Histamine H1 receptor blockers (abbreviated AGP) tau ua haujlwm rau noob neej txog xya caum xyoo. Lawv ib txwm nyob rau hauv kev thov hauv tshuaj. Tawm tsam keeb kwm yav dhau los no, lawv tsis ntev los no tau siv yam tsis muaj kws kho mob cov tshuaj, uas yog qhov txaus ntshai. Feem ntau, cov blockers no tau siv los kho cov kab mob ua xua, txawm li cas los xij, lawv feem ntau siv rau hauv kev kho mob ntawm cov kab mob xws li mob ntsws, mob ntsws thiab cov txheej txheem autoimmune, uas, ntawm chav kawm, cuam tshuam txog kev paub niaj hnub ntawm lawv cov keeb kwm.
Tom ntej no, cia peb saib ze dua ntawm H1 histamine receptor blockers, nrhiav seb lawv cov yam ntxwv zoo li cas, thiab ntxiv rau, nrhiav seb lawv yog leej twg nyob rau tiam thib ob.
Definition: dab tsi yog receptor blockers?
H1-histamine receptor blockers yog tshuaj. Muaj ntau ntau yam tshuaj uas cuam tshuam rau kev tso tawm, thiab ntxiv rau, cov dynamics, kinetics thiab metabolism ntawm histamine. Cov no suav nrog, tshwj xeeb, physiological thiab inverse histamine agonists.
Keeb kwm, lo lus "antihistamines" yog hais txog cov tshuaj uas thaiv H1-histamine receptors. Txij li thaum xyoo 1937, thaum cov nyhuv antihistamine ntawm ib qho kev sib xyaw ua ke yav dhau los yog thawj zaug tau lees paub, kev txhim kho tau ua tiav nrog rau kev txhim kho cov tshuaj tiv thaiv kab mob. Tam sim no cia peb mus rau kev txiav txim siab cov yam ntxwv ntawm cov khoom siv kho mob.
Txoj kev ntawm cov nyiaj no
Ntau qhov kev tshawb fawb tau pom tias histamine, vim nws cov teebmeem ntawm cov neeg ua pa ntawm tib neeg txoj kev ua pa, tawv nqaij thiab ob lub qhov muag, ua rau cov tsos mob ntawm kev ua xua, thiab cov tshuaj tiv thaiv uas xaiv los thaiv histamine H1 receptors tuaj yeem nres thiab tiv thaiv nws.
Feem ntau ntawm cov tshuaj antihistamine siv muaj ntau yam tshuaj tshwj xeeb uas ua rau lawv ua ib pawg cais. Cov no suav nrog cov teebmeem hauv daim ntawv ntawm antipruritic, decongestant, antispastic, anticholinergic, antiserotonin, sedative thiab tshuaj loog hauv zos, thiab ntxiv rau, kev tiv thaiv ntawm histamine-induced bronchial spasm. Ib txhia ntawm lawv yog tus yam ntxwv tsis yog los ntawm histamine blockade, tab sis los ntawm cov yam ntxwv nta.
Mechanism ntawm kev sib tw inhibition
Cov tshuaj tiv thaiv kab mob tuaj yeem thaiv cov teebmeem ntawm histamineH1 receptors ntawm cov txheej txheem ntawm kev sib tw inhibition. Tab sis lawv cov affinity rau cov receptors no tsawg dua piv rau histamine. Yog li, cov tshuaj no tsis tuaj yeem tshem tawm cov tshuaj histamine, uas yog khi rau cov receptor.
Lawv tsuas tuaj yeem thaiv cov khoom tso tawm thiab tsis muaj neeg nyob. Raws li, H1 hom blockers yog qhov zoo tshaj plaws los tiv thaiv kev tsis haum tshuaj tam sim ntawd, thiab thaum muaj cov tshuaj tiv thaiv uas twb tshwm sim lawm, nws tiv thaiv kev tso tawm ntawm ib feem tshiab ntawm histamine.
Los ntawm lawv cov qauv tshuaj, feem ntau ntawm cov tshuaj no tau muab cais ua amines, soluble hauv cov rog, uas muaj cov qauv zoo ib yam. Lawv lub hauv paus yog sawv cev los ntawm ib pab pawg neeg aromatic los yog heterocyclic. Lawv muaj nws txuas nrog kev pab los ntawm ib tug molecule ntawm nitrogen, carbon los yog oxygen nrog ib tug amino pawg. Lub hauv paus txiav txim siab qhov hnyav ntawm kev ua haujlwm antihistamine nrog rau qee yam ntawm cov khoom. Paub txog cov muaj pes tsawg leeg, nws muaj peev xwm txiav txim siab ua ntej lub zog ntawm cov tshuaj nrog rau nws cov teebmeem, piv txwv li, nws muaj peev xwm tsim kom muaj peev xwm nkag mus rau hauv cov ntshav-hlwb teeb meem. Tom ntej no, nrhiav seb hom tshuaj twg muab faib ua.
Tseem ntawm antagonists
Muaj ntau qhov kev faib tawm ntawm H1 histamine receptor antagonists, txawm hais tias tsis muaj leej twg suav tias feem ntau lees txais hnub no. Raws li ib qho kev faib tawm nrov, cov tshuaj antihistamine muab faib ua cov tshuaj thawj zaug thiabtiam thib ob.
