Kev txhaj tshuaj Ziconotide, ua lag luam li Prialt, yog ib qho khoom siv hluavtaws omega conotoxin MVIIA, uas belongs rau qeb ntawm intrathecal analgesics. Nws tau pom zoo rau kev ua lag luam los ntawm US FDA thiab European Union hauv 2004. Cov tshuaj no yog tsim rau cov neeg mob mob hnyav uas tsis tau teb rau lwm yam kev kho mob analgesic (xws li systemic analgesics lossis intrathecal morphine), tshwj xeeb tshaj yog rau mob qog noj ntshav thiab refractory neuropathic mob. Nws cov txheej txheem ntawm kev ua haujlwm yog txhawm rau txhawm rau tshwj xeeb N- hom voltage-gated calcium channel (CaV2.2) nyob rau hauv tus txha caj qaum dorsal horn, inhibit qhov tso tawm ntawm qhov mob neurotransmitters, thiab muaj cov yam ntxwv ntawm kev tsis quav ntsej, tsis kam rau siab, thiab muaj kev nyab xeeb siab ntawm kev txiav tawm.
Cov khoom tsim
Ziconotide Polyacetate COA
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| Certificate of Analysis | ||
| Compound npe | Ziconotide Polyacetate | |
| Qib | Pharmaceutical qib | |
| CAS Nr. | 107452-89-1 | |
| Ntau | 30g | |
| Ntim txheem | PE hnab + Al foil hnab | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 202601090088 | |
| MFG | Peb 9, 2026 | |
| EXP | Peb 8, 2029 | |
| Qauv |
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| Yam khoom | Enterprise txheem | Kev txheeb xyuas qhov tshwm sim |
| Qhov tshwm sim | Dawb los yog yuav luag dawb hmoov | Ua raws |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug li 5.0% | 0.54% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.42% |
| Hnyav Hlau | Pb Tsawg dua lossis sib npaug li 0.5ppm | N.D. |
| Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Hg Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Cd Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Purity (HPLC) | Ntau dua lossis sib npaug li 99.0% | 99.98% |
| Ib leeg impurity | <0.8% | 0.52% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 95 |
| E. Coli | Tsawg dua lossis sib npaug li 2MPN / g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (los ntawm GC) | Tsawg dua lossis sib npaug li 5000ppm | 500ppm ua |
| Cia | Khaws rau hauv qhov chaw kaw, tsaus, thiab qhuav hauv qab -20 degree | |
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| Chemical Formula: | C97H170N34O30S5 |
| Exact Mass: | 2511 |
| Molecular Luj: | 2513 |
| m/z: | 2511 (100.0%), 2513 (95.3%), 2511 (40.8%), 2513 (22.6%),2511 (21.5%), 2454 (17.2%), 2453 (12.6%), 2452 (12.0%), 2455 (11.7%), 2453 (11.2%), 2454 (6.5%), 2454 (6.2%), 2453 (5.9%), 2455 (4.5%), 2453 (4.0%), 2456 (3.9%), 2452 (3.8%), 2455 (2.8%), 2454 (2.7%), 2455 (2.5%), 2456 (2.0%), 2453 (2.0%), 2455 (1.9%), 2452 (1.9%), 2454 (1.6%), 2456 (1.5%), 2455 (1.4%), 2456 (1.4%), 2455 (1.3%), 2453 (1.1%), 2452 (1.1%), 2456 (1.1%), 2457 (1.0%) |
| Elemental Analysis: | C, 47.50; H, 6.99; N, 19.42; O, 19.57; S, 6.54 |
Cov ntaub ntawv noj tshuaj uas twb muaj lawm suav nrog cov tshuaj txhaj tshuaj nrog cov concentration ntawm 25mg / ml thiab 100mg / ml, uas tau muab tshuaj intrathecally los ntawm implantable lossis sab nraud infusion twj. Feem ntau cov kev phiv tshwm sim muaj xws li lub paj hlwb (xws li kiv taub hau, ataxia), digestive system ( xeev siab) thiab urinary system ( tso zis ). Contraindications muaj xws li keeb kwm ntawm kev ua xua, mob hlwb, kab mob intracranial, thiab los ntshav. Cov tshuaj yog metabolized los ntawm peptidase thiab tawm hauv daim ntawv ntawm cov amino acids, nrog tsawg dua 1% ntawm thawj cov tshuaj tawm hauv cov zis.
Mob qog noj ntshav yog ib qho ntawm cov tsos mob tshwm sim, nyuaj, thiab tsis tu ncua ntawm cov neeg mob qog noj ntshav thaum lub sijhawm thiab tom qab kev kho mob, cuam tshuam rau lawv txoj kev noj qab haus huv thiab lub neej zoo. Txawm hais tias muaj kev nce ntxiv hauv kev ntsuam xyuas thiab kev tswj xyuas qhov mob ntsig txog kev kho mob qog noj ntshav, qhov tshwm sim ntawm qhov mob tseem muaj txog li 55%. Txawm hais tias cov tshuaj opioid ib txwm muaj peev xwm muab tau qee qhov kev ua kom tsis zoo, lawv muaj teeb meem xws li kev mob tshwm sim thiab kev quav yeeb tshuaj, ua rau mob tsis txaus.Kev txhaj tshuaj Ziconotide, raws li tsis yog opioid analgesic, muab kev xaiv tshiab rau kev kho mob qog noj ntshav.
1. Mob qog noj ntshav tsis txaus
Hauv kev kho mob qog noj ntshav, nws tsuas yog siv los daws qhov teeb meem nyuaj ntawm kev mob qog noj ntshav tsis txaus. Kev kho mob nyuaj rau mob qog noj ntshav yog hais txog qhov mob uas tsis tuaj yeem tswj tau zoo txawm tias muaj kev cuam tshuam zoo ntawm cov tshuaj analgesics thiab adjuvant therapy, lossis qhov twg cov neeg mob tsis tuaj yeem zam kev kho mob vim yog cov tshuaj phiv tshuaj thiab lwm yam laj thawj. Cov tshuaj analgesic tshuaj suav nrog ntau yam, suav nrog cov tshuaj nonsteroidal los tiv thaiv -cov tshuaj tiv thaiv kab mob, uas feem ntau siv tshuaj tua kab mob, tshuaj tua kab mob, thiab tshuaj tiv thaiv- mob los ntawm inhibiting cov synthesis ntawm prostaglandins hauv lub cev. Feem ntau muaj xws li ibuprofen, aspirin, thiab lwm yam; Cov tshuaj tsis muaj zog opioid, xws li codeine, muaj cov nyhuv analgesic tsis muaj zog tab sis kuj muaj qee qhov kev pheej hmoo ntawm kev quav tshuaj; Cov tshuaj opioid muaj zog, xws li morphine thiab fentanyl, feem ntau yog siv cov tshuaj tua kab mob muaj zog hauv kev kho mob, tab sis ntev - siv tau yooj yim tuaj yeem ua rau mob siab rau thiab kev quav tshuaj. Adjuvant therapy cov tshuaj muaj xws li cov tshuaj tiv thaiv kev nyuaj siab, xws li amitriptyline, uas tuaj yeem txhim kho lub siab lub ntsws ntawm cov neeg mob thiab txo qis qhov mob los ntawm kev tswj cov neurotransmitters;
Cov tshuaj Anticonvulsant, xws li carbamazepine, feem ntau yog siv los kho cov mob neuropathic los ntawm kev ua kom cov hlab ntsha hauv cov hlab ntsha kom txo tau qhov mob.
Qhov ua rau ntawm hom mob qog noj ntshav tsis txaus ntseeg no yog qhov nyuaj heev.
