Tam sim no sijhawm rau ntshav qab zib noj cov tshuaj sulfonamide muaj suab thaj hauv nruab nrab thiab cov tshuaj noj loj loj yog siv. Lawv tshwj xeeb tshaj yog nyob rau hauv cov neeg laus cov neeg mob uas cuam tshuam mus rau kev puv. Nws muaj peev xwm siv cov tshuaj sulfonamide ua ke nrog kev txhaj tshuaj insulin hauv kev mob ntshav qab zib mellitus hauv cov tub ntxhais hluas kom txo qis cov tshuaj insulin. Thaum insulin-tiv thaiv cov ntaub ntawv ntawm cov ntshav qab zib mellitus, kev siv sulfanilamide npaj rau qee qhov xwm txheej ua rau muaj txiaj ntsig zoo, muaj zog ua kom muaj kev cuam tshuam ntawm insulin thiab tshem tawm cov txiaj ntsig ntawm qhov cuam tshuam-insulin thiab insulin inhibitors. Hauv cov menyuam yaus thiab tub ntxhais hluas mob ntshav qab zib mellitus nyob rau hauv rooj plaub ntawm cov tsis txaus insulin, qab zib-txo cov tshuaj sulfonamide tsis muaj txiaj ntsig.
Cov kev xav tsis zoo ntawv cov piam thaj txo qis sulfanilamide tshuaj muaj feem me me, tab sis qee qhov, txo qis cov qe ntshav dawb, platelets thiab neutrophils tuaj yeem pom hauv cov ntshav.

Qee qhov mob nco ntsoov cov tsos ntawm xeev siab. Ua xua tuaj yeem ua tau. Kev siv cov tshuaj sulfonamide uas muaj suab thaj txo qis yog ua rau muaj menyuam hauv plab thiab menyuam thaum ntxov, nrog rau lub raum ua rau lub raum puas thiab mob ntsws. Hauv cov hluas thiab cov hluas, exacerbation ntawm cov suab thaj nyhuv ntawm STH. Hauv cov rooj plaub no, cov tshuaj sulfonamide uas muaj suab thaj txo qis tuaj yeem pab txo qis hyperglycemia thiab tuaj yeem ua ke nrog kev npaj tshuaj insulin.

Tam sim no yog muab cov lus qhia hauv qab zib-txo cov sulfanilamide: BZ-55 (padisan, oranil, inepol, carbutamide, glucidoral, bukarban), D-860 (rastinone, tolbutamide, butamide, artosin, orinase, orabet, dolipol, thiab lwm yam).

Tam sim no ntau heev kev tshawb nrhiav nws tau pom tias BZ-55 (nadizan thiab nws cov analogues) muaj cov suab thaj txig txo qis dua piv rau cov tshuaj ntawm D-860 pawg. Txawm li cas los xij, cov tshuaj ntawm D-860 pawg (rastinone thiab nws cov analogues) tsis muaj tshuaj lom tsawg.

Cov piam thaj txo qis cov tshuaj sulfa teem sijhawm 0.5 g 1-2-3 zaug ib hnub. Koj tuaj yeem nce lub koob rau 3 g nyob rau ib hnub. Tab sis nws yog qhov zoo dua rau kev txhawm rau kom tsis txhob mob me ntsis txhawm rau txhawm rau zam kom tsis txhob muaj cov nyhuv tshuaj lom.
Cov tshuaj r-607 (chlorpropamide, diabenesis, oradian) yog siv hauv 250 mg ntsiav tshuaj. Qhov nruab nrab txhua hnub koob ntawm 250-500 mg. Cov tshuaj r-607 yog qhov feem ntau sib piv hauv kev sib piv nrog lwm cov kua qab zib thiab sulfonamide.

Cyclamide (K-386) nyob rau hauv nws cov qauv hauv paus sawv ze ze rau tolbutamide (D-860).
Txog kev tswj hwm qhov ncauj kho ntshav qab zib biguanides yog siv, uas los ntawm cov qauv hauv tshuaj lom neeg tuaj yeem muab faib ua peb pawg: phenethylbiguanides (DWI, phenformin, dibotin), butylbiguanides (silubin, buformip, adebite) thiab dimethylbiguanides glucofage, metformin). DVVI muaj nyob rau hauv 25 mg ntsiav tshuaj, qhov koob tshuaj txhua hnub yog 125 mg, koob tshuaj txhua hnub ntau tshaj yog 150 mg. Glucophage yog dosed hauv ntsiav tshuaj ntawm 0.5 g 2-3 zaug ib hnub. Qhov koob tshuaj siab tshaj txhua hnub ntawm 3 g.

