CN102743757A - Medicament for treating overactive bladder caused by bladder outlet obstruction - Google Patents
Medicament for treating overactive bladder caused by bladder outlet obstruction Download PDFInfo
- Publication number
- CN102743757A CN102743757A CN201210235796XA CN201210235796A CN102743757A CN 102743757 A CN102743757 A CN 102743757A CN 201210235796X A CN201210235796X A CN 201210235796XA CN 201210235796 A CN201210235796 A CN 201210235796A CN 102743757 A CN102743757 A CN 102743757A
- Authority
- CN
- China
- Prior art keywords
- bladder
- urethra
- blocking agent
- receptor blocking
- receptor inhibitor
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to the field of medicaments, in particular relates to a medicament for treating overactive bladder caused by bladder outlet obstruction, and specifically relates to application of an M3 receptor inhibitor and an alpha1-A receptor inhibitor in preparation of a medicament for treating overactive bladder caused by bladder outlet obstruction. The medicament for treating the bladder outlet obstruction consists of the following components in parts by weight: 15 to 20 parts of M3 receptor inhibitor, and 0.5 to 2 parts of alpha1-A receptor inhibitor. By investigating the indexes of bladder sensory function, bladder detrusor pressure, highest urine flow rate, vesical neck pressure, functional urethral length, urethral closing area and the like, the M3 receptor inhibitor and the alpha1-A receptor inhibitor applied to treatment of the overactive bladder caused by the bladder outlet obstruction have a good effect.
Description
Technical field
The present invention relates to field of medicaments, particularly the hyperactive medicine of bladder due to the treatment bladder outflow obstruction.
Background technology
Sphincter is meant a kind of belt muscle that is distributed in some wall of the lumen of humans and animals body, when sphincters contract, can close tube chamber, makes tube chamber open during diastole, often is in contraction state at ordinary times.Generally receive autonomic nerve domination or hormonal regulation.Traditional theory is thought: the inside and outside sphincter of urethra is the most important in the urine control, when both all damage, urinary incontinence will inevitably occur.But in anatomy, do not have so-called " urethra internal sphincter " such anatomical structure, the many phenomenons in the clinical position can not be carried out satisfactory explanation with the inside and outside sphincter of urethra.Hundreds of routine posterior urethral stricture and locking patient through accepting for medical treatment confirm: these patients perform the operation through the perineum approach; Although the abundant cicatrix of excision urethra behind whole section of membranous part to the neck of bladder in operation; Urethra internal sphincter on the traditional musculus sphincter of external urethra and the function has all suffered destruction; But after coincideing with normal anterior urethra and neck of bladder, the patient still can recover good urinary continence.We drain VCU to such patient, find urinary incontinence enough then not occur like newly-built urethral length, shorten like urethral length, and urinary incontinence is then arranged.Its all prostate postoperative urine incontinence musculus sphincters of external urethra of reports such as Gudziak all are normal.The inside and outside sphincter of traditional urethra is all destroyed, urinary incontinence but do not occur; Real urinary incontinence patient behind the operation on prostate, the musculus sphincter of external urethra is normal.Above-mentioned phenomenon and traditional view promptly urinate control fully per urethram sphincter influence run counter to.
Zhang Jiahua teaches the new mechanism " under the normal condition of urethra other factor (sphincter, innervation etc.), the length of functional urethra and function (elasticity, pressure etc.) are the most important factors of urethra control urine " that proposed urethra control urine in 2000.Urethra source property paruria disease is exactly due to FUL and pressure (elasticity) change.The parameter of these two indexs of reflection has FUL and urethra to close area in urodynamics, and wherein most important aggregative indicator is that urethra is closed area, and this index does not at home and abroad obtain paying attention to and using always.
