塞浦西他啶
化合物
(重定向自赛庚啶)
此条目需要精通或熟悉医学的编者参与及协助编辑。 (2020年12月15日) |
塞浦西他啶(Cyproheptadine),或名赛庚啶 ,是第一代抗组织胺药,具有抗乙酰胆碱和局部麻醉的功能,也是儿童抗过敏药水希普利敏的主要成分。
临床资料 | |
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读音 | (/ˌsaɪproʊˈhɛptədiːn/[1] |
商品名 | Periactin, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682541 |
核准状况 | |
怀孕分级 |
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给药途径 | Oral |
ATC码 | |
法律规范状态 | |
法律规范 |
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药物动力学数据 | |
血浆蛋白结合率 | 96 to 99% |
药物代谢 | Hepatic,[3][4] mostly CYP3A4 mediated. |
生物半衰期 | 8.6 hours[2] |
排泄途径 | 粪便 (2–20%; of which, 34% as unchanged drug) 与 肾 (40%; none as unchanged drug)[3][4] |
识别信息 | |
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CAS号 | 129-03-3 969-33-5(盐酸盐) |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.004.482 |
化学信息 | |
化学式 | C21H21N |
摩尔质量 | 287.41 g·mol−1 |
3D模型(JSmol) | |
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医疗使用
编辑- 塞浦西他啶用于治疗过敏反应 (特别是花粉症).[6] 用于此目的证实有效,但是第二代抗组织胺药像是酮替酚与氯雷他定也有相同的结果,且副作用较少。[7]
- 它也被用作偏头痛的预防性治疗。在2013年的一项研究中,开始治疗后7至10天内,患者的偏头痛发生率显著降低。这些患者在服药前偏头痛发作的平均频率为每月8.7次,开始治疗后3个月降至每月3.1次。[7][8] 在英国和其他一些国家/地区,药品仿单上有此用法。
- 它也被药品“仿单核准适应症外的使用”在婴儿周期性呕吐症候群的治疗。这种用途的唯一证据来自回顾性研究。[9]
- 塞浦西他啶有时被“仿单核准适应症外的使用”,以改善服用抗精神病药物的患者的静坐不能。[10]
- 它也被药品“仿单核准适应症外的使用”于治疗各种皮肤病,包括精神性搔痒症|[11]、药物诱发的多汗症(出汗过多)[12],以及预防表浅性单纯性水疱性表皮松解症的水疱形成。[13]
- 该药物的作用之一是食欲增加和体重增加,这导致该药物在消瘦的儿童以及囊肿性纤维化患者中用于此目的(在美国为“仿单核准适应症外的使用”)。[14][15][16]
- 它也使用在“仿单核准适应症外的使用”治疗中度至重度血清素综合症,与使用血清素类药物有关的复杂症状,像是选择性5-羟色胺再摄取抑制剂 (与单胺氧化酶抑制剂),以及在血清素产生的类癌肿瘤导致血液中5-羟色胺升高的案例。[17][18]
副作用
编辑- 镇静和困倦(通常是短暂的)Sedation and sleepiness (often transient)
- 头晕 Dizziness
- 协调不佳 Disturbed coordination
- 混乱 Confusion
- 躁动不安 Restlessness
- 兴奋 Excitation
- 紧张 Nervousness
- 震颤 Tremor
- 易怒 Irritability
- 失眠 Insomnia
- 感觉异常 Paresthesias
- 神经炎 Neuritis
- 抽搐 Convulsions
- 欣快感 Euphoria
- 幻觉 Hallucinations
- 歇斯底里 Hysteria
- 模糊 Faintness
- 皮疹和水肿的过敏表现 Allergic manifestation of rash and edema
- 发汗 Diaphoresis
- 荨麻疹 Urticaria
- 对光敏感 Photosensitivity
- 急性迷路炎 Acute labyrinthitis
- 复视(双眼) Diplopia (seeing double)
- 眩晕 Vertigo
- 耳鸣 Tinnitus
- 低血压 Hypotension (low blood pressure)
- 心悸 Palpitation
- 期前收缩 Extrasystoles
- 过敏性休克 Anaphylactic shock
- 溶血性贫血 Hemolytic anemia