Tshuaj butylbiguanide (silubin) yog dosed hauv ntsiav tshuaj ntawm 50 mg. Cov koob tshuaj txhua hnub ntawm 150 mg. Qhov koob tshuaj ntau tshaj txhua hnub yog 300 mg. Cov tshuaj noj ntawm cov tshuaj silubin yog cov tshuaj Hungary adebit. Tam sim no, hauv tebchaws Askiv, kev npaj ntev silubin tau txais - rau 24 teev (Silubin retard).

Kev Loj Loj ua rau cov ntshav qog ua kom qis, ua kom muaj zog ntawm cov tshuaj insulin. Ua kom cov piam thaj muaj kev nkag siab los ntawm cov ntaub so ntswg. Ua kom cov ntsiab lus ntawm lactic thiab pyruvic acid nyob rau hauv cov ntshav nrog kev qhia txog cov piam thaj thiab txo cov gluconeogenesis. Ntxiv rau, biguanides txhim kho oxidative phosphorylation hauv cell mitochondria. Muaj cov kev soj ntsuam pom tias cov khoom noj loj hauv cov neeg mob ntshav qab zib, nquag rog, txo cov insulin tso tawm ntau dhau, txo qhov qab los noj mov, thiab txhawb kom poob phaus. Nyob rau hauv kev sib piv rau cov piam thaj-txo sulfanilamide kev npaj, biguanides muaj txiaj ntsig zoo rau cov hluas thiab ntshav qab zib thaum me nyuam yaus thaum kev tsim cov tshuaj endogenous insulin yog txo qis.

Toxic nyhuv lojmuas me ntsis, txawm li cas los xij, xeev ntuav, ntuav, mob hauv thaj tsam epigastric tau pom. Qee tus neeg mob uas siv sijhawm ntev bnguanides sau txog qhov tsis muaj zog, poob phaus. Kev sib xyaw ua ke nrog cov tshuaj insulin pab ua kom cov metabolism hauv kev ua haujlwm. Bnguanide kev npaj ua ke nrog cov suab thaj txo qis sulfanilamide muab cov txiaj ntsig zoo hauv insulin-resistant cov ntshav qab zib.

Tsom ntsoov rau hauv kev kho mob retinopathy yuav tsum tsom rau kev them nyiaj mob ntshav qab zib. Kev npaj tshuaj anabolic steroid yog kev pom zoo, kev kho mob vitamin, lidase txhim kho permeability ntawm cov hlab ntshav, tab sis tsis pom zoo nyob rau hauv muaj cov hemorrhages. Hauv cov xwm txheej no, calcium chloride, rutin, thiab vicalin tau qhia. Hauv qhov muaj ntshav qab zib ua kom rov ua mob ntshav siab thiab mob ntshav siab, txo qis hauv ntshav siab nrog cov tshuaj antihypertensive yog qhia.

Nrog ntshav qab zib nephropathy Nws yog qhov nyuaj rau kev them rov qab rau cov ntshav qab zib, vim qhov tseem yuav muaj cov ntshav qog ntshav. Qhov kev coj ua ntawm kev txhaj tshuaj me me ntawm cov tshuaj insulin, muab fractionally, yog ua raws cov theem ntawm cov piam thaj hauv ntshav, vim tias tsis muaj suab thaj hauv kev kuaj zis. Hauv kev noj zaub mov, nws yog ib qho tsim nyog yuav tsum tau txwv ntsev, rog, nqaij yuav tsum tau muab rhaub. Txhawm rau txhim kho cov protein synthesis, cov tshuaj anabolic steroid (nerabol, retabolil, thiab lwm yam) tau sau tseg. Thaum uremia, mob plab zom mov, oxygen, ntshav ntxiv, thiab cov tshuaj plob plawv tau siv.

Hauv kev kho mob polyneuritis Kev pom zoo tawm dag zog, zaws, tawm dag zog lub cev yog kev pom zoo. Kev tsim nyog los ntawm kev siv tshuaj insulin, kev kho tshuaj vitamin (complex B1, B6, B12, thiab C) txhim kho cov neeg mob.

Puas yog sulfonamides tshuaj tua kab mob los yog tsis?

Yog lawm, sulfonamides yog cais pawg ntawm cov tshuaj tua kab mob, txawm hais tias thaum pib, tom qab kev tsim tawm ntawm penicillin, lawv tsis muaj nyob rau hauv kev faib tawm. Tau ntev, tsuas yog cov ntuj lossis ib nrab hluavtaws sib txuas tau suav hais tias yog "tiag tiag", thiab thawj cov sulfonamide thiab nws cov lus qhia raug coj los ua ke los ntawm cov thee tar tsis yog xws li. Tab sis tom qab ntawd qhov xwm txheej tau hloov pauv.

