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药品详细

Terlipressin(特利加压素)

化学结构式图
中文名
特利加压素
英文名
Terlipressin
分子式
C52H74N16O15S2
化学名
(2S)-6-amino-2-{[(2S)-1-{[(4R,7S,10S,13S,16S,19R)-19-{2-[2-(2-aminoacetamido)acetamido]acetamido}-13-benzyl-10-(2-carbamoylethyl)-7-(carbamoylmethyl)-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-4-yl]carbonyl}pyrrolidin-2-yl]formamido}-N-(carbamoylmethyl)hexanamide
分子量
Average: 1227.372
Monoisotopic: 1226.496097158
CAS号
14636-12-5
ATC分类
H01B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Terlipressin is an analogue of vasopressin used as a vasoactive drug in the management of hypotension. It has been found to be effective when norepinephrine does not help. [Wikipedia]

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Pesaturo AB, Jennings HR, Voils SA: Terlipressin: vasopressin analog and novel drug for septic shock. Ann Pharmacother. 2006 Dec;40(12):2170-7. Epub 2006 Dec 5. Pubmed
    2. Klein M, Weksler N, Borer A, Koyfman L, Kesslin J, Gurman GM: Terlipressin facilitates transport of septic patients treated with norepinephrine. Isr Med Assoc J. 2006 Oct;8(10):691-3. Pubmed
    3. Leone M, Charvet A, Delmas A, Albanese J, Martin C, Boyle WA: Terlipressin: a new therapeutic for calcium-channel blockers overdose. J Crit Care. 2005 Mar;20(1):114-5. Pubmed
    4. Matok I, Vard A, Efrati O, Rubinshtein M, Vishne T, Leibovitch L, Adam M, Barzilay Z, Paret G: Terlipressin as rescue therapy for intractable hypotension due to septic shock in children. Shock. 2005 Apr;23(4):305-10. Pubmed
    5. Kam PC, Williams S, Yoong FF: Vasopressin and terlipressin: pharmacology and its clinical relevance. Anaesthesia. 2004 Oct;59(10):993-1001. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Polypeptides
    • Phenethylamines
    • Phenylpropylamines
    • Lactams
    • Amphetamines
    Substructures
    • Polypeptides
    • Hydroxy Compounds
    • Phenols and Derivatives
    • Amino Ketones
    • Aliphatic and Aryl Amines
    • Pyrrolidines
    • Benzene and Derivatives
    • Carboxylic Acids and Derivatives
    • Organic Disulfides
    • Carbamates and Derivatives
    • Phenethylamines
    • Heterocyclic compounds
    • Aromatic compounds
    • Carboxamides and Derivatives
    • Phenylpropylamines
    • Lactams
    • Phenyl Esters
    • Amphetamines
    适应症
    药理
    Indication Commonly used to stop bleeding of varices in the food pipe (oesophagus).
    Pharmacodynamics Terlipressin is a medicine similar to a naturally occurring hormone present in the body, known as antidiuretic hormone (ADH) or vasopressin. ADH has two main effects in the body. Firstly, it causes narrowing of blood vessels (vasoconstriction), thereby limiting blood flow to a particular area of the body. It also acts on receptors in the kidney to retain water in the body, which helps to prevent excessive loss of water in the urine.
    Mechanism of action Terlipressin, an analogue of vasopressin, acts on three different receptors, vasopressin receptor V1a (which initiates vasoconstriction, liver gluconeogenesis, platelet aggregation and release of factor VIII), vasopressin receptor V1b (which mediates corticotrophin secretion from the pituitary) and vasopressin receptor V2 which controls free water reabsorption in the renal medullar. The binding of terlipressin to the V2 receptor activates adenylate cyclase which causes the release of aquaporin 2 channels into the cells lining the renal medullar duct. This allows water to be reabsorbed down an osmotic gradient so the urine is more concentrated.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Approximately 30%
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties Not Available
    Predicted Properties
    Property Value Source
    water solubility 1.67e-01 g/l ALOGPS
    logP -1.6 ALOGPS
    logP -10 ChemAxon
    logS -3.9 ALOGPS
    pKa (strongest acidic) 9.43 ChemAxon
    pKa (strongest basic) 10.26 ChemAxon
    physiological charge 2 ChemAxon
    hydrogen acceptor count 17 ChemAxon
    hydrogen donor count 16 ChemAxon
    polar surface area 512.85 ChemAxon
    rotatable bond count 25 ChemAxon
    refractivity 305.18 ChemAxon
    polarizability 123.88 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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