Cloperastine hydrochlorideraws li ib tug tshuaj, muaj ib tug series ntawm lub cev yam ntxwv. Nws yog ib qho tsis muaj xim tsis muaj pob tshab lossis dawb zoo rau coarse crystalline hmoov nrog rau qee qib ntawm crystallinity, uas muab nws cov khoom sib txawv hauv qhov tsos. Cov mis mos molecular C20H24ClNO · HCl los yog C20H25Cl2NO, CAS C20H25Cl2NO. Cov khoom no muaj qee yam acidity, uas yuav txiav txim siab los ntawm cov pab pawg acidic (xws li chloride ions) hauv nws cov qauv molecular. Cov khoom no muaj tsib lub ntsiab lus: carbon (C), hydrogen (H), chlorine (Cl), nitrogen (N), thiab oxygen (O). Ntawm lawv, cov pa roj carbon ntau tshaj plaws (kwv yees li 65.57%), tom qab ntawd chlorine (li 19.36%). Kev kho mob ntawm cov tshuaj no feem ntau yog kho hnoos qhuav, uas yog, hnoos tsis muaj los yog me me phlegm. Nws alleviates cov tsos mob hnoos qhuav los ntawm inhibiting qhov chaw hnoos thiab txo qhov hnoos reflex. Cov txheej txheem ntawm kev ua no ua rau nws muaj txiaj ntsig zoo hauv kev kho cov tsos mob hnoos qhuav tshwm sim los ntawm kab mob ua pa sab saud, mob ntsws ntsws, mob ntsws ntev, thiab lwm yam mob. Txawm li cas los xij, nws yuav tsum tau muab sau tseg tias cov khoom no tsuas yog siv rau hauv chav kuaj.
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Tshuaj Formula |
C20H24ClNO |
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Exact Mass |
329 |
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Molecular Luj |
330 |
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m/z |
329 (100.0%), 331 (32.0%), 330 (21.6%), 332 (6.9%), 331 (2.2%) |
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Elemental Analysis |
C, 72,82; H, 7,33; Yog ', 10,75; N, 4,25; 4.85, ib |
Txoj kev synthesis ntawmcloperastine hydrochloride(tseem hu ua chlorpheniramine hydrochloride lossis hnoos syrup hydrochloride) tuaj yeem ua tiav los ntawm ntau txoj hauv kev, uas feem ntau vam khom cov txheej txheem kev sib txuas thiab cov ntsiab lus tshuaj tiv thaiv hauv cov tshuaj lom neeg.
Basic synthetic txoj kev
Lub synthesis ntawm chlorpheniramine hydrochloride feem ntau muaj ntau cov kauj ruam, nrog rau kev xaiv ntawm raw cov ntaub ntawv, cov synthesis ntawm intermediates, thiab cov ntsev tsim cov tshuaj tiv thaiv ntawm cov khoom kawg. Txoj kev yooj yim synthesis yuav suav nrog cov kauj ruam tseem ceeb hauv qab no:
Xaiv cov khoom pib tsim nyog, uas feem ntau suav nrog cov tebchaw uas muaj benzene rings, pyridine rings, thiab lwm yam qauv, nrog rau cov kua qaub uas siv rau kev tsim ntsev xws li hydrogen chloride lossis hydrochloric acid.
Los ntawm cov txheej txheem ntawm cov tshuaj lom neeg xws li hloov pauv cov tshuaj tiv thaiv, cov tshuaj tiv thaiv condensation, cov tshuaj tiv thaiv etherification, thiab lwm yam, cov ntaub ntawv pib tau hloov mus rau hauv cov khoom nruab nrab uas muaj lub hom phiaj tshuaj pob txha. Cov tshuaj tiv thaiv no yuav xav tau cov catalysts, cov kuab tshuaj, thiab cov tshuaj tiv thaiv tshwj xeeb xws li kub, siab, pH, thiab lwm yam.
Purification ntawm intermediates kom tshem tawm impurities thiab txhim kho cov purity ntawm cov khoom. Kev lim dej tuaj yeem suav nrog recrystallization, distillation, rho tawm, thiab lwm yam.
Cov purified nruab nrab yog reacted nrog hydrogen chloride los yog hydrochloric acid los tsim chlorpheniramine hydrochloride. Cov kauj ruam no yog ib qho ntawm cov kauj ruam tseem ceeb hauv cov txheej txheem synthesis, uas txiav txim siab cov khoom thiab qhov zoo ntawm cov khoom kawg.
