Ib tug tuaj yeem hais tias qhov kev tshawb pom ntawm penicillin thaum pib ntawm lub xyoo pua xeem dhau los yog ib qho kev hloov pauv. Thaum Ntiaj Teb Tsov Rog II, thawj cov tshuaj tua kab mob tau cawm ntau lab tus tub rog raug mob los ntawm sepsis. Penicillin tau dhau los ua ib qho txiaj ntsig zoo thiab tib lub sijhawm pheej yig tshuaj rau ntau yam kab mob loj nrog cov pob txha loj, qhov txhab purulent. Sij hawm dhau mus, lwm cov chav kawm ntawm cov tshuaj tua kab mob tau ua ke.
yam ntxwv dav dav
Hnub no twb muaj ntau cov tshuaj uas muaj nyob rau hauv lub ntiaj teb no loj heev ntawm cov tshuaj tua kab mob - tshuaj ntawm tej yam ntuj tso los yog semi-synthetic keeb kwm uas muaj peev xwm mus rhuav tshem tej pawg ntawm pathogens los yog tiv thaiv lawv txoj kev loj hlob los yog kev loj hlob. Mechanisms, spectra of action of antibiotics tuaj yeem sib txawv. Nyob rau tib lub sijhawm, hom tshiab thiab hloov kho cov tshuaj tua kab mob tshwm sim. Lawv ntau haiv neeg yuav tsum tau systematization. Nyob rau hauv peb lub sij hawm, kev faib cov tshuaj tua kab mob yog txais raws li lub mechanism thiab spectrum ntawm kev txiav txim, raws li zoo raws li cov qauv tshuaj. Raws li cov txheej txheem ntawm kev ua, lawv muab faib ua:
- bacteriostatic, kev loj hlob inhibiting lossisKev tsim tawm ntawm cov kab mob pathogenic microorganisms;
- bactericidal, uas pab tua kab mob.
Basic mechanisms of action of antibiotics:
- kev ua txhaum ntawm cov kab mob ntawm phab ntsa;
- kev tawm tsam ntawm cov protein synthesis hauv lub cell microbial;
- ua txhaum ntawm permeability ntawm cytoplasmic membrane;
- inhibition ntawm RNA synthesis.
Beta-lactams - penicillins
Los ntawm cov qauv tshuaj, cov tshuaj no tau muab cais raws li hauv qab no.
tshuaj tua kab mob beta-lactam. Cov txheej txheem ntawm kev ua ntawm cov tshuaj tua kab mob lactam yog txiav txim siab los ntawm lub peev xwm ntawm cov pab pawg ua haujlwm no txhawm rau khi cov enzymes koom nrog hauv kev sib txuas ntawm peptidoglycan, lub hauv paus ntawm cov kab mob sab nrauv ntawm cov kab mob. Yog li, kev tsim ntawm nws cov phab ntsa ntawm tes yog suppressed, uas yuav pab kom tsis txhob muaj kev loj hlob los yog kev loj hlob ntawm cov kab mob. Beta-lactams muaj toxicity tsawg thiab tib lub sijhawm zoo bactericidal. Lawv sawv cev rau pawg loj tshaj plaws thiab muab faib ua cov pab pawg uas muaj cov qauv tshuaj zoo sib xws.
Penicillins yog ib pawg ntawm cov tshuaj cais tawm ntawm qee cov kab mob pwm thiab ua cov kab mob bactericidal. Cov txheej txheem ntawm kev txiav txim ntawm cov tshuaj tua kab mob ntawm penicillin series yog vim qhov tseeb tias, rhuav tshem cov phab ntsa ntawm tes ntawm cov kab mob, lawv rhuav tshem lawv. Penicillins yog ntuj thiab semi-synthetic keeb kwm thiab yog dav-spectrum tebchaw - lawv yuav siv tau nyob rau hauv kev kho mob ntawm ntau yam kab mob tshwm sim los ntawm streptococci thiab staphylococci. Tsis tas li ntawd,Lawv muaj cov cuab yeej ntawm kev xaiv, ua haujlwm tsuas yog ntawm cov kab mob, tsis cuam tshuam rau cov kab mob macroorganism. Penicillins muaj lawv qhov tsis zoo, uas suav nrog qhov tshwm sim ntawm cov kab mob tsis zoo rau nws. Ntawm cov natural, feem ntau yog benzylpenicillin, phenoxymethylpenicillin, uas yog siv los tiv thaiv meningococcal thiab streptococcal kab mob vim tsis tshua muaj toxicity thiab tsawg nqi. Txawm li cas los xij, nrog kev siv sijhawm ntev, lub cev tiv thaiv kab mob tuaj yeem tshwm sim, uas yuav ua rau txo qis hauv nws cov txiaj ntsig. Semi-synthetic penicillins feem ntau yog tau los ntawm cov ntuj tsim los ntawm kev hloov kho tshuaj los muab cov khoom xav tau - amoxicillin, ampicillin. Cov tshuaj no muaj zog dua tiv thaiv kab mob tiv thaiv biopenicillins.
