Impilo, Amalungiselelo
Lo mshini wezenzo kwamaphilisi: texte
Ungase bathi ukuthuthukiswa wamavukelambuso kwaba ukutholakala nge-penicillin akuzange e ekuqaleni kwekhulu lamashumi amabili. Phakathi kwempi yezwe yesibili, lo muthi lokuqala ukulondolozwa izigidi amasosha alimele kusukela septicemia. Penicillin ngempumelelo futhi ngezinye izidakamizwa ashibhile esifanayo kusukela ezihlukahlukene yizifo eziyingozi kanye waphuka sina, izilonda ukonakala. Ngokuhamba kwesikhathi, kwathiwa kwemiqondo, kanye nezinye amakilasi kwama-antibiotic.
izici Jikelele
Namuhla kukhona inqwaba imikhiqizo okuqondene nezwe enkulukazi yemithi elwa namagciwane - izinto odabuka yemvelo noma ephuma kabili zokwenziwa ukuthi unekhono ukubhubhisa amaqembu athile nezilwanyana ezincane pathogenic noma zivimbela ukukhula yabo noma ukukhiqizwa kabusha. Izinqubo yesenzo kwamaphilisi spectra kungaba ezahlukene. Ngokuhamba kwesikhathi, izinhlobo ezintsha kanye ukuhlela kabusha kwama-antibiotic. Kuyinto ngokwehlukahlukana kwabo kudinga systematization. Esikhathini sethu sibuyele emakhaya, samukela ngezigaba kwamaphilisi ngokuvumelana lo mshini wezenzo zebanga, kanye isakhiwo sazo sekhemikhali. Ngokusho indlela izenzo zaso uhlukaniswe:
- bacteriostats, okuyinto ukucindezela ukukhula noma ukukhiqizwa kabusha microorganism pathogenic;
- microbicides, ezinomthelela ukubhujiswa amagciwane.
Izinqubo eyisisekelo isinyathelo kwamaphilisi:
- kokunikezwa kwe-webhaktheriya cell udonga;
- okusithiyayo wamaprotheni zamagama kuseli webhaktheriya;
- ukwephulwa permeability we ulwelwesi cytoplasmic;
- okusithiyayo RNA zamagama.
Beta-lactam imithi elwa namagciwane - penicillins
Ngokusho isakhiwo amakhemikhali lezi zakhi ihlukaniswa kanje.
Beta-lactam antibiotic. Lo mshini wezenzo lactam imithi elwa namagciwane kuncike ikhono leqembu obusebenzayo ukubophela enzyme ehilelekile synthesis peptidoglycan - izisekelo uma kubanda ulwelwesi olungaphandle amaseli silwanyana. Ngakho, ke engasenamahloni kumiswa iseli izindonga, okuyinto enomthelela ukumisa ukukhula noma ukukhiqizwa kabusha amagciwane. Beta-lactams ube ubuthi ongaphakeme, futhi ngesikhathi esifanayo nomphumela omuhle amagciwane. Zimelela iqembu elikhulu futhi zihlukaniswe subgroups ukuthi abe efanayo amakhemikhali isakhiwo.
