71-63-6_洋地黄毒甙CAS号:71-63-6/洋地黄毒甙中英文名/分子式/结构式

洋地黄毒甙的其他展现形式

相关化合物

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简介

地吉妥辛，别名洋地黄毒苷
处方药
【洋地黄毒苷】(digitoxin)分子式C41H64O13，分子量764.95，CAS登录号：71-63-6。白色结晶性粉末，无臭。熔点256-257℃。比旋光度`[\alpha]_D^20 4.8`度（C=1.2，二氧六环）。略溶于氯仿，微溶于乙醇、乙醚，不溶于水。由玄参科植物毛地黄（亦称“洋地黄”或“紫花洋地黄”）的叶中提取制的。

名称和标识符

MDL	MFCD00003686
InChIKey	WDJUZGPOPHTGOT-XUDUSOBPSA-N
Inchi	InChI=1S/C41H64O13/c1-20-36(46)29(42)16-34(49-20)53-38-22(3)51-35(18-31(38)44)54-37-21(2)50-33(17-30(37)43)52-25-8-11-39(4)24(15-25)6-7-28-27(39)9-12-40(5)26(10-13-41(28,40)47)23-14-32(45)48-19-23/h14,20-22,24-31,33-38,42-44,46-47H,6-13,15-19H2,1-5H3/t20-,21-,22-,24-,25+,26-,27+,28-,29+,30+,31+,33+,34+,35+,36-,37-,38-,39+,40-,41+/m1/s1
SMILES	C[C@H]1O[C@](O[C@@H]2[C@@H](C)O[C@](O[C@H]3[C@@H](O)C[C@@](O[C@@H]4C[C@](CC[C@]5([H])[C@]6([H])CC[C@@]7(C)[C@]5(O)CC[C@@H]7C(CO8)=CC8=O)([H])[C@]6(C)CC4)([H])O[C@@H]3C)([H])C[C@@H]2O)([H])C[C@H](O)[C@@H]1O

