Introduction
ZALLOPON KHUG yog qhia rau lub luv luv -}}}} lub sij hawm kho mob ntawm insomnia hauv cov neeg mob muaj kev nyuaj siab pw tsaug zog. Cov chaw kuaj mob tshawb nrhiav qhia tau tias Zerveplon tuaj yeem ua rau lub sijhawm pw tsaug zog, tab sis nws tsis tau pom tias nws tuaj yeem ua kom muaj sijhawm pw tsaug zog thiab txo tus naj npawb ntawm etakenings.
Cov ntsiab lus
Lub npe siv tshuaj 【
Cov npe Generic: Zertplon ntsiav tshuaj
Lag Luam Lub Npe: Huining
Lus Askiv Lub Npe: ZALLPON KHO
【Cov Khoom xyaw】Zalplon.
Chemical Name: N - [3 - (3 - cyanopyrazolo[1,5 - a]pyrimidin - 7 - yl)phenyl] - N - ethylacetamide
Molecular cov mis: C17h15n5o
Molecular hnyav: 305.33
Profarser 【НCov khoom no yog zaj duab xis -} coated ntsiav tshuaj. Tom qab tshem cov txheej, nws zoo li cov neeg dawb lossis tawm - dawb.
【Kev qhia】
Nws yog siv rau luv luv - lub sij hawm kho mob ntawm insomnia nrog kev nyuaj hauv kev ntog pw tsaug zog. Cov kev tshawb fawb soj ntsuam qhia tau hais tias nws tuaj yeem ua rau lub sijhawm luv luv pw tsaug zog, tab sis nws tsis tau pom tias nce kev pw tsaug zog ntev thiab txo tus naj npawb ntawm etakenings.
【Cov Lus Qhia】5mg
【Kev Pab Siv thiab Kev Siv Ntau】Rau cov neeg laus, txoj hauv kev siv lub qhov ncauj yog 5mg {{mg ({2}} cov ntsiav tshuaj), coj ua ntej mus pw lossis thaum muaj teeb meem poob tsaug zog. Rau cov neeg mob uas muaj lub cev hnyav dua, cov tshuaj pom zoo muab 5mg (1 ntsiav tshuaj (1 ntsiav tshuaj) ib zaug. Rau cov neeg laus neeg cov neeg mob, thiab cov neeg mob ntshav qab zib nrog cov siab tsis txaus, cov ntsiav tshuaj pom zoo yog 5mg (1 ntsiav tshuaj) ib hmos ib hmos. Lub sijhawm muaj tsawg rau 7 -} 10 hnub. Yog tias tus mob tsis tau txhim kho tom qab 7-10 hnub ntawm noj cov tshuaj, tus kws kho mob yuav tsum ntsuas dua qhov ua rau tus neeg mob insomnia.
Cov nyom tshwm sim】Tom qab noj zaleplon, cov tshuaj tiv thaiv me me yuav tshwm sim: qhov ncauj tsaug zog, tsis muaj kev npau taws, tsis muaj kev npau taws, tsis meej, thiab lwm yam kev pom, thiab tsis pom kev zoo nkauj. Lwm cov kev sib raug zoo suav nrog:
① Tom qab noj ZALPLON (10 lossis 20mg), luv - lub sijhawm nco ploj yuav tshwm sim txog 1 teev tom qab. Cov nyhuv muaj zog dua ntawm 20mg koob tshuaj, tab sis cov nyhuv no ploj tom qab 2 teev.
② Tom qab noj ZALPLON (10 lossis 20mg), qhov kev cia siab sedative thiab kev tsis sib haum xeeb tshwm sim txog 1 teev tom qab, tab sis cov nyhuv no ploj tom qab 2 teev.
③ rov ua haujlwm insomnia yog koob -. Cov chaw sim kho mob qhia tias tsis muaj lossis tsawg tsawg tsawg dua rau thawj hmo tom qab cheem cov tshuaj hauv 5mg pawg, tab sis nws ploj mus rau lub hnub nyoog thib ob.
④ Hloov pauv leukhytosis yog qee zaus.
⑤ Hloov pauv ntawm cov chaw hla kev tau pom.
【Contraindications 【
1. Confaindicated nyob rau hauv cov neeg mob ua xua rau cov khoom no.
2. Conraindicated nyob rau hauv cov neeg mob uas mob siab loj thiab lub raum tsis txaus.
3. Conraindicated nyob rau hauv cov neeg mob nrog pw tsaug zog apnea syndrome.
4. Conraindicated nyob rau hauv cov neeg mob nrog myasthenia gravis.
5. Conraindicated nyob rau hauv cov neeg mob uas muaj mob dyspnea loj lossis mob hauv siab.
【Cov kev ceev faj】Txhawm rau kom muaj kev nyab xeeb thiab siv tau zoo ntawm Zervlon, cov kev ceev faj hauv qab no yuav tsum tau ceeb toom:
1. Cov khoom no yog qhov thib ob -} Chav Kawm Txuj Ci Hauv Tebchaws. Nws yuav tsum tau siv nruj me ntsis raws li lub teb chaws cov kev cai ntawm cov tshuaj psychotropic thiab raws li kev taw qhia tus kws kho mob.
2. Tsis txhob tshaj lub sijhawm siv tau sau los ntawm tus kws kho mob. Ntev - kev siv sijhawm yuav ua rau vam. Cov neeg mob nrog keeb kwm kev quav yeeb tshuaj yuav tsum siv nws nrog kev ceev faj.
3. Yog tias tus cwj pwm thiab kev tsis ncaj ncees yog pom tom qab noj zeroplon, hu rau tus kws kho mob.
4 Yog tias koj haus cawv, koj yuav tsum qhia tus kws kho mob. Cawv yog txwv tsis pub siv lub sijhawm Zervor lossis lwm cov tshuaj tsaug zog.
5. Tsis txhob siv cov khoom no tshwj tsis yog ntau tshaj 4 teev ntawm kev pw tsaug zog tuaj yeem ua kom tiav.
6. Tsis txhob nce ntau npaum li cas ntawm ZervePon yam tsis muaj tus kws kho mob cov kev taw qhia.
7. Thaum noj Zervon lossis lwm lub sijhawm pw tsaug zog thawj zaug, paub tias cov tshuaj no tseem muaj qee qhov kev cuam tshuam rau hnub tom ntej. Ceevfaj thaum cov haujlwm uas xav tau lub siab kom pom tseeb, xws li tsav tsheb lossis ua haujlwm tshuab.
8. Nyuaj rau kev ntog pw tsaug zog yuav tshwm sim rau thawj lossis thib ob hmo tom qab cheem cov tshuaj.
9. Yog tias koj xeeb tub, txog plab, lossis kev pub niam mis, qhia tus kws kho mob.
10. Tsis txhob faib ZALPON nrog lwm tus. Khaws cov tshuaj kom txhob ncav cuag cov menyuam yaus.
11. Yog koj muaj kev nyuaj siab, qhia kws kho mob. Tus kws kho mob yuav tsum tau muab cov tshuaj tsawg kawg rau cov neeg mob uas muaj kev nyuaj siab los tiv thaiv overdose.
12 ZerverPon yuav siv sij hawm sai. Nws yuav tsum tau noj ua ntej mus pw lossis thaum muaj teeb meem ntog pw tsaug zog hauv txaj.
13. Txhawm rau ua kom Zervon ua haujlwm zoo dua, tsis txhob nqa cov khoom no tam sim ntawd tom qab high- rog noj mov.
14
15. Thaum siv hauv kev sib xyaw ua ke nrog cov yeeb tshuaj ua yeeb yam ntawm lub hlwb, tom qab- kev cuam tshuam yuav raug aggragistic vim muaj kev tsaug zog thaum sawv ntxov. Cov tshuaj no suav nrog: tshuaj los kho cov kab mob hlwb (xws li siv tshuaj tiv thaiv kab mob (xws li tshuaj edi {}} ayramines).
【Siv rau cev xeeb tub thiab lactating poj niam】Kev nyab xeeb ntawm kev noj cov khoom no thaum cev xeeb tub tsis tau lees paub los ntawm cov ntaub ntawv, thiab cov khoom no yog metabolized rau hauv niam mis. Yog li, cov khoom no yog contraindicated nyob rau hauv cov niam lactating niam, thiab poj niam uas tab tom yuav yog lossis twb cev xeeb tub lawm.
【Siv rau cov menyuam】Kev nyab xeeb ntawm cov khoom no hauv cov menyuam yaus tsis tau lees paub los ntawm cov ntaub ntawv, yog li cov khoom no contraindicated nyob rau hauv cov menyuam yaus (qis dua 18 xyoo).
【Siv rau cov neeg mob laus】Cov khoom no tuaj yeem siv rau cov neeg laus, suav nrog cov neeg tshaj li 75 xyoo. Piv nrog cov zaub mov noj qab haus huv, cov khoom lag luam hauv cov neeg mob thiab cov poj niam laus, suav nrog ntau dua li hnub nyoog 75 xyoo, suav qhov sib txawv. Txij li cov neeg laus neeg mob muaj kev nkag siab ntau dua ntawm cov tshuaj tsaug zog, cov tshuaj pom zoo tau 5mg.
【Tshuaj sib cuam tshuam】
Nrog Central Ntshav Tshuaj
Ethang: Cov khoom no tuaj yeem txhim kho kev puas tsuaj ntawm ethanol ntawm lub hauv paus ntawm lub hlwb, tab sis tsis cuam tshuam rau cov chaw muag tshuaj ntawm ethanol.
IMIPRAMINE: Tom qab kev sib xyaw ua ke ntawm cov khoom no thiab imipramine, cov qib ntawm kev ua kom raug txo qis, thiab lub cev muaj zog {}} lub hlwb ua yog tsis txaus ntseeg. Qhov kev sib txuam yog cov tshuaj ntsiav tshuaj, tsis muaj kev hloov vaj kws hloov chaw.
PAROXETINE: Tsis muaj kev sib cuam tshuam thaum cov khoom no ua ke nrog paroxetine.
ThiFoidazine: Tom qab cov khoom lag luam no thiab Thioridazine, cov qib ntawm kev ua kom muaj kev lom zem, thiab lub cev muaj zog} kev mob hlwb yog qhov tsis txaus ntseeg. Qhov kev sib txuam yog cov tshuaj ntsiav tshuaj, tsis muaj kev hloov vaj kws hloov chaw.
Nrog enzyme - incovents / inhibing tshuaj: thaum cmax, CMAX thiab AUC ntawm cov khoom no raug txo los ntawm 4 zaug.
Nrog DiphenhydruajNine: Tsis muaj kev sib cuam tshuam ntawm kev sib txuas, tab sis vim tias ob qho tib si muaj cov teebmeem kev sedative, cov xim tshwj xeeb yuav tsum tau them thaum siv ua ke.
Nrog cov tshuaj uas cuam tshuam rau lub raum tshem tawm: Tsis muaj ib qho kev hloov pauv ntawm cov khw muag tshuaj uas hloov pauv thaum ua ke nrog ibuprofen.
【Tshuaj ntau tshaj li】Muaj cov kev tshawb fawb me me ntawm ZervalPon ntau dhau. Nyob rau hauv pre {- kev tshawb nrhiav hauv kev soj ntsuam, nws tau sau tseg tias cov tshuaj ntau dhau ntawm cov yeeb tshuaj muaj cov leeg ntshav nruab nrab inhibool teebmeem. Cov tsos mob muaj xws li: kev tsaug zog, nkees, thiab tsis meej pem. Cov tsos mob muaj xws li: Ataxia, hypomyotonia, thiab qee zaum fa thiab kev tuag.
Pom zoo kev kho mob: kho raws li cov ntsiab cai tswj hwm kev haus tshuaj ntau dhau los, thiab muaj kev txhawb nqa thiab cov tsos mob. Kev tshawb nrhiav tsiaj qhia tias Flumazenil tuaj yeem txwv tsis meej Zerverplon, tab sis nws tsis tau siv tus kws kho mob.
【Pharmacology thiab Toxicology】
Pharmacological txiav txim siab
Raws li cov qauv hypnotic, cov qauv tshuaj ntawm Zallon yog txawv ntawm benzodiazepines, barbiturates, thiab lwm yam paub. Nws yuav siv nws cov tshuaj pharapacological los ntawm kev ua yeeb yam ntawm aminobutyric acid {}}}- bz) receptor complex. Tsis - Cov chaw kuaj mob tuaj yeem xaiv khi rau qhov ω1 receptor ntawm lub paj nruag Gaba receptor complex. Cov kev sim ua kev sim ntawm Zervlon kom lim Gaba recepted Gaba receptors (() {}}}} {{}}
Kev Tshawb Fawb Txog Kev Sib Tw
Muaj me nyuam yaus
Nyob rau hauv kev ua me nyuam toxicity ntsuam xyuas, nas tau muab tshuaj rau zalplon ntawm 100mg / Kg / hnub (hloov pauv qhov siab tshaj plaws) ua ntej mating, uas tuaj yeem ua rau kev tuag thiab txo fertility. Tom ntej kev tshawb fawb pom tias Zervon feem ntau yog ua rau muaj kev puas tsuaj rau lub fertility ntawm poj niam tsiaj. Thaum lub sij hawm Teratogenic rhiab lub sij hawm, cev xeeb tub tau hais txog cov dej hiav txwv ntawm lub cev (hloov dua siab tshiab rau tib neeg lub cev), thiab tsis muaj qhov tseeb ntawm Teratogenic cov teebmeem tau pom. Txawm li cas los xij, tom qab cov nas tsuag tau raug tswj hwm ZALLONS ntawm 100MG / KG / KG / HNUB, cov fetuses pom kev loj hlob ntawm kev txawv txav ua ntej thiab tom qab yug. Cov tshuaj no kuj tseem tuaj yeem ua rau niam muaj kuab lom, ua rau muaj cov kuab lom thiab lub cev yuag qeeb nce thaum lub sijhawm siv zog. Qhov koob tshuaj uas tsis muaj kev cuam tshuam rau kev txhim kho ntawm cov nas yog 10mg / 1 hnub (hloov dua siab tshiab raws li lub cev thaj chaw ntawm lub cev, kwv yees li ntawm 5 tus koob tshuaj tiv thaiv tib neeg). Ntawm tag nrho cov koob tshuaj tiv thaiv, kev txhim kho ntawm cov embryos thiab fetuses hauv luav tsis muaj kev cuam tshuam. Nyob rau hauv kev sim perinatal, poj niam nas tau muab z faleplon ntawm 7mg / kg / kab / hnub thaum lub sijhawm cev xeeb tub thiab lub sijhawm lactation. Lub pastebirth thiab tshaj tawm - Natal tuag ntawm cov tsiaj uas muaj kev loj hlob ntawm cov tsiaj uas tau nce, thiab kev loj hlob thiab kev loj hlob ntawm lub cev qeeb. Tsis muaj niam muaj kuab lom tau pom ntawm cov koob tshuaj no. Qhov koob tshuaj tsis muaj kev cuam tshuam rau kev txhim kho tshiab yog 1mg / kg / hnub (hloov raws li thaj chaw thaj tsam lub cev, kwv yees li ntawm 0.5 zaug rau tib neeg cov koob tshuaj). Qhov kev tshawb fawb no qhia tau tias kev nthuav tawm cov tsiaj rau cov tshuaj hauv kev ua haujlwm hauv kev ua haujlwm hauv lawv cov kev tsis sib haum xeeb thiab kev loj hlob.
Kev tiv thaiv caj ces
Nyob rau hauv cov vitro Suav hamster ovary cell chromosome kev ntsuas, seb puas muaj cov yam ntxwv metabolic, uas tuaj yeem ua rau cov qauv metabolic, uas tuaj yeem ua rau cov kab ke metabolic, uas tuaj yeem ua rau cov kab ke metabolic, uas tuaj yeem ua rau cov kab ke mevoog Nyob rau hauv cov hauv Vitro Lymphocyte kuaj, tsuas yog thaum nws tau txais kev ntsuas siab tshaj plaws thiab nyob rau hauv cov kev ua kom muaj peev xwm ntawm cov metabolic activator tuaj yeem ua rau cov lej chromosomal. Zalllon pom tsis muaj mutagenicity nyob rau hauv cov kab mob vitro Amester Cution Microocyte unscheduled DNA synthesis xeem.
Carcinogenicity
Lub neej taug kev carcinogenicity kev ntsuam xyuas tau nqa tawm ntawm nas thiab nas. Cov nas tau muab tshuaj txuas ntxiv zalplon ntawm 25, 50, 100, thiab 200mg / kg / {{{} lub sij hawm qhov kev pom zoo tshaj plaws rau tib neeg cov koob tshuaj). Qhov tshwm sim ntawm Hepatocellular Adenoma hauv cov poj niam nas nyob rau hauv lub siab- ib pawg tau nce. Hamsters tau raug tswj hwm mus tsis tu ncua zaleplon ntawm 1, 10, 20mg / kg / {{14} {{{14} {{14} 0.5 - 10
【Pharmacokinetics】Raws li cov ntawv ceeb toom rau cov ntaub ntawv txawv teb chaws, cov neeg muag tshuaj tau kawm ntau dua 500 tus poj niam noj qab haus huv (suav nrog cov ntxhais hluas thiab cov neeg mob uas muaj kab mob lossis mob raum lossis mob raum. Hauv kev noj qab nyob zoo, cov tshuaj npauj npaim ntawm ib qho - Dose Administration ntawm 60mg thiab ib zaug {hnub tau kawm txog 10 hnub tau kawm. Zervlon tau nrawm nrawm, ncav cuag lub ncov siab ntev hauv li 1 teev, thiab cov kev tshem tawm ib nrab {} lub neej (T1 / 2) yog li 1 teev. Ib zaug -}} Kev tswjhwm txhua hnub ntawm Zaleplon tsis ua rau cov tshuaj lom zem, thiab hauv kev kho tshuaj, nws cov tshuaj papapaconetics yog koob tshuaj-}.
1. Kev nqus
Tom qab kev tswj hwm ntawm Zervon, nws yog sai thiab txo kev nqus, ncav cuag cov ntshav ntshav siab kawg li ntawm 1 teev. Nws lub npe tsis muaj peev xwm yog kwv yees li 30%. Muaj ib tug tseem ceeb ua ntej -} dhau lawm.
2. Kev xa tawm
ZALLLON yog Lipophilic compound. Tom qab cov thawj coj ntawm kev tswj hwm, lub ntim ntawm kev faib tawm yog kwv yees li 1l / kg. Tus nyob hauv Vitro Plasma cov protein khi yog kwv yees li 60% ± 15%, thiab tsis muaj kev cuam tshuam txog kev hloov pauv ntawm cov protein khi tus nqi. Qhov piv tau ntawm Zaleplon hauv cov ntshav thiab ntshav yog kwv yees li 1, qhia tias Zervon tau faib rau cov ntshav yam tsis muaj kev faib tawm hauv cov ntshav liab.
3. Cov metabolism
Tom qab cov thawj coj ntawm qhov ncauj, zalplon yog dav metabolized. Hauv zis, tsawg dua 1% ntawm koob tshuaj yog cov tshuaj qub. ZALLLON feem ntau hloov dua siab tshiab rau 5 -}}}}}}} desethyl zervlon los ntawm aldehyde oxidase. ZALLLON tsis tshua muaj metabolized rau descalplon los ntawm cyp3A4 thiab tau hloov siab heev rau 5-Oxy-desthyl zaleplon los ntawm aldehyde oxidase. Cov metabolites no tau hloov mus rau hauv cov plaubhau ua tebchaw thiab ua cov zis. Txhua Zervlon Metabolites tsis muaj kev ua tshuaj.
4. Excretion
Tom qab qhov ncauj lossis kev tswj hwm lub cev, Zervon tau tshem tawm sai sai. Qhov nruab nrab T1 / 2 yog li 1 teev. Lub Qhov ncauj Plasma tshem tawm tus nqi ntawm ZALPLON yog kwv yees li 3l / h / kg, thiab qhov kev txiav txim siab ntshav ntshav ntshav ntshav yog kwv yees li 1l / kg. If the hepatic blood flow is normal and renal clearance is ignored, the estimated hepatic extraction rate of zaleplon is 0.7, indicating that the first-pass effect of zaleplon is very significant.
Tom qab noj radiolabeled ZALPON, 70% tuaj yeem rov qab tau hauv cov zis tsis pub dhau 48 teev (71% tuaj yeem rov qab tau tsis pub dhau 6 hnub), suav nrog txhua Zervepon Metabolites thiab lawv cov kua pleev. Tsis tas li ntawd, 17% tuaj yeem rov qab tau nyob rau hauv cov quav, feem ntau 5 {{{{}} oxy-zervon.
5. Cov zaub mov ntawm cov zaub mov
Hauv cov neeg laus noj qab nyob zoo, siab- rog} rog thiab cov zaub mov tsis muaj kwv yees li 2 teev, thiab cov CMAX yog txo los ntawm kwv yees li 35%. AUC thiab tshem tawm ib nrab ntawm- lub neej ntawm zaleplon tsis cuam tshuam ntau. Qhov no qhia tau tias noj zallon tam sim ntawd tom qab lub siab - kua roj thiab indigestible noj yuav muaj kev cuam tshuam lub sijhawm nyob ntawd.
Cov txiaj ntsig ntawm peb lub Tshuaj Ntsuam Xyuas Tshuaj ntawm Zaleplon hauv cov neeg laus qhia tias lub tsev muag tshuaj txawv ntawm cov tub ntxhais hluas.
Gender: Tsis muaj qhov sib txawv ntawm cov chaw muag tshuaj ntawm tus txiv neej zealplon ntawm tus txiv neej thiab poj niam.
Kev Sib Tw: Siv cov haiv neeg dawb los ua tus sawv cev ntawm cov neeg Esxias, kev kawm txog ZALPLON tau ua. Rau pab pawg no, CMAX thiab AUC tau nce ntxiv los ntawm 37% thiab 64% feem. Qhov no yuav cuam tshuam nrog qhov sib txawv ntawm lub cev hnyav, lossis nws yuav yog vim qhov sib txawv ntawm cov haujlwm enzyme los ntawm kev noj haus, ib puag ncig, lossis lwm yam.
Mob siab puas: Zallplon yog thawj metabolized los ntawm daim siab thiab tom qab ntawd undergoes system metabolism. Nws tus nqi tshem tawm qhov ncauj yog txo los ntawm 70% thiab 87% hauv cov neeg mob them thiab cov neeg mob decompensated. Piv nrog cov neeg noj qab nyob zoo, qhov no ua rau muaj kev txo qis hauv nruab nrab cmax thiab AU. Yog li ntawd, cov neeg mob uas muaj mob me me mus rau lub siab mob lub siab yuav tsum txo cov tshuaj ntawm zerve ntawm zereplon tsim nyog. Cov neeg mob uas muaj lub siab puas yog qhov tsis pom zoo kom coj Zervor.
Lub raum puas tsuaj: txij li tsawg dua 1% ntawm cov tshuaj qub ntawm ZerveSplon tau raug hloov pauv ntawm nws cov tshuaj papinokinetics hauv cov neeg mob raum tsis txaus. Yog li ntawd, tsis tas yuav kho qhov ntau npaum li cas rau cov neeg mob uas muaj mob me me rau kev puas tsuaj ntawm lub raum puas tsuaj, tab sis xav tau kev tshawb fawb ntxiv rau cov neeg mob uas muaj kev puas tsuaj loj.
【Cia】Muab cia rau hauv qhov chaw tsaus thiab foob.
【Ntim】Ntim hauv tshuaj ntsuab PVC tawv nplooj ntawv thiab ppt aluminium ntawv ci cov kab hlwv los khi pob luam ntawv pob ntawv {}}} ntsiav tshuaj ib phaj, 1 phaj rau ib lub thawv.
【Tas sij hawm】24 lub hlis
【Qauv】Ch.p {. 2020}, Tshooj II.
【Kev Pom Zoo】Gualoao Zhunzi H20052234
【Nta】
1. Kev pib sai, txo qis pw tsaug zog lub sijhawm
2. Tshem tawm sai sai, tiag tsis muaj Hangover ua tau zoo
3. Yuav luag tsis cuam tshuam txog kev txawj ntse thiab psycomotrotor muaj nuj nqi
4. Tsis muaj kev rho tawm cov tsos mob, tsawg dua rexound rawomnia tom qab ua haujlwm ntawm kev noj tshuaj
Cim npe nrov: Zalplon ntsiav tshuaj, Tuam Tshoj Zertplon ntsiav tshuaj tsim khoom, cov chaw muag khoom, Hoobkas