Lwm yam beta-lactams
Cephalosporins tau txais los ntawm cov nceb ntawm tib lub npe, thiab lawv cov qauv zoo ib yam li cov qauv ntawm penicillins, uas piav txog tib yam kev tsis zoo. Cephalosporins ua rau plaub tiam. Cov tshuaj thawj tiam yog siv ntau zaus hauv kev kho mob me me los ntawm staphylococci lossis streptococci. Cephalosporins tiam thib ob thiab thib peb muaj zog dua tiv thaiv kab mob gram-tsis zoo, thiab tiam thib plaub yog cov tshuaj muaj zog tshaj plaws uas siv los kho cov kab mob hnyav.
Carbapenems zoo tiv thaiv kab mob Gram-positive, Gram-negative thiab anaerobic kab mob. Lawv qhov zoo dua yog qhov tsis muajtiv thaiv kab mob rau cov tshuaj txawm tias tom qab siv ntev.
Monobactams kuj yog beta-lactams thiab muaj cov txheej txheem zoo sib xws ntawm cov tshuaj tua kab mob, uas muaj kev cuam tshuam cov phab ntsa ntawm tes ntawm cov kab mob. Lawv siv los kho ntau yam kab mob.
YMacrolides
Nov yog pab pawg thib ob. Macrolides yog cov tshuaj tua kab mob ntuj nrog cov qauv kev sib tw. Lawv yog ib tug multi-membered lactone nplhaib nrog txuas carbohydrate residues. Cov khoom ntawm cov tshuaj nyob ntawm seb muaj pes tsawg tus carbon atoms hauv lub nplhaib. Muaj 14-, 15- thiab 16-cov koom ua ke. Lub spectrum ntawm lawv qhov kev ua ntawm microbes yog dav heev. Cov txheej txheem ntawm kev ua ntawm cov tshuaj tua kab mob ntawm cov kab mob microbial muaj nyob rau hauv lawv cov kev cuam tshuam nrog ribosomes thiab yog li cuam tshuam cov synthesis ntawm cov protein nyob rau hauv lub cell ntawm cov kab mob los ntawm suppressing cov kev tshwm sim ntawm ntxiv tshiab monomers rau cov peptide saw. Sib sau ua ke hauv cov hlwb ntawm lub cev tiv thaiv kab mob, macrolides kuj ua rau kev puas tsuaj ntawm cov kab mob hauv lub cev.
Macrolides yog qhov muaj kev nyab xeeb tshaj plaws thiab muaj tshuaj lom tsawg tshaj plaws ntawm cov tshuaj tua kab mob uas paub thiab muaj txiaj ntsig tsis yog Gram-zoo nkaus xwb tab sis kuj yog cov kab mob Gram-negative. Thaum siv lawv, qhov kev xav tsis zoo ntawm cov tshuaj tiv thaiv tsis tau pom. Cov tshuaj tua kab mob no yog tus cwj pwm los ntawm cov nyhuv bacteriostatic, tab sis ntawm qhov siab siab lawv tuaj yeem muaj cov kab mob bactericidal ntawm pneumococci thiab lwm yam kab mob. Raws li cov txheej txheem ntawm kev npaj, macrolides muab faib ua ntuj thiab semi-synthetic.
thawj tshuaj los ntawmIb chav kawm ntawm ntuj macrolides yog erythromycin, tau txais nyob rau hauv nruab nrab ntawm lub xyoo pua xeem thiab siv tau zoo tiv thaiv kab mob gram-zoo resistant rau penicillins. Ib tiam tshiab ntawm cov tshuaj nyob rau hauv pab pawg no tshwm sim nyob rau hauv lub 70s ntawm lub xyoo pua 20th thiab yog tseem nquag siv.