别名信息

- 中文别名 -

洋地黄毒甙洋地黄毒苷二硫胺毛地黄毒苷毛地黄毒苷标准品洋地黄毒甙 USP标准品洋地黄毒甙标准品(JP) 洋地黄毒苷 EP标准品洋地黄毒苷(RG) 洋地黄毒苷标准品

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- 英文别名 -

Digitoxin Digitoxin solution DIGITOXIN(P) DIGITOXIN(RG) [3H]-Digitoxin Acedoxin Cardigin De-Tone digicor Digilong Digimed Digitrin Ditaven Myodigin Natigal tridigitoxosyldigitoxigenin 5β,20(22)-Cardenolide-3β,14-diol-3-(O-2,6-dideoxy-β-D-ribo-hexopyranosyl-[1→4]-O-2,6-dideoxy-β-D-ribo-hexopyranosyl-[1→4]-2,6-dideoxy-β-D-ribo-hexopyranosyl)oxy Digitoxoside Lanatoxin Panlanat DIGITOXIN [WHO-DD] Digitoxin (JAN/USP/INN) tradigal Digitoxinum Card-20(22)-enolide, 3-((O-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1-4)-O-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1-4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl)oxy)-14-hydroxy, (3beta,5beta)- Tox21_111659 DIGITOXIN (EP MONOGRAPH) DIGITOXIN [USP IMPURITY] 4-[(1R,3aS,3bR,5aR,7S,9aS,9bS,11aR)-7-{[(2R,4S,5S,6R)-5-{[(2S,4S,5S,6R)-5-{[(2S,4S,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy}-4-hydroxy-6-methyloxan-2-yl]oxy}-4-hydroxy-6-methyloxan-2-yl]oxy}-3a-hydroxy-9a,11a-dimethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-1-yl]-2,5-dihydrofuran-2-one Card-20(22)-enolide, 3-((O-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-O-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl)oxy)-14-hydroxy-, (3beta,5beta)- Digitoxin, British Pharmacopoeia (BP) Reference Standard 71-63-6 Digilanid 8006-96-0 EINECS 200-760-5 (3beta,5beta)-3-((O-2,6-DIDEOXY-beta-D-RIBO-HEXOPYRANOSYL-(1->4)-O-2,6-DIDEOXY-beta-D-RIBO-HEXOPYRANOSYL-(1->4)-2,6-DIDEOXY-beta-D-RIBO-HEXOPYRANOSYL)OXY)-14-HYDROXYCARD-20(22)-ENOLIDE Purodigin, crystalline 3beta-[2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1-4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1-4)-2,6-dideoxy-beta-D-ribo-hexopyranosyloxy]-14-hydroxy-5beta-card-20(22)-enolide BDBM46356 Monodigitoxoside Card-20(22)-enolide, 3-[(O-2,6-dideoxy-.beta.-D-ribo-hexopyranosyl-(1?4)-O-2,6-dideoxy-.beta.-D-ribo-hexopyranosyl-(1?4)-2,6-dideoxy-.beta.-D-ribo-hexopyranosyl)oxy]-14-hydroxy-, (3.beta.,5.beta.)- Digitoksim Mono-digitoxid DIGITOXIN (USP MONOGRAPH) DIGITOXIN [USP-RS] Crystodigin (TN) Digitoxigenin-tridigitoxosid D00297 NCGC00159428-02 Digitoxigenin-tridigitoxosid [German] Carditoxin Cristapurat 3beta-((2,6-DIDEOXY-beta-D-RIBO-HEXOPYRANOSYL-(1->4)-2,6-DIDEOXY-beta-D-RIBO-HEXOPYRANOSYL-(1->4)-2,6-DIDEOXY-beta-D-RIBO-HEXOPYRANOSYL)OXY)-14-HYDROXY-5beta-CARD-20(22)-ENOLIDE DIGITOXIN [JAN] Digitoxigenin tridigitoxoside Digipural SCHEMBL20940 Digitoxin 100 microg/mL in Acetonitrile SR-01000721879-2 Digitophyllin Cardidigin Digitoxina [INN-Spanish] Digitoxin [USP:INN:BAN:JAN] MLS000069787 Digitaline (TN) inhibits Na+/K+ ATPase Card-20(22)-enolide, 3-((O-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1.fwdarw.4)-O-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1.fwdarw.4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl)oxy)-14-hydroxy-, (3beta,5beta)- EPA Pesticide Chemical Code 097002 Carditalin DIGITOXIN [VANDF] Tri-digitoxoside NCGC00142623-02 Digitalis (3beta,5beta)-3-((O-2,6-Dideoxy-beta-D-ribohexopyranosyl-(1-4)-O-2,6-dideoxy-bet a-D-ribo-hexopyranosyl-(1-4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl)oxy)-14-hydro xycard-20(22)-enolide LT00244784 5.beta.