Hajoale nako ea lefu la tsoekere ho sebelisoa lithethefatsi tse phahameng tse nang le tsoekere tse ngata tsa sulfonamide le li-biguanide. Li sebetsa hantle haholo ho bakuli ba tsofetseng ba tloaetseng ho tlala. Ho a khonahala ho sebelisa lithethefatsi tsa sulfonamide hammoho le liente tsa insulin ho mellitus e matla ea lefu la tsoekere ho batho ba bacha e le ho fokotsa palo ea liente tsa insulin. Maemong a mefuta e sa sebetsaneng le insulin ea lefu la tsoekere, ts'ebeliso ea litokisetso tsa sulfanilamide maemong a mang e fana ka phello e ntle, e eketsang ketso ea insulin le ho felisa phello ea li-contra-factor le insulin inhibitors. Ho bongoaneng le bongoaneng mellitus maemong a khaello ea insulin e felletseng, lithethefatsi tse fokotsang tsoekere tsa sulfonamide ha li na thuso.
E fosahetse ketso lithethefatsi tse fokotsang tsoekere se nang le tsoekere li nyane, empa maemong a mang, ho fokotseha ha lisele tse tšoeu tsa mali, liplatelete le li-neutrophils li ka bonoa maling.

Ba bang a kula hlokomela ponahalo ea ho nyekeloa ke pelo. Liponahatso tsa allergic lia khoneha. Ts'ebeliso ea lithethefatsi tse fokotsang tsoekere e tsoekere e tšoaetsanoa boimana le bongoaneng, ka ts'enyo e mpe ea menoana le cirrhosis. Bocheng le bonyaneng, ho eketsoa hoa phello ea tsoekere ho STH. Maemong ana, lithethefatsi tse fokotsang tsoekere tsa sulfonamide li ka thusa ho fokotsa hyperglycemia mme li ka kopanngwa le litokisetso tsa insulin.

Hajoale li fanoe litokisetso tse latelang tsa tsoekere tse fokotsang tsoekere: BZ-55 (padisan, oranil, inepol, carbutamide, glucidoral, bukarban), D-860 (rastinone, tolbutamide, butamide, artosin, orinase, orabet, dolipol, jj).

Hajoale tse ngata patlisiso ha fumaneha hore BZ-55 (nadizan le analogues ea eona) li na le ts'ebetso e fokotsang tsoekere haholo ha e bapisoa le lithethefatsi tsa sehlopha sa D-860. Leha ho le joalo, lithethefatsi tsa sehlopha sa D-860 (rastinone le analogues ea sona) ha li na chefo.

Lithethefatsi tse theolelang tsoekere beha linako tse 0,5 g ka makhetlo a 1-2 ho isa ho a mararo ka letsatsi. O ka eketsa tekanyetso ho isa ho 3 g ka letsatsi. Empa ho molemo ho latela litlhare tse itekanetseng e le ho qoba litlamorao tsa lithethefatsi.
Lithethefatsi r-607 (chlorpropamide, diabenesis, oradian) e sebelisoa matlapeng a 250 mg. Karolelano ea letsatsi le letsatsi ea 250-500 mg. Lithethefatsi r-607 ke tsona tse sebetsang ka ho fetisisa ha li bapisoa le lithethefatsi tse ling tse theolelang tsoekere le sulfonamide.

Cyclamide (K-386) ka sebopeho sa eona sa sebopeho se eme haufi le tolbutamide (D-860).
Bakeng sa tsamaiso ea molomo kalafo ea lefu la tsoekere Biguanides e sebelisoa, eo ka sebopeho sa lik'hemik'hale e ka arohanoang ka lihlopha tse tharo: phenethylbiguanides (DWI, phenformin, dibotin), butylbiguanides (silubin, buformip, adebite) le dimethylbiguanides glucofage, metformin). DVVI e fumaneha ka har'a matlapa a 25 mg, tekanyetso ea letsatsi le letsatsi ke 125 mg, lethal dose le phahameng ka ho fetisisa la letsatsi ke 150 mg. Glucophage e tšeloa matlapeng a 0,5 g makhetlo a 2-3 ka letsatsi. Tekanyo e phahameng ka ho fetisisa ea letsatsi le letsatsi ea 3 g.