Functional urethra is: pressure is higher than the urethra of bladder rest pressure, and this section urethra is the urethra of control urine.Urethra is closed area: the graphics area that FUL and pressure thereof constituted, the both length of reflection function property urethra, the pressure of reflection function property urethra again.Through the length and the pressure (tension force) of regulatory function urethra, make urethra close area and reach normally, treatment urethra source property paruria disease.Promptly increase function urethral length and pressure with the treatment urinary incontinence, reduce function urethral length and pressure with the treatment dysuria.According to above-mentioned viewpoint, to carrying out clinical research before and after the 25 routine BPH patient TUVP arts, postoperative 2～4 week check urine power checks that the result shows: (3.8～8.9cm) reduce to 3.7cm (3.1～4.8cm) to FUL by 6.2cm.Urethra is closed area by 1850mm.cmH
2O (1250～2918mm.cmH
2O) reduce to 385mm.cmH
2O (248～707mm.cmH
2O), after all extubation in patients, dysuria disappears.Except operation, also do not carry out based on the study medication of above-mentioned viewpoint.
Summary of the invention
The object of the present invention is to provide the new application of a kind of M3 receptor blocking agent and α 1-A receptor blocking agent, this is applied as, and the bladder hyperkinesia provides new thinking due to the treatment bladder outflow obstruction.
For realizing above-mentioned purpose, technical scheme of the present invention is:
M3 receptor blocking agent and α 1-A receptor blocking agent are united the application in the hyperactive medicine of bladder due to the preparation bladder outflow obstruction.Said bladder outflow obstruction is the bladder outflow obstruction due to benign prostatic hyperplasia or the non-prostatic hyperplasia.Because the M3 receptor blocking agent is the highest medicine of selectivity in the m receptor retarder medicaments, α 1-A receptor blocking agent is the highest medicine of selectivity in the α receptor retarder medicaments, therefore adopts M3 receptor blocking agent and α 1-A receptor blocking agent Combined application.
The bladder hyperkinesia has many reasons, mainly causes bladder sensation increased functionality and smooth muscle over-activity by bladder outflow obstruction (like benign prostatic hyperplasia, female bladder outflow obstruction).Main at present employing m receptor blocker is treated.But because main diseases does not obtain handling and improving because of the bladder outflow obstruction, dysuria appears in some patient, even urine retention, and curative effect is affected.
α 1-A receptor blocking agent can relax prostate and back urethral smooth muscle reduce the function urethral resistance, remove the bladder outflow obstruction.Wherein tamsulosin hydrochloride also has the effect of α 1-D receptor blocking agent, lax detrusor of bladder.Therefore M3 receptor blocking agent and α 1-A receptor blocking agent Combined application both can have been treated the hyperactive cause of disease of bladder, can work in coordination with lax detrusor of bladder again, reached better therapeutic effect.Reduce the generation of dysuria complication simultaneously.
Further, said M3 receptor blocking agent comprises tolterodine L-tartrate, succinic acid Suo Linaxin.
Further, said α 1-A receptor blocking agent comprises Tamsulosin, tamsulosin hydrochloride.
Two of the object of the invention is to provide the hyperactive pharmaceutical composition of bladder due to the treatment bladder outflow obstruction; The said composition medicine is collaborative each other, and is evident in efficacy aspect treatment bladder hyperkinesia benign prostatic hyperplasia and that the female bladder outflow obstruction is caused.
Be the treatment above-mentioned purpose, technical scheme of the present invention is:
Be used to treat the medicine of bladder outflow obstruction, form by following component by weight: M3 receptor blocking agent 15-20 part, α 1-A receptor blocking agent 0.5-2 part, said M3 receptor blocking agent comprises tolterodine L-tartrate, succinic acid Suo Linaxin; Further, said α 1-A receptor blocking agent comprises Tamsulosin, tamsulosin hydrochloride.
Further, form by following component by weight: 0.1 part of tamsulosin hydrochloride, 20 parts of tolterodine L-tartrates.
Beneficial effect of the present invention is: from bladder sensation function, detrusor of bladder pressure, Qmax and neck of bladder press, function urethral length and urethra are closed area etc., and index is investigated, M3 receptor blocking agent and α 1-A receptor blocking agent Combined application are to best results in the hyperactive treatment of bladder due to the bladder outflow obstruction.