Cloperastine hydrochloride, raws li cov tshuaj tiv thaiv kab mob hauv nruab nrab tsis muaj zog, muaj cov txheej txheem tseem ceeb ntawm kev ua haujlwm los ntawm inhibiting qhov chaw hnoos medullary, thaiv cov khoom xa tuaj ntawm cov hnoos reflex arc, thiab muaj cov tshuaj tiv thaiv tsis muaj zog thiab cov teebmeem bronchospasmolytic. Nws cov lus qhia tsis yog tsuas yog npog cov kab mob ua pa, tab sis kuj txuas mus rau ntau qhov chaw xws li kev ua xua, rov ua haujlwm tom qab, thiab kev kho mob rau cov qog.
Cov kab mob ua pa: kev tswj xyuas tag nrho los ntawm kev kis tus kab mob mus rau cov kab mob obstructive ntev
1. Tus Kab Mob Ua Ntsig Upper Respiratory Infection (URI)
Mob khaub thuas: Tus kab mob no nkag mus rau hauv lub ntsws ua pa sab sauv, ua rau mob caj pas thiab hnoos qhuav, uas tuaj yeem cuam tshuam lub chaw hnoos sai sai thiab txo cov tsos mob, tshwj xeeb tshaj yog rau cov neeg mob hnoos thaum hmo ntuj cuam tshuam rau kev pw tsaug zog.
Mob pharyngitis: Kev mob ntawm caj pas ua rau muaj kev hnov mob ntawm qhov hnoos qeev, thiab cov tshuaj txo cov hnoos qeev los ntawm kev hnoos hauv nruab nrab, kom tsis txhob muaj kev puas tsuaj ntxiv rau hauv caj pas (xws li lub suab qaum edema).
Cov ntaub ntawv kho mob: Hauv cov neeg mob khaub thuas, ib koob tshuaj ntawm qhov ncauj ntawm 20mg ua rau txo qis 60% hnoos ntau zaus hauv 30 feeb, kav ntev li 4 teev, thiab txhim kho kev pw tsaug zog zoo.
2. Tus kab mob ua pa qis
Mob bronchitis: Kab mob los yog kab mob tuaj yeem ua rau mob ntawm bronchial mucosa, stimulating hnoos reflex. Nws tuaj yeem siv ua ke nrog cov tshuaj expectorants (xws li ambroxol) txhawm rau txhawm rau hnoos qhuav thiab txhawb cov hnoos qeev.
Pneumonia: Mob ntsws ua rau hnoos nrog cov hnoos qeev tuab. Cov tshuaj yuav tsum tau siv los tiv thaiv hnoos thaum soj ntsuam hom kab mob (cov kab mob / kab mob). Cov kab mob pneumonia yuav tsum tau muab tshuaj tua kab mob ua ke.
Cov ntaub ntawv kho mob: Ib tus neeg mob hnub nyoog 35 xyoo uas muaj mob bronchitis tau noj 20mg ntawm chlorpheniramine hydrochloride thiab 30mg ntawm ambroxol peb zaug ib hnub. Tom qab peb hnub, qhov hnoos ntau zaus txo los ntawm 75%, thiab cov hnoos qeev ua nyias thiab yooj yim rau hnoos.
3. Tus kab mob Chronic obstructive pulmonary disease (COPD)
Mob ntsws ntsws ntev: Kev haus luam yeeb ntev lossis ib puag ncig muaj kuab paug tuaj yeem ua rau mob ntsws ntev, nrog rau kev hnoos qhuav thiab hnoos qeev. Chlorpheniramine hydrochloride tuaj yeem txo qhov hnoos qhuav, tab sis yuav tsum tau zam thaum siv ib leeg (raws li nws yuav inhibit expectoration).
Emphysema: Kev puas tsuaj ntawm cov qauv alveolar ua rau muaj kev txwv huab cua, thiab hnoos feem ntau ua rau hnoos qhuav. Cov tshuaj tuaj yeem ua ke nrog ntev - ua haujlwm bronchodilators (xws li tiotropium bromide) txhawm rau txhim kho cov tsos mob.
Cov ntaub ntawv tshawb fawb: Hauv cov neeg mob COPD ruaj khov, cov qhab nia hnoos ntawm pab pawg kho mob ua ke (chlorpheniramine hydrochloride + tiotropium bromide) tau txo los ntawm 40% piv rau cov pab pawg kho nrog cov tshuaj bronchodilators ib leeg.