Cov tshuaj uas thaiv H1 histamine receptors uas yog thawj tiam feem ntau hu ua sedatives (raws li cov kev mob tshwm sim tseem ceeb), piv rau cov tshuaj uas tsis yog tshuaj sedating uas yog rau tiam thib ob. Tam sim no, tiam thib peb tseem raug cais tawm, uas suav nrog cov tshuaj tshiab hauv daim ntawv ntawm cov tshuaj metabolites, uas, ntxiv rau cov tshuaj tiv thaiv siab tshaj plaws, pom tias tsis muaj cov teebmeem sedative thiab cov teebmeem cardiotoxic yam ntxwv ntawm cov tshuaj thib ob.
Ntxiv rau, raws li cov qauv tshuaj (uas feem ntau nyob ntawm X-daim ntawv cog lus), cov tshuaj tiv thaiv kab mob tau muab faib ua ntau pawg: ethanolamines nrog rau ethylenediamines, alkylamines, quinuclidine derivatives, alphacarboline, piperazine, phenothiazine thiab piperidine.
Cia peb xav txog H1 histamine receptor blockers kom ntxaws ntxiv.
thawj thiab thib ob tiam tshuaj
Yog li, thawj tiam tshuaj suav nrog cov khoom kho mob hauv daim ntawv ntawm Diphenhydramine, Benadryl, Doxylamine, Antazolin, Mepyramine, Quifenadine, Sequifenadine, Suprastin thiab lwm yam.
H1 histamine receptor blockers ntawm 2nd tiam muaj xws li Akrivastine nrog rau Astemizole, Dimentinden, Oxotamide, Terfenadine, Loratadine, Mizolastine, Soventol, Claritin, "Kestin" thiab lwm yam.
Loratadine ua cov tshuaj tiv thaiv kab mob thib ob zoo tshaj plaws
siv davCov tshuaj thib ob yog tam sim no ib yam tshuaj hu ua Loratadine. Cov nyhuv antihistamine ntawm cov tshuaj no nce mus txog qhov siab tshaj plaws tom qab yim mus rau kaum ob teev. Nws kav ntev tshaj nees nkaum plaub teev. Nws yog tsim nyog hais tias cov cuab yeej no tau kawm zoo, thiab tsis tshua muaj kev cuam tshuam tsis zoo rau cov neeg mob. Nws qhov ntau npaum li cas nyob ncaj qha rau hnub nyoog, thiab ntxiv rau, ntawm lub cev hnyav.
Active metabolite - yog dab tsi?
Cov nquag metabolite ntawm H1 histamine receptor blockers yog cov tshuaj nquag ntawm cov tshuaj tom qab cov tshuaj tau ua tiav los ntawm lub cev. Feem ntau ntawm cov tshuaj saum toj no rhuav tshem, raws li txoj cai, nyob rau hauv daim siab, ua raws li los ntawm kev tsim cov ntaub ntawv nquag ntawm cov metabolites uas ua lub luag haujlwm tseem ceeb hauv kev siv cov txiaj ntsig kho mob tsim nyog. Yog tias daim siab ua haujlwm tsis zoo, qee cov tshuaj tuaj yeem sau rau hauv tib neeg lub cev, uas yuav ua rau lub sijhawm QT ncua sij hawm ntawm electrocardiogram nrog kev txhim kho ntxiv ntawm ventricular pirouette tachycardia.
Cov lus qhia tseem ceeb rau kev siv tshuaj
Qhov taw qhia tseem ceeb rau kev sau tshuaj rau cov neeg mob yog qhov sib txawv ntawm kev noj qab haus huv vim muaj ntau yam kev tsis haum tshuaj nyob rau hauv daim ntawv ntawm atopic dermatitis, kev tsis haum tshuaj, urticaria, kab tom, thiab lwm yam. tshuaj yog tias lawv thaivhistamine receptors nyob rau hauv lub cev. Ua tsaug rau cov txheej txheem no, tso tawm cov khoom siv roj ntsha mus rau hauv cov ntshav thiab cov ntaub so ntswg, uas yog lub luag haujlwm rau kev txhim kho kev ua xua, nres lossis txo qis.
Yog li, cov tshuaj siv ntau tshaj plaws rau kev kho kev ua xua yog tshuaj tiv thaiv kab mob. Cov tshuaj no thaiv cov tshuaj histamine, uas yog tsim thaum muaj kev tsis haum tshuaj. Yog li ntawd, nyob rau hauv cov kev tshwm sim hais tias tsis muaj kev kho mob tshwm sim ntawm kev tsis haum tshuaj nyob rau hauv ib tug neeg, ces cov tshuaj no yuav tsum tsis txhob noj rau kev tiv thaiv, vim hais tias lawv tsuas yuav tsis muaj dab tsi tshwm sim. Cov tshuaj no yog ib qho ntawm cov laus tshaj plaws hauv kev lag luam tshuaj. Nws yog ib nqi sau cia hais tias thawj ntawm lawv yog synthesized nyob rau hauv lub forties ntawm lub xyoo pua xeem. Niaj hnub no, muaj peb tiam ntawm cov tshuaj no.