Lithethefatsi butylbiguanide (silubin) e thehiloe matlapeng a 50 mg. Tekanyetso ea letsatsi le letsatsi ea 150 mg. Tekanyetso e phahameng ka ho fetisisa ea letsatsi le letsatsi ea 300 mg. Analogue ea silubin ke adebit ea lithethefatsi tsa Hungary. Hajoale Engelane, ho ile ha fumanoa tokiso ea silubin e nkileng nako e telele - ka lihora tse 24 (sekepe sa Silubin).

Biguanides baka hypoglycemia, e eketsang ketso ea insulin. Eketsa phallo ea tsoekere ka lisele. Eketsa litaba tsa lactic le pyruvic acid maling le kenyelletso ea tsoekere le fokotsa gluconeogeneis. Ntle le moo, li-biguanides li ntlafatsa phosphorylation e tsoang seleng mitochondria. Ho na le maikutlo a hore li-biguanides ho bakuli ba nang le lefu la tsoekere, ba nang le botenya haholo, ba fokotsa ho tsoa ka bongata ha insulin, ba fokotsa takatso ea lijo le ho phahamisa boima ba 'mele. Ha ho bapisoa le litokisetso tsa shibfanilamide tse fokotsang tsoekere, li-biguanides li sebetsa hantle tsoekere ea bongoaneng le bongoaneng ha tlhahiso ea insulin ea tlhaho e fokotsoa haholo.

Litlamorao biguanides hanyane, leha ho le joalo, ho nyekeloa, ho hlatsa, bohloko sebakeng sa epigastric li bonoa. Bakuli ba bang ba neng ba sebelisa li-bnguanides nako e telele ba hlokometse bofokoli, ho theola boima ba 'mele. Motsoako oa motsoako o nang le insulin o thusa ho etsa hore metabolism e fetohe. Litokisetso tsa Bnguanide hammoho le lithethefatsi tse nang le tsoekere tse fokotsang tsoekere li fana ka phello e ntle mefuteng ea insulin e hananang le lefu la tsoekere.

Shebana mekhoa ea phekolo retinopathy e lokela ho ikemisetsa ho lefella lefu la tsoekere. Ho khothalletsoa litokisetso tsa anabolic steroid, kalafo ea vithamine, sekoaelo se ntlafatsa boleng ba methapo ea mali, empa ha e khothalletsoe boteng ba li-hemorrhages. Maemong ana, ho bontšoa calcium chloride, rutin le vicalin. Ka boteng ba lefu la tsoekere la retinopathy le khatello ea mali, ho fokotseha ha khatello ea mali le lithethefatsi tsa antihypertensive ho bontšoa.

Le lefu la tsoekere nephropathy Ho thata ho lefella lefu la tsoekere, ho latela monyetla oa maemo a hypoglycemic. Tsamaiso ea litekanyetso tse nyane tsa insulin, e tsamaisoang hanyane ka hanyane, e ipapisitse le boemo ba tsoekere ea mali, kaha ha ho na tsoekere litekong tsa moroto. Ho phepo e nepahetseng, hoa hlokahala ho fokotsa letsoai, mafura, nama e lokela ho belisoa. Ho ntlafatsa motsoako oa liprotheine, ho laetsoe lithethefatsi tsa anabolic steroid (nerabol, retabolil, jj.). Maemong a uremia, lesapo la mokokotlo, oksijene, tšelo ea mali le lithethefatsi tsa pelo li sebelisoa.

Ka kalafo ea polyneuritis Ho khothaletsoa boikoetliso ba 'mele, ho silila, boikoetliso ba' mele. Phekolo ea insulin e nepahetseng, kalafo ea vithamine (tataiso B1, B6, B12, le C) e ntlafatsa boemo ba bakuli.

Na litlamorao tsa sulfonamides kapa che?

E, sulfonamides ke sehlopha se arohaneng sa lithibela-mafu, leha ho le joalo, kamora ho qaptjoa ha penicillin, ha ba ka ba kenyelelloa mokhatlong. Ka nako e telele, metsoako ea tlhaho feela kapa e entsoeng ka maiketsetso e ne e nkuoa e le "ea nnete", 'me sulfonamide ea pele le lihlahisoa tsa eona tse entsoeng ka theko ea mashala li ne li se joalo. Empa hamorao maemo a ile a fetoha.

