
gabapentinoid

gabapentinoids, jyanna α2δ legands mhanoon dekhil olakhale jaate, heey aushadhancha eka varg aahe jeey avarodhak neurotransmitter gamma-eminobuteric acid (gaba) (i.eae., gaba analogue) jeey α2δ up-ekak asalelya voltage-aadharit calcium vahinyanna (vhee. dii. see. see.) avarodhit karatat. yaa thikanala 'gabapentin receptor' (α2δ subunit) mhanoon sambodhale gele aahe, kaaran teey gabapentin aanee pregabalin yaa aushadhanche lakshya aahe.
vaidyakiyadrushtya vaparlya jaanarya gabapentinoidsmadhye gabapentin, pregabellin aanee mirogabellin, tasech gabapentin prodrug, gabapentin enacarbil yancha samavesh hoto. yavyatirikt, feniboot gabab receptor agonist mhanoon karya karnyachya tyachya krutivyatirikt gabapentinoid mhanoon karya karate asey aadhalun aale aahe. imagabalinsarkhe aanakhi pratirup chikitsalayin chachanyanmadhye aahet parantu adyap manjur jhalele naheet. vaidnyanik sanshodhanat vaparale jaanare parantu vaidyakeey vaparasathi manjur naan kelele itar gabapentinoids mhanje atagabalin, 4-methylpregabaline aanee pii. dii.-217,014.
vaidyakeey vapar.
apasmaracha aajaar, postherpetic neuralgia, madhumehachya neuropathyshy sambandhit neuropathic vedna, fibromyalgia, samanyikrut chinta vikar aanee aswasth paay syndromechya upcharansathi gabapentinoidsla manyata denyat aalee aahe. gabapentinoidschya kahee label-nasalelya vaparanmadhye nidranash, ardhashishi, samajik bheeti, panic disorder, unmad, dvidhruvi vikar aanee daroo kadhoon ghenyachya upcharancha samavesh hoto. pathichya khalchya tivra vedanet gabapentinoidschya vaparavar vidyaman purave maryadit aahet aanee konatyahi darshavilelya fayadhyashivay pratikool parinamancha lakshaniy dhoka darshavtat. mukhya dushparinamadhye khaleel goshtincha samavesh hotoh zope aanee thakwa jaanavane, raktadab qamee hone, malmal, ulatya hone aanee glucomatus visual hallucination.
aushadhashastra.
pharmacodynamics.
gabapentinoids heey vishisht prakarchya sahayyak α2δ upghatak sthalavaril legands aahet aanee tyadvare α2δ upghatak-yukt vhee. dii. see. ess. chey avarodhak mhanoon karya karatat. done aushadh-bandhankari α2δ upghatak aahet, α2δ-1 aanee α2δ-2, aanee gabapentinoids yaa done sthalansathi samaan aatmiyata darshavtat (aanee mhanunach tyanchyamadhye nivadaktecha abhav aahe). gabapentinoids heey α2δ vdCC upghatkala bandhanyasathi nivadak asatat. tathapi, feniboot advitiyapane qamee aakarshan asalelya (eka abhyasat ~ 5-teey 10 putt) gabab receptorshee dekhil bandhale jaate aanee eka agonist mhanoon karya karate. gabapentinoids heey gaba analogue asale taree, gabapentin aanee pregabalin heey gaba receptors bandhale jaat naheet, 'inn vivo' madhye gaba receptor agonistmadhye rupantarit hott naheet aanee gaba vahtook kinwa chayapachayat badal karat naheet. gabapentin aanee pregabalinchya sambandhit krutinmadhye α2δ-yukt vhee. dii. see. see. chya pratibandhavyatirikt itar konatyahi yantranedvare madhyasthi kelee jaate yacha sadhya konatahi purava nahee. tathapi, gabapentinsarkhe gabapentinoids, parantu pregabalin nahee, heey keey. vhee. voltage-gated potassium channell (keey. see. aine. kyu.) sakriy karatat asey aadhalun aale aahe.
