Nreeb Navigation
Chloramphenicol yog cov tshuaj tua kab mob sib kis dav sib cais los ntawm Streptomyces venezuela. Nws muaj qhov cuam tshuam rau ntau yam kab mob aerobic gram-positive thiab kab mob gram-negative, anaerobic Bacteroides, Rickettsia, Chlamydia thiab mycoplasma, tshwj xeeb rau Salmonella, Influenza bacillus thiab Bacteroides, thiab lwm yam.
Chloramphenicol yog xim dawb lossis tsis muaj xim zoo li cov nplaim paj, nrog cov ntsiab lus melting 149.7 ~ 150.79C, yooj yim yaj hauv methanol, ethanol, propanol thiab ethyl acetate, me ntsis soluble hauv ether thiab chloroform, tsis yaj hauv roj av ether thiab benzene. Chloramphenicol yog qhov ruaj khov heev, thiab nws cov kua dej tsis poob tom qab 5 teev ntawm kev rhaub. Chloramphenicol molecule muaj pawg para-nitrophenyl, propylene glycol thiab dichloroacetamide pawg. Raws li muaj 2 asymmetric carbon atoms hauv chloramphenicol molecule, muaj 4 qhov isomers kho qhov muag ntawm chloramphenicol, uas tsuas yog L-isomer muaj peev xwm tua kab mob.
Cov tshuaj kev teeb tsa ntawm chloramphenicol muaj peb ntu: p-nitrophenyl, propylene glycol thiab dichloroacetamide, thiab nws cov tshuaj tua kab mob feem ntau cuam tshuam nrog propylene glycol.
Chloramphenicol yog xim dawb rau daj me ntsis, tsis muaj ntxhiab, iab heev, tsis yaj hauv dej, soluble hauv ethanol thiab acetone, thiab me ntsis soluble hauv benzene thiab roj av ether. Nws tuaj yeem tswj hwm nws cov tshuaj tua kab mob ntau dua 5 xyoos nyob rau hauv lub xeev qhuav, thiab cov kua dej txaus tuaj yeem tswj hwm nws cov haujlwm tau ntau lub hlis hauv lub tub yees lossis hauv qhov tsaus ntuj ntawm chav sov. Ib puag ncig alkaline yooj yim rhuav tshem nws cov tshuaj tua kab mob thiab ruaj khov rau cua sov. Cov ntsev ntsev ntawm chloramphenicol succinate muaj qhov ua tau zoo hauv dej thiab tsim nyog raws li kev npaj txhaj tshuaj. Cov tshuaj ester uas tseem tshuav tuaj yeem ua rau raug ncua lossis hmoov haum rau menyuam yaus txiav txim siab ntawm lawv cov kev iab.
Chloramphenicol tshuaj tua kab mob tuaj yeem ua haujlwm ntawm 50S subunit ntawm cov kab mob ribonucleoprotein lub cev thiab thaiv cov protein sib sau ua ke. Lawv yog cov tshuaj tua kab mob broad-spectrum antibacterial.
70S ribosome ntawm cov kab mob hauv lub cev yog lub hauv paus tseem ceeb ntawm cov cell rau kev sib txuas ntawm cov protein, thiab nws suav nrog ob lub subunits, 50S thiab 30S. Chloramphenicol thim rov qab khi rau 50S subunit txhawm rau thaiv qhov kev ua ntawm transpeptidylase, cuam tshuam nrog cov amino acid-tRNA davhlau ya nyob twg nrog cov amino acid thiab 50S subunit binding, yog li cuam tshuam kev tsim peptide saw tshiab thiab txwv tsis pub muaj protein ntau synthesis.
Txij thaum chloramphenicol tseem tuaj yeem khi rau 70S ntawm tib neeg mitochondria, nws tseem tuaj yeem tiv thaiv cov protein synthesis ntawm tib neeg mitochondria, ua rau muaj tshuaj lom rau tib neeg lub cev. Vim tias kev khi ntawm chloramphenicol rau 70S ribosomes yog thim rov qab, nws tau txiav txim siab ua cov kab mob bacteriostatic tshuaj tua kab mob, tab sis nws kuj tseem tuaj yeem muaj cov kab mob tua kab mob ntawm qee cov kab mob ntawm cov tshuaj ntau ntau, thiab nws tseem tuaj yeem ua haujlwm tau zoo rau mob khaub thuas bacilli ntawm qis dua
Chloramphenicol muaj qhov cuam tshuam rau ob qho tib si Gram-positive thiab Gram-negative cov kab mob, thiab muaj qhov muaj zog ntxiv rau tom kawg. Ntawm lawv, cuam tshuam rau tus kab mob typhoid bacillus, khaub thuas bacillus, parainfluenza bacillus thiab bacillus pertussis muaj zog dua lwm yam tshuaj tua kab mob. Nws kuj tseem muaj txiaj ntsig zoo tiv thaiv kab mob rickettsiae xws li mob khaub thuas, tab sis nws cov txiaj ntsig ntawm gram-positive cocci tsis zoo li tshuaj penicillin thiab tshuaj tetracycline. Cov kab mob tua kab mob ntawm kev ua haujlwm yog khi rau 50S subunit ntawm ribosome txhawm rau tiv thaiv peptide acyltransferase, yog li inhibiting protein hluavtaws.
Chloramphenicol tshuaj tua kab mob tuaj yeem ua haujlwm ntawm 50S subunit ntawm cov kab mob ribonucleoprotein lub cev thiab thaiv cov protein synthesis. Lawv yog cov tshuaj tua kab mob broad-spectrum antibacterial.
70S ribosome ntawm cov kab mob hauv lub cev yog lub hauv paus tseem ceeb ntawm cov cell rau kev sib txuas ntawm cov protein, thiab nws suav nrog ob lub subunits, 50S thiab 30S. Chloramphenicol thim rov qab khi rau 50S subunit txhawm rau thaiv qhov kev ua ntawm transpeptidylase, cuam tshuam kev sib xyaw ntawm cov amino acid-tRNA davhlau ya nyob twg thiab 50S kev sib cais subunit, yog li cuam tshuam kev tsim peptide saw tshiab thiab txwv tsis pub muaj protein ntau synthesis.
Txij thaum chloramphenicol tseem tuaj yeem khi rau 70S ntawm tib neeg mitochondria, nws tseem tuaj yeem tiv thaiv cov protein synthesis ntawm tib neeg mitochondria, ua rau muaj tshuaj lom rau tib neeg lub cev.
Nws yog cov tshuaj tua kab mob dav-spectrum antibacterial. Nws tuaj yeem tawg mus rau hauv cov kab mob sib kis los ntawm kev ua kom muaj roj ntau, feem ntau ua rau 50s ntawm cov kab mob 70s ribosome, txwv tsis pub transpeptidase, thaiv kev loj hlob ntawm peptide saw, txwv tsis pub tsim peptide saw, thiab tiv thaiv cov protein synthesis. Cov kab mob uas rhiab heev rau cov khoom no tseem muaj cov kab mob tua kab mob ntawm qhov siab.
Chloramphenicol feem ntau muaj qhov ua tau zoo ntawm cov kab mob Gram-tsis zoo dua li cov kab mob Gram-positive. Cov kab mob rhiab muaj xws li Enterobacteriaceae (xws li Escherichia coli, Enterobacter aerogenes, Klebsiella, Salmonella, thiab lwm yam) thiab Bacillus anthracis, pneumococcus, streptococcus, Listeria, Staphylococcus, thiab lwm yam Chlamydia, Leptospira thiab Rickettsia kuj tseem nkag siab cov khoom no. Cov khoom no tseem muaj txiaj ntsig zoo rau cov kab mob anaerobic xws li Clostridium tetani, Perfringens, Actinomycetes, Lactobacillus, Fusobacterium, thiab lwm yam.
Cov kab mob muaj kev txhim kho qeeb rau chloramphenicol thiab feem ntau tsim cov acetyltransferase tau los ntawm plasmid xa khoom. Qee hom kab mob qee yam kab mob (Pseudomonas aeruginosa, Proteus, Klebsiella, thiab lwm yam) kuj tseem tau hloov pauv qhov permeability ntawm cov phab ntsa ntawm cov kab mob, yog li ntawd chloramphenicol tsis tuaj yeem nkag mus rau cov kab mob thiab tiv taus.
Chloramphenicol tau ua tiav cais tawm thawj zaug hauv xyoo 1947. Nws tau muab tshuaj sib xyaws ua ke nyob rau xyoo tom ntej. Nws tau siv los ua tshuaj tua kab mob muaj txiaj ntsig zoo rau kev kho mob khaub thuas, kab mob rickettsial thiab lwm yam kab mob sib kis, tab sis tsawg leej ntawm lawv tau tshawb pom sai sai uas lawv tsim cov ntshav tsis txaus tom qab siv chloramphenicol. Qhov no yog qhov teeb meem hnyav ntawm tus neeg mob lub pob txha pob txha hematopoietic tsis ua haujlwm los ntawm cov tshuaj, yog li nws qhov kev thov dav dav raug txwv.
Txawm li cas los xij, txij li xyoo 1970, kev kis mob los ntawm kab mob khaub thuas bacillus thiab Bacteroides fragilis tiv taus ampicillin tau lees paub thiab maj mam nce ntxiv. Kev kho mob nyuaj yog qhov nyuaj, thaum chloramphenicol muaj txiaj ntsig zoo dua rau hom kab mob no. Cov xwm txheej ntawm chloramphenicol hauv kev kho mob tau txais kev tshuaj xyuas tshiab. Nws ntseeg tias txawm hais tias chloramphenicol muaj cov kab mob pob txha lom, nws tseem yog cov tshuaj tua kab mob muaj txiaj ntsig ntev li ntev tau nws tau siv raws li qhov xav tau. Tam sim no, nws tsuas yog siv hauv tsev kho mob rau kev kho mob ntawm cov kab mob sib kis saum toj no thiab mob khaub thuas, tab sis hauv daim ntawv thov, nws yog qhov yuav tsum tau ua nruj me ntsis ua raws cov lus qhia, siv qhov tsim nyog noj, thiab saib xyuas kom muaj tshuaj lom kom ua tiav lub hom phiaj ntawm kev nyab xeeb thiab siv tshuaj tau zoo.
Muaj cov pawg hauv qab no:
A. Cov ntshav
Aplastic anemia yog qhov hnyav tshaj plaws, uas feem ntau tshwm sim 2 txog 8 lub lis piam tom qab siv tshuaj, thiab cov neeg tuag ntau dua 50%. Nws tau tshwm sim raws li kev txo qis ntawm txhua lub qe ntshav, thiab feem ntau ntawm lawv tuag vim los ntshav, kis kab mob thiab lwm yam. Tsis muaj kev sib raug zoo ruaj khov ntawm nws qhov tshwm sim thiab ntau npaum li cas, thiab cov kab mob pathogenesis tsis paub meej thiab tej zaum yuav cuam tshuam nrog cov keeb kwm qub.
Lwm qhov yog tshuaj lom myelosuppression, nrog rau kev kuaj pom ntawm ntshav tsis txaus lossis leukopenia thiab thrombocytopenia. Nws tshwm sim muaj feem cuam tshuam nrog kev noj tshuaj ntau npaum li cas. Qhov teeb meem no nquag tshwm sim thaum cov ntshav cov ntshav ntau dua 25μg/ml, tab sis nws tuaj yeem rov zoo tom qab siv tshuaj. Nws cov kab mob tshwm sim yog qhov ua haujlwm ntawm mitochondria ntawm cov leeg pob txha hlwb los ua ke cov protein raug txwv ib ntus.
B. Grey tus menyuam mob
Cov menyuam mos thiab menyuam mos yug ntxov tau txais chloramphenicol ntau thiab ua rau cov hlab ntshav tsis ua haujlwm, uas tshwm sim raws li mob plab, ntuav, tawv nqaij daj, cyanosis, circulatory thiab ua tsis taus pa, thiab feem ntau tuag nyob rau ob peb teev tom qab pib. Cov kab mob tshwm sim yog qhov tsis muaj peev xwm khi ntawm daim siab glucuronic acid hauv cov menyuam mos ntxov lossis menyuam yug tshiab thiab tsis muaj peev xwm ntawm glomerulus los lim chloramphenicol, uas ua rau kom nce qib dawb chloramphenicol hauv lub cev thiab ncaj qha inhibits oxidative phosphorylation ntawm cov txheej txheem ntawm tes mitochondria.
C. Kev zom zaub mov
Ua rau me ntsis xeev siab, ntuav, raws plab, anorexia thiab lwm yam.
D. Lub paj hlwb
Ob peb tus neeg mob yuav muaj qhov muag tsis pom kev (neuritis) lossis kab mob hauv lub paj hlwb (peripheral neuritis). Tsawg tus neeg mob muaj mob taub hau, nyuaj siab, thiab puas hlwb.
Txij li thaum chloramphenicol tuaj yeem ua rau muaj kev phom sij loj, nws tsuas yog siv hauv tsev kho mob rau tus mob ua npaws ua rau mob typhoid, mob khaub thuas bacillus, mob Bacteroides fragilis hnyav, mob hauv lub paj hlwb, streptococcus pneumoniae lossis meningococcal meningitis thiab cov neeg mob penicillin-allergic.
Kev kawm ntev dhau los yuav tsum raug zam, thiab cov neeg mob uas muaj keeb kwm ntawm kev txawv txav hauv lub cev los ntawm cov tshuaj yuav tsum tsis txhob siv nws. Txhua tus neeg mob kho nrog chloramphenicol yuav tsum tau tshuaj xyuas cov qe ntshav dawb, reticulocytes thiab platelets thaum pib kho, thiab tshuaj xyuas txhua 3 rau 4 hnub. Yog tias leukopenia tshwm sim, cov tshuaj yuav tsum nres tam sim ntawd. Cov menyuam mos thiab menyuam yaus yuav tsum tau saib xyuas zoo thaum ua ntawv thov chloramphenicol, thiab kev saib xyuas cov ntshav tuaj yeem ua tau yog tias muaj kev tso cai.
Thiamphenicol thiab chloramphenicol yog tib chav tshuaj tua kab mob, tshwj tsis yog tias pawg nitro ntawm lub nplhaib benzene ntawm chloramphenicol tau hloov los ntawm pab pawg methylsulfone, thiab nws cov tshuaj tua kab mob zoo ib yam li ntawm chloramphenicol. Thiamphenicol feem ntau yog tshem tawm los ntawm ob lub raum, thiab qhov ua kom muaj zog hauv cov zis ntau dua li ntawm chloramphenicol. Yog li ntawd, qhov koob tshuaj yuav tsum tau txo qis thaum lub raum ua haujlwm tsis zoo. Txawm hais tias muaj hematological lom, tab sis lawv txhua qhov hloov pauv tau, thiab aplastic anemia tsis tshwm sim. Qee lub tebchaws ntseeg tias nws qhov ua tau zoo dua li chloramphenicol, tab sis Tuam Tshoj tsis xav li ntawd.
Feem ntau, chloramphenicol yog cov tshuaj tua kab mob muaj txiaj ntsig zoo, yog tias koj siv nws zoo. Chloramphenicol muaj ntau cov kev mob tshwm sim uas hnyav heev, tab sis nws muaj txiaj ntsig zoo dua li lwm yam tshuaj tua kab mob tiv thaiv kab mob typhoid bacilli, influenzae bacilli, parainfluenza bacilli, pertussis bacilli, kis kab mob xws li mob khaub thuas.
References