Quinolones ua haujlwm li cas?

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• Quinolones yog dab tsi?
  1. Lus txhais
  2. Antibacterial mechanism
  3. nta
  4. Tshuaj Kev Sib Thoob
• Kev faib tawm Quinolone
• Quinolones ua haujlwm li cas?
  1. Lub hauv paus ntsiab lus ntawm kev nqis tes ua
  2. Daim ntawv thov
  3. Fluoroquinolones Kev phiv tshuaj
• Fluoroquinolones Kev phiv tshuaj
  1. Muaj kev phom sij
  2. Outlook
• xaus

Quinolones yog dab tsi?

1. Lus txhais

Quinolones, tseem hu ua pyridone acids, yog cov tshuaj tua kab mob tua kab mob uas muaj cov qauv yooj yim ntawm 4-quinolones. Quinolones tsom cov kab mob deoxyribonucleic acid (DNA), cuam tshuam DNA gyrase, thiab txuas ntxiv ua rau puas tsuaj rau cov kab mob DNA kom ua tiav cov tshuaj tua kab mob.

Xyoo 1979, Norfloxacin tau tsim tawm, thiab tom qab ntawd tau tsim cov tshuaj quinolones tshiab uas muaj fluorine, feem ntau hu ua fluoroquinolones . Cov tshuaj Quinolone tau muab faib ua plaub tiam neeg, thiab tiam neeg thib peb tau siv dav. Cov tshuaj siv feem ntau suav nrog norfloxacin , ofloxacin , ciprofloxacin , fleroxacin, thiab lwm yam. Cov tshuaj no muaj cov teebmeem bactericidal rau ntau yam kab mob Gram-negative, thiab siv dav hauv kev kho mob ntawm cov kab mob genitourinary, kab mob plab hnyuv, thiab kev kho mob ntawm cov kab mob gram-negative hauv txoj hlab pa thiab cov tawv nqaij.

2. Antibacterial mechanism

Cov enzymes uas siv rau cov tshuaj quinolone yog cov kab mob DNA gyrase thiab topoisomerase IV. Rau feem ntau cov kab mob gram-negative, DNA gyrase yog lub enzyme tseem ceeb rau quinolones . Rau feem ntau cov kab mob gram-positive, quinolones feem ntau inhibit cov kab mob topoisomerase IV, uas yog ib qho helicase uas tuaj yeem tso cov chromosomes uas sib txuas thaum lub sijhawm DNA replication.

3. nta

Nws muaj cov tshuaj tua kab mob muaj zog thiab nthuav dav cov kab mob tua kab mob. Nws feem ntau tawm tsam cov kab mob Gram-negative thiab tseem muaj txiaj ntsig zoo rau cov kab mob Gram-positive. Nws tau faib dav hauv lub cev thiab tuaj yeem nkag mus rau cov pob txha, pob qij txha thiab cov ntaub so ntswg uas feem ntau cov tshuaj tsis tuaj yeem nkag mus. Quinolones tsis tshua muaj kev tiv thaiv los ntawm lawv tus kheej, thiab tsis muaj kev tiv thaiv khaub thuas nrog lwm cov tshuaj tua kab mob, uas muaj txiaj ntsig zoo rau kev sib xyaw ntawm lwm cov tshuaj tua kab mob.