The specific embodiment
120 cases of accepting for medical treatment have been collected in this research, and the patient is the women, 20～76 years old age, average 55.6 years old.All there are lower urinary tract symptoms such as urgent micturition, frequent micturition, urine rheology are thin, dribbling, dysuria in the main suit.Sample examination is confirmed no bacterial infection; Further urodynamics test is diagnosed as the bladder hyperkinesia.
The hyperactive application of bladder due to the female bladder outflow obstruction of embodiment 1 M3 receptor blocking agent
The patient takes Tolterodine tartrate (tolterodine L-tartrate) 4mg separately, and once a day, frequent micturition, some alleviation of symptoms of urgency further attenuate but dysuria increases the weight of, urinates line.Except Tolterodine tartrate, succinic acid Suo Linaxin also is the M3 receptor blocking agent, and its effect is identical.
The inventor thinks, the only lax detrusor of bladder of above-mentioned treatment, and do not handle the cause of disease, so curative effect is limited.The result of tissue pathology checking of above-mentioned corrective surgery excision shows: the hypertrophy due to the urethral tissue chronic inflammatory; Analyze the cause of disease that female urethra blocks and possibly be chronic urethritis, vaginitis, pelvic inflammatory disease and cause urethra chronic inflammatory hypertrophy; Cause function prolonged urethra, increased pressure; Urethra is closed area to be increased, and causes urethral obstruction, dysuria.And then the enhancing of bladder function compensatory, urine urgency-frequency appears.
The inventor further thinks: under the normal condition of urethra other factor (musculus sphincter of external urethra and innervation), the length of function urethra and function (the stopper effect of elasticity, pressure, mucosa pad) are urethra control urine two most important factors.Aggregative indicator on urodynamics is that urethra is closed area.The reduction capability urethral length just can be alleviated dysuria and urine retention or/and urethra pressure reduces urethra and closes area; Otherwise increase the function urethral length or/and urethra pressure then can be treated stress incontinence.Above-mentioned 40 patients are because the function urethral length prolongs, increased pressure, cause urethra to close area and increase, and cause dysuria, and then the enhancing of detrusor of bladder functional compensation property, frequent micturition occurs, serious appearance urine retention.In treatment bladder hyperkinesia simultaneously, must alleviate earlier and block, just can reach curative effect preferably.
The hyperactive application of bladder due to the female bladder outflow obstruction of embodiment 2 α 1-A receptor blocking agents
Tamsulosin hydrochloride is the specificity blocker of α 1 receptor subtype; And α 1 receptor that the bladder efferent tract exists is mainly α 1A receptor; Therefore; These article have the blocking effect of high selectivity to α 1 receptor on urethra, bladder neck and the prostate smooth muscle, make smooth muscle loosening, and the urethra pressure drop is low and then make urethra close area to dwindle.Except tamsulosin hydrochloride; Tamsulosin hydrochloride also is α 1 a receptor receptor blocker; All can have the blocking effect of high selectivity to α 1 receptor on urethra, bladder neck and the prostate smooth muscle, and then make smooth muscle loosening, the urethra pressure drop is low and then make urethra close area to dwindle.
Case 40 examples similar with instance 1 are taken tamsulosin hydrochloride 0.2mg separately, and dysuria is alleviated, and urine urgency-frequency only alleviates a little, do not reach good therapeutic effect.The inventor thinks that this scheme is only removed and blocked, and does not use the atony of bladder medicine, is the reason of unsatisfactory curative effect.
The hyperactive application of bladder due to embodiment 3 M3 receptor blocking agents and the α 1-A receptor blocking agent associating female bladder outflow obstruction
Other gets 40 routine female patients and takes tamsulosin hydrochloride (trade name is breathed out happy) 0.2mg and tolterodine L-tartrate (commodity are called She Niting) 4mg; Once a day; After 1 week; Symptoms such as above-mentioned patient's urgent micturition, frequent micturition, urine rheology are thin, dribbling, dysuria are eased, and patient's bladder capacity enlarges, and each urine amount increases.After 6 weeks, symptom disappears basically.