4. Cov kab mob ntsws tshwj xeeb
Tuberculosis: Cov kab mob mycobacterium tuberculosis ua rau hnoos qhuav, thiab cov tshuaj tuaj yeem txo cov tsos mob, tab sis yuav tsum ua raws li cov qauv kev kho tuberculosis (xws li "quadruple therapy") yuav tsum tau ua.
Interstitial fibrosis ntawm lub ntsws: Interstitial o ntawm lub ntsws ua rau hnoos qhuav, thiab tuaj yeem ua ke nrog glucocorticoids (xws li prednisone) kom txo tau qhov mob.
Cov ntaub ntawv kho mob: Ib tus neeg mob hnub nyoog 60 xyoo uas muaj mob ntsws ntsws ntsws tau kho nrog 10mg ntawm clopidogrel hydrochloride peb zaug hauv ib hnub raws li kev kho mob los tiv thaiv tuberculosis. Tom qab ob lub lis piam, qhov hnoos ntau zaus tau txo los ntawm 50% thiab lub neej zoo tuaj.
Cov kab mob ua xua: kev cuam tshuam los ntawm kev ua pa mus rau ntawm daim tawv nqaij
1. Kev ua xua ua pa
Allergic rhinitis: Cov tshuaj histamine tso tawm ua rau congestion thiab edema ntawm qhov ntswg mucosa, ua rau qhov ntswg congestion, los ntswg qhov ntswg, thiab hnoos. Nws tuaj yeem inhibit histamine mediated hnoos reflex thiab txo cov tsos mob ntawm qhov ntswg.
hnoos variant asthma (CVA): ib hom mob hawb pob uas ua rau hnoos qhuav, uas cov tshuaj tuaj yeem ua ke nrog cov tshuaj nqus tau corticosteroids (xws li budesonide) los tswj txoj hlab ntsws.
Cov ntaub ntawv tshawb fawb: Hauv cov neeg mob CVA, qhov hnoos qeev ntawm cov pab pawg kho mob ua ke (chlorpheniramine hydrochloride + budesonide) tau mus txog 92%, uas yog 15% siab dua li ntawm pawg tshuaj hormone ib leeg.
2. tawv nqaij ua xua
Urticaria: Kev nthuav tawm ntawm cov hlab ntsha me hauv daim tawv nqaij thiab cov mucous membranes tuaj yeem ua rau liab thiab khaus, uas tuaj yeem txo cov tshuaj histamine mediated vasodilation thiab txo cov tsos mob khaus khaus.
Tshuaj ua pob khaus: Cov pob khaus tawv nqaij tshwm sim los ntawm kev tsis haum tshuaj, uas cov tshuaj tuaj yeem pab cov tshuaj tiv thaiv kab mob (xws li loratadine) los tswj kev tsis haum tshuaj.
Cov ntaub ntawv kho mob: Ib tus neeg mob 25- xyoo uas muaj urticaria tau noj 10mg ntawm chlorpheniramine hydrochloride thiab 10mg ntawm loratadine ib hnub ib zaug. Tom qab 3 hnub, cov pob khaus ploj thiab khaus khaus tag nrho.
Postoperative thiab post- cov tsos mob raug mob: kev sib koom tes tswj kev mob thiab hnoos
1. Kev hnoos tom qab phais
Kev phais hauv lub hauv siab: xws li lub ntsws resection thiab thoracoscopy, hnoos tom qab phais yuav ua rau mob incision los yog pneumothorax. Nws tuaj yeem cuam tshuam qhov chaw hnoos thiab txo qhov stimulation ntawm incision los ntawm hnoos.
Kev phais plab sab sauv: xws li cholecystectomy lossis subtotal gastrectomy, tom qab hnoos hnoos tuaj yeem ua rau mob plab thiab cuam tshuam rau qhov txhab zoo. Cov tshuaj tuaj yeem siv ua ke nrog tshuaj tua kab mob (xws li acetaminophen).
Cov ntaub ntawv kho mob: Hauv cov neeg mob uas tau phais hauv siab, kev siv tom qab siv 20mg clopidogrel hydrochloride peb zaug hauv ib hnub ua rau 65% txo qhov hnoos ntau zaus thiab 40% txo qhov mob qhov txhab.
2. Tom qab hnoos
Rib fracture: Kev hnoos yuav ua rau muaj kev sib txhuam ntawm qhov chaw tawg, ua rau mob hnyav. Chlorpheniramine hydrochloride tuaj yeem txo qhov hnoos thiab yuav tsum tau kho lub hauv siab (xws li lub hauv siab bandaging).
