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Yog-spiramycine-a-macrolide

Puas yog spiramycine yog macrolide?

Muab lo rau  Lub ib hlis ntuj 15, 2021, Kho los ntawm Jason, Qeb  

Spiramycine yog dab tsi?

1. Lus txhais

Spiramycin yog hmoov dawb lossis daj me ntsis, muaj ntxhiab me ntsis; me ntsis hygroscopic. Spiramycine yog soluble hauv methanol, ethanol, acetone thiab ether, yuav luag tsis yaj hauv dej, thiab tsis yaj hauv roj av ether. Nws yog ib qho macrolide hmoov tshuaj tua kab mob tau txais los ntawm kab lis kev cai nruab nrab ntawm Streptomyces ambofaciens. Spiramycin yog acetate ntawm acetylspiramycin. Tom qab kev tswj hwm qhov ncauj, pab pawg acetyl raug tshem tawm kom pom muaj zog tiv thaiv kab mob. Spiramycin yog ib tus kab mob bacteriostatic muaj zog, thiab nws muaj cov kab mob tua kab mob tsuas yog nyob rau qhov siab heev.

Spiramycine muaj cov tshuaj tua kab mob muaj zog thiab cov kab mob tua kab mob tom qab lub cev (PAE) hauv lub cev, tuaj yeem txhim kho phagocytosis ntawm phagocytes, thiab tau nthuav dav hauv lub cev. Spiramycine muaj qhov siab dua hauv cov ntaub so ntswg ntau dua erythromycin tshuaj thiab muaj cov kev mob tshwm sim tsawg dua li erythromycin. Spiramycine tuaj yeem siv los kho pob ntseg, qhov ntswg, caj pas thiab kab mob ua pa los ntawm cov kab mob gram-positive thiab qee yam kab mob gram tsis zoo. Nws yog qhov tsim nyog rau kev kho mob ntawm otitis media, periodontitis, mob sinusitis thiab lwm yam kab noj hniav hauv qhov ncauj thiab pob ntseg pob ntseg pob ntseg los ntawm cov kab mob rhiab. Nws kuj tseem tuaj yeem siv los kho tus mob toxoplasmosis.

Spiramycin (SPM) yog cov tshuaj tiv thaiv kab mob macrolide kaum rau. Nws cov acetylated derivative, acetylspiramycin, muaj cov yam ntxwv ntawm cov ntaub so ntswg siab, tsis muaj tshuaj lom, thiab ua haujlwm ntev vivo. Nws muaj txiaj ntsig zoo rau mob qog noj ntshav, mob qog ntshav hauv lub cev thiab periodontitis. Omura siv kev sim isotope los ua pov thawj tias lub nplhaib lactone ntawm SPM tau tsim los ntawm 5 cov molecules ntawm acetic acid, 1 molecule ntawm propionic acid, 1 molecule ntawm butyric acid thiab 1 molecule ntawm qhov tsis paub ua ntej (ob chav carbon).

Kev sib xyaw biosynthesis ntawm lub nplhaib lactone pib los ntawm cov qauv ntawm propionyl-CoA, ua raws los ntawm cov qauv ntawm 2-methylmalonyl-CoA. Peb cov pa roj carbon sib txuas tsis yog tsuas yog ua cov txheej txheem ua ntej rau biosynthesis ntawm SPM, tab sis tseem ua kom muaj kev sib txuas ntawm propionyl-CoA carboxylase. Peb lub mycaminoses hauv cov molecule tau muab los ntawm cov piam thaj ua tiav, N-methyl thiab C-methyl pawg ntawm mycaminos tau muab los ntawm methionine, thiab qhov chaw ntawm nitrogen atoms ntawm N-methyl pawg tsis tau piav qhia meej.

2. Cov teebmeem tshuaj

Rovamycine yog macrolide tshuaj tua kab mob tau txais los ntawm kab lis kev cai nruab nrab ntawm Streptomyces ambofaciens. Spiramycin yog acetate ntawm acetylspiramycin. Tom qab kev tswj hwm qhov ncauj, pab pawg acetyl raug tshem tawm kom pom muaj zog tiv thaiv kab mob. Rovamycine yog tus muaj zog bacteriostatic tus neeg sawv cev, thiab nws muaj cov kab mob tua kab mob tsuas yog nyob rau qhov siab heev. Nws cov txheej txheem tua kab mob yog tib yam li erythromycin. Los ntawm kev koom ua ke nrog 50S subunit ntawm cov kab mob ribonucleoprotein lub cev, nws tiv thaiv kev txuas ntxiv ntawm peptide saw thiab cuam tshuam rau kev sib txuas ntawm cov kab mob protein kom ua tiav cov tshuaj tua kab mob.

Cov kab mob tua kab mob ntawm spiramycin zoo ib yam li erythromycin, thiab nws cov tshuaj tua kab mob tsis muaj zog li erythromycin, thiab nws lub qhov ncauj bioavailability kuj tseem qis dua erythromycin. Txawm li cas los xij, ntau yam erythromycin-resistant Staphylococcus aureus yog rhiab rau spiramycin. Ib qho ntxiv, spiramycin muaj cov tshuaj tiv thaiv kab mob tom qab zoo dua li erythromycin.

Cov kab mob tau pom ib nrab kev tiv thaiv kab mob rau spiramycin thiab erythromycin. Spiramycine muaj cov tshuaj tua kab mob muaj zog tiv thaiv Staphylococcus aureus, hemolytic streptococcus, pneumococcus, diphtheria, Bacillus anthracis thiab Clostridium; ntxiv rau, spiramycine muaj cov tshuaj tua kab mob muaj zog tiv thaiv Listeria thiab Catabranham Bacteria, Neisseria gonorrhoeae, Campylobacter fetus, Bacillus influenzae, Bacillus pertussis, Bacteroides, Perfringens, Propionibacterium acnes, Peptococcus thiab Peptostreptococcus, Chlamydia, Treponema pallidum, Toxoplasma, Cryptosporidium thiab lwm yam.

3. Pharmacokinetics

Qhov ncauj acetylspirillum spiramycin tsis muaj kev cuam tshuam los ntawm cov kua qaub, li 40% tau nqus. Qhov ncauj spiramycin 100mg, 200mg, mus txog qhov siab tshaj plaws ntshav hauv 2h, feem 0.8mg/L, 1mg/L. Cov tshuaj tau nthuav dav dav tom qab nqus tau. Kev mloog zoo nyob hauv cov zis, pus, hnoos qeev hauv lub ntsws thiab cov nqaij hauv lub ntsws yog siab dua cov ntshav cov ntshav, thiab thaum cov ntshav cov ntshav poob mus rau qhov tsawg kawg nkaus, tseem muaj cov tshuaj siab ntau nyob hauv cov nqaij.

Qhov siab ntawm cov tshuaj hauv lub cev yog siab hauv lub ntsws, lub siab, thiab cov kua tsib (cov concentration hauv cov kua tsib tuaj yeem ncav cuag 7-10 npaug ntawm cov ntshav cov ntshav). Spiramycin tuaj yeem nkag mus rau hauv macrophages, ntxiv rau los ntawm cov teeb meem hauv plab thiab cov ntshav-cerebrospinal kua teeb meem. Cov concentration ntawm cov kua dej hauv lub paj hlwb yog 65% ntawm cov ntshav siab. Tom qab cov tshuaj tau nqus, nws yog thawj zaug metabolized hauv lub siab rau acetylspiramycin. Ib nrab-lub neej ntawm spiramycin ntev dua li ntawm erythromycin thiab acetylspiramycin, thiab nws sib sau ua ke hauv lub cev tom qab rov ua dua.