• Cov tshuaj tua kab mob dav dav, tshwj xeeb tshaj yog rau aerobic gram-negative bacilli, suav nrog Pseudomonas aeruginosa, muaj cov tshuaj tua kab mob muaj zog, thiab muaj cov tshuaj tua kab mob zoo rau Staphylococcus aureus thiab tsim cov enzyme-tsim Staphylococcus aureus. Qee hom tsiaj kuj muaj kev cuam tshuam rau tuberculosis, mycoplasma, chlamydia thiab kab mob anaerobic.
• Nws ua tau zoo hais lus thiab tau nthuav dav hauv lub cev. Cov ntshav khi cov protein ntau tsawg, thiab ntshav ib nrab lub neej yog qhov ntev. Ib feem ntawm nws tau tso tawm los ntawm ob lub raum hauv nws daim ntawv qub, nrog cov zis siab, thiab lwm qhov yog metabolized los ntawm lub siab.
• Nws muaj qee qhov tsis zoo thiab ua siab ntev rau qhov zoo. Xeev siab, ntuav, tsis qab los noj mov, ua pob, mob taub hau thiab kiv taub hau tuaj yeem pom. Qee zaum, muaj cov tsos mob ntawm lub hlwb xws li qaug dab peg, uas tuaj yeem daws tau los ntawm kev siv tshuaj. Txhua Cov tshuaj fluoroquinolones tuaj yeem ua rau muaj kab mob sib kis hauv cov menyuam yaus thiab tsiaj thiab sib koom ua ke thiab ua rau menyuam yaus, yog li lawv yuav tsum tsis txhob siv rau menyuam yaus lossis cov pojniam xeeb tub.
• Nws yog qhov tsim nyog rau cov kab mob tso zis los ntawm cov kab mob rhiab (xws li Staphylococcus aureus, Pseudomonas aeruginosa, plab hnyuv-tsis zoo bacilli, Campylobacter thiab Neisseria gonorrhoeae, thiab lwm yam), mob qog noj ntshav, mob qog noj ntshav, mob ua pa, mob plab zom mov thiab pob txha, sib koom tes, thiab cov nqaij mos kis.
• Ib chav kawm ntawm cov tshuaj uas tuaj yeem ua rau deoxyribonucleic acid (DNA) ntawm cov kab mob thiab ua rau tsis tuaj yeem ua rau puas tsuaj rau cov kab mob chromosomes. Vim tias cov qauv sib txawv thiab cov txheej txheem ntawm kev ua ntawm cov tshuaj no, tsis muaj kev tiv thaiv kab mob sib kis hauv cov tshuaj tua kab mob. Nws feem ntau ua rau cov kab mob tsis zoo, thiab muaj kev cuam tshuam tsis zoo rau cov kab mob zoo tshwj tsis yog Staphylococcus aureus. Feem ntau siv ntau yam suav nrog pipemidic acid, norfloxacin, norfloxacin, thiab ciprofloxacin ua.
• Cov kev tsis zoo suav nrog:
  • Cov kab mob plab zom mov nrog xeev siab thiab lwm yam tsis xis nyob.
  • Cov kev tawm tsam hauv nruab nrab tuaj yeem ua rau pom cov tsos mob ntawm lub hlwb thiab tseem ua rau qaug dab peg.
  • Nws tuaj yeem cuam tshuam rau kev txhim kho pob txha mos, yog li cov poj niam cev xeeb tub thiab cov menyuam yaus hnub nyoog qis dua yuav tsum siv nws nrog ceev faj.
  • Qee zaum kev ua xua xws li ua pob tawv nqaij tuaj yeem tshwm sim.
  • Kev siv hnyav hnyav ntev tuaj yeem ua rau lub siab puas.

4. Tshuaj Kev Sib Thoob

• Cov tshuaj Alkaline, tshuaj anticholinergic, thiab H2 receptor blockers tuaj yeem txo qis cov kua qaub hauv plab thiab nqus cov tshuaj no. Yog li tsis txhob coj lawv ua ke.
• Ob leeg rifampicin tshuaj (RNA synthesis inhibitor) thiab chloramphenicol (protein synthesis inhibitor) tuaj yeem txo qis cov tshuaj hauv chav kawm no, ua rau muaj kev cuam tshuam ntawm nalidixic acid thiab norfloxacin kom ploj tag, thiab ib nrab ua rau muaj txiaj ntsig ntawm fluoxinic acid thiab ciprofloxacin ua.
• Fluoroquinolones inhibit cov metabolism hauv theophylline. Thaum ua ke nrog theophylline, cov ntshav cov ntshav ntawm theophylline yuav nce ntxiv, thiab theophylline cov tshuaj lom tuaj yeem tshwm sim, yog li yuav tsum tau saib xyuas.

Kev faib tawm Quinolone

Quinolones raug muab faib ua thawj, thib ob, thib peb thiab thib plaub tiam raws li qhov kev txiav txim ntawm kev tsim kho tshiab thiab lawv cov khoom tua kab mob.

