Nafarelin acetate is a gonadotropin-releasing hormone (GnRH) agonist proven as effective as danazol in treating endometriosis. Its proposed mechanism of action is the desensitization of pituitary GnRH receptors leading to a decrease in gonadotropin release, and ovarian hormone serum concentrations similar to those achieved in postmenopausal women.
Item name: Nafarelin Acetate
CAS: 86220-42-0
Molecular Formula: C68H89N17O16
Formula Weight: 1400.54
In children, nafarelin acetate was rapidly absorbed into the systemic circulation after intranasal administration. Maximum serum concentrations (measured by RIA) were achieved between 10 and 45 minutes. Following a single dose of 400 µg base, the observed peak concentration was 2.2 ng/mL, whereas following a single dose of 600 µg base, the observed peak concentration was 6.6 ng/mL. The average serum half-life of nafarelin following intranasal administration of a 400 µg dose was approximately 2.5 hours. It is not known and cannot be predicted what the pharmacokinetics of nafarelin will be in children given a dose above 600 µg.
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