antajanan α-amino aaml-lucine aanee-isolucin, jeey rasayanik sanrachanet gabapentinoids jawalun julatat, teey gabapentin aanee pregabalin (udaa.jee.aay. see. 50 = 71 nm.-isolucinesathi), aanee manvi cerebrospinal dravpadarthat sukshmamolar sandratevar (udaa.jee.,-leucinesathi 12.9 microne,-isolucinsathi 4.8 microne). asey gruhit dharale gele aahe qee teey upaghatakanche antarjanit legands asoo shakatat aanee teey gabapentinoidschya parinamancha spardhatmak virodh karoo shakatat. tyanusar, gabapentin aanee pregabalinmadhye α2δ upaghatkasathi nanomolar sambandh asale taree, tyanchi shakti "inn vivo" qamee sukshmamolar shreneet aahe aanee antarjan-amino esiddware bandhanyasathi spardha hii yaa visangatisathi jababdar asalyache mhatale gele aahe.
eka abhyasat, undaranchya mendut vyakt kelelya α2δ upaghatkasathi gabapentinoidschi aatmiyata (qee) moolye gabapentinsathi 0.05 microne, ("aar")-fenibutsathi 23 microne, ("ess")-fenibutsathi 39 microne aanee backlofensathi 156 microne asalyache aadhalun aale. gabab receptorsathi tyanche sambandh (qee) gabapentinsathi> 1 miimii, ("aar")-fenibutsathi 92 microne, ("ess")-fenibutsathi> 1 miimii aanee backlofensathi 6 microne hote. gababchya sapeksh α2δ upaghatkasathi backlofenchya qamee aatmiyata (26 putt farak) chya aadhare, α2δ upaghatkasathi tyache aatmiyata aushadhashastriy mahatva asanyachi shakyata nahee.
clinical abhyasanmadhye pregabalinane gabapentinpeksha lakshaniyaritya jaast samarthya (sumare 2.5-fold) darshavile aahe.
pharmacokinetics.
shoshan.
gabapentin aanee pregabalin heey mothya tatasth amino acid transporter 1 (latt 1, slc 7aii 5),-lucine aanee-fenilalenin sarkhya amino esidsathiche transporterdware madhyasthi kelelya sakriy vahtook prakriyedvare aatadyanmadhun shoshale jaatat. yaa vahanadvare phaar qamee (10 peksha qamee aushadhe) vahtook kelee jaatat. keval latt1 dware vahoon nenyat yenanya gabapentinchya ulat, pregabalinchi vahtook keval latt1 dwarech navhe tarr itar vahakandvare dekhil kelee jaate asey disate. latt 1 sahajpane santrupt karata yenyajoga aahe, tyamule gabapentinche pharmacokinetics heey qamee jaivupalabdhatesaha aanee uchch matret vilambit shikhar patalisah, matrevar avalambun asatat. yaulat, pregabalinchya babatit asey nahee, jeey resheey pharmacokinetics darshavate aanee shoshan santrupt hott nahee. tyachpramane, gabapentin enacarbilchi vahtook latt 1 dware navhe tarr monocarboxylate vahak 1 (emm. see. tii. 1) aanee soodiyam-aadharit multivitamine vahak (ess. emm. vhee. tii.) dware kelee jaate aanee 2,800 mii. gra. chya matreparyant aushadhasah jaivupalabdhatechi konatihi sampruktata disun aaleli nahee. gabapentin aanee prigabalinpramanech, backlophane, fenibootcha jawalcha analogue (backlophane visheshtah 4-chlorophenibute aahe), latt 1 dware vahoon nela jaato, jaree too vahatukkartyasathi tulanene kamkuvat thurr aahe.
