Pharmacological teebmeem ntawm Roxithromycinde

Pharmacological Action
Roxithromycin yog ib tiam tshiab ntawm cov tshuaj tua kab mob macrolide, ib qho khoom siv hluavtaws 14 tus tswv cuab macrolide. Nws cov txheej txheem ntawm kev ua haujlwm yog tib yam li erythromycin. Nws tsuas yog khi rau cov kab mob 50S ribosome subunit, thiab inhibits cov kab mob protein synthesis los ntawm kev thaiv peptide hloov mus thiab mRNA translocation, yog li ua si lub luag haujlwm ntawm cov kab mob. Nws cov yam ntxwv yog tias nws tuaj yeem nkag mus rau hauv macrophages, lub ntsws hlwb, alveoli, thiab cov qe ntshav dawb polymorphonuclear. Cov tshuaj tua kab mob ntawm roxithromycin zoo ib yam li erythromycin, thiab nws cov tshuaj tua kab mob hauv vitro zoo ib yam li erythromycin. Cov nyhuv antibacterial hauv vivo yog 1-4 lub sij hawm muaj zog dua li ntawm erythromycin. Roxithromycin muaj qhov cuam tshuam me ntsis ntawm cov kab mob Gram zoo dua li erythromycin, thiab muaj zog dua rau Legionella pneumophila dua li erythromycin. Cov tshuaj tua kab mob tiv thaiv kab mob Chlamydia pneumoniae, Mycoplasma pneumoniae, thiab Ureaplasma urealyticum zoo ib yam li lossis me ntsis muaj zog dua li ntawm erythromycin. Roxithromycin muaj zog tiv thaiv kab mob tiv thaiv Staphylococcus aureus (tshwj tsis yog MRSA), streptococci (xws li Hom A, B, C streptococci thiab Streptococcus pneumoniae, tab sis tsis suav rau Hom G thiab Enterococcus), Corynebacterium, Listeria, Catamora (Catarrhococcus, thiab lwm yam), Nws kuj muaj qee yam cuam tshuam rau lub qhov ncauj Bacteroides, Bacteroides niger, digestive coccus, Peptostreptococcus, Propionibacterium acnes thiab lwm yam kab mob anaerobic, nrog rau toxoplasma encephalitis, chlamydia, mycoplasma, ureaplasma urealyticum, umponemall, thiab lwm yam. Nws muaj cov nyhuv tsis muaj zog ntawm helicobacter, gonococcus, meningococcus, Bordetella pertussis, thiab lwm yam. Roxithromycin tuaj yeem cuam tshuam cov kab mob Gram zoo feem ntau, thiab nws cov tshuaj tua kab mob tiv thaiv cov kab mob xws li Staphylococcus aureus, Staphylococcus epidermidis, Pneumococcus, Streptococcus pyogenes, Infococcus pyogenes, Inf. , thiab Legionella hauv cov kab mob ua pa thiab daim tawv nqaij zoo ib yam li erythromycin. Nws muaj txiaj ntsig zoo tiv thaiv kab mob urinary thiab kev ua me nyuam los ntawm Chlamydia trachomatis thiab Ureaplasma urealyticum, thiab tawm tsam Treponema pallidum.

Pharmacokinetics
Roxithromycin yog acid resistant thiab tsis puas los ntawm gastric acid. Nws yog absorbed zoo los ntawm txoj hnyuv thiab muaj ntshav siab (cov ntshav siab tshaj plaws ntawm Roxithromycin yog qhov siab tshaj plaws ntawm tag nrho cov tshuaj macrolide). Tom qab ib koob tshuaj ntawm ib qhov ncauj ntawm 150mg, cov ntshav tshuaj concentration tau mus txog qhov siab tshaj plaws tom qab 2 teev, nrog rau qhov nruab nrab ntawm 6.6-7.9 μ g / mL. Tom qab nqus tau, nws qhov kev faib tawm hauv cov ntaub so ntswg thiab cov kua hauv lub cev yog siab dua li ntawm erythromycin. Cov tshuaj concentration hauv tonsils, sinuses, nruab nrab pob ntseg, ntsws, hnoos qeev, prostate, thiab lwm yam urogenital cov ntaub so ntswg tuaj yeem ncav cuag cov kev kho mob zoo. Tab sis cov ntsiab lus tsawg heev hauv cov kua mis. Lub cheeb tsam nyob rau hauv cov tshuaj concentration lub sij hawm nkhaus (AUC) thiab cov ntshav siab cov tshuaj concentration yog ncaj qha proportional rau cov koob tshuaj. Cov protein binding tus nqi ntawm roxithromycin yog 96 feem pua ​​​​ntawm cov ntshav concentration ntawm 2.5mg / L, thiab qhov kev tshem tawm ib nrab ntawm lub neej yog 8.4-15.5h, uas ntev dua li erythromycin. Cov tshuaj feem ntau raug tso tawm hauv lawv daim ntawv qub nrog quav, thiab qee qhov kuj raug tshem tawm raws li hypoglycemic metabolites. Lwm kwv yees li 7.4 feem pua ​​​​yog tawm los ntawm cov zis. Hauv cov neeg mob lub raum tsis txaus, ib nrab-lub neej ntev ntev thiab thaj chaw nyob rau hauv cov tshuaj concentration lub sij hawm nkhaus (AUC) nce. Hauv cov neeg mob uas mob ntshav siab mob siab, ib nrab lub neej tuaj yeem txuas ntxiv tau ob zaug. Qhov nqus tau ntawm roxithromycin tsis cuam tshuam los ntawm lub hnub nyoog, thiab feem ntau muaj qee qhov tsis zoo tshwm sim thiab tsis muaj tshuaj lom.