Macrolides kuj suav nrog cov tshuaj tua kab mob semi-synthetic - azolides thiab ketolides. Nyob rau hauv lub azolide molecule, ib tug nitrogen atom nyob rau hauv lub lactone nplhaib ntawm cuaj thiab kaum carbon atoms. Tus neeg sawv cev ntawm azolides yog azithromycin nrog lub dav spectrum ntawm kev ua thiab kev ua haujlwm ntawm cov kab mob gram-positive thiab gram-negative, qee qhov anaerobes. Nws yog qhov ruaj khov ntau dua nyob rau hauv ib puag ncig acidic dua li erythromycin, thiab tuaj yeem khaws cia hauv nws. Azithromycin yog siv rau ntau yam kab mob ntawm txoj hlab ntsws, genitourinary system, hnyuv, tawv nqaij thiab lwm yam.
Ketolides yog tau los ntawm kev ntxiv ib pawg keto rau peb lub atom ntawm lub nplhaib lactone. Lawv txawv los ntawm cov kab mob tsawg dua thaum piv nrog macrolides.
Tetracyclines
Tetracyclines belongs rau chav kawm ntawm polyketides. Cov no yog cov tshuaj tua kab mob broad-spectrum nrog cov nyhuv bacteriostatic. Lawv thawj tus neeg sawv cev, chlortetracycline, raug cais nyob rau hauv nruab nrab ntawm lub xyoo pua xeem los ntawm ib qho ntawm cov kab lis kev cai ntawm actinomycetes, lawv kuj hu ua radiant fungi. Ob peb xyoos tom qab ntawd, oxytetracycline tau txais los ntawm ib pawg ntawm cov kab mob tib yam. Tus neeg sawv cev thib peb ntawm pawg no yog tetracycline, uas yog thawj zaug tsim los ntawm kev hloov kho tshuaj ntawm nws cov tshuaj chlorine derivative, thiab ib xyoos tom qab kuj raug cais tawm ntawm actinomycetes. Lwm yamCov tshuaj ntawm pawg tetracycline yog cov khoom siv hluavtaws semi-synthetic derivatives ntawm cov tshuaj no.
Tag nrho cov tshuaj no zoo ib yam hauv cov qauv tshuaj thiab cov khoom, hauv kev ua haujlwm tawm tsam ntau hom kab mob gram-zoo thiab gram-tsis zoo, qee cov kab mob thiab protozoa. Lawv kuj tseem tiv taus cov kab mob ntawm cov kab mob. Cov txheej txheem ntawm kev ua ntawm cov tshuaj tua kab mob ntawm cov kab mob ntawm tes yog txhawm rau txo cov txheej txheem ntawm cov protein biosynthesis hauv nws. Thaum cov tshuaj molecules ua rau cov kab mob gram-tsis zoo, lawv nkag mus rau hauv lub cell los ntawm kev yooj yim diffusion. Cov txheej txheem ntawm kev nkag mus ntawm cov tshuaj tua kab mob rau hauv cov kab mob Gram-zoo tseem tsis tau kawm txaus, txawm li cas los xij, muaj qhov kev xav tias tetracycline molecules cuam tshuam nrog qee cov hlau ions uas nyob hauv cov kab mob hauv cov kab mob los tsim cov tshuaj sib txuas. Nyob rau hauv rooj plaub no, cov saw yog tawg nyob rau hauv tus txheej txheem ntawm tsim cov protein tsim nyog rau cov kab mob ntawm tes. Cov kev sim tau pom tias cov kab mob bacteriostatic ntau ntawm chlortetracycline txaus los tua cov protein synthesis, txawm li cas los xij, cov tshuaj muaj ntau ntau yuav tsum tau ua rau inhibit synthesis ntawm nucleic acids.
Tetracyclines yog siv los tiv thaiv kab mob raum, ntau yam kab mob ntawm daim tawv nqaij, kab mob ua pa thiab ntau yam kab mob. Yog tias tsim nyog, lawv hloov cov tshuaj penicillin, tab sis nyob rau xyoo tas los no kev siv tetracyclines tau poob qis, uas cuam tshuam nrog kev tshwm sim ntawm microbial tsis kam rau cov tshuaj tua kab mob no. Kev siv ntawm notshuaj tua kab mob raws li ib tug additive rau tsiaj pub, uas ua rau ib tug txo nyob rau hauv cov tshuaj thaj chaw ntawm cov tshuaj vim qhov tshwm sim ntawm tsis kam mus rau nws. Txhawm rau kov yeej nws, kev sib xyaw nrog cov tshuaj sib txawv uas muaj cov txheej txheem sib txawv ntawm cov tshuaj tua kab mob ntawm cov tshuaj tua kab mob. Piv txwv li, cov tshuaj kho tau zoo dua los ntawm kev siv ib txhij ntawm tetracycline thiab streptomycin.
Aminoglycosides
Aminoglycosides yog cov tshuaj tua kab mob ntuj tsim thiab semi-synthetic nrog kev ua haujlwm dav dav, muaj cov aminosaccharide residues hauv cov molecule. Thawj aminoglycoside yog streptomycin, cais los ntawm ib cheeb tsam ntawm radiant fungi twb nyob rau hauv nruab nrab ntawm lub xyoo pua xeem thiab nquag siv nyob rau hauv kev kho mob ntawm ntau yam kab mob. Ua cov kab mob bactericidal, cov tshuaj tua kab mob ntawm pab pawg hais tau zoo txawm tias muaj kev tiv thaiv tsis zoo. Cov txheej txheem ntawm kev txiav txim ntawm cov tshuaj tua kab mob ntawm cov kab mob microbial yog tsim kom muaj zog covalent bonds nrog cov proteins ntawm ribosomes ntawm cov kab mob thiab kev puas tsuaj ntawm cov protein synthesis tshwm sim hauv cov kab mob ntawm tes. Cov txheej txheem ntawm cov kab mob bactericidal ntawm aminoglycosides tsis tau kawm tag nrho, piv rau cov nyhuv bacteriostatic ntawm tetracyclines thiab macrolides, uas tseem cuam tshuam cov protein synthesis hauv cov kab mob. Txawm li cas los xij, aminoglycosides paub tias ua haujlwm tsuas yog nyob rau hauv cov xwm txheej aerobic, yog li lawv tsis ua haujlwm zoo hauv cov ntaub so ntswg nrog cov ntshav tsis zoo.
Tom qab pom cov tshuaj tua kab mob thawj zaug - penicillin thiab streptomycin, lawv tau pib siv dav hauv kev kho cov kab mob uas tsis ntev los no cov teeb meem ntawm cov kab mob tau siv rau cov tshuaj no tshwm sim. Tam sim nostreptomycin feem ntau yog siv ua ke nrog lwm cov tshuaj tiam tshiab los kho cov kab mob ntsws lossis kab mob tsis tshua muaj xws li kab mob plague. Hauv lwm qhov xwm txheej, kanamycin yog tshuaj, uas kuj yog thawj tiam aminoglycoside tshuaj tua kab mob. Txawm li cas los xij, vim muaj cov tshuaj lom neeg siab ntawm kanamycin, gentamicin, tshuaj thib ob, tam sim no nyiam, thiab cov tshuaj aminoglycoside thib peb yog amikacin, uas tsis tshua muaj siv los tiv thaiv kab mob los ntawm kev quav tshuaj rau nws.
Levomycetin
Levomycetin, lossis chloramphenicol, yog cov tshuaj tua kab mob ntuj tsim nrog qhov dav tshaj plaws ntawm kev ua haujlwm, tawm tsam ntau tus kab mob gram-zoo thiab gram-tsis zoo, ntau cov kab mob loj. Raws li cov qauv tshuaj, qhov no derivative ntawm nitrophenylalkylamines yog thawj zaug tau los ntawm kab lis kev cai ntawm actinomycetes nyob rau hauv nruab nrab ntawm lub xyoo pua 20th, thiab ob xyoos tom qab nws kuj tau synthesized tshuaj.
Levomycetin muaj cov nyhuv bacteriostatic ntawm cov kab mob. Cov txheej txheem ntawm kev ua ntawm cov tshuaj tua kab mob ntawm cov kab mob ntawm tes yog txhawm rau txhawm rau ua haujlwm ntawm catalysts rau kev tsim cov peptide bonds hauv ribosomes thaum lub sij hawm tsim cov protein. Cov kab mob tsis kam mus rau levomycetin tshwm sim qeeb heev. Cov tshuaj no yog siv rau tus mob typhoid kub taub hau los yog dysentery.
YGlycopeptides thiab lipopeptides
Glycopeptides yog cyclic peptide compounds uas yog cov tshuaj tua kab mob ntuj los yog semi-synthetic nrog nqaimspectrum ntawm kev ua ntawm qee yam kab mob ntawm cov kab mob. Lawv muaj cov kab mob bactericidal ntawm cov kab mob gram-zoo, thiab tuaj yeem hloov cov tshuaj penicillin thaum muaj kev tiv thaiv rau nws. Cov txheej txheem ntawm kev ua ntawm cov tshuaj tua kab mob ntawm cov kab mob tuaj yeem piav qhia los ntawm kev tsim cov ntawv cog lus nrog cov amino acids ntawm peptidoglycan ntawm phab ntsa ntawm tes thiab, yog li, kev tawm tsam ntawm lawv cov synthesis.
Thawj glycopeptide, vancomycin, tau txais los ntawm actinomycetes coj los ntawm av hauv Is Nrias teb. Nws yog ib qho tshuaj tua kab mob ntuj uas nquag ua rau cov kab mob txawm tias thaum lub caij yug me nyuam. Thaum pib, vancomycin tau siv los hloov cov tshuaj penicillin thaum muaj kev fab tshuaj rau nws hauv kev kho mob. Txawm li cas los xij, qhov nce ntawm cov tshuaj tiv thaiv tau dhau los ua teeb meem loj. Hauv xyoo 1980, teicoplanin, tshuaj tua kab mob los ntawm pawg glycopeptides, tau txais. Nws raug sau rau tib yam kab mob, thiab ua ke nrog gentamicin, nws muab cov txiaj ntsig zoo.
Thaum kawg ntawm lub xyoo pua 20th, ib pab pawg tshiab ntawm cov tshuaj tua kab mob tshwm sim - lipopeptides cais los ntawm streptomycetes. Raws li lawv cov qauv tshuaj, lawv yog cyclic lipopeptides. Cov no yog cov tshuaj tua kab mob nqaim-spectrum nrog cov kab mob bactericidal tiv thaiv kab mob gram-zoo, nrog rau staphylococci resistant rau beta-lactam tshuaj thiab glycopeptides.
Cov txheej txheem ntawm kev ua ntawm cov tshuaj tua kab mob yog qhov sib txawv ntawm cov uas twb paub lawm - nyob rau hauv lub xub ntiag ntawm calcium ions, lipopeptide tsim muaj zog bonds nrog cov kab mob cell membrane, uas ua rau nws depolarization thiab cuam tshuam ntawm protein synthesis, vim li ntawd ntawm uas cov cell ua phem tuag. Ua ntejib tug tswv cuab ntawm chav kawm lipopeptide yog daptomycin.
daptomycin
YPolyenes
Pab pawg tom ntej yog tshuaj tua kab mob polyene. Niaj hnub no muaj kev loj hlob ntawm cov kab mob fungal uas nyuaj rau kho. Txhawm rau tiv thaiv lawv, cov tshuaj tua kab mob yog npaj - tshuaj tua kab mob ntuj lossis semi-synthetic polyene. Thawj cov tshuaj tiv thaiv kab mob hauv nruab nrab ntawm lub xyoo pua xeem yog nystatin, uas tau cais tawm ntawm kab lis kev cai ntawm streptomycetes. Lub sijhawm no, ntau cov tshuaj tua kab mob polyene tau los ntawm ntau hom kab mob fungal - griseofulvin, levorin thiab lwm yam - tau suav nrog hauv kev kho mob. Tam sim no tiam plaub polyenes twb tau siv lawm. Lawv tau txais lawv lub npe vim muaj ob peb daim ntawv cog lus hauv cov molecules.