1. Thawj-tiam quinolones muaj cov tshuaj tua kab mob tsuas yog tiv thaiv Escherichia coli, Shigella, Klebsiella, thiab ob peb Proteus. Ntau yam tshwj xeeb suav nrog nalidixic acid thiab pyrrolic acid, thiab lwm yam, uas tau tshem tawm vim tsis muaj txiaj ntsig zoo.
2. Lub cim thib ob quinolones tau nthuav dav lawv cov kab mob tua kab mob thiab muaj qee yam tshuaj tua kab mob tiv thaiv Enterobacter, Citrobacter, Pseudomonas aeruginosa, thiab Serratia. Pipemidic acid feem ntau yog siv hauv tsev. Ib qho ntxiv, muaj Cinoxacin thiab Miloxacin, uas tau tsim tawm txawv teb chaws. Vim tias lawv cov kev mob tshwm sim yog qhov tseem ceeb, tshwj tsis yog rau pipemidic acid, lwm tus tau raug tshem tawm.
3. Cov kab mob tua kab mob ntawm cov cim thib peb quinolones tau nthuav dav ntxiv, thiab nws tseem muaj cov tshuaj tua kab mob rau cov kab mob gram-zoo xws li staphylococci, thiab nws cov tshuaj tua kab mob rau qee cov kab mob gram-tsis zoo ntxiv. Cov khoom tseem ceeb suav nrog Norfloxacin, Ofloxacin, Levofloxacin, Pefloxacin, Enoxacin, Ciprofloxacin thiab lwm yam. Muaj cov tshuaj fluorine atoms hauv cov qauv ntawm cov tshuaj no. Yog li ntawd, nws yog hu ua Cov tshuaj fluoroquinolone.
4. Piv nrog rau cov tshuaj peb tiam dhau los, quinolones plaub tiam raug hloov kho. Kev qhia txog 8-methoxyl pawg hauv cov qauv pab txhawb kev ua haujlwm tiv thaiv anaerobe, thaum lub nplhaib nitro-dioxy tus qauv ntawm C-7 txoj haujlwm ntxiv dag zog rau kev tiv thaiv kab mob gram-zoo thiab tswj hwm qhov qub anti-Gram-negative cov kab mob ua haujlwm.

Cov kev phom sij me dua, tab sis tus nqi kim dua. Nws tau txhim kho cov tshuaj tiv thaiv kab mob tiv thaiv kab mob gram-positive, txhim kho cov kab mob anaerobic suav nrog Bacteroides fragilis, thiab cov kab mob zoo xws li Mycoplasma pneumoniae, Chlamydia pneumoniae, Legionella thiab Mycobacterium tuberculosis. Cov khoom lag luam feem ntau tau ncua lub neej ib nrab, xws li gatifloxacin, trovafloxacin, clinfloxacin, thiab moxifloxacin.

Quinolones ua haujlwm li cas?

1. Lub hauv paus ntsiab lus ntawm kev nqis tes ua

Cov pob txha yooj yim ntawm cov tshuaj tua kab mob quinolone yog cov qauv nitrogen (hetero) ob chav cyclic. Quinolones thiab lwm yam tshuaj tua kab mob muaj cov ntsiab lus sib txawv ntawm kev ua haujlwm. Lawv tsom mus rau cov kab mob deoxyribonucleic acid (DNA). Cov DNA ob txoj hlua ntawm cov kab mob yog ntswj rau hauv cov voj voog lossis cov kauv (hu ua supercoils). Cov enzyme uas ua rau DNA supercoils hu ua DNA gyrase. Quinolones cuam tshuam cov enzyme no thiab ua rau muaj kev puas tsuaj rau cov kab mob DNA, yog li cov cell tsis tuaj yeem faib. Lawv qhia txog kev lom tshuaj rau cov kab mob.

Tam sim no, qhov tsis kam ntawm qee cov kab mob rau ntau yam tshuaj tua kab mob tuaj yeem nthuav dav vim yog kis plasmid. Cov chav kawm ntawm cov tshuaj no tsis cuam tshuam los ntawm cov tshuaj tiv thaiv plasmid. Yog li, tsis muaj kev tiv thaiv khaub thuas ntawm cov tshuaj no thiab ntau yam tshuaj tua kab mob.

