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前列腺素类药

前列腺素是一组广泛存在于体内的自体活性物质,参与调节多种生理功能。胃肠道中的主要前列腺素包括前列腺素E(PGE)、前列腺素F(PGF)以及前列环素(PGI)。其中,胃部的前列腺素含量丰富,尤其在黏膜层中最为显著。

这类药物保护胃黏膜主要通过以下机制:

  1. 抑制胃酸分泌:前列腺素能有效抑制胃酸分泌,其抑酸效果与用药剂量成正比。它对基础和刺激后的胃酸分泌均有抑制作用。
  2. 强烈的细胞保护作用:前列腺素对某些有害物质引起的胃黏膜损伤具有防护作用。例如,在动物实验中,大剂量的阿司匹林或吲哚美辛会导致胃出血、溃疡甚至坏死;若提前给予前列腺素,则可防止这些病变的发生,并且这种效果与剂量密切相关。前列腺素通过多种方式保护细胞:增加胃黏液合成和分泌,促进十二指肠上皮细胞释放碳酸氢盐,抑制消化道中的组胺、五肽胃泌素及胃酸的分泌,对抗血栓素A2引起的血管收缩作用,以及增强细胞修复能力。

用于保护胃黏膜的主要前列腺素类药物包括喜克溃(米索前列醇)、恩前列素、利奥前列素、阿巴前列素、曲莫前列素和罗沙前列醇。其中,只有喜克溃已被正式应用于临床治疗。

喜克溃(米索前列醇)以片剂形式提供,每片含200微克。推荐剂量为每次口服200微克,每日4次(餐前及睡前服用)。疗程通常为4至8周。

中文名称 英文名称 CAS号 化学式 结构式图片
群博龙环已甲基碳酸酯 Trenbolone cyclohexylmethylcarbonate 23454-33-3 C26H34O4
群博龙环已甲基碳酸酯
米索前列醇酸 7-[3-Hydroxy-2-(4-hydroxy-4-methyloct-1-enyl)-5-oxocyclopentyl]heptanoic acid 112137-89-0 C21H36O5
米索前列醇酸
科里内酯 (1S,5R,6S,7R)-7-benzoyloxy-6-hydroxymethyl-2-oxabicyclo[3.3.0]octan-3-one 39746-00-4 C15H16O5
科里内酯
硫前列酮 Sulprostone 60325-46-4 C23H31NO7S
硫前列酮
甲烯前列素 meteneprost 61263-35-2 C23H38O4
甲烯前列素
氯前列烯醇钠 cloprostenol sodium 62561-03-9 C22H28ClO6*Na
氯前列烯醇钠
比马前列素 bimatoprost 155206-00-1 C25H37NO4
比马前列素
曲沃前列素 travoprost 157283-68-6 C26H35F3O6
曲沃前列素
曲前列尼尔 treprostinil 81846-19-7 C23H34O5
曲前列尼尔
拉坦前列素 latanoprost 130209-82-4 C26H40O5
拉坦前列素
恩前列素 enprostil 73121-56-9 C23H28O6
恩前列素
异丙基乌诺前列酮 rescula 120373-24-2 C25H44O5
异丙基乌诺前列酮
度他雄胺 dutasteride 164656-23-9 C27H30F6N2O2
度他雄胺
奥洛前列素 methyl 7-[(1R,2R,3R)-3-hydroxy-2-[(E,3S,5S)-3-hydroxy-5-methylnon-1-enyl]-5-oxocyclopentyl]-6-oxoheptanoate 70667-26-4 C23H38O6
奥洛前列素
地诺前列酮 dinoprostone 363-24-6 C20H32O5
地诺前列酮
地诺前列素 dinoprost 551-11-1 C20H34O5
地诺前列素
吉美前列素 gemeprost 64318-79-2 C23H38O5
吉美前列素
卡巴他赛 carbazitaxel 183133-96-2 C45H57NO14
卡巴他赛
卡前列素氨基丁三醇 carboprost tromethamine 58551-69-2 C4H11NO3*C21H36O5
卡前列素氨基丁三醇
卡前列素 Carboprost 35700-23-3 C21H36O5
卡前列素
前列地尔 ALPROSTADIL 745-65-3 C20H34O5
前列地尔
依前列醇 Epoprostenol 35121-78-9 C20H32O5
依前列醇
伊洛前列素苯甲酰甲基酯 Iloprost phenacyl ester 78919-13-8 C30H38O5
伊洛前列素苯甲酰甲基酯
伊洛前列素 5-{(E)-(1S,5S,6R,7R)-7-hydroxy-6-[(E)-(3S,4RS)-3-hydroxy-4-methyl-1-octen-6-ynyl]-bicyclo[3.3.0]octa-3-ylidene)-pentanoic acid 78919-13-8 C22H32O4
伊洛前列素
他氟前列素 tafluprost 209860-87-7 C25H34F2O5
他氟前列素
Prosta-2,13-dien-1-oicacid,11,15-dihydroxy-16,16-dimethyl-9-oxo-,methylester,(2E,11a,13E,15R)-(?脿)-(9CI) Gemeprost 64318-79-2 C23H38O5
Prosta-2,13-dien-1-oicacid,11,15-dihydroxy-16,16-dimethyl-9-oxo-,methylester,(2E,11a,13E,15R)-(?脿)-(9CI)
9-羟基-19,20-二去甲前列腺烷酸 7-(2-hexyl-5-hydroxy-cyclopentyl)-heptanoic acid 56695-65-9 C18H34O3
9-羟基-19,20-二去甲前列腺烷酸
(5E,13E)-11,15-二羟基-9-氧代前列腺-5,13-二烯-1-酸 (+/-)-prostaglandin E<sub>2</sub> 363-24-6 C20H32O5
(5E,13E)-11,15-二羟基-9-氧代前列腺-5,13-二烯-1-酸
(3aR,4S,5R,6aS)-(-)-六氢-4-(羟甲基)-2-氧代-2H-环戊并[b]呋喃-5-基 1,1'-联苯-4-甲酸酯 (-)-Corey lactone 5-(4-phenylbenzoate) 31752-99-5 C21H20O5
(3aR,4S,5R,6aS)-(-)-六氢-4-(羟甲基)-2-氧代-2H-环戊并[b]呋喃-5-基 1,1'-联苯-4-甲酸酯
(2E,11Α,13E,15S,17S)-11,15-二羟基-17,20-二甲基-9-氧代前列-2,13-二烯-1-酸(2E,11Α,13E,15S,17S)-11,15-DIHYDROXY-17,20-DIMETHYL-9-OXOPROSTA-2,13-DIEN-1-OICACID limaprost 74397-12-9 C22H36O5
(2E,11Α,13E,15S,17S)-11,15-二羟基-17,20-二甲基-9-氧代前列-2,13-二烯-1-酸(2E,11Α,13E,15S,17S)-11,15-DIHYDROXY-17,20-DIMETHYL-9-OXOPROSTA-2,13-DIEN-1-OICACID
(+)-5-反式-氯前列醇 D-Cloprostenol 57968-81-7 C22H29ClO6
(+)-5-反式-氯前列醇
—— tromethamine prostaglandin 58551-69-2 C4H11NO3*C21H36O5
tromethamine prostaglandin
—— Estrumate (TN) 55028-72-3 C22H28ClNaO6
Estrumate (TN)
—— 5-[3,3a,4,5,6,6a-Hexahydro-5-hydroxy-4-(3-hydroxy-4-methyl-1-octen-6-ynyl)pentalen-2(1H)-ylidene]pentanoic acid 78919-13-8 C22H32O4
5-[3,3a,4,5,6,6a-Hexahydro-5-hydroxy-4-(3-hydroxy-4-methyl-1-octen-6-ynyl)pentalen-2(1H)-ylidene]pentanoic acid
—— 4-Diethylaminosalicylicacid 99631-11-5 C23H28O6
4-Diethylaminosalicylicacid
—— 16-(3-chlorophenoxy)-17,18,19,20-tetranorprostaglandin F2 alpha 40665-92-7 C22H29ClO6
16-(3-chlorophenoxy)-17,18,19,20-tetranorprostaglandin F2 alpha
—— epoprostenol sodium 61849-14-7 C20H31O5*Na
epoprostenol sodium
—— [(4R,5R)-4-(hydroxymethyl)-2-oxo-3,3a,4,5,6,6a-hexahydrocyclopenta[b]furan-5-yl] 4-phenylbenzoate 31752-99-5 C21H20O5
[(4R,5R)-4-(hydroxymethyl)-2-oxo-3,3a,4,5,6,6a-hexahydrocyclopenta[b]furan-5-yl] 4-phenylbenzoate
—— sodium;4-[(1R,2R,3aS,8bS)-2-hydroxy-1-[(3S)-3-hydroxy-4-methyloct-1-en-6-ynyl]-2,3,3a,8b-tetrahydro-1H-cyclopenta[b][1]benzofuran-5-yl]butanoate 88475-69-8 C24H29O5*Na
sodium;4-[(1R,2R,3aS,8bS)-2-hydroxy-1-[(3S)-3-hydroxy-4-methyloct-1-en-6-ynyl]-2,3,3a,8b-tetrahydro-1H-cyclopenta[b][1]benzofuran-5-yl]butanoate
—— Dtxcid0028955 60325-46-4 C23H31NO7S
Dtxcid0028955
—— Prostaglandin I2; Prostacyclin 61849-14-7 C20H31NaO5
Prostaglandin I2; Prostacyclin
—— sodium;4-[(2R,3aS,8bS)-2-hydroxy-1-[(E,3S)-3-hydroxy-4-methyloct-1-en-6-ynyl]-2,3,3a,8b-tetrahydro-1H-cyclopenta[b][1]benzofuran-5-yl]butanoate 88475-69-8 C24H29NaO5
sodium;4-[(2R,3aS,8bS)-2-hydroxy-1-[(E,3S)-3-hydroxy-4-methyloct-1-en-6-ynyl]-2,3,3a,8b-tetrahydro-1H-cyclopenta[b][1]benzofuran-5-yl]butanoate
—— (3aR-(3aalpha,4alpha,5beta,6aalpha))-Hexahydro-4-(hydroxymethyl)-2-oxo-2H-cyclopenta(b)furan-5-yl benzoate 39746-00-4 C15H16O5
(3aR-(3aalpha,4alpha,5beta,6aalpha))-Hexahydro-4-(hydroxymethyl)-2-oxo-2H-cyclopenta(b)furan-5-yl benzoate
—— ICI 80996 sodium salt 55028-72-3 C22H28ClNaO6
ICI 80996 sodium salt
—— 15(S)-15-methyl-PGF2alpha 58551-69-2 C21H36O5
15(S)-15-methyl-PGF2alpha
—— beraprost sodium 88475-69-8 C24H29O5*Na
beraprost sodium
—— (+/-)-15-Deoxy-[16RS]-16-hydroxy-16-methylprostaglandin E1 112137-89-0 C21H36O5
(+/-)-15-Deoxy-[16RS]-16-hydroxy-16-methylprostaglandin E1
—— Sodium 4-(2-hydroxy-1-(3-hydroxy-4-methyloct-1-en-6-yn-1-yl)-2,3,3a,8b-tetrahydro-1H-cyclopenta[b]benzofuran-5-yl)butanoate 88475-69-8 C24H29NaO5
Sodium 4-(2-hydroxy-1-(3-hydroxy-4-methyloct-1-en-6-yn-1-yl)-2,3,3a,8b-tetrahydro-1H-cyclopenta[b]benzofuran-5-yl)butanoate
—— (Z)-7-((1R,2R,3R)-3-hydroxy-2-((R,E)-3-hydroxy-4-phenoxybut-1-enyl)-5-oxocyclopentyl)-N-(methylsulfonyl)hept-5-enamide 60325-46-4 C23H31NO7S
(Z)-7-((1R,2R,3R)-3-hydroxy-2-((R,E)-3-hydroxy-4-phenoxybut-1-enyl)-5-oxocyclopentyl)-N-(methylsulfonyl)hept-5-enamide
—— 5-[(3aS,5R,6aS)-5-hydroxy-4-[(E,3S)-3-hydroxy-4-methyloct-1-en-6-ynyl]-3,3a,4,5,6,6a-hexahydro-1H-pentalen-2-ylidene]pentanoic acid 78919-13-8 C22H32O4
5-[(3aS,5R,6aS)-5-hydroxy-4-[(E,3S)-3-hydroxy-4-methyloct-1-en-6-ynyl]-3,3a,4,5,6,6a-hexahydro-1H-pentalen-2-ylidene]pentanoic acid