Safinamide: Mushonga Wekutanga weAnti Anti-Parkinson mumakore gumi

Mishonga inogona kubatsira avo vane chirwere chePasinson gare gare

Muna March 2017, FDA yakagamuchira safinamide (Xadago) yekushandiswa kwekliniki muUnited States. Safinamide ndiyo yekutanga mishonga inogamuchirwa neRDA kuti ipe chirwere cheParkinson mumakore anodarika gumi. Icho chimiro chekugadzirisa, kana kuwedzera-pane kurapwa, kushandiswa pamwe chete nevevodopa.

Zvirwere zvePacinsinson zvakatsanangurwa

Chirwere chePasinsinson chirwere chekufamba chinowedzera zvishoma nezvishoma uye chinotanga pamakore anenge makumi matanhatu.

Zviratidzo zvinosanganisira kudedera, kuoma, kunonoka kufamba, uye kushaya mari yakaenzana. Ichi chirwere chinopedzisira chinoguma nezvinetso nekufamba, kutaura, nezvimwe zviitiko zvekugara kwezuva nezuva. MuUnited States, vanenge 50 000 vanhu vanoonekwa kuti vane chirwere chePasinson gore negore.

Kunyange zvazvo pasina mushonga wePalinson's disease, kune marapirwo anobatsira nehutano hwekutarisira, kusanganisira zvinotevera:

Zvinosuruvarisa, hapana marapirwo anononoka kana kumisa kufambira mberi kwechirwere cheParkinson.

Levodopa ndiyo yakanyanya kunyanya uye yakakurumbira mishonga inoshandiswa kurapa chirwere chePalinson; zvisinei, zvinogadziriswa zvinopedzisira zvichipedza nguva uye zvinogona kutungamirira kumagumisiro asina kunaka kusanganisira dyskinesia .

Zvinodhaka zvinosanganisira COMT inhibitors, dopamine agonists, uye kwete-dopaminergic-kurapa-dzakadai se anticholinergic mishonga uye amantadine-inogona kushandiswa seimwe nzira kune levodopa, kuwedzera kune levodopa, kana pamwe chete.

Mune vanhu vane chirwere chePasinson chapamusoro, apo mishonga inopera, huro hwehupfungwa hunokurudzira (chirwere chepfungwa) hunogona kuonekwa sekubatsira kuderedza zviratidzo.

Kazhinji, mishonga yakachengeterwa vanhu vane zviratidzo zvave zvakaoma zvakakwana kuti zvipindire nemabasa ekugara kwezuva nezuva. Levodopa inowanzova mushonga wekusarudzwa kune vanhu vane makore makumi matanhatu nemapfumbamwe vane mararamiro avanoita zvakakanganisika. Vanhu vaduku vanopfuura 65 vanogona kurapwa ne dopamine agonist.

Zvinodhaka zvinotanga pamwero wakaderera zvikuru uye kurapwa kunowanzomira kwenguva yakareba sezvinobvira. Zvisinei, tsvakurudzo inobatsira kutungamira chirongwa che "kutanga pasi uye kuenda kunonoka" nemadhora e levodopa akabatanidzwa. Maererano nemunyori Peter Jenner:

Kuiswa kwaL-Dopa [levodopa] mune avo vane nguva refu yezvirwere kana kuwedzerwa kwepamusoro kunogona kuunza nguva shomanana yezvinobudirira musati matambudziko emotokari aoneka. Munguva pfupi yapfuura, kuchengetedza chirwere cheL-dopa pasi pe 400 mg pazuva pazuva rekutanga rePED rakaratidzwa kuderedza dambudziko rekudzivirira dyskinesia.

Zvisinei, Jenner anoenderera mberi achicherechedza zvinotevera:

Kushandiswa kwekutanga kweL-dopa kwakaratidzwawo kuti ndiyo inonyatsoshanda kurapwa kwemagetsi zviratidzo uye kwete kuisa njodzi yenguva refu ye dyskinesia.

Zvechokwadi, uchapupu hunopesana hwakadaro hunosimbisa kuti zvishomanana zvatinoziva nezvehutano uye kurapwa kwechirwere chePasinson.

Safinamide: Inoshanda Sei?

Mune vanhu vane chirwere chePasinson, uropi hahukwanisi kubereka zvakakwana zvehutachiona hunonzi dopamine .

Masero anounza dopamine angafa kana kuti haana kuoma. Dopamine inofanirwa kuti yakwanise kugadziriswa motokari uye kufamba.

Kunyanya, dopamine inotumira zviratidzo muuropi iyo inobatanidzwa mukufamba kwakanaka, kune chinangwa sekudya, kunyora, uye kuverenga. Kufanana selegeline uye rasagaline, safinamide rudzi rwe MAO-B inhibitor, iro rinodzivisa kuparara kwedopamine uye nokudaro rinowedzera maitiro aro muuropi.

