Indlela yokusebenza ye antibiotics: ITEKISI

Wena wayenokuthi uphuhliso olululo yaba kokufunyanwa penicillin ekuqaleni kwenkulungwane yamashumi amabini. Ngexesha Second World War, olwa yokuqala wasindisa izigidi amajoni ababuleweyo ukusuka septicemia. Penicillin olusebenzayo kwaye iziyobisi ngexesha elifanayo zanela ezahlukahlukeneyo izifo ezinkulu kwizaphuko ezinzulu, nokulimala. Ekuhambeni kwexesha, oko kuhlanganiswa, kunye nezinye iindidi antibiotics.

iimpawu ngokubanzi

Namhlanje kukho inani elikhulu lweemveliso akwi kwihlabathi elikhulu antibiotics - izinto eziphuma zendalo okanye semi-zokwenziwa ukuba bayakwazi ukutshabalalisa amaqela athile ezincinane yayintsholongwane eyosulela okanye zinqanda ukukhula okanye ukuzala. Iindlela of action-ntsholongwane spectra kunokuba ezahlukeneyo. Ekuhambeni kwexesha, iindidi ezintsha nangokuthi kuhlenga-ntsholongwane. It azifani zabo kufuna systematization. Ekuhambeni kwexesha lethu, siye yamkela ukuhlelwa antibiotics ngokungqinelana indlela amanyathelo kunye ezininzi, ngokunjalo kubume imichiza. Ngokutsho indlela yazo yokusebenza wohlulwe:

• bacteriostats, leyo abayithintelayo ukukhula okanye yokuzala ezincinane izifo;
• microbicides, isandla kutshatyalaliswe iintsholongwane.

Iindlela ezisisiseko isenzo antibiotics:

• ephula udonga yeseli bacteria;
• inhibition protein kudibaniso kwiseli bacteria;
• ukuhlukunyezwa permeability le ndizayo cytoplasmic;
• inhibition RNA yokuqaphela.

antibiotics Beta-lactam - penicillins

Ngokutsho isakhiwo eekhemikhali ezi zihlanganisi zihlelwa ngolu hlobo lulandelayo.

antibiotics Beta-lactam. Indlela yokusebenza antibiotics lactam kuxhomekeke ekukwazini iqela ezisebenzayo ukubophelela enzayim ababandakanyekayo Yindibanisela peptidoglycan - neziseko inwebu olungaphandle iiseli silwanyana. Ngoko, loo nto, ekhululeke ukuyilwa ezindongeni, into leyo eyenza igalelo ekuyekeni ukukhula okanye lokwanda iintsholongwane. Beta-lactams babe zinetyhefu esezantsi, kwaye ngexesha elinye nemiphumo emihle bactericidal. Zimele iqela elikhulu yaye zahlulwe nomnye abe isakhiwo imichiza efanayo.

Penicillins - liqela kwezinto ukhululwe amathanga ezithile ngumngundo kunye nefuthe bactericidal. Indlela yokusebenza -ntsholongwane penicillin ngenxa yokuba ngokutshabalalisa udonga iseli ezincinane, ukuba ndingabonakalisi. Penicillins na imvelaphi yendalo okanye esondeleyo-zokwenziwa kwaye iikhompawundi ze emininzi ebanzi amanyathelo - ukuba isetyenziswe ukunyanga izifo ezininzi ezibangelwa streptococci kunye staphylococci. Ngaphezu koko, kufuneka ukuba impahla selectivity ngokwenza kuphela kwi-micro-eziphilayo, ngaphandle kokuchaphazela macro-eziphilayo. Penicillins kuneengxaki, ezibandakanya kukuvela ukuxhathisa kwegciwane noko. Of penicillin zixhaphakileyo zendalo G, penicillin asetyenziswa ukulwa usulelo meningococcal kwaye streptococcal ngenxa zinetyhefu esezantsi kunye nendleko eziphantsi. Noko ke, ukuze unikholekise ixesha elide kunokuba umzimba umzimba ukuba ichiza, ngaloo isehlisa ukusebenza kwayo. penicillins semi-eyenziweyo bavame livela zendalo ukuguqulwa imichiza zakubonelela iipropati ezinqwenelekayo - amoxicillin, ampicillin. La machiza kufuneka umsebenzi elingaphezulu ukuchasana iintsholongwane ukumelana biopenitsillinam.

