Ginshikai na mataki na maganin rigakafi: texte

Kana iya ce cewa juyin juya halin Musulunci ci gaba da aka gano penicillin a farkon karni na ashirin. A lokacin yakin duniya na biyu, na farko da kwayoyin ajiye miliyoyin rauni sojoji daga septicemia. Penicillin zama tasiri da kuma a lokaci guda mai rahusa kwayoyi daga da dama tsanani cututtuka da tsanani samu karaya, kwamin na tara raunuka. A tsawon lokaci, shi aka hada, da sauran azuzuwan na maganin rigakafi.

Janar halaye

Yau akwai babban adadin kayayyakin na zuwa sararin duniya na maganin rigakafi - abubuwa na halitta ko Semi-roba asalin cewa suna da ikon hallaka wasu kungiyoyin na pathogenic microorganisms ko hana su girma, ko haifuwa. A sunadaran da mataki na maganin rigakafi a jere iya zama daban-daban. A tsawon lokaci, sabon iri da kuma gyare-gyare na maganin rigakafi. Shi ne su bambancin bukatar amfaninsa. A zamaninmu, muna soma wani rarrabuwa na maganin rigakafi bisa ga tsarin ba da aikin da iyaka, kazalika a sinadaran tsarin. Bisa ga tsarin ba da aikin ne zuwa kashi:

• bacteriostats, wanda kashe da ci gaban ko haifuwa na pathogenic microorganisms.
• microbicides, wanda da taimako zuwa ga halaka da kwayoyin cuta.

Ainihin sunadaran da mataki na maganin rigakafi:

• take hakkin da kwayan cell bango.
• hanawa na gina jiki kira a cikin kwayan cell.
• take hakkin permeability na cytoplasmic membrane.
• hanawa na RNA kira.

Beta-lactam maganin rigakafi - penicillins

Bisa ga sinadaran tsarin na wadannan mahadi suna classified kamar haka.

Beta-lactam maganin rigakafi. Ginshikai na mataki lactam maganin rigakafi dogara da ikon na aikin kungiyar su ɗaure da enzymes da hannu a cikin kira na peptidoglycan - kwasfa na matsanancin membrane na kananan kwayoyin Kwayoyin. Saboda haka, shi hana samuwar cell ganuwar, wanda na taimaka wa lõkacin fatara da ci gaban ko haifuwa na kwayoyin. Beta-lactams da low yawan guba, da kuma a lokaci guda mai kyau bactericidal sakamako. Su wakilci mafi girma a kungiyar da kuma ya kasu kashi subgroups da cewa suna da irin wannan sinadaran tsarin.

Penicillins - suna da wani rukuni na abubuwa saki daga wasu mazauna kyawon tsayuwa da bactericidal sakamako. Ginshikai na mataki na maganin rigakafi penicillin saboda gaskiyar cewa ta lalata cell bango na kwayoyin, sun hallaka su. Penicillins ne na halitta, ko Semi-roba asalin da suke mahadi mai fadi bakan na mataki - su za a iya amfani da magani na da yawa cututtuka da streptococci da staphylococci. Bugu da kari, suna da dukiya na selectivity da aiki kawai a kan micro-kwayoyin, ba tare da shafi Macro-kwayoyin. Penicillins da drawbacks, wanda sun hada da abin da ya faru na kwayan juriya a cikinta. Daga cikin na kowa halitta penicillin G, penicillin da cewa ana amfani da su yãƙi meningococcal da streptococcal cututtuka saboda da low yawan guba da kuma low cost. Duk da haka, ga dogon lokacin da yarda iya zama cikin jiki ta rigakafi da miyagun ƙwayoyi, game da shi, rage ingancinta. Semi-roba penicillins ake kullum samu daga halitta da sinadaran gyara don goya so Properties - amoxicillin, ampicillin. Wadannan kwayoyi da hakan aiki da kwayoyin cuta resistant zuwa biopenitsillinam.