Niaj hnub no sulfonamides yog ib pawg loj ntawm cov tshuaj tua kab mob ntawm bacteriostatic kev txiav txim siab, nquag tawm tsam ntau ntawm cov kab mob ntawm cov kis thiab mob. Ua ntej lawm, cov tshuaj tua kab mob sulfonamide siv feem ntau ntawm cov tshuaj. Tab sis dhau sijhawm, lawv feem ntau tau poob lawv qhov tseem ceeb vim kev hloov pauv thiab kev tawm tsam ntawm cov kab mob, thiab niaj hnub no, cov kab mob sib xyaw ua ke tau siv ntau dua rau cov hom phiaj kho.

Kev faib tawm sulfonamides

Nws yog qhov tseem ceeb tshaj plaws tias cov tshuaj sulfonamide tau tshawb pom thiab tau pib siv rau cov tshuaj muaj txiaj ntsig ntau dua li ntxov ntawm penicillin. Qhov ua kom zoo rau kev kho qee yam kev lag luam (tshwj xeeb, hais tawm lossis "liab ploog") tau tshwm sim los ntawm tus kws kho mob German tus kws tua kab mob Gerhard Domagk hauv xyoo 1934. Ua tsaug rau qhov kev sib tw no, nquag tawm tsam streptococci, nws kho nws tus ntxhais, thiab nyob rau xyoo 1939 nws tau rais los ua tus muaj npe hu ua Nobel Awardreven.

Qhov tseeb hais tias cov kab mob bacteriostatic muaj txiaj ntsig tsis yog los ntawm qhov tsis zoo ntawm cov qauv tshaj tawm, tab sis los ntawm aminobenzenesulfamide (aka "dawb streptocide" thiab cov tshuaj yooj yim tshaj plaws hauv cov pab pawg sulfonamides) tau tshawb pom xyoo 1935. Nws tau dhau los ntawm nws txoj kev hloov kho uas txhua qhov kev npaj ntawm chav kawm tau muab coj los ua ke yav tom ntej, ntau yam ntawm uas tau dav siv hauv tshuaj thiab kho tsiaj. Muaj qhov zoo sib xws ntawm cov tshuaj tiv thaiv kev ua kom ua haujlwm, lawv sib txawv hauv cov qauv pharmacokinetic.

Qee cov tshuaj ua kom nrawm nrawm thiab faib tawm, thaum lwm cov nqus tau ntev dua. Muaj qhov sib txawv ntawm lub sijhawm ua los ntawm kev tawm ntawm lub cev, vim hais tias cov hom ntawm cov sulfonamides li nram no:

• Kev ua yeeb yam luv luv, ib nrab-lub neej ntawm uas tsawg dua 10 teev (streptocid, sulfadimidine).
• Sij Hawm Nruab Nrab, uas nws T 1 /₂10-24 teev - sulfadiazine, sulfamethoxazole.
• Kev ncua sijhawm ntev (T ib nrab-lub neej ntawm 1 txog 2 hnub) - sulfadimethoxin, sulfonomethoxin.
• Superlong - sulfadoxine, sulfamethoxypyridazine, sulfalene - uas yog cov tawm ntev dua 48 teev.

Qhov kev faib tawm no yog siv rau cov tshuaj hauv qhov ncauj, txawm li cas los xij, muaj cov sulfanilamides uas tsis yog adsorbed los ntawm kev mob plab (phthalyl sulfathiazole, sulfaguanidine), thiab kuj muaj nyiaj sulfadiazine npaj tshwj xeeb rau kev siv tshuaj pleev.

Ua tiav cov npe ntawm sulfanilamide npaj

Cov npe ntawm cov tshuaj tua kab mob sulfanilamide siv rau hauv cov tshuaj niaj hnub nrog cov npe lag luam thiab cov ntsiab lus ntawm daim ntawv tso tawm yog nthuav tawm hauv lub rooj:

Txhua cov tshuaj tua kabmob sulfonamide los ntawm cov npe tshuaj muaj tam sim no. Qee qhov chaw hais txog lwm cov tshuaj ntawm pab pawg no (piv txwv li Urosulfan), uas tau muab ncua ntev. Tsis tas li ntawd, muaj cov tshuaj sulfanilamide siv tshwj xeeb hauv kev kho tsiaj.

Lub tshuab ntawm kev txiav txim ntawm sulfonamides

Tiv thaiv kev loj hlob ntawm cov kab mob pathogens (cov kab mob gram-negative thiab gram-zoo, qee qhov protozoa) yog vim muaj qhov sib xws ntawm cov qauv tshuaj ntawm para-aminobenzoic acid thiab sulfonamide. PABA yog qhov tsim nyog rau lub xov tooj ntawm tes los ua ke ib qho tseem ceeb tshaj plaws ntawm kev txhim kho - folate thiab dihydrofolate. Txawm li cas los xij, thaum nws cov lwg me pauv los hloov cov qauv sulfanilamide, cov txheej txheem no tau cuam tshuam thiab kev loj hlob ntawm cov kab mob nres.

Tag nrho cov tshuaj thawm hauv lub zom zaws nrog cov khoom sib txawv thiab ntau qib ntawm kev nqus. Cov uas tsis tau adsorbed nyob rau hauv txoj hnyuv tau qhia rau kev kho mob ntawm txoj hnyuv. Kev faib tawm cov ntaub so ntswg yog qhov ncaj ncees, cov metabolism yog nqa tawm hauv daim siab, nthuav tawm - feem ntau dhau los ntawm ob lub raum. Nyob rau tib lub sijhawm, depot sulfonamides (ua yeeb yam ntev thiab ntev ntev) tau nqus rov qab rau hauv cov hlab plawv, uas piav qhia txog lub neej ntev ib nrab.

Kev taw qhia rau kev siv sulfonamides

Tiv thaiv kev loj hlob ntawm cov kab mob pathogens (cov kab mob gram-negative thiab gram-zoo, qee qhov protozoa) yog vim muaj qhov sib xws ntawm cov qauv tshuaj ntawm para-aminobenzoic acid thiab sulfonamide. PABA yog qhov tsim nyog rau lub xov tooj ntawm tes los ua ke ib qho tseem ceeb tshaj plaws ntawm kev txhim kho - folate thiab dihydrofolate. Txawm li cas los xij, thaum nws cov lwg me pauv los hloov cov qauv sulfanilamide, cov txheej txheem no tau cuam tshuam thiab kev loj hlob ntawm cov kab mob nres.

Tag nrho cov tshuaj thawm hauv lub zom zaws nrog cov khoom sib txawv thiab ntau qib ntawm kev nqus. Cov uas tsis tau adsorbed nyob rau hauv txoj hnyuv tau qhia rau kev kho mob ntawm txoj hnyuv. Kev faib tawm cov ntaub so ntswg yog qhov ncaj ncees, cov metabolism yog nqa tawm hauv daim siab, nthuav tawm - feem ntau dhau los ntawm ob lub raum. Nyob rau tib lub sijhawm, depot sulfonamides (ua yeeb yam ntev thiab ntev ntev) tau nqus rov qab rau hauv cov hlab plawv, uas piav qhia txog lub neej ntev ib nrab.

Ua xua rau sulfonamides

Qib siab ntawm allergenicity ntawm kev sib xyaw ua ke sulfanilamide yog qhov teeb meem tseem ceeb ntawm lawv txoj kev siv. Qhov tshwj xeeb nyuaj hauv qhov no yog kev kho tus mob ntsws pneumocystis hauv cov neeg muaj tus kabmob HIV, vim tias Biseptol yog siv tshuaj rau xaiv rau lawv. Txawm li cas los xij, nws yog nyob rau hauv pawg no ntawm cov neeg mob uas qhov ntxim nyiam ntawm kev tsim kev tsis haum tshuaj rau kev sib koom tes co-trimoxazole nce kaum npaug.

Vim li no, nrog rau kev fab tshuaj rau sulfanilamides, Biseptol thiab lwm yam kev sib xyaw ua ke raws li kev sib koom tes co-trimoxazole yog contraindicated rau tus neeg mob. Intolerance feem ntau tshwm sim los ntawm kev tawm pob me me, kub taub hau kuj yuav tshwm sim, thiab cov lus sib xyaw ntawm cov ntshav (neutro- thiab thrombocytopenia) yuav hloov. Hauv cov teeb meem tshwj xeeb tshaj yog - Lyell thiab Stevens-Johnson syndromes, erythema multiforme, anaphylactic shock, Quincke's edema.

Kev fab tshuaj rau sulfonamides yuav tsum muaj kev tshem tawm cov tshuaj uas ua rau nws, nrog rau kev siv tshuaj tiv thaiv kev ua xua.

Lwm yam phiv los ntawm sulfonamides

Ntau cov tshuaj ntawm cov pab pawg no lom thiab ua tsis tau zoo, uas yog cov laj thawj rau kev txo qis hauv lawv txoj kev siv tom qab nrhiav tau ntawm penicillin. Ntxiv rau kev ua xua, lawv tuaj yeem ua rau mob dyspeptic, mob taub hau thiab mob plab, mob plab, mob hnoos qeev, mob hlab ntshav, mob ntsws, mob txha nqaj qaum, mob polyuria, mob raum tsis ua haujlwm, mob hlwb nephropathy, myalgia thiab arthralgia. Ntxiv rau, qhov kev pheej hmoo ntawm kev txhim kho crystalluria nce, yog li koj yuav tsum tau haus tshuaj ntau thiab haus dej ntau alkaline.

Kev cuam tshuam nrog lwm yam tshuaj

Tsis pom tus ntoo khaub lig-tiv thaiv nrog lwm cov tshuaj tua kab mob hauv sulfonamides. Thaum ua ke nrog cov tshuaj tiv thaiv qhov ncauj hypoglycemic thiab coagulants tsis ncaj, lawv cov nyhuv ua tau zoo dua. Nws tsis pom zoo kom muab cov tshuaj tua kab mob-sulfonamides kuj nrog thiazide diuretics, rifampicin thiab cyclosporine.

Dab tsi yog qhov txawv ntawm sulfonamides thiab sulfonamides

Txawm hais tias tus ntawv sau npe yuav tsum, cov npe tshuaj lom neeg no sib txawv hauv paus. Sulfonamides (code rau ATX C03BA) yog diuretics - tshuaj tso ntshav. Cov tshuaj pab pawg tau muab rau kev mob ntshav siab, puffiness, gestosis, ntshav qab zib insipidus, kev rog thiab lwm yam kab mob nrog los ntawm kev txuam nrog cov kua hauv lub cev.

Sulfonamides

Sulfonamides - antimicrobial derivatives khub (π)-aminobenzenesulfamide - amide ntawm sulfanilic acid (para-aminobenzene sulfonic acid). Ntau yam ntawm cov tshuaj no tau siv cov tshuaj tua kab mob tua neeg txij li ib nrab xyoo nees nkaum. ib nkawm niam txiv-Aminobenzenesulfamide - chav sib txig yooj yim tshaj plaws - tseem hu ua dawb streptocide thiab tseem siv tshuaj. Kev nkag siab me ntsis hauv cov qauv, sulfonamide pronosil (liab streptocide) yog thawj qhov tshuaj nyob hauv pawg no thiab, feem ntau, thawj cov tshuaj tua kab mob tua kab mob hauv ntiaj teb.

Xyoo 1934, G. pom cov khoom muaj zog tua kab mob.Domagk. Xyoo 1935, cov kws tshawb fawb ntawm Pasteur lub koom haum (Fabkis) pom tias nws yog sulfanilamide feem ntawm cov lwg me uas muaj cov tshuaj tua kab mob, thiab tsis yog cov qauv uas muab nws cov xim. Nws tau pom tias "txoj hauv kev ua haujlwm" ntawm liab streptocide yog sulfanilamide, uas tau tsim thaum lub cev metabolism (streptocide, dawb streptocide). Kev tawm tsam liab tau ploj mus siv, thiab raws li ntawm sulfanilamide molecule, ntau ntawm nws cov txhais tau raug coj los ua ke, ntawm qee qhov tau siv dav hauv tshuaj.

Pharmacological cov tsis muaj

Sulfanilamides ua cov kab mob bacteriostatically, uas yog, lawv muaj cov tshuaj kho mob hauv cov kab mob tshwm sim los ntawm cov kab mob gram-zoo thiab gram-tsis zoo, qee qhov protozoa (pathogens ntawm malaria, toxoplasmosis), chlamydia (nrog mob hnyuv, paratrachoma).

Lawv cov kev ua yog feem ntau cuam tshuam nrog kev ua txhaum ntawm kev tsim los ntawm cov kab mob me me ntawm kev loj hlob yam tsim nyog rau lawv txoj kev loj hlob - folic thiab dihydrofolic acids thiab lwm yam tshuaj, cov molecule ntawm uas suav nrog para-aminobenzoic acid. Lub tshuab kev ntawm kev ua yog txuam nrog cov txheej txheem zoo sib xws ntawm cov sulfanilamide tawg nrog ib nkawm niam txiv-aminobenzoic acid (PABA) - lub zog ntawm cov dihydropteroate synthetase, uas coj cov dihydropteroic acid, uas ua rau kev sib tw inhibition ntawm dihydropteroate synthetase. Qhov no, nyeg, ua rau muaj kev cuam tshuam hauv kev ua ke ntawm dihydropteroic dihydrofolate, thiab tom qab ntawd tetrahydrofolate, thiab raws li qhov ua rau muaj kev cuam tshuam ntawm cov synthesis ntawm nucleic acids hauv cov kab mob.

Yuav kom tau txais kev kho mob kom zoo, lawv yuav tsum yog cov tshuaj kho mob kom txaus kom tiv thaiv tau cov kab mob uas siv cov kab mob para-aminobenzoic acid uas muaj nyob hauv cov ntaub so ntswg. Cov tshuaj sulfonamide tsis txaus los sis tsis kho qhov kev kho thaum ntxov yuav ua rau muaj kev tawm tsam ntawm cov kab mob uas tsis haum rau cov tshuaj sulfonamides ntxiv. Feem ntau cov kab mob tseem ceeb hauv tsev kho mob tam sim no tiv thaiv sulfonamides. Nws yuav tsum tau yug los rau hauv lub siab tias qee cov tshuaj, cov qauv ntawm cov uas suav nrog cov seem ntawm para-aminobenzoic acid (piv txwv li novocaine), tuaj yeem muaj cov nyhuv antisulfanilamide.

Tus nqi tshuaj kho mob kho kom raug |

2.5.2.2. Cov tshuaj Sulfa

Sulfanilamides - cov tshuaj tua kab mob antivicrobial, cov khoom noj ntawm sulfanilic acid amide (dawb streptocide). Lawv qhov kev tshawb pom tau lees paub qhov kev twv ua ntej ntawm P. Ehrlich txog kev xaiv kev puas tsuaj rau cov kab mob me me los ntawm cytotoxic tshuaj ntawm cov txiaj ntsig resorptive. Thawj cov tshuaj ntawm pawg no chob (liab mob ntshav liab) tiv thaiv kev tuag ntawm nas. muaj tus mob heflytic streptococcus tso ib zaug ntawm kaum zaus.

Rau lub hauv paus ntawm sulfanilamide molecule hauv ib nrab xyoo 30s, ntau lwm cov tebchaw tau muab coj los ua ke (norsulfazole, ethazole, sulfazine, sulfacyl, thiab lwm yam). Qhov tshwm sim ntawm cov tshuaj tua kab mob tau txo qis kev txaus siab rau sulfonamides, tab sis lawv tsis tau poob lawv qhov tseem ceeb hauv chaw kho mob, tam sim no lawv tau siv "ua ntev" (sulfapyridazine, sulfalene, thiab lwm yam) thiab tshwj xeeb tshaj yog cov tshuaj sib xyaw (co-trimoxazole thiab nws cov analogues, uas suav nrog trimethoprim ntxiv rau sulfonamide) Cov. Cov tshuaj muaj ntau qhov pom ntawm cov tshuaj tua kabmob (gram-zoo thiab gram-cov kab mob tsis zoo, chlamydia, qee qhov protozoa - pathogens ntawm malaria thiab toxoplasmosis, pathogenic fungi - actinomycetes, thiab lwm yam).

Sulfanilamides tau muab faib ua pawg hauv qab no:

2. Cov tshuaj uas tau xau tag nrho rau hauv txoj hnyuv plab, tab sis maj mam dhau los ntawm lub raum (ua haujlwm ntev): sulfamethoxypyridazine (sulfapyridazine), sulfonomethoxin, sulfadimethoxin, sulfalene.

Cov thawj thiab pawg thib ob, uas tau zoo rau hauv lub plab zom mov, yog siv los kho cov kab mob sib kis, qhov thib peb - ​​rau kev kho mob ntawm txoj hnyuv (cov tshuaj tsis nqus thiab ua rau cov lumen ntawm cov hnyuv), plaub - feem ntau, thiab thib tsib (suav tshuaj sib xyaw nrog trimethoprim) tau zoo ua nrog kev kis kab mob ntawm txoj hlab ua pa thiab mob txeeb zig, mob plab hnyuv.

Mechanism ntawm kev ua. Sulfanilamides ua rau bacteriostasis. Lawv yog cov kev sib tw ntawm kev tawm tsam ntawm para-aminobenzoic acid (PABA), uas tsim nyog rau cov kab mob me me los ua ke cov folic acid: qhov tom kawg hauv coenzyme daim ntawv (dihydrofolate, tetrahydrofolate) koom nrog kev tsim cov purine thiab pyrimidine hauv paus, uas ua kom muaj kev loj hlob thiab kev loj hlob ntawm cov kab mob me. Sulfanilamides nyob ze rau hauv cov qauv tshuaj rau PABA thiab yog li ntawd tau ntes los ntawm cov kab mob me me los ntawm PABA. Raws li qhov tshwm sim, qhov hluavtaws ntawm folic acid nres. Tib neeg lub hlwb tsis muaj peev xwm coj los ua ke cov folic acid (nws los nrog zaub mov), uas qhia txog kev xaiv cov tshuaj tiv thaiv antimicrobial ntawm cov tshuaj no. Sulfanilamides tsis cuam tshuam rau cov kab mob uas lawv tus kheej tsim PABA. Nyob rau ntawm muaj pus, ntshav, cov nqaij rhuav tshem cov khoom uas muaj ntau ntawm PABA, cov tshuaj yuav tsis ua haujlwm. Cov tshuaj uas tsim PABA los ntawm cov tshuaj biotransformation (novocaine, dicaine) yog sulfonamide antagonists.

Cov tshuaj sib xyaw: co-trimoxazole (bactrim, biseptol), sulfatone, uas, ntxiv rau cov tshuaj sulfa (sulfamethoxazole, sulfamonomethoxine), suav nrog trimethoprim, yog cov neeg muaj zog tiv thaiv tua kab mob. Trimethopriminhibiting dihydrofolic acid reductase, nws thaiv nws txoj kev hloov pauv mus rau nquag tetrahydrofolic acid. Yog li no, nrog kev qhia txog kev sib xyaw ua ke sulfanilamide, tsis tsuas yog cov kev sib txuas ntawm cov folic acid yog inhibited, tab sis kuj nws hloov dua siab tshiab rau nquag coenzyme (tetrahydrofolate). Cov tshuaj muaj cov kab mob bactericidal tiv thaiv cov kab mob gram-zoo thiab gram-tsis zoo.

Qhov tseem ceeb ntawm kev tswj hwm ntawm sulfonamides yog los ntawm lub qhov ncauj. Nyob rau hauv txoj hnyuv me, lawv tau nrawm thiab nqus tag nrho (tshwj tsis yog rau cov tshuaj hnyav dua - phthalazole, phthazine, salazosulfanilamides, tshuaj rau cov mob plab hnyuv), khi rau plasma cov protein nyob rau hauv cov ntshav, thiab tom qab ntawd, maj mam tso tawm los ntawm daim ntawv cog lus, pib nthuav tawm cov haujlwm antimicrobial, tsuas yog pub dawb yog antimicrobial feem. Yuav luag txhua qhov sulfonamides kis tau cov ntaub so ntswg zoo, nrog rau hepatohematic, ntshav-hlwb, placental. Lawv yog cov biotransformed hauv daim siab, qee qhov yog zais rau hauv bile (tshwj xeeb tshaj yog cov ua ntev ntev, uas yog li ntawd ntse siv rau cov mob plab biliary).

Txoj kev tseem ceeb ntawm biotransformation ntawm sulfonamides yog acetylation. Acetylated metabolites plam lawv cov kev ua haujlwm tiv thaiv kab mob, yog cov dej tsis zoo, thiab hauv cov kua qaub acid, cov zis tuaj yeem ua rau cov khoom siv ua kom muaj kev puas tsuaj lossis ua rau cov hlaus rov qab los. Yog tias mob txeeb zig, mob sulfonamides, uas yog me ntsis acetylated thiab tawm hauv cov zis ua dawb (urosulfan, etazole).

Lwm txoj kev ntawm biotransformation yog glucuronidation. Feem ntau siv tshuaj yeeb ntev (sulfadimethoxine, sulfalene) plam kev ua si los ntawm khi rau glucuronic acid. Cov txiaj ntsig glucuronides tau yooj yim soluble (tsis muaj kev phom sij ntawm crystalluria).

Txawm li cas los xij, lawv cov kev teem sijhawm thaum hnub nyoog me me yog qhov txaus ntshai heev, txij li kev ua haujlwm tsis haum ntawm glucuronyl transferase (glucuronidation catalyst) ua rau kev txuam nrog sulfonamide hauv cov ntshav thiab intoxication. Sulfonamides thiab lawv cov khoom lag luam biotransformacin tsuas yog tawm hauv cov zis nkaus xwb. Nrog rau mob raum, excretion qeeb qeeb - cov teebmeem phiv lom yuav tshwm sim.

Txawm hais tias cov lus tshaj tawm xaiv ntawm qhov kev nqis tes ua, cov tshuaj sulfonamide muab rau ntau qhov kev tsis haum: kev ua xua, ua kev puas tsuaj rau cov plab hnyuv lossis plab (ob lub raum, mob siab), cov hlab ntsha hauv lub cev, cov ntshav thiab cov ntshav muaj ntshav. Qhov mob uas nquag tshwm sim yog crystalluria yog vim li cas los ntawm crystallization ntawm sulfonamides thiab lawv cov acetylated metabolites hauv ob lub raum, ureters, thiab lub zais zis. Thaum nag lossis daus, lawv tsim cov xuab zeb, pob zeb, ua kom lub raum mob rau lub raum, txhaws cov zis thiab ua rau lub plab hlaub. Txog kev tiv thaiv, muaj dej haus ntau txaus yog tus kws kho mob, tso zis acidity yog txo (citrates lossis sodium bicarbonate raug sau rau alkalize zis). Kev siv cov kev sib txuas ua ke muaj 2-3 sulfonamides zoo heev (qhov tshwm sim ntawm crystalluria yog txo los ntawm 2-3 zaug).

Ntshav mob tshwm sim los ntawm cyanosis, methemoglobinemia, hemolytic anemia, leukopenia, agranulocytosis.

Cyanosis kev txhim kho yog qhov tshwm sim ntawm qhov thaiv ntawm erythrocyte carbonic anhydrase, uas ua rau cov nyom xa rov qab los ntawm cov pa roj carbon dioxide thiab cov pa hemoglobin. Kev txwv tsis pub los ntawm cov kev ua ntawm peroxidases thiab catalases txhawb kev tsub zuj zuj ntawm peroxides hauv cov ntshav liab thiab tom qab lub oxidation ntawm hemoglobin hlau (methemoglobin). Cov ntshav liab uas muaj cov tshuaj sulfa hemoglobin plam lawv qhov osmotic tsis kam thiab yog lysed (hemolytic anemia).

Hauv cov leeg pob txha, nyob rau hauv cawv ntawm sulfonamides, kev puas tsuaj rau cov ntshav tsim cov ntshav muaj peev xwm pom tau, uas ua rau kev txhim kho ntawm agranulocytosis, kev mob ntshav khov tsis txaus.

Kev tsim cov qe ntshav muaj tshwm sim nrog txoj cai koom nrog cov folic acid, uas lub cev tau txais nrog cov zaub mov, lossis los ua cov khoom tseem ceeb ntawm saprophytic microbial muaj mob ntawm cov hnyuv: sulfonamides inhibit plab hnyuv saprophytic microorganisms nrog kev siv lub sijhawm ntev, thiab yog tias muaj qhov tsis txaus ntawm folic acid nrog zaub mov, ces aplastic anemia yuav tshwm sim.

Qhov tshwm sim ntawm cov leukopenia yog vim qhov thaiv ntawm cov enzymes uas muaj zinc, uas tau pom muaj ntau hauv cov qe ntshav dawb. Qhov ncaj qha ua rau lub cev ntawm sulfonamides ntawm leukocytes yog ib qho kev tso dag ntawm aniline kuj tseem ceeb.

Qhov kev ua ntawm sulfonamides ntawm lub hauv nruab nrab lub paj hlwb nws ua rau nws tus kheej nyob rau hauv daim ntawv ntawm kiv taub hau, mob taub hau, qeeb hloov, kev nyuaj siab. Kev puas tsuaj rau peripheral poob siab hauv daim ntawv ntawm neuritis, polyneuritis (hypovitaminosis B 1, tsis muaj kabmob choline acetylation).

Sulfanilamides, tshwj xeeb tshaj yog bactrim, yuav tsum tsis txhob raug rau cov poj niam cev xeeb tub, vim tias cov tshuaj no muaj cov nyhuv teratogenic thiab ua rau muaj kev phom sij rau tus me nyuam hauv plab. Cov poj niam xeeb tub yuav tsum tsis txhob noj tshuaj sulfonamides, txij li lawv tawm hauv cov mis los.

Txawm hais tias qhov tseem ceeb ntawm sulfonamides rau kev kho mob hauv tsev kho mob tau tsis ntev los no vim tias muaj ntau ntawm cov kab mob tiv thaiv kab mob, kev sib xyaw tshuaj tseem siv tau: kev ua haujlwm siab, kev tawm tsam qeeb qeeb, thiab qhov feem pua ​​tsawg ntawm cov teeb meem. Lawv siv rau cov mob txeeb zig thiab mob hnyuv, cov kab mob ua pa (mob ntsws, mob otitis, mob ua paug), co-trimoxazole yog tau kho rau cov neeg mob AIDS uas mob ntsws pneumocystic, uas yog qhov tseem ceeb ntawm kev tuag ntawm cov neeg mob no.

Thaum ua ntawv thov saum toj kawg nkaus, nws yuav tsum nco ntsoov tias cov tshuaj tsuas yog ua qhov tsis huv, vim tias qhov hnoos qeev, cov nqaij mos necrotic, thiab cov ntshav muaj cov kab mob PABA ntau, uas inhibits cov tshuaj tiv thaiv ntawm sulfonamides. Yog li, nws yog qhov yuav tsum tau ua ntej kho lub qhov txhab, yaug nrog hydrogen peroxide thiab lwm yam tshuaj tua kab mob, thiab tom qab ntawd siv cov tshuaj. Tsis tas li ntawd, sulfonamides inhibit qhov kev tsim ntawm cov granulations, yog li ntawd, thaum lub sijhawm kho lub qhov txhab, lawv yuav tsum tau hloov los ntawm lwm qhov chaw hauv zos.