gabapentinchi maukhik jaivupalabdhata andaje 80 takke 100 migra darr aath tasanni teen vela dilee jaate, parantu 300 migra darane 60 takke, 400 migra darane 47 takke, 800 migra darane 34 takke, 1,200 migra darane 33 takke aanee 1,600 migra darane 27 takke qamee hote, heey serve ekach matrechya velapatrakasaha. yaulat, pregabalinchi maukhik jaivupalabdhata tyachya sampoorn vaidyakeey matrechya shrenichya (75 teey 900 mii. gra./divas) palikade 90 takkyanpeksha jaast kinwa samaan aahe. pregabalinchya maukhik jaivupalabdhatevar annacha lakshaniy parinam hott nahee. yaulat, annapadarthanmule gabapentinchya kshetra-antargat-vakr patalimadhye sumare 10 takkyanni vaadh hote. lahan aatadyat gabapentinchya sankraman vel vadhavnari aushadhe tyachi maukhik jaivupalabdhata vadhavu shakatat; jevha gabapentinche maukhik morphenes saha-vyavasthapan kele gele (jeey aatadyansambandhi peristalsisla mandavate), tevha gabapentinchya 600 mii. gra. matrechi maukhik jaivupalabdhata 50 takkyanni vadhali. gabapentin enacarbilchi (gabapentin mhanoon) tondawate jaivupalabdhata 68 takkyanpeksha jaast kinwa samaan aahe, moolyankan kelelya serve matranmadhye (2,800 migraparyant), sarasari 75 takke aahe. itar gabapentinoidschya ulat, fenibootchya pharmacokineticscha farsa abhyas jhalela nahee aanee tyachi maukhik jaivupalabdhata adnyat aahe. tathapi, 250 migratchya ekach matret heey kiman 63 takke asalyache disun yeil, heey aarogyadayi svayamsevakanchya mutratoon fenibutcha haah ansh aparivartitpane punarprapt jhaala yaa vastusthitivar aadharit aahe.
100 migratchya qamee matret gabapentinche tii. emm. aii. ex. (velepasoon shikhar pataliparyant) andaje 1.7 taas asate, tarr jaast matret tii. emm. aii. ess. 3 teey 4 tasanparyant vadhate. pregabalincha tii. emm. aii. ex. samanyatah 300 mii. gra. kinwa tyapeksha qamee matret 1 tasapeksha qamee kinwa samaan asato. tathapi, ann heey pregabalinchya shoshanala lakshaniy vilamb karate aanee aushadhachya jaivupalabdhatevar parinam naan karata sarvoch patali lakshaniyaritya qamee karate asey aadhalun aale aahe; upvas kelelya avasthet 0.6 taas aanee aahar dilelya sthiteet 3.2 tasansathi tii. emm. aii. ex. moolye (5 putt farak), aanee aahar dilelya viruddha upvas kelelya sthiteet see. emm. aii. ex. 25-31% neey qamee hote. pregabalinchya ulat, ann gabapentinchya tii. emm. aii. ex. varr lakshaniy parinam karat nahee aanee gabapentinchya see. emm. aii. ex. madhye andaje 10 takkyanni vaadh karate. gabapentin enacarbilchya (sakriy gabapentin mhanoon) twarit-muktichya (ir) nirmiticha tii. emm. aii. ex. ekach matresah serve matranmadhye (350-2,800 migra) sumare 2.1 teey 2.6 taas aanee serve matranmadhye (350-2,100 migra) 1.6 teey 1.9 taas varanvar dilyabarobar asato. yaulat, gabapentin enacarbilchya vistarit-mukti (ex. aar.) nirmiticha tii. emm. aii. ex. upvas kelelya avasthet 1,200 mii. gra. chya ekach matret sumare 5.1 taas aanee aahar dilelya sthiteet 1,200 mii. gra. chya ekach matret 8.4 taas asato. fenibootcha tii. emm. aii. ex. nondavala gelela nahee, parantu uchch matra (1-3 gramm) ghenanya manoranjak vaparkartyanmadhye tondawate sevan kelyanantar, anukrame 2 teey 4 taas aanee 5 teey 6 tasanni krutichi suruvat aanee shikhar parinam jhalyache varnan kele gele aahe.
vitaran.
