奥昔布宁氯片
组成
oxyspas-2.5片
¤每个未涂布平板包含：
奥昔布宁氯的USP ............ 2.5毫克

描述
•奥昔布宁是一种人工合成的叔胺酯。它具有抗胆碱能（抗胆碱），解痉药和局部麻醉剂（抗胆碱能药物被用于治疗多种疾病，如胃肠痉挛，膀胱痉挛，气喘，晕车，肌肉痉挛，某些有毒化合物中毒，以及属性。辅助麻醉）。
它抑制muscurinic行动平滑肌肉乙酰胆碱，从而放松膀胱平滑肌。（化合物乙酰胆碱是周围神经系统（PNS）和中枢神经系统的神经递质）
 

药
毒蕈碱型胆碱受体的行动
◊奥昔布宁反对乙酰胆碱诱导的刺激副交感神经的毒蕈碱受体网站

逼尿肌和其他平滑肌的行动
◊奥昔布宁对平滑肌的直接作用膀胱（逼尿肌松弛作用）

尿动力学性能的影响
◊有一些有益的尿动力学的影响，如减少在排空和灌浆阶段的最大膀胱压力，增加膀胱容量，奥昔布宁

药代动力学
口服吸收~~ 100％
发病行动30 - 60分钟
presystemic的代谢~~ 94％
血浆半衰期
范围
平均0.84 - 2.90h
1.6h
血浆蛋白招投标83 - 85％

排尿（排尿）反射
o在此反射弧，副交感神经纤维，引起逼尿肌的收缩和放松内部尿道括约肌。
Ø排尿，还没有发生，因为尿道外括约肌保持关闭。
o有自愿尿道外括约肌松弛，排尿发生

主治
»Oxyspas被表示为缓解症状与神经性膀胱疾病的患者或特发性逼尿肌不稳定膀胱不稳定（如尿急，尿频，尿失禁）。
»此外，Oxyspas也可能被用于5岁以下儿童夜尿多。

用法用量与管理
成人：
常用剂量是5毫克，每天2 - 3次。
»最大推荐剂量是5毫克，每日4次。

在5岁以下儿童患者：
常用剂量为2.5毫克，一天两次。
最大推荐剂量为5毫克，每日3次。
»对于夜尿，在过去的剂量应给予睡前。

膀胱奥昔布宁
O的奥昔布宁膀胱当局已展开调查，作为一种抗胆碱能副作用减少，而维持临床疗效的手段。

方法
直径为5毫克片剂粉碎，溶解在30ml蒸馏水两次或三次每日。
O的解决方案，然后通过保​​留至少30-60分钟的膀胱灌注导管注入。

灌注的理想人选
»与逼尿肌反射亢进引起的神经系统疾病，在其中已经存在的导尿管的患者。
»患者没有响应或不能耐受其他药物治疗。
可能需要膀胱手术的病人会是谁。
»失败后口服奥昔布宁治疗的患者。

膀胱奥昔布宁的好处口服制剂
•迅速吸收
•达到较高的血药浓度比口服
•免费的抗胆碱能副作用表明，肝代谢物口服奥昔布宁是负责的副作用
•同样有效改善膀胱功能障碍
•吸收没有改变，由于当地膀胱损伤如尿路感染或pH值

禁忌
•与未经治疗的闭角型青光眼患者和患者的前房狭窄角度。
•胃肠道部分或完全阻塞，麻痹性肠梗阻，老年人或衰弱的病人肠道乏力，巨结肠症，中毒性巨结肠合并溃疡性结肠炎，重症结肠炎。
•尿路梗阻
•急性出血心血管状态不稳定
•证明产品过敏
•5岁以下儿童。

警告和注意事项
药物相互作用
如果Oxyspas管理与其他抗胆碱能药物，酚噻嗪，洋地黄和三环类抗抑郁药一起◊应小心。
一般
◊时，在高温环境存在管理Oxyspas可引起中暑。
◊Oxyspas使用不当，可能有害的，不完全性肠梗阻，腹泻可能是其中最早的迹象。
◊Oxyspas可引起嗜睡或视力模糊，因此患者应注意驾车时或使用重型机械。
◊酒精或其他镇静药物可以增强由Oxyspas造成嗜睡。
◊良性前列腺增生或前列腺癌应该被淘汰。
肾脏和肝脏受损
◊使用谨慎

怀孕
◊在怀孕Oxyspas安全已不成立，因此应在怀孕期间使用，只有在医生认为，潜在的好处大于风险。
哺乳
◊如果Oxyspas母乳中排出，因此应谨慎行事管理哺乳母亲时，它不知道。
儿科使用
◊奥昔布宁不建议在5岁以下儿童使用。

副作用
最常见的副作用是口干，便秘，视力模糊，恶心，腹部不适，颜面潮红，排尿困难。
•不太常见的副作用包括头痛，头晕，嗜睡，皮肤反应，心律失常，兴奋中枢神经系统的影响，及尿潴留。

过量
•超过剂量的症状可能包括中枢神经系统的兴奋的迹象，潮红，发热，心动过速，低血压，呼吸衰竭，瘫痪和昏迷。
治疗应是对症和支持。
•活性炭可以管理。
•毒扁豆碱可被视为扭转抗胆碱能中毒症状。

Oxybutynin Chloride Tablets
COMPOSITION
Oxyspas-2.5 Tablets
¤ Each uncoated tablet contains:
Oxybutynin chloride USP ............2.5 mg

DESCRIPTION
• Oxybutynin is a synthetic tertiary amine ester. It possesses anticholinergic (antimuscarinic), spasmolytic and local anaesthetic properties .(Anticholinergic drugs are used to treat a variety of disorders such as gastrointestinal cramps, urinary bladder spasm, asthma, motion sickness, muscular spasms, poisoning with certain toxic compounds, and as an aid to anesthesia. )
• It inhibits the muscurinic action of acetylcholine on smooth muscles and consequently relaxes the bladder smooth muscles.( The chemical compound acetylcholine is a neurotransmitter in both the peripheral nervous system (PNS) and central nervous system ...)

