Metronidazole chewable ntsiav tshuajsawv cev rau tus neeg mob- tus phooj ywg tsim cov tshuaj tua kab mob nitroimidazole, sib txuas ua haujlwm tiv thaiv kab mob anaerobic thiab protozoa nrog kev txhim kho palatability thiab yooj yim ntawm kev tswj hwm. Qhov kev tshuaj xyuas no tshawb txog lawv cov kev siv tshuaj kho mob, qhov zoo ntawm cov tshuaj pharmacokinetic, kev txiav txim siab rau menyuam yaus thiab cov neeg laus, kev tsim kho tshiab, thiab kev nyab xeeb profiles. Los ntawm kev daws cov teeb meem kev ua raws li kev coj ua thiab nthuav dav kev siv tau yooj yim, cov ntsiav tshuaj no ua lub luag haujlwm tseem ceeb hauv kev kho tshuaj tua kab mob niaj hnub no.
|
|
|
Mechanism of Action: Targeting Anaerobes thiab Protozoa
Metronidazole txoj kev ua tau zoo yog hauv paus hauv nws cov kev xaiv toxicity-nws tsuas yog ua rau cov kab mob anaerobic thiab qee cov protozoa, ua rau tib neeg lub hlwb thiab cov kab mob aerobic tsis ua mob. Nov yog cov kauj ruam -los ntawm - cov txheej txheem:
Cov ntaub ntawv loj nyiaj txiag:
Uptake los ntawm cov kab mob: Cov kab mob anaerobic (piv txwv li, Bacteroides fragilis, Clostridioides difficile) thiab protozoa (xws li Trichomonas vaginalis, Giardia lamblia) cia siab rau qis -redox- muaj peev xwm thauj cov tshuab hluav taws xob kom muaj sia nyob hauv cov pa oxygen{{6.}} Cov tshuab no nquag tso cov metrolyl mus rau hauv lub cell, tsom cov tshuaj 50-100x siab dua hauv tib neeg cov ntshav. Cov kab mob aerobic tsis muaj cov thauj khoom no, piav qhia txog metronidazole qhov nqaim spectrum
Khw Muag Khoom Loj:
Kev ua kom dhau los ntawm Nitro Group Txo: Hauv cov kab mob, nitroreductase enzymes (xws li, ferredoxin reductase hauv cov kab mob, NADPH-dependent reductases hauv protozoa) txo cov metrolyl's nitro pawg (-NO₂) rau cov kab mob sib kis- feem ntau tshwj xeeb tshaj yog cov nitro radical. Cov kauj ruam no yog cov pa oxygen-sensitive: oxygen inhibits nitroreductase, yog li metrolyl ua haujlwm zoo tshaj plaws hauv cov ntaub so ntswg hypoxic (xws li, plab abscesses, plab lumen, lossis necrotic qhov txhab).
Muaj Cov Ntaub Ntawv Loj:
DNA puas thiab tuag Cell: Cov nitro radical anion khi covalently rau cov kab mob DNA, ua rau strand so, hla -txuas, thiab kev hloov pauv hauv paus. Tsis zoo li tib neeg lub hlwb (uas muaj cov txheej txheem kho DNA zoo li nucleotide kho), anaerobes thiab protozoa tsis muaj kev kho kom zoo. Qhov no irreversible DNA puas cuam tshuam replication thiab transcription, ua rau bactericidal los yog protozoicidal teebmeem (tsis yog tsuas yog kev loj hlob inhibition).
Cov txheej txheem no yog concentration-dependent- qib tshuaj ntau dua hauv cov kab mob ua kom tua neeg, ua kom qhov tseeb ntau npaum li cas tseem ceeb rau kev kho mob.
Pharmacokinetic Properties
Metabolism
Feem ntau ntawm metrolyl (kwv yees li 60% mus rau 80%) yog metabolized hauv daim siab los ntawm cytochrome P450 (CYP) enzyme system, feem ntau los ntawm CYP3A4 thiab CYP2B6. Lub ntsiab metabolite yog 2-hydroxymethylmetronidazole, uas khaws cia li ntawm 30% mus rau 50% ntawm niam txiv cov tshuaj tiv thaiv kab mob. Lwm cov metabolites me muaj xws li metrolyl N-oxide thiab glucuronide conjugates, uas tsis ua haujlwm.