gabapentin, pregabalin aanee feniboot heey serve rakt-menducha adthala paar karatat aanee madhyavarti majjasansthet pravesh karatat. tathapi, tyanchya qamee lipophilicitymule, gabapentinoidsla rakt-menduchya adthalyachya palikade sakriy vahatukichi aavashyakta asate. latt 1 heey rakt-menduchya adthalyavar atyant vyakt hote aanee tyachyashi jodalelya gabapentinoidsche mendut parivahan karate. latt1 dware madhyasthi kelelya gabapentinchya aatadyansambandhi shoshanapramane, latt1 dware rakt-menduchya adthalyachya palikade gabapentinchi vahtook santrupt aahe. gabapentin pii-glycoprotein (aii. bii. see. bii. 1) kinwa aukton 2 (ess. ell. see. 22aii. 5) sarkhya itar aushadh vahatukdaranshi bandhale jaat nahee.
gabapentin aanee pregabalin heey lakshaniyaritya plazma prathinanshi (<1%) jodalele naheet. fennyboot analogue backlofenmadhye 30 takkeche qamee plazma prathin bandhan disun yete.
chayapachay.
gabapentin, pregabalin aanee feniboot yaa sarvanmadhye chayapachay qamee kinwa qamee hote. yaulat, gabapentinche utpadan mhanoon kaam karananya gabapentin enacarbilche sakriy honyasathi utsechakeey jalvichhedan hone aavashyak aahe. heey aatadyanmadhil vishisht nasalelya esteresesdware aanee yakrutatil kahee pramanat kele jaate.
nirmulan.
gabapentin, pregabalin aanee feniboot heey serve mutratoon mutrapindadware kadhoon takale jaatat. tyaa sarvanche tulanene qamee kalavadhiche ardhayushya aahe, jyachi nond keleli moolye anukrame 5 teey 7 taas, 6.3 taas aanee 5.3 taas aahet. tyachpramane, gabapentin enacarbil iir (sakriy gabapentin mhanoon) chey antim ardh-ayushya andaje 4.5 teey 6.5 taas qamee asate. gabapentinche nirmulan ardh-ayushya vadhana matransah vadhavale gele aahe; abhyasanchya eka maliket, teey 200 migrassathi 5.4 taas, 400 migrassathi 6.7 taas, 800 migrassathi 7.3 taas, 1,200 migrassathi 9.3 taas aanee 1,400 migrassathi 8.3 taas hote, heey serve ekach matret dile gele. tyachya qamee nirmulan ardh-aayushyamule, upcharatmak patali rakhanyasathi gabapentin darroj 3 teey 4 vela dene aavashyak aahe. tyachpramane, vaidyakeey abhyasanmadhye pregabalin divasatoon 2 teey 3 vela dile gele aahe. feniboot dekhil divasatoon 3 vela ghetale jaate. yaulat, gabapentin enacarbil divasatoon donada aanee gabapentin xr (brand naav grallis) divasatoon ekada ghetale jaate.
rasayanshastra.
gabapentinoids heey gabache 3-paryayi vyutpann aahet; mhanoon, teey gaba analogue tasech γ-amino acid aahet. visheshtah, pregabalin heey ("s")-(+)-3-isobutyl-gaba aahe, fenibut heey 3-fenil-gaba aahe aanee gabapentin heey 3 sthanavar cyclohexen ringsah (kinwa, kahee pramanat ayogya naav, 3-cyclohexyl-gaba) gabache vyutpann aahe. gabapentinoids dekhil α-emino acid-lucine aanee-isolucineshy jawalun julatat aanee tyanchya pharmcodynamicschya sandarbhat tyanchya gabashi sanrachanatmak samanatepeksha heey adhik prasangik asoo shakate.
itihas.
neurantine yaa brand navane gabapentinla meey 1993 madhye united kingadammadhe apasmarachya upcharasathi pratham manyata denyat aalee aanee 1994 madhye americet tyache vipanan karnyat aale. tyanantar, meey 2002 madhye americet postherpetic neuralgiachya upcharasathi gabapentinla manyata denyat aalee. gabapentinchi eka samanya aavrutti 2004 madhye americet pahilyanda upalabdh jhaali. garalise yaa brand navane, gabapentinchya divasatoon ekdachya upcharasathi, gabapentinchya vistarit-prakashan sutrala janewari 2011 madhye united statesmadhye postherpetic neuralgiachya upcharasathi manyata denyat aalee.