Ntawm qhov tod tes, cov qog lawv tus kheej muaj zog invasiveness thiab tuaj yeem cuam tshuam ncaj qha rau cov hlab ntsha, pob txha, lossis cov kabmob hauv nruab nrog cev. Thaum cov qog ua rau cov hlab ntsha, lawv tuaj yeem cuam tshuam cov qauv thiab kev ua haujlwm ntawm cov hlab ntsha, ua rau cov hlab ntsha txawv txav thiab ua rau mob hnyav. Piv txwv li, qog nqaij hlav ntawm cov leeg txha caj qaum tuaj yeem ua rau mob hnyav, uas tuaj yeem cuam tshuam ntau yam ceg los yog lub cev. Thaum cov qog nkag mus rau cov pob txha, lawv tuaj yeem ua rau cov pob txha puas thiab ua rau cov pob txha mob, uas feem ntau hnyav thiab hnyav dua thaum ua haujlwm. Thaum cov qog nkag mus rau hauv lub cev, lawv tuaj yeem ua rau lub cev tsis ua haujlwm thiab mob. Piv txwv li, mob qog noj ntshav ua rau lub siab tuaj yeem ua rau mob plab thiab mob hauv plab sab xis.
Ntawm qhov tod tes, ntau txoj hauv kev siv hauv kev kho mob qog, xws li kev phais, xov tooj cua, kev siv tshuaj khomob, thiab lwm yam, kuj tuaj yeem ua rau cov hlab ntsha puas tsuaj. Thaum lub sij hawm phais, cov hlab ntsha peripheral tej zaum yuav inevitably raug puas, ua rau postoperative mob syndrome. Kev kho hluav taws xob, thaum tua cov qog hlwb, kuj tseem tuaj yeem ua rau muaj kev puas tsuaj rau cov ntaub so ntswg ib puag ncig, ua rau hluav taws xob - ua rau mob neuropathy thiab mob. Cov tshuaj kws khomob muaj qee yam toxicity thiab tuaj yeem ua rau puas tsuaj rau lub paj hlwb, ua rau mob neuropathic.
Kev them nyiaj yug Case: Hauv cov xwm txheej nplua nuj ntawm kev kho mob, ntau tus neeg mob mob qog noj ntshav muaj teeb meem loj heev los ntawm kev ua haujlwm tsis zoo ntawm cov tshuaj tua kab mob. Ua piv txwv tus neeg mob uas mob qog nqaij hlav pancreatic siab heev. Mob qog noj ntshav pancreatic nws tus kheej yog nto moo rau nws cov malignancy siab thiab muaj zog cov tsos mob. Tom qab kuaj mob, tus neeg mob nquag tau txais kev kho tus qauv.
Hais txog kev tswj mob, tus kws kho mob tau siv siab -dose hydrocodone sustained- tso cov ntsiav tshuaj thiab hydromorphone raws li cov txheej txheem niaj hnub. Hydroxyketone sustained- cov ntsiav tshuaj tso tawm yog ib qho tshuaj opioid muaj zog uas ua rau muaj kev ua xua los ntawm kev khi rau opioid receptors, muab kev mob hnyav thiab ruaj khov. Hydromorphone kuj yog ib qho tshuaj tua kab mob muaj zog nrog qhov pib sai thiab luv luv ntawm kev ua. Txawm li cas los xij, txawm hais tias siv ob lub zog tshuaj tua kab mob, tus neeg mob qhov kev tswj xyuas qhov mob tseem tsis txaus siab. Kev mob tshwm sim ntau zaus tshwm sim, nrog kev mob hnyav thaum lub sijhawm txhua ntu, ua rau tus neeg mob tsis tuaj yeem mob thiab cuam tshuam rau lawv lub neej txhua hnub, xws li noj mov, pw tsaug zog, thiab kev ua ub no, ua rau muaj kev poob qis hauv lawv lub neej zoo.