Lub siab ua haujlwm ua lub luag haujlwm tseem ceeb hauv metrolyl metabolism. Hauv cov neeg mob uas muaj qhov tsis zoo ntawm lub siab mus rau qhov hnyav, qhov kev tshem tawm ntawm metrolyl raug txo, ua rau kom cov ntshav plasma ntau ntxiv thiab ntev ib nrab - lub neej. Qhov no yuav tsum tau hloov kho ntau npaum li cas kom tsis txhob muaj tshuaj tsub zuj zuj thiab kev pheej hmoo ntawm kev tsis zoo, tshwj xeeb yog neurotoxicity. Hauv qhov sib piv, cov neeg mob uas mob siab mob siab tsis zoo feem ntau tsis xav tau kev hloov pauv ntau npaum li cas, vim tias cov metabolism tseem tsis zoo.
Metrolyl thiab nws cov metabolites feem ntau yog tawm hauv cov zis. Kwv yees li ntawm 20% mus rau 30% ntawm cov tshuaj tau muab tso tawm tsis hloov pauv hauv cov zis, thaum qhov seem yog tawm los ua cov metabolites. Ib feem me me (kwv yees li 10%) yog tawm hauv cov quav. Kev tshem tawm ib nrab ntawm - lub neej ntawm metrolyl yog kwv yees li 8 teev nyob rau hauv cov neeg laus noj qab haus huv, uas zoo sib xws nyob rau hauv ntau qhov ncauj formulations.
Hauv cov neeg mob lub raum tsis ua haujlwm, kev tso tawm ntawm metrolyl thiab nws cov metabolites raug txo. Txawm li cas los xij, vim tias cov tshuaj niam txiv feem ntau metabolized hauv daim siab, kev hloov tshuaj tsuas yog tsim nyog rau cov neeg mob uas muaj lub raum tsis zoo (creatinine tshem tawm).<30 mL/min) or those undergoing hemodialysis. Hemodialysis removes approximately 50% of the drug from the plasma, so a supplementary dose is often recommended after dialysis to maintain therapeutic concentrations. Peritoneal dialysis has a minimal effect on metrolyl clearance and does not require dosage adjustments.
Cov kab mob Protozoal
Trichomoniasis
Trichomoniasis yog ib hom kab mob sib kis los ntawm kev sib deev (STI) tshwm sim los ntawm Trichomonas vaginalis. Nws yog cov tshuaj ntawm kev xaiv rau kev kho mob trichomoniasis, nrog rau ib koob tshuaj ntawm qhov ncauj (2 g) yog tus txheej txheem kev kho mob rau cov txiv neej thiab poj niam. Lub chewable formulation yog ib qho zoo tshaj lwm txoj rau cov pa ntsiav tshuaj rau qhov kev qhia no, vim nws yooj yim rau kev tswj hwm thiab tuaj yeem noj nrog lossis tsis muaj zaub mov. Nws yog ib qho tseem ceeb uas yuav tsum tau kho ob tus neeg koom tes ib txhij los tiv thaiv kev rov ua dua tshiab, thiab cov khoom noj uas ua rau lub palatability tuaj yeem txhim kho kev ua raws li cov ntsiab lus no.
Giardiasis
Giardiasis yog kab mob plab hnyuv los ntawm Giardia lamblia, uas kis tau los ntawm cov zaub mov tsis huv lossis dej. Nws yog thawj -tus neeg sawv cev rau kev kho mob ntawm giardiasis, nrog rau cov koob tshuaj ntawm 250 mg peb zaug ib hnub twg rau 5 mus rau 7 hnub (los yog 500 mg ob zaug ib hnub rau 7 hnub) rau cov neeg laus. Hauv cov menyuam yaus, qhov koob tshuaj yog raws li qhov hnyav (15 mg / kg / hnub muab faib ua peb koob rau 5 txog 7 hnub). Cov tshuaj chewable yog tshwj xeeb tshaj yog muaj txiaj ntsig rau cov neeg mob menyuam yaus, uas feem ntau muaj teeb meem nqos cov ntsiav tshuaj. Kev sim tshuaj ntsuam xyuas tau pom tias cov ntsiav tshuaj metrolyl chewable tau txais kev kho mob ntawm 80% mus rau 90% hauv giardiasis, uas yog piv rau lwm cov tshuaj.