-Card-20(22)-enolide, 3.beta.,14-dihydroxy-, 3-[tris-(digitoxoside)] USEPA/OPP Pesticide Code: 097002 D0M3QP Digitoxosidum DIGITOXIN (USP-RS) Tox21_302269 3beta-(2,6-Dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyloxy)-14-hydroxy-5beta,14beta-card-20(22)-enolide CARD-20(22)-ENOLIDE, 3-((O-2,6-DIDEOXY-BETA-D-RIBO-HEXOPYRANOSYL-(HEXOPYRANOSYL-(1-4)-2,6-DIDEOXY-BETA-D-RIBO-HEXOPYRANOSYL)OXY)-14-HYDROXY-,(3BETA, 5BETA)- Coramedan 1339-93-1 Card-20(22)-enolida, 3-[(o-2,6-dideoxi-?-d-ribo-hexopiranosil-(1?4)-o-2,6-dideoxi-?-d-ribo-hexopiranosil-(1?4)-2,6-dideoxi-?-d-ribo-hexopiranosil)oxi]-14-hidroxi-, (3?,5?)- AS-75726 DIGOXIN IMPURITY A (EP IMPURITY) cid_441207 CHEMBL254219 Digitoxin [INN:BAN:JAN] Tri-digitoxoside [German] Card-20(22)-enolide, 3-((O-2,6-dideoxy-.beta.-D-ribo-hexopyranosyl-(1-4)-O-2,6-dideoxy-.beta.-D-ribo-hexopyranosyl-(1-4)-2,6-dideoxy-.beta.-D-ribo-hexopyranosyl)oxy)-14-hydroxy-, (3beta,5beta)- Digitaline Digitoxine DIGITOXINUM [WHO-IP LATIN] 4-((1S,2S,5S,11S,7R,10R,14R,15R)-5-{5-[5-((2S,4S,5S,6R)-4,5-dihydroxy-6-methyl (2H-3,4,5,6-tetrahydropyran-2-yloxy))(4S,5S,2R,6R)-4-hydroxy-6-methyl(2H-3,4,5 ,6-tetrahydropyran-2-yloxy)](4S,5S,2R,6R)-4-hydroxy-6-methyl(2H-3,4,5,6-tetrah ydropyran-2-yloxy) REGID_for_CID_441207 Digimerck NCGC00142623-03 Asthenthilo CHEBI:28544 DIGITOXIN [HSDB] Digitoksin Tardigal C41H64O13 CCRIS 7116 (3beta,5beta)-3-((O-2,6-Dideoxy-beta-D-ribo-hexopyranosyl-(1-4)-O-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1-4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl)oxy)-14-hydroxycard-20(22)-enolide Digitoxin (JP15/USP/INN) DIGITOXIN [MI] Caswell No. 349 4-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(((2R,4S,5S,6R)-5-(((2S,4S,5S,6R)-5-(((2S,4S,5S,6R)-4,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-4-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-4-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one AKOS015915863 NSC 7529 DIGITOXIN (USP IMPURITY) Digitoxina Lanostabil CP4071 (3beta,5beta)-3-{[2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl]oxy}-14-hydroxycard-20(22)-enolide NCGC00142623-04 NCGC00094652-06 DB01396 Digitaline cristallisee Digitossina UNII-E90NZP2L9U Digitaline nativelle NSC7529 CS-5502 CCG-208538 NCGC00255265-01 WDJUZGPOPHTGOT-XUDUSOBPSA-N NSC-7529 3beta-[2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyloxy]-14-hydroxy-5beta-card-20(22)-enolide Digicor Digitoxin [BAN:INN:JAN] SMR000058529 Digitoxin for LC assay HSDB 215 DIGITOXIN [EP MONOGRAPH] Q-100791 ACon0_000319 Digitoxin, European Pharmacopoeia (EP) Reference Standard 3.BETA.