Entecavir Ntseyog cov tshuaj tua kab mob tsuas yog siv los kho tus kab mob siab ntev B (HBV). Nws yog Guanine nucleoside analogue nrog cov tshuaj lom neeg lub npe 2 {}} amino-4-hydrotylcentyl] -1,9-purin-6-ib monohydrate. Cov qauv molecular yog c ₁ hu ₁ n ₅ O α ₅ ₂ ₂ ₂ ₂ ₂ ₂ ₂ ₂ ₂ ₂, nrog lub cev hnyav molecular ntawm 295.3. Nws yog ib qho nyias nyias zaj duab xis coated ntsiav tshuaj thiab tshwm sim dawb tom qab tshem tawm cov txheej. Haum rau cov kab mob nquag ua dua tshiab thiab txhawb nqa nce siab ntawm Serum Alanine aminotRanserase (alt). Mob siab Athology qhia txog cov mob qis (suav nrog them nyiaj thiab decompensated hlab ntsha cov neeg mob). Lub Inhibithat tas li (KI) ntawm entecavir triphosphate ntawm HBV DNA cov nyhuv ntawm cellular yog 0.004 μ mitues tsis muaj zog (ki qhov tseem ceeb ntawm 18 mus rau 160 μ m).
Cov ntaub ntawv ntxiv ntawm kev sib txuas lus:
| Khoom npe | Entecavir Ntse | Entecavir tsiav tshuaj | Entecavir Txhaj |
| Khoom Yam | Phau ntawv | Tsoom qab | kua |
| Khoom Siv Purity | Ntau dua los yog sib npaug rau 99% | Ntau dua los yog sib npaug rau 99% | Ntau dua los yog sib npaug rau 99% |
| Cov Khoom Qhia Khoom Khoom | 0.1mg / 1mg | 0.5mg | 0.1mg / 2.5mg |
| Khoom daim ntawv | Noj ib leeg | Noj ib leeg | Organic Synthesis |
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Entecavir COA
Entecavir Ntse, Suav lub npe yog entecavir, uas yog ib cov tshuaj tiv thaiv tiv thaiv dav rau kev kho kab mob siab ntev b (CHB). Txij li thaum nws pib, entecavir tau dhau los ua tus thawj tawm- Line cov tshuaj rau kev ua haujlwm hauv ntiaj teb B Ntiaj Teb vim nws cov kev tiv thaiv kev nyab xeeb, kev nyab xeeb zoo, thiab tus nqi tsawg. Cov hauv qab no yog cov lus qhia ntxaws ntxaws ntawm nws lub hom phiaj:
Tub Ntxhais Tub Ntxhais: Kev Kho Mob Ntawm Kab Mob Siab Qaum B (HBV)
Entecavir NtseYog thawj {-} kab tsuag antiviral kho rau tus kab mob siab B (HBV), nrog kev ua haujlwm kom muaj nuj nqi, thiab kev ncua kab mob kev ua haujlwm. Qhia tau xws li:
Haum rau cov neeg mob uas muaj tus kab mob rov ua haujlwm (qib siab
Xws li cov neeg mob uas muaj tus kab mob siab (mob siab ua haujlwm yog qhov tsis zoo) thiab lub siab ua haujlwm yog qhov tsis zoo (ascites, hepatic encephany thiab lwm yam teeb meem).
Ntev tus kab mob siab B hauv menyuam yaus
Suitable for children and adolescents under the age of 2 to 18 with compensatory liver disease caused by chronic HBV infection, and those who have received initial treatment with nucleosides (ie have not received antiviral therapy with other nucleoside analogues).
Ib qho ntawm cov xwm txheej hauv qab no yuav tsum tau ntsib:
Tus kab mob replication yog nquag (HBV DNA qib siab yog siab) thiab theem ntshav siab txuas ntxiv (feem ntau dhau ntawm cov kev txwv siab tshaj plaws ntawm 2 zaug).
Mob siab Athology qhia qhov me me mus rau qhov roj loj thiab / lossis fibrosis.
Mechanism ntawm Kev Ua: Tseem ceeb nyob rau hauv inhibiting hbv replication
Entecavir yog guanine nucleoside analogue uas tau tawm tsam kev tawm tsam kev tawm tsam los ntawm cov txheej txheem hauv qab no:
Phosphorylation ua kom zoo & muaj kev xaiv tau yooj yim ntawm HBV
Entecavir yog phosphorylated rau hauv triphosphate (etv - tp) hauv lub hlwb, nrog ib nrab} Lub neej ntawm kwv yees li 15 teev, thiab tuaj yeem tswj hwm tau ntev.
Kev sib tw inhibition ntawm HBV polymerase
ETOK - Tp Sib xeem nrog HBV polymerase, deoxyguanphat (DGTP), kom inhibit peb txoj haujlwm ntawm viral polymerase:
Ua kom muaj HBV polymerase: txwv tiv thaiv qhov pib viral RNA synthesis.
Tsim cov kev hloov pauv ntawm cov kev sib txuas tsis zoo ntawm cov lus tsis zoo ntawm MRA: thaiv cov ntawv sau rov qab ntawm cov neeg tsis zoo ntawm DNA.
Synthesis ntawm HBV DNA zoo strand: inhibits qhov txuas ntxiv ntawm tus kab mob sib txuas tau zoo, yog li thaiv cov kev sib tw sib deev.
Lub inhibition tas li (KI) ntawm ETV - tp ntawm HBV DNA Polymerase yog 0.0012 μ m, qhia tau muaj cov nyhuv muaj zog.
Cov teeb meem Inisignes nyhuv ntawm cellular dna polymerase (, Δ) thiab mitochondrial tsis muaj zog (Ki tus nqi ntawm 18-160 μ m), txo qis rau cov hauv hlwb.
Kho kom zoo: zoo inhibits cov kab mob thiab txhim kho daim siab muaj nuj nqi
Ntau lub chaw kuaj mob tau lees paub tias qhov ua tau zoo ntawm entecavir hauv kev kho kab mob siab B:
Cov Neeg Laus Pib Cov Neeg Siv Kho Mob
Kev Ua Haujlwm Uas Virvolog: Tom qab 48 lub limtiam ntawm kev kho, kwv yees li 67% rau 76% ntawm cov neeg mob 'Qib HBV Lna txo qis cov qib (<300 copies/mL), significantly better than lamivudine (approximately 36%).
Cov lus teb biochemical: kwv yees li 68% rau 72% ntawm cov neeg mob alt cov qib rov qab mus rau ib txwm, uas yog siab tshaj li ntawm Lamivudine (kwv yees li 55%).
Kev Txhim Kho Kev Koom Tes: Tom qab 48 lub lim tiam ntawm kev kho, kwv yees li 70% rau 72% ntawm cov neeg mob pom kev txo qis hauv daim siab o thiab mob fibrosis.
Cov neeg mob uas tau ua txhaum Lamivudine Kev Kho Mob
Rau cov neeg mob uas lamivudine tiv taus lossis kev kho tsis yog ua haujlwm tsis muaj ob npaug rau 1 mg / hnub, thiab tom qab 48 lub lis piam ntawm kev kho:
Txog 22% rau 39% ntawm cov neeg mob muaj qib HBV DNA uas tsis pom.
Txog 38% rau 40% ntawm cov neeg mob muaj lawv cov qib Al Al Al Al tau rov qab los ua ib txwm muaj.
Cov ntaub ntawv kho ntev
Tom qab 5 xyoo ntawm kev kho kev ua yeeb yam, qhov tshwm sim ntawm cov neeg mob tshiab tsuas yog 1.2%, thaum lub sij hawm kho tshuaj tiv thaiv cov neeg mob Lamivudine yog 51%.
Kev kho lub sijhawm ntev tuaj yeem txo qis kev pheej hmoo ntawm daim siab ntawm daim siab ua kom mob cancer thiab mob qog noj ntshav.
Cov neeg mob pediaric
Qhov kev ua tau zoo ntawm cov neeg mob pediatric muaj hnub nyoog 2 txog 18 xyoo zoo ib yam li cov neeg laus. Tom qab 48 lub lim tiam ntawm kev kho:
Kwv yees li ntawm 46% ntawm cov neeg mob pediatric nrog lub phaus ntau dua los yog sib npaug rau 0.5 mg ntsiav tshuaj muaj lawv cov qib HBV tau txo qis cov qib.
Cov menyuam yaus muaj qhov hnyav<32.6 kg have a virological response rate comparable to adults after using entecavir oral solution.
Kev Siv thiab Dosage Hloov Kho rau Cov Neeg Tshwj Xeeb
Kev siv thiab muab tshuaj ntau ntawm cov entecavir hauv cov neeg tshwj xeeb tshwj xeeb yuav tsum tau hloov kho raws li cov xwm txheej tshwj xeeb:
Cov neeg mob uas muaj tus tsis muaj npe tsis txaus
Entecavir feem ntau yog ua rau lub raum, thiab qhov kev tshem tawm tus nqi ntawm cov neeg mob lub raum tsis txaus. Qhov ntau npaum li cas yuav tsum tau hloov kho:
Creatinine tshem tawm tus nqi ntau dua los yog sib npaug rau 50 ml / min: Tsis muaj kev hloov kho qhov yuav tsum tau hloov kho (0.5 mg / hnub).
Creatinine tshem tawm tus nqi ntawm 30-50 ml / min: 0.5 mg txhua 48 teev.
Creatinine tshem tawm tus nqi 10-30 ml / min: 0.5 mg txhua 72 teev.
Creatinine Kev Tshem Tawm<10 mL/min or hemodialysis/CAPD: once every 5-7 days, 0.5 mg each time.
Hemodialysis cov neeg mob yuav tsum noj nws tom qab lim ntshav.
Cov neeg mob uas muaj lub siab tsis sib xws
Cov neeg mob uas muaj lub siab tsis sib xws (suav nrog txoj kev noj tshuaj lom zem) tsis tas yuav kho lawv cov nqi kho mob, tab sis kaw ntawm daim siab ua haujlwm, bilumines ua haujlwm, bilumin, albumin, thiab lwm yam) yog qhov tsim nyog.
Cov poj niam cev xeeb tub
Cov kev tshawb fawb ntawm kev cuam tshuam ntawm utecavir rau cov poj niam cev xeeb tub tsis yog txaus, thiab nws tsuas yog siv thaum nws muaj txhij txhua, nrog kev txiav txim siab ntawm nws cov txiaj ntsig thiab kev xav.
Cov poj niam cev xeeb tub siv cov kws muaj kev phom sij yuav ua rau muaj kev pheej hmoo ntawm tus neeg mob HIV / HID / HBV yuav tsum tau txais kev kho mob HIV
Lactating poj niam
Entecavir NtseTej zaum yuav tau txais kev zais ntawm cov niam mis, thiab lactating poj niam yuav tsum ncua pub niam mis thiab hloov mus rau kev pub mis cuav.
Cov neeg mob pediaric
Kev nyab xeeb thiab ua tau zoo ntawm cov menyuam yaus hnub nyoog qis dua 2 xyoos tsis tau tsim thiab tsis pom zoo rau kev siv.
Cov menyuam hnub nyoog 2 txog 18 yuav tsum kho lawv cov koob tshuaj raws li lawv qhov hnyav:
Qhov hnyav hnyav dua los yog sib npaug rau 32.6 kg: 0.5 mg / hnub (ntsiav tshuaj lossis cov lus daws teeb meem).
Nyhav li ntawm 10 kg rau<32.6 kg: Use entecavir oral solution, with dosage calculated based on body weight.
Cov neeg mob laus
Lub raum muaj nuj nqi ntawm cov neeg mob laus tshaj 65 xyoos yuav poob qis, thiab cov tshuaj yuav tsum muab kho kom haum raws li kev kho lub txim uas muaj catural.
Noj tshuaj laj kev ceev faj thiab soj ntsuam
Txhawm rau kom muaj kev nyab xeeb thiab siv tau zoo ntawm entecavir, cov kev ceev faj hauv qab no yuav tsum tau ua:
Sijhawm ntawm cov tshuaj: ensecavir yuav tsum tau noj ntawm ib lub plab khoob (tsawg kawg 2 teev ua ntej lossis tom qab noj mov) kom tsis txhob noj cov zaub mov muaj kev cuam tshuam.
Lub sijhawm kho mob: Mob kab mob siab B yuav tsum muaj kev kho mob ntev li cas (xws li HBAG xwm txheej, thiab lwm yam) thiab yog txiav txim siab los ntawm tus kws kho mob qhov kev tshuaj xyuas.
HBAG Cov neeg mob zoo: Kev kho mob yuav tsum txuas ntxiv 12 lub hlis tom qab HBV DNA Undetectable thiab HBV DNOCONVERSION (ploj ntawm HBEAG thiab ARTISH HBE).
HBAG Cov Neeg Mob Tsis Zoo: Kev kho mob yuav tsum tau txuas ntxiv kom txog thaum hbsag seroconversion lossis poob ntawm kev ua tau zoo (xws li kis tus kab mob).
Kev saib xyuas tom qab kev sib txuas ntawm cov tshuaj noj: tsis muaj tshuaj yuav ua rau muaj kab mob siab, tshwj xeeb tshaj yog cov neeg mob decompensated rau kab mob siab. Kaw saib xyuas ntawm daim siab muaj nuj nqi (alt, bilirubin, thiab lwm yam) thiab qib HBV DNA yuav tsum tau ua yam tsawg 4 lub hlis tom qab tsis siv tshuaj.
Kev sib cuam tshuam yeeb tshuaj: entecavir tsis yog substrate, inhibitor, lossis inducer ntawm CYP450 system thiab muaj tsawg dua kev cuam tshuam nrog lwm cov tshuaj.
Txawm li cas los xij, thaum siv hauv kev sib xyaw ua ke nrog cov tshuaj uas tau sib tw rau kev tso pa tawm los ntawm cov pa luam yeeb los ntawm cov tshuaj lom zem (xws li immunosuppressants), nws tuaj yeem ua rau cov ntshav tshuaj ntxiv thiab yuav tsum tau saib xyuas kom ze.
Cov neeg mob tsis kam lees: Cov lus siv HBV tsis yeem, xws li RTS202, RTM250 thiab lwm yam tshuaj kho mob).
Taboos thiab ceev faj
Cov xwm txheej hauv qab no txwv lossis siv entecavir nrog ceev faj:
Qho piav
Nws yog contraindicated rau cov tib neeg uas ua xua rau entecavir lossis cov khoom xyaw rau hauv cov qauv.
Cov neeg mob HIV / HBV Co Co tsis tau txais kev kho mob HAART yog contraindicated (uas yuav ua rau HIV tsis tawm tsam).
Siv nrog ceev faj
Cov neeg mob uas muaj cov nyiaj tsis txaus yuav tsum tau kho lawv cov nqi.
Cov neeg mob nrog decompensated daim siab ua haujlwm yuav tsum tau saib xyuas kom zoo.
Cev xeeb tub thiab cov poj niam coj ua lactating yuav tsum hnyav qhov zoo thiab kev pom zoo.
Cov menyuam cov neeg mob xav tau nruj me ntsis tswj cov khoom pom thiab muab tshuaj.
Cim npe nrov: Entecavir ntsiav tshuaj, cov chaw muag khoom, chaw tsim khoom, Hoobkas, lag luam wholesale, yuav, nqe, loj, loj, loj, loj, rau muag