CN1739516A - Application of penehyclidine hydrochloride in preparing medicine - Google Patents
Application of penehyclidine hydrochloride in preparing medicine Download PDFInfo
- Publication number
- CN1739516A CN1739516A CN 200510088049 CN200510088049A CN1739516A CN 1739516 A CN1739516 A CN 1739516A CN 200510088049 CN200510088049 CN 200510088049 CN 200510088049 A CN200510088049 A CN 200510088049A CN 1739516 A CN1739516 A CN 1739516A
- Authority
- CN
- China
- Prior art keywords
- application
- present
- amyl ethyl
- ethyl quin
- quin ether
- 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
Abstract
The present invention relates to the application of penehyclidine hydrochloride in preparing medicine, and is especially the application of penehyclidine hydrochloride in preparing medicine for treating asthma, chronic bronchitis and other chronic obstructive respiratory tract diseases. Animal experiment and clinical observation prove the remitting effect of penehyclidine hydrochloride on asthma, chronic bronchitis and other chronic obstructive respiratory tract diseases. The present invention expands the medicinal use of penehyclidine hydrochloride.
Description
Technical field:
The present invention relates to the application of amyl ethyl quin ether hydrochloride, particularly amyl ethyl quin ether hydrochloride application in clinical medicine for gastroenteropathy, ophthalmic diseases, respiratory tract disease, central nervous system disease, anesthesia, urogenital tract renal colic and irritative symptoms of bladder, anti-septic shock, anti-biliary colic etc.
Background technology:
Amyl ethyl quin ether hydrochloride, English name: Penehyclidine Hydrochloride, its chemistry 3-(2-cyclopenta-2-hydroxyl-2-phenyl ethoxy) quinuclidine hydrochloride by name, molecular formula: C
20H
29NO
2CHl, molecular weight: 351.92.Before this, have been found that and confirm that amyl ethyl quin ether hydrochloride has the effect and the clinical efficacy of rescue organophosphate poisoning, but does not find other clinical medicine effects.
Summary of the invention:
The objective of the invention is by animal experiment and clinical observation, propose the new indication of amyl ethyl quin ether hydrochloride, amyl ethyl quin ether hydrochloride is for the application of gastroenteropathy, ophthalmic diseases, respiratory tract disease, central nervous system disease, anesthesia, urogenital tract renal colic and irritative symptoms of bladder, anti-septic shock, anti-biliary colic etc. in clinical medicine.
The application of amyl ethyl quin ether hydrochloride in pharmacy, the chemistry of the main component of described amyl ethyl quin ether hydrochloride are called 3-(2-cyclopenta-2-hydroxyl-2-phenyl ethoxy) quinuclidine hydrochloride, molecular formula: C
20H
29NO
2HCl, molecular weight: 351.92, it is characterized in that: treatment and application in the cholinolytic effect clinical medicine aspect gastroenteropathy or ophthalmic diseases or respiratory tract disease or central nervous system disease or anesthesia or urogenital tract renal colic and irritative symptoms of bladder or anti-septic shock or anti-biliary colic.
Amyl ethyl quin ether hydrochloride of the present invention application of gastroenteropathy in clinical medicine comprises: the treatment of A, peptic ulcer is used; B, alleviate gastrointestinal tension force or move hyperfunction and be applicable to the treatment application of intestinal motility that excitation bowel syndrome, guanethidine cause hyperfunction and dysentery and rectal distention stimulation symptom; C, inhibition salivation, the parkinson disease sialorrhea, the treatment of the saliva dysphagia that the esophagus mechanical obstruction is caused is used.
Amyl ethyl quin ether hydrochloride of the present invention application of ophthalmic diseases in clinical medicine comprises: A, platycoria, prevent that the treatment of adhesion from using at examination of ocular fundus and iritis, keratitis; B, be used for optometry and join the adjusting paralysis of mirror and use.
Amyl ethyl quin ether hydrochloride of the present invention application of respiratory tract disease in clinical medicine comprises: the application of A, alleviation flu and acute and chronic rhinitis; The application of B, relieving asthma.
Amyl ethyl quin ether hydrochloride of the present invention application of central nervous system disease in clinical medicine mainly comprises: be used for the application of parkinson disease treatment.
The application that amyl ethyl quin ether hydrochloride of the present invention is anaesthetized in clinical medicine is meant: preanesthetic medication.
The present invention in clinical according to the different syndromes dosed administration.
The present invention can be made into different dosage form according to clinical needs, administering mode comprises whole body administration and topical, that dosage form comprises is oral, subcutaneous injection, intramuscular injection, intravenous injection, nasal drop, spray, wherein oral, subcutaneous injection, intramuscular injection, the hydrochloric amyl ethyl quin ether 0.01～10mg of the every preparation unit of intravenous injection, the concentration of nasal drop, spray is 0.025～3%.
Pharmacological toxicology of the present invention: the present invention is the selectivity anticholinergic agent, can enter in the brain by blood brain barrier.Its energy blockage of acetylcholine is to the agonism of brain endogenous toxin potash receptor (m receptor) and nicotine receptor (n receptor); Therefore, the maincenter poisoning symptom that antagonism organophosphorus poison (pesticide) poisoning preferably causes is as convulsions, maincenter respiratory and circulatory failure and dysphoria etc.Simultaneously, in periphery the agonism of stronger blockage of acetylcholine to m receptor arranged also; Thereby the muscarinic poisoning symptom that the organic squama poisonous substance of antagonism (pesticide) poisoning preferably causes is as bronchial muscular spasm and secretions increase, perspiration, sialorrhea, myosis and gastrointestinal tract smooth muscle spasm or contraction etc.It can also increase respiratory frequency and respiratory flow, but since this product to M
2Receptor does not have obvious effect, so heart rate is not had obvious influence; The periphery n receptor there is not obvious antagonism.Toxicity of the present invention is less, mice LD
50Be 261.7mg/Kg (im) that 71.2mg/Kg (iv); Rat LD
50450.7mg/Kg (im), 71.2mg/Kg (iv); The long term toxicity test of rat and Canis familiaris L. except that some common cholinolytic reactions occurring, does not see that other are unusual, and intramuscular injection local excitation Sal is up to specification.Mutagenicity test is negative; Dosage does not have obviously general genitality toxicity in being equivalent to 75 times of people's consumptions; In being equivalent to 300 times of people's consumptions, do not see teratogenesis and fetal toxicity, also do not see the behavior teratogenesis.
Pharmacokinetics of the present invention: behind the intramuscular injection 1mg of the health adult amyl ethyl quin ether hydrochloride, can detect amyl ethyl quin ether hydrochloride in 2 minutes in blood, about 0.56 hour blood drug level peaking, peak concentration are 13.20 μ g/L, and the elimination half-life is about 10.35 hours.Zoopery shows: the present invention is distributed to each tissue of whole body, and is more with submaxillary gland, lung, spleen, intestinal.This product is mainly by urine and defecate, and total the drainage was dosage 94.17% in 24 hours.
Pharmacodynamic study before amyl ethyl quin ether hydrochloride of the present invention is clinical, behind pharmacodynamic study, find:
(1), antiasthmatic effect
1, to the guinea-pig isolated trachea effect: its tool resists significantly that trachea shrinks PA due to the A
2Value is 6.99 ± 1.25, and atropinic PA
2Value is 10.51 ± 3.30.
2, to the Guinea pig lung bar effect of exsomatizing: can resist the contraction that Ach causes, ED
50Be 1.21 ± 2.58 * 10
-7Mol/L, and atropinic ED
50Be 0.20 ± 0.27 * 10
-7
3, to Cavia porcellus medicine antiasthmatic effect: amyl ethyl quin ether hydrochloride 1mg/ml, the tangible antiasthmatic effect of the equal tool of 0.5mg/ml spray delivery, the isoproterenol effect of its 0.5mg/ml spraying dosage and 0.5mg/ml is suitable.
(2), reduce nasal mucosa secretion, watery nasal discharge and sneeze effect
Amyl ethyl quin ether hydrochloride 1mg/ml, each 2 of 0.5mg/ml collunariums are after collunarium is given Cavia porcellus, all can significantly suppress the nasal mucosa telangiectasis that causes by histamine phosphate, make that the nasal discharge secretion obviously reduces due to the histamine, each 2 of 1mg/ml concentration collunariums, sneeze obviously alleviates.
(3), to stomach, ileum, colon, gallbladder, the stem effect of separating of bladder
1, amyl ethyl quin ether hydrochloride can suppress the autonomous contraction of stripped Cavia porcellus stomach, ileum, colon, gallbladder, bladder, and stripped stomach, ileum, colon, gallbladder, cystospasm contraction that antagonism Ach causes have tangible spasmolysis.The spasmolysis of bladder contraction obviously is better than atropine due to its antagonism Ach.