Amebiasis
Amebiasis yog ib qho kab mob uas tshwm sim los ntawm Entamoeba histolytica, uas tuaj yeem tshwm sim raws li plab hnyuv amebiasis (diarrhea, dysentery) lossis extraintestinal amebiasis (siab abscesses, ntsws abscesses). Nws yog siv los kho cov kab mob sib kis ntawm amebiasis (extraintestinal thiab mob plab hnyuv amebiasis), vim nws muaj txiaj ntsig zoo tiv thaiv theem trophozoite ntawm cov kab mob cab. Tus qauv koob tshuaj rau plab hnyuv amebiasis yog 750 mg peb zaug ib hnub twg rau 5 mus rau 10 hnub, thaum lub plab hnyuv amebiasis (xws li daim siab abscess), qhov koob tshuaj yog 500 txog 750 mg peb zaug ib hnub rau 5 mus rau 10 hnub. Tom qab kev kho mob nrog metrolyl, luminal amebicide (xws li, paromomycin) feem ntau yog siv los tshem tawm cov cyst theem thiab tiv thaiv kev rov qab los. Cov tshuaj chewable formulation yog pab tau rau cov neeg mob uas mob plab hnyuv amebiasis uas yuav nyuaj rau nqos vim xeev siab lossis mob plab.
Cov tshuaj sib cuam tshuam
Disulfiram-Zoo li kev tshwm sim
Lub neej-Kev hem thawj ntawm plab hnyuv thiab mob plawv toxicity
Qhov zoo tshaj plaws -cov ntaub ntawv sau tseg thiab txaus ntshai cuam tshuam nrog metrolyl yog nws cov tshuaj tiv thaiv nrog cawv (ethanol) thiab cawv- muaj cov khoom lag luam, uas ua rau muaj kev cuam tshuam ntawm disulfiram (ib hom tshuaj siv los kho kev haus cawv). Qhov kev cuam tshuam no tshwm sim vim metrolyl inhibition ntawm aldehyde dehydrogenase (ALDH), ib qho enzyme tseem ceeb rau ethanol metabolism.
Mechanism
Thaum noj ethanol, nws yog thawj zaug metabolized rau acetaldehyde (ib qho tshuaj lom nruab nrab) los ntawm cawv dehydrogenase. Feem ntau, acetaldehyde tau hloov pauv mus rau qhov tsis muaj teeb meem acetic acid los ntawm ALDH. Metrolyl khi irreversibly rau ALDH, thaiv cov kauj ruam no thiab ua rau acetaldehyde mus rau hauv cov hlab ntsha.
Clinical Manifestations
Cov tsos mob feem ntau tshwm sim li ntawm 15-30 feeb ntawm kev haus cawv thiab tuaj yeem kav ntev li ob peb teev. Lawv suav nrog:
Kev xeev siab, ntuav, thiab mob plab heev
Tshem tawm ntawm lub ntsej muag, caj dab, thiab hauv siab
tachycardia (lub plawv dhia ceev) thiab palpitations
Hypotension (tsis tshua muaj ntshav siab).
Mob taub hau, kiv taub hau, thiab tsis meej pem
Hauv cov xwm txheej hnyav: arrhythmias, myocardial infarction, lossis qaug dab peg
Ntawm -Risk Products
Dej cawv (npias, cawv, cawv, cocktails).
Cawv- muaj cov tshuaj (xws li, qee cov tshuaj hnoos hnoos, tshuaj ntxuav qhov ncauj, tshuaj pleev gels, thiab cov tshuaj tinctures xws li tincture ntawm opium)
Cov khoom noj uas muaj cawv ntau (piv txwv li, cov tais diav flambeed, qee cov kua ntses).