PHARMACOLOGY
Action on the Muscarinic Cholinergic Receptors
◊ Oxybutynin opposes acetylcholine-induced stimulation of parasympathetic muscarinic receptor sites

Action on Detrusor and Other Smooth Muscle
◊ Oxybutynin has a direct-acting relaxant effect on the smooth muscle (detrusor muscle) of the urinary bladder

Effects on Urodynamic Properties
◊ Oxybutynin has a number of beneficial urodynamic effects, such as reducing maximum bladder pressure during both the emptying and filling phases, and increasing bladder volume

Pharmacokinetics
Oral absorption	~100%
Onset of action	30 − 60 min
Presystemic metabolism	~94%
Plasma half-life
Range Mean	0.84 − 2.90h 1.6h
Plasma protein biding	83 − 85%

Micturition (urination) reflex
ø In this reflex arc, parasympathetic fibres causes contraction of detrusor muscle and relaxation of internal urethral sphincter .
ø Urination does not yet occur, because the external urethral sphincter remains closed .
ø There is voluntary relaxation of external urethral sphincter and urination takes place

Indications
» Oxyspas is indicated for the relief of symptoms of bladder instability (i.e. urgency, frequency, urge incontinence) in patients with neurogenic bladder disorders or idiopathic detrusor instability.
» Additionally, Oxyspas may also be used in nocturnal enuresis in children over 5 years of age.

Dosage & Administration
Adults :
» The usual dosage is 5-mg 2--3 times a day.
» The maxi: recommended dose is 5 mg 4 times a day.

Paediatric patients over the age of 5 years :
» The usual dose is 2.5 mg two times a day.
» The maximum recommended dose is 5 mg three times a day.
» For nocturnal enuresis, the last dose should be given before bedtime.

Intravesical Oxybutynin
Ø Intravesical administration of oxybutynin has been investigated as a means of decreasing anticholinergic side effects while maintaining clinical efficacy .

Method
ø A 5 mg tablet is crushed and dissolved in 30ml distilled water twice or thrice daily .
ø The solution is then instilled via an intravesical catheter which is retained in the bladder for minimum of 30-60 minutes.

Ideal candidate for intravesical instillation
» Patients with detrusor hyperreflexia caused by neurological diseases, in whom urinary catheters are already present .
» Patients not responding or intolerant to other drug therapy .
» In patients who would be likely to require bladder surgeries .
» Patients after failed oral oxybutynin therapy .

Benefits of Intravesical Oxybutynin over oral preparation
• Rapidly absorbed
• Attains higher plasma concentrations than oral
• Free of anticholinergic side effects suggests that a hepatic metabolite of oral oxybutynin is responsible for side effects
• Equally efficacious in improving bladder dysfunction
• Absorption not altered due to local bladder damage i.e. UTI or by the pH

Contraindications
• Patients with untreated closed angle glaucoma and in patients with narrow anterior chamber angles.
• Partial or complete obstruction of the gastrointestinal tract, paralytic ileus, intestinal atony of the elderly or debilitated patient, megacolon, toxic megacolon complicating ulcerative colitis,and severe colitis.
• Obstructive uropathy
• Unstable cardiovascular status in acute haemorrhage
• Demonstrated hypersensitivity to the product
• Children below 5 years of age.

Warnings and Precautions
Drug interactions
◊ Care should be taken if Oxyspas is administered together with other anticholinergic agents, phenothiazines, digitalis and tricyclic antidepressants.
General
◊ Oxyspas when administered in the presence of high environmental temperature can cause heat prostration.
◊ Oxyspas use is inappropriate, possibly harmful in incomplete intestinal obstruction, of which diarrhoea may be the earliest sign.
◊ Oxyspas can cause drowsiness or blurred vision hence the patient should be cautioned while driving or using heavy machinery.
◊ Alcohol or other sedative drugs can enhance the drowsiness caused by Oxyspas.
◊ BPH or prostate cancer should be eliminated .
Renal & Hepatic impairment
◊ Use with caution

Pregnancy
◊ The safety of Oxyspas in pregnancy has not been established and hence it should be used in pregnancy only if, in the opinion of the physician, the potential benefits outweigh the risks.
Lactation
◊ It is not known if Oxyspas is excreted in breast milk and hence caution should be exercised when administering it to nursing mothers.
Paediatric use
◊ Oxybutynin is not recommended for use in children below 5 years of age.

Side effects
• The most frequently reported side effects are dry mouth, constipation, blurred vision, nausea, abdominal discomfort, facial flushing, and difficulty in micturition.
• Less frequent side effects include headache, dizziness, drowsiness, skin reactions, cardiac arrhythmias, excitatory CNS effects, and urinary retention.

Overdosage
• Symptoms of over-dosage may include signs of central nervous system excitation, flushing, fever,tachycardia, hypotension, respiratory failure, paralysis and coma.
• The treatment should be symptomatic and supportive.
• Activated charcoal can be administered .
• Physostigmine may be considered to reverse the symptoms of anticholinergic intoxication.

Presentation
1 strip……..10 tablets