-((2,6-DIDEOXY-.BETA.-D-RIBO-HEXOPYRANOSYL-(1->4)-2,6-DIDEOXY-.BETA.-D-RIBO-HEXOPYRANOSYL-(1->4)-2,6-DIDEOXY-.BETA.-D-RIBO-HEXOPYRANOSYL)OXY)-14-HYDROXY-5.BETA.-CARD-20(22)-ENOLIDE DIGOXIN IMPURITY A [EP IMPURITY] BRN 0076678 DTXSID0022933 Cardiolanata CARD-20(22)-ENOLIDE, 3-((O-2,6-DIDEOXY-.BETA.-D-RIBO-HEXOPYRANOSYL-(1->4)-O-2,6-DIDEOXY-.BETA.-D-RIBO-HEXOPYRANOSYL-(1->4)-2,6-DIDEOXY-.BETA.-D-RIBO-HEXOPYRANOSYL)OXY)-14-HYDROXY-, (3.BETA.,5.BETA.)- Digitalin, crystalline 3beta-(2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyloxy)-14-hydroxy-5beta-card-20(22)-enolide SBI-0051348.P003 E90NZP2L9U D89676 SMP1_000096 3-[(3S,5R,8R,9S,10S,13R,14S,17R)-3-[(2R,4S,5S,6R)-5-[(2S,4S,5S,6R)-5-[(2S,4S,5S,6R)-4,5-dihydroxy-6-methyl-tetrahydropyran-2-yl]oxy-4-hydroxy-6-methyl-tetrahydropyran-2-yl]oxy-4-hydroxy-6-methyl-tetrahydropyran-2-yl]oxy-14-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one Digitoxine [INN-French] (3.BETA.,5.BETA.)-3-((O-2,6-DIDEOXY-.BETA.-D-RIBO-HEXOPYRANOSYL-(1->4)-O-2,6-DIDEOXY-.BETA.-D-RIBO-HEXOPYRANOSYL-(1->4)-2,6-DIDEOXY-.BETA.-D-RIBO-HEXOPYRANOSYL)OXY)-14-HYDROXYCARD-20(22)-ENOLIDE DigitoXin, USP ACon1_000610 Digitalinum verum Card-20(22)-enolide, 3-((O-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1-4)-O-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1-4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl)oxy)-14-hydroxy-, (3beta,5beta)- CAS-71-63-6 (3beta,5beta)-3-((O-2,6-DIDEOXY-beta-D-RIBO-HEXAPYRANOSYL-(1->4)-2,6-DIDEOXY-beta-D-RIBO-HEXOPYRANOSYL)OXY)-14-HYDROXYCARD-20(22)-ENOLIDE C12H13F13N2O3 C01AA04 LMST01120018 Mono-digitoxid [German] GTPL6782 DTXCID102933 Digitoxin, >=92% (HPLC), powder Pandigal A572A148-EC30-47D2-A32A-C9D8A93F8EFC Tox21_111659_1 DIGITOXIN [WHO-IP] EN300-123649 BRD-K63668566-001-01-7 Digisidin Card-20(22)-enolide, 3-[(O-2,6-dideoxy-.beta.-D-ribo-hexopyranosyl-(1.fwdarw.4)-O-2,6-dideoxy-.beta.-D-ribo-hexopyranosyl-(1.fwdarw.4)-2,6-dideoxy-.beta.-D-ribo-hexopyranosyl)oxy]-14-hydroxy-, (3.beta.,5.beta.)- C06955 Crystalline digitalin Q423890 HY-B1357 (3.BETA.,5.BETA.)-3-((O-2,6-DIDEOXY-.BETA.-D-RIBO-HEXAPYRANOSYL-(1->4)-2,6-DIDEOXY-.BETA.-D-RIBO-HEXOPYRANOSYL)OXY)-14-HYDROXYCARD-20(22)-ENOLIDE Mono-glycocard 3-[(3S,5R,8R,9S,10S,13R,14S,17R)-3-[(2R,4S,5S,6R)-5-[(2S,4S,5S,6R)-5-[(2S,4S,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-14-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one NCGC00142623-05 Digitoxin, United States Pharmacopeia (USP) Reference Standard Crystodigin DIGITOXIN [USP MONOGRAPH] DIGITOXIN [ORANGE BOOK] Purodigin D0542 C12-H13-F13-N2-O3 Glucodigin digitoxin Digitossina [DCIT] Unidigin Purpurid Digitoxinum [INN-Latin] MEGxp0_001901 Z1552200029 4-[(3S,5R,8R,9S,10S,13R,14S,17R)-3-[(2R,4S,5S,6R)-5-[(2S,4S,5S,6R)-5-[(2S,4S,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-14-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-5H-furan-2-one DIGITOXINUM [HPUS] DIGITOXIN [INN]

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物化性质

实验特性

LogP	3.24730
PSA	182.83000
Merck	14,3163
折射率	17 ° (C=2, CHCl3)
沸点	654.47°C (rough estimate)
熔点	240 °C (dec.) (lit.)
闪点	华氏：48.2 °F 摄氏：9 °C
溶解度	chloroform: soluble
浓度	1.0 mg/mL in methanol
颜色与性状	Powder
溶解性	溶于酸、氯仿、丙酮和吡啶，微溶于水和石油醚。无臭，味苦。
比旋光度	D20 +4.8° (c = 1.2 in dioxane)
密度	1.0971 (rough estimate)

计算特性

精确分子量	764.43500
氢键供体数量	5
氢键受体数量	13
可旋转化学键数量	7
同位素质量	764.43469209g/mol
重原子数量	54
复杂度	1410
同位素原子数量	0
确定原子立构中心数量	20
不确定原子立构中心数量	0
确定化学键立构中心数量	0
不确定化学键立构中心数量	0
共价键单元数量	1
疏水参数计算参考值（XlogP）	2.3
表面电荷	0
拓扑分子极性表面积	183

安全信息纠错

符号：	GHS06 GHS08
RTECS号	IH2275000
WGK Germany	3
安全术语	6.1(a)
安全说明	S45
包装等级	II
包装类别	II
风险术语	R23/25; R33
危险等级	6.1(a)
危险品标志	T
危险品运输编号	UN 2811
危害声明	H301-H331-H373
警示性声明	P261-P301 + P310-P311
储存条件	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
PackingGroup	Ⅰ
危险类别码	23/25-33
信号词	Danger
TSCA	Yes
毒性	LD50 in guinea pigs, cats (mg/kg): 60.0, 0.18 orally (Foerster)
HazardClass	6.1
FLUKA BRAND F CODES	3-10

国际标准相关数据

EINECS

200-760-5

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参考资料

Beilstein

76678

化合物详情（旧版）

SMILES

CC1[C@@H](O)[C@H](O)C[C@@H](O1)O[C@H]2[C@H](O)C[C@@H](OC2C)O[C@H]3[C@H](O)C[C@@H](OC3C)O[C@@H]4C[C@@H]5[C@@](CC4)(C)[C@@H]6[C@@H](CC5)[C@]7(O)[C@@](CC6)(C)[C@@H](C8=CC(=O)OC8)CC7

洋地黄毒苷简介

由玄参科植物毛地黄（亦称“洋地黄”或“紫花洋地黄”）的叶中提取制的。洋地黄毒苷脂溶性较高、口服吸收效果好，大都经肝代谢，代谢产物经肾排出，也有相当一部分经胆道排出而形成肝肠循环，t1/2长达5~7天，故作用时间也较长，属于长效强心苷药物。能加强心肌收缩力、减慢心率、抑制传导。主要用于治疗充血性心功能不全。能蓄稷，过量可产生毒性反应。用药期间忌用钙注射剂。

洋地黄毒苷物化性质

性状：白色结晶性粉末，无臭。熔点256-257℃。比旋光度`[\alpha]_D^20 4.8`度（C=1.2，二氧六环）。略溶于氯仿，微溶于乙醇、乙醚，不溶于水。

洋地黄毒苷药物分析方法

方法名称：洋地黄毒苷的测定—分光光度法

应用范围：本方法采用分光光度法测定洋地黄毒苷（C41H64O13）的含量。

本方法适用于洋地黄毒苷。

方法原理：取本品适量，经过自装填料为硅藻土的色谱柱分离后，收集部分经纯化，加入新制的碱性三硝基苯酚试液，摇匀，在22-25℃的暗处放置30分钟，照紫外-可见分光光度法，立即在485nm波长处，测定吸光度，计算，即得。

试剂：

1. 乙醇

2. 碱性三硝基苯酚

3. 三氯甲烷

4. 苯

仪器设备： 1. 可见分光光度计

2. 自制色谱柱

取长约200mm，内径约25mm、下端具有活塞的色谱管，底部填少许脱脂棉，取处理过的硅藻土（取色谱用的硅藻土150g，加稀盐酸1000mL，煮沸10分钟，放冷，滤过，用水洗涤至洗液遇pH试纸显中性，在105℃干燥后，再在500℃炽灼2小时，放冷）2g，加水1mL，充分混合，分次装入色谱管内，每次均用平头玻璃棒轻压使平；另取处理过的硅藻土3g，加甲酰胺2mL与水1mL，充分混匀，同法装柱，上覆一小块脱脂棉，轻压使平。

试样制备：供试品溶液的制备

精密称取本品10mg，置50mL量瓶中，加三氯甲烷10mL溶解后，加苯（同上法处理）稀释至刻度，摇匀，精密量取10mL，加入色谱注中，以苯（同上法处理）-三氯甲烷（3：1）洗脱，流速为每分钟不超过4mL，收集洗脱液于250mL量瓶中，至近刻度时，另加三氯甲烷稀释至刻度，摇匀作为供试品溶液。

注：“精密称取”系指称取重量应准确至所称取重量的千分之一。“精密量取”系指量取体积的准确度应符合国家标准中对该体积移液管的精度要求。

操作步骤：供试品的测定

精密量取上述洗脱液25mL与对照品溶液5mL，分别置锥形瓶中，在水浴上蒸干，残渣中各加乙醇0.5mL，蒸干，放冷至室温精密加入70%乙醇5mL，密塞，在22-25℃放置15分钟，并时时振摇，在精密加新制的碱性三硝基苯酚试液3mL，摇匀，在22-25℃的暗处放置30分钟，照紫外-可见分光光度法，在485nm波长处，依法测定吸光度，计算，即得。

洋地黄毒苷的药理作用

洋地黄毒苷在治疗量时，对心脏的作用表现为：

1、正性肌力作用：是一种直接作用，而不是通过神经机制实现的。其正性肌力作用是由于Na-K-ATP酶的抑制，钠、钾离子通过心肌细胞膜主动转运之能量，即由此酶提供。洋地黄毒苷与Na-K-ATP酶在细胞膜上可逆性结合，阻止了ATP的结合，阻抑Na和K的主动转运，钠泵失活，结果是细胞内Na增加，K减少，洋地黄苷类的电直接生理作用及毒性是由此而来的，细胞内Na增加能刺激Na-Ca2+交换增多，而使细胞内钙离子的增加可能是洋地黄毒苷产生正性肌力作用的基础。洋地黄毒苷对心力衰竭具有有益的血流动力学改变作用，可增加衰竭心脏的心排血量和心脏做功。洋地黄毒苷使心肌收缩力增加可导致心氧耗量增加，但同时使心脏收缩期心室腔中排血量增加，残余血量减少，又能反射性的使心率下降和降低外周血管阻力。心脏溶剂随之缩小和心率减慢。因此，心肌总的耗氧量减少。

2。电生理作用：治疗剂量的洋地黄毒苷轻度降低窦房结的自律性，使房室结传到时间和不应期延长，致使房室传导减慢，心房肌的应激性降低，缩短心房肌的不应期而延长房室结的不应期。这是由于迷走神经张力增高，抗肾上腺素能作用于程度较轻的神经直接作用引起的。中毒量洋地黄毒苷引起的电生理作用改编为自律性增高，抑制传导性可导致各种心率失常发生

3.自主神经系统作用

洋地黄毒苷作用于心肌，只有拟迷走和拟交感神经作用。迷走神经传导由中枢释放的冲动，对心脏活动发生持续的抑制性影响，是窦性心律减慢，房室传导延缓，心房不应期缩短。洋地黄毒苷的拟交感神经作用增加窦房结的兴奋节律；加快心肌和房室对兴奋的传导；增强心房肌和心室肌的收缩力。大剂量的洋地黄毒苷还能兴奋中枢神经系统，并可因较肝神经兴奋增强而诱发异位性心律失常。洋地黄毒苷属于非极性洋地黄毒苷的拟交感神经作用较强，只有较强的正性肌力作用，但易诱发或加重异位性心律失常。

4、血管作用

洋地黄毒苷的直接兴奋血管平滑肌或血管运动中枢作用，可使外周血管阻力增加

5、肾脏作用

对肾脏本身有轻微的直接和间接地利尿作用。

洋地黄毒苷的药动学

口服吸收迅速而完全，生物利用度高达90%以上，服药后1h血浆药物浓度达峰值，经4h达显效，6-12h达峰效应。主要经肝微粒体酶代谢消除，消除半衰期一般为4-7天。由肝汁排出，再循环后，最终由尿排出，80%皆为无活性代谢物。

适应症

低输出量性充血性心力衰竭、心房颤动和心房扑动、阵发性室上性心动过速。

禁忌症

Ⅱ度或Ⅲ度房室传导阻滞或窦性心动过缓、肥厚型梗阻性心肌病、预激综合征、心肌外的机械因素如心包填塞、缩窄性心包炎、严重心尖瓣狭窄所致心力衰竭和高钙血症。

注意事项

1、严重心肌损害及肾功能不全者慎用。肝病患者不宜用

2、本品主要口服，肌内注射很少采用，因易引起注射部位疼痛，且与口服生物利用度相同。

不良反应

洋地黄毒苷治疗量大约是中毒量的60%，易中毒，中毒量约为致死量的

60%。洋地黄毒苷中毒的临床表现为：1.消化系统：厌食、流涎、恶心、呕吐、腹泻及腹痛。心功能不全时，胃肠道淤血加重时的胃肠道症状应于洋地黄毒苷重度相区别

2.神经系统中毒症状：疲惫、头痛、失眠、忧郁、眩晕、精神错乱、定向障碍、梦魇及不安等，幻觉和其他精神反应等

3眼部改变：瞳孔放大，畏光、色觉改变、闪光、视力降低等，偶尔有暂时失明

4、心律失常：心率失常可能是洋地黄毒苷中毒的首发症状。任何类型的心律失常皆可发生。最常见的是室性早搏二联律或三联律，多源性室性早搏，非阵发性房室交界性心动过速伴房室分离，其发生尤其多见于原有心房颤动的患者。扭转型室性心动过速提示为洋地黄中毒已达晚期。

洋地黄毒苷的用法用量

洋地黄毒苷制剂的治疗应注重剂量的个体化。洋地黄毒苷的传统用法分为两个步骤，先短期内给予全效量，以基本控制心力衰竭症状，这一剂量也称为洋地黄化量，然后给与较小剂量维持，使血药浓度稳定与有效治疗浓度范围内保持疗效。给予全效量可口服洋地黄毒苷每次0.1mg,每天3-4次，至总量0.8-1.2mg。维持量为口服每天0.1mg。

在强心剂中，洋地黄最独特的作用为增强心肌收缩力的同时可减慢心率，而且无耐药性，服用方便，价格低廉，与利尿剂、ACE抑制剂合用有相加疗效，而且可抑制心衰时出现的神经内分泌活性增高，对心衰自然病程无不利影响，不增加病死率。

药物相互作用

1.洋地黄毒毒苷与利尿剂合用时，易因低钾血症而诱发心律失常，氢氯噻嗪不改变洋地黄毒毒苷的药动学，但非保钾利尿剂与洋地黄毒毒苷合用，可因利尿剂致低钾血症而增加洋地毒苷的毒性。

2.奎尼丁与洋地黄毒毒苷合用可使洋地黄毒毒苷血浆浓度显著增高。

3.维拉帕米与洋地黄毒毒苷合用，可使血清洋地黄毒毒苷浓度稍有增高。

4.巴比妥盐、苯妥英钠与洋地黄毒毒苷合用，因可使肝微粒体酶活力增高，故使血清洋地黄毒毒苷合用，因可使肝微粒体酶活力增高，故使血清洋地黄毒毒苷浓度降低。

5.考来烯胺树脂与洋地黄毒毒苷合用，在肠道内可吸附洋地黄毒毒苷，可使洋地黄毒毒苷生物利用度降低。

洋地黄毒苷中毒

洋地黄毒苷（锹吉妥辛、地支毒）为慢效强心苷类药物，其作用缓慢而持久。

口服全效量为0.7～1.2mg，于48～72h内分次口服；维持量为每次0.05～0.1mg，l/d;极量每次0.4mg，1mg/d。肌注常用量为每次0.2～1mg。口服几乎完全吸收，经2～4h起效，8～12h达最大效应。作用维持2～3周，静脉注射30min见效，4～8h达最大效应，由于有较大的蓄积作用，可能引起洋地黄中毒。人中毒血药浓度>0.0045mg/dl，成人致死量3mg。

临床表现

初期可见恶心、呕吐、腹泻、头晕、手足感觉异常及全身无力、黄视、绿视等。病情进一步加重可见情绪变化、不安、定向不能、精神错乱、噩梦、幻觉，视物模糊。

重症可见低血压、各种心律失常，如各种期前收缩，室速、室颤、房室传导阻滞、心动过缓、窦房阻滞、窦性停搏。

治疗

洋地黄毒苷中毒的治疗要点为：

见地高辛的治疗要点。

扩展阅读

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