Further set forth the present invention below in conjunction with embodiment.Should be understood that these embodiment only are used to explain the present invention, and unrestricted scope of the present invention.The reagent of the method for unreceipted actual conditions and undeclared prescription is according to normal condition and carries out or dispose in the following example, and the product in unreceipted source all can obtain through the market approach.
Claims (6)
1.M3 receptor blocking agent and α 1-A receptor blocking agent are united the application in the hyperactive medicine of bladder due to the preparation bladder outflow obstruction.
2. application according to claim 1 is characterized in that: said bladder outflow obstruction is the bladder outflow obstruction due to benign prostatic hyperplasia or the non-prostatic hyperplasia.
3. application according to claim 1 is characterized in that: said M3 receptor blocking agent comprises tolterodine L-tartrate, succinic acid Suo Linaxin.
4. application according to claim 1 is characterized in that: said α 1-A receptor blocking agent comprises Tamsulosin, tamsulosin hydrochloride.
5. be used to treat the medicine of bladder outflow obstruction; It is characterized in that: form by following component by weight: M3 receptor blocking agent 15-20 part; α 1-A receptor blocking agent 0.5-2 part; Said M3 receptor blocking agent comprises tolterodine L-tartrate, succinic acid Suo Linaxin, and said α 1-A receptor blocking agent comprises Tamsulosin, tamsulosin hydrochloride.
6. medicine according to claim 5 is characterized in that, is made up of following component by weight: 0.1 part of tamsulosin hydrochloride, 20 parts of tolterodine L-tartrates.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210235796XA CN102743757A (en) | 2012-07-09 | 2012-07-09 | Medicament for treating overactive bladder caused by bladder outlet obstruction |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210235796XA CN102743757A (en) | 2012-07-09 | 2012-07-09 | Medicament for treating overactive bladder caused by bladder outlet obstruction |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102743757A true CN102743757A (en) | 2012-10-24 |
Family
ID=47024480
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210235796XA Pending CN102743757A (en) | 2012-07-09 | 2012-07-09 | Medicament for treating overactive bladder caused by bladder outlet obstruction |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102743757A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106562968A (en) * | 2015-10-13 | 2017-04-19 | 南京华威医药科技开发有限公司 | Pharmaceutical composition containing tamsulosin hydrochloride and solifenacin succinate |
| CN116432564A (en) * | 2023-06-15 | 2023-07-14 | 天津市第五中心医院 | Urodynamic state analysis method and analysis system |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1658859A (en) * | 2002-06-07 | 2005-08-24 | 山之内制药株式会社 | Therapeutic agent for overactive bladder |
| US20090131469A1 (en) * | 2005-02-25 | 2009-05-21 | Astellas Pharma Inc. | Pharmaceutical agent comprising solifenacin |
| CN101754760A (en) * | 2007-07-20 | 2010-06-23 | 安斯泰来制药株式会社 | Pharmaceutical composition for amelioration of lower urinary tract symptom associated with prostatomegaly |
| CN102307579A (en) * | 2009-02-04 | 2012-01-04 | 安斯泰来制药株式会社 | Pharmaceutical composition for oral administration |
-
2012
- 2012-07-09 CN CN201210235796XA patent/CN102743757A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1658859A (en) * | 2002-06-07 | 2005-08-24 | 山之内制药株式会社 | Therapeutic agent for overactive bladder |
| US20090131469A1 (en) * | 2005-02-25 | 2009-05-21 | Astellas Pharma Inc. | Pharmaceutical agent comprising solifenacin |
| CN101754760A (en) * | 2007-07-20 | 2010-06-23 | 安斯泰来制药株式会社 | Pharmaceutical composition for amelioration of lower urinary tract symptom associated with prostatomegaly |
| CN102307579A (en) * | 2009-02-04 | 2012-01-04 | 安斯泰来制药株式会社 | Pharmaceutical composition for oral administration |
Non-Patent Citations (4)
| Title |