Penicillins - iqembu izinto ukhululeka amakoloni ezithile isikhunta futhi umphumela amagciwane. Lo mshini wezenzo kwamaphilisi penicillin akuzange kusize ngenxa yokuthi ngokubhubhisa odongeni cell microorganism, ukubhubhisa kubo. Penicillins kukhona odabuka yemvelo noma ephuma kabili zokwenziwa futhi compounds of a spectrum ebanzi isenzo - angasetshenziswa ekwelapheni izifo eziningi zibangelwa streptococci futhi staphylococci. Ngaphezu kwalokho, banayo impahla selectivity ngokwenza kuphela amagciwane, ngaphandle ezithinta vumelekile umzimba. Penicillins babe nemiphumela ethile engathandeki, ezifaka hlangana ukuhlahluba okuvela ukuzabalaza kwama-bacterium nalokho. Of ezivamile penicillin akuzange kusize zemvelo G, penicillin akuzange kusize ukuthi zisetshenziselwa ukulwa nezifo meningococcal futhi streptococcal ngenxa ubuthi bayo ongaphakeme futhi eziphansi. Nokho, ukwamukelwa eside kungaba amasosha omzimba omzimba izidakamizwa, ngaleyo ndlela kuncishiswe ekulenzeni libe namandla. Semi-zokwenziwa penicillins ngokuvamile ethathwe emvelo ngokuthulisa ukuguqulwa amakhemikhali ukuze udlulisele izakhiwo oyifunayo - amoxicillin, ampicillin. Le mithi abe umsebenzi ephakeme ngokumelene amagciwane amelana biopenitsillinam.
Okunye beta-lactams
Cephalosporins etholakala isikhunta of the gama elifanayo, nokwakheka kwawo kuyafana isakhiwo penicillins echaza ukusabela okufanayo ezingezinhle. akhawunti Cephalosporins kwaze kwadlula izizukulwane ezine. izidakamizwa isizukulwane yokuqala asetshenziselwa kaningi ukwelapha izifo omnene zibangelwa staphylococci noma streptococci. Eyesibili neyesithathu cephalosporins isizukulwane ngaphezulu asebenzayo ngokumelene amagciwane Gram-negative, futhi kwesizukulwane sesine ketshezi - izidakamizwa ezinamandla kakhulu esetshenziswa ukuthonya ngamagciwane okunzima.
Carbapenems ngempumelelo isinyathelo igremu-HIV, amalutshwana-negative futhi anaerobic amagciwane. sici sabo esihle yisona ukungabi khona ukuzabalaza kwama-bacterium emuthini ngisho nangemva kwenkathi ende uhlelo lwayo lokusebenza.
Monobactams ziyasebenza nakubantu beta-lactams futhi ube indlela efanayo isinyathelo kwamaphilisi, nethonya ezindongeni cell kwamagciwane. Basuke asetshenziselwa ukwelapha ezihlukahlukene izifo ezahlukene.
macrolides
Lona iqembu lesibili. Macrolides - imithi elwa namagciwane yemvelo, okuyinto akheke eziyinkimbinkimbi eyindilinga. Zimelela polynomial lactone indandatho enamathiselwe carbohydrate moieties. Kusukela kuma-athomu e-carbon esiyingini kuxhomeke izakhiwo zomuthi. Hlukanisa 14-, 15- futhi compounds 16-membered. Nomkhakha we isinyathelo amagciwane ubanzi ngokwanele. Lo mshini wezenzo kwamaphilisi esitokisini microbial iwukuba ukusabela nabo ribosomes futhi ngaleyo ndlela ukwephulwa wamaprotheni zamagama kuseli ye silwanyana ngu ezivimbela entsha monomer kwalokho ukusabela iketango peptide. Yebo, ukuqongelela e omzimba amaseli, macrolides wenziwa kubulawe intracellular kwamagciwane.
Macrolides ziphephile kakhulu futhi kancane ezinobuthi futhi phakathi kwemithi elwa namagciwane eyaziwa ngempumelelo yokulwa hhayi kuphela Gram-HIV, kodwa amagciwane ezimbi. ukusetshenziswa kwabo ningagcini engathandeki ohlangothini ukusabela. Lezi imithi ngokweqile zifana nokuthela libhekene umphumela bacteriostatic, kodwa at lokuhlala eliphezulu, ingase ibe nomphumela amagciwane ku pneumococci namanye nezilwanyana ezincane. Njengoba indlela ngokukhiqiza macrolides zihlukaniswe yemvelo kanye semisynthetic.
