酢酸ナファレリン 化学特性,用途語,生産方法
外観
白色~うすい黄色, 結晶~粉末
溶解性
水に可溶
用途
ゴナドトロピン放出ホルモン
(Gn-RH)誘導体です。Gn-RH 受容体との親
和性を高めた化合物であり、生物活性が増強
し、持続的作用を示します。
効能
子宮内膜症治療薬, 性腺刺激ホルモン放出ホルモン受容体作動薬
商品名
ナサニール (ファイザー)
説明
Nafarelin acetate is a synthetic decapeptide agonist analog of the natural
gonadotropin-releasing hormone, differing in the amino acid at position 6 where
D-naphthylalanine has been substituted for glycine. This substitution gives nafarelin
greater potency and a substantially longer half-life than the endogenous hormone.
Nafarelin acetate administered as a nasal spray, suppresses estrogen levels on repeated
dosing and is indicated for the management of endometriosis. It also has orphan drug
status for use in precocious puberty.
使用
Nafarelin Acetate is a gonadotropin-releasing hormone agonist. Treatment with Nafarelin improves sleep disturbances and anxiety-depression. Nafarelin is also used in the treatment of estrogen-dependent gynecologic disorders such as endometriosis and uterine leiomyomas.
臨床応用
Nafarelin acetate, contains D Nal(2)6 [Nal = 3-(2-naphthyl)-Ala] in place of Gly6, but the C-terminus, Gly10-NH2, is identical
with natural GnRH. Nafarelin acetate is available as a 0.2% nasal spray for the relief
of endometriosis. Estrogen, of course, is needed for the growth of endometrial tissue; thus, decreased estrogen leads to shrinkage of errant endometrial tissue. The observed side effects of nafarelin acetate are related to falling estrogen levels and include decreased libido,
amenorrhea, hot flashes, and vaginal dryness. When used consistently, nafarelin acetate will
inhibit ovulation and stop menstruation.
Nafarelin acetate also is used in children, male and female, for the treatment of central
precocious puberty. By suppressing the release of LH, the estradiol or testosterone levels fall to
prepubertal levels; early secondary sexual development is arrested, linear growth and skeletal
maturation are slowed, and in girls, menstruation stops.
酢酸ナファレリン 上流と下流の製品情報
原材料
準備製品