|---|
| 曾明辉等: "酒石酸托特罗定片联合坦洛新治疗膀胱过度活动症的疗效", 《广东医学》 * |
| 杨国联: "酒石酸托特罗定和坦索罗辛治疗下尿路症状疗效分析", 《中国现代医生》 * |
| 林昀等: "坦索罗辛联合托特罗定治疗女性膀胱过度活动症的疗效观察", 《海峡药学》 * |
| 陈平: "索利那新联合坦索罗辛治疗良性前列腺增生伴膀胱过度活动症的疗效分析", 《中国保健营养》 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106562968A (en) * | 2015-10-13 | 2017-04-19 | 南京华威医药科技开发有限公司 | Pharmaceutical composition containing tamsulosin hydrochloride and solifenacin succinate |
| CN106562968B (en) * | 2015-10-13 | 2019-08-13 | 南京华威医药科技集团有限公司 | Pharmaceutical composition comprising tamsulosin hydrochloride and succinic acid Solifenacin |
| CN116432564A (en) * | 2023-06-15 | 2023-07-14 | 天津市第五中心医院 | Urodynamic state analysis method and analysis system |
| CN116432564B (en) * | 2023-06-15 | 2023-08-18 | 天津市第五中心医院 | Urodynamic state analysis method and analysis system |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Madersbacher et al. | Conservative management in neuropathic urinary incontinence | |
| Staskin et al. | Efficacy and safety of oxybutynin chloride topical gel for overactive bladder: a randomized, double-blind, placebo controlled, multicenter study | |
| Zinner et al. | Pharmacotherapy for stress urinary incontinence: present and future options | |
| Eapen et al. | Gender differences in overactive bladder | |
| Almeida et al. | Urodynamic and clinical evaluation of 91 female patients with urinary incontinence treated with perineal magnetic stimulation: 1-year followup | |
| Jhang et al. | Transurethral incision of the bladder neck improves voiding efficiency in female patients with detrusor underactivity | |
| Miller et al. | The causes and consequences of overactive bladder | |
| Hsiao et al. | Medical treatment of female overactive bladder syndrome and treatment-related effects | |
| Rashid et al. | Urinary incontinence: pathophysiology and management outline | |
| CN102743757A (en) | Medicament for treating overactive bladder caused by bladder outlet obstruction | |
| Hashim et al. | Pharmacological management of women with mixed urinary incontinence | |
| Li et al. | Prevention of catheter-related bladder discomfort–pudendal nerve block with ropivacaine versus intravenous tramadol: study protocol for a randomized controlled trial | |
| Manchana et al. | Bethanechol chloride for the prevention of bladder dysfunction after radical hysterectomy in gynecologic cancer patients: a randomized controlled trial study | |
| Jaszczyński et al. | Post-irradiation bladder syndrome after radiotherapy of malignant neoplasm of small pelvis organs: an observational, non-interventional clinical study assessing VESIcare®/solifenacin treatment results | |
| Beder et al. | Overactive bladder in women | |
| Deutchman et al. | Stress urinary incontinence in women: diagnosis and medical management | |
| CN105579036A (en) | Agents for improving vesicourethral dyssynergia | |
| Ashok et al. | Detrusor overactivity: an overview | |
| Barkin et al. | The practical update for family physicians in the diagnosis and management of overactive bladder and lower urinary tract symptoms | |
| Hasbi et al. | The effectiveness between tamsulosin and solifenacin combined with tamsulosin on treatment of ureteral stent-related symptoms | |
| Burimsittichai | Comparison of intravenous tramadol and ketamine for prevention of catheter-related bladder discomfort after laparoscopic surgery: a randomized, placebo-controlled, double-blind study | |
| Radoja et al. | Coital urinary incontinence and female sexual function | |
| Agarwal et al. | Neurological evaluation of urinary incontinence in the female patient | |
| Conde-Santos et al. | 468 STUDY OF SAFETY AND URODYNAMIC CHARACTERIZATION OF TREATMENT WITH TAMSULOSIN, TOLT ERODINE AND TAMSULOSIN PLUS TOLT ERODINE, IN MEN WITH LUTS | |
| Sarica et al. | Conservative management of overactive bladder in children: Evaluation of clinical and urodynamic results |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C12 | Rejection of a patent application after its publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20121024 |