2, amyl ethyl quin ether hydrochloride intravenous injection 0.01mg/Kg, 0.02mg/Kg, 0.05mg/Kg oral administration thing 0.1mg/Kg, 0.2mg/Kg, 0.5mg/Kg all can suppress to anaesthetize the caused stomach of tame Ach, ileum, colon, gallbladder, cystospasm contraction, the tangible spasmolysis of tool.
Clinical effectiveness of the present invention is:
A, all effective to the hyperfunction stomachache that causes of internal organs smooth muscle movement, diarrhoea, biliary colic, renal colic, the enuresis, urinary incontinence and irritative symptoms of bladder;
The symptom of panting that b, energy relieving asthma, chronic bronchitis inflammation and other chronic obstructive respiratory tract disease cause;
C, the tetanic and symptom of trembling of Parkinson's disease patients can be alleviated, and sialorrhea and excessive sweating can be suppressed;
D, can alleviate the common cold initial stage symptom as nasal obstruction, rhinorrhea etc. and acute and chronic rhinitis;
E, preanesthetic medication are effective;
F, effective to septic shock;
G, at the platycoria of ophthalmology and regulate aspect the paralysis effective.
The present invention proposes new indication of amyl ethyl quin ether hydrochloride and application thereof, has expanded the pharmaceutical applications of amyl ethyl quin ether hydrochloride, and has tangible curative effect effect for new indication.
The specific embodiment:
Embodiment 1
The application of the present invention in preparation treatment gastroenteropathy medicine comprises: the treatment of A, peptic ulcer is used; B, alleviate gastrointestinal tension force or move hyperfunction and be applicable to the treatment application of intestinal motility that excitation bowel syndrome, guanethidine cause hyperfunction and dysentery and rectal distention stimulation symptom; C, inhibition salivation, the parkinson disease sialorrhea, the treatment of the saliva dysphagia that the esophagus mechanical obstruction is caused is used.
Application method can be selected for use oral or intramuscular injection or intravenous injection, preferable amount ranges 0.01～10mg/ time.
Embodiment 2
Application in the clinical medicine of the present invention in ophthalmic diseases comprises: A, platycoria, prevent that the treatment of adhesion from using at examination of ocular fundus and iritis, keratitis; B, be used for optometry and join the adjusting paralysis of mirror and use.
Drug formulation can be selected eye drop for use or be coated with an agent, and preferred concentration is 0.03～3%.
Embodiment 3
Application in the clinical medicine of the present invention in respiratory tract disease comprises: the application of A, alleviation flu and acute and chronic rhinitis; The application of B, relieving asthma.
Drug formulation can be selected nasal drop or spray for use, and preferred concentration is 0.025～2.8.
Embodiment 4
Application at central nervous system disease in the clinical medicine of the present invention mainly comprises: be used for the application of parkinson disease treatment.
Application method can be selected for use oral or intramuscular injection or intravenous injection, and preferable amount ranges is 0.01～8.8mg/ time.
Embodiment 5
The application of anaesthetizing in the clinical medicine of the present invention mainly is meant premedication, and application method can be selected intramuscular injection or intravenous injection or subcutaneous injection for use, and preferable amount ranges is 0.02～8mg/ time.
Embodiment 6
In the application of urogenital tract renal colic and irritative symptoms of bladder, application method can be selected for use oral or intramuscular injection or intravenous injection in the clinical medicine of the present invention, and preferable amount ranges is 0.03～8.9mg/ time.
Embodiment 7
In the application of anti-septic shock, application method can be selected intramuscular injection or intravenous injection or subcutaneous injection for use in the clinical medicine of the present invention, and preferable amount ranges is 0.05～9.5mg/ time.
Embodiment 8
Treatment and application in the clinical medicine of the present invention aspect anti-biliary colic, application method can be selected for use oral or intramuscular injection or intravenous injection, and preferable amount ranges is 0.02～8.5mg/ time.
Claims (3)
1, the purposes of amyl ethyl quin ether hydrochloride in preparation treatment relieving asthma, chronic bronchitis inflammation and chronic obstructive respiratory tract disease medicine.
2, purposes as claimed in claim 1 is characterized in that: the administering mode of pharmaceutical preparation is whole body administration or topical, and that dosage form comprises is oral, subcutaneous injection, intramuscular injection, intravenous injection, nasal drop, spray.