Okunye beta-lactams

Cephalosporins afumaneka fungi kwegama elifanayo, nesakhiwo yabo iyafana ngesakhiwo penicillins echaza indlela efanayo ezingalunganga. Cephalosporins akhawunti ngenxa izizukulwana zazine. iziyobisi sizukulwana sokuqala asetyenziswa ngokufuthi unyango lwezifo abanomoya zibangelwa staphylococci okanye streptococci. Le cephalosporins sesibini nesesithathu isizukulwana esebenzayo ngakumbi ukulwa iintsholongwane ezimbi-Igram, kwaye nakwesesine isizukulwana iziyobisi - amachiza zinamandla osetyenziswayo ukuphembelela izifo kakhulu.

Carbapenems ngempumelelo ngokuvumelana gram-HIV, gram-HIV kunye anaerobic iintsholongwane. osemqoka yabo HIV ukungabikho ukumelana ziibhakteriya ukuba ichiza emva kwexesha elide isicelo sayo.

Monobactams kwakhona isicelo beta-lactams kunye zinendlela efanayo amanyathelo-ntsholongwane, na nkucetelo ezindongeni iseli iintsholongwane. Zisetyenziswa ukunyanga iintlobo ezahlukeneyo zamangenelela.

macrolides

Eli qela lesibini. Macrolides - antibiotics zendalo, apho kukho isakhiwo oluntsonkothileyo elibujikele. Bamele ring lactone moieties carbohydrate polynomial eqhotyoshelweyo. Ukususela inani athom kwekhabhoni ijikazi zixhomekeke kwiimpawu beziyobisi. Ukwahlula 14, 15 kunye nemixube-16-membered. Le spectrum yesenzo amagciwane ibanzi ngokwaneleyo. Indlela yokusebenza ye antibiotics kwiseli ngeentsholongwane kukuba ngokuhlanganisa nabo ribosomes ngoko kophulwa kwe protein kudibaniso esiseleni le silwanyana ngokuthi ziyibuyisela monomer Ngaphezu reactions ezintsha kwikhonkco peptide. Lokwandisa eziseleni amajoni omzimba, macrolides wenza kunye nokubulala intracellular amagciwane.

Macrolides kakhulu ezikhuselekileyo ngaphantsi ziyityhefu kwaye phakathi antibiotics ezaziwayo olusebenzayo ngokuchasene kuphela Igram-HIV, kodwa iintsholongwane ezimbi. ukusetyenziswa kwazo akukho bephawula ukusabela icala ezingathandekiyo. Le mithi luphawulwa ukusebenza bacteriostatic, kodwa zoqhaphelo eziphakamileyo, enokuba nempembelelo bactericidal kwi pneumococci kunye namanye amagciwane. Njengoko unendlela yokuvelisa macrolides zahlulwe zibe yendalo semisynthetic.

Ichiza yokuqala kwiklasi ye zendalo macrolides erythromycin Kwafunyanwa phakathi khulu lokugqibela leminyaka kwaye iye isetyenziswe ngempumelelo nxamnye iintsholongwane gram-HIV enganyangekiyo nxamnye penicillin. kwabonakala Isizukulwana esitsha lwamachiza kweli qela kwi 70s kwinkulungwane yama-20 kwaye zisetyenziswa kakhulu ukuza kuthi ga ngoku.

antibiotics Macrolide nayo semi - azolides kunye ketolides. Azolide I ring lactone kwi molecule, phakathi athom carbon yesithoba neyeshumi yayiquka nitrogen atom. Representative azolides azithromycin yi spectrum ezibanzi amanyathelo kwaye umsebenzi malunga gram-HIV kunye gram-HIV iintsholongwane, ezinye anaerobes. Kuyinto kakhulu isitali olune medium ngakumbi, xa kuthelekiswa ne-erythromycin, kwaye bangaqokelela kuyo. Azithromycin lisetyenziswa ezahlukahlukeneyo izifo phecana yokuphefumla, womchamo, kwesisu, ulusu kunye nabanye.

Ketolides walungisa ngokuthi kuqhotyoshelwe atom wesithathu ring nee lactone. Yokuba intsholongwane ngaphantsi mkhwa-ukwakha, xa kuthelekiswa ne macrolides.

tetracyclines

Tetracyclines i udidi polyketides. It antibiotics ebanzi-spectrum impembelelo bacteriostatic. Ummeli lokuqala kubo - chlortetracycline, eyedwa phakathi kwenkulungwane yokugqibela omnye iinkcubeko actinomycetes, nayo ayesithi unyulu. Kwiminyaka embalwa kamva oxytetracycline sele evela thanga ngulo mngundo efanayo. Ilungu lesithathu eli qela tetracycline, leyo wadalwa kuqala a loguqulelo chemical ithe yayo chloro, kunye nonyaka kamva nayo ingadibani actinomycetes. Yonke eminye imithi kwiqela tetracycline ezi yezabelo semi-zokwenziwa of ezi zinto.