Spiramycin siv

Spiramycin-siv
Spiramycin-siv

1. indications

  • Nws yog qhov tsim nyog rau kev kho mob ntawm cov kab mob ua pa thiab cov tawv nqaij thiab cov nqaij mos mos ua los ntawm cov kab mob rhiab, suav nrog: pharyngitis, tonsillitis, mob ntsws, mob ntsws, pyoderma, erysipelas thiab ua npaws liab.
  • Nws yog qhov tsim nyog rau kev kho mob ntawm qhov ncauj thiab otolaryngology kis los ntawm cov kab mob rhiab, xws li otitis media, periodontitis, thiab mob sinusitis.
  • Nws kuj tseem tuaj yeem siv los kho tus mob toxoplasmosis.

2. siv

Cov kab mob tua kab mob ntawm spiramycine zoo ib yam li lwm yam macrolide hmoov tshuaj tua kab mob. Vim tias kev tso tawm qeeb thiab cov ntaub so ntswg muaj zog, cov tshuaj tua kab mob hauv lub cev zoo dua li cov tshuaj tua kab mob zoo sib xws, tshwj xeeb tshaj yog rau pneumococcus thiab streptococcus.

Ntawm qhov tod tes, vim kev tso tawm qeeb, tsiaj txhu thiab nqaij qaib rau tib neeg noj yuav tsum siv sijhawm ntev dua cov tshuaj ua ntej raug tua.

Spiramycine yog tshuaj tua kab mob macrolide. Nws cov kab mob tua kab mob zoo ib yam li erythromycin. Nws feem ntau muaj kev cuam tshuam rau Gram-positive cov kab mob thiab qee cov kab mob Gram-negative, rickettsiae thiab cov kab mob loj, xws li streptococcus, meningococcus, Bacillus pertussis, Mycoplasma pneumoniae, Bacillus diphtheria, Chlamydia trachomatis, Leptospira thiab Clostridium thiab lwm yam Spiramycine muaj kev cuam tshuam zoo rau cov kab mob tiv taus tshuaj penicillin, tshuaj streptomycin, tshuaj tetracycline thiab chloramphenicol. Clinically nws feem ntau yog siv rau kev kis kab mob los ntawm ntau yam kab mob rhiab, xws li kab mob hauv lub ntsws, kab mob tso zis, mob meningitis, mastitis, osteomyelitis, kub taub hau, otitis media, kab mob hauv qhov ncauj thiab qhov ncauj thiab mob ntsws.

Spiramycine muaj cov tshuaj tua kab mob muaj zog thiab tiv thaiv kab mob tiv thaiv kab mob (PAE) hauv vivo, uas tuaj yeem txhim kho phagocytosis ntawm phagocytes. Acetylspiramycin yog cov tshuaj tua kab mob nrog cov tshuaj tua kab mob uas muaj 16-membered macrolide ring, thiab nws cov txiaj ntsig tau zoo uas tsis muaj kev phom sij loj, thiab feem ntau yog siv thawj qhov kev xaiv rau kis kab mob xws li kab mob aerobic gram-positive thiab anaerobic cocci, nrog rau hloov rau tib neeg ua xua rau beta lawm tshuaj tua kab mob.

3. pab

  • Cov neeg laus: 0.8 ~ 1.2g ib hnub, faib ua 3 ~ 4 zaug; rau cov mob hnyav, nws tuaj yeem nqa mus txog 1.6 ~ 2g ib hnub.
  • Cov menyuam yaus: Qhov koob tshuaj txhua hnub yog 20-30 mg/kg, siv li 2 txog 4 zaug.

4. Acetylspiramycin

A. Txhais

Acetylspiramycin yog acetate ntawm spiramycin. Tom qab kev tswj hwm qhov ncauj, pab pawg acetyl raug tshem tawm kom pom muaj zog tiv thaiv kab mob. Acetylspiramycin yog tus muaj zog bacteriostatic tus neeg sawv cev, thiab tsuas yog muaj cov kab mob tua kab mob ntawm cov tshuaj ntau ntxiv.

Nws cov txheej txheem tua kab mob yog tib yam li erythromycin. Los ntawm kev koom ua ke nrog 50S subunit ntawm cov kab mob ribonucleoprotein lub cev, nws tiv thaiv kev txuas ntxiv ntawm peptide saw thiab cuam tshuam rau kev sib txuas ntawm cov kab mob protein kom ua tiav cov tshuaj tua kab mob. Cov tshuaj tua kab mob ntawm acetylspiramycin zoo ib yam li spiramycin, tab sis nws cov tshuaj tua kab mob muaj zog dua li ntawm spiramycin. Cov kab mob tua kab mob ntawm acetylspiramycin zoo ib yam li erythromycin, thiab nws cov tshuaj tua kab mob tsis zoo li erythromycin, thiab nws qhov ncauj bioavailability kuj tseem qis dua erythromycin. Txawm li cas los xij, ntau yam erythromycin-resistant Staphylococcus aureus nkag siab rau acetylspiramycin.

Ib qho ntxiv, acetylspiramycin muaj cov tshuaj tiv thaiv kab mob tom qab zoo dua li erythromycin. Cov kab mob tau pom ib nrab kev tiv thaiv kab mob rau acetylspiramycin thiab erythromycin. Acetylspiramycin muaj cov tshuaj tua kab mob muaj zog tiv thaiv Staphylococcus aureus, Streptococcus hemolyticus, Pneumococcus, Diphtheria, Bacillus anthracis thiab Clostridium; Tsis tas li ntawd, Acetylspiramycin muaj cov tshuaj tua kab mob muaj zog tiv thaiv Listeria thiab Catab, Lanhamella, Neisseria gonorrhoeae, Campylobacter fetus, Bacillus influenzae, Bacillus pertussis, Bacteroides, Perfringens, Propionibacterium acnes, Peptococcus thiab Peptostreptocompomas, kab.

Acetylspiramycin ntsiav tshuaj tuaj yeem tiv thaiv Streptococcus pneumoniae, Streptococcus pyogenes, Enterobacter faecalis, thiab lwm yam. Txawm li cas los xij, cov tsos mob no yuav tsis muaj kev cuam tshuam loj, tsuav yog koj tsum tsis noj tshuaj, cov tsos mob no yuav ploj mus. Ib qho ntxiv, kuv ceeb toom koj tias acetylspiramycin raug tso tawm los ntawm kab mob hauv lub siab, yog li nws tsis pom zoo rau cov neeg mob lub siab tsis zoo thiab lub raum tsis txaus los noj cov tshuaj.

B. Qhia

Haum rau tonsillitis, mob ntsws, mob ntsws, pharyngitis, otitis media, tawv nqaij thiab cov nqaij mos kis los ntawm cov kab mob rhiab xws li Staphylococcus, Streptococcus pyogenes, Streptococcus pneumoniae, Meningococcus, Neisseria gonorrhoeae, Diphtheria, Mycoplasma, Treponema pneumoniae, thiab lwm yam, ua npaws liab, mob hniav thiab qhov muag, thiab lwm yam.

Clinically, nws feem ntau yog siv rau kev kis mob los ntawm Staphylococcus aureus, Streptococcus, Pneumoniae Bacillus, Escherichia coli, Neisseria gonorrhoeae, xws li mob ntsws, mob ntsws, mob hauv lub ntsws, ua npaws liab, mob pob txha, mob pob txuv, mob qog noj ntshav, mob qog noj ntshav, mob hauv lub cev thiab lwm yam.

C. Kev phiv tshuaj

Cov phom sij tseem ceeb ntawm cov tshuaj acetylspiramycin yog cov tsos mob ntawm lub plab xws li mob plab, xeev siab, ntuav, tsis qab los noj mov, thiab kev tawm tsam tshuaj xws li pob khaus hauv zos lossis hauv lub cev thiab khaus, tab sis cov no feem ntau tsis xav tau kev kho tshwj xeeb thiab tuaj yeem rov zoo lawv tus kheej tom qab lub sijhawm.

Txawm li cas los xij, yog tias muaj kev tsis haum tshuaj loj tshwm sim, xws li ua pa luv, ntshav siab poob, thiab lwm yam, nws yog qhov mob sai mus ntsib kws kho mob tam sim. Ib qho ntxiv, cov neeg mob uas muaj lub siab thiab lub raum ua haujlwm tsis zoo yuav tsum tsis txhob siv cov tshuaj, vim tias cov tshuaj yuav ua rau lub siab thiab lub raum puas tsuaj.

Spiramycin phiv los

Spiramycin-phiv-tshwm sim
Spiramycin-phiv-tshwm sim

1. Teeb meem tsis haum

  • Cov kab mob plab zom mov yog me dua li erythromycin, feem ntau suav nrog xeev siab, ntuav, lub qhov ncauj qhuav thiab tsis qab los noj mov. Feem ntau nws tshwm sim thaum siv tshuaj ntau dhau, thiab cov tsos mob ploj tom qab siv tshuaj.
  • Qee zaum kev ua xua xws li ua pob tawv nqaij thiab ua pob ua xua tuaj yeem pom.
  • Qee zaum cov tsos mob ntawm kiv taub hau, mob taub hau, tsaug zog, thiab qaug zog tshwm sim.

2. Contraindications

Nws tau txwv rau cov neeg mob uas ua xua rau spiramycine, erythromycin thiab lwm yam cov macrolides. Spiramycin tuaj yeem nkag mus rau hauv lub tsho me nyuam, yog li nws yog qhov tsim nyog los ntsuas qhov zoo thiab qhov tsis zoo los txiav txim siab seb yuav siv nws rau poj niam cev xeeb tub.

Tsis muaj cov ntaub ntawv los qhia seb tshuaj spiramycin tau tawm hauv cov kua mis, tab sis ntau cov tshuaj macrolide tuaj yeem tso tawm hauv niam mis. Yog li cov poj niam uas pub niam mis yuav tsum siv cov khoom no nrog ceev faj, thiab ncua kev pub niam mis yog tias tsim nyog. Thiab qhov ua tau zoo thiab nyab xeeb ntawm cov neeg mob menyuam yaus hauv 6 lub hlis tsis tau txiav txim siab.

3. Tshuaj Kev Sib Thoob

  • Siv ua ke nrog metronidazole, nws muaj cov tshuaj tiv thaiv kab mob sib xyaw ua ke ntawm Bacteroides fragilis hauv kev sim hauv vitro.
  • Thaum siv nrog trimethoprim, nws muaj cov tshuaj tiv thaiv kab mob sib kis ntawm Haemophilus khaub thuas bacilli.
  • Kev siv ua ke nrog cytochrome P450 metabolites tuaj yeem ua rau kom muaj zog ntawm carbamazepine, terfenadine, cyclohexylbarbital thiab phenytoin hauv cov ntshav.
  • Thaum ua ke nrog levodopa/carbidopa/carbidopa, thaj chaw nyob hauv qab lub sijhawm nkhaus (AUC) ntawm levodopa tuaj yeem txo qis.

4. ceev faj

  • Qee zaum, tsis xis nyob hauv plab, xws li xeev siab, ntuav, tsis qab los noj mov, tso quav, thiab raws plab.
  • Kev tsis haum tshuaj yog tsawg.
  • Contraindicated rau cov poj niam cev xeeb tub lossis poj niam thaum lub sijhawm lactation.

xaus

Spiramycine belongs rau cov tshuaj tua kab mob macrolide. Spiramycine thiab erythromycin muaj cov tshuaj tiv thaiv kab mob tib yam thiab cov tshuaj tua kab mob zoo ib yam. Thiab spiramycin muaj lub zog tiv thaiv kab mob qis dua li erythromycin. Txawm li cas los xij, ntau cov kab mob tiv taus erythromycin tshuaj yog rhiab rau spiramycine, yog li spiramycine thiab erythromycin tuaj yeem sib ntxiv.

BALLYA muab a ballya-spiramycin-xeem qhia rau koj yog tias muaj tshuaj spiramycin seem hauv cov khoom noj thiab pub.

References

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