Hand sanitizers with >60% ethanol (yog tias noj lossis nqus los ntawm daim tawv nqaij tawg).
Kev taw qhia
Tsis txhob haus cawv tag nrho -muaj cov khoom siv thaum kho metronidazole thiab tsawg kawg 72 teev tom qab koob tshuaj zaum kawg (kom tso cai rau ALDH kev ua kom rov zoo).
Qhia cov neeg mob txog cov dej cawv zais (piv txwv li, cov tshuaj ntxuav qhov ncauj uas sau tias "cawv-dawb" tsis muaj kev nyab xeeb, tab sis cov "ethanol" lossis "ethyl cawv" tsis yog).
Kev sib cuam tshuam nrog Warfarin thiab Lwm Qhov Ncauj Anticoagulants: Muaj Kev Txhaum Los Ntshav
Metronidazole txhim kho cov nyhuv anticoagulant ntawm warfarin (vitamin K antagonist) thiab lwm yam tshuaj (xws li, phenprocoumon, acenocoumarol), ua rau muaj kev pheej hmoo ntawm txoj sia - hem los ntshav. Qhov kev sib cuam tshuam no yog ib qho ntawm feem ntau tshaj tawm hauv kev kho mob.
Mechanism:
Pharmacokinetic Interaction: Metronidazole inhibits cytochrome P450 (CYP) enzymes (feem ntau CYP2C9) hauv daim siab, uas metabolize warfarin (tshwj xeeb tshaj yog muaj zog S-warfarin enantiomer). Txo warfarin metabolism ua rau cov ntshav plasma ntau dua thiab ntev ib nrab -lub neej.
Pharmacodynamic Interaction: Metronidazole kuj tseem tuaj yeem txo cov synthesis ntawm cov vitamin K- nyob ntawm cov ntshav txhaws (II, VII, IX, X) hauv daim siab, ntxiv dag zog rau coagulation.
Clinical Manifestations:
Ntev prothrombin lub sij hawm (PT) thiab thoob ntiaj teb normalized piv (INR).
Ntshav los ntshav (xws li, qhov ntswg los ntshav, cov pos hniav los ntshav, bruising, ntshav hauv zis / quav)
Los ntshav hnyav (piv txwv li, gastrointestinal hemorrhage, los ntshav intracranial)
Kev taw qhia:
Yog tias kev tswj hwm tsis tuaj yeem zam tau, saib xyuas INR tsis pub dhau 3-5 hnub txij li pib metronidazole thiab kho cov tshuaj warfarin raws li qhov xav tau (feem ntau txo 20–50%).
Txuas ntxiv saib xyuas INR rau 1-2 lub lis piam tom qab txiav tawm metronidazole, vim tias kev sib cuam tshuam yuav tshwm sim kom txog thaum metronidazole raug tshem tawm tag nrho.
Rau cov neeg mob ntawm qhov ncauj ncaj qha anticoagulants (DOACs, piv txwv li, apixaban, rivaroxaban), kev sib cuam tshuam tsawg dua tab sis tseem ua tau -nug kws muag tshuaj lossis kws tshuaj hematologist rau kev taw qhia.
Kev Nyab Xeeb Profile: Cov teebmeem tsis zoo thiab contraindications
Thaum metronidazole feem ntau ua tau zoo- zam, nws tuaj yeem ua rau muaj kev phom sij (AEs) xws li mob me mus rau qhov hnyav. Kev nkag siab txog cov kev pheej hmoo no pab txhim kho kev nyab xeeb ntawm tus neeg mob.
Tej yam tshwm sim tsis zoo
Feem ntau AEs mob me thiab daws nrog kev kho tiav:
Gastrointestinal (GI): xeev siab (feem ntau), ntuav, raws plab, mob plab, metallic saj hauv qhov ncauj. Lub chewable formulation's flavouring txo cov xim hlau saj piv rau cov qauv ntsiav tshuaj
Neurological: mob taub hau, kiv taub hau, qaug zog. Cov no feem ntau yog me me thiab tsis tas yuav hloov kho koob.