Cov tshuaj sib cuam tshuam
1. Kev sib xyaw ua ke ntawm roxithromycin thiab sulfamethoxazole (1:19) tuaj yeem ua rau cov nyhuv inhibitory ntawm Haemophilus influenzae los ntawm 2-4 zaug, thiab qhov tshwm sim ntawm cov tshuaj tiv thaiv tuaj yeem txo los ntawm 47.2 feem pua ​​​​rau 10.0 feem pua. .
2. Thaum ua ke nrog proton twj tso kua mis inhibitors (xws li lansoprazole thiab omeprazole), lub systemic bioavailability ntawm roxithromycin tsis hloov, tab sis nws muaj peev xwm nce lub zos concentration ntawm roxithromycin nyob rau hauv lub plab. Cov nyhuv no tuaj yeem pab ua ke ntawm roxithromycin thiab proton twj tso kua mis inhibitors kom tshem tawm Helicobacter pylori.
3. Thaum siv ua ke nrog warfarin, roxithromycin tuaj yeem cuam tshuam cov metabolism ntawm warfarin, nce cov ntshav concentration ntawm warfarin, thiab ua rau muaj kev pheej hmoo los ntshav.
4. Thaum ua ke nrog cov tshuaj benzodiazepine xws li prazoram, diazepam, midazolam, thiab triazolam, roxithromycin tuaj yeem cuam tshuam lub siab enzymes lub luag haujlwm rau cov metabolism hauv benzodiazepine, ua rau kom nce ntshav concentration ntawm cov tshuaj benzodiazepine los ntawm kev txo cov clearance npaum li cas, ncua ib nrab-lub neej, thiab nce. faib ntim.
5. Kev sib xyaw ua ke ntawm roxithromycin thiab pimozide tuaj yeem cuam tshuam cov metabolism ntawm pimozide, ua rau muaj kev nce hauv cov ntshav concentration ntawm cov tom kawg thiab ua rau qee yam mob plawv tsis zoo, xws li QT ncua sij hawm ntev, arrhythmia, thiab tuag sai sai.
6. Thaum siv nrog digoxin, roxithromycin tuaj yeem tshem tawm cov plab hnyuv microbiota uas tuaj yeem ua rau digoxin tsis ua haujlwm, ua rau digoxin degradation hauv lub cev thiab nce hauv digoxin ntshav concentration, ua rau muaj tshuaj lom.
7. Kev siv roxithromycin ua ke nrog clopidogrel tuaj yeem ua rau muaj qhov nce hauv cov ntshav concentration ntawm clopidogrel.
8. Kev sib xyaw ntawm roxithromycin thiab astemizole tuaj yeem ua rau muaj kev nce hauv cov ntshav concentration ntawm astemizole.
9. Roxithromycin yog siv ua ke nrog cyclosporine, thiab nws tuaj yeem txhawb kev nqus ntawm cyclosporine thiab cuam tshuam rau nws cov metabolism, ua rau muaj kev nce hauv cov ntshav concentration ntawm cyclosporine.
10. Kev sib xyaw ntawm roxithromycin thiab ergotamine derivatives tuaj yeem ua rau mob ergot lom (xws li peripheral vasospasm).
11. Kev noj roxithromycin ua ke nrog cov tshuaj tiv thaiv kev yug menyuam tsis muaj txiaj ntsig rau kev ua haujlwm ntawm cov tshuaj tiv thaiv qhov ncauj.
12. Roxithromycin tsis tshua muaj txiaj ntsig rau carbamazepine thiab ranitidine.
13. Cov tshuaj pharmacokinetic ntawm roxithromycin ntawm theophylline zoo ib yam li erythromycin, tab sis nws kuj yog me me. Nws tuaj yeem ua kom ntev lub neej ib nrab ntawm theophylline los ntawm 8 feem pua ​​thiab tshem tawm los ntawm 16 feem pua. Thaum siv ua ke nrog theophylline, qhov koob tshuaj ntawm theophylline tsis tas yuav txo qis, tab sis nws cov tshuaj concentration yuav tsum tau saib xyuas.
14. Tsis zoo li erythromycin, roxithromycin tsis cuam tshuam rau cov tshuaj pharmacokinetic ntawm carbamazepine thiab tuaj yeem siv ib txhij.