Shaanxi BLOOM Tech Co., Ltd. yog ib tug ntawm cov uas paub txog manufacturers thiab lwm tus neeg ntawm cimetidine hmoov cas 51481-61-9 nyob rau hauv Suav teb. Txais tos rau cov lag luam wholesale zoo siab cimetidine hmoov cas 51481-61-9 muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Cimetidine hmoovCov mis mos molecular yog C10H16N6S, CAS 51481-61-9, thiab tus txheeb ze molecular hnyav yog 252.34g/mol. Dawb los yog dawb dawb hmoov, iab, deliquescent, insoluble nyob rau hauv dej, me ntsis soluble nyob rau hauv ethanol thiab chloroform, soluble nyob rau hauv acetic acid, nitric acid, concentrated hydrochloric acid thiab sodium hydroxide tov. Nws tshwm sim raws li cation nyob rau hauv ib puag ncig acidic thiab raws li ib tug nruab nrab daim ntawv nyob rau hauv ib tug nruab nrab los yog alkaline ib puag ncig. Cov tshuaj nrog qis pKa thiab qib siab dua ntawm ionization feem ntau yog siv los kho cov kab mob xws li peptic ulcer thiab hyperacidity. Nws cov qauv molecular tshwj xeeb txiav txim siab tias nws muaj qee yam kev ua haujlwm lom neeg thiab cov tshuaj pharmacological, tab sis nws kuj ua rau nws yooj yim rau deliquescence thiab photolysis thiab lwm yam, yog li nws yuav tsum tau khaws cia thiab siv nrog kev saib xyuas. Nws yog ib hom H2 receptor antagonist, feem ntau yog siv los kho mob plab, peptic ulcer thiab lwm yam kab mob tshwm sim los ntawm hyperacidity.
Cov ntaub ntawv ntxiv ntawm chemical compound:
yam khoom
Cimetidine +. COA
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Tshuaj Formula |
C19H20O3 |
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Exact Mass |
296 |
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Molecular Luj |
296 |
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m/z |
296 (100.0%), 297 (20.5%), 298 (2.0%) |
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Elemental Analysis |
C, 77.00; H, 6.80; O, 16.20 |
Cimetidine hmoovyog ib yam tshuaj uas inhibits qhov tso tawm ntawm gastric acid. Nws lub luag haujlwm tseem ceeb ntawm kev ua haujlwm yog kev sib tw inhibiting histamine receptor H2 ntawm lub plab mucosa, yog li txo qis acidity ntawm gastric kua txiv thiab cov kua qaub ntawm gastric secretion. Ntxiv nrog rau kev siv los kho cov kab mob hauv plab xws li peptic ulcer thiab reflux esophagitis, Cimetidine muaj ntau yam kev siv tshuaj kho mob.
1. Peptic ulcer thiab gastroesophageal reflux kab mob:
Cimetidine yog thawj H2 receptor antagonist tsim rau kev kho mob peptic ulcer, uas txhawb kev kho mob los ntawm kev txo cov kua qaub hauv plab thiab kev tiv thaiv kab mob plab. Nyob rau tib lub sijhawm, Cimetidine kuj tseem siv los kho tus kab mob gastroesophageal reflux, uas tuaj yeem txo qhov mob substernal, acid regurgitation, belching thiab lwm yam tsos mob, thiab txo qhov tshwm sim ntawm esophageal spasm.
2. Zollinger-Ellison syndrome thiab PEPSI kab mob:
Zollinger-Ellison Syndrome yog ib yam kab mob uas tsis tshua muaj tshwm sim los ntawm cov qog nqaij hlav hauv plab hnyuv thiab txiav txiav uas zais cov kua qaub ntau hauv plab. Cimetidine, tshuaj uas inhibits gastric acid secretion, tau qhia nws qhov tseem ceeb hauv kev kho mob Zollinger-Ellison syndrome.
Tsis tas li ntawd, Cimetidine kuj tseem siv rau hauv cov kab mob tsis tshua muaj kab mob gastritis PEPSI, uas tuaj yeem txo cov tsos mob ntawm cov neeg mob uas muaj tus kab mob no thiab txhawb kev txhim kho ntawm tus mob.