Zonke ezi izinto ezifanayo kubume iikhemikhali neempawu umsebenzi nxamnye iintlobo ezininzi iintsholongwane gram-HIV kunye gram-HIV, ezinye iintsholongwane, lenyama. Zinyamezela ngamakhoboka kunye ezincane. Indlela yokusebenza ye antibiotics kwi iseli yebhaktiriya kukuba zokuyifihla kwinkqubo protein biosynthesis. Isenzo ezo molekyuli ichiza Igram-negative iintsholongwane baya kudlula kulo iiseli yi kwe- elula. Indlela elalana ye amasuntswana zintsholongwane ntsholongwane gram-HIV ayikaqondwa kakuhle, kodwa kukho intelekelelo yokuba iimolekyuli tetracycline basebenzisane ion zesinyithi ezithile ukuba xa iiseli iintsholongwane ukwenza iikhompawundi ezintsonkothileyo. Ngenxa yoko kukho umsantsa ezikwi ngexesha protein amagama eziyimfuneko ukuze iseli amagciwane. Amalinge wabonisa ukuba chlortetracycline bacteriostatic boxinzelelo ezaneleyo ukuze kuthintelwe iiprotini yokuqaphela, kodwa inhibition nucleic acid amagama kufuna eliphezulu lamanani ichiza.

Tetracyclines zisetyenziswa ekulweni isifo sezintso, zizifo ezahlukahlukeneyo eluswini, yokuphefumla kunye nezinye izifo ezininzi. Ukuba kuyimfuneko, bona indawo penicillin, kodwa kwiminyaka yakutshanje, ukusetyenziswa tetracyclines lehlile kakhulu, ngenxa ukuvela yokunganyangeki ezincinane kweli qela antibiotics. indima okugwenxa eyadlalwa ukusetyenziswa olwa njengoko isongezo, ukondla izilwanyana, nto leyo kwehle elapha beziyobisi ngenxa kukuvela ukuxhathisa kuyo. Ukuloyisa, baqeshwa kunye ukuhlanganiswa ngemithamo yokuba ngeendlela ezahlukeneyo amanyathelo elwa of antibiotics. Umzekelo, isiphumo unyango kunyuswa isicelo ngaxeshanye tetracycline streptomycin.

aminoglycosides

Aminoglycosides - antibiotics zendalo semi-zokwenziwa kunye kuluhlu olubanzi kakhulu lomsebenzi, equlethe kwi iintsalela molecule aminosaharidov. Waba streptomycin aminoglycoside yokuqala, owayengahlali nwe fungi ray embindini khulu lokugqibela leminyaka kwaye asetyenziswe kokubonakalayo ukunyanga ezahlukahlukeneyo izifo. Njengoko bactericide, antibiotics eqela wathi zisebenza nokuba ngesaphulelo ngamandla nezifo. Indlela yokusebenza ye antibiotics kwiseli ngeentsholongwane yi ukuyilwa iibhondi covalent kunye iiprothini kunye ribosomes silwanyana nokutshatyalaliswa protein kudibaniso kwi reactions iseli yebhaktiriya olomeleleyo. Akukaqondwa kakuhle indlela aminoglycoside isiphumo bactericidal, ngokuchaseneyo amanyathelo bacteriostatic of tetracyclines kunye macrolides nazo kuwuhlambela protein kudibaniso kwiiseli bacteria. Nangona kunjalo, kuyaziwa ukuba aminoglycosides besebenza kuphela phantsi kweemeko aerobic, ngoko babonisa ukusebenza phantsi zomzimba kunye nobonelelo egazini.

Emva zintsholongwane yokuqala - penicillin streptomycin, baza baqalisa ukuba njalo ngokubanzi asetyenziswe ukunyanga nasiphi na isifo ukuba kungekudala kakhulu bekukho ingxaki ekufumaneni Cya ezisetyenziswa kula machiza. Okwangoku, streptomycin isetyenziswa kakhulu xa idityaniswe nezinye isizukulwana entsha amayeza okunyanga isifo sephepha okanye, namhlanje izifo ezinqabileyo ezifana ezifana sibetho. Kwezinye iimeko eyabelwe kanamycin, nto leyo nayo isizukulwana yokuqala aminoglycoside olwa nawo. Noko ke, ngenxa yokuba ubungozi aphezulu kanamycin gentamicin okukhethwayo ngoku - ukulungiselela isizukulwana yesibini, kwesesithathu kunye nokulungiselela amikacin yi aminoglycoside - ke kunqabile kusetyenziswa ukukhusela rhurha kuwo iintsholongwane.

chloramphenicol

Chloramphenicol okanye chloramphenicol, i zintsholongwane yendalo kunye emininzi ebanzi inyathelo, olusebenzayo inani elikhulu eziphilayo Igram-akhabayo kunye navumelanayo-Igram, uninzi iintsholongwane ezinkulu. Isakhiwo chemical elithi nitrofenilalkilaminov, lwafunyanwa kuqala inkcubeko actinomycetes embindini kwinkulungwane yama-20, yaye kwiminyaka emibini kamva nayo kuhlelwe afana.

Chloramphenicol lubanesiphumo bacteriostatic kwi iintsholongwane. Indlela yokusebenza ye antibiotics kwi iseli yebhaktiriya kukuba ukucinezela umsebenzi lo kuvala inkqubo ukuyilwa iibhondi peptide ngakwicala leeprothini amagama xa ribosomes. ukuba chloramphenicol uxhathiso ntsholongwane uvela kancinane kakhulu. Ichiza asetyenziswe esifo izifo okanye shigellosis.

Glycopeptides kunye lipopeptides

Glycopeptides - a khompawundi peptide elibujikele ezo zintsholongwane yendalo okanye semisynthetic kunye spectrum imxinwa umsebenzi iintlobo ezithile ezincinane. Ukuba namandla nempembelelo bactericidal kwi iintsholongwane gram-HIV, kwaye endaweni penicillin kwimeko yokunganyangeki kuyo. Indlela yokusebenza ye antibiotics kwi Cya kungachazwa ukuyilwa konxulumano acid kunye peptidoglycan iseli eludongeni, ngokwenjenjalo abathintela kuyondelelaniswe zabo.

glycopeptide Okokuqala - vancomycin, yaveliswa evela actinomycetes, ndiwuthabathile kumhlaba India. It is a zintsholongwane wemvelo olusebenzayo Cya nkqu ngexesha lokwanda. Ekuqaleni, vancomycin yayisetyenziswa ilalela kwimeko penicillin nezidlo kuyo ekunyangeni izifo. Nangona kunjalo, ukwanda ukunganyangeki ngamachiza kube yingxaki enkulu. Kule minyaka ingama-80 yayifunyenwe teicoplanin - i-zintsholongwane evela kwiqela glycopeptides. Waye waqeshwa kwi izifo ezifanayo, yaye kunye gentamicin, unika iziphumo ezihle.

Ekupheleni kwenkulungwane yama-20, iqela elitsha antibiotics - lipopeptides ingadibani Streptomyces. Afana ke lipopeptides elibujikele. Le zintsholongwane kunye spectrum imxinwa amanyathelo, sibonise isiphumo bactericidal nxamnye gram-HIV neentsholongwane, kwaye staphylococci ukuba abamelana nemithi beta-lactam kunye glycopeptides.

Indlela yokusebenza-ntsholongwane ezahlukeneyo kakhulu kwabo sele kwaziwa - iifomu lipopeptide phambi ikhalsiyam ion obusenyongweni kunye iseli inwebu iintsholongwane leyo ekhokelela depolarization kunye nokuphazamiseka yayo leeprothini yokuqaphela, ukuze iseli ngolunya uyafa. Ummeli yokuqala kwiklasi ye lipopeptides - daptomycin.

Ngokumalunga daptomycin ukuze kuqatshelwe izinga ebalulekileyo yomsebenzi bactericidal, kwaye okona kubalulekileyo - ukungabikho cross-ukuxhathisa, okanye ubuncinane olucothayo kakhulu lasungulwa ngenxa yokuba kukho indlela entsha ngokupheleleyo ntshukumo antibiotics yafakwa isakhiwo kweziyobisi.

polyenes

Iqela elilandelayo - antibiotics polyene. Namhlanje kukho ukuphazamiseka enkulu izifo ezinzwaneni esiba nzima ukunyanga. Ukuphelisa kwazo izinto nokubola - antibiotics polyene yendalo okanye esondeleyo-zokwenziwa. Ichiza lokuqala nokubola isekhona phakathi kwenkulungwane lokugqibela baqalisa Nystatin, elo ingadibani kwinkcubeko Streptomyces. Ngeli xesha, i yezonyango kwakukho antibiotics polyene ezininzi, livela iintlobo zeenkcubeko amagciwane - griseofulvin, Levorinum kunye nabanye. Siye safumana nje ukusetyenziswa polyenes sele besizukulwana sesine. igama Common bavuka Bulelani ubukho iibhondi ezininzi kabini kule iimolekyuli.