Yezvinyorwa, safinamide inogadzirisawo kusununguka kwegutamate; zvisinei, chiitiko chaicho chechiito ichi pamabasa ekurapa kwechirwere hazvizivikanwi.

Kusiyana nezvimwe MAO-B inhibitor, iyo inogona kurongerwa yoga kune avo vane chirwere chePasinson yekutanga-kutanga , safinamide inoshandiswa kushandiswa pamwe chete nedzimwe mhando dze antiparkinson zvinodhaka zvezvekupedzisira-chirwere chechirwere, zvikurukuru levodopa uye dopamine agonists.

Vanhu pavanotanga kurapwa kwezviratidzo zveParkinson, zvinodhaka zvinowanzoshanda zvakanaka uye zviratidzo zvinodzorwa zuva rose. Pakati pemakore mashanu ne10, zvisinei, kubudirira kwezvinodhaka zvePalinson zvinowanzoitika kune vanhu vazhinji, uye kuronga zviratidzo kunowedzera kuoma kuderedza.

Kunyanya, kune vanhu vane pakati pekupedzisira-chirwere chePalinson's disease, kuchinja kwemoto kana kushanduka kwemisungo miviri (dyskinesia uye kupisa ) inotanga kuomera.

Dyskinesia inonyanya kutaurwa kune vanhu vanotora levodopa uye inopisa simba remishonga yekurapa. Kuratidzwa kweDyskinesia bodes zvisina kunaka nekuremekedza kujekesa uye kunofanirwa kunonoka kwenguva yakareba. Uyezve, zviratidzo zvisiri-motor, zvakadai sekuora mwoyo, kuora mwoyo, uye kukanganisa, izvo zvinokanganisa zvishoma kana zvinodhaka zvinokonzerwa nedopaminergic, zvakare zvinetso.

Varwere ivavo vanobhadhara mushure mekurapa kwakakwana kwakagara kwenguva yakaoma kurapa mune fashoni inochengetedza kufamba uye hupenyu hwehupenyu.

Mune mamwe mazwi, kamwechete levodopa inomira kushanda zvakare, muchidimbu nokuti hatinzwisisi hutachiwana hwekuderedzwa uku, zvakaoma kuti vanhu vadzokere kune imwe tsanangudzo yepamusoro uye mararamiro ehupenyu akaonekwa kare munguva yezvirwere apo levodopa nedzimwe dopaminergic agents vakanga vari kushanda.

Uyezve, kunyange kana magetsi akabatanidzwa mukati maro, zvisingaiti motokari zvakadai sekusawirirana kwepfungwa, kushaya hope, uye kuora mwoyo kwemazuva ano kunonetsa kune avo vane chirwere chePasinson.

Zvinosuruvarisa, hatigoni kufanotaura kuti vanhu vane chirwere chePasinson gare gare vachaita sei kuchinja uye motokari. Kakawanda, chirwere chehutachiona, chirwere chetachiona, urefu hwekurapa neyevodopa, levodopa madheji, hutano, uye kuyerwa kwemuviri zvinotendwa kuti zvinotora mukana mukugadzirisa kwekupedzisira.

PASI uye OFF Times

"NGUVA nguva" inoreva nguva iyo mishonga inoshanda zvakakwana uye zviratidzo zvePalinson's disease zvinodzorwa.

"HURI nguva" inoreva nguva iyo mishonga inopera uye zviratidzo zvePasinson, zvakadai sokudengenyeka, kusagadzikana, uye kuoma kunofambazve.

Kuwedzerwa kwe safinamide kumishonga yemishonga yevanhu vane chirwere chePacinson chakakwira ichi kutora levodopa inowedzera chikamu cheUN panguva uye inoderedza nguva YAKAPA.

Safinamide Clinical Trials

Migumisiro inobva maitiro maviri emakiriniki emakirini akajekesa maitiro anobatsira ekushandisa safinamide pakati pevanhu vane chirwere chePasinson chinopfuura. Vaya vatori vechikamu vakanga vaonekwa kuti vane chirwere chePasinson mumakore matatu kana mashanu.

Chirwere chekutanga chemakiriniki chakaongorora vatora 669 vane motokari kuchinja. Vaya vatori vechikamu vakagamuchira safinamide pamwe chete nemamwe mishonga inonzi antiparkinson kana placebo (kwete safinamide) nemamwe madhiragi anonzi antiparkinson.

Avhareji PAKUVA yevatori vechikamu yaiva pakati peawa 9.3 uye 9.5. Pashure pemwedzi mitanhatu yekuedzwa, KUNA nguva yakawedzerwa muzvikamu zvose zvevarwere; zvisinei, NEI nguva dzaive nemaminitsi makumi matatu kwenguva refu kune avo vanotora safinamide.

