Safinamide: Mankhwala Oyamba a Anti-Parkinson M'zaka 10

Chithandizo chingathandize omwe ali ndi matenda a Parkinson

Mu March 2017, a FDA adavomereza safinamide (Xadago) kuti agwiritse ntchito kuchipatala ku United States. Safinamide ndi mankhwala atsopano ovomerezedwa ndi FDA kuti athetse matenda a Parkinson m'zaka zoposa 10. Ndilo njira yowonjezereka, kapena kuwonjezera-mankhwala, yogwiritsidwa ntchito limodzi ndi levodopa.

Matenda a Parkinson afotokozedwa

Matenda a Parkinson ndi matenda osokoneza bongo omwe amayamba pang'onopang'ono ndipo amayamba pomwe ali ndi zaka 60.

Zizindikilo zimaphatikizapo kunjenjemera, kuuma, kufooketsa kayendetsedwe ka kayendetsedwe kake, ndi kuchepetsa ndalama. Matendawa pamapeto pake amachititsa mavuto poyenda, kuyankhula, ndi zinthu zina zomwe zimachitika tsiku ndi tsiku. Ku United States, anthu pafupifupi 50,000 amapezeka ndi matenda a Parkinson chaka chilichonse.

Ngakhale palibe chithandizo cha matenda a Parkinson, pali mankhwala omwe amathandizira ndi kasamalidwe ka zizindikiro, kuphatikizapo zotsatirazi:

Mwamwayi, palibe mankhwala omwe amalepetsa kapena kuchepetsa kupitirira kwa matenda a Parkinson.

Leviodopa ndi mankhwala opambana kwambiri komanso otchuka omwe amagwiritsidwa ntchito pochiza matenda a Parkinson; Komabe, zotsatira zake zimafooka pakapita nthawi ndipo zingayambitse zotsatira zoipa monga dyskinesia .

Mankhwala osokoneza bongo, kuphatikizapo COMT inhibitors, agonist a dopamine, ndi mankhwala omwe sali a dopaminergic, monga mankhwala oteteza anticholinergic ndi amantadine, angagwiritsidwe ntchito ngati njira zina za levodopa, kuwonjezera pa levodopa, kapena kuphatikiza wina ndi mnzake.

Kwa anthu omwe ali ndi matenda a Parkinson apamwamba, pamene mankhwala amalephera, ubongo wa ubongo (ubongo wa ubongo) ukhoza kuganiziridwa kuti uthandizire kuchepetsa zizindikiro.

Kawirikawiri, mankhwala amawasungira anthu omwe zizindikiro zawo zakhala zovuta kwambiri kuti zisokoneze ntchito za tsiku ndi tsiku. Levodoopa kawirikawiri ndi mankhwala osankhidwa omwe ali ndi zaka 65 kapena kuposerapo omwe moyo wawo umasokonezeka kwambiri. Anthu osakwana 65 angathe kuchiritsidwa ndi dopamine agonist.

Mankhwala amayamba pa mlingo wotsika kwambiri ndipo mankhwala amachedwa kuchedwa mwamsanga. Komabe, kafukufuku wothandizira pulogalamu yotsogolera ya "kuyamba pansi ndi kupita pang'onopang'ono" ndi mlingo wa levodopa ndi wosakaniza. Malinga ndi wolemba Peter Jenner:

Kuyamba kwa L-Dopa [levodopa] kwa omwe ali ndi nthawi yayitali kapena kupitirira kwa mlingo waukulu kungapangitse nthawi yofupikitsa yopindulitsa musanayambe kuwopsa kwa magalimoto. Posachedwapa, kusunga mlingo wa L-dopa pansi pa 400 mg pa tsiku kumayambiriro kwa PD kunayesedwa kuchepetsa chiopsezo chotenga dyskinesia.

Komabe, Jenner akupitiriza kuona zotsatirazi:

Kugwiritsiridwa ntchito kwa L-dopa kunayanjananso kuti ndi njira yabwino kwambiri yothandizira magalimoto komanso kuti asakhudze chiopsezo cha nthawi yayitali ya dyskinesia.

Zoonadi, umboni wotsimikiziransowu ukutsindika zochepa zomwe timadziwa zokhudza matenda ndi chithandizo cha matenda a Parkinson.

Safinamide: Zimagwira Ntchito Motani?

Kwa anthu omwe ali ndi matenda a Parkinson, ubongo subala mankhwala okwanira otchedwa dopamine .

Maselo omwe amabweretsa dopamine amafa kapena amalephera. Dopamine ndi yofunika kuti yoyendetsa galimoto yoyenera ndi kuyenda.

Makamaka, dopamine imatumiza zizindikiro mu ubongo zomwe zimakhudzidwa ndi kayendetsedwe kosavuta, kopindulitsa monga kudya, kulemba, ndi kuyimba. Monga selegeline ndi rasagaline, safinamide ndi mtundu wa MAO-B inhibitor, umene umalepheretsa kuwonongeka kwa dopamine ndipo motero umachulukitsa zigawo zake mu ubongo.

Zindikirani, safinamide imatsanso kumasulidwa kwa glutamate; Komabe, zotsatira zenizeni zachitachi pazochiritsira za mankhwala sizidziwika.

Mosiyana ndi zina zotetezedwa ndi MAO-B, zomwe zingapangidwe zokha kwa anthu omwe ali ndi matenda a Parkinson oyambirira, safinamide imagwiritsidwa ntchito pothandizana ndi mitundu ina ya mankhwala ophera antiparkinson kwa matenda otha msinkhu, makamaka a levodopa komanso agonist a dopamine.

Pamene anthu ayamba kulandira chithandizo cha zizindikiro za Parkinson, mankhwala amagwiritsidwa ntchito bwino ndipo zizindikiro zimayendetsedwa tsiku lonse. Komabe, pakati pa zaka zisanu ndi zisanu, mankhwala a Parkinson omwe amagwiritsidwa ntchito masiku ano amatha kuyenda mwa anthu ambiri, ndipo kumakhala kovuta kwambiri kuchepetsa vutoli.

Mwachindunji, mwa anthu omwe ali ndi nthawi yochedwa Parkinson, matenda osokoneza bongo kapena kutuluka kwa minofu (dyskinesia ndi kuzizira ) amayamba kulima.

Dyskinesia imatchulidwa kwambiri mwa anthu omwe amatenga levodopa ndipo ndi zotsatira zowawa za mankhwala osokoneza bongo. Mawonetseredwe a dyskinesia bodes mosavuta potsata malingaliro ndipo ayenera makamaka kuchedwa malinga ndi momwe mungathere. Kuwonjezera pamenepo, zizindikiro zosagwirizana ndi matenda, monga dementia , depression, ndi malingaliro, omwe amakhudzidwa pang'ono ndi mankhwala ophera dopaminergic, amakhalanso vuto.

Odwala omwe amadwala chithandizo chokwanira chomwe chakhalapo kwa nthawi yayitali ndi ovuta kuchichitira mofananamo kuti azikhala ndi moyo wabwino.

Mwa kuyankhula kwina, kamodzi ka levodopa imaleka kugwira ntchito, mbali imodzi chifukwa sitingamvetsetse vutoli, zimakhala zovuta kuti anthu abwerere ku malo otsogolera omwe ali ndi matenda omwe ali ndi matendawa pamene levodopa ndi ena a dopaminergic anali kugwira ntchito.

Komanso, ngakhale ngati mavuto akugwedezeka, osagwiritsa ntchito magalimoto monga matenda a maganizo, matenda ogona, ndi matenda a 'dementia' amakhala ovuta kwa omwe ali ndi matenda a Parkinson.

Mwamwayi, sitingadziwe kuti ndi anthu ati omwe ali ndi matendawa a Parkinson omwe adzasinthasintha. Kwachilendo, matenda, nthawi ya matenda, kutalika kwa mankhwala ndi levodopa, levodopa mlingo, chiwerewere, ndi kulemera kwa thupi onse amakhulupirira kuti zimathandiza pafupipafupi.

PA ndi Times Times

"PAMENE nthawi" imatanthauza nthawi imene mankhwala akugwira ntchito bwino ndipo zizindikiro za matenda a Parkinson zimayendetsedwa.

"Nthawi" imatanthauza nthawi imene mankhwala amatha ndipo zizindikiro za Parkinson, monga mantha, kugwedezeka, ndi kuyenda movutikira zimabweranso.

Kuwonjezera kwa safinamide kumayendedwe a mankhwala a anthu omwe ali ndi matenda a Parkinson opambana omwe amachititsa levodopa amachulukitsa kuchuluka kwa ON nthawi ndipo amachepetsa nthawi.

Safinamide Clinical Trials

Zotsatira zochokera ku mayesero awiri a chipatala zakhala zikuwonetsa phindu la ntchito ya safinamide pakati pa anthu okhala ndi matenda a Parkinson apamwamba kwambiri. Ophunzirawa adapezeka kuti ali ndi matenda a Parkinson zaka zitatu kapena zisanu.

Chiyeso choyambitsa chipatala chinayambitsa anthu 669 omwe ali ndi kusintha kwa magalimoto. Ophunzirawa analandira safinamide kuphatikizapo mankhwala ena oletsa antiparkinson kapena placebo (palibe safinamide) ndi mankhwala ena oletsa antiparkinson.

Avereji pa nthawi ya ophunzira anali pakati pa maola 9.3 ndi 9.5. Pambuyo pa miyezi isanu ndi umodzi yoyezetsa, nthawi zina zowonjezera m'magulu onse odwala; Komabe, nthawi zina zinkakhala pafupi ndi mphindi makumi atatu zomwe zimatenga safinamide.

Pambuyo pa zaka ziwiri zachipatala, pafupifupi nthawi YAM'MBUYO YOTSATIRA TUMIZANI LINKI SINDIKIZANI ILI MU KOPERANI MAPODIKASITI MITU YA NKHANI Choncho patapita zaka ziwiri, anthu omwe amatenga safinamide pamodzi ndi levodopa komanso mankhwala ena a antiparkinson amatha kukhala ndi ora limodzi la mankhwala ochiritsira matenda a Parkinson.

Zindikirani, safinamide yachepetsedwa nthawi YONSE pafupi maminiti 35. Kumbukirani kuti nthawi zina zimatchulidwa nthawi yomwe mankhwala osokoneza bongo amatha, ndipo zizindikiro monga mantha zimayambanso kuwonjezereka.

Kuonjezera kuonjezereka pa nthawi ndi kuchepetsa nthawi, safinamide imathandizanso kuyenda (magalimoto) mwa iwo omwe amatenga. Kuwonjezera pa mlingo wapamwamba, safinamide inathandizanso ndi ntchito za tsiku ndi tsiku komanso moyo wabwino.

Mofananamo zotsatira za mayesero achiwiri, omwe anaphatikizidwa ndi ophunzira 549, akuwonetsa kuwonjezeka kwa nthawi ndi ola limodzi mwa iwo omwe amatenga safinamide poyerekeza ndi omwe amatenga placebo komanso kuchepetsa nthawi. Kuonjezerapo, kusintha kwa ntchito ndi khalidwe la moyo wambiri kunawonanso.

Safinamide Zotsatira Zolakwika Zowonongeka

Chifukwa cha zotsatira zovulaza, 3.7 peresenti ya ophunzira omwe amatenga safinamide amachotsedwa m'mayesero a zachipatala poyerekezera ndi 2.4 peresenti ya iwo omwe amawatenga malo.

Zotsatira zovuta zomwe zimachitika panthawi ya mayesero awa ndi awa:

Pa zizindikirozi, dyskinesia inali pafupifupi kawiri kawirikawiri mwa anthu omwe amatenga safinamide poyerekeza ndi omwe sanatenge (mwachitsanzo, omwe amatenga placebo).

Zovuta zofala koma zovuta kwambiri ndizo zotsatirazi:

Nazi mankhwala ena omwe simuyenera kutenga ngati mutenga safinamide:

Ngakhale anthu omwe ali ndi vuto la impso akhoza kutenga safinamide, omwe ali ndi vuto lalikulu la chiwindi sayenera kumwa mankhwala.

Pansi

Safinamide imathandiza kwambiri kwa anthu omwe ali ndi zaka zochedwa Parkinson matenda omwe amatha kusintha kusintha kwa magalimoto (ie, dyskinesia) komanso kuchepa kwa mankhwala awo (ie, OFF nthawi). Safinamide ingakhale njira yowonjezera yowonjezereka kuchipatala chachikulu ndi levodopa kuposa mankhwala ena owonjezera, kuphatikizapo mazira ena a MAO-B komanso COMT inhibitors. Safinamide ingagwiritsidwe ntchito pothandizana ndi levodopa ndi mankhwala ena a antiparkinson. Safinamide sagwiritsidwa ntchito yokha.

Zotsatira zovuta kwambiri za safinamide ndi dyskenesia, kapena kuwonjezeka kwa kayendetsedwe ka zosayenera. Anthu omwe ali ndi vuto lalikulu la chiwindi kapena omwe amadwala matenda enaake kapena mankhwala ena sayenera kutenga safinamide.

> Zotsatira:

> Chaplin, S. Safinamide: Mankhwala Owonjezera pa Matenda a Parkinson. Wolemba. 2016.

> FDA ikuvomereza mankhwala osokoneza bongo kuti athetse matenda a Parkinson. March 21, 2017. www.fda.gov.

> Jenner, P. Chithandizo cha Zotsatira Zake za Matenda a Parkinson - Njira Zamakono Zamakono Padzikoli komanso M'tsogolo. Kutembenuzidwa Kwasinthidwe kwa Neurodegeneration. 2015; 4: 3.

> Jankovic, J, ndi Aguilar, LG. Njira Zomwe Akuchiritsira Matenda a Parkinson. Matenda a Neuropsychiatric ndi Chithandizo. 2008; 4 (4): 743-757.

> Schapira, AH, et al. Kufufuza za chitetezo ndi kuchitidwa bwino kwa Safinamide monga Levodopa Yophatikiza Pakati pa Odwala Ndi Matenda a Parkinson ndi Zofooketsa Zamagalimoto Zomwe Zilipo Pachiyambi. JAMA Neurology. 2017; 74 (2): 216-224.