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Dab tsi yog-thiamphenicol

Methyl-sulfonyl analog ntawm chloramphenicol: Thiamphenicol

Muab lo rau  Lub ob hlis ntuj 11, 2021, Kho los ntawm Jason, Qeb  

Thiamphenicol yog dab tsi?

1. Lus txhais

Thiamphenicol yog cov tshuaj tua kab mob broad-spectrum of chloramphenicol, uas muaj qhov ua tau zoo ntawm cov kab mob Gram-negative ntau dua li cov kab mob zoo. Nws yog dawb rau dawb-dawb crystalline hmoov lossis muaju ntawm chav sov. Nws tuaj yeem nqus tau sai thiab ua tiav tom qab kev tswj hwm qhov ncauj. Nws yog feem ntau tawm ntawm cov zis hauv nws daim ntawv qub.

Clinically, nws feem ntau yog siv los kho kev ua pa, tso zis, kab mob siab hepatobiliary, typhoid thiab lwm yam kab mob xws li phais plab, phais menyuam thiab menyuam yaus thiab mob ENT, tshwj xeeb yog mob me me mus rau mob hnyav. Cov qauv tshuaj lom neeg zoo ib yam li chloramphenicol. Nws pawg methyl-sulfone hloov chaw nitro pawg ntawm chloramphenicol, uas txo nws cov tshuaj lom. Thaum nws cov kab mob tua kab mob yog 2.5-5 npaug ntau dua li ntawm chloramphenicol.

2. Cov teebmeem tshuaj

Nws cov kab mob tua kab mob thiab cov tshuaj tua kab mob zoo ib yam li cov chloramphenicol. Nws feem ntau nthuav tawm mus rau hauv cov kab mob hauv cov kab mob thiab rov thim rov qab mus rau 50S cov kab mob ntawm cov kab mob ribosome, thaiv qhov kev loj hlob ntawm peptide saw (tuaj yeem cuam tshuam qhov cuam tshuam ntawm transpeptidase), tiv thaiv kev sib txuas ntawm cov protein, yog li ua rau muaj cov kab mob tua kab mob.

Nws cov tshuaj tua kab mob ua tau zoo dua chloramphenicol tshwj tsis yog Streptococcus pyogenes, pneumococcus, Bacillus pertussis thiab Shigella sungii. Nws muaj qhov ua tau zoo ntawm cov kab mob Gram-positive xws li pneumococcus thiab hemolytic streptococcus; nws muaj qhov ua tsis tau zoo ntawm Staphylococcus aureus, Salmonella lossis Escherichia coli, Pneumoniae bacillus, thiab lwm yam tshaj li chloramphenicol. Nws kuj tseem muaj qee yam cuam tshuam rau cov kab mob anaerobic, spirochetes, rickettsia, amoeba, thiab lwm yam.

Thiamphenicol tsis yooj yim nkag mus rau cov kab mob cell phab ntsa, uas ua rau cov tshuaj tua kab mob hauv vitro me ntsis qaug zog dua chloramphenicol. Ntawm qhov tsis sib xws, thiamphenicol tsis khi rau glucuronic acid hauv lub siab, thiab cov ntsiab lus ntawm kev ua haujlwm dawb thiamphenicol hauv cov ntshav siab, yog li nws muaj zog tiv thaiv kab mob, thiab kev txhim kho cov kab mob tiv thaiv thiamphenicol qeeb. Thiab nws tau ua tiav hla kev tiv thaiv nrog chloramphenicol. Thiamphenicol tseem muaj qhov ua kom muaj zog tiv thaiv kab mob (kwv yees li 6 zaug muaj zog dua li chloramphenicol), uas tuaj yeem cuam tshuam cov tshuaj tiv thaiv kab mob immunoglobulin thiab tsim cov tshuaj tiv thaiv kab mob.

3. Pharmacokinetics

Thiamphenicol tau nqus tau zoo tom qab qhov ncauj lossis txhaj tshuaj, thiab nqus tau sai thiab ua tiav. Qhov siab tshaj plaws ntawm cov tshuaj plasma tau mus txog hauv 2 teev tom qab kev tswj hwm qhov ncauj thiab tsis pub dhau 1 teev tom qab txhaj tshuaj intramuscular.