- 诸如白细胞减少症,粒细胞缺乏症和血小板减少症等血液异常 Blood dyscrasias such as leukopenia, agranulocytosis and thrombocytopenia
- 胆汁淤积 Cholestasis
- 对肝脏的影响:
- 上腹窘迫 Epigastric distress
- 食欲不振 Anorexia
- 恶心 Nausea
- 呕吐 Vomiting
- 腹泻 Diarrhea
- 抗胆碱能副作用:
- 视力模糊 Blurred vision
- 便秘 Constipation
- 口腔干燥症(口干) Xerostomia (dry mouth)
- 心动过速(高心率)Tachycardia (high heart rate)
- 尿潴留 Urinary retention
- 排尿困难 Difficulty passing urine
- 鼻塞 Nasal congestion
- 鼻或喉咙干燥 Nasal or throat dryness
- 频尿 Urinary frequency
- 早期月经 Early menses
- 支气管分泌物增厚 Thickening of bronchial secretions
- 胸闷气喘 Tightness of chest and wheezing
- 疲劳 Fatigue
- 寒意 Chills
- 头痛 Headache
- 食欲增加 Increased appetite
- 体重增加 Weight gain
用药过量
编辑过量使用时,有时建议使用活性炭进行洗胃。这些症状通常表明中枢神经系统抑制(或在某些情况下相反地刺激中枢神经系统)和过度的抗胆碱能副作用。小鼠的半数致死量(LD50)为 123 mg/kg,,大鼠的半数致死量为 295 mg/kg 。[3][4]
药理
编辑药效学
编辑塞浦西他啶对此表列出的所有受体均表现为拮抗剂或逆向激动剂。[20]
Site | Ki (nM)[a] | Action[b] | Species | Ref. |
---|---|---|---|---|
H1 | 0.06 | ↓ | Human | |
H2 | ND | ND | ||
H3 | >10,000 | Human | ||
H4 | 202 | Human | ||
M1 | 12 | ↓ | Human | |
M2 | 7 | ↓ | Human | |
M3 | 12 | ↓ | Human | |
M4 | 8 | ↓ | Human | |
M5 | 11.8 | ↓ | Human | |
5-HT1A | 59 | Human | ||
5-HT2A | 1.67 | ↓ | Human | |
5-HT2B | 1.54 | ↓ | Human | |
5-HT2C | 2.23 | ↓ | Human | |
5-HT3 | 228 | Mouse | ||
5-HT6 | 142 | Human | ||
5-HT7 | 123 | Human | ||
D1 | 117 | Human | ||
D2 | 112 | ↓ | Human | |
D3 | 8 | Human | ||
SERT | 4,100 | Rat | ||
NET | 290 | Rat | ||
DAT | ND | ND | ||
塞浦西他啶是一种非常有效的抗组胺药或H1受体的拮抗剂。它在较高浓度下还具有抗胆碱能、抗血清素能和抗多巴胺能活性。它是5-HT2受体的强效拮抗剂,这是其治疗血清素综合症的基础。
药物代谢动力学
编辑化学
编辑研究
编辑在一项规模较小的精神分裂症患者中,辅助使用塞浦西他啶作为辅助治疗,该患者的病情稳定且正在接受其他药物治疗。虽然注意力和口语流利性似乎有所改善,但这项研究规模太小,不足以概括。[23]在另两项针对精神分裂症患者的试验中,也已对其进行了佐剂研究,总共约有50人,并且似乎没有效果。[24]
兽医用途
编辑塞浦西他啶使用在猫的食欲刺激剂[26] ,也可作为哮喘的辅助治疗剂。[27] 可能的副作用包括刺激和攻击行为。[28]它在猫的生物半衰期为 12 小时。[27]
参考资料
编辑- ^ Cyproheptadine. Dictionary.com Unabridged. Random House.
- ^ 2.0 2.1 Gunja N, Collins M, Graudins A. A comparison of the pharmacokinetics of oral and sublingual cyproheptadine. Journal of Toxicology. Clinical Toxicology. 2004, 42 (1): 79–83. PMID 15083941. S2CID 20196551. doi:10.1081/clt-120028749.
- ^ 3.0 3.1 3.2 3.3 CYPROHEPTADINE HYDROCHLORIDE tablet [Boscogen, Inc.]. DailyMed. Boscogen, Inc. November 2010 [26 October 2013]. (原始内容 (PDF)存档于2013-07-04).