Hauv qhov no, tom qab kev ntsuam xyuas dav dav, tus kws kho mob txiav txim siab hloov tus neeg mob mus rau intrathecal txhaj ntawm Ziconotide rau kev kho mob. Kev txhaj tshuaj intrathecal yog ib txoj hauv kev los tswj cov tshuaj ncaj qha rau hauv qhov chaw subarachnoid, uas tuaj yeem ncav cuag qhov chaw ua haujlwm sai, txhim kho kev ua tau zoo ntawm cov tshuaj, thiab txo cov kev mob tshwm sim los ntawm kev siv tshuaj. Tom qab ib lub sij hawm ntawm kev txhaj tshuaj intrathecal nrog Ziconotide, muaj txuj ci tseem ceeb tshwm sim thiab tus neeg mob qhov mob tau txo qis. Qhov zaus ntawm qhov mob tshwm sim tau txo qis, thiab qhov mob ntawm qhov mob kuj tau txo qis heev. Cov neeg mob tuaj yeem noj, pw tsaug zog, thiab koom nrog qee yam haujlwm yooj yim ib txwm, thiab lawv lub neej zoo tau zoo dua qub. Cov ntaub ntawv no qhia meej txog qhov ua tau zoo thiab qhov zoo ntawm Ziconotide hauv kev kho mob qog noj ntshav refractory.
Cov ntaub ntawv qhov chaw: Zoo siab txais tos rau lub vev xaib ntawm lub tuam tsev kho mob ntawm Tuam Tshoj Journal of Pain Medicine! (Qinyun Journal) luam tawm "Kev siv tshuaj muaj txiaj ntsig • Daim ntawv thov ntawm tus neeg mob-tshuaj analgesia thev naus laus zis hauv kev kho mob ntawm tus mob qog nqaij hlav pancreatic 11 mg mob qog noj ntshav"
2. Hom mob qog noj ntshav tshwj xeeb
Kev txhaj tshuaj Ziconotidetau qhia txog kev kho mob zoo rau ntau hom mob qog noj ntshav, suav nrog mob keeb kwm yav dhau thiab mob hnyav, ob hom mob uas ua rau mob hnyav rau cov neeg mob. Kev mob tom qab yog qhov mob tsis tu ncua uas cuam tshuam cov neeg mob zoo li qhov tsis pom shackle. Hom mob no tuaj yeem tshwm sim los ntawm cov yam ntxwv xws li compression tas li, ntxeem tau, lossis cov lus teb ntawm cov qog. Qib ntawm qhov mob yog qhov ruaj khov, tab sis nws yuav nyob mus ntev, cuam tshuam rau tus neeg mob lub neej txhua hnub thiab lub siab lub ntsws. Cov neeg mob yuav hnov ntxhiab, ntxhov siab, thiab ntxhov siab vim yog mob tom qab tsis tu ncua, txo lawv lub neej zoo. Qhov mob tawg, ntawm qhov tod tes, yog qhov mob tam sim ntawd thiab mob siab heev uas tsis tuaj yeem xav txog thiab feem ntau tawm tsam yam tsis muaj tus neeg mob tiv thaiv, ntes lawv ntawm tus neeg saib xyuas. Qhov zaus thiab qhov hnyav ntawm qhov mob tshwm sim txawv ntawm ib tus neeg mus rau lwm tus. Qee tus neeg mob yuav ntsib nws ntau zaus hauv ib hnub, thaum lwm tus tuaj yeem ntsib nws ib zaug ob peb hnub.
Txawm li cas los xij, qhov mob theem thaum txhua qhov kev tawm tsam yog qhov hnyav heev, zoo li rab riam txiav lossis hluav taws xob poob siab, ua rau mob hnyav rau tus neeg mob. Vim qhov nyuaj ntawm kev kwv yees thiab tswj kev mob hnyav, cov neeg mob ntsib teeb meem ntau dua thaum txoj kev kho mob.
Los ntawm kev txhaj tshuaj intrathecal tas mus li, nws tuaj yeem ua ncaj qha rau ntawm N- hom calcium channels hauv tus txha caj qaum dorsal horn, exerting nws tshwj xeeb analgesic nyhuv. Rau kev mob keeb kwm yav dhau, kev sib kis ntawm qhov mob tshwm sim tuaj yeem ua rau tsis tu ncua thiab ruaj khov, tswj kev mob thiab tswj tus neeg mob qhov mob ntawm theem qis, yog li txhim kho tus neeg mob lub neej zoo. Rau qhov mob tawg, nws tuaj yeem txo nws qhov zaus thiab siv qhov pib. Nws txo qhov tshwm sim ntawm qhov mob tshwm sim los ntawm kev tswj cov excitability ntawm lub paj hlwb thiab txo qhov rhiab heev ntawm neurons rau mob stimuli. Lub caij no, nws cov txiaj ntsig txhawb nqa tuaj yeem tswj hwm lub xeev ruaj khov ntawm tus txha caj qaum dorsal horn neurons thiab tiv thaiv qhov mob hnyav tshwm sim los ntawm kev tawm dag zog ntau dhau ntawm cov neurons.
Cov ntaub ntawv tshawb fawb: txhawm rau txheeb xyuas qhov ua tau zoo ntawmKev txhaj tshuaj Ziconotidehauv kev kho cov mob qog noj ntshav tshwj xeeb, kev tshawb fawb ntau qhov chaw tseem ceeb uas muaj 200 tus neeg mob mob qog noj ntshav tau ua rau hauv - tshawb nrhiav qhov tob. Hauv txoj kev tshawb no, cov kws tshawb fawb tau ua raws li kev tshawb fawb tshawb fawb thiab cov qauv tsim los tswj kev txhaj tshuaj intrathecal rau 200 tus neeg mob uas muaj ntau hom thiab theem mob qog noj ntshav, thiab ua 12 lub lis piam soj ntsuam thiab ua raws li - nce. Cov txiaj ntsig kev tshawb fawb pom tau tias tom qab 12 lub lis piam ntawm kev txhaj tshuaj intrathecal, 65% ntawm cov neeg mob ua tiav qhov mob ntawm 30% lossis ntau dua. Cov ntaub ntawv no qhia tau hais tias nws cov txiaj ntsig tseem ceeb hauv kev kho mob qog noj ntshav. Qhov tseem ceeb tshaj, txoj kev tshawb fawb kuj pom tias muaj qhov txo qis hauv qhov tshwm sim ntawm qhov mob hnyav heev hauv cov neeg mob. Qhov no txhais tau hais tias tom qab tau txais kev kho mob, cov neeg mob tsis tsuas yog tswj tau lawv qhov mob tom qab, tab sis kuj tseem txhim kho qhov mob hnyav uas tau ua rau lawv nyuaj siab rau lub sijhawm ntev. Cov neeg mob tuaj yeem ntsib lawv qhov mob thiab lub neej nyob ntsiag to, thiab lawv lub neej zoo tau zoo dua qub.
Cov ntaub ntawv qhov chaw: "Kev mob tshwm sim thiab kev ceev faj ntawm Prialt Ziconotide" luam tawm los ntawm Zhihu Kem
FAQ
Puas yog ziconotide muaj zog dua morphine?
Cov kev tshawb fawb no tau qhia tias ziconotide muaj zog dua li morphine thiab tshwj xeeb tshaj yog ua tau zoo hauv cov qauv ntawm kev mob tsis tu ncua (ntev ntsuas hauv feeb mus rau teev) thiab mob ntev (ntev ntsuas hauv cov xuab moos mus rau hnub).
Puas yog ziconotide yog peptide?
Ziconotide (tseem hu ua SNX-111) yog neurotoxic peptide muab los ntawm lub khob hliav qab Conus magus suav nrog 25 amino acids nrog peb daim ntawv cog lus disulphide.
Thaum twg ziconotide tau pom zoo los ntawm FDA?
Ziconotide tau tso cai FDA tso cai rau lub Kaum Ob Hlis 28, 2004 rau kev lag luam los ntawm TerSera therapeutics LLC. nyob rau hauv lub npe Prialt. Txog niaj hnub no, ziconotide tsuas yog calcium channel thaiv peptide tau pom zoo siv los ntawm FDA.
Ziconotide yog dab tsi?
Ib qho hluavtaws, nonopiod, nees nkaum-tsib amino acid polybasic peptide analogue ntawm ib qho omega-conotoxin muab tau los ntawm marine snail Conus magus nrog rau kev ua xua.
Cim npe nrov: Ziconotide txhaj tshuaj, Tuam Tshoj ziconotide txhaj tshuaj manufacturers, lwm tus neeg
