盐酸哌仑西平

作用与用途药代动力学适应症生物活性体外研究体内研究盐酸哌仑西平试剂级价格

盐酸哌仑西平

CAS号:29868-97-1
英文名:Pirenzepine hydrochloride
中文名:盐酸哌仑西平
CBNumber:CB1245572
分子式:C19H22ClN5O2
分子量:387.87
MOL File:29868-97-1.mol

盐酸哌仑西平化学性质

熔点 :248-250°C
储存条件 :Inert atmosphere,2-8°C
溶解度 :H₂O: 50 mg/mL
形态 :powder
颜色 :white
水溶解性 :Soluble to 100 mM in water
敏感性 :Hygroscopic
CAS 数据库 :29868-97-1(CAS DataBase Reference)

安全信息

WGK Germany :2
RTECS号 :UU7883000
海关编码 :2933.99.7500
毒性 :dog,LD50,intravenous,62500ug/kg (62.5mg/kg),Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 19, Pg. 544, 1988.

盐酸哌仑西平化学药品说明书

盐酸哌仑西平
盐酸哌仑西平片

盐酸哌仑西平性质、用途与生产工艺

作用与用途盐酸哌仑西平为一种具有选择性的抗胆碱能药物，对胃壁细胞的毒蕈碱受体有高度亲和力，而对平滑肌、心肌和唾液腺等的毒蕈碱受体的亲和力低，故应用一般治疗剂量时，仅能抑制胃酸分泌，而很少有其它抗胆碱药物对瞳孔、胃肠平滑肌、心脏、唾液腺和膀胱肌等的副作用。剂量增大则可抑制唾液分泌，只有大剂量才能抑制胃肠平滑肌和引起心动过速。本品不能透过血脑屏障，故不影响中枢神经系统。人口服、肌注或静注本品后，无论是基础胃酸分泌，还是由外源性五肽胃泌素、胰岛素引起的胃酸分泌均受到抑制。本品对胃液的pH影响不大，主要是使胃液（包括胃蛋白酶原和胃蛋白酶）分泌量减少，从而使胃最大酸分泌和最高酸分泌下降。
药代动力学口服吸收不完全，绝对生物利用度为20%～30%，与食物同服可减少吸收。血药浓度于2～3小时达峰值。体内分布广泛，除脑和胚胎组织外的所有器官和组织均有分布，其中以肝、肾的浓度最高。血浆蛋白结合率为10%～12%。体内很少代谢，85%以原形药从肾脏和胆道排泄。口服量的4%～8%从尿中排出，90%从粪便排出。给药后 3～4日方能全部排泄，但未见有药物蓄积。半衰期为10～12小时。
适应症盐酸哌仑西平为抑酸药。临床主要用于各种酸相关性疾患，如：十二指肠溃疡、胃溃疡、胃-食管反流症、高酸性胃炎、应激性溃疡、急性胃粘膜出血、胃泌素瘤等。
生物活性 Pirenzepine dihydrochloride (LS519) 是一种选择性 M1 型毒蕈碱受体拮抗剂。
体外研究

The antisecretory properties of pirenzepine on gastric acid and pepsin secretion may be attributed to the antagonistic activity of the drug on muscarinic M1 receptors of gastric intramural plexuses, whereas the effect on parietal muscarinic M2 receptors seems of less importance. Additional inhibitory mechanisms on gastric secretion may be represented by pirenzepine-induced increase in somatostatin release from gastrointestinal system. Significant cytoprotective properties of pirenzepinehave been observed on a variety of experimentally induced peptic ulcerations. Pirenzepine (5-500 μg/mL) inhibits agonist-(acetylcholine-, carbachol- or nicotine-) induced contractions of the toad isolated rectus abdominis muscle, and depresses electrically provoked twitches of the rat phrenic nerve-hemidiaphragm muscle preparation.
体内研究

Pirenzepine is potent in impairing learning of an avoidance; much higher doses are required to antagonize other central muscarinic effects. Pirenzepine is found to impair passive avoidance learning when given i.c.v. 20 min pre-training. The median latencies in pirenzepine-treated animals are 79.5, 11, 27 and 25.5 seconds with doses of 0.03, 0.1, 0.3 and 1 μg per mouse respectively. Acid and pepsin secretion stimulated by either bethanechol or the vagus are inhibited in a dose-responsive manner by pirenzepine. Pirenzepine (5-25 mg/kg i.v.) depresses indirect electrical stimulation-evoked twitches of the cat tibialis anterior and soleus muscle preparations.
用途用于胃及十二指肠溃疡、急性胃粘膜出血等症。