Dermatological: pob khaus, pruritus (khaus). Tsis tshua muaj, urticaria (ua pob khaus) yuav tshwm sim ..
Cov teebmeem loj heev
Cov no xav tau kev kho mob tam sim ntawd thiab kev kho mob:
Neurotoxicity: Peripheral neuropathy (numbness/tingling in hands/feet), seizures, encephalopathy (confusion, hallucinations). Risk is higher with high doses (>2 g/day) or prolonged use (>14 hnub), tshwj xeeb tshaj yog rau cov neeg mob siab / raum tsis zoo
Hematological: Leukopenia (cov qe ntshav dawb tsawg), thrombocytopenia (tsawg platelets). Saib xyuas cov ntshav suav (CBC) hauv cov neeg mob ntev -lub sij hawm kho
Kev Ua Phem Tsis Txaus Siab: anaphylaxis (ua tsis taus pa nyuaj, o ntawm lub ntsej muag / caj pas), Stevens-Johnson syndrome (mob tawv nqaij hlwv). Cov no yog txoj sia - hem thiab xav tau kev saib xyuas xwm txheej ceev
Hepatotoxicity: Siab siab enzymes (ALT, AST), jaundice (daj ntawm daim tawv nqaij / qhov muag). Tsis tshua muaj tab sis muaj ntau dua nyob rau hauv cov neeg mob ua ntej - kab mob siab uas twb muaj lawm.
Cov lus nug nquag
Koj puas tuaj yeem zom cov ntsiav tshuaj metronidazole?
+
-
nqos tag nrho.Tsis txhob txiav, tawg lossis zom. Noj tag nrho cov tshuaj hauv koj daim ntawv xaj kom tshem koj tus kab mob, txawm tias koj zoo dua tom qab thawj ob peb koob tshuaj. Koj cov koob tshuaj yuav tsum tau hloov ntau zaus kom pom qhov ua haujlwm zoo tshaj rau koj.
Kuv puas tuaj yeem noj metronidazole nrog sertraline?
+
-
Metronidazole (Flagyl) tuaj yeem cuam tshuam nrog cawv thiab lwm yam tshuaj. Piv txwv li,metronidazole tuaj yeem cuam tshuam nrog sertraline (Zoloft)thiab warfarin (Jantoven). Metronidazole yog siv los kho ntau yam kab mob thiab kab mob parasitic rau cov neeg laus.
Dab tsi yuav tsum zam thaum noj metronidazole?
+
-
Tsis txhob haus cawv thaum koj noj cov tshuaj metronidazole lossis kua lossis siv cov tshuaj suppositories. Txuas ntxiv kom tsis txhob haus cawv rau 2 hnub tom qab koj ua tiav koj txoj kev kho mob. Qhov no muab sijhawm rau cov tshuaj tawm hauv koj lub cev. Qhov no yog qhov tseem ceeb vim tias metronidazole tuaj yeem hnov mob nrog cawv ua rau muaj kev phiv ntau.
Puas muaj zog metronidazole?
+
-
Metronidazole yog cais raws li ib tugmuaj zog tshuaj tua kab mobvim nws qhov dav -spectrum kev ua haujlwm tawm tsam ntau yam kab mob anaerobic, suav nrog cov cuam tshuam nrog BV thiab trichomoniasis. Koj yuav tsum tsis txhob haus cawv thaum noj metronidazole thiab tsawg kawg 48 teev tom qab ua tiav cov kev kho mob.
Puas yog metronidazole pheej hmoo?
+
-
Cov kev mob tshwm sim hnyav tsis tshua muaj thiab tshwm sim tsawg dua 1 ntawm 1,000 tus neeg. Tsis txhob noj metronidazole thiab hu rau tus kws kho mob lossis hu rau 111 tam sim no yog tias: cov tawv nqaij dawb ntawm koj ob lub qhov muag tig daj, lossis koj cov tawv nqaij hloov daj (qhov no yuav tsis pom tseeb ntawm cov tawv nqaij xim av lossis xim dub) - cov no tuaj yeem yog cov tsos mob ntawm daim siab lossis lub gallbladder.
Cim npe nrov: metronidazole chewable ntsiav tshuaj, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom