Mankhwala Osokoneza Bongo Amene Amalimbana ndi Matenda a Parkinson Kuyambira pachiyambi
Mankhwala otchedwa dopamine agonists monga Requip (ropinirole) ndi Mirapex (pramipexole) amagwiritsidwa ntchito kwambiri pochiza zizindikiro za matenda a Parkinson , makamaka m'mayambiriro oyambirira.
Dopamine agonists nthawi zambiri amalembedwa ndi akatswiri a sayansi ya ubongo monga njira yowonjezera nthawi yomwe munthu amayamba asanayambe (kapena kuwonjezera) mlingo wawo wa levodopa .
Levodopa ndi mankhwala othandiza kwambiri kwa Parkinson, koma mphamvu yake imachepetsanso munthu ali pa mankhwala.
Kuwonjezera pa kukhala wocheperapo ndi levodopa pochiza zizindikiro zamagalimoto , dopamine agonists sachita kanthu kuti achepetse matendawa.
Zovutazi zachititsa akatswiri kuti apange dopamine agonist, yotchedwa D-512, yomwe imangowoneka yopambana kuposa ena omwe amagwiritsa ntchito njira zotha kuyendetsa njinga zamagetsi koma ikhoza kuteteza maselo a mitsempha omwe alipo, omwe akhoza kuika ma breki pa matenda a munthu (chodabwitsa feat).
Ndikofunika kumvetsetsa kuti D-512 ali m'zaka zoyambirira zafukufuku. Ndipotu, zangophunziridwa zinyama. Komabe, ndi sitepe yoyamba yopeza mankhwala omwe amagonjetsa matenda a Parkinson kuyambira pachiyambi.
Chidule cha D-512
Matenda a Parkinson amatanthauza kuwonongeka kwa maselo a mitsempha ya dopamine m'dera la ubongo lotchedwa substantia nigra.
Popeza dopamine ndi mankhwala a ubongo (omwe amatchedwa neurotransmitter) omwe amafunikira kuti thupi lisunthike, zizindikiro zamagalimoto zimachokera ku imfa.
Ngakhale pali zizindikiro zambiri zamagalimoto zomwe zimagwirizana ndi matenda a Parkinson, makhadi anayi ndi awa:
- Kudzitukumula
- Bradykinesia (kuchepa kukhoza kusuntha)
- Kulemera
- Kusasintha kwa positi
Monga dopamine agonist, D-512 imamangiriza ku dopamine receptors, kapena malo otsekemera, mu ubongo. Pogwiritsa ntchito mofulumira izi, D-512 imatsanzira ubongo wa dopamine (kotero ubongo umaganiza kuti uli ndi dopamine pomwe siili).
D-512 ndi yosiyana ndi ena a dopamine agonists, ngakhale, chifukwa ali ndi mgwirizano wapamwamba wa dopamine receptors. Izi zikutanthauza kuti zikhoza kumangika mosavuta komanso molimba kwambiri, zomwe zimapangitsa kuti zikhale zotalika.
Kuwonjezera pa kukhala ndi chiyanjano chokwanira cha dopamine receptors, D-512 amakhulupirira kuti amateteza maselo a mitsempha ya dopamine omwe akadali amoyo, mwachidziwikire pochepetsa kuchepetsa nkhawa ya mchere (chinthu chofunikira ku "chifukwa chake" kumbuyo kwa matenda a Parkinson). Pochepetsa nkhawa ya okosijeni, D-512 idzaonedwa kuti ili ndi antioxidant.
M'mawu ena, ochita kafukufuku amakhulupirira kuti D-512 ikhoza kukhala chithandizo chosinthira matenda a Parkinson chifukwa chakuti chikhoza kuchepetsa kukula kwake.
Sayansi Pambuyo pa D-512: Phunziro la Zinyama
Mu kafukufuku wina ku British Journal of Pharmacology, ubongo wa makoswe unaphatikizidwa ndi 6-hydroxydopamine (dopamine neurotoxin kuti atsatire matenda a Parkinson mwa anthu). Kenaka, makoswe anapatsidwa D-512 kapena Wothandizira (ropinirole), ndipo zotsatirazo zinafanizidwa.
Zotsatira
Zotsatira zophunzirira zinawulula ubongo wapamwamba ndi D-512 mwazi kuposa ropinirole.
Komanso, pamene D-512 ndi ropinirole zowonjezera kayendetsedwe kake (mu makoswe) ku digiri imodzimodziyo pambuyo pa jekeseni, nthawi ya kuyendetsa galimoto inali yaitali kwa D-512 kuposa ropinirole.
Zowonjezereka, zotsatira zotsutsana ndi Parkinsoni za ropinirole zinatha pafupifupi maola awiri pamene mphamvu ya anti-Parkinsonian ya D-512 inatha kwa maola anayi.
Zotsatira zoyipa: Dyskinesia
D-512 inkawoneka kuti imayambitsa dyskinesia, koma molimbika mofanana monga Requip (ropinirole), mu makoswe. Dyskinesia imatanthawuza kusuntha kosazolowereka monga kukongolera kapena kusokoneza komwe sikuchokera kwa munthu.
Ndikofunika kuzindikira kuti ngakhale dyskinesias ndi zotsatira zofala za levodopa, zikupezeka pafupifupi 50 peresenti ya anthu omwe ali ndi matenda a Parkinson pazaka zisanu, ndizochepa kwambiri mwa anthu omwe amatenga agopistine a dopamine.
Ndipotu, kafukufuku amasonyeza kuti dyskinesias, pamene munthu akutenga dopamine agonists yekha, amapezeka pafupifupi 5 mpaka 7 peresenti ya anthu omwe ali ndi Parkinson-ndipo ngati dyskinesias imachitika, nthawi zambiri zimakhala zovuta kwambiri ndipo zimachitika mtsogolo.
Pansi
Zonsezi, dyskinesias si vuto lalikulu mwa anthu omwe amatenga dopamine agonists okha (popanda levodopa), kotero kuti akadakalipo phindu lopindulitsa kwambiri la kutenga D-512, poyerekeza ndi ena a agonist a dopamine monga Requip (ropinirole) .
Kumbukirani, izi ndi phunziro la nyama, choncho ndi mofulumira kwambiri kuti tipeze ziganizo. Mfundo yaikulu apa ndi yakuti zotsatira za D-512 ziyenera kumasuliridwa kuti zigwiritsidwe ntchito kwa anthu.
Agulu a Dopamine ndi Udindo Wawo M'zizindikiro Zosakhala Zogwiritsira Ntchito
Kuphatikizapo kuchiza matenda amtundu wa matenda a Parkinson, umboni wa sayansi umasonyeza kuti dopamine agonists amapindula popanda zizindikiro, makamaka mavuto a maganizo monga nkhawa, kuvutika maganizo, ndi / kapena kusowa chidwi.
Dopamine agonists angathandizenso mavuto ena monga kugonana kapena thukuta, komanso mavuto ena ogona mu matenda a Parkinson ngati matenda osagwira ntchito kapena kugona kwagona.
Izi zikulonjeza, monga akatswiri akuyang'ana mochulukira pa zizindikiro zosagwirizana ndi magalimoto, chifukwa nthawi zambiri zimayambira kale kuposa zizindikiro zamagalimoto ndipo zingawonongeke.
Izi zanenedwa, sizikudziwikiratu kuti D-512 idzakhala yabwino kuposa zida zowononga dopamine monga Requip (ropinirole) kapena Mirapex (pramipexole) pochepetsa zizindikiro zosadziwika.
Mawu Ochokera
Mu phunziro la zinyama tatchulidwa, kupindula kwakukulu kwa D-512 pamwamba pa Kukonzekera (ropinirole) ndiko kuti kumatenga nthawi yaitali komanso kuli bwino pa zotsatira zake zapamwamba.
Komabe, maphunziro ochuluka amafunikira kuti amvetsetse bwino ngati makina ngati D-512 ndi abwino kwambiri kusiyana ndi agopistine a dopamine masiku ano ochiza anthu ndi Parkinson.
Kuwonjezera pa zizindikiro zamagalimoto ndi zotsatira zake, zifukwa zina zimayenera kuganiziridwa ngati moyo wa munthu, nthawi yotsatiridwa kuti ayambe levodopa, ndipo ngati D-512 alidi kusintha matenda (akhoza kuteteza maselo a mitsempha ya dopamine omwe akadalibe kukhala moyo).
> Zotsatira:
> Fufuzani A, Stamelou M, Mencacci N, Schapira AH, Bhatia KP. Ropinirole monotherapy inachititsa kuti dyskinesias adwale kwambiri m'thupi la Parkinson. Mov Disord . 2013 Jul; 28 (8): 1159-60.
> Lindenbach D, D B B, Conti MM, Mayi SM, Dutta AK, Bishopu C. D-512, buku la dopamine D2 / 3 receptor agonist, limasonyeza mphamvu yowonongeka ya Parkinsonian kuposa ropinirole mu makoswe a Parkinsonian. Br J Pharmacol. 2017 Sep; 174 (18): 3058-71.
> Poewe W et al. Kuchulukitsa-kutulutsidwa kwapakati pa matenda a Parkinson: kuyesedwa kwa masabata makumi atatu ndi atatu. Neurology. 2011 Aug 23; 77 (8): 759-66.
> Michael J. Fox Foundation Kufufuza kwa Parkinson. D-512: Novel, Multifunctional D2 / D3 Mlandira Agonist kwa Chithandizo cha Matenda a Parkinson.
> Schaeffer E, Berg D. Dopaminergic njira zothandizira kuti zisakhale zamoto zizindikiro za Parkinson. CNS Mankhwala Osokoneza Bongo . 2017 Jul; 31 (7): 551-70.