Kajeno sulfonamides ke sehlopha se seholo sa lithibela-mafu tsa ketso ea bacteriostatic, e sebetsang khahlanong le mefuta e mengata ea likokoana-hloko ea ts'oaetso le ts'oaetso ea tšoaetso. Pejana, lithibela-mafu tsa sulfonamide hangata li ne li sebelisoa likarolong tse fapaneng tsa meriana. Empa ha nako e ntse e tsamaea, boholo ba bona bo lahlile bohlokoa ba bona ka lebaka la phetoho le ho hanyetsa baktheria, 'me matsatsing ana, liakhente tse kopaneng hangata li sebelisoa bakeng sa kalafo.

Sehlopha sa li-sulfonamides

Hoa hlokomeleha hore lithethefatsi tsa sulfonamide li ile tsa fumanoa 'me tsa qala ho sebelisoa bakeng sa merero ea bongaka pejana ho feta penicillin. Litlamorao tsa kalafo ea dae e meng ea liindasteri (haholoholo, expressionosyl kapa "red Cryptocide") li senotsoe ke setsebi sa baktheria sa Jeremane Gerhard Domagk ka 1934. Ka lebaka la komporo ena, e neng e sebetsa khahlanong le streptococci, o ile a folisa morali oa hae, 'me ka 1939 a ba setho sa likhau tsa Moputso oa Nobel.

Taba ea hore phello ea bacteriostatic ha e hlahisoe ke karolo e sa bonahaleng ea molek'hule, empa ke aminobenzenesulfamide (aka "white streptocide" le ntho e bonolo sehlopheng sa sulfonamides) e fumanoe ka 1935. Ke ka phetoho ea eona moo litokisetso tse ling tsohle tsa sehlopha li ileng tsa hlophisoa nakong e tlang, tse ngata eo e sebelisoang haholo ho tsa bongaka le meriana ea bongaka. Ho ba le pono e ts'oanang ea ts'ebetso ea antimicrobial, ba fapana ka litekanyetso tsa pharmacokinetic.

Lithethefatsi tse ling li kenella ka potlako le ho tsamaisoa, ha tse ling li ananeloa nako e telele. Ho na le phapang nakong ea ho chona ho tsoa 'meleng, ka lebaka leo mefuta e latelang ea sulfonamides e khetholloang:

• Nako e khuts'oane, halofo ea bophelo ba eona e ka tlase ho lihora tse 10 (streptocid, sulfadimidine).
• Nako e mahareng, eo T 1 /₂Lihora tse 10 - 24 - sulfadiazine, sulfamethoxazole.
• Ketso ea nako e telele (T halofo ea bophelo ho tloha matsatsing a 1 ho isa ho a mabeli) - sulfadimethoxin, sulfonomethoxin.
• Superlong - sulfadoxine, sulfamethoxypyridazine, sulfalene - e qotsitsoeng nako e telele ho feta lihora tse 48.

Sehlopha sena se sebelisoa bakeng sa meriana ea molomo, leha ho le joalo, ho na le li-sulfanilamides tse sa phatlalatsoang ho tsoa mokokotlong oa mpa (phthalyl sulfathiazole, sulfaguanidine), le sulfadiazine e etselitsoeng feela tšebeliso ea li-topical.

Lenane le felletseng la litokisetso tsa sulfanilamide

Lethathamo la lithibela-mafu tsa sulfanilamide tse sebelisitsoeng morieng oa kajeno o nang le mabitso a khoebo le sesupo sa mofuta oa tokollo li hlahisitsoe ka har'a tafole:

Lithibela tsohle tsa sulfonamide tse tsoang lenaneng la lithethefatsi li fumaneha hajoale. Mehloli e meng e bua ka lithethefatsi tse ling tsa sehlopha sena (mohlala, Urosulfan), tseo e leng khale li khaotsoe. Ntle le moo, ho na le lithibela-mafu tsa sulfanilamide tse sebelisoang feela litlhare tsa bongaka.

Mochine oa ts'ebetso oa sulfonamides

Ho emisa kholo ea likokoana-hloko (li-microorganism tsa gram-negative le gram, tse ling tsa protozoa) li bakoa ke ho tšoana ha sebopeho sa lik'hemik'hale tsa para-aminobenzoic acid le sulfonamide. PABA e hlokahala bakeng sa sele hore e kopanye lintho tsa bohlokoa ka ho fetisisa tsa nts'etsopele - folate le dihydrofolate. Leha ho le joalo, ha molek'hule ea eona e nkeloa sebaka ke sebfanilamide, ts'ebetso ena ea senyeha mme kholo ea pathogen ea emisa.

Lithethefatsi tsohle li kenngoa ka har'a tšilo ea lijo le ka lebelo le fapaneng la ho monya. Tsena tse sa phatlalatsoang ka har'a tšilo ea lijo li bontšoa kalafo ea tšoaetso ea mala. Ho ajoa ha linama ho tšoana hantle, metabolism e etsoa ka har'a sebete, excretion - haholo-holo ka liphio. Ka nako e ts'oanang, depot sulfonamides (e sebetsang ka nako e telele le e telele-ho feta) e kenella kahare ho li-renal tubules, tse hlalosang nako e telele ea bophelo.

Matšoao bakeng sa ts'ebeliso ea sulfonamides

Ho emisa kholo ea likokoana-hloko (li-microorganism tsa gram-negative le gram, tse ling tsa protozoa) li bakoa ke ho tšoana ha sebopeho sa lik'hemik'hale tsa para-aminobenzoic acid le sulfonamide. PABA e hlokahala bakeng sa sele hore e kopanye lintho tsa bohlokoa ka ho fetisisa tsa nts'etsopele - folate le dihydrofolate. Leha ho le joalo, ha molek'hule ea eona e nkeloa sebaka ke sebfanilamide, ts'ebetso ena ea senyeha mme kholo ea pathogen ea emisa.

Lithethefatsi tsohle li kenngoa ka har'a tšilo ea lijo le ka lebelo le fapaneng la ho monya. Tsena tse sa phatlalatsoang ka har'a tšilo ea lijo li bontšoa kalafo ea tšoaetso ea mala. Ho ajoa ha linama ho tšoana hantle, metabolism e etsoa ka har'a sebete, excretion - haholo-holo ka liphio. Ka nako e ts'oanang, depot sulfonamides (e sebetsang ka nako e telele le e telele-ho feta) e kenella kahare ho li-renal tubules, tse hlalosang nako e telele ea bophelo.

Allergy ho sulfonamides

Tekanyo e phahameng ea allergenicity ea litokisetso tsa sulfanilamide tse kopaneng ke bothata bo ka sehloohong ba ts'ebeliso ea bona. Ho thata ka ho fetisisa ntlheng ena ke kalafo ea pneumocystis pneumonia ho batho ba nang le tšoaetso ea HIV, hobane Biseptol ke lithethefatsi tse ikhethileng bakeng sa bona. Leha ho le joalo, ke sehlopheng sena sa bakuli moo menyetla ea ho ba le karohano ea mefuta-futa ea Co-trimoxazole e eketsang makhetlo a leshome.

Ka hona, ka allergy ho sulfanilamides, Biseptol le litokisetso tse ling tse kopaneng tse thehiloeng ho Co-trimoxazole li ngolisitsoe ho mokuli. Ho se mamelle hangata ho bonahatsoa ke makhopho a manyane a akaretsang, feberu le eona e ka hlaha, 'me sebopeho sa mali (neutro- le thrombocytopenia) se ka fetoha. Maemong a tebileng haholo - li-syndromes tsa Lyell le Stevens-Johnson, erythema multiforme, ho makala ha anaphylactic, edema ea Quincke.

Allergy ho sulfonamides e hloka ho felisoa ha moriana o e bakileng, hammoho le ts'ebeliso ea lithethefatsi tse khahlanong le allergic.

Litla-morao tse ling tsa sulfonamides

Lithethefatsi tse ngata sehlopheng sena li na le chefo ebile ha li mamelloe hantle, e neng e le lebaka la phokotso ea ts'ebeliso ea bona kamora ho sibolloa ha penicillin. Ntle le allergies, e ka baka mathata a dyspeptic, hlooho le mahlaba a ka mpeng, ho hloka thahasello, neuritis ea mokokotlo, hematopoiesis, bronchospasm, polyuria, dysfunction ea renal, nephropathy e bohloko, myalgia le arthralgia. Ho feta moo, menyetla ea ho ba le crystalluria e eketseha, ka hona, o hloka ho noa meriana e mengata le ho noa metsi a mangata a alkaline.