Sauran beta-lactams

Cephalosporins aka samu daga fungi na wannan sunan, kuma su tsari ne kama da tsarin penicillins da ya bayyana wannan m dauki. Cephalosporins asusu na hudu zamaninsu. farko tsara kwayoyi suna amfani da mafi sau da yawa da magani daga m cututtuka suna lalacewa ta hanyar staphylococci ko streptococci. Biyu da na uku ƙarni cephalosporins mafi aiki da gram-korau kwayoyin cuta, da kuma tsara ta huɗu na abu - mafi m kwayoyi amfani da tasiri mai tsanani cututtuka.

Carbapenems yadda ya kamata aiki a kan gram-tabbatacce, gram-korau da anaerobic kwayoyin. Su tabbatacce alama ne babu kwayan juriya ga miyagun ƙwayoyi ko da bayan wani dogon lokaci na aikace-aikace.

Monobactams ma nema to beta-lactams da kuma samun irin wannan inji na mataki na rigakafi, ne tasiri a cell ganuwar da kwayoyin cuta. Suna amfani da su bi wani iri-iri daban-daban cututtuka.

macrolides

Wannan shi ne karo na biyu da kungiyar. Macrolides - halitta maganin rigakafi, wanda da wani hadadden cyclic tsarin. Su wakiltar polynomial lactone zobe a haɗe carbohydrate moieties. Daga cikin yawan carbon atoms a zobe dogara ne a kan kaddarorin da miyagun ƙwayoyi. Rarrabe 14-, 15- kuma 16-membered mahadi. Da bakan mataki na microbes ne fadi da isa. Ginshikai na mataki na maganin rigakafi kan da ake dasu cell ne ta maida martani su tare da ribosomes kuma, da ita take hakkin na gina jiki kira a cikin cell na kananan kwayoyin da inhibiting sabon monomer Bugu da kari halayen da peptide sarkar. Tara a rigakafi da tsarin Kwayoyin, macrolides yi da kuma kwayuka kisan microbes.

Macrolides ne mafi aminci da kasa mai guba da kuma daga cikin da aka sani maganin rigakafi tasiri da ba kawai gram-tabbatacce, amma korau kwayoyin. Su yi amfani da ba a lura ba a ke so gefen halayen. Wadannan maganin rigakafi ne halin da bacteriostatic sakamako, amma a high yawa, zai iya samun wani bactericidal sakamako a kan pneumococci da kuma wasu wasu kwayoyin. A matsayin hanya ga samar da macrolides kasu kashi na halitta da kuma semisynthetic.

A farko miyagun ƙwayoyi daga aji na halitta macrolides erythromycin aka samu a tsakiyar karni na karshe kuma an yi amfani da nasarar da gram-tabbatacce kwayoyin resistant da penicillin. Wani sabon ƙarni na kwayoyi a cikin wannan kungiya ta bayyana a cikin 70s na karni na 20th kuma yadu amfani ya zuwa yanzu.

Macrolide maganin rigakafi ne ma Semi - azolides da ketolides. Azolide The lactone zobe a cikin DNA, tsakanin tara da goma carbon atoms hada da nitrogen zarra. Wakilin azolides azithromycin ne m bakan da aikin da kuma aiki zuwa ga gram-tabbatacce kuma gram-korau kwayoyin cuta, wasu anaerobes. Yana da yafi barga a wani acidic matsakaici, kamar yadda idan aka kwatanta da erythromycin, da kuma iya tara a shi. Azithromycin da ake amfani a da dama cututtuka na numfashi fili, urinary fili, hanji, fata da sauransu.

Ketolides shirya by attaching da uku zarra keto lactone zobe. Su kasa al'ada-forming kwayoyin cuta, idan aka kwatanta da macrolides.

tetracyclines

Tetracyclines ne a aji na polyketides. Yana maganin rigakafi m-bakan bacteriostatic tasiri. A farko wakilin su - chlortetracycline, aka ware a tsakiyar karni na karshe daya daga cikin al'adu na actinomycetes, wanda kuma ake kira annuri namomin kaza. A 'yan shekarun baya oxytetracycline an samu daga cikin mallaka na wannan naman gwari. The uku memba na wannan kungiya shi ne tetracycline, wanda aka fara halitta da wani sinadaran gyara ta chloro wanda aka samu, da kuma wani shekara daga baya kuma ware daga actinomycetes. All sauran kwayoyi na tetracycline kungiyar ne Semi-roba Kalam na wadannan mahadi.

Duk wadannan abubuwa suna kama a sinadaran tsarin da kaddarorin aiki da yawa siffofin gram-tabbatacce kuma gram-korau kwayoyin cuta, wasu ƙwayoyin cuta, da kuma protozoa. Su ne resistant zuwa buri da kuma kwayoyin. Ginshikai na mataki na maganin rigakafi a kwayan cell ne zuwa kashe shi a cikin tsari na gina jiki biosynthesis. A mataki na miyagun ƙwayoyi kwayoyin a gram-korau kwayoyin da suka wuce a cikin sel by sauki yadawa. Ginshikai na shigar azzakari cikin farji daga cikin kwayoyin barbashi a gram-tabbatacce kwayoyin da aka har yanzu talauci gane, amma akwai jita-jitar cewa tetracycline kwayoyin hulɗa tare da ions na wasu karafa da cewa su ne a cikin kwayoyin jikinsu da kwayoyin cuta ta samar da hadaddun mahadi. Kamar wancan akwai rata a cikin sarkar a lokacin gina jiki kira zama dole ga kwayan cell. Gwaje-gwaje da tabbatar da cewa bacteriostatic chlortetracycline yawa isa ya hana gina jiki kira, amma ga hanawa na nucleic acid kira na bukatar high yawa daga cikin miyagun ƙwayoyi.

Tetracyclines ake amfani da su a yaki da koda cuta, daban-daban fata cututtuka, na numfashi da kuma wasu cututtuka. Idan dole, su maye gurbin penicillin, amma a 'yan shekarun nan, da yin amfani da tetracyclines muhimmanci rage, saboda zargin da juriya da kwayoyin wannan rukuni na maganin rigakafi. Korau irin rawa da yin amfani da kwayoyin a matsayin ƙari ga abincin dabbobi, sakamakon rage warkewa Properties na da miyagun ƙwayoyi saboda abin da ya faru na jure shi. Don shawo kan shi, an nada tare da wani hade da daban-daban kwayoyi da ciwon daban-daban inji na antimicrobial mataki na maganin rigakafi. Alal misali, lura da sakamako inganta ta lokaci daya aikace-aikace na tetracycline da streptomycin.

aminoglycosides

Aminoglycosides - halitta da kuma Semi-roba maganin rigakafi tare da wani sosai m bakan da aiki, dauke da kwayoyin a cikin sharan aminosaharidov. Ya zama na farko da aminoglycoside streptomycin, ya zama ruwan dare daga mazauna na ray fungi a tsakiyar karni na karshe, kuma rayayye yi amfani da magani daga wani iri-iri cututtuka. Kamar yadda bactericide, maganin rigakafi na ce kungiyar masu tasiri ko da a karfi da rage rigakafi. Ginshikai na mataki na maganin rigakafi kan da ake dasu cell ne da samuwar karfi covalent shaidu da sunadaran da ribosomes kananan kwayoyin halakar gina jiki kira a cikin kwayan cell halayen. Ba cikakken gane inji aminoglycoside bactericidal sakamako, kamar yadda tsayayya wa bacteriostatic mataki na tetracyclines da macrolides kuma karya gina jiki kira a kwayan Kwayoyin. Duk da haka, an san cewa aminoglycosides ne aiki ne kawai a karkashin aerobic yanayi, don haka suka nuna low yadda ya dace a kyallen takarda tare da matalauta jini wadata.

Bayan na farko da kwayoyin - penicillin da streptomycin, suka fara a haka yadu a yi amfani da magani daga wani cuta da cewa jimawa akwai wani matsala da samun amfani da kwayoyin zuwa wadannan kwayoyi. A halin yanzu, streptomycin ake amfani da yafi a hade tare da sauran latest ƙarni na kwayoyi zuwa bi da tarin fuka ko irin wannan, a yau rare cututtuka kamar annoba. A wasu lokuta sanya kanamycin, wanda shi ne ma ƙarni na farko na aminoglycoside kwayoyin. Duk da haka, saboda da high yawan guba na kanamycin a halin yanzu fĩfĩta gentamicin - shiri na biyu ƙarni, tsara ta uku da kuma shirye-shiryen da amikacin ne aminoglycoside - shi ne da wuya amfani da su hana jaraba cikinta kwayoyin.

chloramphenicol

Chloramphenicol ko chloramphenicol, shi ne halitta kwayoyin da fadi da bakan da aikin, aiki a kan wani babban yawan gram-tabbatacce kuma gram-korau kwayoyin, da yawa daga cikin manyan ƙwayoyin cuta. A sinadaran tsarin da aka samu nitrofenilalkilaminov, aka farko samu daga al'adun actinomycetes a tsakiyar karni na 20th, kuma bayan shekaru biyu kuma hada chemically.

Chloramphenicol yana da wani bacteriostatic sakamako a kan kwayoyin. Ginshikai na mataki na maganin rigakafi a kwayan cell ne zuwa kashe na ayyuka na kara kuzari samuwar aiwatar da peptide bond a gina jiki kira a lokacin da ribosomes. to chloramphenicol juriya a kwayoyin tasowa sannu a hankali sosai. Da miyagun ƙwayoyi a yi amfani da cutar typhoid ko shigellosis.

Glycopeptides da lipopeptides

Glycopeptides - a cyclic peptide mahadi wanda suke halitta, ko semisynthetic kwayoyin da kunkuntar bakan da aiki na wani damuwa daga kwayoyin. Su exert wani bactericidal sakamako a kan gram-tabbatacce kwayoyin cuta, da kuma iya maye gurbin penicillin a harka na jure shi. Ginshikai na mataki na maganin rigakafi kan kwayoyin za a iya bayyana ta da samuwar Hadin tare da amino acid da kuma cell bango peptidoglycan, game da shi suppressing su kira.

Da farko glycopeptide - vancomycin, da aka samar daga actinomycetes, dauka daga ƙasa na India. Yana da wani halitta kwayoyin da cewa shi ne aiki da kwayoyin, ko da a cikin kiwo kakar. Da farko, vancomycin aka yi amfani a matsayin mai sauyawa a yanayin saukan penicillin alerji zuwa da shi a lura da cututtuka. Duk da haka, da karuwa a miyagun ƙwayoyi juriya ya zama babbar matsala. A cikin shekaru 80 da aka samu teicoplanin - wani kwayoyin daga cikin rukuni na glycopeptides. Ya aka nada a wannan cututtuka, da kuma a hade tare da gentamicin, ya bada sakamako mai kyau.

A karshen karni na 20th, wani sabon rukuni na maganin rigakafi - lipopeptides ware daga Streptomyces. Chemically su ne cyclic lipopeptides. Wannan kwayoyin da kunkuntar bakan na mataki, exhibiting a bactericidal sakamako da gram-tabbatacce kwayoyin cuta, da kuma staphylococci da suke resistant zuwa beta-lactam kwayoyi da kuma glycopeptides.

Ginshikai na mataki na maganin rigakafi muhimmanci daban-daban daga wadanda aka riga aka sani - da lipopeptide siffofin a gaban alli ions karfi shaidu da jikin tantanin na kwayoyin cuta wadda take kaiwa zuwa depolarization kuma ta rushewa daga furotin kira, sabõda haka, qeta cell mutu. A farko wakilin aji na lipopeptides - daptomycin.

Game da daptomycin iya lura da wani gagarumin kudi na bactericidal aiki, da kuma mafi muhimmanci - da rashin giciye-juriya, ko a kalla sosai jinkirin da samuwar saboda gaskiyar cewa wani sabon gaba daya inji na mataki na maganin rigakafi kafa a cikin tsarin da abu.

polyenes

A gaba kungiya - polyene maganin rigakafi. Yau akwai wata babbar karuwa a fungal cututtuka suna da wuya mu bi. Don magance su ne antifungal abubuwa - halitta, ko Semi-roba polyene maganin rigakafi. A farko antifungal miyagun ƙwayoyi ne har yanzu a tsakiyar karni na karshe fara Nystatin, wanda aka ware daga Streptomyces al'adu. A wannan lokacin, da likita yi hada yawa polyene maganin rigakafi, samu daga wani iri-iri na fungal al'adu - griseofulvin, Levorinum da sauransu. Mun kawai samu ta yin amfani da polyenes riga tsara ta huɗu. Common sunan da suka samu godiya ga gaban da dama biyu shaidu a cikin kwayoyin.

Ginshikai na mataki na polyene maganin rigakafi saboda da samuwar sinadaran shaidu da jikin tantanin sterols a fungi. Polyene kwayoyin haka saka a cikin cell membrane da kuma siffofin ion aike tashar ta hanyar abin da aka gyara mika zahiri Kwayoyin, abu don ta kawar. A low allurai polyenes mallaka fungistatic aiki da kuma a high - fungicide. Duk da haka, su aiki ba a rufe da kwayoyin da ƙwayoyin cuta.

Polymyxin - halitta maganin rigakafi samar da ƙasa kwayoyin spore. A far, su aka yi amfani da 40-ies karni na karshe. Wadannan formulations bambanta bactericidal sakamako, wanda aka sa ta lalacewar da cytoplasmic membrane na kananan kwayoyin Kwayoyin haddasa ta hallaka. Polymyxin tasiri da gram-korau kwayoyin da suke da wuya jaraba kwayoyin. Duk da haka, da muni yawan guba takaita su yi amfani da a far. Mahadi wannan kungiya - polymyxin B sulfate da polymyxin sulfate M ake amfani da wuya da kuma kawai a matsayin shirye-shirye ajiye.

antitumor maganin rigakafi

Actinomycin samar da wasu ray fungi, da cytostatic sakamako. Halitta actinomycins a tsarin ne hromopeptidami iri dabam-dabam da amino acid a cikin peptide sarƙoƙi da cewa sanin su da nazarin halittu aiki. Actinomycin jawo hankalin da hankali na kwararru kamar antitumor maganin rigakafi. Ginshikai na mataki saboda da samuwar wani isasshe barga shaidu na peptide sarƙoƙi da miyagun ƙwayoyi da biyu Helix DNA daga cikin kananan kwayoyin da kuma game da shi tarewa da kira na RNA.

Dactinomycin, sakamakon a cikin 60s na karni na 20th, shi ne na farko anticancer wakili wanda ya sami yin amfani da oncologic far. Duk da haka, saboda da manyan yawan gefen sakamakon wannan magani yana da wuya amfani. Yanzu mun samu karin aiki antineoplastic kwayoyi.

Anthracyclines - wani musamman karfi da zanga-ƙari wakili ware daga Streptomyces. Ginshikai na mataki na maganin rigakafi hade da samuwar ternary gidaje tare da DNA, sarƙoƙi da sarƙar hutu. Kuma a karo na biyu zai yiwu inji na antimicrobial mataki saboda samar da free radicals cewa oxidize ciwon daji Kwayoyin.

Na halitta anthracyclines za a iya kira daunorubicin da doxorubicin. Nau'in maganin rigakafi bisa ga tsarin ba da aikin a kan kwayoyin cuta classifies su kamar yadda microbicides. Duk da haka, su high yawan guba tilasta don bincika sabuwar mahadi da cewa an shirya synthetically. Da yawa daga cikinsu an samu nasarar yi amfani da Oncology.

Maganin rigakafi yi dogon zama wani ɓangare na likita yi da kuma rayuwar dan Adam. Godiya a gare su, suka ci da yawa cututtuka, wanda a karnoni da aka dauke m. A halin yanzu, akwai wani bambancin da wadannan mahadi, wanda na bukatar ba kawai rarrabuwa na maganin rigakafi bisa ga tsarin ba da aikin da bakan, amma kuma a kan wasu halaye.