Monoket

Monoket

Lub npe: isosorbide mononitrate hmoov
Daim ntawv noj tshuaj: ntsiav tshuaj
Hoob tshuaj: Cov neeg sawv cev Antianginal

Tshuaj kho los ntawm Varixcare.cz. Hloov kho zaum kawg ntawm Lub Ib Hlis 22, 2021.



Ntawm Nplooj Ntawv no
Nthuav dav

Monoket lub npe khoom lag luam tau raug txiav tawm hauv Asmeskas Yog tias cov khoom lag luam dav dav ntawm cov khoom no tau pom zoo los ntawm FDA, tej zaum yuav muaj generic equivalents muaj .



Monoket Nqe lus piav qhia

Monoket® ib, cov organic nitrate, yog vasodilator uas cuam tshuam rau ob leeg hlab ntsha thiab leeg. Cov qauv ua piv txwv yog C.6H9TSIS YOG6thiab lub cev hnyav yog 191.14. Cov tshuaj lom npe rau Monoket® ibyog 1,4: 3,6-Dianhydro-D-glucitol 5-nitrate thiab cov tshuaj muaj cov qauv hauv qab no:

Monoket® ibmuaj nyob rau hauv 10 mg thiab 20 mg ntsiav tshuaj. Txhua lub ntsiav tshuaj tseem muaj cov khoom xyaw tsis ua haujlwm: lactose, talc, colloidal silicon dioxide, hmoov txhuv nplej siab, microcrystalline cellulose thiab txhuas stearate.



Monoket - Clinical Pharmacology

Isosorbide mononitrate yog lub zog loj metabolite ntawm isosorbide dinitrate (ISDN), thiab feem ntau ntawm cov chaw kho mob ntawm dinitrate yog qhov ua rau mononitrate.

Lub hauv paus tseem ceeb ntawm kev siv tshuaj tua kab mob ntawm isosorbide mononitrate yog so ntawm cov leeg leeg leeg thiab ua rau muaj kev nthuav dav ntawm cov hlab ntsha sab hauv thiab cov leeg, tshwj xeeb tshaj yog tom kawg. Kev tso pa tawm ntawm cov leeg ntshav txhawb nqa cov hlab ntshav sab hauv thiab txo qis ntshav rov qab mus rau lub plawv, yog li txo qis sab laug ventricular kawg-diastolic siab thiab pulmonary capillary wedge siab (preload). Arteriolar so txo ​​cov kab mob vascular tiv thaiv, systolic arterial siab, thiab txhais tau tias ntshav siab (tom qab thauj khoom). Dilatation ntawm cov hlab ntsha hauv lub plawv kuj tshwm sim. Qhov tseem ceeb txheeb ze ntawm kev txo qis ua ntej, kev txo qis tom qab thiab kev txhim kho kab mob plawv tseem tsis tau txiav txim siab.

Pharmacodynamics

Cov txheej txheem kev noj tshuaj rau feem ntau siv cov tshuaj niaj hnub tau tsim los muab cov ntshav ntshav ntau ntxiv tsis tu ncua ntau dua li qhov ua tau zoo. Lub tswv yim no tsis tsim nyog rau cov organic nitrates. Ntau qhov kev soj ntsuam kuaj mob tau zoo tau siv kev sim ua haujlwm txhawm rau tshuaj xyuas qhov ua tau zoo ntawm cov tshuaj nitrates tsis tu ncua. Hauv feem ntau ntawm cov kev sim no, cov neeg sawv cev ua haujlwm tsis txawv ntawm cov placebo tom qab 24 teev (lossis tsawg dua) ntawm kev kho tas mus li. Kev sim ua kom kov yeej kev siab ntev los ntawm kev nce tshuaj ntxiv, txawm tias ua rau cov tshuaj nyob deb dhau ntawm cov uas tau siv tas li, tau ua tsis tiav tas li. Tsuas yog tom qab nitrates tsis tuaj ntawm lub cev tau ob peb teev lawm lawv cov kev ua haujlwm antianginal tau rov qab los.



Lub sijhawm tsis muaj tshuaj txaus txaus kom zam kev ua siab ntev rau isosorbide mononitrate tsis tau txhais meej. Hauv qhov kev tswj hwm nkaus xwb ntawm ob zaug ib hnub isosorbide mononitrate uas tau qhia kom zam kev txhim kho kev ua siab ntev, ob koob tshuaj Monoket® ibntsiav tshuaj tau muab 7 teev sib nrug, yog li muaj qhov sib txawv ntawm 17 teev ntawm qhov koob thib ob ntawm txhua hnub thiab thawj koob ntawm hnub tom ntej. Siv tus lej ntawm ib nrab-lub neej ntev ntawm isosorbide mononitrate qhov txiaj ntsig no zoo ib yam nrog cov uas tau txais rau lwm cov organic nitrates.

Lub asymmetric ob zaug-ib hnub regimen ntawm Monoket® ibcov ntsiav tshuaj tau ua tiav zam qhov rov cuam tshuam loj/tshem tawm cov teebmeem. Qhov xwm txheej thiab qhov loj ntawm cov xwm txheej zoo li no tau tshwm sim, hauv kev tshawb fawb ntawm lwm cov nitrates, kom muaj kev ntseeg siab raws li lub sijhawm siv tshuaj nitrate.

Pharmacokinetics

Monoket® ibyog nrawm thiab nqus tau tag nrho los ntawm txoj hnyuv. Hauv tib neeg, Monoket® ibtsis yog thawj zaug dhau cov metabolism hauv lub siab. Qhov tsis txaus ntseeg txaus ntawm isosorbide mononitrate los ntawm Monoket® ibntsiav tshuaj yog ze li 100%. Peak ntshav ntau ntau feem ntau tshwm sim li ntawm 30-60 feeb. Monoket® ibnthuav tawm cov koob tshuaj sib npaug tshaj qhov pom zoo koob tshuaj. Cov zaub mov tsis cuam tshuam loj rau kev nqus lossis nqus tau ntawm Monoket® ib. Kev tswj hwm Metoprolol tsis hloov pauv kev muag tshuaj ntawm Monoket® ib. Qhov ntim ntawm kev faib tawm yog kwv yees li 0.6 L/kg. Plasma protein khi ntawm Monoket® ibtau pom tias tsawg dua 5%.

Thaum radiolabelled isosorbide mononitrate tau muab rau tib neeg txhawm rau txhawm rau txheeb xyuas cov txheej txheem kev zom zaub mov, kwv yees li ib nrab ntawm cov koob tshuaj tau pom tawm thiab tso tawm hauv lub cev raws li isosorbide thiab sorbitol. Ib feem peb ntawm cov koob tshuaj tau suav rau raws li kev sib txuas ntawm niam txiv cov tshuaj hauv cov zis. Tsis muaj ib qho ntawm cov metabolites no yog vasoactive. Tsuas yog 2% ntawm cov koob tshuaj tau tso tawm raws li cov tshuaj tsis hloov pauv.

Kev tshem tawm ib nrab-lub neej ntawm Monoket® ibyog li 5 teev. Tus nqi ntawm kev tshem tawm yog tib yam hauv cov tub ntxhais hluas noj qab haus huv, hauv cov neeg mob uas muaj ntau qib ntawm lub raum, lub siab lossis lub plawv tsis ua haujlwm thiab hauv cov neeg laus. Thaum radiolabelled isosorbide mononitrate tau muab rau tib neeg, 93% ntawm cov koob tshuaj tau tso tawm hauv 48 teev mus rau hauv cov zis. Kev tshem tawm ntawm lub raum tau ua tiav zoo tom qab 5 hnub; kev tso quav tawm tsuas yog 1% ntawm qhov koob tshuaj.

Monoket® ibtsis muaj kev paub txog kev ua haujlwm ntawm lub raum thiab lub siab. Hauv cov neeg mob uas muaj qib sib txawv ntawm lub raum tsis ua haujlwm, kev hloov tshuaj ntau npaum li tsis tsim nyog. Hauv cov neeg mob uas mob siab rau daim siab, cov tshuaj pharmacokinetic tom qab txhaj ib zaug ntawm Monoket® ibtau zoo ib yam li cov txiaj ntsig pom hauv cov neeg pab dawb noj qab haus huv.

Isosorbide mononitrate raug tshem tawm ntawm cov ntshav thaum lub sij hawm hemodialysis; txawm li cas los xij, ib koob tshuaj ntxiv los txhawm rau them rau cov tshuaj poob yog tsis tsim nyog. Hauv cov neeg mob uas niaj hnub siv tshuaj tua kab mob hauv lub cev tas mus li, cov ntshav tau zoo ib yam li cov neeg mob uas tsis tau lim ntshav.

Clinical Trials

Kev mob hnyav thiab mob ntev ua rau lub cev tiv thaiv kab mob ntawm Monoket® ibtau lees paub hauv kev sim tshuaj. Kev siv tshuaj kho mob ntawm Monoket® ibtau kawm hauv 21 cov neeg mob angina pectoris ruaj khov. Tom qab txhaj tshuaj ib zaug ntawm Monoket® ib, 20 mg, kev tawm dag zog lub cev tau nce 42.7% tom qab ib teev, 29.6% tom qab 6 teev, thiab 25% tom qab yim teev thaum piv rau cov placebo. Tswj kev sim ntawm ib koob tshuaj Monoket® ibcov ntsiav tshuaj tau qhia tias cov tshuaj antianginal muaj nyob txog 1 teev tom qab txhaj tshuaj, nrog cov txiaj ntsig siab tshaj pom los ntawm 1-4 teev tom qab txhaj tshuaj.

Hauv ib qho kev sim tshuaj ntau ntau hauv cov tshuaj placebo, Monoket® ibtau pom tias muaj kev nyab xeeb thiab muaj txiaj ntsig zoo thaum lub sijhawm mob hnyav thiab mob ntev (3 lub lis piam) kho mob angina pectoris. Ob puas kaum plaub (214) cov neeg mob tau cuv npe hauv qhov kev sim siab; 54 tus neeg mob tau raug xaiv kom tau txais cov placebo thiab 106 tus neeg mob tau raug xaiv kom tau txais 10 lossis 20 mg ntawm Monoket® ibob zaug ib hnub xya teev sib nrug. Qhov loj tshaj plaws ntawm Monoket® ib, piv rau cov placebo, yog nyob rau ib hnub - ib koob. Txawm hais tias 14 teev tom qab txhaj thawj zaug ntawm hnub 14, nce kev tawm dag zog vim yog Monoket® ibyog cov ntaub ntawv tseem ceeb, qhov nce yog kwv yees li ib nrab ntawm qhov pom 2 teev tom qab txhaj thawj zaug ntawm ib hnub. Hnub 21, ob teev tom qab thawj koob tshuaj Monoket® ibyog 60 txog 70% ntawm qhov pom nyob rau hnub ib.

dawb oval ntsiav tshuaj 377

Kev Qhia thiab Kev Siv rau Monoket

Monoket® ibtau qhia rau kev tiv thaiv thiab kev kho mob ntawm angina pectoris vim yog kab mob hauv lub plawv. Qhov pib ntawm kev ua ntawm qhov ncauj isosorbide mononitrate tsis nrawm txaus rau cov khoom no kom muaj txiaj ntsig hauv kev rho menyuam tawm qhov mob rov qab mob.

Kev txiav txim siab

Isosorbide mononitrate yog contraindicated rau cov neeg mob uas ua xua rau nws.

Tsis txhob siv Monoket® hauv cov neeg mob uas noj qee yam tshuaj rau kev ua haujlwm tsis zoo (phosphodiesterase inhibitors), xws li sildenafil, tadalafil, lossis vardenafil. Kev siv ua ke tuaj yeem ua rau mob hypotension hnyav, syncope, lossis myocardial ischemia.

Tsis txhob siv Monoket® ibhauv cov neeg mob uas tab tom noj cov tshuaj soluble guanylate cyclase stimulator riociguat. Kev siv ua ke tuaj yeem ua rau hypotension.

Lus ceeb toom

Kev nthuav dav ntawm cov teebmeem vasodilatory ntawm Monoket® iblos ntawm sildenafil tuaj yeem ua rau mob hypotension hnyav. Lub sijhawm kawm thiab kev tso tshuaj ntawm kev sib cuam tshuam no tseem tsis tau kawm. Kev saib xyuas kev saib xyuas tsim nyog tsis tau kawm, tab sis nws zoo li tsim nyog los kho qhov no raws li kev noj tshuaj nitrate ntau dhau, nrog kev nce ntawm qhov qis thiab nrog qhov nruab nrab ntim nthuav dav.

Cov txiaj ntsig ntawm isosorbide mononitrate hauv cov neeg mob uas mob myocardial infarction lossis lub plawv tsis ua haujlwm tsis tau tsim. Vim tias qhov cuam tshuam ntawm isosorbide mononitrate nyuaj rau txiav sai, cov tshuaj no tsis pom zoo hauv cov chaw no.

Yog tias isosorbide mononitrate tau siv nyob rau hauv cov xwm txheej no, ua tib zoo saib xyuas kev noj qab haus huv lossis saib xyuas lub cev yuav tsum tau siv kom tsis txhob muaj kev phom sij ntawm hypotension thiab tachycardia.

Cov kev ceev faj

dav dav

Kev mob hnyav heev, tshwj xeeb tshaj yog nrog lub cev ncaj, tuaj yeem tshwm sim txawm tias me me ntawm isosorbide mononitrate. Vim li no cov tshuaj no yuav tsum tau siv nrog ceev faj hauv cov neeg mob uas tej zaum yuav ntim ntau dhau los yog leej twg, vim li cas los xij, twb yog hypotensive. Hypotension tshwm sim los ntawm isosorbide mononitrate tuaj yeem ua ke nrog kev tsis sib haum xeeb bradycardia thiab nce angina pectoris.

Kev kho nitrate tuaj yeem ua rau mob angina ntau ntxiv los ntawm hypertrophic cardiomyopathy. Hauv cov neeg ua haujlwm hauv kev lag luam uas tau kis mus ntev rau cov neeg tsis paub (suav tias yog siab) koob tshuaj organic nitrates, kev ua siab ntev tshwm sim tshwm sim. Mob hauv siab, mob myocardial infarction, thiab txawm tias tuag sai sai tau tshwm sim thaum lub sijhawm tshem tawm ntawm nitrates ib ntus los ntawm cov neeg ua haujlwm no, ua rau pom tias muaj kev ntseeg tiag tiag ntawm lub cev. Qhov tseem ceeb ntawm cov kev soj ntsuam no rau niaj hnub, kev siv tshuaj kho mob ntawm qhov ncauj isosorbide mononitrate tsis paub.

Cov Ntaub Ntawv rau Cov Neeg Mob

Cov neeg mob yuav tsum tau qhia tias qhov ua tau zoo antianginal ntawm Monoket® ibcov ntsiav tshuaj tuaj yeem tswj hwm los ntawm kev ua tib zoo ua raws lub sijhawm teem tseg ntawm kev txhaj tshuaj (ob koob tshuaj sib nrug xya teev). Rau cov neeg mob feem ntau, qhov no tuaj yeem ua tiav los ntawm kev txhaj thawj koob tshuaj thaum sawv ntxov thiab koob thib ob 7 teev tom qab.