Quinolones yog cov tshuaj tua kab mob uas feem ntau ua rau cov kab mob gram-tsis zoo thiab muaj qhov cuam tshuam tsis zoo rau cov kab mob gram-positive (qee qhov ntau yam muaj cov tshuaj tua kab mob zoo dua ntawm Staphylococcus aureus).

2. Daim ntawv thov

Quinolone tshuaj tua kab mob yog ib chav kawm ntawm cov tshuaj uas tib neeg thiab tsiaj txhu siv. Vim tias lawv cov tshuaj tua kab mob dav, muaj zog tiv thaiv kab mob, tsis muaj kev tiv thaiv kab mob nrog lwm cov tshuaj tua kab mob, thiab muaj kev phiv tsawg, lawv tau siv dav hauv kev tswj kab mob ntawm tsiaj txhu, aquaculture thiab lwm yam kev lag luam, suav nrog qaib, ducks, geese, npua, nyuj, Yaj, ntses, cws, roob ris, thiab lwm yam.

Enrofloxacin , yog ib hom tshuaj tua kab mob fluoroquinolone, muaj cov yam ntxwv ntawm kev tua kab mob dav dav, muaj zog tua kab mob, ua haujlwm sai, faib dav hauv lub cev thiab tsis muaj kev sib xyaw nrog lwm cov tshuaj tua kab mob. Nws tiv thaiv thiab kho cov kab mob bacterial thiab mycoplasmosis hauv tsiaj txhu thiab nqaij qaib.

Hauv kev tiv thaiv thiab tswj cov kab mob npua, lawv kuj ua tau zoo tiv thaiv Pseudomonas aeruginosa, Klebsiella, Escherichia coli, Enterobacter, Campylobacter, Shigella, Salmonella , Aeromonas Gram-negative bacilli thiab cocci suav nrog genus, Haemophilus, Yersinia, Serratia, Vibrio, Proteus, Brucella, Pasteurella Genus, Erysipelas, Bordetella, Staphylococcus, Mycoplasma thiab Chlamydia.

Ntxiv rau, nws muaj cov teebmeem zoo rau cov kab mob synergistic sulfa-resistant, gentamicin-resistant Pseudomonas aeruginosa, penicillin-resistant Staphylococcus aureus, thiab tylosin lossis tiamulin-resistant Mycoplasma.

3. Fluoroquinolones Kev phiv tshuaj

• Cov kab mob plab zom mov: xeev siab, ntuav, tsis xis nyob, mob, thiab lwm yam;
• Cov kev tawm tsam hauv nruab nrab: mob taub hau, kiv taub hau, pw tsis zoo, thiab lwm yam, ua rau muaj kev puas siab puas ntsws;
• Vim tias chav kawm ntawm cov tshuaj no tuaj yeem cuam tshuam γ-aminobutyric acid (GABA), nws tuaj yeem ua rau qaug dab peg, yog li cov uas muaj keeb kwm mob vwm yuav tsum siv lawv nrog ceev faj;
• Cov tshuaj hauv chav kawm no tuaj yeem cuam tshuam kev txhim kho pob txha mos, yog li cov poj niam cev xeeb tub thiab cov menyuam yaus hnub nyoog qis dua yuav tsum siv lawv nrog kev ceev faj;
• Crystaluria tuaj yeem tsim tawm, tshwj xeeb tshaj yog nyob rau hauv cov zis alkaline;
• Kev siv tshuaj loj lossis siv sijhawm ntev ntawm cov tshuaj no tuaj yeem ua rau lub siab puas.

Yav tom ntej ntawm quinolones

1. Muaj kev phom sij

Cov tshuaj Quinolone tau siv dav hauv kev kho tib neeg thiab tsiaj txhu kab mob. Vim tias qhov seem ntawm cov tshuaj quinolone hauv cov nqaij tsiaj, cov tshuaj tua kab mob quinolone tau sau rau hauv tib neeg lub cev tom qab tib neeg noj cov nqaij nqaij, lawv tuaj yeem ua rau mob hnyav rau tib neeg cov kab mob. Cov tshuaj muaj txiaj ntsig cuam tshuam rau kev kho tib neeg kab mob. Raws li cov lus hais mus, tshuaj yog tshuaj lom nyob rau hauv ib txoj kev. Kev noj ntev ntawm cov khoom noj tau los ntawm tsiaj uas muaj quinolones yog qhov phem rau tib neeg lub cev.

Kev noj zaub mov tsiaj txhu mus sij hawm ntev thiab cov khoom noj khoom haus kho mob patent Suav uas muaj cov tshuaj QNs tsawg tsawg tuaj yeem ua rau kis tau tus kab mob tiv thaiv tshuaj, yog li cuam tshuam rau kev ua haujlwm ntawm cov tshuaj no. Yog li ntawd, qhov teeb meem ntawm cov khoom seem quinolone tau nyiam ntau dua thiab ntau dua. Pawg Neeg Sib Koom Tes ntawm Cov Kws Tshaj Lij Khoom Noj Khoom Haus ntawm Lub Koom Haum Khoom Noj thiab Kev Ua Liaj Ua Teb ntawm United Nations thiab Lub Koom Haum Kev Noj Qab Haus Huv Ntiaj Teb thiab European Union tau tsim cov kev txwv siab tshaj plaws rau ntau yam quinolones hauv cov nqaij tsiaj txhu. US FDA tau tshaj tawm xyoo 2005 tias kev siv enrofloxacin , ib yam tshuaj tua kab mob siv los kho cov kab mob hauv cov nqaij qaib, raug txwv.

Tuam Tshoj kuj tau teev tseg rau xyoo 2002 qib siab tshaj plaws ntawm 7 QNs tshuaj suav nrog ciprofloxacin , danofloxacin, enrofloxacin , sarafloxacin, difloxacin, oxolinic acid thiab flumequine hauv cov leeg nqaij tsiaj yog 10 ～ 500μg / kg. Cov txheej txheem tseem ceeb ntawm kev tshuaj xyuas cov quinolones seem hauv cov nqaij tsiaj yog enzyme-linked immunosorbent assay (EL ISA), high performance liquid chromatography (HPLC) thiab kua chromatography 2 mass spectrometry (LC2MS).

2. Outlook

Quinolones , cov tshuaj tua kab mob dav dav, feem ntau yog siv rau kev kho mob rau tib neeg cov kab mob. Yuav kom tsis txhob muaj kev puas tsuaj rau tib neeg lub cev los ntawm kev noj cov khoom noj tsiaj uas muaj cov quinolone seem, nws yog ib qho tsim nyog los tsim cov tshuaj quinolone tshwj xeeb rau tsiaj.

Rau cov tsiaj tshwj xeeb, muaj sarafloxacin, enrofloxacin, danofloxacin, marbofloxacin, orbifloxacin, danofloxacin thiab lwm yam. Danoxacin tau siv los kho kab mob los ntawm cov kab mob thiab mycoplasma hauv nyuj, npua, qaib thiab lwm yam tsiaj, thiab muaj cov tshuaj tua kab mob zoo rau cov kab mob loj hauv lub ntsws ua pa. Orbifloxacin yog siv los kho mob ntsws thiab mob raws plab hauv npua thiab nyuj.

Txawm li cas los xij, nws yog qhov yuav tsum tau ntsuas kev nyab xeeb ntawm tsiaj tshwj xeeb quinolones rau tib neeg.

xaus

Quinolones muaj cov tshuaj tua kab mob dav dav thiab muaj zog tua kab mob. Ua ke nrog cov txheej txheem tshwj xeeb ntawm kev ua haujlwm ntawm quinolones, nws tuaj yeem siv nrog lwm cov tshuaj tua kab mob yam tsis txhawj txog kev tiv thaiv tshuaj.

BALLYA muab cov khoom siv kuaj mob Quinolones sai los qhia rau koj seb puas muaj cov quinolones seem hauv cov khoom noj mis nyuj uas koj noj txhua hnub.

References

• Wikipedia: Quinolone tshuaj tua kab mob
• NCO: Quinolones