3. Purpura nephritis:
Purpura nephritis yog ib yam kab mob autoimmune tshwm sim los ntawm glomerular puas, lub raum tsis ua haujlwm, thiab hematuria. Cimetidine, raws li ib qho tshuaj uas muaj cov nyhuv antihistamine, tuaj yeem cuam tshuam qhov permeability ntawm glomerular hauv qab daim nyias nyias, yog li txo qhov pom ntawm proteinuria thiab hematuria. Tsis tas li ntawd, Cimetidine tseem tuaj yeem txo qhov kev tiv thaiv kab mob los ntawm kev txo qis kev tawm tsam ntawm T hlwb ntawm ob lub raum, yog li txhim kho lub raum ua haujlwm.
4. Mob cancer mis thiab prostate:
Cimetidine tau pom tias inhibit qhov kev loj hlob thiab kis ntawm lub mis thiab prostate cancer. Nws cov txheej txheem tuaj yeem cuam tshuam nrog nws txoj haujlwm ntawm inhibiting histamine thiab txo qhov tso tawm ntawm kev hloov pauv. Cimetidine tau dhau los ua ib qho tshuaj adjuvant feem ntau siv hauv kev kho mob cancer ntawm lub mis thiab prostate.
5. Immunomodulators:
Cimetidine tuaj yeem cuam tshuam rau kev tsim thiab kev ua haujlwm ntawm lub cev tiv thaiv kab mob xws li T hlwb, B hlwb thiab macrophages los ntawm inhibiting cov nyhuv ntawm histamine, thiaj li ua tiav cov nyhuv ntawm kev tiv thaiv kab mob. Nws tuaj yeem siv los kho cov kab mob autoimmune xws li mob caj dab rheumatoid, psoriasis, thiab Behcet's kab mob, thiab muaj kev nyab xeeb thiab kev ua siab ntev.
6. Cov kab mob ntawm daim tawv nqaij:
Cimetidine kuj tseem siv tau los kho ntau yam kab mob ntawm daim tawv nqaij, xws li mob urticaria, vitiligo, thiab kab mob edematous. ntawm kev kho mob.
Nyob rau hauv luv luv, Cimetidine tsis yog tsuas yog ib tug tshuaj rau kev kho mob ntawm peptic ulcer, tab sis kuj muaj ntau yam kev siv nyob rau hauv cov kab mob glomerular, mob cancer, kev tiv thaiv kab mob thiab lwm yam teb. Cimetidine muaj qhov dav -spectrum pharmacological teebmeem, thiab tau raug pov thawj tias muaj txiaj ntsig zoo hauv kev kho mob ntau yam.
Cimetidine hmoovyog ib qho tshuaj siv dav hauv kev kho mob plab. Nws cov txheej txheem synthesis feem ntau suav nrog: 4-amino-2-picoline derivative method, thiocyanate method, polyethylene glycol (PEG) method, kua theem tshuaj tiv thaiv txoj kev, microwave-pab synthesis thiab lwm txoj kev. Cov txheej txheem no tau piav qhia hauv qab no:
Cov txheej txheem hluavtaws ntxov tshaj plaws ntawm Cimetidine yog 4-amino-2-picoline derivative txoj kev, thiab nws cov kauj ruam tseem ceeb suav nrog cov tshuaj tiv thaiv ntawm benzimide thiab ethyl isocyanate los tsim 3-(2-methyl-4-azapyridine Azol-5-yl)-N-phenyl reduction ntawm txhuas thiab thermal polycondensation muab Cimetidine.
Qhov kom zoo dua ntawm txoj kev no yog cov tshuaj tiv thaiv yooj yim, cov khoom siv raw yooj yim tau txais, thiab cov txiaj ntsig tau siab li 80%, tab sis tseem muaj qee yam tsis xws luag, xws li yuav tsum tau siv aluminium hydroxide thiab siab - kub thermal condensation cov tshuaj tiv thaiv, uas yuav ua rau muaj kev puas tsuaj rau ib puag ncig thiab tib neeg kev noj qab haus huv.
Txoj kev thiocyanate yog ib txoj kev uas feem ntau siv hauv kev npaj Cimetidine. Cov kauj ruam tseem ceeb yog siv tert-butyl thiocyanate thiab 2-picoline ua cov ntaub ntawv pib los ua kom muaj 3-(2-methyl-4- Azapyrazol-5-yl)-N-phenylpropanamide, ua raws li kev txo qis thiab thermal polycondensation los tsim Cimetidine.
Txoj kev no muaj qhov zoo ntawm cov txiaj ntsig siab (ntau dua 90%), kev ua haujlwm yooj yim, thiab nkag tau yooj yim rau cov khoom siv raw. Txawm li cas los xij, thiocyanate siv nyob rau hauv nws yog volatile thiab muaj ib tug stimulating nyhuv ntawm lub cev, yog li nws yuav tsum tau kev tiv thaiv.
Txoj kev PEG yog ib txoj kev tshiab ntawm kev sib xyaw Cimetidine. Nws lub hauv paus ntsiab lus yog ntxiv PEG uas muaj cov khoom ua ntej ntawm Cimetidine thiab cov kua qaub catalyst (xws li potassium dihydrogen phosphate) rau hauv cov tshuaj tiv thaiv ua ke. PEG compounds yog soluble nyob rau hauv dej thiab tiv thaiv cov precursor tebchaw los ntawm hydrolysis, oxidation los yog acidification.
Txoj kev no muaj qhov zoo ntawm kev ua haujlwm yooj yim, muaj txiaj ntsig siab, thiab tsis muaj kev puas tsuaj rau ib puag ncig. Txawm li cas los xij, kev ua haujlwm ntawm PEG compound yog qhov nyuaj thiab yuav tsum tau ua tib zoo ua haujlwm, thiab cov teeb meem xws li PEG crystallization thiab degradation yuav tshwm sim thaum lub sijhawm ua haujlwm, uas cuam tshuam rau cov txiaj ntsig.
Cov kua dej -theem tshuaj tiv thaiv txoj kev yog ib qho yooj yim thiab yooj yim hluavtaws txoj kev rau Cimetidine. Nws lub hauv paus ntsiab lus yog los ua 2-picoline, tert-butyl thiocyanate thiab benzimide nyob rau hauv cov kua-theem cov tshuaj tiv thaiv. Cimetidine tuaj yeem tau txais tom qab txo cov alumina thiab thermal polycondensation cov tshuaj tiv thaiv.
Txoj kev no muaj qhov zoo ntawm kev ua haujlwm yooj yim thiab lub sijhawm luv luv, tab sis cov tshuaj tiv thaiv yuav tsum muaj qhov sib thooj ntawm cov molar piv ntawm benzimide thiab tert -butyl thiocyanate yog 1: 2, thiab cov txheej txheem tshuaj tiv thaiv yog qhov nyuaj rau kev tswj, yuav tsum tau rov kuaj dua thiab ua kom zoo dua.
Microwave-pab synthesis txoj kev yog ib hom tshiab ntawm Cimetidine synthesis txoj kev, nws lub ntsiab tseem ceeb yog nyob rau hauv lub microwave cua sov, siv microwave- pab,
Ceev cov tshuaj tiv thaiv ceev. Cov kauj ruam tshwj xeeb suav nrog: ntxiv ethyl thiocyanate thiab isopropanol rau lub microwave reactor, ntxiv ntau tshaj 2-picoline, thiab ua haujlwm microwave-pab cua sov nrog lub zog ntawm li 50%, kom txog rau thaum cov xim ntawm cov tshuaj hloov ntawm lub teeb mus rau qhov tsaus ntuj, thiab cov tshuaj tiv thaiv dhau ntawm cov nag lossis daus tau raug rho tawm thiab huv si.
Txoj kev no muaj qhov zoo ntawm cov tshuaj tiv thaiv ceev ceev, siab yield, thiab kev ua haujlwm yooj yim. Txawm li cas los xij, vim qhov kev tawm tsam hnyav tuaj yeem tshwm sim los ntawm microwave cua sov, nws yog ib qho tsim nyog yuav tsum tau ua tib zoo saib xyuas kev nyab xeeb.
Nyob rau hauv tas li ntawd, muaj ntau yam synthetic txoj kevCimetidine hmoov, thiab ib txoj kev tsim nyog tuaj yeem xaiv rau kev npaj raws li qhov xav tau tiag tiag. Cov kev sib txawv muaj lawv tus kheej qhov zoo thiab qhov tsis zoo ntawm kev ua haujlwm nyuaj, tawm los, lub sijhawm ua haujlwm, ib puag ncig tus phooj ywg, thiab cuam tshuam rau tib neeg kev noj qab haus huv thiab kev nyab xeeb.
kev phiv tshuaj
Cimetidine, raws li ib tug classic histamine H ₂ receptor antagonist, tau ua lub luag haujlwm tseem ceeb hauv kev kho mob ntawm gastric acid ntsig txog kab mob txij li thaum nws pib xyoo 1976. Nws cov hmoov formulation (Cimetidine Powder) tseem siv rau hauv kev kho mob vim nws yooj yim ntawm kev hloov kho thiab kev tswj tshwj xeeb (xws li kev noj zaub mov hauv qhov ntswg). Txawm li cas los xij, nrog rau hauv - kev tshawb fawb tob ntawm nws cov tshuaj siv tshuaj thiab kev soj ntsuam ntev - lub sijhawm soj ntsuam, nws cov tshuaj tiv thaiv tsis zoo tau maj mam ua kom pom tseeb.
Tej yam tshwm sim tsis zoo
Cov tshuaj tiv thaiv digestive
Mob plab: Qhov tshwm sim yog li ntawm 5% -10%, uas yog ntau dua nyob rau hauv cov theem pib ntawm cov tshuaj thiab tej zaum yuav muaj feem xyuam rau txoj hnyuv microbiota imbalance los yog hloov nyob rau hauv plab hnyuv pH tom qab gastric acid suppression. Cov tsos mob tshwm sim yog cov quav dej, 3-5 zaug hauv ib hnub, uas txo qis 1-2 hnub tom qab txiav cov tshuaj.
Kev cem quav: Qee tus neeg mob me me (kwv yees li 2% -3%) muaj kev mob plab hnyuv peristalsis vim txo qis hauv plab acid secretion, ua rau muaj teeb meem hauv kev tso quav, tshwj xeeb tshaj yog cov neeg laus.
xeev siab/ ntuav: Qhov tshwm sim yog li ntawm 3% -5%, uas tej zaum yuav muaj feem xyuam rau ncaj qha stimulation ntawm pais plab mucosa los yog central paj hlwb los ntawm cov tshuaj. Nws feem ntau txhim kho tom qab kho cov koob tshuaj lossis kev sib txuas nrog cov tshuaj prokinetic.
Central paj hlwb teb
Mob taub hau/ kiv taub hau: Qhov tshwm sim yog kwv yees li 4% -8%, uas tej zaum yuav muaj feem xyuam rau qhov tsis yog - tshwj xeeb antagonism ntawm histamine H ₁ receptors los ntawm cov tshuaj tom qab dhau los ntawm cov ntshav-hlwb barrier (BBB). Nws feem ntau yog mob me thiab kav ntev li 1-3 hnub.
Pw tsaug zog / qaug zog: Kwv yees li 3% -5% ntawm cov neeg mob qhia txog kev tsaug zog thaum nruab hnub, tshwj xeeb tshaj yog nyob rau theem pib ntawm kev siv tshuaj, uas tej zaum yuav cuam tshuam nrog kev cuam tshuam hauv nruab nrab.
Kev puas siab puas ntsws: tsis tshua muaj tab sis hnyav, nrog rau kev ntxhov siab, kev nyuaj siab, delirium (tshwj xeeb tshaj yog cov neeg laus lossis cov neeg mob hnyav), nrog rau qhov tshwm sim ntawm 0.1% -0.5%. Kev rov qab tuaj yeem ua tiav hauv 48 teev tom qab tsis siv tshuaj.
Cimetidine tuaj yeem inhibit histamine synthesis hauv lub hlwb, cuam tshuam nrog lub sijhawm pw tsaug zog, thiab cov neeg laus muaj kev cuam tshuam ntau dua rau kev koom tes vim muaj ntshav nce ntxiv -b hlwb barrier permeability.
Endocrine system teb
Cov nyhuv Antiandrogenic: Lub sij hawm ntev siab - siv koob tshuaj (Ntau dua lossis sib npaug li 1.6g ib hnub) tuaj yeem ua rau txiv neej lub mis loj hlob (kwv yees li 1% -2%), txo libido, erectile kawg (0.5% -1%), thiab poj niam galactorrhea (0.3% -0.8%). Cov txheej txheem yog inhibit qhov hypothalamic pituitary gonadal axis thiab txo qis testosterone secretion.
Nce prolactin: Kwv yees li 5% -10% ntawm cov neeg mob muaj kev nce siab me ntsis ntawm cov tshuaj prolactin (PRL), tab sis tsuas yog ob peb (li 1%) tau ntsib kev kho mob galactorrhea.
Hematological system tshuaj tiv thaiv
Peb muab ntau yam khoom sib kis, suav nrog cov sprockets, cov hlua khi, lub zog, txuas txuas, racks, hubs, pulleys, lub tes tsho taper, bearing rooj, thiab lwm yam.
Kev phiv loj heev
Neurotoxicity
Trembling delirium: Hauv kev kho mob plab hnyuv hauv cov neeg haus dej cawv, nws tuaj yeem ua rau muaj kev tshee, hnov lus, thiab tsis meej pem zoo ib yam li cawv tshem tawm syndrome, nrog qhov tshwm sim ntawm li 0.05% -0.1%. Cov txheej txheem yuav cuam tshuam nrog qhov tsis sib xws ntawm gamma aminobutyric acid (GABA) system thiab BBB nkag mus ntawm Cimetidine thaum tshem tawm cawv.
Kev qaug dab peg: tsis tshua muaj heev (<0.01%), may be related to lowering the seizure threshold or drug interactions (such as in combination with phenytoin sodium).
Txoj hauv kev kho mob: Tso tshuaj tam sim ntawd, muab 5-10mg ntawm diazepam txhaj tshuaj kom tswj cov tsos mob, thiab siv phenobarbital yog tias tsim nyog.
Hepatotoxicity
Kev nce qib transaminase: Kwv yees li 2% -5% ntawm cov neeg mob muaj kev nce siab ntawm ALT / AST (<3-fold upper limit), which is usually asymptomatic and reversible after discontinuation of medication.
Mob lub siab mob: tsis tshua muaj heev (<0.01%), manifested as jaundice and coagulation disorders, requiring immediate discontinuation of medication and supportive treatment.
Mechanism: Tej zaum nws yuav tiv thaiv kab mob -kev kho mob siab cell puas lossis metabolic toxicity.
Kev ua xua
Rash / Urticaria: Qhov tshwm sim yog kwv yees li 1% -3%, feem ntau yog hom I hypersensitivity tshwm sim, tshwm sim raws li erythema thiab khaus, uas tuaj yeem txo tau los ntawm kev noj tshuaj tiv thaiv kab mob tom qab tsis siv tshuaj.
Vascular edema: tsis tshua muaj (<0.1%), may involve the larynx and cause difficulty breathing, requiring emergency treatment (subcutaneous injection of adrenaline 0.3-0.5mg).
Hla kev ua xua: Cov tib neeg uas ua xua rau lwm tus H ₂ receptor antagonists (xws li ranitidine) muaj kev pheej hmoo ntawm kev ua xua rau Cimetidine.
Cim npe nrov: Cimetidine hmoov CAS 51481-61-9, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom