Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm clonidine hydrochloride hmoov cas 4205-91-8 hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo clonidine hydrochloride hmoov cas 4205-91-8 muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Clonidine Hydrochloride hmoovyog ib hom tshuaj uas feem ntau siv los tswj cov ntshav siab, lossis ntshav siab. Nws belongs rau cov chav kawm ntawm cov tshuaj hu ua central alpha-2 adrenergic agonists, uas ua haujlwm los ntawm kev ua haujlwm ntawm cov receptors tshwj xeeb hauv lub hlwb kom txo qis cov kev xav tawm, yog li txo lub plawv dhia thiab peripheral vascular tsis kam.
Qhov no nplua, dawb kom tawm -cov hmoov dawb yog cov ntsev hydrochloride ntawm clonidine, cov tshuaj sib xyaw nrog cov khoom tsim tshuaj. Thaum muab tshuaj, los ntawm qhov ncauj los yog transdermally, nws pab txo cov ntshav siab los ntawm kev txhawb nqa kev so ntawm cov hlab ntsha thiab txo lub plawv ua haujlwm.
Tshaj li nws cov teebmeem antihypertensive, nws kuj tau qhia rau kev kho mob ntawm kev tsis txaus siab hyperactivity disorder (ADHD) nyob rau qee kis, tshwj xeeb tshaj yog thaum siv los ua kev kho mob ntxiv. Tsis tas li ntawd, nws pom daim ntawv thov hauv kev tswj cov tsos mob tshem tawm cuam tshuam nrog opioid detoxification thiab cawv tshem tawm, vim nws lub peev xwm los txo kev ntxhov siab thiab ntxhov siab.
Qhov tseem ceeb, kev siv yuav tsum tau ua tib zoo saib xyuas los ntawm cov kws kho mob vim muaj kev phiv xws li qaug zog, qhov ncauj qhuav, kiv taub hau, thiab cem quav. Nws yog ib qho tseem ceeb uas yuav tsum tau ua raws li cov tshuaj noj nruj me ntsis thiab kom paub txog kev cuam tshuam nrog lwm cov tshuaj, tshwj xeeb tshaj yog cov uas cuam tshuam rau ntshav siab lossis lub plawv dhia.
Zuag qhia tag nrho,clonidine hydrochloride hmoovsawv cev rau qhov kev xaiv kho mob muaj txiaj ntsig hauv kev kho mob ntshav siab thiab lwm yam mob, tab sis nws cov txiaj ntsig yuav tsum raug ntsuas los ntawm kev pheej hmoo thiab cov kev mob tshwm sim nyob rau hauv kev saib xyuas kev kho mob.
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Tshuaj Formula |
C9H10Cl3N3 |
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Exact Mass |
265 |
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Molecular Luj |
267 |
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m/z |
265 (100.0%), 267 (95.9%), 269 (30.6%), 266 (9.7%), 268 (9.3%), 271 (3.3%), 270 (3.0%), 266 (1.1%), 268 (1.1%) |
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Elemental Analysis |
C, 40,55; H, 3,78; lwj, 39,90; Ib., 15.76 |
Synthesis method
A. Synthesis of Intermediate 1
Ntxiv 188ml formic acid thiab 100.0g 2,6-dichloroaniline rau cov tshuaj tiv thaiv lub hwj, kub thiab do hauv cov roj da dej kom yaj, do thiab reflux ntawm 95℃-100℃rau 5h, ces txias rau chav tsev kub, ces txias rau 0 degree, do thiab crystallize rau 2h, lim thiab qhuav kom tau dawb ntawm 72%.
B. Synthesis ntawm Intermediate 2
Ntxiv 70ml thionyl chloride thiab 92g intermediate 1 rau cov tshuaj tiv thaiv lub khob thiab do, txias rau 0℃hauv dej khov- da dej, thiab ntxiv ib qho sib xyaw ntawm 141ml thionyl chloride thiab 156ml sulfonyl chloride. Tom qab qhov sib ntxiv ua tiav, qhov kub thiab txias tau nce mus rau chav sov, thiab tom qab ntawd nce mus rau 40℃thiab stirred rau cov tshuaj tiv thaiv rau 20 teev. Tom qab lub kaw lus yog yaj, nws yog distilled nyob rau hauv lub siab txo kom txog thaum tsis muaj ib feem, 300 ml ntawm dichloromethane ntxiv, thiab qhov kub thiab txias yog txias rau 5℃nyob rau hauv ib tug dej khov - da dej. Ib qho tshuaj dichloromethane ntawm 131 g ntawm ethylenediamine yog ntxiv dropwise. Tom qab qhov sib ntxiv ua tiav, qhov kub thiab txias tau nce mus rau chav sov. Cov tshuaj tiv thaiv yog nres rau 2 teev. Tom qab cov tshuaj tiv thaiv tiav, 200 ml dej ntxiv rau hauv lub cev, nplawm rau 30 feeb, thiab tso cai rau sawv ntsug rau stratification. Lub aqueous theem yog muab rho tawm nrog 100 ml * 2 ntawm dichloromethane, lub aqueous theem yog muab pov tseg, cov organic theem yog ua ke, ntxuav nrog dej 3 zaug, ntxuav nrog 10% sodium hydroxide ob zaug, thiab ntxuav nrog saturated brine ib zaug, thiab lub dichloromethane txheej yog sau thiab concentrated kom tau ntxiv intermediate 00ml 2. 2, Ntxiv activated carbon, do thiab cua sov kom reflux, lim thaum kub, ntxiv 20ml ntawm hydrogen chloride -ethanol tov rau lub filtrate, kom sov thiab do rau 30min, txias ib txwm mus rau chav tsev kub, txias rau 0℃thiab do kom crystallize rau 3h, lim, yaug lub lim ncuav mog qab zib nrog ib tug me me npaum li cas ntawm ethanidine dissolves clover, qhuav clover. hydrochloride hauv 300ml dej, do hauv chav tsev kub rau 1h, lim kom tshem tawm cov teeb meem insoluble, txias kom qis dua 10℃hauv dej khov-dej da dej, kho pH rau 10 nrog 25% sodium hydroxide, ua kom dawb precipitate, lim, yaug lub ncuav mog qab zib lim nrog dej me me, thiab tau txais 60 { white.2g.
C. Synthesis ntawm clonidine hydrochloride
Ntxiv 250ml ntawm ethanol thiab 60.3g ntawm nruab nrab 2 mus rau 500ml tshuaj tiv thaiv lub raj mis, do thiab cua sov kom reflux. Tshem tawm cov teeb meem insoluble thaum kub, ntxiv 29.2g ntawm hydrogen chloride -ethanol tov rau cov lim, do hauv qab reflux rau 30min, ces txias rau chav tsev kub lawm, ces txias rau 0℃-5℃thiab do kom crystallize rau 3h, lim nrog suction, yaug lub lim ncuav mog qab zib nrog ib tug me me npaum li cas ntawm hydrochloride khoom. Ntxiv cov khoom ntub dej uas tau txais hauv cov kauj ruam dhau los mus rau 1-liter cov tshuaj tiv thaiv lub raj mis, ntxiv 250ml ntawm ethyl acetate, thiab do hauv chav sov li 1 teev. Tom qab ntawd lim, yaug lub ncuav mog qab zib lim nrog ib qho me me ntawm ethyl acetate, thiab qhuav kom tau 48.9g ntawm cov khoom dawb, nrog cov txiaj ntsig ntawm 90.01%.
Kev noj tshuaj
Dosage thiab kev tswj hwm ntawmclonidine hydrochloride hmoovNws txawv nyob ntawm seb lub hom phiaj kho. Hauv qab no yog cov koob tshuaj tshwj xeeb thiab kev siv:
- Txo cov ntshav siab:Pib koob tshuaj: 0.1 mg ob zaug ib hnub. Cov koob tshuaj nce ntxiv: 0.1-0.2mg ib hnub ntawm 2-4 hnub raws li xav tau. Kev Noj Qab Haus Huv Feem Ntau: 0.3-0.9mg / hnub hauv 2-4 koob tshuaj qhov ncauj. Hauv kev kub ntxhov hnyav uas xav tau kev kho mob xwm txheej ceev: pib nrog 0.2mg ntawm qhov ncauj, ua raws li 0.1mg ib teev nce mus txog thaum tswj cov ntshav siab diastolic lossis tag nrho ntawm 0.7mg tau mus txog, tom qab siv tshuaj kho mob.
- Menopausal kub flashes: koob tshuaj: 0.025-0.075mg ib zaug, ob zaug ib hnub.
- Mob hnyav dysmenorrhea: koob tshuaj: 0.025mg ntawm qhov ncauj ob zaug ib hnub twg rau 14 hnub ua ntej thiab thaum lub sij hawm cev xeeb tub.
- Migraine: Cov koob tshuaj: 0.025mg ib zaug, 2-4 zaug ib hnub, mus txog 0.05mg 3 zaug ib hnub.
- Cov kev ceev faj: Heev: 0.6mg ib zaug, 2.4mg ib hnub. Ua ntej siv Colistin Hydrochloride, koj yuav tsum sab laj nrog kws kho mob thiab noj cov tshuaj raws nraim li tau hais tseg. Colistin Hydrochloride tuaj yeem ua rau qee qhov tsis zoo, xws li lub qhov ncauj qhuav, kiv taub hau, txo qis kev ua haujlwm ntawm kev sib deev, thiab lwm yam. Yog tias cov tsos mob tsis xis nyob, koj yuav tsum nrhiav kev kho mob. Cov koob tshuaj yuav tsum maj mam txo thaum nres cov tshuaj kom tsis txhob rov ua kom ntshav siab.
Cov ntaub ntawv saum toj no tsuas yog siv rau kev siv xwb, qhov tshwj xeeb ntau npaum li cas thiab kev siv yuav tsum tau hloov kho raws li tus kheej qhov xwm txheej thiab tus kws kho mob cov lus qhia. Thaum siv colistin hydrochloride, ntshav siab thiab lub plawv dhia yuav tsum tau saib xyuas tsis tu ncua kom ntseeg tau tias cov tshuaj muaj txiaj ntsig thiab kev nyab xeeb.
- Cov txiaj ntsig: Colistin Hydrochloride feem ntau yog siv los kho cov xwm txheej kub ntxhov. Nws nkag mus rau hauv lub cev thiab txhawb nqa adrenal receptors nyob rau hauv lub paj hlwb, uas ua rau lub sympathetic paj hlwb nyob rau hauv lub hauv paus paj hlwb atrophy, yog li txo cov ntshav siab.
- Kev ceeb toom: Colistin Hydrochloride feem ntau tsis suav tias yog thawj - kab kev kho mob ntshav siab, yog li cov neeg mob yuav tsum ua raws li lawv tus kws kho mob cov lus qhia thaum xaiv cov tshuaj antihypertensive xaiv cov tshuaj uas haum rau lawv tus kheej.
Kev kho mob migraine
- Kev Ua Tau Zoo: Colistin Hydrochloride tuaj yeem siv los kho mob taub hau migraine. Tsis tas li ntawd, nws tseem tuaj yeem kho kub kub thiab mob khaub thuas uas tshwm sim thaum cev xeeb tub hauv cov poj niam.
- TXOJ CAI TSHIAB: Qee qhov kev phiv tshwm sim tuaj yeem tshwm sim nrog kev siv cov tshuaj colistin hydrochloride xws li kiv taub hau, qaug zog, thiab kev nyuaj siab. Qee tus neeg mob kuj tuaj yeem ua rau xeev siab, ntuav, insomnia thiab palpitations.