Lub txheej txheem ntawm kev ua ntawm cov tshuaj tua kab mob polyene yog vim tsim cov tshuaj tiv thaiv nrog cov sterols ntawm cov cell membranes hauv cov fungus. Lub polyene molecule yog li kev koom ua ke rau hauv lub cell membrane thiab tsim ib qho ionic hlau channel los ntawm cov khoom ntawm lub xovtooj mus rau sab nraud, ua rau nws tshem tawm. Polyenes yog fungistatic ntawm koob tshuaj tsawg thiab fungicidal ntawm cov koob tshuaj siab. Txawm li cas los xij, lawv txoj haujlwm tsis txuas mus rau cov kab mob thiab kab mob.
Polymyxins yog cov tshuaj tua kab mob ntuj tsim los ntawm cov kab mob hauv av. Hauv kev kho mob, lawv pom daim ntawv thov hauv 40s ntawm lub xyoo pua xeem. Cov tshuaj no yog tus cwj pwm los ntawm cov kab mob bactericidal, uas yog tshwm sim los ntawm kev puas tsuaj rau cytoplasmic membrane ntawm lub cell ntawm cov kab mob, ua rau nws tuag. Polymyxins zoo tiv thaiv kab mob Gram-negative thiab tsis tshua muaj tus cwj pwm tsim. Txawm li cas los xij, toxicity siab dhau txwv lawv siv hauv kev kho mob. Cov tshuaj ntawm cov pab pawg no - polymyxin B sulfate thiab polymyxin M sulfate tsis tshua siv thiab tsuas yog ua cov tshuaj cia.
tshuaj tiv thaiv kab mob antiineoplastic
Actinomycins yog tsim los ntawm qee cov fungi radiant thiab muaj cov nyhuv cytostatic. Ntuj actinomycins yog chromopeptides nyob rau hauv cov qauv, txawv nyob rau hauv amino acids nyob rau hauv peptide chains, uas txiav txim siab lawv lom lom. Actinomycins nyiam cov kws kho mob tshwj xeeb ua cov tshuaj tua kab mob antitumor. Lawv cov txheej txheem ntawm kev ua haujlwm yog vim tsim cov nyiaj ruaj khov txaus ntawm peptide chains ntawm cov tshuaj nrog ob lub helix ntawm DNA ntawm cov kab mob thiab kev thaiv ntawm RNA synthesis raws li qhov tshwm sim.
Dactinomycin, tau txais hauv 60s ntawm lub xyoo pua 20th, yog thawj cov tshuaj tiv thaiv kab mob uas siv rau hauv kev kho mob oncological. Txawm li cas los xij, vim muaj kev phiv ntau, cov tshuaj no tsis tshua siv. Tam sim no tau txais cov tshuaj tiv thaiv kab mob ntau dua.
Anthracyclines yog cov tshuaj tua kab mob uas muaj zog heev uas cais tawm ntawm streptomycetes. Cov txheej txheem ntawm kev ua ntawm cov tshuaj tua kab mob yog txuam nrog kev tsim ntawm triple complexes nrog DNA chains thiab rhuav tshem ntawm cov chains. Ib qho kev ua haujlwm thib ob ntawm kev siv tshuaj tua kab mob kuj tseem ua tau, vim yog kev tsim cov dawb radicals uas oxidize cov qog nqaij hlav cancer.
Ntawm cov tshuaj anthracyclines, daunorubicin thiab doxorubicin tuaj yeem hais tau. Kev faib tawm ntawm cov tshuaj tua kab mob raws li cov txheej txheem ntawm kev ua ntawm cov kab mob cais lawv ua bactericidal. Txawm li cas los xij, lawv cov toxicity siab yuam kev tshawb nrhiav cov tebchaw tshiab uas tau txais hluavtaws. Ntau ntawm lawv tau ua tiav siv hauv oncology.
Tshuaj tua kab mob tau nkag mus rau kev kho mob ntev thiab tib neeg lub neej. Ua tsaug rau lawv, ntau yam kab mob tau kov yeej, uas tau ntau pua xyoo tau suav tias yog kho tsis tau. Tam sim no, muaj ntau yam ntawm cov tebchaw uas tsis yog tsuas yog kev faib tawm ntawm cov tshuaj tua kab mob raws li cov txheej txheem thiab spectrum ntawm kev ua, tab sis kuj raws li ntau lwm yam yuav tsum tau.
