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Dab tsi-tshuaj tua kab mob-yog-macrolides

Cov tshuaj tua kab mob dab tsi yog macrolides?

Muab lo rau  Lub ib hlis ntuj 3, 2021, Kho los ntawm Jason, Qeb  

Macrolides yog dab tsi?

Cuam Tshuam yog cov lus dav dav rau chav kawm ntawm cov tshuaj tua kab mob nrog 12-16 carbon lactone ring hauv cov qauv txheej txheem, uas txwv tsis pub cov kab mob sib xyaw ua ke los ntawm kev thaiv cov haujlwm peptide acyltransferase hauv ribosome rau 50s.

Nws yog tus neeg sawv cev tiv thaiv kab mob sai, feem ntau yog siv rau kev kho mob xws li aerobic gram-positive thiab negative cocci, qee yam kab mob anaerobic, Legionella, Mycoplasma thiab Chlamydia. Cov kev tshawb fawb tau qhia tias ntxiv rau cov tshuaj tua kab mob, macrolide tshuaj tua kab mob kuj tseem muaj lwm yam kev siv tshuaj lom neeg dav.

Yog tias koj haus mis nyuj hauv tsev, Ballya tseem tuaj yeem ua macrolides kuaj qhia rau koj paub yog tias muaj macrolides seem hauv cov mis koj haus hauv 10 feeb.

Kev faib tawm Macrolides

Tshuaj tua kab mob macrolide xa mus rau 14 txog 16-membered macrolide tshuaj tua kab mob (xws li erythromycin derivatives, acetylspiramycin, thiab lwm yam). Qhov tseeb, cov tshuaj tua kab mob macrolide feem ntau suav nrog: 14 txog 16-membered macrolide tshuaj tua kab mob, 24- lossis 31-membered macrolide tshuaj tua kab mob (xws li tacorolimus thiab sirolimus) Sirolimus, tiv thaiv kab mob, polyene macrolide tshuaj tua kab mob (xws li amphotericin B thiab pentamycin, tshuaj tua kab mob fungal), thiab 18-membered tshiab macrolide tshuaj tua kab mob (fidaxomycin, tshuaj kho mob rau Clostridium difficile infection) thiab lwm yam.

Feem ntau hais lus, tus macrolide tshuaj tua kab mob hais txog cov tshuaj tua kab mob dav-dav uas tsim los ntawm Streptomyces. Lawv muaj cov qauv txheej txheem lactone yooj yim thiab ua tau zoo tiv thaiv kab mob Gram-positive thiab Gram-negative, tshwj xeeb tshaj yog tiv thaiv Mycoplasma, Chlamydia, Legionella, Spirochetes thiab Rickettsia.

Raws li tus naj npawb ntawm cov pa roj carbon muaj nyob hauv cov keeb ntawm cov qauv lactone, nws tuaj yeem faib ua 14-membered, 15-membered thiab 16-membered ring macrolide tshuaj tua kab mob. Kev ua lag luam macrolide tshuaj tua kab mob feem ntau tau muab faib ua peb pawg, uas yog, erythromycin tshuaj, medicin thiab tshuaj spiramycin. Erythromycin thiab nws (ester) derivatives (xws li erythromycin ethylsuccinate, roxithromycin, clarithromycin, dirithromycin thiab fluerythromycin) koom nrog 14-membered macrolide Antibiotics. Azithromycin muab los ntawm erythromycin tshuaj yog thawj 15-membered azamacrolide (azalide) tshuaj tua kab mob los ua lag luam, thaum midenomycin thiab nws cov txiaj ntsig, thiab spiramycin thiab nws cov txiaj ntsig tau los ntawm 16-membered macrolide. Ib qho ntxiv, cov khoom lag luam tshiab ketolides telithromycin kuj yog koom nrog 14-membered cov macrolides.

Lub npe hu ua thawj tiam macrolide tshuaj tua kab mob xa mus rau erythromycin tshuaj thiab nws cov ester derivatives. Cov khoom suav nrog erythromycin, erythromycin ethylsuccinate, erythromycin stearate, erythromycin ethyl carbonate, Erythromycin acetate, erythromycin lactobionate, erythromycin li al. Cov tshuaj tua kab mob macrolide tiam thib ob suav nrog azithromycinroxithromycin, clarithromycin, dirithromycin thiab tylosin. Cov tshuaj tua kab mob macrolide tiam thib peb tsuas yog ua lag luam telithromycin.

Erythromycin yog cov tshuaj tua kab mob macrolide tsim los ntawm Streptomyceserythreus. Nws muaj cov tshuaj tiv thaiv kab mob dav dav tiv thaiv kab mob ua pa rau sab sauv xws li Mycoplasma, Chlamydia thiab Legionella pneumophila, thiab tau siv dav los kho kab mob ua pa kab mob rau ntau dua plaub caug xyoo. Kev ua haujlwm qis ntawm erythromycin ntseeg tau tias yog los ntawm kev sib cuam tshuam ntawm nws 6-hydroxyl, 9-carbonyl, thiab 8-hydrogen, yog li nws tsis ruaj khov hauv cov kua qaub thiab sai sai ua rau cov khoom tsis muaj zog.

Qhov tsis txaus acid no ua rau erythromycin poob nws cov tshuaj tua kab mob thiab nws cov bioavailability tau txo qis heev. Yog li ntawd, kev hloov kho cov qauv ntawm cov chaw no thiab kov yeej lawv cov acid acid instability tau dhau los ua kev tshawb fawb hotspot hauv xyoo 1880s. Yog li, lub cim thib ob ntawm macrolide tshuaj tua kab mob-clarithromycin, azithromycin, roxithromycin, Dirithromycin thiab fluoroerythromycin tuaj ua, thiab lawv tau mus ua lag luam xyoo 1990. Piv nrog erythromycin, cov tshuaj macrolide tiam thib ob muaj cov yam ntxwv hauv qab no:

  • Ruaj khov rau cov kua qaub, muaj lub qhov ncauj siab bioavailability;
  • Ntshav tshuaj concentration, cov ntaub so ntswg thiab cov tshuaj intracellular concentration siab thiab ruaj khov;
  • Plasma ib nrab-lub neej tau ncua ntev, tshwj tsis yog tias ib nrab-lub neej ntawm rotamycin thiab miokamycin nyob ze rau ntawm erythromycin, lwm qhov yog ntev dua erythromycin. Plasma ib nrab-lub neej ntawm roxithromycin thiab azithromycin yog 8.4 ~ 15.5 h thiab 48 ~ 72 h feem, uas ua rau cov neeg mob ua raws;
  • Qhov tsis zoo ntawm lub plab zom mov tshwm sim los ntawm nws kuj tseem me me.
ClassificationTus sawv cev
Cuam Tshuam1. 14 lub nplhaib: erythromycin, clarithromycin, roxithromycin, dierythromycin thiab hais txog.
2. 15-ntiv nplhaib: Azithromycin.
3. 16 - ntiv nplhaib: Medemycin, kitasamycin, spiramycin, thiab lwm yam.
Cov tshuaj tua kab mob KetolactoneCov qauv zoo ib yam rau cov tshuaj tua kab mob macrolide, lawv nquag siv los kho kab mob ua pa los ntawm cov kab mob tiv taus cov tshuaj tua kab mob macrolide, xws li telomycin quinerythromycin.
Tsis-antimicrobial macrolidesXws li tacrolimus, pimelimus, thiab sirolimus, siv los ua tus kab mob plague-inhibitor lossis ua tus tswj kab laum-kab mob plague.
Tshuaj lom macrolidesCov tshuaj lom ua los ntawm cov kab mob thiab siv feem ntau hauv kev kho mob Mycobacterium.

Macrolides Mechanism ntawm kev nqis tes ua

Macrolides-Mechanism-of-action
Macrolides-Mechanism-of-action

Dab tsi txhua tus paub nrog yog cov tshuaj tua kab mob ntawm macrolides. Ntxiv rau, macrolides muaj lwm yam teebmeem.

1. Cov kab mob tua kab mob

Nws ua los ntawm inhibiting synthesis ntawm cov protein. Feem ntau nws yog tus kab mob bacteriostatic sai thiab muaj tshuaj tua kab nyob rau qhov siab.

Nws muaj txiaj ntsig zoo tiv thaiv kab mob G+ feem ntau, qee cov kab mob G, kab mob hauv lub cev thiab qee cov kab mob atypical (muaj cov tshuaj tua kab mob muaj zog tiv thaiv Staphylococcus, ntau pab pawg streptococci, pneumococcus, tetanus, anthracis, diphtheria, gonococcus Serratia, Neisseria meningitidis, Bacillus pertus, Legionella, thiab lwm yam; nws kuj muaj cov tshuaj tua kab mob zoo tiv thaiv kab mob atypical xws li Treponema pneumoniae, Leptospira, Mycoplasma mob ntsws, Chlamydia, Toxoplasma gondii, thiab atypical mycobacterium.)

Macrolides muaj zog tom qab siv tshuaj tua kab mob (PAE) tiv thaiv aerobic G+ cocci.

2. Cov nyhuv tsis-antibacterial

Ntxiv nrog rau cov tshuaj tua kab mob ntawm cov tshuaj macrolides, lawv kuj ua lub luag haujlwm tseem ceeb hauv kev tiv thaiv kab mob thiab tswj kev tso pa tawm, tswj kev tiv thaiv kab mob, thiab txuag cov tshuaj hormones.

Los tiv thaiv thiab tswj kev tso pa tawmNws muaj feem cuam tshuam rau kev txwv tsis pub tso tawm cov tshuaj ua kom sib cuam tshuam, txo qis tso zis, txo qis neutrophil chemotaxis thiab nplaum, thiab txhawb kev mob qog noj ntshav apoptosis.
Kev Siv Tshuaj Tiv ThaivMacrolides tseem tuaj yeem cuam tshuam nrog cov kab mob sib txuas ua ke cov protein ntau txawm tias qis dua MIC, qhia tias cov tshuaj tiv thaiv kab mob ntawm cov tshuaj no tsis yog nyob ntawm lawv cov tshuaj tua kab mob ncaj qha, tab sis lawv cov tshuaj tiv thaiv kab mob, uas yog qhov cuam tshuam ncaj qha.
Hormone txuag nyhuvTxo qhov ntau npaum li cas ntawm cov tshuaj hormone-dependent lossis cov tshuaj tiv thaiv mob hawb pob thiab txo qhov tsis zoo ntawm cov tshuaj hormones.
Cov tshuaj tua kab mobIntercellular adhesion molecule-1 yog rhinovirus receptor ntawm cov hlab ntsws epithelial. Macrolides siv cov tshuaj tiv thaiv kab mob los ntawm kev txwv nws txoj cai, thiab tseem tuaj yeem tiv thaiv kev tsim cov tshuaj tua kab mob cytokines uas tshwm sim los ntawm kev kis tus kab mob.
Txhawb kev mob plab zom movErythromycin muaj cov nyhuv zoo li motilin thiab tuaj yeem txhawb kev zom plab.

Cov ntaub ntawv kho mob

Raws li peb hais los saum no, cov tshuaj macrolide muaj cov kab mob antibacterial thiab tsis-antibacterial. Yog li, thaum peb tham txog daim ntawv thov kho mob, peb kuj tham txog nws los ntawm ob yam no.

1. Clinical daim ntawv thov ntawm antibacterial

Macrolides tuaj yeem ua rau feem ntau cov kab mob

A. Kab mob Streptococcal

Nws tuaj yeem siv los kho mob tonsillitis, mob pharyngitis, sinusitis, kub taub hau, cellulitis, thiab lwm yam tshwm sim los ntawm streptococcus.

B. Kab mob Legionnaires

Nws tuaj yeem kho mob ntsws thiab mob ntsws tau txais los ntawm zej zog los ntawm Legionella pneumophila, Legionella mykdad thiab lwm yam kab mob Legionella.

C. Kab mob Mycoplasma thiab Chlamydia

Nws tuaj yeem kho kab mob qhov muag xws li kab mob sib kis los ntawm Chlamydia trachomatis; kab mob ua pa xws li mob ntsws thiab mob ntsws ua rau mob ntsws ntsws/chlamydia; thiab cov kab mob urogenital xws li mob urethritis, ncauj tsev menyuam thiab kab mob hauv lub plab los ntawm bronchial/chlamydia.

D. Corynebacterium tus kab mob

Nws tuaj yeem kho tus mob diphtheria, kab mob coryneform, sepsis, thiab lwm yam. Erythromycin tuaj yeem tshem tawm tus kab mob diphtheria bacillus thiab ua tau zoo txhim kho qhov mob ntawm tus neeg mob kis mob diphtheria thiab mob hnyav. Qhov ua tau zoo tuaj yeem ncav cuag 90% hauv cov neeg laus, tab sis nws tsis tuaj yeem hloov pauv qhov kev kis mob hnyav.

E. Kab mob Helicobacter pylori

Clarithromycin tuaj yeem ua ke nrog lwm cov tshuaj kom tshem tawm Helicobacter pylori kev kis mob.

F. Kab mob Mycobacterium avium

Clarithromycin thiab azithromycin tuaj yeem siv rau kev kho mob ntawm mycobacteria uas tsis muaj mob xws li Mycobacterium avium hauv cov neeg mob tsis muaj tshuaj tiv thaiv kab mob.

G. Lwm Yam

Nws tuaj yeem hloov pauv penicillin rau cov neeg mob staphylococcal, streptococcal lossis pneumococcal kis mob rau penicillin. Nws kuj tseem tuaj yeem siv los kho cov tawv nqaij thiab cov nqaij mos mos kis los ntawm cov kab mob rhiab. Nws tuaj yeem siv los ua lwm yam tshuaj rau kev kho mob ntawm cryptosporidiosis thiab toxoplasmosis.

2. Kev siv tshuaj kho mob lwm yam tshaj li cov tshuaj tua kab mob

Qhov thib ob, qhov tsis-tiv thaiv kab mob ntawm macrolides kuj tseem siv dav hauv tsev kho mob.

A. Kab mob ua pa

Tshuaj tiv thaiv kab mob, tswj kev tso pa tawm thiab tiv thaiv kab mob tiv thaiv kab mob macrolides uas tsis vam khom cov kab mob tua kab mob yog qhov laj thawj tseem ceeb rau lawv siv thoob plaws hauv cov pa.

a Diffuse panbronchiolitis (DPB)

Cov tshuaj muaj txiaj ntsig zoo tshaj plaws rau kev kho DPB (16-lub ntsej muag lub ntsej muag tau ua pov thawj tsis muaj txiaj ntsig), thiab nws cov txheej txheem ntawm kev nqis tes cuam tshuam nrog nws cov tshuaj tiv thaiv kev cuam tshuam thiab muaj peev xwm tswj kev tiv thaiv kab mob, thiab muaj me ntsis ua nrog tiv thaiv kab mob.

b. Mob ntev sinusitis (CRS)

Tam sim no, ntau dua 30% ntawm cov neeg mob CRS tseem muaj cov tsos mob uas nyuaj rau kev tswj hwm tom qab kho tas. Biofilm tej zaum yuav yog qhov tseem ceeb hauv kev tshwm sim thiab ua haujlwm tsis tu ncua thiab rov ua dua CRS. Yog li ntawd, cov tshuaj uas tuaj yeem decompose lossis tiv thaiv kev tsim cov biofilms tau dhau los ua qhov kev xaiv tshiab rau kev kho mob refractory CRS.

Macrolides muaj lub luag haujlwm tiv thaiv kev kis kab mob, tiv thaiv kab mob, tiv thaiv kev tiv thaiv kab mob, tiv thaiv cov hnoos qeev, thiab tiv thaiv kab mob biofilm tsim. Lawv tau siv hauv tsev kho mob los kho tus mob CRS.

European Society of Allergy thiab Clinical Immunology CRS thiab Nasal Polyp Diagnosis and Treatment Guidelines (EPOS 2012 Edition) tau taw qhia tias kev siv cov tshuaj macrolide mus ntev xws li clarithromycin hauv kev kho mob sinusitis ntev tuaj yeem ua tau zoo ib yam li kev phais lossis kev siv tshuaj hormone. .

Suav CRS Kev Txheeb Xyuas thiab Kev Qhia Kho Mob Suav (tsab ntawv 2012) taw qhia: 14-ntiv nplhaib cov tshuaj macrolide tuaj yeem siv rau CRS yam tsis muaj qhov ntswg, kho cov tshuaj tsis zoo, tsis muaj eosinophilia, IgE ib txwm, tsis haum tshuaj Tsis ua xua CRS cov neeg mob kuaj tsis zoo. Nws raug nquahu kom txhaj tshuaj me me cov macrolides (1/2 qhov koob tshuaj pom zoo) tau noj qhov ncauj ntev, thiab chav kawm ntawm kev kho yuav tsum tsis txhob luv dua 12 lub lis piam.

c. Cov kab mob ntsws ntev ntev (COPD)

Xyoo 2007 Cov Lus Qhia rau Kev Txheeb Xyuas thiab Kho Tus Mob Nyuaj Mob Nyuaj Nyuaj Hauv Suav Tebchaws tau taw qhia tias rau kev mob hnyav ntawm qib I thiab II COPD, cov kab mob me me feem ntau yog Haemophilus influenzae, Streptococcus pneumoniae, Moraxella catarrhalis, thiab lwm yam. Macrolides tuaj yeem siv rau kev kho mob. .

Xyoo 2014, Lancet Phau Ntawv Xov Xwm Kev Kho Mob Ua Ntej tau qhia tias azithromycin yuav tsum raug txiav txim siab raws li kev saib xyuas kev kho mob rau cov neeg mob COPD uas muaj kev tawm tsam ntau zaus thiab tiv taus cov txheej txheem kev kho mob.

Xyoo 2015, American Thoracic Society/European Society of Respiratory Diseases "Kev Pom Zoo ntawm Cov Kab Mob Nyuaj Quaj Mob" tau taw qhia tias kev siv lub sijhawm ntev cov macrolides tuaj yeem tiv thaiv kev ua kom rov zoo dua qub ntawm COPD.

Ib qho ntxiv, macrolides kuj tseem tuaj yeem kho tus mob bronchiectasis, pulmonary cystic fibrosis, mob hawb pob, cryptogenic teeb tsa kev mob ntsws, thiab kab mob ua pa. Txawm li cas los xij, qee qhov pov thawj tam sim no tsis txaus lossis muaj teeb meem, thiab xav tau kev tshawb fawb ntxiv los txheeb xyuas lawv.

B. Kab mob plab zom mov

Raws li tus motilin receptor agonist, nws tuaj yeem txhawb txoj hnyuv peristalsis. Tam sim no, erythromycin thiab azithromycin feem ntau siv.

Nws tuaj yeem siv rau kev kho mob ntawm lub plab zom mov tsis zoo xws li mob plab zom mov neurogenic mob, mob tom qab phais plab zom mov tsis meej, mob plab; vim nws cov tshuaj tiv thaiv HP, nws tuaj yeem siv los kho mob plab.

C. Cov qog nqaij hlav

Vim tias nws cov tshuaj tiv thaiv kab mob tshwj xeeb, nws tuaj yeem siv los kho cov qog, xws li erythromycin thiab roxithromycin. Ib qho ntxiv, peb yuav tsum tau ceev faj ntawm 2018 Asmeskas FDA ceeb toom tias kev siv azithromycin mus sij hawm ntev tom qab kev hloov pauv qia cell hematopoietic tuaj yeem ua rau muaj kev pheej hmoo ntawm cov qog nqaij hlav rov tshwm sim.

D. Cov kab mob tiv thaiv kab mob

Nws feem ntau yog siv hauv cov xwm txheej cuam tshuam nrog HP kis, xws li mob caj dab rheumatoid. Nws kuj tseem tuaj yeem kho cov kab mob autoimmune zoo xws li alopecia areata, autoimmune thrombocytopenic purpura thiab Sjogren's syndrome.

E. Kab mob ntawm daim tawv nqaij

Nws tau siv los kho cov kab mob ntawm daim tawv nqaij uas tsis zoo xws li psoriasis, vitiligo, ua xua purpura, thiab rosacea los ntawm ntau lub tswv yim xws li tiv thaiv HP, tiv thaiv kev mob, tiv thaiv kev ua xua thiab tiv thaiv kab mob.

Macrolides Kev phiv tshuaj

Macrolides-Sab-teebmeem
Macrolides-Sab-teebmeem

1. Txoj hnyuv tsis ua haujlwm

Feem ntau, nws tuaj yeem cuam tshuam nrog kev mob plab zom mov. Qhov tshwm sim ntawm erythromycin siab dua li lwm cov tshuaj.

2. Kev puas siab puas ntsws thiab ua xua dermatitis

Lub siab puas yog me me ntawm qhov ib txwm muaj, thiab daim ntawv thov loj-ntev mus ntev tuaj yeem ua rau tus kab mob siab mob cholestatic. Tom qab esterification, cov tshuaj xws li roxithromycin, erythromycin ethylsuccinate, thiab azithromycin muaj feem ntau ua rau mob cholestatic jaundice, yog li lawv yuav tsum siv sijhawm luv. Zam lossis tsis siv nws thaum cov ntshav transaminase nce ntau dua peb npaug ntawm qhov txwv ib txwm.

3. arrhythmia

Cuam Tshuam tuaj yeem ua rau QT ncua sijhawm mus ntev, thiab tuaj yeem ua rau torsades de pointes, thiab txawm tias lub plawv tsis ua haujlwm lossis tuag sai sai. Txawm hais tias qhov xwm txheej tsis zoo no tsis tshua muaj, nws ua rau tuag taus. Xyoo 2013, Tsoom Fwv Saib Xyuas Khoom Noj thiab Tshuaj Hauv Teb Chaws Asmeskas tseem tau tshaj tawm lus ceeb toom tias azithromycin muaj peev xwm ua rau tuag taus. Yog li ntawd, cov neeg mob uas muaj kev pheej hmoo ntawm lub plawv dhia yuav tsum ntsuas qhov zoo thiab qhov tsis zoo ua ntej siv tshuaj.

4. Ototoxicity

Kev siv tshuaj ntev tuaj yeem ua rau hnov ​​lus tsis zoo, tsis zoo, thiab tinnitus, uas tsis tshua muaj thiab nyob ntawm qhov xav tau koob tshuaj. Feem ntau nws tshwm sim tsis pub dhau 1-2 lub lis piam ntawm kev siv tshuaj, thiab nws muaj peev xwm tshwm sim thaum siv tshuaj ntau. Nws tuaj yeem rov zoo tom qab siv tshuaj lossis txo qhov koob tshuaj.

5. Lwm tus

Kev ua xua, ua rau lub paj hlwb puas, thiab lwm yam.

xaus

Nws yuav tsum raug sau tseg tias daim ntawv thov mus sij hawm ntev ntawm cov macrolides tau coj los txog qhov teeb meem tiv thaiv tshuaj tua kab mob. Cov tshuaj tiv thaiv tus nqi tau nce ob npaug hauv 10 xyoo dhau los, thiab cov naj npawb ntawm cov tshuaj sau tshuaj muaj feem cuam tshuam nrog cov tshuaj tiv thaiv tus nqi hauv cheeb tsam. Yog li siv cov tshuaj kom tsim nyog thiab zam kev tsim txom.

References

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