Thaum lub Cuaj Hlis 2010, US Food and Drug Administration (FDA) tau tso cai rau clonidine hydrochloride txuas ntxiv -tso tawm cov ntsiav tshuaj hauv qhov muaj zog ntawm 0.1mg thiab 0.2mg (branded li Kapvay los ntawm Shionogi Inc.). Qhov kev pom zoo no tau cim lub ntsiab lus tseem ceeb vim nws yog thawj tus qauv ntawmclonidine hydrochloride hmoovtshwj xeeb tau tso cai los ntawm FDA rau kev kho mob ntawm kev tsis txaus siab hyperactivity disorder (ADHD) hauv cov menyuam yaus hnub nyoog 6 txog 17 xyoo.
Kapvay yog qhia rau kev siv raws li kev kho mob monotherapy lossis ua ib qho ntxiv rau cov tshuaj stimulant hauv kev tswj cov tsos mob ADHD. Nws qhov kev pom zoo qhia txog lub luag haujlwm tshwj xeeb uas nws ua hauv kev kho mob arsenal tiv thaiv ADHD, tshwj xeeb tshaj yog tib yam tsis yog -cov tshuaj stimulant pom zoo siv nrog rau cov tshuaj stimulants los txhim kho cov txiaj ntsig kev kho mob.
Kev nthuav tawm - kev tsim tawm kom ntseeg tau tias muaj kev tso tawm ntawm clonidine hydrochloride nyob rau lub sijhawm txuas ntxiv, muab cov ntshav ruaj khov dua thiab muaj peev xwm txo qhov zaus ntawm koob tshuaj piv rau tam sim - tso tawm cov qauv. Qhov no tuaj yeem txhim kho kev ua raws li tus neeg mob thiab yooj yim, tshwj xeeb tshaj yog nyob rau hauv cov neeg mob.
Kev pom zoo ntawm Kapvay lees paub qhov kev xav tau rau ntau hom kev kho mob hauv ADHD, lees paub tias tsis yog txhua tus neeg mob teb txaus rau stimulants ib leeg. Los ntawm kev muab lwm txoj kev kho mob los yog kev kho ntxiv, Kapvay hais txog qhov kev xav tau tseem ceeb hauv kev tswj hwm ntawm ADHD, muaj peev xwm txhim kho lub neej zoo rau ntau tus menyuam yaus thiab cov tub ntxhais hluas uas tawm tsam nrog tus mob no.
Nws tseem ceeb heev uas yuav tsum nco ntsoov tias, zoo li txhua yam tshuaj, Kapvay yuav tsum tau muab tshuaj thiab saib xyuas los ntawm tus kws kho mob. Kev txiav txim siab siv Kapvay, ib leeg lossis ua ke nrog cov tshuaj stimulants, yuav tsum ua raws li kev soj ntsuam dav dav ntawm tus neeg mob cov tsos mob, keeb kwm kev kho mob, thiab muaj peev xwm txaus ntshai thiab cov txiaj ntsig. Kev soj ntsuam ze rau cov kev mob tshwm sim, xws li qaug zog, qhov ncauj qhuav, thiab ntshav siab, yog qhov tseem ceeb los xyuas kom muaj kev nyab xeeb thiab kev kho mob zoo.
kev phiv tshuaj
Clonidine Hydrochloride, raws li ib qho ₂ adrenergic receptor agonist, yog dav siv los ua kev kho mob rau cov kab mob xws li kub siab, tsis hnov lus tsis zoo siab (ADHD), tshem tawm syndrome (xws li opioid lossis cawv dependence), thiab migraine. Nws daim ntawv hmoov feem ntau yog siv los tsim cov tshuaj npaj los yog kev tshawb fawb txog kev tshawb fawb, tab sis kev sib cuag ncaj qha lossis siv tsis raug yuav ua rau muaj kev phom sij loj.
