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Sulfonamide tseem hu ua p-aminobenzene sulfonamide, p-aniline sulfonamide, p-sulfonamide aniline, thiab nws cov mis mos molecular yog C6H8N2O2S. Nws yog cov hmoov dawb lossis hmoov siv lead ua, tsis muaj ntxhiab, nrog qhov iab me ntsis. Nws tuaj yeem siv los npaj cov kua nplaum tshuaj sulfa rau kev siv sab nraud thiab tiv thaiv kev mob, thiab nws tseem yog cov khoom siv tseem ceeb rau kev sib xyaw ntawm tshuaj sulfa.
Yog koj noj khoom noj siv mis, Ballya tseem tuaj yeem ua a kev ntsuam xyuas sulfonamides los qhia koj yog tias muaj sulfonamides seem hauv lawv.
Sulfonamides (SAs) yog cov lus dav dav rau chav kawm ntawm cov tshuaj nrog p-aminobenzenesulfonamide tus qauv, thiab yog chav kawm tshuaj siv tshuaj kho mob los tiv thaiv thiab kho kab mob sib kis. Sulfonamides yog hom tshuaj tua kab mob uas nquag siv hauv cov tshuaj niaj hnub no. Lawv muaj cov tshuaj tua kab mob dav, tuaj yeem noj tau ntawm qhov ncauj, thiab nqus tau sai. Qee cov sulfonamides (xws li sulfadiazine, SD) tuaj yeem nkag mus rau cov kua dej hauv lub cev los ntawm cov ntshav-hlwb teeb meem, uas muaj kev ruaj khov, thiab tsis yooj yim dua.
Sulfonamide tau muab coj los ua ib nrab ntawm azo dyes thaum ntxov li xyoo 1908. Xyoo 1932, tus kws tshawb fawb German K. Mitch tau tsim cov tshuaj azo liab liab Bailangduoxin; Txij xyoo 1932 txog 1935, G. Domark pom tias nws muaj cov tshuaj kho tau zoo ntawm qee yam kab mob hauv cov tsiaj sim. Tom qab qhov kev tshawb pom lub sijhawm no tau luam tawm xyoo 1935, nws ua rau muaj kev nkag siab zoo hauv ntiaj teb tshuaj. Xyoo 1939, Domak yeej qhov khoom plig Nobel hauv Physiology thiab Tshuaj rau kev txhim kho ntawm Pua pua Wave. Tsis ntev, tus kws tshawb fawb Fab Kis txoj kev tshawb fawb tau hais meej tias cov tshuaj tua kab mob ntawm Bailangduoxi yog vim sulfonamide tsim los ntawm nws cov metabolism hauv cov tsiaj lub cev.
Txhawm rau nthuav dav cov tshuaj tua kab mob ntawm sulfa thiab txhim kho nws cov tshuaj tua kab mob, cov kws tshawb fawb hauv Tebchaws Europe thiab Tebchaws Meskas tau hloov kho nws cov qauv hauv ntau txoj hauv kev, sib sau ua ke ntau txhiab leej. sulfa sib xyaw (raws li txheeb cais hauv xyoo 1945, ntau dua 5,000), thiab xaiv 30 ntawm lawv. Ntau yam tshuaj sulfa uas muaj txiaj ntsig zoo thiab muaj tshuaj lom tsawg, xws li: pyridoxine, sulfadiazine (SP), sulfadiazine (SD), phthaloyl sulfathiazole (PST), sulfathiazole (ST), sulfamidine (SG), Sulfaisoxazole (SIZ), Sulfamethazine ( SM2) raug tsim tawm.
Tom qab qhov tshwm sim ntawm tshuaj penicillin thiab lwm yam tshuaj tua kab mob, vim lawv cov tshuaj tiv thaiv kab mob siab dua, kev siv tshuaj sulfa tau cuam tshuam. Txawm li cas los xij, tshuaj sulfa muaj qhov zoo ntawm cov khoom ruaj khov, tsim khoom yooj yim, tus nqi qis, noj tau yooj yim, thiab lwm yam, yog li lawv ib txwm ua lub luag haujlwm tseem ceeb hauv cov tshuaj tua kab mob.
Xyoo 1956, thawj qhov ua yeeb yam ntev sulfa tshuaj uas tuaj yeem noj ib hnub ib zaug, sulfamethoxine (3-sulfa-6-methoxypyridazine), ua rau muaj kev txhim kho tshiab hauv kev thov tshuaj sulfa. Tom qab ntawd, qee qhov ua haujlwm nruab nrab sulfadiazines, xws li sulfamethoxazole, lossis sulfadiazine (SMZ), uas tau noj ob zaug ib hnub, tau tshwm sim, thiab qhov ua haujlwm nruab nrab ntawm sulfadiazine tau hais meej. Ib qho ntxiv, ob yam kev ua yeeb yam ntev-ntev tau pom: 2-sulfa-3-methoxypyrazine (nws tuaj yeem noj ib zaug txhua 2 rau 3 hnub), 2-sulfa-5,6-dimethoxypyrimidine (nws tau noj ib zaug ib lub lim tiam, Yog li ntawd, nws hu ua sulfadoxine).
Xyoo 1960, cov tshuaj tua kab mob sib xyaw ua ke trimethoprim (TMP) tau tshawb pom, uas tuaj yeem txhim kho cov tshuaj tua kab mob ntawm sulfa tshuaj los ntawm ob peb zaug mus rau kaum ob zaug, thiab nthuav dav cov tshuaj tua kab mob, uas ntxiv dag zog rau kev kho mob ntawm tshuaj sulfa. Cov khoom siv dav tshaj plaws hauv kev kho mob yog sulfadiazine, dipyrimidine (SD+TMP), sulfamethoxazole, sib xyaw trimethoprim (SMZ+TMP), thiab sulfamethazine.
Ib qho ntxiv, hauv daim ntawv thov kho mob ntawm tshuaj sulfa, qee hom tsiaj tau pom los tiv thaiv carbonic anhydrase, thiab qee qhov muaj kev phiv los ntawm kev txo cov ntshav qab zib. Tom qab cov txheej txheem sib xyaw ua ke thiab tshuaj xyuas, sulfa diuretics sawv cev los ntawm tshuaj hydrochlorothiazide thiab sulfonamide qhov ncauj hypoglycemic tshuaj sawv cev los ntawm tolbutamide tau tsim thaum kawg.
Nws yog chav kawm ntawm cov tshuaj sib txuas tshuaj uas muaj cov tshuaj tua kab mob thiab yog cov tshuaj p-aminobenzenesulfonamide (sau ua sulfonamide). Sulfonamides yog cov tshuaj bacteriostatic, uas txwv kev loj hlob thiab kev tsim cov kab mob los ntawm kev cuam tshuam nrog kev zom zaub mov ntawm cov kab mob folate. Tsis zoo li tib neeg thiab tsiaj txhu tsiaj, cov kab mob uas nkag siab rau cov tshuaj sulfa tsis tuaj yeem siv folic acid ncaj qha hauv ib puag ncig ib puag ncig.
Lawv tsuas tuaj yeem siv p-aminobenzoic acid (PABA) thiab dihydropteridine, uas yog catalyzed los ntawm dihydrofolate synthase hauv cov kab mob. Dihydrofolate tau muab coj los ua ke, thiab tom qab ntawd tetrahydrofolate tau tsim los ntawm kev txiav txim ntawm dihydrofolate reductase. Daim ntawv ua haujlwm ntawm tetrahydrofolate yog hloov lub cev ntawm ib chav tsev carbon, uas ua lub luag haujlwm tseem ceeb hauv kev tsim cov purine thiab pyrimidine nucleotides. Cov qauv ntawm cov tshuaj sulfa zoo ib yam li p-aminobenzoic acid, yog li nws tuaj yeem sib tw nrog p-aminobenzoic acid rau dihydrofolate synthase thiab cuam tshuam rau kev sib xyaw ntawm dihydrofolate, yog li cuam tshuam rau kev tsim cov nucleic acid thiab cuam tshuam kev loj hlob thiab rov ua dua ntawm cov kab mob.
Cov tshuaj sulfonamide feem ntau yog dawb los yog me ntsis daj crystalline hmoov, uas yooj yim zuj zus thaum raug rau lub teeb pom ib tsos tsaus tsawv. Feem ntau ntawm cov tshuaj no muaj qhov ua tau qis heev hauv cov dej thiab muaj qhov sib xyaw tau yooj yim hauv dilk alkali, tab sis lawv yooj yim soluble hauv dej tom qab tsim sodium ntsev, thiab nws cov kua dej muaj zog alkaline.
Tom qab rov sib cuag ntawm cov kab mob thiab tshuaj, qhov ua rau cov tshuaj txo qis lossis txawm tias ploj mus. Cov kab mob muaj peev xwm tiv taus cov tshuaj sulfa, tshwj xeeb tshaj yog thaum qhov ntau npaum lossis kev kho mob tsis txaus. Qhov ua rau cov tshuaj tiv thaiv tuaj yeem yog cov kab mob hloov pauv cov txheej txheem hauv metabolic, xws li tsim ntau dihydrofolate synthase, lossis siv ncaj qha folic acid nyob ib puag ncig. Cov kab mob hauv plab feem ntau kis los ntawm kev hloov pauv ntawm R factor.
Thaum ua ke nrog cov tshuaj tua kab mob sib xyaw ua ke, nws tuaj yeem txo lossis ncua qhov pib ntawm kev tiv thaiv tshuaj. Cov kab mob muaj kev tiv thaiv hla mus rau ntau yam tshuaj sulfa, uas yog, tom qab cov kab mob txhim kho kev tiv thaiv rau ib qho tshuaj sulfa, lawv kuj tuaj yeem ua haujlwm txawm tias muaj lwm cov tshuaj sulfa. Tab sis tsis muaj kev tiv thaiv hla nrog lwm cov tshuaj tua kab mob.
Cov chav kawm ntawm cov tshuaj no tuaj yeem nqus tau tom qab kev tswj hwm qhov ncauj, tab sis cov ntshav plasma ntawm cov tshuaj nyob rau lwm lub sijhawm. Raws li nws t1/2, nws tuaj yeem faib ua peb pawg: ua luv luv sulfonamides (t1/2 txog 6 teev), ua haujlwm nruab nrab sulfonamides (t1/2 ze rau 12 teev) thiab ua haujlwm ntev sulfonamides (t1/2) ntau tshaj 24 teev). Tam sim no, daim ntawv thov kho mob tseem ceeb yog ua haujlwm nruab nrab sulfamethoxazole (SMZ) thiab sulfadiazine (SD). Lwm tus tau siv me ntsis.
Hom sulfonamides no nqus tau tsis zoo tom qab kev tswj hwm qhov ncauj, thiab feem ntau ua rau muaj cov kab mob bacteriostatic hauv cov hnyuv. Muaj sulfaguanidine (SG), succinthiazole (SST), phthalosulfothiazole (PST), thiab phthalosulfonamide (siramide, PSA) Tos.
Sulfasalazine tsis tau nqus qhov ncauj, muaj qhov tshwj xeeb zoo rau cov ntaub so ntswg sib txuas, thiab tso tawm sulfapyridine los ntawm cov nqaij sib txuas ntawm cov phab ntsa hauv plab txhawm rau qhib cov tshuaj tua kab mob, tiv thaiv kev mob thiab tiv thaiv kev tiv thaiv. Nws yog qhov muaj txiaj ntsig zoo rau kev kho mob uas tsis yog yam tshwj xeeb. Vim yog txoj kev kho mob ntev, cov tsos mob xws li xeev siab, ntuav, tawv nqaij ua xua thiab ua npaws ua npaws yuav tshwm sim.
feem ntau suav nrog sulfacetamide sodium (SA: SC-Na), methanesulfadiazine (SML), thiab nyiaj sulfadiazine (SD-Ag).
Txij li cov tshuaj sulfa yog cov tshuaj tua kab mob ntau dua li kev ua kom tsis muaj menyuam, yog li yog kom ntseeg tau tias muaj cov tshuaj tua kab mob ntawm cov tshuaj sulfa, cov ntshav muaj txiaj ntsig zoo yuav tsum tau tswj kom ntev txaus.
Cov tshuaj hauv qhov ncauj sulfa feem ntau yog nqus rau hauv txoj hnyuv, thiab cov ntshav ntshav nce mus txog qhov siab tshaj hauv 4 txog 6 teev. Tom qab nqus tau, cov tshuaj tau faib rau hauv ntau cov ntaub so ntswg ntawm lub cev, nrog cov ntsiab lus siab tshaj plaws hauv ntshav, daim siab, thiab lub raum. Feem ntau cov tshuaj sulfa tuaj yeem nkag mus rau hauv cov kua dej hauv hlwb. Tom qab cov tshuaj tau nqus mus rau hauv cov ntshav, feem ntau ntawm nws tau ua ke nrog cov ntshav ntshav.
Cov tshuaj sulfa ua ke ib ntus poob nws cov tshuaj tua kab mob, tsis tuaj yeem nkag mus rau hauv cov kua dej hauv lub paj hlwb, thiab tsis tuaj yeem hloov pauv los ntawm daim siab thiab tso tawm los ntawm lub raum. Tab sis kev sib xyaw ua ke yog qhov xoob, thiab muaj qhov tso me me los ntawm lub sijhawm, yog li nws tsis cuam tshuam rau kev ua tau zoo. Kev ua yeeb yam ntev sulfonamides muaj qib siab rau cov ntshav protein, yog li lawv tuaj yeem tswj tau lub cev ntev. Sulfonamides tseem tuaj yeem nkag mus rau hauv qhov mob ua paug thiab lwm yam dej ntws tawm, thiab nkag mus rau hauv menyuam hauv plab los ntawm txoj hlab ntshav, yog li cov poj niam cev xeeb tub yuav tsum tau ceev faj thaum siv tshuaj sulfa.
Sulfonamides feem ntau yog metabolized hauv lub siab, qee qhov ua ke nrog glucuronic acid thiab ua tsis tau zoo, thiab qee qhov ntawm lawv dhau los ua acetylated sulfonamides los ntawm acetylation. Tom qab acetylation ntawm sulfonamides, qhov ua kom poob qis, tshwj xeeb tshaj yog nyob rau hauv cov kua qaub. Nws yog ib qho yooj yim uas yuav ua rau cov kua hauv cov zis thiab ua rau lub raum puas. Qib ntawm acetylation ntawm ntau yam tshuaj sulfa sib txawv.
Lub cev tseem ceeb ntawm cov tshuaj sulfa (tshwj tsis yog cov uas nyuaj rau nqus) yog lub raum. Nws tau tso tawm hauv cov zis raws li tus qauv thiab acetylated sulfonamide thiab me me ntawm glucuronic acid conjugate. Ib feem ntawm nws yog tawm los ntawm cov kua tsib thiab cov hnyuv, thiab rov nqus los ntawm daim siab thiab hnyuv.
Cov tshuaj Sulfa uas nyuaj rau nqus tsis tshua muaj tshwm sim tsis zoo. Qhov tshwm sim ntawm kev yooj yim nqus cov kev phiv tshuaj yog li 5%.
Feem ntau suav nrog ua pob ua pob thiab ua npaws ua npaws. Feem ntau nws tshwm sim 5 txog 9 hnub tom qab siv tshuaj, tshwj xeeb yog hauv menyuam yaus. Muaj kev ua xua sib txawv ntawm cov tshuaj sulfa, yog li thaum tus neeg mob ua xua rau ib yam tshuaj sulfa, nws tsis muaj kev nyab xeeb hloov mus rau lwm cov tshuaj sulfa. Thaum muaj kev tsis haum tshuaj tshwm sim, cov tshuaj yuav tsum nres tam sim ntawd. Cov tshuaj sulfa uas ua haujlwm ntev muaj tus lej siab rau cov ntshav protein, thiab tseem muaj cov tshuaj tib neeg nyob hauv cov ntshav ob peb hnub tom qab siv tshuaj, yog li lawv txaus ntshai heev.
Vim tias qhov txo qis ntawm acetylsulfonamide, tshwj xeeb tshaj yog thaum cov zis muaj kua qaub, muaju tau yooj yim ua rau cov kua hauv lub raum, ua rau muaj cov tsos mob xws li hematuria, dysuria, thiab tso zis tso zis. Txhawm rau tiv thaiv qhov tshwm sim ntawm cov tshuaj lom lom no, cov ntsuas hauv qab no tuaj yeem tiv thaiv: ntxiv bicarbonate lossis citrate kom alkalinize cov zis thiab nce qhov kev tso tawm ntawm qhov tso tawm; haus dej ntau tuaj yeem ua rau tso zis ntau ntxiv thiab tseem txo qhov tso tawm kom pom meej; cov neeg laus thiab cov uas muaj lub raum tsis zoo yuav tsum tau siv nrog ceev faj.
Sulfonamides tuaj yeem tiv thaiv kev tsim cov pob txha pob txha pob txha dawb thiab ua rau muaj leukopenia. Qee zaum tsis muaj granulocytes tuaj yeem pom thiab yuav rov zoo tom qab siv tshuaj. Kev siv tshuaj sulfa ntev yuav tsum kuaj ntshav. Kev tsis txaus ntawm cov piam thaj 6-phosphate dehydrogenase tuaj yeem ua rau hemolytic anemia. Sulfonamides tuaj yeem nkag mus rau hauv menyuam hauv plab los ntawm leej niam thiab sib tw nrog bilirubin pub dawb rau cov ntshav ntshav khi cov chaw, ua rau muaj kev nkag siab ntau ntxiv ntawm bilirubin dawb thiab ua rau kernicterus. Nws tsis haum rau cov poj niam cev xeeb tub, cov menyuam yug tshiab, tshwj xeeb yog menyuam mos ntxov.
Cov tsos mob no feem ntau yog los ntawm cov tshuaj sulfa ntau tshaj.
Sulfanilamide tshuaj muaj lawv tus kheej qhov txiaj ntsig zoo dua li tshuaj tua kab mob, tab sis thaum cov kab mob txhim kho kev tiv thaiv, txhua yam tshuaj sulfanilamide ua tsis tau zoo. Ib qho ntxiv, koj yuav tsum ua raws kws kho mob cov lus qhia thaum koj xav tau siv cov tshuaj zoo li no.
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