Tom qab kev tswj hwm txhua 6 txog 8 teev, nws tuaj yeem nthuav tawm sai thiab dav hauv ntau cov ntaub so ntswg ntawm lub cev. Ntawm lawv, cov ntsiab lus hauv lub raum, tus po, lub siab, thiab lub ntsws yog siab dua, thiab cov ntsiab lus hauv lub raum thiab lub siab yog li 3 txog 4 zaug uas ntawm tib koob tshuaj chloramphenicol. Nws tuaj yeem ncav cuag qee qhov kev nkag siab hauv cov ntaub so ntswg. Vim tias muaj cov kab mob nkag mus rau hauv lub cev, cov concentration hauv cov kua tsib kuj tseem siab. Nws yog qhov yooj yim nkag mus rau cov ntshav-cerebrospinal kua teeb meem thiab nkag mus rau hauv lub paj hlwb, thiab tseem tuaj yeem nkag mus rau hauv cov mis thiab cov hnoos qeev hauv me me.

Plasma ib nrab ntawm lub neej yog 1.5h, thiab nws tau khi me ntsis rau cov ntshav protein. Thiamphenicol tsis ua ke nrog glucuronic acid hauv lub siab, thiab tawm los ntawm cov kua tsib hauv nws daim ntawv qub, thiab ib feem ntawm nws yog zais los ntawm lub raum tubules. 70% mus rau 90% ntawm cov tshuaj tau tso tawm hauv cov zis hauv 24 teev. Cov neeg laus noj 0.5g ntawm qhov ncauj, thiab tso zis ntau ntxiv tom qab 12 teev txog li 400μg/ml. Kev tso zis tso zis raug txo qis thaum lub raum ua haujlwm poob qis, thiab tej zaum yuav muaj qhov nyiam ua kom ntau ntau hauv lub cev.

Kev siv Thiamphenicol

Kev siv-ntawm-Thiamphenicol
Kev siv-ntawm-Thiamphenicol

1. indications

Thiamphenicol yog siv rau kev kis kab mob ntawm cov kab mob ua pa, kab mob siab hepatobiliary, cov tso zis thiab cov zom zaub mov los ntawm tus kab mob khaub thuas bacillus, E. coli, thiab Salmonella uas rhiab rau thiamphenicol. Nws kuj tseem muaj qee yam cuam tshuam rau ua npaws kub cev, kub cev paratyphoid thiab brucellosis; nws kuj tseem siv rau kab mob gonorrhea thiab gonococcal urethritis.

Clinically, nws yog siv los kho cov kab mob ua pa, tso zis, lub siab thiab lub zais zis, mob khaub thuas thiab lwm yam tsos mob ntawm kev phais plab, ob lub cev xeeb tub thiab poj niam txiv neej, thiab ENT kab mob, tshwj xeeb yog mob me me mus rau mob hnyav.

Hauv ntau qhov chaw kuaj mob tau teeb tsa los ntawm 15 lub tsev kho mob hauv Shanghai, tag nrho ntawm 344 tus neeg mob tau cuv npe, suav nrog 176 tus neeg mob uas ua pa, tso zis, tso zis, thiab mob plab zom mov, 121 tus kab mob ntsws, thiab 47 daim tawv nqaij. Cov txiaj ntsig zoo yog 88%, 86%, thiab 53%, feem. Ntawm lawv, kev kho mob pustular psoriasis tau muaj txiaj ntsig zoo tshaj plaws, thiab qhov xwm txheej tau tswj tau sai tom qab siv tshuaj. Raws li kev tshaj tawm txawv teb chaws, thiamphenicol tau ua tiav siv los kho tus kab mob gonococcal urethritis hauv Nyij Pooj thiab Europe. Ib koob tshuaj ntawm qhov ncauj ntawm 2.5g muaj cov txiaj ntsig zoo ib yam spectinomycin tshuaj thiab cefuroxime.

Txij xyoo 1960 txog 1974, Fab Kis ib leeg tau kho ntau dua 6 lab tus neeg mob thiamphenicol. Ntawm 15,796 tus neeg mob tau tshaj tawm los ntawm lub tsev kho mob, suav nrog tus kab mob gonorrhea, daim siab thiab gallbladder, tso zis, plab hnyuv, ua pa, mob qog noj ntshav thiab mob otolaryngology, nrog rau tus kab mob pertussis thiab salmonella, ntau dua 90% ua tiav "zoo" kho cov teebmeem.

Nws kuj tseem tau siv rau pustular psoriasis, 1 txog 1.5g ib hnub, muab faib ua ob zaug, chav kho mob yog 10 hnub txog 4 lub lis piam, kho 5 tus neeg mob, 4 tus neeg zoo. Tom qab siv tshuaj, ua npaws kub sai sai, cov pustules raug tswj, qhov mob sib koom tau raug txo qis, ua pob liab vog ploj lossis erythema ploj zuj zus.

2. Kev siv thiab ntau npaum li cas

  • Cov neeg laus: Kev tswj qhov ncauj: 1.5 ~ 3.0g ib hnub, faib ua 3 ~ 4 koob. Cua-soluble nqus tau: 5% txog 10% thiamphenicol tov tuaj yeem siv rau huab cua-soluble nqus tau. Intra-thoracic, kab noj hniav hauv plab, thiab zais zis: 0.5 ~ 1g txhua lub sijhawm.
  • Kev tswj qhov ncauj rau menyuam yaus: 25-50 mg/kg ib hnub hauv 4 qhov faib faib.
  • Rau tus mob khaub thuas: 3g hais lus txhua hnub rau thawj rau 3 hnub, 1.5ga hnub rau hnub plaub txog rau hnub thib rau, thiab 4g txhua hnub tom qab ntawd;
  • Rau tus kab mob gonorrhea: ib koob tshuaj 2.5g.
  • Kev txhaj tshuaj intramuscular, txhaj tshuaj txhaj tshuaj: koob tshuaj yog tib yam li qhov ncauj.

3. Veterinary tshuaj Thiamphenicol

Thiamphenicol yog tshuaj uas tib neeg thiab tsiaj siv tau. Nws yog siv rau txoj kev ua pa, tso zis thiab mob plab hnyuv tshwm sim los ntawm cov kab mob rhiab xws li Haemophilus influenzae, Escherichia coli, Salmonella, thiab lwm yam.

Veterinary Thiamphenicol yog lwm cov khoom lag luam ntawm chloramphenicol. Nws muaj cov tshuaj tua kab mob muaj zog los ntawm kev txwv tsis pub ua ke ntawm cov kab mob TRAN thiab ribosomes. Nws yog cov tshuaj siv tshuaj kho tsiaj nrog cov dav siv dav, tsis muaj tshuaj lom thiab tsis muaj seem thiab muaj zog tiv thaiv kab mob ntau dua li chloramphenicol. Nws muaj txiaj ntsig zoo hauv ib koob tshuaj. Cov ntshav ntshav tuaj yeem tswj tau ntau dua 17 teev, thiab cov txiaj ntsig muaj zog thiab kav ntev.

Nws feem ntau yog siv los kho mob plab thiab ua pa kab mob los ntawm Salmonella, E. coli thiab Pasteurella, xws li kub taub hau paratyphoid hauv cov menyuam yaus tsiaj, rub hauv plab menyuam, mob plab hauv menyuam yaj, rub tawm, nqaij qaib typhoid, salmonella enteritis hauv dev thiab miv, mob ntev sinusitis, Pneumonia, avian cholera, thiab lwm yam, thiab lub paj hlwb hauv cov dev thiab miv tshwm sim los ntawm cov kab mob anaerobic thiab prostatitis hauv cov dev thiab miv uas tshwm sim los ntawm cov kab mob gram-negative, thiab qhov muag kis kab mob thiab endometritis.

Raws li cov khoom noj ntxiv, nws muaj txiaj ntsig zoo tiv thaiv kev mob plab hnyuv ntawm npua thiab qaib los ntawm Salmonella.

Thiamphenicol tseem tuaj yeem kho tus kab mob liab liab, kab mob kis kab mob rau menyuam yaus, kab mob hauv plab, kab noj dub tshwm los ntawm Vibrio, Streptococcus, Pseudomonas, Edwards, thiab Aeromonas hauv ntses thiab cws, thiab kab mob gill rot, kab mob kab mob, cov kab mob hauv qhov quav, cov dej tuaj pwm kab mob, tshee tshee, ntses vibriosis, kab mob pseudomonas, kab mob ascites, kab mob Edwards, Suav roob ris kab mob, kab mob Herpes, kab mob qhov muag dawb.

Thiamphenicol phiv los

Thiamphenicol-side-effects
Thiamphenicol-side-effects

1. Cov kev phiv tshuaj

  • Kev tiv thaiv pob txha pob txha: Cov pob txha pob txha thim rov qab yog qhov cuam tshuam loj tshaj plaws ntawm cov tshuaj no. Qhov tshuaj tiv thaiv no cuam tshuam nrog kev siv tshuaj thiab chav kho mob, thiab nws yog ib txwm muaj rau cov neeg mob ntshav siab ntau dua 25μg/ml. Cov tsos mob tshwm sim yog ntshav tsis txaus, thiab tuaj yeem nrog nrog leukopenia thiab thrombocytopenia.
  • Aplastic anemia: Aplastic anemia tsis tshua muaj tom qab siv tshuaj. Cov tsos mob tshwm sim suav nrog ntshav ntws los ntawm thrombocytopenia, nrog rau petechiae, ecchymosis, thiab qhov ntswg los ntshav, nrog rau cov tsos mob ntawm tus kab mob tshwm sim los ntawm neutropenia, xws li kub cev, mob caj pas, thiab jaundice.
  • Grey baby syndrome: Tsis muaj lus ceeb toom ntawm "grey baby syndrome" tshwm sim los ntawm cov tshuaj hauv cov menyuam mos thiab menyuam yug tshiab. Tsuas yog cov xwm txheej ntawm cov xim daj ntseg ib ntus tau tshaj tawm.
  • Hepatotoxicity: Cov neeg mob uas muaj kab mob siab ua ntej yuav ua rau daj ntseg, daim siab ua rau lub cev rog dhau, thiab txawm tias mob hnyav heev tom qab siv tshuaj.
  • Kev ua xua: tawv nqaij ua pob, ua pob rau hnub ci, mob angioedema, ua npaws tshuaj thiab lwm yam kev tsis haum tshuaj tom qab siv tshuaj, thiab cov tsos mob tshwm sim me me, thiab lawv tuaj yeem rov zoo dua tom qab siv tshuaj.
  • Nervous system: Peripheral neuritis thiab optic neuritis tuaj yeem tshwm sim tom qab siv tshuaj ntev, pom tias hnov ​​tsis hnov ​​lus, tsis tsaug zog, pom kev xav tsis meej, tsis nco qab thiab lwm yam tsos mob ntawm lub paj hlwb, feem ntau thim rov qab. Kuj tseem muaj cov ntawv ceeb toom ntawm qhov muag tsis pom los ntawm qhov muag tsis pom tom qab siv tshuaj ntev.
  • Cov kab mob plab zom mov: Cov tsos mob ntawm txoj hnyuv xws li tsis qab los noj mov, xeev siab, ntuav, tsis xis nyob hauv plab thiab raws plab feem ntau tshwm sim tom qab noj tshuaj, thiab qhov tshwm sim yog li 10% lossis tsawg dua.
  • Kev kis tus kab mob ob zaug: Tom qab siv tshuaj ntev, cov paj ntoo ib txwm nyob hauv lub cev txo qis, ua rau kis mob ob zaug.
  • Lwm tus: Qee tus neeg mob uas muaj ntshav qab zib-6-phosphate dehydrogenase tsis txaus tuaj yeem tsim hemolytic anemia tom qab siv tshuaj; kev tswj hwm qhov ncauj mus sij hawm ntev tuaj yeem cuam tshuam cov hnyuv hauv lub cev thiab cuam tshuam kev sib xyaw ntawm cov vitamin K thiab ua rau muaj ntshav ntau ntxiv.

2. Thiamphenicol toxicity

Thiamphenicol antibacterial spectrum zoo ib yam li chloramphenicol, tab sis cov tshuaj tua kab mob tsis zoo li chloramphenicol. Kev nqus qhov ncauj tau ua tiav, thiab ntshav ib nrab ntawm lub neej yog 1.5h. Qhov koob tshuaj ib txwm rau cov neeg laus yog 1 txog 2g/d, faib ua 3 txog 4 zaug. Cov kev phom sij tsis zoo hauv kev siv cov tshuaj no tsawg dua li ntawm chloramphenicol, feem ntau yog cov kab mob plab zom mov, thiab tsis muaj tshuaj lom rau cov kab mob hematopoietic, uas tuaj yeem ua rau mob hlab ntsha hauv nruab nrog cev. Tsis muaj daim ntawv tshaj qhia txog tus menyuam grey syndrome. Cov neeg mob uas lub raum tsis txaus yuav raug kev txom nyem tag nrho lub taub hau.

Xeev siab, ntuav, tsis qab los noj mov, glossitis, thiab stomatitis tuaj yeem tshwm sim thaum siv qhov ncauj. Cov neeg mob uas muaj kab mob siab tam sim no tuaj yeem muaj jaundice, daim siab rog nkag mus, thiab txawm tias mob hnyav heev.

3. Teeb meem xav tau mloog

  • Cov ntshav yuav tsum tau kuaj xyuas tas li thaum lub sijhawm kho. Txog kev kho mus sij hawm ntev, yuav tsum suav cov reticulocyte kom pom qhov tsis zoo ntawm cov ntshav hauv lub sijhawm.
  • Yog tias cov qe ntshav dawb suav ntau zuj zus, cov tshuaj yuav tsum raug tso tseg tam sim ntawd.
  • Kev tshem tawm ntawm thiamphenicol tau txo qis hauv cov neeg mob uas lub raum tsis txaus, thiab tej zaum yuav muaj qhov sib txuam hauv lub cev thiab yuav tsum siv qis.
  • Txoj kev tooj tooj liab sulfate tuaj yeem ua rau muaj txiaj ntsig tsis raug thaum ntsuas cov piam thaj hauv zis.
  • Thaum siv tshuaj, ib puag ncig tag nrho cov ntshav yuav tsum tau tshuaj xyuas tas li; rau kev kho mob mus sij hawm ntev, yuav tsum suav cov reticulocyte; yog tias tsim nyog, kev kuaj pob txha yuav tsum tau ua txhawm rau txheeb xyuas qhov tsis zoo ntawm cov txheej txheem ntshav hauv lub sijhawm.
  • Thaum cev xeeb tub, tshwj xeeb yog thaum cev xeeb tub lig lossis yug menyuam, cov poj niam yuav tsum sim zam kev siv nws. Kev pub niam mis yuav tsum raug ncua rau cov poj niam pub niam mis.
  • Vim yog lub cev tsis muaj zog enzyme tsis zoo thiab lub raum ua haujlwm tsis zoo hauv cov menyuam mos, cov tshuaj raug tso tawm los ntawm ob lub raum qeeb dua li cov neeg laus, yog li thov thiamphenicol rau cov menyuam yug tshiab tuaj yeem yooj yim ua rau cov ntshav ntshav ntau dhau thiab cov tshuaj lom lom (cov tsos mob menyuam yaus).

Thiamphenicol kev cia siab

Thiamphenicol hydrochloride glycinate tau siv hauv tsev kho mob feem ntau yog siv rau kab mob ua pa, ua npaws kub taub hau, tso zis, tso zis, mob plab hnyuv, thiab mob ntsws ntev thiab lwm yam kab mob ntsws thib ob.

Thiamphenicol hydrochloride glycinate tuaj yeem nrawm hydrolyze hauv lub cev kom tso thiamphenicol thiab ua haujlwm tiv thaiv kab mob. Hauv kev kho mob thib ob ntawm cov kab mob sib kis hauv lub ntsws xws li mob hnoos hawb pob, thiamphenicol glycinate hydrochloride tuaj yeem tswj hwm los ntawm nqus pa thiab txhaj tshuaj ua pa, thiab thiamphenicol tuaj yeem tswj qhov ncauj lossis txhaj tshuaj lossis txhaj tshuaj.

Thiamphenicol hydrochloride glycinate tau kuaj pom tias nws muaj txiaj ntsig zoo thiab muaj kev nyab xeeb, uas tuaj yeem kho tus kab mob ntawm ntau yam kab mob rau kev xaiv tshuaj. Thiamphenicol hydrochloride glycinate rau kev txhaj tshuaj yog qhov tshwj xeeb hauv ib qho, yog li kev cia siab rau kev ua lag luam yog qhov ua tau zoo heev.

xaus

Thiamphenicol yog cov tshuaj tua kab mob dav dav ntawm chloramphenicol. Piv nrog chloramphenicol, cov tshuaj lom ntawm thiamphenicol qis dua. Tib lub sijhawm, thiamphenicol yog ntxiv rau chloramphenicol. Thiamphenicol muaj txiaj ntsig zoo rau cov kab mob tso zis, mob plab hnyuv thiab ua pa kab mob.

BALLYA muab a thiamphenicol xeem los qhia koj yog tias muaj thiamphenicol seem hauv cov khoom siv mis koj noj txhua hnub.

References

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