Tom qab tracheal intubation: Cov neeg mob uas muaj cua tshuab cua feem ntau muaj kev hnoos qhuav tom qab extubation. Cov tshuaj tuaj yeem txo cov tsos mob thiab txhawb kev kho mob ua pa.
Cov ntaub ntawv kho mob: Ib tus neeg mob hnub nyoog 40 xyoo uas muaj pob txha pob txha tau noj 10mg ntawm clopidogrel hydrochloride peb zaug ib hnub. Tom qab peb hnub, hnoos ntau zaus txo los ntawm 70% thiab qhov mob txo qis.
Cov tsos mob ntsig txog qog: qhov tseem ceeb ntawm kev kho mob rau kev txhim kho lub neej zoo
1. Mob ntsws cancer
Mob qog noj ntshav hauv lub ntsws: hnoos qhuav los ntawm qog nqaij hlav los yog compression ntawm lub bronchi tuaj yeem txo cov tsos mob, tab sis cov qog nqaij hlav thiab kev kho mob (xws li phais / kws khomob) yuav tsum tau soj ntsuam.
Tom qab xov tooj cua kho mob ntsws cancer: hluav taws xob puas rau bronchial mucosa ua rau hnoos qhuav, thiab cov tshuaj siv tau ua ke nrog cov tshuaj tiv thaiv mucosal (xws li sucralfate).
Cov ntaub ntawv tshawb fawb: Hauv cov neeg mob uas muaj mob qog noj ntshav siab, qhov kev txhim kho ntawm cov tsos mob hnoos tom qab siv chlorhexidine hydrochloride yog 60%, thiab kev pw tsaug zog zoo ntawm cov neeg mob tau zoo tuaj.
2. Mediastinal qog
Thymoma/Neurogenic Tumor: Cov qog compresses lub trachea lossis bronchi, ua rau hnoos qhuav. Cov tshuaj tuaj yeem txo cov tsos mob, tab sis qhov tseem ceeb yuav tsum tau muab rau kev kho cov qog (xws li kev phais phais).
Cov ntaub ntawv kho mob: Ib tus neeg mob hnub nyoog 55 xyoo uas mob qog nqaij hlav mediastinal tau kho nrog 20mg clopidogrel hydrochloride peb zaug hauv ib hnub thaum tos kev phais. Qhov hnoos ntau zaus tau txo los ntawm 50%, thiab lub xeev preoperative ruaj khov.
Cloperastine hydrochlorideinhibits HERGK + tam sim no nyob rau hauv ib tug muaj zog concentration- nyob rau hauv raws li nrog ib tug IC50 tus nqi ntawm 27 nM.Ntawm hnoos suppressants, cloperastine muaj antitussive thiab antianemic kev ua si thiab kuj yog siv nyob rau hauv bronchomuscular chemotherapy. Cloperastine yog ib qho tseem ceeb ua rau hnoos hnoos uas tseem muaj cov tshuaj tiv thaiv kab mob thiab tshuaj opioid, tab sis tsis muaj tshuaj loog.
Pharmacological Applications
Raws li ib qho tsis yog -cov tshuaj tiv thaiv hnoos hauv nruab nrab, clepivastine siv nws cov hnoos qeev los ntawm inhibiting qhov chaw hnoos. Nws cov nyhuv hnoos tsis muaj zog dua li ntawm codeine, tab sis nws tsis yog - siab ntev thiab tsis yog - quav, uas ua rau nws siv dav hauv kev kho mob. Cloperastine muaj txiaj ntsig zoo hauv kev txo cov hnoos qhuav tsis tu ncua uas tsis muaj hnoos qeev los ntawm kev mob hnyav ntawm lub ntsws sab saud, mob ntsws ntev, mob ntsws thiab mob ntsws cancer. Nws cov txheej txheem ntawm kev hnoos hnoos muaj xws li inhibiting bronchial du nqaij spasm, relieving bronchial mucosal congestion thiab edema, thiab yog li ua rau hnoos suppression. Tsis tas li ntawd, H1 receptor blocking nyhuv ntawm clepivastine kuj txo cov kev tsis haum tshuaj, ntxiv kev pab tiv thaiv hnoos.
