Ugqirha loPhando olwalwela izifo ze-Parkinson ukususela ekuqaleni
Imithi ebizwa ngokuthi i-dopamine agonists efana ne-Requip (ropinirole) kunye neM Mirapex (pramipexole) isetyenziswa ngokuqhelekileyo ukunyanga iimpawu zesifo sika- Parkinson , ngokukodwa kwizigaba zokuqala.
I-dopamine agonists idla ngokumiselwa ngama-neurologists njengendlela yokwandisa ixesha elithathayo ngaphambi kokuba umntu aqale (okanye ukwandisa) umthamo wabo we- levodopa .
I-Levodopa yimizi ephumelelayo yeParkinson, kodwa ukuphumelela kwayo kuyancipha xa umntu esele emilonyeni.
Ukongeza kokungaphantsi kwe-levodopa ekuphatheni iimpawu zeemoto , i-dopamine agonists ayenzi nto yokunciphisa eso sifo.
Ezi zihlaziyi zenze abaphandi bakwazi ukuphuhlisa i-dopamine agonist, ebizwa ngokuba yi-D-512, engabonakali nje ephezulu kunezinye i-dopamine i-agonists ngokwemigaqo yokulawula iimpawu zeemoto kodwa inokukhusela iisensi zeentsholongwane ezikhoyo, ezinokubeka iibhuleki kwisifo somntu (ephawulekayo feat).
Kubalulekile ukuqonda ukuba i-D-512 iphakathi kwezigaba zokuqala zophando. Enyanisweni, ifundwa kuphela kwizilwanyana. Sekunjalo, kuyisinyathelo esihle sokuqala ekufumaneni iyeza elilwa nesifo se-Parkinson ukususela ekuqaleni.
Ubume be-D-512
Isifo sika-Parkinson siquka ukulahlekelwa kwee-cell ze-dervamine zeselence kwingingqi yengqondo ebizwa ngokuba yi-substantia nigra.
Ekubeni i-dopamine yikhemikhali yengqondo (ebizwa ngokuba yi-neurotransmitter) efunekayo ukuze umzimba uphume, impawu (ezinxulumene nokuhamba) zivela kule lahleko.
Nangona kukho impawu zeemoto ezihambelana nesifo sikaParkinson, ezine ezikhawulezileyo zi:
- Ukuphumla
- I-Bradykinesia (ukunciphisa amandla okuhambisa)
- Ubunzima
- Ukungazinzi kwesithuba
Njenge-dopamine agonist, i-D-512 ibophelela kwi-dopamine receptors, okanye iisayithi zokungena, kwingqondo. Ngokukhupha ngokukhawuleza la ma-receptors, u-D-512 ulinganisa i-brain dopamine yengqondo (ngoko ingqondo icinga ukuba i-dopamine xa ingenayo).
I-D-512 ihluke kwezinye i-dopamine agonists, nangona kunjalo, kuba inxulumene ne-dopamine receptors. Oku kuthetha ukuba iyakwazi ukubopha ngokulula kunye nokuqina ngakumbi, okwenza ihlale ide.
Ukongezelela ekubeni nobudlelwane obunzulu be-dopamine receptors, i-D-512 ikholelwa ukuba ikhusela i-cell-producing-cell cells ezisekhona, mhlawumbi ngokunciphisa uxinzelelo lwe-oxidative (into ebalulekileyo "ukuba kutheni" emva kwesifo sika-Parkinson). Ngokunciphisa uxinzelelo lwe-oxidative, i-D-512 iya kuthathwa njengento ene-antioxidant.
Ngamanye amazwi, abaphandi bakholelwa ukuba i-D-512 ingaba yonyango lokuguqula isifo se-Parkinson ngenxa yokuba inganciphisa intuthuko yayo.
I-Science emva kwe-D-512: IsiFundo sezilwanyana
Kwisifundo esithile kwiBritish Journal ye-Pharmacology, ubuchopho beenkozi befakwe kwi-6-hydroxydopamine (i-dopamine neurotoxin ukulingisa isifo se-Parkinson kubantu). Emva koko, iiphunga zanikwa i-D-512 okanye zixhoba (ropinirole), kwaye imiphumo yafaniswa.
Iziphumo
Iziphumo zophando zityhila ubuchopho obuphezulu kunye negazi le-D-512 kune-ropinirole.
Ngaphezu koko, ngelixa ii-D-512 kunye ne-ropinirole zanda ukunyakaza ngokuzenzekelayo (kwiiriti) ukuya kwisidanga esifanayo emva kokujova, ixesha lokusebenza kweemoto lide lide kwi-D-512 kune-ropinirole.
Ngokukodwa, i-anti-Parkinsonian impembelelo ye-ropinirole yahlala kuphela malunga neeyure ezimbini ngelixa i-anti-Parkinsonian effect ye-D-512 yahlala ubuncinane kwieyure ezine.