Umuthi wokuqala iziqu ekilasini zemvelo macrolides erythromycin etholwe phakathi nekhulu leminyaka eledlule futhi iye yasetshenziswa ngempumelelo ngokumelene amagciwane igramu-HIV ukumelana ngokumelene penicillin akuzange kusize. Isizukulwane esisha izidakamizwa kule Bavele 70s kwekhulu lama-20 futhi kusetshenziswa kakhulu kuze kube manje.
imithi elwa namagciwane Macrolide nazo lulwimi - azolides futhi ketolides. Azolide I lactone indandatho engqamuzaneni, phakathi lesishiyagalolunye kuya kweleshumi ama-athomu carbon kuhlanganisiwe nitrogen athomu. Omele azolides azithromycin kuyinto spectrum ezibanzi yesenzo nomsebenzi maqondana igremu-HIV futhi igremu-negative amagciwane, abanye anaerobes. Kuyinto esitebeleni okuningi ku-medium-esidi, kunalapho erythromycin, futhi bangathola amaphuzu kulo. Azithromycin isetshenziswa ezihlukahlukene izifo yaleli pheshana yokuphefumula, ngomgudu womchamo, wamathumbu, isikhumba kanye nabanye.
Ketolides okulungiselelwe axube athomu lwesithathu keto lactone indandatho. Mancane amagciwane sekuwumkhuba, uma kuqhathaniswa nabangu macrolides.
tetracyclines
Tetracyclines ikilasi ka polyketides. It imithi elwa namagciwane ezibanzi-spectrum ithonya bacteriostatic. Omele wokuqala wabo - chlortetracycline, ahlukanisa phakathi nekhulu leminyaka eledlule omunye Emasikweni actinomycetes, obizwa nangokuthi amakhowe akhishwa imisebe yalo. Eminyakeni embalwa kamuva oxytetracycline itholiwe kusuka ikoloni ukhunta efanayo. Ilunga wesithathu leli qembu tetracycline, yakhishwa okokuqala adalwe ukuguqulwa amakhemikhali chloro yayo esuselwe, futhi ngemva konyaka futhi wahlukaniswa actinomycetes. Zonke ezinye izidakamizwa tetracycline beqembu nemikhiqizo semi zokwenziwa of lezi zakhi.
Zonke lezi zinto zifana ngezindlela chemical isakhiwo nezakhiwo umsebenzi lokulwa nezinhlobo eziningi zama-bacterium igremu-HIV futhi igremu-negative, abanye amagciwane, lenyama. Ziyakwazi ukumelana imilutha nezinto ezincane eziphilayo. Lo mshini wezenzo kwamaphilisi cell webhaktheriya kuyinto yokulicindezela enqubeni wamaprotheni biosynthesis. Isenzo yezinhlayiya izidakamizwa e Gram-negative amagciwane zidlula ku amaseli by okusheshayo elula. Mshini sokungena izinhlayiya-antibiotic e amagciwane igramu-HIV ayikaqondwa kahle, kodwa kukhona kokuqagela ukuthi tetracycline molecule uxhumane ion of izinsimbi ezithile ezisebusweni amaseli-bacterium ukwakha compounds eziyinkimbinkimbi. Ngakho kukhona igebe esikuziphathimandla ngesikhathi amaprotheni zamagama ezidingekile cell virus. Ukuhlolwa wafakazela ukuthi chlortetracycline bacteriostatic lokuhlala esanele zivimbela amaprotheni zamagama, kodwa okusithiyayo of nucleic acid zamagama kudinga lokuhlala eliphezulu zomuthi.
Tetracyclines asetshenziswa ekulweni nesifo sezinso, tesikhumba ahlukahlukene, zokuphefumula kanye nezinye izifo eziningi. Uma kudingeka, esikhundleni penicillin akuzange kusize, kodwa eminyakeni yamuva, ukusetshenziswa tetracyclines kakhulu kwehle, ngenxa ukuvela ukumelana nezilwanyana ezincane kuleli qembu kwama-antibiotic. indima Negative eyadlalwa ukusetshenziswa antibiotic i okufakiwe kuze kokudla kwezilwane, okuholela kwehle izakhiwo zokwelapha zomuthi ngenxa nesenzakalo yokumelana ke. Ukuze unqobe ke, amiswa nge inhlanganisela yemithi ehlukene kokuba indlela ezahlukene isinyathelo elwa namagciwane kwama-antibiotic. Ngokwesibonelo, umphumela ukwelashwa okuthuthukiswa isicelo ngesikhathi esisodwa tetracycline ne-streptomycin.
aminoglycosides
Aminoglycosides - imithi elwa namagciwane yemvelo kanye lulwimi zokwenziwa nge spectrum ezibanzi kakhulu yomsebenzi, eliqukethe e izinsalela-molecule aminosaharidov. Waba aminoglycoside streptomycin lokuqala ukuzihlanganisa amakoloni ray isikhunta phakathi nekhulu leminyaka eledlule futhi ngenkuthalo esetshenziswa ekwelashweni kwe-ezihlukahlukene nezifo. Njengoba bactericide, imithi elwa namagciwane yeqembu wathi kuphumelela ngisho ngesikhathi amasosha omzimba encishisiwe kakhulu. Lo mshini wezenzo kwamaphilisi esitokisini microbial Ukwakheka kwezitho izibopho eziqinile covalent ne amaprotheni ribosomes silwanyana ukubhujiswa amaprotheni zamagama e-webhaktheriya iseli ukusabela. Bengayiqondi ngokugcwele indlela aminoglycoside umphumela amagciwane, kunokusebenza isinyathelo bacteriostatic ka tetracyclines futhi macrolides nazo ziphula amaprotheni zamagama kumaseli virus. Nokho, kuyaziwa ukuthi aminoglycosides abakhuthele kuphela ngaphansi kwezimo aerobic, ngakho ukukhombisa kahle ongaphakeme ezicutshini nge abampofu liningi igazi.
Ngemva lo muthi lokuqala - penicillin ne-streptomycin, baqala ukuba ngakho kabanzi ekwelapheni isifo yimuphi ukuthi maduze kwakukhona nenkinga yokuthola nezilwanyana ezincane esetshenziswa le mithi. Okwamanje, i-streptomycin isetshenziswa ngokuyinhloko lihambisana namanye isizukulwane yakamuva izidakamizwa ukuze aphathe sofuba noma enjalo, namuhla izifo ezingavamile ezifana isifo. Kwezinye izimo babelwe kanamycin, okuyilona elisebenzayo futhi isizukulwane sokuqala aminoglycoside antibiotic. Nokho, ngenxa ubuthi eliphezulu kanamycin gentamicin okwamanje ayethanda - ukulungiswa isizukulwane sesibili, kwesizukulwane sesithathu ukulungiswa amikacin kuyinto aminoglycoside - it is kuyaqabukela esetshenziswa ukuvimbela ukuluthwa nalokho nezilwanyana ezincane.
chloramphenicol
Chloramphenicol noma chloramphenicol, kuyinto-antibiotic engokwemvelo nge spectrum ebanzi isinyathelo, esebenzayo ku inqwaba Gram-HIV futhi Gram-negative eziphilayo, eziningi amagciwane ezinkulu. On isakhiwo sazo sekhemikhali isuselwe nitrofenilalkilaminov, labonakala okokuqala etholakala nesiko actinomycetes phakathi nekhulu lama-20, futhi ngemva kweminyaka emibili futhi kuhlelwe umqondo amakhemikhali.
Chloramphenicol kunomphumela bacteriostatic ku nezilwanyana ezincane. Lo mshini wezenzo kwamaphilisi cell webhaktheriya kuyinto ukucindezela umsebenzi we kulethe kumiswa inqubo peptide izibopho amaprotheni zamagama lapho ribosomes. ukuze chloramphenicol ukumelana in amagciwane eba kancane kakhulu. Umuthi elisetshenziswa yi-typhoid isifo noma shigellosis.
Glycopeptides futhi lipopeptides
Glycopeptides - a eyindilinga peptide compounds okuyizinto-antibiotic engokwemvelo noma semisynthetic nge spectrum emincane umsebenzi amagciwane athile nezilwanyana ezincane. Bona kunethonya nomphumela amagciwane ku amagciwane igramu-HIV, futhi Ungashintshanisa penicillin akuzange kusize uma ukumelana naso. Lo mshini wezenzo kwamaphilisi ku nezilwanyana ezincane zingachazwa ngezinqubo kumiswa ukuxhumana nge-amino acid kanye cell udonga peptidoglycan, kanjalo abacindezela zamagama abo.
glycopeptide Okokuqala - vancomycin, lalikhishwa actinomycetes, othathwe lakwa-India. Kuyinto-antibiotic engokwemvelo ukuthi iyasebenza ngokumelene ezincane, ngisho zikhwelwe. Ekuqaleni, vancomycin yayisetshenziswa njengesikhungo esikhundleni uma penicillin akuzange kusize yokungezwani komzimba ukuze ke ekwelapheni izifo. Nokho, ukwanda yokumelana nomuthi sekuyinkinga enkulu. Eminyakeni engu-80 etholwe teicoplanin - i-antibiotic kusukela iqembu glycopeptides. Wamiswa ngesikhathi izifo efanayo, futhi lihambisana gentamicin, ubapha imiphumela emihle.
Ekupheleni kwekhulu lama-20, iqembu elisha kwamaphilisi - lipopeptides behlukene Streptomyces. Amakhemikhali zingabantu lipopeptides eyindilinga. Lokhu-antibiotic nge spectrum emincane isinyathelo, bembonisa nomphumela amagciwane ngokumelene amagciwane igramu-HIV, futhi staphylococci amelana beta-lactam izidakamizwa glycopeptides.
Lo mshini wezenzo kwamaphilisi ngokuphongoza salabo abaziwa kakade - amafomu lipopeptide ebukhoneni calcium ion izibopho eziqinile ne ulwelwesi cell-bacterium okuholela depolarization futhi ukuphazamiseka yayo amaprotheni zamagama, ukuze cell ezinonya uyafa. Omele lokuqala ekilasini lipopeptides - daptomycin.
Nge kungenzeka ngokuphathelene daptomycin kuqashelwe ngesilinganiso abalulekile umsebenzi amagciwane, futhi okubaluleke - ukuntuleka cross-Ukumelana, noma okungenani kakhulu kancane lasungulwa ngenxa yokuthi indlela entsha ngokuphelele yesenzo kwamaphilisi lithathwa isakhiwo ketshezi.
polyenes
Iqembu elilandelayo - imithi elwa namagciwane polyene. Namuhla kukhona yokwanda omkhulu izifo fungal kuthiwa kunzima ukuyelapha. Ukuze ulwe nabo kukhona izinto antifungal - zemvelo noma ephuma kabili zokwenziwa polyene antibiotic. Umuthi wokuqala antifungal namanje phakathi nekhulu leminyaka eledlule waqala Nystatin, okwakubekelwa behlukene Streptomyces isiko. Phakathi nale nkathi, kwezokwelapha kuhlanganisiwe polyene imithi elwa namagciwane amaningi, lisuselwa encazelweni ezihlukahlukene fungal amasiko - griseofulvin, Levorinum nabanye. Sithole nje ukusetshenziswa polyenes isivele kwesizukulwane sesine. Igama elijwayelekile sebewelele sibonga khona izibopho eziningana kabili amangqamuzana.