Indlela yokusebenza-ntsholongwane polyene ngenxa ukuyilwa imixokelelwane imichiza kunye sterols iseli inwebu in nomngundo. Ngaloo ndlela Polyene molecule okulungiswe yeseli inwebu kunye neefom Ion igxunyekwe lijelo apho amacandelo ukwandisa iiseli ngokwangaphandle, ekhokelela ukupheliswa yayo. Ngeedosi ephantsi polyenes ilifa umsebenzi fungistatic kunye aphezulu - fungicide. Nangona kunjalo, umsebenzi wabo kungakhankanywanga kwiintsholongwane.

Polymyxin - antibiotics zendalo eziveliswa iintsholongwane ibihlungu. Xa unyango, baye asetyenziswe kwi-imi- 40 kwinkulungwane yokugqibela. Ezi imixube kwahluka ukusebenza bactericidal, nto leyo zibangelwa umonakalo inwebu cytoplasmic iiseli silwanyana ebangela intshabalalo yayo. Polymyxin olusebenzayo ukulwa iintsholongwane gram-HIV kwaye iintsholongwane kunqabile enamazinga. Noko ke, ubuthi ophezulu kakhulu sinqande ukusebenzisa kwabo kunyango. Zithako eli qela - sulfate polymyxin B kunye polymyxin sulfate M zisetyenziswa enqabile yaye kuphela amalungiselelo yolondolozo.

antibiotics antitumor

Ama-actinomycins akhiqizwa ngumbungulu oqhaqhaqhayo, unempembelelo ye-cytostatic. I-actinomycins yemvelo kwisakhiwo i-chromopeptides eyahlukileyo kuma-amino acids kumaketanga eep peptide, enokumisela umsebenzi wabo wezinto eziphilayo. I-Actinomycins ithatha ingqalelo kwiingcali njengezithandabuzo ezichasayo. Indlela yokusebenza kwabo yenziwa ngenxa yokwakhiwa kwezibophelelo ezizinzileyo zamaketanga zeep peptide zokulungiselela kunye ne-helix kabini ye-DNA ye-microorganism kunye nokukhutshwa ngenxa ye-synthesis ye-RNA.

I-Dactinomycin, efunyenwe kwiminyaka ye-60 ye-20 ye-20, yaba yipilisi yokuqala ye-antitumor efunyenwe kunyango lwe-oncological. Nangona kunjalo, ngenxa yenani elikhulu lemiphumo engalindelekanga le nkunkuma ayifumanekanga. Izidakamizwa ezithintekayo zifumaneke ngoku.

I-Anthracyclines zizinto ezinqabileyo kakhulu ezinqabileyo kwi-streptomycetes. Inkqubo yesenzo se-antibiotics idibaniswa nokubunjwa kwee-complexes ezintathu kunye ne-DNA ethungelwano kunye nokugqitywa kwezi ntambo. Inkqubo yesibini yesenzo sokulwa ne-antimicrobial isenzeka, ngenxa yokuveliswa kwama-radicals amahhala adibanisa iseli somzimba.

Phakathi kwe-anthracycline yemvelo, i-daunorubicin kunye ne-doxorubicin ingachazwa. Ukwahlulelwa kwee-antibiotics ngokwemigudu yesenzo kwiibhaktheriya zibahlukanisa njenge-bactericidal. Nangona kunjalo, i-toxicity yabo ephakamileyo yabangela ukuba bajonge iimveliso ezintsha ezithe zafunyanwa ngokuchanekileyo. Zininzi zazo zisetyenziswe ngempumelelo kwi-oncology.

Iintsholongwane zangexesha elide ziye zabandakanyeka kwiindlela zonyango kunye nobomi bomntu. Ndiyabulela, izifo ezininzi zatshatyalaliswa, ezo zingaphi iinkulungwane ezininzi zazingathatyathwa. Okwangoku, kukho uluhlu oluhlukeneyo lwala maqulunqa ukuba alufunwa kuphela ukuhlelwa kwee-antibiotics ngokwendlela kunye neembonakalo zenzo, kodwa nakweminye impawu ezininzi.