Cloperastine yog ib qho tshuaj antihistamine uas thaiv H1 receptors thiab txo cov histamine stimulation ntawm mast hlwb thiab eosinophils, yog li txo cov tsos mob ntawm kev tsis haum tshuaj. Cov cuab yeej no ua rau Cloperastine zoo hauv kev kho mob ntawm cov tsos mob tshwm sim los ntawm kev tsis haum tshuaj xws li allergic rhinitis thiab urticaria. Tsis tas li ntawd, Cloperastine tuaj yeem inhibit gastric acid secretion thiab txo cov plab hnyuv puas tsuaj los ntawm kev sib tw antagonism ntawm histamine H2 receptors ntawm lub plab phab ntsa hlwb, uas tsim nyog rau kev kho mob ntawm cov tsos mob tsis xis nyob tshwm sim los ntawm gastric acid ntau dhau, xws li kub siab thiab acid reflux.
Cloperastine muaj qee yam sedative nyhuv, uas tuaj yeem txhim kho kev pw tsaug zog zoo, thiab ua rau nws pab txo kev ntxhov siab thiab ntxhov siab. Cov txheej txheem ntawm kev ua haujlwm no ua rau Cloperastine muaj txiaj ntsig hauv kev kho mob insomnia. Txawm li cas los xij, nws yuav tsum tau muab sau tseg tias ntev - siv Cloperastine tuaj yeem ua rau muaj kev vam khom, yog li nws yuav tsum tau siv raws li kev qhia ntawm tus kws kho mob thiab tus neeg mob lub cev yuav tsum tau saib xyuas kom zoo.
Cloperastine muaj peev xwm ua rau me ntsis txo cov nqaij ntshiv bronchial du spasm, ib qho cuab yeej uas yog siv los kho cov kab mob ua pa xws li bronchial hawb pob thiab mob ntsws ntsws ntev (COPD). Los ntawm kev so cov leeg nqaij bronchial, loperastine txhim kho tus neeg mob ua pa thiab txo cov tsos mob xws li dyspnea.
Cloperastine tuaj yeem ua rau muaj kev phiv xws li qaug zog thiab kiv taub hau, yog li koj yuav tsum tsis txhob tsav lub tsheb lossis ua lwm yam haujlwm uas yuav tsum tau ua kom muaj siab ntau thaum siv.
- Rau cov poj niam cev xeeb tub thiab pub niam mis, Cloperastine yuav tsum tau siv nrog ceev faj nyob rau hauv kev saib xyuas kev kho mob kom tsis txhob cuam tshuam rau kev noj qab haus huv ntawm tus me nyuam hauv plab los yog me nyuam mos.
- Yog tias tus neeg mob nrog cov tsos mob hnoos pom tseeb, kev siv cov tshuaj loperastine rau kev hnoos hnoos tuaj yeem cuam tshuam qhov hnoos reflex, ua rau hnoos qeev tsis yooj yim rau hnoos, ces yuav tsum tau siv nrog cov tshuaj expectorant.
- Cov kev siv tshwj xeeb thiab ntau npaum li cas ntawm loperastine yuav tsum tau txiav txim los ntawm tus kws kho mob raws li tus neeg mob lub hnub nyoog, qhov hnyav thiab tus mob, thiab lwm yam. Cov neeg mob yuav tsum ua raws li tus kws kho mob cov lus qhia.
Nyob rau hauv cov ntsiab lus, raws li ib tug tshuaj nrog central hnoos suppressant nyhuv, raws li zoo raws li antihistamine thiab opioid -zoo li kev ua si (tab sis tsis muaj tshuaj loog nyhuv), loperastine muaj ntau yam kev siv nyob rau hauv hnoos, antihistamine, central nervous system inhibition thiab bronchial nqaij so. Txawm li cas los xij, nws cov kev mob tshwm sim thiab contraindications yuav tsum tau muab sau tseg thaum siv nws, thiab cov tshuaj yuav tsum tau siv rationally raws li kev qhia ntawm tus kws kho mob.
ua faq
Yuav ua li cas yog lub mechanism ntawm kev txiav txim ntawm cloperastine hydrochloride?
Cov txheej txheem ntawm kev ua ntawm Cloperastine Hydrochloride koom nrog ntau txoj hauv kev uas sib koom ua ke rau nws txoj kev ua tau zoo hauv kev txo cov tsos mob hnoos. Feem ntau, Cloperastine Hydrochloride ua haujlwm los ntawmexerting ib qho kev ua haujlwm hauv nruab nrab ntawm qhov hnoos chaw nyob hauv medulla oblongata ntawm lub hlwb.
Cov kev phiv ntawm cloperastine HCL yog dab tsi?
Cim npe nrov: cloperastine hydrochloride cas 14984-68-0, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom