Sulfanilamides - mndandanda wa mankhwala, zikuonetsa, ntchito

Pakadali pano nthawi yodwala matenda ashuga mankhwala ochepetsa shuga a sulfonamide ndi biguanides amagwiritsidwa ntchito. Amathandiza kwambiri odwala okalamba omwe amakonda msanga. Ndizotheka kugwiritsa ntchito mankhwala a sulfonamide kuphatikiza jakisoni wa insulin mu shuga yayikulu mellitus mwa achinyamata kuti muchepetse kuchuluka kwa jakisoni wa insulin. Pankhani ya insulin yogonjetsedwa ndi matenda a shuga, kugwiritsa ntchito njira za sulfanilamide mu zochitika zina kumapereka zotsatira zabwino, zomwe zimapangitsa insulini ndikuchotsa zotsatira za zotsutsana ndi insulin zoletsa. Muubwana ndi achinyamata matenda a shuga mellitus pa vuto lathunthu la insulin, mankhwala ochepetsa shuga a sulfonamide satha.
Zosasangalatsa machitidwe mankhwala ochepetsa shuga a syfanilamide ndi ochepa, koma nthawi zina, kutsika kwamitsempha yamagazi, mapulateleti ndi ma neutrophils amatha kuonedwa m'magazi.

Ena kudwala onani mawonekedwe a nseru. Kuwonetsera kwa mziwi kumatheka. Kugwiritsa ntchito mankhwala ochepetsa shuga a sulfonamide amadzipaka pakati komanso ubwana, ndikuwonongeka kwambiri kwa impso ndi matenda amitsempha. Muubwana ndi unyamata, kuchuluka kwa shuga wa STH. Muzochitika izi, mankhwala ochepetsa shuga a sulfonamide angathandize kuchepetsa hyperglycemia ndipo akhoza kuphatikizidwa ndi kukonzekera kwa insulin.

Pakadali pano amaperekedwa zotsatirazi zochepetsa shuga za syfanilamide zotsatirazi: BZ-55 (padisan, oranil, inepol, carbutamide, glucidoral, bukarban), D-860 (rastinone, tolbutamide, butamide, artosin, orinase, orabet, dolipol, etc.).

Pakalipano kafukufuku zidapezeka kuti BZ-55 (nadizan ndi fanizo lake) amachepetsa shuga kwambiri poyerekeza ndi mankhwala a gulu la D-860. Komabe, mankhwala a gulu la D-860 (rastinone ndi analogies) sakhala oopsa.

Mankhwala ochepetsa shuga a shuga yoika 0,5 g 1-2-3 pa tsiku. Mutha kuonjezera mlingo mpaka 3 g patsiku. Koma ndikwabwino kutsatira mankhwala osavomerezeka kuti mupewe kuwopsa kwa mankhwalawo.
Mankhwala r-607 (chlorpropamide, diabenesis, oradian) amagwiritsidwa ntchito pamapiritsi a 250 mg. Wapakati tsiku lililonse 250-500 mg. Mankhwala a r-607 ndiwogwira ntchito kwambiri poyerekeza ndi ena omwe amachepetsa shuga ndi mankhwala a sulfonamide.

Cyclamide (K-386) m'mapangidwe ake oyimilira ayima pafupi ndi tolbutamide (D-860).
Zokhudza pakamwa chithandizo cha matenda ashuga Biguanides amagwiritsidwa ntchito, omwe mwa mawonekedwe a mankhwala amatha kugawidwa m'magulu atatu: phenethylbiguanides (DWI, phenformin, dibotin), butylbiguanides (silubin, buformip, adebite) ndi dimethylbiguanides glucofage, metformin). DVVI imapezeka m'mapiritsi a 25 mg, mlingo wa tsiku ndi tsiku ndi 125 mg, mlingo wapamwamba kwambiri watsiku ndi tsiku ndi 150 mg. Glucophage amalembedwa mapiritsi a 0,5 g katatu patsiku. Mulingo wapamwamba kwambiri tsiku lililonse wa 3 g.

Mankhwala butylbiguanide (silubin) amalembedwa pamapiritsi a 50 mg. Tsiku mlingo wa 150 mg. Mlingo wapamwamba kwambiri wa tsiku ndi tsiku wa 300 mg. Analogue ya silubin ndi mankhwala achi Hungary adebit. Pakadali pano ku England, kukonzekera kwa silubin kwa nthawi yayitali kunapezeka - kwa maola 24 (Silubin retard).

Biguanides chifukwa hypoglycemia, potrate insulin. Kuchuluka kwa shuga ndikupezeka ndi minofu. Kuchulukitsa zomwe zili ndi lactic ndi pyruvic acid m'magazi ndikumayambika kwa glucose ndikuchepetsa gluconeogeneis. Kuphatikiza apo, Biguanides amathandizira phosphorylation mu cell mitochondria. Pali zina zomwe zimawona kuti ma biguanides odwala omwe ali ndi matenda ashuga, amakonda kunenepa kwambiri, amachepetsa kwambiri kutulutsa insulin, amachepetsa chilimbikitso, ndipo amalimbikitsa kuchepa thupi. Mosiyana ndi kukonzekera kuchepetsa shuga kwa sulufanamide, ma biguanides amagwira ntchito makamaka pakubwera kwa ana ndi matenda ashuga wa ana pamene kupanga kwa insulin kwayamba kuchepa.

Zowopsa khwawa pang'ono, komabe, nseru, kusanza, kupweteka m'dera la epigastric kumawonedwa. Odwala ena omwe amagwiritsa ntchito bnguanides nthawi yayitali adazindikira kufooka, kuwonda. Kuphatikiza mankhwala ndi insulin kumathandizira kusintha kagayidwe kachakudya kagayidwe kachakudya. Kukonzekera kwa Bnguanide kuphatikiza ndimankhwala ochepetsa shuga a sulufilamide kumapereka zotsatira zabwino mu insulin zotsutsana ndi shuga.

Yambirani mankhwalawa retinopathy iyenera kukhala ndi cholinga chobwezera shuga. Kukonzekera kwa anabolic steroid kumalimbikitsidwa, mavitamini amathandizira, kuvindikira kumapangitsa kuti mitsempha ikhale yamavuto ambiri, koma osavomerezeka pamaso pa zotupa za m'mimba. Muzochitika izi, calcium chloride, rutin, ndi vicalin zimawonetsedwa. Pamaso pa matenda a shuga a retinopathy komanso matenda oopsa, kuchepa kwa kuthamanga kwa magazi ndi mankhwala a antihypertensive kumasonyezedwa.

Ndi matenda ashuga nephropathy Ndikosavuta kulipirira matenda ashuga, chifukwa cha kuthekera kwa mikhalidwe ya hypoglycemic. Makonzedwe ang'onoang'ono a insulin, omwe amaperekedwa pang'ono, amatengera kuchuluka kwa shuga m'magazi, popeza mulibe shuga pakuyesa kwamkodzo. Pazakudya, ndikofunikira kuchepetsa mchere, mafuta, nyama iyenera kuwiritsa. Kusintha kaphatikizidwe ka mapuloteni, mankhwala a anabolic steroid (nerabol, retabolil, etc.) ndi omwe amapatsidwa. Pankhani ya uremia, kupweteka kwam'mimba, mpweya, kuthiridwa magazi, ndi mankhwala a mtima.

Mankhwalawa polyneuritis Physiotherapy, kutikita minofu, masewera olimbitsa thupi amalimbikitsidwa. Chithandizo cha insulin choyenera, mankhwala a vitamini (ovuta B1, B6, B12, ndi C) amasintha mkhalidwe wa odwala.

Kodi ma sulfonamides maantibayotiki kapena ayi?

Inde, sulfonamides ndi gulu lopatula la maantibayotiki, ngakhale poyamba, atapangidwa ndi penicillin, sanaphatikizidwe pagulu. Kwa nthawi yayitali, zinthu zachilengedwe zokha kapena zopangidwa zokha zomwe zimawonedwa kuti ndi "zenizeni", ndipo sulfonamide yoyambirira ndi zotumphukira zake zomwe zimapangidwa kuchokera phula lamalaji sizinali choncho. Koma pambuyo pake zinthu zinasintha.

Masiku ano sulfonamides ndi gulu lalikulu la mabakiteriya omwe ali ndi bacteriostatic kanthu, amagwira motsutsana ndi tizilombo toyambitsa matenda ambiri opatsirana ndi kutupa. M'mbuyomu, mankhwala a sulfonamide ankakonda kugwiritsidwa ntchito zosiyanasiyana. Koma popita nthawi, ambiri aiwo adataya tanthauzo chifukwa chakusinthika komanso kukana mabakiteriya, ndipo masiku ano, othandizira amaphatikizidwa amagwiritsidwa ntchito nthawi zambiri pochiritsa.

Gulu la sulfonamides

Ndizofunikira kudziwa kuti mankhwala a sulfonamide adapezeka ndipo adayamba kugwiritsidwa ntchito ngati mankhwala kale kuposa penicillin. Zotsatira zaku utoto wa utoto wa mafakitale ena (makamaka, pronosyl kapena "red Cryptocide") zidawululidwa ndi wasayansi wazaku Germany wa Gerhard Domagk mu 1934. Chifukwa cha gululi, lomwe linkagwira ntchito molimbana ndi streptococci, adachiritsa mwana wake wamkazi, ndipo mu 1939 adakhala wophunzira wa mphoto ya Nobel.

Chowonadi chakuti bacteriostatic zotsatira sichikhala ndi gawo la molekyulu yotchedwa falosyl, koma ndi aminobenzenesulfamide (aka "oyera streptocide" ndi chinthu chophweka kwambiri m'gulu la sulfonamides) zidapezeka mu 1935. Ndikusintha kwake komwe kukonzekera kwina konse kwamkalasi kunapangidwira m'tsogolo, zambiri Zomwe zimagwiritsidwa ntchito kwambiri ngati mankhwala ndi Chowona Zanyama. Kukhala ndi chiwonetsero chofananira cha antimicrobial kanthu, zimasiyana pamagawo a pharmacokinetic.

Mankhwala ena amatengeka mwachangu ndikugawidwa, pomwe ena amatengeka nthawi yayitali. Pali kusiyana pakutalika kwa kuchotsedwa kwa thupi, chifukwa chomwe mitundu yotsatirayi ya sulfonamides imasiyanitsidwa:

  • Ochita zinthu mwachidule, theka la moyo wake omwe ndi ochepera maola 10 (streptocid, sulfadimidine).
  • Kutalika kwapakatikati, komwe T 1 /2Maola 10 - 24 - sulfadiazine, sulfamethoxazole.
  • Zochitika kwanthawi yayitali (T theka-moyo kuchokera masiku 1 mpaka 2) - sulfadimethoxin, sulfonomethoxin.
  • Superlong - sulfadoxine, sulfamethoxypyridazine, sulfalene - omwe amuchotsa maola opitilira 48.

Gawoli limagwiritsidwa ntchito ngati mankhwala amkamwa, komabe, pali sulufanilamides omwe sanalengezedwe kuchokera m'mimba thirakiti (phthalyl sulfathiazole, sulfaguanidine), komanso sulfadiazine wa siliva wopangidwira ntchito zapakhungu zokha.

Mndandanda wathunthu wa sulfanilamide kukonzekera

Mndandanda wa mankhwala a sodiumfanfanamide omwe amagwiritsidwa ntchito ngati mankhwala amakono omwe ali ndi mayina azamalonda ndikuwonetsa mawonekedwe amomwe amamasulidwa amaperekedwa pagome:

Zogwira ntchito Dzina lamankhwala Mlingo
SulfonamideStreptocideUfa ndi mafuta 10% ogwiritsa ntchito kunja
Streptocid yoyeraWodzaza kunja
Soluble streptocideLiniment 5%
Streptocid-LekTUfa d / nar. ntchito
Mafuta a StreptocideChithandizo chakunja, 10%
SulfadimidineSulfadimezinMapiritsi 0,5 ndi 0,25 g
SulfadiazineSulfazineTab. 500 mg
Sulfadiazine wa silivaSulfarginMafuta 1%
DermazinKirimu d / nar. 1% ntchito
ArgadineKirimu wakunja 1%
Sulfathiazole SilivaArgosulfanKirimu wa Nar.
Sulfamethoxazole kuphatikiza ndi trimethoprimBactrimMapiritsi oimitsidwa
BiseptolTab. 120 ndi 480 mg, kuyimitsidwa, kukhazikika kwa d / kukonzekera kulowetsedwa
BerlocideMapiritsi, kuyimitsidwa.
DvaseptolTab. 120 ndi 480 mg
Co-trimoxazoleTab. 0,48 g
SulfulfaleneSulfulfalene200 mg mapiritsi
SulfamethoxypyridazineSulfapyridazineTab. 500 mg
SulfaguanidineSulginTab. 0,5 g
SulfasalazineSulfasalazineTab. 500 mg
SulfacetamideSulfacyl Sodium (Albucid)Diso limatsika 20%
SulfadimethoxinSulfadimethoxin200 ndi 500 mg mapiritsi
SulfaethidolOlestesinMa suppositories amtundu (ndi benzocaine ndi mafuta a sea buckthorn)
EtazoleTab. 500 mg
PhthalylsulfathiazolePhthalazole0,5 g mapiritsi

Maantibayotiki onse a sulfonamide kuchokera pamndandanda wa mankhwalawa alipo. Olemba ena amatchula mankhwala ena a gululi (mwachitsanzo, Urosulfan), omwe anasiya kalekale. Kuphatikiza apo, pali mankhwala a sodiumfanfanamide omwe amagwiritsidwa ntchito pokhapokha ngati mankhwala a Chowona.

Limagwirira a zochita za sulfonamides

Kuyimitsa kukula kwa tizilombo toyambitsa matenda (ma gram-negative ndi gram-tizilombo tating'onoting'ono, protozoa) ndi chifukwa chofanana ndi kapangidwe kazinthu kazinthu kakapangidwe ka para-aminobenzoic acid ndi sulfonamide. PABA ndiyofunikira kuti khungu lipange zinthu zofunika kwambiri pachitukuko - folate ndi dihydrofolate. Komabe, molekyulu yake ikasinthidwa ndi mawonekedwe a sulfanilamide, njirayi imasokonekera ndipo kukula kwa pathogen kumayima.

Mankhwala onse amamwetsedwa m'mimba yamagetsi ndi kuthamanga kosiyanasiyana ndi madigiri a mayamwidwe. Zomwe sizimatulutsa m'mimba zimasonyezedwa zochizira matumbo. Kugawa minofu ndi yunifolomu, kagayidwe amachitika chiwindi, chimbudzi - makamaka kudzera impso. Nthawi yomweyo, depot sulfonamides (ochita nthawi yayitali komanso yapamwamba kwambiri) amabwezeretsedwanso m'matumbo a impso, omwe amafotokozera moyo wautali.

Zisonyezero zogwiritsira ntchito sulfonamides

Kuyimitsa kukula kwa tizilombo toyambitsa matenda (ma gram-negative ndi gram-tizilombo tating'onoting'ono, protozoa) ndi chifukwa chofanana ndi kapangidwe kazinthu kazinthu kakapangidwe ka para-aminobenzoic acid ndi sulfonamide. PABA ndiyofunikira kuti khungu lipange zinthu zofunika kwambiri pachitukuko - folate ndi dihydrofolate. Komabe, molekyulu yake ikasinthidwa ndi mawonekedwe a sulfanilamide, njirayi imasokonekera ndipo kukula kwa pathogen kumayima.

Mankhwala onse amamwetsedwa m'mimba yamagetsi ndi kuthamanga kosiyanasiyana ndi madigiri a mayamwidwe. Zomwe sizimatulutsa m'mimba zimasonyezedwa zochizira matumbo. Kugawa minofu ndi yunifolomu, kagayidwe amachitika chiwindi, chimbudzi - makamaka kudzera impso. Nthawi yomweyo, depot sulfonamides (ochita nthawi yayitali komanso yapamwamba kwambiri) amabwezeretsedwanso m'matumbo a impso, omwe amafotokozera moyo wautali.

Chiwopsezo kwa sulfonamides

Mlingo wambiri wa ziwengo zophatikizika za sulufanilamide ndiye vuto lalikulu lomwe amagwiritsa ntchito. Chovuta china pamenepa ndi chithandizo cha chibayo chomwe chimapezeka mwa anthu omwe ali ndi kachilombo ka HIV, popeza Biseptol ndiye mankhwala osankhira iwo. Komabe, zili m'gulu ili la odwala komwe mwayi wokhala ndi zovuta zomwe zimayenderana ndi co-trimoxazole umachulukitsa kakhumi.

Chifukwa chake, ndi ziwopsezo za sulufanilamides, Biseptol ndi zina zomwe zimapangidwa motengera co-trimoxazole zimaperekedwa kwa wodwala. Kusalolera nthawi zambiri kumawonetsedwa ndi totupa yaying'ono, kutentha thupi kumatha kukhalanso, ndipo kapangidwe ka magazi (neutro- and thrombocytopenia) kumasintha. M'malo ovuta kwambiri - Lyell ndi Stevens-Johnson syndromes, erythema multiforme, anaphylactic shock, edema ya Quincke.

Chiwopsezo cha sulfonamides chimafuna kuthetsedwa kwa mankhwalawo omwe adayambitsa, komanso kugwiritsa ntchito mankhwala oletsa matupi awo.

Zotsatira zina zoyipa za sulfonamides

Mankhwala ambiri m'gululi ndi oopsa komanso olekeredwa bwino, chomwe chinali chifukwa chochepetsera kugwiritsa ntchito kwawo kwa penicillin atapezeka. Kuphatikiza pa ziwengo, zimayambitsa kusokonezeka kwa mutu, kupweteka mutu ndi m'mimba, kuperewera, zotumphukira neuritis, hematopoiesis, bronchospasm, polyuria, kusowa kwa impso, nephropathy, myalgia ndi arthralgia. Kuphatikiza apo, chiopsezo chokhala ndi makristasi chimawonjezeka, chifukwa chake muyenera kumwa mankhwala ambiri ndikumwa madzi amchere ambiri.

Kuchita ndi mankhwala ena

Kupanikizana ndi maantibayotiki ena mu sulfonamides sikuwunikidwa. Akaphatikizidwa ndi othandizira a hypoglycemic othandizira komanso ma intagulants osagwirizana, mphamvu zawo zimakulitsidwa. Sitikulimbikitsidwa kuphatikiza mankhwala-sulfonamides komanso thiazide diuretics, rifampicin ndi cyclosporine.

Kodi pali kusiyana kotani pakati pa sulfonamides ndi sulfonamides

Ngakhale maina ophatikizika, mankhwala awa ali osiyanasiyana. Sulfonamides (code ya ATX C03BA) ndi okodzetsa - okodzetsa. Mankhwala am'magulu amaperekedwa kwa matenda oopsa, kuzizira, kuperewera kwa shuga, matenda a shuga, kunenepa kwambiri ndi zina zomwe zimayendera limodzi ndi kuchuluka kwa madzi mthupi.

Sulfonamides

Sulfonamides - antimicrobial agents, zotumphukira awiri (π)-aminobenzenesulfamide - gawo lina la sulfanilic acid (para-aminobenzene sulfonic acid). Zambiri mwazinthu izi zakhala zikugwiritsidwa ntchito ngati antibacterial othandizira kuyambira zaka za m'ma 1900. angapo-Aminobenzenesulfamide - gulu losavuta kwambiri la gulu - lomwe limadziwikanso kuti loyera la Cryptocide ndipo likugwiritsidwabe ntchito ngati mankhwala. Chopangidwanso pang'ono, kapangidwe kake ka sulfonamide (red streptocide) chinali mankhwala oyamba m'gululi ndipo, makamaka, mankhwala oyambitsa antibacterial padziko lapansi.

Mu 1934, G. adapeza antibacterial.Domagk. Mu 1935, asayansi ku Pasteur Institute (France) adazindikira kuti ndi gawo la molekyu yomwe inali ndi vuto la antibacterial, osati mawonekedwe omwe anapatsa mtunduwo. Zinapezeka kuti "mfundo yogwira ntchito" yofiyira ya redptocide ndi sulfanilamide, yomwe imapangidwa nthawi ya metabolism (streptocide, white streptocide). Red streptocide yachoka pakugwiritsidwa ntchito, ndipo pamaziko a molekyu ya sulfanilamide, kuchuluka kwake kwazomwe zimapangidwa, zomwe ena adagwiritsidwa ntchito kwambiri ngati mankhwala.

Magawo a Pharmacological

Sulfanilamides amachita bacteriostatic, ndiye kuti, ali ndi zochita za chemotherapeutic m'matenda omwe amayamba chifukwa cha gramu-and gram-negative bacteria, protozoa (tizilombo toyambitsa matenda a malungo, toxoplasmosis), chlamydia (wokhala ndi trachoma, paratrachoma).

Zochita zawo zimagwirizanitsidwa ndi kuphwanya mapangidwe ndi tizilombo tating'onoting'ono tomwe timatulutsa timene timafunika kukula - folic ndi dihydrofolic acid ndi zinthu zina, molekyulu yomwe imaphatikizapo para-aminobenzoic acid. Limagwirira ntchito limagwirizanitsidwa ndi kapangidwe kofanana ndi kachidutswa ka sulfanilamide ndi angapo-aminobenzoic acid (PABA) - gawo laling'ono la enzyme dihydropteroate synthetase, lomwe limapanga dihydropteroic acid, yomwe imabweretsa mpikisano poletsa dihydropteroate synthetase. Izi, zimabweretsa chisokonezo mu kapangidwe ka dihydropteroic dihydrofolate, kenako tetrahydrofolate, ndipo chifukwa chake, kuphwanya kapangidwe ka ma nitic acid m'mabakiteriya.

Kuti mupeze achire, ziyenera kufotokozedwa mu Mlingo wokwanira kuteteza kuti tizilombo tating'onoting'ono togwiritsa ntchito para-aminobenzoic acid okhala ndi minofu. Mlingo wosakwanira wa sulfonamide mankhwala kapena kusiya kumwa mankhwala kumayambiriro kwambiri kungayambitse matenda obwera chifukwa cha tizilombo toyambitsa matenda omwe sangathe kupititsa patsogolo mankhwala a sulfonamides. Ambiri mabakiteriya ofunikira kwambiri pakadali pano amalimbana ndi sulfonamides. Tiyenera kukumbukira kuti mankhwalawa, omwe molekyulu yomwe imaphatikizapo zotsala za para-aminobenzoic acid (mwachitsanzo, novocaine), amatha kukhala ndi mphamvu yotchedwa antisulfanilamide.

Magawo a Pharmacological edit |

2.5.2.2. Mankhwala a Sulfa

Sulfanilamides - antimicrobial agents, zotumphukira za sulfanilic acid amide (oyera streptocide). Kupeza kwawo kunatsimikizira kulosera kwa P. Ehrlich ponena za kuthekera kosankha kuwonongeka kwa tizilombo tating'onoting'ono tambiri ndi mphamvu ya cytotoxic yothandizanso. Mankhwala oyamba a gululi kuboola (red cryptocide) adaletsa kufa kwa mbewa. kachilombo kakhumi matenda owopsa a hemolytic streptococcus.

Pamaziko a molekyulu ya sulfanilamide mu theka lachiwiri la 30s, mankhwala ena ambiri anapangidwa (norsulfazole, ethazole, sulfazine, sulfacyl, etc.). Kupezeka kwa maantibayotiki kwachepetsa chidwi cha sulfonamides, koma sanataye kufunika kwawo, tsopano amagwiritsidwa ntchito kwambiri "-ngokhala nthawi yayitali" (sulfapyridazine, sulfalene, etc.) ndipo makamaka mankhwala osakanikirana (co-trimoxazole ndi ma analogues ake, omwe amaphatikiza trimethoprim kuwonjezera pa sulfonamide) . Mankhwalawa ali ndi mawonekedwe ochulukirapo a antimicrobial action (mabakiteriya abwino komanso gramu-negative, chlamydia, protozoa - tizilombo toyambitsa matenda a malungo ndi toxoplasmosis, bowa wa pathogenic - actinomycetes, etc.).

Ma Sulfanilamides agawidwa m'magulu otsatirawa:

2. Mankhwala osokoneza bongo omwe amamwa kwathunthu m'matumbo, koma pang'onopang'ono ndi impso (achitapo kanthu): sulfamethoxypyridazine (sulfapyridazine), sulfonomethoxin, sulfadimethoxin, sulfalene.

Gulu loyamba ndi lachiwiri, lomwe limalowa bwino m'matumbo, limagwiritsidwa ntchito pochiza matenda amtundu, lachitatu - pochiza matenda am'matumbo (mankhwalawa samatengedwa ndikugwira ntchito pakuwunika kwa kugaya chakudya), wachinayi - makamaka, komanso wachisanu (mankhwala ophatikiza ndi trimethoprim) amagwira ntchito kuchita ndi matenda am'mapapo ndi kwamikodzo, matenda ammimba.

Njira yamachitidwe. Sulfanilamides amayambitsa bacteriostasis. Ndiwotsutsana a para-aminobenzoic acid (PABA), omwe amafunikira kuti tizilombo tating'onoting'ono tisakanikize folic acid: omalizawa mu mawonekedwe a coenzyme (dihydrofolate, tetrahydrofolate) amatenga nawo mbali pakapangidwe kama purine ndi pyrimidine, omwe amatsimikizira kukula ndi kukula kwa tizilombo. Ma sulfanilamides ali pafupi ndi kapangidwe ka mankhwala ku PABA chifukwa chake amagwidwa ndi khungu loyang'anira majeremusi m'malo mwa PABA. Zotsatira zake, kapangidwe ka folic acid amasiya. Maselo aumunthu sangathe kupanga folic acid (imabwera ndi chakudya), yomwe imalongosola kusankha kwa antimicrobial zochita za mankhwalawa. Sulfanilamides samakhudza mabakiteriya omwe amapanga PABA. Pamaso pa mafinya, magazi, mankhwala owononga minofu okhala ndi kuchuluka kwa PABA, mankhwalawa sagwira ntchito. Mankhwala omwe amapanga PABA chifukwa cha biotransfform (novocaine, dicaine) ndi otsutsana ndi sulfonamide.

Mankhwala osakanikirana: Co-trimoxazole (bactrim, biseptol), sulfatone, yomwe, kuphatikiza pa mankhwala a sulfa (sulfamethoxazole, sulfamonomethoxine), akuphatikiza trimethoprim, ndi othandizira kwambiri antibacterial. Trimethoprimkuletsa dihydrofolic acid reductase, imalepheretsa kusintha kwake kukhala tetrahydrofolic acid. Chifukwa chake, poyambitsa kuphatikiza kwa sulfanilamide kukonzekera, osati kuphatikiza kwa folic acid kokha, komanso kusintha kwake kwa coenzyme (tetrahydrofolate). Mankhwalawa ali ndi ntchito ya bactericidal yolimbana ndi gramu-gramu komanso mabakiteriya opanda gram.

Njira yayikulu yoyendetsera sulfonamides kudzera pakamwa. M'matumbo ang'onoang'ono, amatha mwachangu komanso kwathunthu (kupatula mankhwala olemetsa - phthalazole, phthazine, salazosulfanilamides, omwe amalamula matenda am'matumbo), amamangidwa kumapuloteni a plasma m'magazi, kenako, ndikumasulidwa pang'ono ndi pang'ono, ndikuyamba kuwonetsa ntchito yolimbana ndi matenda, chidutswa. Pafupifupi onse sulfonamides amadutsa zotchinga minofu bwino, kuphatikiza hepatohematic, magazi-ubongo, ndi mphamvu. Amawerengeka mu chiwindi, ena amatulutsidwa mu ndulu (makamaka omwe amakhala nthawi yayitali, omwe amagwiritsidwa ntchito bwino matenda amtundu wa biliary.

Njira yayikulu yogwiritsira ntchito biotransfform ya sulfonamides ndi acetylation. Ma metabolite acetylated amataya ntchito yawo ya antibacterial, samasungunuka bwino, ndipo mu acidic mkodzo amatha kupanga makhiristo omwe amawononga kapena kutsekereza njira za aimpso. Pankhani ya matenda a kwamikodzo thirakiti, sulfonamides ndi mankhwala, omwe amayamba kupatsidwa mkodzo mu mawonekedwe aulere (urosulfan, etazole).

Njira ina yopangira biotransformation ndi glucuronidation. Mankhwala omwe akhala akuchita kwa nthawi yayitali (sulfadimethoxine, sulfalene) amataya ntchito pomanga glucuronic acid. Ma glucuronides omwe amayamba kusungunuka mosavuta (palibe chiopsezo cha crystalluria).

Komabe, kuperekera kwawo adakali aang'ono ndi kowopsa kwambiri, chifukwa kusakhazikika kwa glucuronyl transferase (glucuronidation chothandizira) kumabweretsa kuchuluka kwa sulfonamide m'mwazi ndi kuledzera. Ma sulfonamides ndi mankhwala awo a biotransformacin amathandizidwa makamaka mkodzo. Ndi matenda a impso, chimbudzi chimachepetsa - zotsatira zoyipa zimatha kuchitika.

Ngakhale atchulidwe kusankha kwa chochitikacho, mankhwala a sulfonamide amapereka zovuta zambiri: matupi awo sagwirizana, kuwonongeka kwa ziwalo zam'mimba (impso, chiwindi), dongosolo lamanjenje, magazi ndi ziwalo zopanga magazi. Vuto lamafupipafupi ndi crystalluria chifukwa cha crystallization ya sulfonamides ndi ma acetylated metabolites awo mu impso, ureters, ndi chikhodzodzo cha kwamikodzo. Akawupangira, amapanga mchenga, miyala, kukhumudwitsa minofu ya impso, kuphimba kwamkodzo mundawo ndikubweretsa impso. Popewa, chakumwa chochuluka chimayikidwa, mkodzo acidity umachepetsedwa (citrate kapena sodium bicarbonate amalembera mkodzo wamchere). Kugwiritsa ntchito kuphatikiza kwa 2-3 sulfonamides kumathandiza kwambiri (kuthekera kwa crystalluria kumachepetsedwa ndi 2-3 nthawi).

Mavuto amwazi amadziwika ndi cyanosis, methemoglobinemia, hemolytic anemia, leukopenia, agranulocytosis.

Cyanosis imayamba chifukwa cha kutsekeka kwa erythrocyte carbonic anhydrase, komwe kumapangitsa kuti mpweya ubwerere ndi mpweya wa hemoglobin. Kuletsa kwa ntchito ya peroxidases ndi ma catalases kumalimbikitsa kuchuluka kwa peroxides m'magazi ofiira komanso makutidwe ndi okosijeni a hemoglobin iron (methemoglobin). Maselo ofiira okhala ndi sulfa hemoglobin amalephera kukana kwawo kwa osmotic ndipo amalephera (hemolytic anemia).

Mofufupa, mothandizidwa ndi sulfonamides, kuwonongeka kwa maselo opanga magazi kumatha kuchitika, zomwe zimapangitsa kuti agranulocytosis, anplastic anemia.

Kapangidwe ka maselo am'magazi kumachitika ndi kukakamiza kwa folic acid, komwe thupi limalandira ndi chakudya, kapena ngati chinthu chofunikira cha saprophytic tizilombo tating'onoting'ono ta matumbo: sulfonamides tikuletsa tizilombo toyambitsa matumbo a patrophytic omwe amagwiritsidwa ntchito kwa nthawi yayitali, ndipo ngati sipakhala chakudya chokwanira cha folic acid ndi chakudya, ndiye kuti aplasic anemia ingachitike.

Kupezeka kwa leukopenia kumachitika chifukwa cha kutsekeka kwa ma enzymes okhala ndi zinc, omwe amapezeka m'magazi oyera ambiri. Zowopsa za sulfonamides pa leukocytes monga zotumphukira za ailine ndizofunikanso.

Zochita za sulfonamides pamkatikati yamanjenje zimadziwoneka mu mawonekedwe a chizungulire, kupweteka mutu, kusintha pang'onopang'ono, kukhumudwa. Kuwonongeka kwa zotumphukira zamanjenje mu mawonekedwe a neuritis, polyneuritis (hypovitaminosis B 1, kuphwanya choline acetylation).

Sulfanilamides, makamaka bactrim, sayenera kuperekedwa kwa amayi apakati, chifukwa mankhwalawa ali ndi mphamvu yayikulu komanso amakhala pachiwopsezo pakukula kwa fetal. Amayi oyamwitsa sayenera kumwa sulfonamides, chifukwa amuchotsa mkaka.

Ngakhale kufunikira kwa sulfonamides pakuchita zamankhwala kwatsika posachedwa chifukwa kuchuluka kwazovuta zothetsera, mankhwala osakanikirana amagwiritsidwabe ntchito: kuthana ndi antibacterial zochita, kukana kumayamba pang'onopang'ono, komanso kuchuluka kovuta. Amagwiritsidwa ntchito pochotsa matenda amkodzo ndi matumbo, matenda opuma (bronchitis, otitis media, sinusitis), co-trimoxazole amalembedwa kwa odwala a pneumocystic chibayo, omwe ndi omwe amafa kwambiri chifukwa cha odwala.

Mukamagwiritsira ntchito mopitirira muyeso, muyenera kukumbukira kuti mankhwalawa amangokhala ngati bala loyera, popeza kukhalapo kwa mafinya, minofu ya necrotic, ndi magazi zimakhala ndi PABA yambiri, yomwe imalepheretsa antibacterial zochita za sulfonamides. Chifukwa chake, ndikofunikira kuti musanachiritse chilondacho, muzitsuka ndi hydrogen peroxide ndi ma antiseptics ena, ndikugwiritsa ntchito mankhwalawa. Kuphatikiza apo, sulfonamides amalepheretsa mapangidwe a granerals, chifukwa chake, panthawi yakuchiritsa bala, amayenera kulowedwa m'malo ndi njira zina zakomweko.

Kusiya Ndemanga Yanu