Lo mshini wezenzo ka polyene imithi elwa namagciwane ngenxa ukwakheka izibopho zamakhemikhali ne sterols cell ulwelwesi e isikhunta. ngaleyo ndlela Polyene-molecule linamathele ulwelwesi cell kanye namafomu Ion iwumzila yezingxenye ukunweba amaseli ngaphandle nibonakala okuholela ukuqedwa yayo olunezintambo. Ngemithamo ongaphakeme polyenes ifa umsebenzi fungistatic futhi okusezingeni eliphezulu - fungicide. Nokho, umsebenzi wabo engamboziwe lamagciwane.
Polymyxin - imithi elwa namagciwane ngoba zivunywa indawo kwakhiqiza ngu namagciwane asenhlabathini spore. Therapy, baye asetshenziswe-yalolucwaningo 40 ekhulwini elidlule leminyaka. Lezi ukwakhiwa kuhluke umphumela amagciwane, okuyinto kubangelwa ukulimala ulwelwesi cytoplasmic we silwanyana amaseli okubangela ukubhujiswa kwalo. Polymyxin ngempumelelo ngokumelene amagciwane igramu-negative futhi nezilwanyana ezincane akuvamile umlutha. Nokho, ubuthi abawasebenzisayo kukhawulela ukusetshenziswa kwabo kokwelashwa. Compounds yaleli qembu - polymyxin B sulfate kanye polymyxin sulfate M asetshenziswa kuyaqabukela kuphela njengoba amalungiselelo Reserve.
antitumor imithi elwa namagciwane
Actinomycin bakhiqiza ezinye isikhunta ray, nethonya cytostatic. actinomycins ngokwemvelo kwi isakhiwo kukhona hromopeptidami ezihlukahlukayo amino acid e amaketanga peptide ukuthi ukunquma umsebenzi oyizalayo. Actinomycin amehlo ongoti like antitumor antibiotic. Lo mshini wezenzo ngenxa ekwakhekeni izibopho esitebeleni ngokwanele of peptide kwagqashuka amaketanga kuzozonke izidakamizwa ne double Helix DNA lesi silwanyana futhi ngaleyo ndlela ekuvimbeni zamagama RNA.
Dactinomycin, kuphumele 60s kwekhulu lama-20, kuba anticancer ejenti lokuqala okuyinto ithole ukusetshenziswa e therapy oncologic. Nokho, ngenxa inani elikhulu yemiphumela emibi lokhu izidakamizwa kuyaqabukela esetshenziswa. Manje esasizithole izidakamizwa bakhuthele antineoplastic.
Anthracyclines - umenzeli sinamandla kakhulu anti-isimila behlukene Streptomyces. Lo mshini wezenzo kwamaphilisi elihlobene ne kumiswa izakhiwo ternary ngamaketanga DNA futhi kwalezi zibopho ikhefu. Futhi indlela yesibili okungenzeka isenzo elwa namagciwane ngenxa ukukhiqizwa radicals khulula ukuthi oxidize amangqamuzana omdlavuza.
Of anthracyclines yemvelo kungenziwa ngokuthi daunorubicin futhi doxorubicin. Ukwahlukanisa kwamaphilisi ngokuvumelana indlela izenzo zaso ku amagciwane libabiza microbicides. Nokho, ubuthi babo okusezingeni eliphezulu ophoqelelwe ukucinga compounds entsha okuye kwenzelwa synthetically. Abaningi babo ziye zasetshenziswa Oncology ngempumelelo.
Sekuyisikhathi eside Nemithi Elwa Namagciwane babe yingxenye kwezokwelapha futhi ukuphila komuntu. Siyabonga kubo, bahlulwa izifo eziningi, okwaphela amakhulu eminyaka kuthiwa aselapheki. Okwamanje, kukhona izinhlobonhlobo zezinto lezi zakhi, okudinga hhayi kuphela ngezigaba kwamaphilisi ngokuvumelana lo mshini wezenzo kanye spectrum, kodwa futhi kwamanye izici eziningi.
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