達那唑
達那唑(Danazol)為一種用於治療子宮內膜異位症、乳腺小叶增生、遺傳性血管性水腫及其他疾病的藥物[5][1][10][11][12],主要經口服给药[1]。
系统(IUPAC)命名名称 | |
---|---|
(1S,2R,13R,14S,17R,18S)-17-ethynyl-2,18-dimethyl-7-oxa-6-azapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5,9-trien-17-ol | |
临床数据 | |
商品名 | Danatrol, Danocrine, Danol, Danoval, others |
Drugs.com | Monograph |
MedlinePlus | a682599 |
妊娠分级 | |
给药途径 | 口服给药 |
合法狀態 | |
合法状态 |
|
药代动力学数据 | |
生物利用度 | Saturable with dosage, higher with food intake[1] |
蛋白结合度 | 會與白蛋白、SHBG, CBG結合[2][3][4] |
代谢 | 肝臟(CYP3A4)[5][6][7][1][8] |
代謝產物 | • 2-OHM-Ethisterone[6] • Ethisterone[8][9] |
生物半衰期 | Acute: 3–10 hours[5][1] Chronic: 24–26 hours[5] |
排泄 | 尿、糞便[5][1] |
识别 | |
CAS注册号 | 17230-88-5 |
ATC代码 | G03XA01 |
PubChem | CID 28417 |
IUPHAR/BPS | 6942 |
DrugBank | DB01406 |
ChemSpider | 26436 |
UNII | N29QWW3BUO |
KEGG | D00289 |
ChEBI | CHEBI:4315 |
ChEMBL | CHEMBL1479 |
其他名称 | WIN-17757; 2,3-Isoxazolethisterone; 2,3-Isoxazol-17α-ethynyltestosterone; 17α-Ethynyl-17β-hydroxyandrost-4-en-[2,3-d]isoxazole |
化学 | |
化学式 | C22H27NO2 |
摩尔质量 | 337.463 g/mol |
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達那唑具有雄性化的副作用,使其用途大受限制。常見不良反應包含痤疮、多毛症,以及聲音變低沉[1][13]。達那唑的作用機轉複雜,同時具有弱雄激素、弱同化類固醇、弱孕激素,弱抗促性腺激素、弱固醇類合成抑制劑,以及功能性抗動情素藥物[4][7][14][7][14][15]。
達那唑發現於1963年,並於1971年應用於醫學[7][16][17][18]。隨著副作用更少的性腺激素釋放素類似物應用逐漸廣泛,達那唑在治療子宮內膜異位症的角色已被前者所取代[3]。
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延伸閱讀
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