Cardiovascular system teb
Hypotension thiab bradycardia
Clonidine stimulates central alpha ₂ receptors, inhibits sympathetic paj hlwb, ua rau peripheral vasodilation thiab qeeb lub plawv dhia, yog li txo cov ntshav siab. Qhov no yog lub luag haujlwm tseem ceeb rau kev kho mob ntshav siab, tab sis nws kuj tseem tuaj yeem ua rau cov ntshav siab ntau dhau (systolic ntshav siab<90mmHg) or bradycardia (heart rate<60 beats/minute), especially during dose adjustment periods or in combination with other antihypertensive drugs. Patients may present with dizziness, fatigue, blurred vision, and in severe cases, fainting.
Reflex tachycardia
Qee cov neeg mob, tshwj xeeb tshaj yog cov menyuam yaus lossis cov neeg mob ntshav siab orthostatic, tej zaum yuav hnov ntxhiab tachycardia thaum pib noj tshuaj vim tias ntshav siab poob qis, tshwm sim raws li palpitations thiab lub hauv siab nruj, uas feem ntau yog ncua sij hawm thiab tuaj yeem txo tau nrog kev siv tshuaj ntev.
Ntshav siab rebound
Sudden discontinuation los yog tsis siv tshuaj yuav ua rau "rebound hypertension", uas yog ib tug ntse nce nyob rau hauv cov ntshav siab (systolic ntshav siab tuaj yeem nce los ntawm 30-40mmHg), nrog rau mob taub hau, ntxhov siab, tshee, tawm hws ntau dhau, thiab txawm tias kub siab encephalopathy. Qhov tshwm sim no muaj feem xyuam rau kev ua kom sai ntawm lub paj hlwb sympathetic thiab yuav tsum maj mam txo qis thiab txiav cov tshuaj.
Central paj hlwb teb
Sedation thiab tsaug zog
Clonidine tuaj yeem nkag mus rau hauv cov ntshav- lub hlwb thaiv, inhibit qhov hauv nruab nrab ntawm lub paj hlwb, thiab ua rau qaug zog, qaug zog, thiab tsis mloog, tshwj xeeb tshaj yog nyob rau theem pib ntawm kev noj tshuaj lossis nce koob tshuaj. Kwv yees li 10% -25% ntawm cov menyuam yaus uas muaj ADHD qhia txog kev qaug zog, uas yuav cuam tshuam rau kev kawm.
Kev nyuaj siab thiab kev nyuaj siab
Kev siv lub sijhawm ntev tuaj yeem ua rau lossis ua rau muaj kev nyuaj siab ntau ntxiv, ua rau muaj kev xav tsis zoo, tsis txaus siab, thiab pw tsaug zog tsis zoo. Qee tus neeg mob yuav muaj kev ntxhov siab, chim siab, thiab txawm tias kev xav tua tus kheej (tsis tshua muaj tab sis yuav tsum ceev faj).
Kev pw tsaug zog tsis zoo
Xws li insomnia, nquag npau suav, npau suav phem, tshwj xeeb tshaj yog thaum noj tshuaj thaum hmo ntuj. Kwv yees li 5% -10% ntawm cov neeg mob menyuam yaus qhia txog kev pw tsaug zog, uas tej zaum yuav cuam tshuam nrog kev cuam tshuam ntawm cov tshuaj ntawm kev pw tsaug zog.
Kev txawj ntse muaj nuj nqi cuam tshuam
Qee qhov kev tshawb fawb qhia tias kev siv sijhawm ntev - yuav cuam tshuam rau kev paub txog kev ua haujlwm xws li kev nco thiab kev saib xyuas, tshwj xeeb tshaj yog rau cov neeg laus uas xav tau kev saib xyuas.
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