Ib yam li lwm cov nitrates, mob taub hau txhua hnub qee zaum nrog kho nrog isosorbide mononitrate. Hauv cov neeg mob uas tau mob taub hau no, mob taub hau yog tus cim ntawm kev ua haujlwm ntawm cov tshuaj. Cov neeg mob yuav tsum tiv thaiv kev ntxias kom zam kev mob taub hau los ntawm kev hloov kho lub sijhawm ntawm lawv txoj kev kho nrog isosorbide mononitrate, vim tias poob ntawm kev mob taub hau tuaj yeem cuam tshuam nrog kev ua kom tsis muaj peev xwm ua haujlwm antianginal. Aspirin thiab/lossis acetaminophen, ntawm qhov tod tes, feem ntau ua tiav daws isosorbide mononitrate-ntxias mob taub hau uas tsis muaj kev cuam tshuam zoo rau isosorbide mononitrate qhov kev ua haujlwm antianginal.

Kev kho nrog isosorbide mononitrate tuaj yeem cuam tshuam nrog lub teeb taub hau ntawm kev sawv, tshwj xeeb yog tom qab sawv ntawm qhov chaw rov los lossis zaum. Cov txiaj ntsig no yuav tshwm sim ntau dua rau cov neeg mob uas tau haus cawv.

Kev Sib Tham Tshuaj

Kev siv ua ke ntawm Monoket® nrog phosphodiesterase inhibitors nyob rau hauv ib daim ntawv twg yog contraindicated (saib NTAUB NTAWV).

Kev siv isosorbide mononitrate nrog riociguat, soluble guanylate cyclase stimulator, yog txwv tsis pub siv (saib NTAUB NTAWV).

Cov teebmeem vasodilating ntawm isosorbide mononitrate tuaj yeem ntxiv nrog lwm cov vasodilators. Dej cawv, tshwj xeeb, tau pom los nthuav tawm cov txiaj ntsig ntxiv ntawm ntau yam no.

Cim cov tsos mob orthostatic hypotension tau tshaj tawm thaum calcium channel blockers thiab organic nitrates tau siv ua ke. Kev hloov kho koob tshuaj ntawm ob tus neeg sawv cev hauv chav kawm yuav tsim nyog.

Carcinogenesis, Mutagenesis, Kev Tsis Txaus Siab ntawm Fertility

Tsis muaj pov thawj pom tias ua rau muaj mob qog noj ntshav tau pom hauv cov nas raug rau isosorbide mononitrate hauv lawv cov zaub mov noj ntawm qhov ntau txog 900 mg/kg/hnub rau thawj rau lub hlis thiab 500 mg/kg/hnub rau lub sijhawm ntxiv ntawm kev kawm uas cov txiv neej tau txhaj tshuaj txog li 121 lub lis piam thiab poj niam tau txhaj tshuaj txog li 137 lub lis piam. Tsis muaj pov thawj ntawm kev hloov pauv tau pom hauv vitro hauv Salmonella test (Ames test), hauv tib neeg lub cev lymphocytes, hauv Suav hamster cells (V79) lossis, hauv vivo hauv nas micronucleus test. Hauv txoj kev tshawb fawb txog kev muaj menyuam thiab muaj peev xwm ntawm ob tiam ntawm nas, Monoket® ibtsis muaj kev phom sij rau kev yug menyuam lossis kev ua me nyuam nrog rau qhov ncauj ntau txog 120 mg/kg/hnub. Ib koob ntawm 360 mg/kg/hnub tau cuam tshuam nrog kev tuag nce ntxiv hauv kev kho cov txiv neej thiab poj niam thiab txo qis qhov kev xeeb tub. (Saib cov lus kawg ntawm Cev xeeb tub ntu rau kev sib piv ntawm tsiaj-rau-tib neeg.)

Cev xeeb tub

Teratogenic Effects

Cev xeeb tub qeb B

Kev tshawb fawb txog kev rov ua dua tshiab hauv nas thiab luav ntawm koob tshuaj txog li 540 thiab 810 mg/kg/hnub, feem, tau tshaj tawm tsis muaj pov thawj pom tias muaj kev phom sij rau menyuam hauv plab vim isosorbide mononitrate. Txawm li cas los xij, tsis muaj kev tshawb fawb txaus thiab tswj tau zoo hauv poj niam cev xeeb tub. Vim tias kev tshawb fawb txog kev tsim tsiaj tsis yog ib txwm kwv yees tib neeg cov lus teb, Monoket® ibyuav tsum tau siv thaum cev xeeb tub tsuas yog xav tau kom meej.

Cov teebmeem Nonteratogenic

Kev hnyav thaum yug los, kev muaj menyuam hauv plab thiab kev loj hlob, thiab qhov tshwm sim ntawm kev yug menyuam tau cuam tshuam tsis zoo thaum nas cev xeeb tub tau txhaj tshuaj ntawm qhov ncauj ntawm 540 (tab sis tsis yog 270) mg isosorbide mononitrate/kg/hnub thaum lub sijhawm cev xeeb tub thiab pub niam mis. Qhov koob tshuaj no tau cuam tshuam nrog niam lub cev hnyav nce thiab ua rau lub cev tsis muaj zog ntawm leej niam lub zog.

Ntau yam ntawm MRHD*
Hom Cov koob tshuaj txhua hnub Raws li:
(mg/kg) Lub cev hnyav Lub cev nto
Luav 810 1013 375 ib
Nas 900 1125 195
540 675 117
500 625 108
360 450 78
270 ib 338 59

Kev suav xam xav tias tib neeg hnyav 50 kg thiab tib neeg lub cev thaj tsam ntawm 1.46 m2, luav hnyav ntawm 2 kg thiab luav lub cev thaj tsam ntawm 0.163 m2, thiab nas qhov hnyav ntawm 150 g thiab nas lub cev thaj tsam ntawm 0.025 m2. *Qhov siab tshaj plaws pom zoo tib neeg cov tshuaj (MRHD) yog 20 mg twv.

Niam laus

Nws tsis paub tias isosorbide mononitrate raug tso tawm hauv tib neeg cov mis. Vim tias ntau cov tshuaj raug tso tawm hauv tib neeg cov kua mis, yuav tsum tau ceev faj thaum siv isosorbide mononitrate rau tus poj niam laus.

Kev Siv Menyuam Yaus

Kev nyab xeeb thiab ua tau zoo ntawm isosorbide mononitrate hauv cov neeg mob menyuam yaus tsis tau tsim.

Kev siv Geriatric

Kev soj ntsuam soj ntsuam ntawm Monoket® ibtsis suav nrog cov naj npawb txaus ntawm cov hnub nyoog 65 xyoos thiab tshaj saud los txiav txim siab tias lawv teb txawv dua li cov hluas. Lwm qhov kev qhia kho mob tsis tau txheeb xyuas qhov sib txawv ntawm cov lus teb ntawm cov neeg laus thiab cov neeg mob yau. Feem ntau, kev xaiv koob tshuaj rau cov neeg laus yuav tsum tau ceev faj, feem ntau pib ntawm qhov qis kawg ntawm qhov ntau npaum li cas, xav txog qhov ntau dua ntawm kev ua haujlwm tsis zoo ntawm lub siab, lub raum, lossis lub plawv, thiab mob sib thooj lossis lwm yam tshuaj kho mob.

Cov Teeb Meem Tsis Zoo

Mob taub hau yog qhov tshwm sim feem ntau tshwm sim thiab yog qhov ua rau 2% ntawm txhua qhov kev tso tawm los ntawm kev tswj hwm-kev sim tshuaj. Mob taub hau tsawg zuj zus tom qab thawj ob peb hnub ntawm kev kho.

Cov lus hauv qab no qhia txog qhov tshwm sim tsis zoo tshwm sim hauv 1% lossis ntau dua ntawm cov ncauj lus hauv 6 qhov kev sim tshuaj placebo, ua hauv Tebchaws Meskas thiab txawv teb chaws. Tib lub rooj qhia pom qhov ntau zaus ntawm kev tshem tawm rau cov kev tsis zoo no. Hauv ntau qhov xwm txheej tsis zoo yog qhov tsis paub meej txog kev kho tshuaj.

Zaus Ntawm Cov Teeb Meem Tsis Zoo
(Kev txiav tawm) *
*
Qee tus tib neeg tsis ua haujlwm vim ntau yam.
6 Kev Tshawb Fawb Kev Tswj placebo
Dos Cov placebo 5mg ib 10 mg 20 mg / os
Cov neeg mob 160 54 52 159
Mob taub hau 6% (0%) 17% (0%) 13% (0%) 35% (5%)
Qaug zog nees nkaum%) 0% (0%) 4% (0%) 1% (0%)
Upper
Ua pa
Kab mob <1% (0%) 0% (0%) 4% (0%) 1% (0%)
Mob <1% (0%) 4% (0%) 0% (0%) <1% (0%)
Kiv taub hau 1% (0%) 0% (0%) 0% (0%) 4% (0%)
Xeev siab <1% (0%) 0% (0%) 0% (0%) 3% (2%)
Nce
Hnoos <1% (0%) 0% (0%) nees nkaum%) <1% (0%)
Pob khaus 0% (0%) 2% (2%) 0% (0%) <1% (0%)
Plab
Mob <1% (0%) 0% (0%) nees nkaum%) 0% (0%)
Ua xua
Cov tshuaj tiv thaiv 0% (0%) 0% (0%) nees nkaum%) 0% (0%)
Mob plawv
Teeb meem 0% (0%) nees nkaum%) 0% (0%) 0% (0%)
Mob hauv siab <1% (0%) 0% (0%) nees nkaum%) <1% (0%)
Raws plab 0% (0%) 0% (0%) nees nkaum%) 0% (0%)
Yaug 0% (0%) 0% (0%) nees nkaum%) 0% (0%)
Lub siab
Lability 0% (0%) nees nkaum%) 0% (0%) 0% (0%)
Pruritus 1% (0%) 2% (2%) 0% (0%) 0% (0%)

Lwm yam kev phom sij, txhua qhov tshaj tawm los ntawm tsawg dua 1% ntawm cov neeg mob, thiab feem ntau ntawm qhov tsis paub meej txog kev kho tshuaj, yog:

Kev mob plawv: mob myocardial infarction, apoplexy, arrhythmias, bradycardia, edema, kub siab, hypotension, pallor, palpitations, tachycardia.

Dermatologic: tawm hws.

Lub plab zom mov: anorexia, lub qhov ncauj qhuav, dyspepsia, nqhis dej, ntuav, poob phaus.

Genitourinary: teeb meem prostatic.

Lwm yam: amblyopia, mob nraub qaum, saj iab, mob leeg, mob caj dab, paresthesia, susurrus aurium.

Neurologic: ntxhov siab vim, tsis meej pem, kev nyuaj siab, insomnia, nervousness, npau suav phem, nyob tsis tswm, tshee, vertigo.

Ua pa: mob hawb pob, ua tsis taus pa, sinusitis.

Tsis tshua muaj neeg tsawg, cov tshuaj ib txwm muaj ntawm cov organic nitrates tau ua rau muaj methemoglobinemia hauv cov neeg mob zoo ib yam; rau kev sib tham ntxiv ntawm nws qhov kev kuaj mob thiab kev kho mob saib Tshaj dhau . Ib qho ntxiv, cov ntawv ceeb toom tsawg ntawm cov tsos mob ntawm angioedema tau tshaj tawm.

Tshaj dhau

Teebmeem Hemodynamic

Cov teeb meem tsis zoo ntawm isosorbide mononitrate overdose feem ntau yog cov txiaj ntsig ntawm isosorbide mononitrate lub peev xwm los ntxias vasodilatation, venous pooling, txo lub zog tso zis, thiab hypotension. Cov kev hloov pauv hemodynamic no tej zaum yuav muaj cov tsos mob tshwm sim, suav nrog kev nce siab hauv siab, nrog rau ib lossis tag nrho ntawm kev mob taub hau mob taub hau, tsis meej pem, thiab kub cev me ntsis; vertigo; palpitations; nrig txog kev pom teeb meem; xeev siab thiab ntuav (tej zaum nrog colic thiab txawm tias ntshav raws plab); syncope (tshwj xeeb tshaj yog nyob rau hauv txoj hauj lwm ncaj); huab cua tshaib plab thiab ua pa nyuaj, tom qab ntawd ua rau txo kev siv lub tshuab ua pa; diaphoresis, nrog rau ntawm daim tawv nqaij yaug los yog txias thiab clammy; plawv nres thiab bradycardia; tuag tes tuag taw; tsis nco qab; qaug dab peg thiab tuag.

Kev txiav txim siab hauv chav kuaj ntshav ntawm qib isosorbide mononitrate thiab nws cov metabolites tsis muaj dav, thiab cov kev txiav txim siab no, hauv ib qho xwm txheej twg, tsis muaj lub luag haujlwm tsim los tswj isosorbide mononitrate overdose.

Tsis muaj cov ntaub ntawv qhia tias koob tshuaj isosorbide mononitrate zoo li cas yuav ua rau muaj kev phom sij rau tib neeg. Hauv nas thiab nas, muaj kev tuag tseem ceeb ntawm qhov ncauj ntawm 1965 mg/kg thiab 2581 mg/kg, feem.

Tsis muaj cov ntaub ntawv qhia txog kev tawm dag zog lub cev (piv txwv li, kev txav txav los hloov pH ntawm cov zis) uas yuav ua rau tshem tawm isosorbide mononitrate. Isosorbide mononitrate raug tshem tawm ntawm cov ntshav thaum lub sij hawm hemodialysis.

Tsis muaj qhov tshwj xeeb antagonist rau vasodilator cov teebmeem ntawm isosorbide mononitrate tau paub, thiab tsis muaj kev cuam tshuam tau raug tswj hwm txoj kev tshawb fawb raws li kev kho ntawm isosorbide mononitrate overdose. Vim tias qhov hypotension cuam tshuam nrog isosorbide mononitrate overdose yog qhov tshwm sim ntawm venodilatation thiab arterial hypovolemia, kev kho mob ceev faj hauv qhov xwm txheej no yuav tsum tau qhia ncaj qha mus rau qhov nce hauv cov kua hauv nruab nrab. Kev nce siab ntawm tus neeg mob ob txhais ceg yuav txaus, tab sis kev tso ntshav tawm ntawm cov kua ntsev ib txwm lossis cov kua zoo sib xws kuj tseem yuav tsim nyog.

Kev siv epinephrine lossis lwm yam vasoconstrictors hlab ntsha hauv qhov chaw no yuav ua rau muaj kev phom sij ntau dua li qhov zoo.

Hauv cov neeg mob uas muaj kab mob hauv lub raum lossis lub plawv tsis ua haujlwm, kev kho mob ua rau lub hauv paus nthuav dav tsis yog yam tsis muaj kev phom sij. Kev kho mob isosorbide mononitrate overdose hauv cov neeg mob no tej zaum yuav hloov maj mam thiab nyuaj, thiab yuav tsum tau saib xyuas ntau ntxiv.

Methemoglobinemia

Methemoglobinemia tau tshaj tawm hauv cov neeg mob uas tau txais lwm cov organic nitrates, thiab nws tej zaum kuj tseem tuaj yeem tshwm sim ua ib qho kev cuam tshuam ntawm isosorbide mononitrate. Muaj tseeb nitrate ions tso tawm thaum lub sijhawm metabolism ntawm isosorbide mononitrate tuaj yeem oxidize hemoglobin rau hauv methemoglobin. Txawm hais tias hauv cov neeg mob tag nrho yam tsis muaj cytochrome b5 reductase kev ua, txawm li cas los xij, thiab txawm tias piv txwv tias cov nitrate ntau ntawm isosorbide mononitrate tau siv ntau rau oxidation ntawm hemoglobin, kwv yees li 2 mg/kg ntawm isosorbide mononitrate yuav tsum tau ua ntej ib qho ntawm cov neeg mob no tshwm sim hauv tsev kho mob tseem ceeb ( Hem 10%) methemoglobinemia. Hauv cov neeg mob uas muaj kev ua haujlwm ib txwm muaj reductase, kev tsim cov methemoglobin tseem ceeb yuav tsum tau txhaj ntau dua ntawm isosorbide mononitrate. Hauv ib txoj kev tshawb fawb uas 36 tus neeg mob tau txais 2-4 lub lis piam ntawm kev siv tshuaj nitroglycerin txuas ntxiv ntawm 3.1 txog 4.4 mg/hr (sib npaug, hauv kev tswj hwm tag nrho cov tshuaj nitrate ions, mus rau 7.8-11.1 mg ntawm isosorbide mononitrate ib teev), qib nruab nrab methemoglobin ntsuas yog 0.2%; qhov no tau piv rau qhov tau pom hauv cov neeg mob sib xws uas tau txais cov placebo.

Txawm li cas los xij cov kev soj ntsuam no, muaj cov ntaub ntawv ceeb toom ntawm cov methemoglobinemia tseem ceeb hauv kev koom tes nrog kev siv cov tshuaj nitrates ntau dhau. Tsis muaj ib tus neeg mob cuam tshuam tau xav tias ua rau muaj qhov txawv txav.

Methemoglobin qib muaj los ntawm cov chaw kuaj mob feem ntau. Kev kuaj mob yuav tsum raug xav tsis thoob hauv cov neeg mob uas pom cov pa oxygen tsis txaus txawm hais tias lub plawv tsim tawm txaus thiab tsim cov hlab ntsha txaus p02. Ib txwm, cov ntshav methemoglobinemic tau piav qhia tias yog xim av xim av, tsis muaj xim hloov pauv ntawm huab cua.

Thaum kuaj pom methemoglobinemia, kev kho mob ntawm kev xaiv yog methylene xiav, 1-2 mg/kg txhaj tshuaj.

Monoket Dosage thiab Kev Tswj

Cov txheej txheem pom zoo ntawm Monoket® ibntsiav tshuaj yog 20 mg ob zaug ib hnub, nrog rau koob tshuaj xya teev sib nrug. Kev pib koob tshuaj ntawm 5 mg (& frac12; ntsiav tshuaj ntawm 10 mg lub zog siv zog) yuav tsim nyog rau cov tib neeg uas muaj qhov tshwj xeeb me me tab sis yuav tsum nce mus txog tsawg kawg 10 mg los ntawm hnub thib ob lossis thib peb ntawm kev kho. Kev hloov kho tshuaj tsis tsim nyog rau cov neeg laus lossis cov neeg mob uas hloov pauv lub siab lossis lub raum ua haujlwm.

Raws li tau sau tseg saum toj no ( Clinical Pharmacology ), ntau qhov kev tshawb fawb ntawm cov organic nitrates tau qhia tias kev saib xyuas tas li 24 teev cov ntshav ntshav tau ua rau tsis kam ua haujlwm. Asymmetric (2 koob, 7 teev sib nrug) kev noj tshuaj rau Monoket® ibcov ntsiav tshuaj muab lub sijhawm tsis pub muaj nitrate txhua hnub kom txo qis kev txhim kho kev ua siab ntev.

Raws li tau sau tseg hauv qab no Clinical Pharmacology , kev tswj hwm kev tshawb fawb tau pom tias ua siab ntev rau Monoket® ibcov ntsiav tshuaj tshwm sim rau qee qhov thaum siv cov txheej txheem ob zaug ib hnub nyob rau hauv uas ob koob tshuaj tau muab xya teev sib nrug. Cov txheej txheem no tau pom tias muaj txiaj ntsig antianginal pib ib teev tom qab txhaj thawj zaug thiab kav ntev li xya teev tom qab txhaj tshuaj thib ob. Lub sijhawm (yog tias muaj) ntawm kev ua haujlwm antianginal dhau kaum plaub teev tsis tau kawm.

Hauv kev sim tshuaj, Monoket® ibtau muab coj los siv rau hauv ntau yam kev tswj hwm thiab koob tshuaj. Cov koob tshuaj ntau dua 20 mg ob zaug ib hnub (nrog koob tshuaj xya teev sib nrug) tsis tau kawm txaus. Cov koob tshuaj 5 mg ob zaug hauv ib hnub yog qhov ua tau zoo (ua tau zoo raws li kev ua siab ntev ntawm kev tawm dag zog) rau tsuas yog thawj hnub ntawm ob zaug ib hnub (nrog koob tshuaj 7 teev sib nrug) kev tswj hwm.

Yuav muab Monoket li cas

Monoket® ib(isosorbide mononitrate ntsiav tshuaj, USP), 10 mg yog dawb, puag ncig, qhab nia thiab kos '10' ntawm ib sab thiab kos 'SCHWARZ 610' ntawm lwm qhov. Lawv tau muab raws li hauv qab no:

Fwj ntawm 100 NDC 62175-361-01

Monoket® ib(isosorbide mononitrate ntsiav tshuaj, USP), 20 mg yog dawb, puag ncig, qhab nia thiab kos '20' ntawm ib sab thiab kos 'SCHWARZ 620' ntawm lwm qhov. Lawv tau muab raws li hauv qab no:

Fwj ntawm 100 NDC 62175-362-01

Khaws ntawm chav sov tswj 20 ° -30 ° C (68 ° -86 ° F) [Saib USP].

Khaws kaw kom nruj.

Faib los ntawm:
Kremers Urban Pharmaceuticals Inc.
Princeton, NJ 08540, Tebchaws Asmeskas

Luam tawm hauv Asmeskas
CIA72687C
Rev. 3E 01/2015

PRINCIPAL DISPLAY PANEL - 10 mg Tablet Fwj Daim Ntawv Cim

NDC62175-361-01

Monoket® ib
(isosorbide mononitrate
tab, USP)

10 mg

Rx xwb

100 sib sib zog nqus-qhab nia
ntsiav tshuaj

PRINCIPAL DISPLAY PANEL - 20 mg Tablet Fwj Daim Ntawv Cim

NDC62175-362-01

Monoket® ib
(isosorbide mononitrate
tab, USP)

20 mg / os

siv sij hawm ntev sudafed

Rx xwb

100 sib sib zog nqus-qhab nia
ntsiav tshuaj

Monoket
isosorbide mononitrate ntsiav tshuaj
Khoom Qhia
Yam Khoom HLOOV KEV POV THAWJ DRUG LABEL Yam Khoom (Qhov Chaw) NDC: 62175-361
Txoj Kev Tswj QAUV Teem caij DEA
Cov khoom xyaw nquag/nquag muaj nuj nqis
Lub Npe Lub Npe Lub hauv paus ntawm Kev Muaj Zog Lub zog
ISOSORBIDE MONONITRATE (ISOSORBIDE MONONITRATE) ISOSORBIDE MONONITRATE 10 mg
Cov khoom xyaw tsis haum
Lub Npe Lub Npe Lub zog
LACTOSE, TSIS MUAJ TSEEB FORM
TALC
SILICON DIOXIDE Cov
CELLULOSE, MICROCRYSTALLINE
ALUMINIUM STEARATE
Yam Khoom
Xim DAWB Cov qhab nia 2 qab
Zoo ROV Loj 7 hli
Tsw Txoj Cai Luam Tawm 10; XEEB; 610
Muaj
Ntim
# Khoom Code Cov lus piav qhia pob
1 NDC: 62175-361-01 100 TABLET hauv 1 lub raj mis
Cov Lus Qhia Txog Kev Lag Luam
Qeb Qeb Naj Npawb Daim Ntawv Thov lossis Monograph Citation Hnub Pib Ua Lag Luam Hnub Kawg Ua Lag Luam
NDA NDA020215 06/30/1993
Monoket
isosorbide mononitrate ntsiav tshuaj
Khoom Qhia
Yam Khoom HLOOV KEV POV THAWJ DRUG LABEL Yam Khoom (Qhov Chaw) NDC: 62175-362
Txoj Kev Tswj QAUV Teem caij DEA
Cov khoom xyaw nquag/nquag muaj nuj nqis
Lub Npe Lub Npe Lub hauv paus ntawm Kev Muaj Zog Lub zog
ISOSORBIDE MONONITRATE (ISOSORBIDE MONONITRATE) ISOSORBIDE MONONITRATE 20 mg / os
Cov khoom xyaw tsis haum
Lub Npe Lub Npe Lub zog
LACTOSE, TSIS MUAJ TSEEB FORM
TALC
SILICON DIOXIDE Cov
CELLULOSE, MICROCRYSTALLINE
ALUMINIUM STEARATE
Yam Khoom
Xim DAWB Cov qhab nia 2 qab
Zoo ROV Loj 9 hli
Tsw Txoj Cai Luam Tawm 20; XEEB; 620
Muaj
Ntim
# Khoom Code Cov lus piav qhia pob
1 NDC: 62175-362-01 100 TABLET hauv 1 lub raj mis
Cov Lus Qhia Txog Kev Lag Luam
Qeb Qeb Naj Npawb Daim Ntawv Thov lossis Monograph Citation Hnub Pib Ua Lag Luam Hnub Kawg Ua Lag Luam
NDA NDA020215 06/30/1993
Daim ntawv lo -Lannett Tuam Txhab, Inc. (006422406) Cov
Lannett Tuam Txhab, Inc.

Kev Tsis Pom Zoo Kho Mob