Mushure memakore maviri ekurapwa, muvhareji ONI nguva yakagara yakangofanana kune avo vanotora safinamide asi yakaderera kune avo vanotora placebo. Nokudaro pashure pemakore maviri paavhareji, vatori vechikamu vachitora safinamide pamwe ne levodopa pamwe nemamwe mishonga antiparkinson vakawana imwe imwe nguva yekurapa kwezviratidzo zvePalinson's disease.

Yezvinyorwa, safinamide yakaderedzwa MUSI nguva nemaminitsi makumi matatu. Yeuka kuti nguva dzisingarevi dzinoreva nguva iyo antiparkinson zvinodhaka, uye zviratidzo zvakadai sekudengenyeka zvakare zvakare kuwedzera.

Mukuwedzera pakuwedzerwa paZUVA uye kupfupika nguva, safinamide yakavandudza kufamba (motokari) kune avo vanoitora. Uyezve pamusana wepamusoro, safinamide yakabatsirawo nemabasa ekugara kwezuva uye hupenyu hwehupenyu.

Saizvozvowo zvinokonzerwa nekuedzwa kwechipiri, kunosanganisira 549 vatori vechikamu, vanoratidza kuwedzera kweII nguva neawa imwe chete kune avo vanotora safinamide kana vachienzanisa nevaya vanotora placebo pamwe nekuderedza munguva OFF. Uyezve, kuvandudzwa kwekushanda uye hutano hwehupenyu hwakawanda hwakaonekwa zvakare.

Safinamide Negative Side Effects

Nemhaka yemigumisiro yakaipa, 3.7 muzana yevatori vechikamu vanotora safinamide vakadzingwa kunze kwekuongororwa kwemakiriniki kana vachienzaniswa ne4% yevaya vanotora placebo.

Migumisiro yakaipa yakajairika inowanikwa panguva iyi miedzo yekliniki yaisanganisira zvinotevera:

Pakati pezviratidzo izvi, dyskinesia yaive yakawanda kaviri inowanikwa nevanhu vanotora safinamide kana vachienzanisa nevaya vasingatori (kureva, avo vanotora placebo).

Zvishoma zvinowanzoitika asi zvakanyanya kuipa zvinokuvadza zvinosanganisira zvinotevera:

Heano mamwe mishonga yausingafaniri kutora kana uri kutora safinamide:

Kunyange zvazvo vanhu vane kupererwa kwetsvo kunogona kutora safinamide, avo vane chirwere chakakomba chechiropa havafaniri kutora mishonga.

Pasi Pasi

Safinamide inobatsira zvikuru kune avo vari pakati pekupedzisira-chirwere chePasinson's chirwere chinosangana nekuchinja kwemotokari (kureva, dyskinesia) nekuderera mukubudirira kwemishonga yavo (kureva, OFF times). Safinamide inogona kunge iri nani kuwedzera kurapa kwekutanga kurapwa nevevodopa kune mamwe maitiro ekuwedzera, kusanganisira mamwe MAO-B inhibitors uye COMT inhibitors. Safinamide inogonawo kushandiswa pamwe chete nevevodopa nedzimwe mishonga antiparkinson. Safinamide haishandisi yoga.

Nyaya yakawanda inonyanya kushanda ye safinamide is dyskenesia, kana kuwedzerwa kwemaitiro asingabatsiri. Vanhu vane zvinetso zvakakomba zvechiropa kana avo vanotora zvimwe zvirwere zvinodhaka kana mamwe mishonga havafaniri kutora safinamide.

> Sources:

> Chaplin, S. Safinamide: Kuwedzera kwekurapa kwezvirwere zvePasinson. Prescriber. 2016.

> FDA inobvumira mishonga yekubata zvirwere zve Parkinson. March 21, 2017. www.fda.gov.

> Jenner, P. Kurapa Kwemamwe Matanho Ezvirwere zvePasinsinson - Mafirosiro Epamusoro Parizvino uye munguva Yemberi. Translational Neurodegeneration. 2015; 4: 3.

> Jankovic, J, naAguilar, LG. Nzira Inoenderana Nekurapwa Kwezvirwere zvePasinsinson. Neuropsychiatric Disease uye Treatment. 2008; 4 (4): 743-757.

> Schapira, AH, et al. Kuongororwa kweKuchengetedzwa uye Kubudirira kweSafaamide seLeododopa Yakagadziriswa Muvarwere NeChipinson Zvirwere uye Mafambisi eMotokari A Randomized Clinical Trial. JAMA Neurology. 2017; 74 (2): 216-224.