3, purposes as claimed in claim 1 or 2 is characterized in that: described oral, subcutaneous injection, intramuscular injection, the hydrochloric amyl ethyl quin ether 0.01～10mg of the every preparation unit of intravenous injection, the concentration of nasal drop, spray is 0.025～3%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510088049 CN1739516A (en) | 2002-08-16 | 2002-08-16 | Application of penehyclidine hydrochloride in preparing medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510088049 CN1739516A (en) | 2002-08-16 | 2002-08-16 | Application of penehyclidine hydrochloride in preparing medicine |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB021336172A Division CN1219513C (en) | 2002-08-16 | 2002-08-16 | Application of amyl ethyl quin ether hydrochloride |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1739516A true CN1739516A (en) | 2006-03-01 |
Family
ID=36092141
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200510088049 Pending CN1739516A (en) | 2002-08-16 | 2002-08-16 | Application of penehyclidine hydrochloride in preparing medicine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1739516A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102218061A (en) * | 2011-04-29 | 2011-10-19 | 成都力思特制药股份有限公司 | Application of penehyclidine hydrochloride in preparation of medicine for treating motion sickness |
| CN102525909A (en) * | 2012-02-29 | 2012-07-04 | 黄绍渊 | Method for preparing penehyclidine hydrochloride injection |
-
2002
- 2002-08-16 CN CN 200510088049 patent/CN1739516A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102218061A (en) * | 2011-04-29 | 2011-10-19 | 成都力思特制药股份有限公司 | Application of penehyclidine hydrochloride in preparation of medicine for treating motion sickness |
| CN102218061B (en) * | 2011-04-29 | 2012-07-04 | 成都力思特制药股份有限公司 | Application of penehyclidine hydrochloride in preparation of medicine for treating motion sickness |
| CN102525909A (en) * | 2012-02-29 | 2012-07-04 | 黄绍渊 | Method for preparing penehyclidine hydrochloride injection |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US9694027B2 (en) | Pyrazole derivative and use thereof for medical purposes | |
| JP5744947B2 (en) | Combination of alpha-2 receptor agonist (clonidine) and antimuscarinic agent (oxybutynin) for the treatment of fluency | |
| EA021303B1 (en) | Methods of treating or preventing emesis using growth hormone secretagogues | |
| WO2000009127A1 (en) | Remedies for multiple sclerosis | |
| WO2002034264A1 (en) | Remedies for amyotrophic lateral sclerosis (als) | |
| TW201034659A (en) | Treatment of autoimmune diseases | |
| CN1219513C (en) | Application of amyl ethyl quin ether hydrochloride | |
| CN1739516A (en) | Application of penehyclidine hydrochloride in preparing medicine | |
| CN1739511A (en) | Application of penehyliclidine hydrochloride in preparing medicine | |
| CA1318595C (en) | 2-alkoxy-n-(1-azabicyclo[2.2.2]oct-3-yl) benzamides and thiobenzamides | |
| US10487058B2 (en) | Cyclopropyl unsaturated quinoline compound used as leukotriene receptor antagonist and applications thereof | |
| CN1930123A (en) | Medicinal composition for prevention or treatment of overactive bladder accompanying nervous disorder | |
| MXPA04004572A (en) | Method for treating autoimmune diseases. | |
| CN1739517A (en) | Application of penehyclidine hydrochloride in preparing medicine | |
| CN1739518A (en) | Application of penehyclidine hydrochloride in preparing medicine | |
| WO2020051568A1 (en) | NEW USE OF R-ENANTIOMER OF ADRENERGIC β2 RECEPTOR AGONISTS FOR TREATMENT OF INFLAMMATORY BOWEL DISEASE AND ITS EXTRA INTESTINAL MANIFESTATIONS | |
| US7446128B2 (en) | Agent for treating interstitial cystitis | |
| CN106924175B (en) | Pharmaceutical composition for treating multiple sclerosis | |
| Souza-Machado et al. | Severe asthma associated with myasthenia gravis and upper airway obstruction | |
| WO2004016590A1 (en) | The salts of the quinuclidine derivatives and the preparation and applications thereof | |
| CN1281241C (en) | Medicine for treating chronic bronchitis and its preparation method | |
| CN1293881C (en) | Compound antitussive | |
| CN111184706B (en) | Active medicine for preventing and treating cholecystitis and application thereof | |
| US20060100290A1 (en) | Treatment of allergic rhinitis and asthma | |
| CN1709891A (en) | Medicinal compound, its composition and use in pharmaceutical process |
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 |
Open date: 20060301 |