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药品详细

Pirenzepine(哌仑西平)

化学结构式图
中文名
哌仑西平
英文名
Pirenzepine
分子式
C19H21N5O2
化学名
2-[2-(4-methylpiperazin-1-yl)acetyl]-2,4,9-triazatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-10-one
分子量
Average: 351.4023
Monoisotopic: 351.169524941
CAS号
28797-61-7
ATC分类
A02B 未知
药物类型
small molecule
阶段
approved
商品名
Bisvanil;Gasteril;Gastrozepin;Leblon;Pirenzepin;Pirenzepina [INN-Spanish];Pirenzepine Gastrozepin;Pirenzepinum [INN-Latin];Tabe;Ulcosan;
同义名
基本介绍

An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as cimetidine and ranitidine. It is generally well tolerated by patients. [PubChem]

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Czepita D: [Fundamentals of modern treatment of myopia] Ann Acad Med Stetin. 2005;51(2):5-9. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Benzodiazepines
    • Lactams
    Substructures
    • Benzodiazepines
    • Amino Ketones
    • Pyridines and Derivatives
    • Piperazines
    • Benzene and Derivatives
    • Aliphatic and Aryl Amines
    • Carboxylic Acids and Derivatives
    • Aminopyridines and Derivatives
    • Heterocyclic compounds
    • Aromatic compounds
    • Carboxamides and Derivatives
    • Lactams
    • Benzoyl Derivatives
    • Benzamides
    • Anilines
    适应症
    gastric acid RELATED DISORDERS 中和胃酸;
    药理
    Indication For the treatment of peptic ulcer, gastric ulcer, and duodenal ulcer.
    Pharmacodynamics Pirenzepine belongs to a group of medications called antispasmodics/anticholinergics. These medications are used to relieve cramps or spasms of the stomach, intestines, and bladder. Pirenzepine is used to treat duodenal or stomach ulcers or intestine problems. It can be used together with antacids or other medicine in the treatment of peptic ulcer. It may also be used to prevent nausea, vomiting, and motion sickness.
    Mechanism of action Pirenzepine is a muscarinic receptor antagonist and binds to the muscarinic acetylcholine receptor. The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    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
    Pathway Name SMPDB ID
    Smp00246 Pirenzepine Pathway SMP00246
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    logP 0.6 Not Available
    Caco2 permeability -6.36 ADME Research, USCD
    Predicted Properties
    Property Value Source
    water solubility 6.82e-01 g/l ALOGPS
    logP 1.26 ALOGPS
    logP 0.85 ChemAxon
    logS -2.7 ALOGPS
    pKa (strongest acidic) 9.57 ChemAxon
    pKa (strongest basic) 7.59 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 5 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 68.78 ChemAxon
    rotatable bond count 2 ChemAxon
    refractivity 100.93 ChemAxon
    polarizability 37.11 ChemAxon
    药物相互作用
    食物相互作用
    • Take 30 minutes before breakfast and at bedtime.

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