Impembelelo ecaleni: iDyskinesia
I-D-512 yaqatshelwa ukuba ibangele i-dyskinesia, kodwa ibe yomelele njengokuba ixhoba (ropinirole), kwiiliti. I-Dyskinesia ibhekisela kwiminyango engaqhelekanga njengobungqingili okanye ukuxubha okungekho kolawulo lomntu.
Kubalulekile ukuba uqaphele ukuba ngelixa i-dyskinesias yinto echaphazelekayo yecala levodopa, eyenzeka kuma-50 ekhulwini abantu abanesifo sika-Parkinson kwiminyaka emihlanu, abaxhomekekanga kubantu abathwala i-dopamine agonists.
Enyanisweni, uphando lubonisa ukuba i-dyskinesias, xa umntu ethatha i-dopamine i-agonists yodwa, ivela kuma-5 ukuya kuma-7 ekhulwini abantu abano-Parkinson-kwaye ukuba i-dyskinesias iyenzeka, ngokuqhelekileyo ikhuselekileyo kwaye iyenzeka kamva.
Okukwintsusa
Kukho konke, i-dyskinesias ayiyinkxala enkulu kubantu abenza i-dopamine agonists yedwa (ngaphandle kwe-levodopa), ngoko kusekho ukuphucula umgangatho wempembelelo yokuthatha i-D-512, xa kuthelekiswa namanye ama-agonist njenge-Requip (ropinirole) .
Khumbula, oku kufundwa kwezilwanyana, ngoko kusenjenje kakhulu ukuba wenze izigqibo. Umgca apha apha kukuba imiphumo ye-D-512 kufuneka iguqulelwe ekusebenziseni abantu.
I-Dopamine Agonists kunye Nendima Yabo KwiiMpawu ezingezizo
Ukongezelela ukunyanga iimpawu zeemoto kwisifo se-Parkinson kwisigaba sokuqala, ubungqina besayensi bubonisa ukuba i-dopamine i-agonist inceda iimpawu ezingekho iimoto, ingakumbi iingxaki zengqondo ezifana nokuxhalaba, ukuxinezeleka, kunye / okanye ukunganakwa.
I-dopamine i-agonists inokuphucula iingxaki ezithile ezizimeleyo ezifana nomsebenzi wesondo okanye ukukhupha, kunye neengxaki ezithile zokulala kwisifo sika-Parkinson njengesihlungu somlenze ongenasiphelo okanye ukuhlukana kokulala.
Oku ku thembisa, njengoko iingcali zijolise ngakumbi nangaphezulu kwiimpawu ezingezizo iimoto, njengoko zihlala ziqala ngaphaya kweempawu zeemoto kwaye ziyakunciphisa.
Oko kwathiwa, akucaci ukuba ingaba i-D-512 yayiza kuphakama kwi-dopamine i-agonists njenge-Requip (ropinirole) okanye iM Mirapex (pramipexole) ekunciphiseni le miqondiso engeyiyo imoto.
ILizwi
Kwisifundo sezilwanyana esicacisiwe, inzuzo enkulu ye-D-512 ngaphezu kweSixhoba (ropinirole) kukuba ihlala ixesha elide kwaye ingcono kwimpembelelo yayo.
Sekunjalo, uphando olongezelelweyo lufunekayo ukuqonda kangcono ukuba i-compound efana ne-D-512 ingcono kunokuba i- dopamine i-agonists yangoku ilapha abantu abane-Parkinson.
Ngaphandle kweempawu zeemoto kunye nemiphumo emibi, ezinye izinto kufuneka zibhekwe njengomgangatho wobomi bomntu, ixesha lihlehliselwe ukuqala i-levodopa, nokuba ingaba i-D-512 ishintsho-isifo (ingaba ikhusele i-cell anti-producing cells philayo).
> Imithombo:
> Batla A, Stamelou M, Mencacci N, Schapira AH, Bhatia KP. I-Ropinirole monotherapy yenza ukuba i-dyskinesias iguquke kakhulu kwi-disease ye-Parkinson. Disv Disord . 2013 Jul; 28 (8): 1159-60.
> Lindenbach D, Das B, Conti MM, Iimfuno ze-SM, iDutta AK, uBhishophu C. D-512, i-dopamine ye-dopamine ye-D2 / 3 ye-agonist ye-receptor, ibonisa ukusebenza kwe-greate anti-Parkinsonian ukuphumelela kune-ropinirole kuma-ratsinsonian rats. Br J Pharmacol. 2017 Sep; 174 (18): 3058-71.
> Poewe W et al. I-pramipexo enwetshiwe kwipilisi yaseParkinson yokuqala: isilingo esingama-33 esesigxina. Neurology. 2011 uAgasti 23; 77 (8): 759-66.
> UMichael J. Fox Foundation UkuPhando kweParkinson. D-512: iNveli, i-Multifunctional D2 / D3 I-Agonist ye-Receiver yokuPhathwa kwezifo ze-Parkinson.
> Schaeffer E, Berg D. I-Dopaminergic therapies yeempawu ezingekho imoto kwisifo sikaParkinson. CNS Iziyobisi . 2017 Julayi; 31 (7): 551-70.