- ^ 4.0 4.1 4.2 4.3 PRODUCT INFORMATION PERIACTIN® (cyproheptadine hydrochloride) (PDF). Aspen Pharmacare Australia. Aspen Pharmacare Australia Pty Ltd. 17 November 2011 [26 October 2013]. (原始内容 (PDF)存档于29 October 2013).
- ^ Fischer, Jnos; Ganellin, C. Robin. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 547 [2020-12-15]. ISBN 9783527607495. (原始内容存档于2021-08-29) (英语).
- ^ MedlinePlus Drug Information: Cyproheptadine. [2020-12-15]. (原始内容存档于2008-10-01).
- ^ 7.0 7.1 De Bruyne, P; Christiaens, T; Boussery, K; Mehuys, E; Van Winckel, M. Are antihistamines effective in children? A review of the evidence. Archives of Disease in Childhood. January 2017, 102 (1): 56–60. PMID 27335428. S2CID 21185048. doi:10.1136/archdischild-2015-310416.
- ^ Saito, Y; Yamanaka, G; Shimomura, H; Shiraishi, K; Nakazawa, T; Kato, F; Shimizu-Motohashi, Y; Sasaki, M; Maegaki, Y. Reconsideration of the diagnosis and treatment of childhood migraine: A practical review of clinical experiences. Brain & Development. May 2017, 39 (5): 386–394. PMID 27993427. S2CID 34703034. doi:10.1016/j.braindev.2016.11.011.
- ^ Salvatore, S; Barberi, S; Borrelli, O; Castellazzi, A; Di Mauro, D; Di Mauro, G; Doria, M; Francavilla, R; Landi, M; Martelli, A; Miniello, VL; Simeone, G; Verduci, E; Verga, C; Zanetti, MA; Staiano, A; SIPPS Working Group on, FGIDs. Pharmacological interventions on early functional gastrointestinal disorders. Italian Journal of Pediatrics. 16 July 2016, 42 (1): 68. PMC 4947301 . PMID 27423188. doi:10.1186/s13052-016-0272-5.
- ^ Taylor, David; Paton, Carol; Kapur, Shitij. The Maudsley Prescribing Guidelines in Psychiatry. John Wiley & Sons. 2015: 85 [2020-12-15]. ISBN 9781118754573. (原始内容存档于2021-08-28) (英语).
- ^ Szepietowski, JC; Reszke, R. Psychogenic Itch Management 50. 2016: 124–32. ISBN 978-3-318-05888-8. PMID 27578081. doi:10.1159/000446055.
|journal=
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- ^ Pfendner, Ellen G.; Bruckner, Anna L. Epidermolysis Bullosa Simplex. GeneReviews. October 13, 2016 [2020-12-15]. PMID 20301543. (原始内容存档于2020-10-22).
- ^ Ciproheptadina, estimulante del apetito (Cyproheptadine, appetite stimulant). [2020-12-15]. (原始内容存档于2020-10-24).
- ^ Bioplex NF. [2020-12-15]. (原始内容存档于2018-04-18).
- ^ Harrison ME, Norris ML, Robinson A, Spettigue W, Morrissey M, Isserlin L. Use of cyproheptadine to stimulate appetite and body weight gain: A systematic review.. Appetite. 2019, 137: 62–72. PMID 30825493. S2CID 72333631. doi:10.1016/j.appet.2019.02.012.
- ^ Rossi, S (编). Australian Medicines Handbook 2013. Adelaide: The Australian Medicines Handbook Unit Trust. 2013. ISBN 978-0-9805790-9-3.
- ^ Iqbal, MM; Basil, MJ; Kaplan, J; Iqbal, MT. Overview of serotonin syndrome. Annals of Clinical Psychiatry. November 2012, 24 (4): 310–8. PMID 23145389.
- ^ Chertoff, Jason. Cyproheptadine-Induced Acute Liver Failure. ACG Case Reports Journal. 8 July 2014, 1 (4): 212–213. PMC 4286888 . PMID 25580444. doi:10.14309/crj.2014.56.
- ^ 20.0 20.1 Roth, BL; Driscol, J. PDSP Ki Database. Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. [14 August 2017]. (原始内容存档于2021-08-28).
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