pregabalin, lira yaa brand navane, 2004 madhye europemadhye manjur karnyat aale aanee september 2005 madhye americet epilepsy, postherpetic neuralgia aanee madhumehachya neuropathyshy sambandhit neuropathic vedna yaa upcharansathi sadar karnyat aale. tyanantar juuna 2007 madhye united statesmadhye fibromyalgiachya upcharasathi yala manyata denyat aalee. 2005 madhye europemadhye samanyikrut chinta vikaravaril upcharansathi pregabalinla dekhil manyata denyat aalee, jaree united statesmadhye yaa sanketasathi tyala manyata denyat aaleli nahee.
gabapentin enacarbil, horizont yaa brand navane, april 2011 madhye restless legg syndromechya upcharasathi united statesmadhye sadar karnyat aale aanee juuna 2012 madhye postherpetic neuralgiachya upcharasathi manjur karnyat aale. 
anvifen, fenibut aanee noofen yaa brand navankhali vikale jaanare fenibut, 1960 chya dashakat russiamadhye chinta, nidranash aanee itar vividh paristhitinchya upcharansathi sadar karnyat aale. 2015 paryant too gabapentinoid mhanoon kaam karat asalyache aadhalun aale navhate.
lyorisal yaa brandnamkade vikale jaanare backlophane 1977 madhye americet lagoo karnyat aale kaaran rasayanikdrushtya fenibutsarkhech asate parantu samanyatah gabapentinoid manale jaat nahee. janewari 2019 madhye japanmadhye neuropathic vedna aanee postherpetic neuralgiachya upcharasathi tarlige yaa brand navane mirogabalinala manyata denyat aalee.
samaj aanee sanskruti.
manoranjanatmak vapar.
gabapentinoids uchch matret utsah nirman karatat, jyacha parinam gabergic central nervous system depressants sarkhya alcohole, γ-hydroxybuteric acid (jee. etch. bii.) aanee benzodiazepines sarkhya prabhavansah hoto aanee manoranjak aushadhe mhanoon vaparali jaatat (3-20 vela vishisht clinical matra). ekoon durupyogachi kshamata alcohole, benzodiazepines, opioids, cycostimulants aanee itar avaidh aushadhansarkhya itar aushadhanchya tulanet qamee aanee lakshaniyaritya qamee manali jaate. konatyahi paristhitit, tyachya manoranjanatmak kshamatemule, pregabalin haah united statesmadhil anusuchi vhee niyantrit padarth aahe. april 2019 madhye, united kingdamne aushadhancha gairavapar kayada 1971 antargat aanee aushadh niyam 2001 chya gairavaparantargat anusuchi 3 mhanoon gabapentin aanee pregabellin heey shreni see aushadh mhanoon anusuchit kele. tathapi, canada kinwa austreliyamadhye haah niyantrit padarth nahee aanee feniboots itar gabapentinoids dekhil niyantrit padarth naheet. tyamule, teey bahutek kayadeshir madak padarth aahet.
gabapentinoidschi sahishnuta varanvar vaparlyane khoop vegane vikasit hott asalyache nondavale gele aahe, jaree bund jhalyavar dekhil lavkar nasht hote aanee nidranash, malmal, dokedukhi aanee atisar yasarkhi maghar ghenyachi lakshane nondavali gelee aahet. feniboots, tivra punaravartit chinta yasarkhi adhik gambhir maghar lakshane nondavali gelee aahet. gabapentinoidschya jalad sahishnutemule, vaparkarte anekada tyanche doses vadhavtat, tarr itar vaparkarte tyanche doses bajula thevu shakatat aanee sahishnuta talhanyasathi qamee pramanat vaparu shakatat.