Ho sebelisana le meriana e meng

Ho hanyetsa ka matla le lithibela-mafu tse ling ho sulfonamides ha ho bonoe. Ha e kopantsoe le li-agent tsa hypoglycemic tsa molomo le li-coagulants tse sa tobang, phello ea bona ea ntlafatsoa. Ha ho kgothaletswe ho kopanya lithibela-mafu-sulfonamides hape le thiazide diuretics, rifampicin le cyclosporine.

Phapang ke efe pakeng tsa sulfonamides le sulfonamides

Leha ho na le mabitso a kopaneng, metsoako ena ea lik'hemik'hale e fapane haholo. Sulfonamides (khoutu ea ATX C03BA) ke diuretics - diuretics. Lithethefatsi tsa sehlopha li laetsoe khatello ea mali, puffiness, gestosis, lefu la tsoekere, botenya le mafu a mang a tsamaeang le ho bokellana ha mokelikeli 'meleng.

Sulfonamides

Sulfonamides - litlamorao tsa antimicrobial para (π)-aminobenzenesulfamide - sethala sa sulfanilic acid (para-aminobenzene sulfonic acid). Bongata ba lintho tsena li sebelisitsoe e le li-antibacterial agents ho tloha bohareng ba mashome a mabeli a lilemo. banyalani-Aminobenzenesulfamide - k'holeseterole e bonolo ka ho fetisisa - eo hape e bitsoang white Cryptocide mme e ntse e sebelisoa ho tsa bongaka. Ho rarahane ho feta sebopeho, sulfonamide expressionos (red streptocide) e ne e le setlhare sa pele sehlopheng sena mme ka kakaretso e le sethethefatsi sa pele sa antibacterial lefatšeng.

Ka 1934, G. o ile a fumana thepa ea antibacterial.Domagk. Ka 1935, bo-rasaense ba Setsing sa Pasteur (Fora) ba ile ba fumana hore ke karolo ea molek'hule ea sulfanilamide e neng e na le phello ea antibacterial, eseng sebopeho se e fang 'mala. Ho ile ha fumaneha hore "molao-motheo o sebetsang" oa lefutso le bofubelu ba lefufuble ke sulfanilamide, e thehiloeng nakong ea metabolism (streptocide, streptocide e tšoeu). Red streptocide ha e sa sebelisoa, 'me motheong oa molek'hule oa sulfanilamide palo e kholo ea lihlahisoa tsa eona li entsoe, tseo ba bang ba sebelisitsoeng haholo ho tsa bongaka.

Litekanyetso tsa Pharmacological

Sulfanilamides e sebetsa ka bongata ka bongata, ke hore, ba na le ts'ebetso ea chemotherapeic ho ts'oaetso e bakoang ke libaktheria tse ntle le gram, tse ling tsa protozoa (likokoana-hloko tsa mala, toxoplasmosis), chlamydia (e nang le trachoma, paratrachoma).

Ketso ea bona e amana haholo le tlolo ea sebopeho sa likokoana-hloko tsa lintho tse hola tse hlokahalang bakeng sa nts'etsopele ea bona - li-acid le dihydrofolic acid le lintho tse ling, molek'hule eo e kenyelletsang para-aminobenzoic acid. Mochine oa ts'ebetso o hokahana le sebopeho se tšoanang le sekhechana sa sulfanilamide le banyalani-aminobenzoic acid (PABA) - karolo e kaholimo ea enzyme dihydropteroate synthetase, e hlophisang dihydropteroic acid, e lebisang ho tlhodisanong ea thibelo ea dihokopthale ea synthetase. Sena, se lebisa pherekanong ho dihydropteroic dihydrofolate, ebe tetrahydrofolate, 'me ka lebaka leo, e le tlolo ea tlholeho ea motsoako oa li-acid tsa bacteric.

Ho fumana phello ea kalafo, li tlameha ho fuoa tekanyetso e lekaneng ho thibela monyetla oa likokoana-hloko tse sebelisang para-aminobenzoic acid e ka har'a lithane. Tekanyetso e sa lekanang ea lithethefatsi tsa sulfonamide kapa ho khaotsa kalafo ho sa le pele ho ka lebisa ho hlaha ha mefuta e meng e thibelang likokoana-hloko e sa khonehang ho nts'etsapele ketso ea sulfonamides. Boholo ba baktheria ea bohlokoa ka har'a kliniki e haelloa ke sulfonamides. Ho tlameha ho hopoloa hore lithethefatsi tse ling, molek'hule ea tsona e kenyelletsa karolo e setseng ea para-aminobenzoic acid (mohlala, novocaine), e ka ba le phello e boletsoeng ea antisulfanilamide.

Litekanyetso tsa Pharmacological |

2.5.2.2. Lithethefatsi tsa Sulfa

Sulfanilamides - li-antimicrobial agents, li-derivatives tsa sulfanilic acid amide (streptocide e tšoeu). Ho sibolla ha bona ho netefalitse polelo e boletsoeng esale pele ea P. Ehrlich mabapi le monyetla oa ho senya likokoana-hloko ka li-cytotoxic dintho tse ling. Setlhare sa pele sa sehlopha sena hlabiloe (streptocide e khubelu) thibela lefu la litoeba. tšoaetsoa ke lethal e bolaeang kotsi ka makhetlo a leshome ea hemolytic streptococcus.

Motheong oa molek'hule oa sulfanilamide halofong ea bobeli ea 30s, metsoako e meng e mengata e ne e entsoe (norsulfazole, ethazole, sulfazine, sulfacyl, jj.). Ho hlaha ha lithibela-mafu ho felisitse thahasello ho sulfonamides, empa ha ba lahleheloe ke bohlokoa ba bona ba bongaka, joale ba sebelisoa ka mokhoa o batsi "nako e telele" (sulfapyridazine, sulfalene, jj) mme haholo-holo lithethefatsi tse kopantsoeng (Co-trimoxazole le li-analogues tsa eona, tse kenyeletsang trimethoprim ho kenyelletsa sulfonamide) . Lithethefatsi li na le bongata ba liketsahalo tsa antimicrobial (litlamorao tse ntle le gram-negative, chlamydia, li-protozoa tse ling - likokoana-hloko tsa mala le toxoplasmosis, fungi ea pathogenic - actinomycetes, jj).

Sulfanilamides e arotsoe ka lihlopha tse latelang:

2. Lithethefatsi tse kenelletseng ka botlalo mokhoeng oa mpa, empa li pepesetsoa butle-butle ke liphio (e nkang nako e telele): sulfamethoxypyridazine (sulfapyridazine), sulfonomethoxin, sulfadimethoxin, sulfalene.

Lihlopheng tsa pele le tsa bobeli, tse kenelletseng hantle ka mpeng ea mpa, li sebelisetsoa ho alafa tšoaetso ea methapo, ea boraro - bakeng sa kalafo ea mafu a ka mpeng (lithethefatsi ha li nkoe le ho sebetsa ka leseli la tšilo ea lijo), ea bone - haholoholo, 'me ea bohlano (lithethefatsi tse kopaneng le trimethoprim) li sebetsa hantle. sebetsanang le tšoaetso ea methapo ea ho hema le ho ntša metsi, mafu a ka mpeng.

Mokhoa oa ketso. Sulfanilamides e baka bacteriostasis. Ke bahanyetsi ba tlholisano ba li-para-aminobenzoic acid (PABA), e hlokahalang bakeng sa likokoana-hloko ho etsa mofuta oa folic acid: ea morao-rao ka sebopeho sa coenzyme (dihydrofolate, tetrahydrofolate) e ameha ho thehoeng ha metheo ea purine le pyrimidine, e netefatsang kholo le kholo ea likokoana-hloko. Li-Sulfanilamides li haufi le sebopeho sa lik'hemik'hale ho PABA, ka hona li ts'oaroa ke sele e nyane ho fapana le PABA. Ka lebaka leo, motsoako oa folic acid o emisitsoe. Lisele tsa motho ha li khone ho kopanya folic acid (e tla le lijo), e hlalosang khetho ea ketso ea antimicrobial ea lithethefatsi tsena. Sulfanilamides ha e ame libaktheria tseo ka botsona li thehang PABA. Ka boteng ba pus, mali, lihlahisoa tsa tšilafalo ea lisele tse nang le palo e kholo ea PABA, meriana ena ha e sebetse. Meriana e thehang PABA ka lebaka la biotransformation (novocaine, dicaine) ke bahanyetsi ba sulfonamide.

Lithethefatsi tse kopaneng: co-trimoxazole (bactrim, biseptol), sulfatone, eo, ntle le lithethefatsi tsa sulfa (sulfamethoxazole, sulfamonomethoxine) li kenyelletsa trimethoprim, ke li-antibacterial tse sebetsang haholo. Trimethoprime thibela dihydrofolic acid reductase, e thibela phetoho ea eona ea ts'ebetso ea tetrahydrofolic acid. Ka hona, ka kenyelletso ea litokisetso tsa sulfanilamide tse kopaneng, eseng feela motsoako oa folic acid o thibetsoe, empa le phetoho ea eona ea coenzyme (tetrahydrofolate) e sebetsang. Lithethefatsi li na le ts'ebetso ea bactericidal khahlanong le li-bacteria tsa gram tse ntle le gram.

Mokhoa o ka sehloohong oa tsamaiso ea sulfonamides ke molomong. Ka mpeng e nyane, e kenella ka potlako ebile e kenelletse ka botlalo (ntle le lithethefatsi tse boima haholo - phthalazole, phthazine, salazosulfanilamides, e laetsoeng ts'oaetso ea mala), e tlama liprotheine tsa plasma maling, 'me ebe, ka mor'a nakoana, e lokollotsoe tlamong, e qala ho bonts'a ts'ebetso ea antimicrobial, ke mahala feela e bakang likokoana-hloko karoloana. Hoo e batlang e le sulfonamides kaofela e fetisetsa lithibelo tsa lithane hantle, ho kenyeletsa le hepatohematic, mali-bokong, le sethala. Li-biotransformed ka har'a sebete, tse ling li bolokiloe ka har'a li-bile (haholo-holo tse tšoarellang nako e telele, ka lebaka leo li sebelisoa ka katleho bakeng sa ts'oaetso ea pampiri ea phepelo ea methapo.

Mokhoa o ka sehloohong oa biotransformation ea sulfonamides ke acetylation. Li-metabolites tse nang le asiti li lahleheloa ke tšebetso ea tsona ea antibacteria, ha e qhibilihe habonolo, 'me tikolohong ea acidic, moroto o ka theha likristale tse senya kapa tsa koala methapo ea kutlo. Tabeng ea ts'oaetso ea ts'ebetso ea moroto, ho fanoa ka sulfonamides, e nang le acetylated hanyane mme e hlahisoa ka har'a moroto ka mokhoa oa mahala (urosulfan, etazole).

Mokhoa o mong oa biotransformation ke glucuronidation. Lithethefatsi tse ngata tse nkang nako e telele (sulfadimethoxine, sulfalene) li lahleheloa ke mosebetsi ka ho tlama glucuronic acid. Li-glucuronides tse hlahisoang li qhibiliha habonolo (ha ho na kotsi ea crystalluria).

Leha ho le joalo, ho beoa ha bona ba sa le banyenyane ho kotsi haholo, hobane ho se sebetse hantle ha phepelo ea glucuronyl (glucuronidation catalyst) ho lebisa ho bokellaneng ha sulfonamide maling le ho taoleng. Li-sulfonamides le lihlahisoa tsa tsona tsa biotransformacin li hlahisoa haholo ka har'a moroto. Ka lefu la liphio, excretion e ea lieha - litla-morao tse nang le chefo li ka hlaha.

Ho sa tsotelloe tšebetso eo a e khethileng, lithethefatsi tsa sulfonamide li fana ka mathata a mangata: ho kula ho sa foleng, ho senya litho tsa parenchymal (liphio, sebete), tsamaiso ea methapo, mali le litho tse etsang mali. Ho rarahana khafetsa ke crystalluria ka lebaka la crystallization ea sulfonamides le li-metabolites tsa tsona tse nang le acetylated maling, li-ureters le lesapo la mokokotlo. Ha a hlasimolohile, a etsa lehlabathe, majoe, a halefisa lisele tsa menoana, a koala mokhoa oa ho ntša metsi 'me a lebisa ho colic. Bakeng sa thibelo, ho nooa joala bo bongata, acidity ea moroto ea fokotseha (li-citrate kapa bicarbonate ea sodium li laetsoe ho alkalize urine). Ts'ebeliso ea metsoako e nang le sulfonamides ea 2-3 e sebetsa hantle haholo (monyetla oa "crystalluria" o fokotsehile ka makhetlo a 2-3).

Mathata a mali a bontšoa ke cyanosis, methemoglobinemia, hemolytic anemia, leukopenia, agranulocytosis.

Cyanosis e hlaha ka lebaka la thibelo ea erythrocyte carbonic anhydrase, e thatafatsang ho khutla ha carbon dioxide le oxygenation ea hemoglobin. Thibelo ea ts'ebetso ea li-peroxidase le li-catalases li khothalletsa ho bokella ha li-peroxides liseleng tse khubelu tsa mali le oxidation e latelang ea hemoglobin iron (methemoglobin). Lisele tse khubelu tsa mali tse nang le sulfa hemoglobin li lahleheloa ke matla a tsona a ho hlaka ebile li lys (hemolytic anemia).

Mokokotlong oa masapo tlasa ts'usumetso ea sulfonamides, ho ka bonoa tšenyo ea lisele tse bopa mali, e lebisang tlhabong ea agranulocytosis, anemia ea mali.

Ho boptjoa ha metsoako ea lisele tsa mali ho etsahala ka karolo e tlamang ea folic acid, eo 'mele o e fumanang ka lijo, kapa e le sehlahisoa sa bohlokoa sa saprophytic microbial flora ea mala: sulfonamides inhibit intestinal saprophytic microorganisms e nang le tšebeliso ea nako e telele,' me haeba ho sa lekane ho ja folic acid ka lijo, joale anemia ea aplasiki e ka hlaha.

Ho hlaha ha leukopenia ho bakoa ke thibelo ea li-enzyme tse nang le zinki, tse fumanehang ka bongata liseleng tse tšoeu tsa mali. Tšusumetso e tobileng ea sulfonamides ho leukocytes joalo ka melemo ea aniline le eona e bohlokoa.

Ketso ea sulfonamides tsamaisong ea methapo e bohareng e iponahatsa e le mokhoa oa ho tsekela, hlooho e bohloko, karabelo e potlakileng, khatello ea maikutlo. Tšenyo ea methapo ea methapo ea kutlo ka mokhoa oa neuritis, polyneuritis (hypovitaminosis B 1, mafutsana a choline acetylation).

Li-sulfanilamides, haholo-holo bactrim, ha lia lokela ho fuoa basali ba baimana, hobane lithethefatsi tsena li na le phello ea teratogenic mme li beha kotsi holima kholo ea "fetal". Basali ba mooki ha baa lokela ho nka li-sulfonamides, kaha li entsoe ka lebese.

Le ha bohlokoa ba sulfonamides bakeng sa boikoetliso ba bongaka bo sa tsoa fokotseha ka lebaka la palo e kholo ea mefuta e meng e hanyetsanang, lithethefatsi tse kopaneng li ntse li sebelisoa haholo: ts'ebetso e phahameng ea antibacterial, ho hanyetsa ho ntse ho hola butle, le liperesente tse tlase tsa mathata. E sebelisoa bakeng sa tšoaetso ea moroto le mala, mafu a ho hema (bronchitis, otitis media, sinusitis), co-trimoxazole e fuoe bakuli ba AIDS ba nang le pneumocystic pneumonia, e leng eona sesosa se ka sehloohong sa lefu la bakuli ba joalo.

Ha e sebelisoa ka holimo, ho lokela ho hopoloa hore lithethefatsi li sebetsa leqebeng le hloekileng feela, hobane boteng ba pus, tishu ea necrotic, le mali li na le bongata ba PABA, bo thibelang ts'ebetso ea antibacterial ea sulfonamides. Ka hona, ho hlokahala ho phekola leqeba pele, o hlapise ka hydrogen peroxide le li-antiseptics tse ling, ebe o sebelisa sethethefatsi sena. Ntle le moo, sulfonamides e thibela ho etsoa ha granerals, ka hona, nakong ea pholiso ea leqeba, ba tlameha ho nkeloa sebaka ke mekhoa e meng ea lehae.