Nafarelin
Absorption
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.
Nafarelin
side effects and Toxicity
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.
Nafarelin
Patient Information
Nafarelin
Organisms Affected
Humans and other mammals