Lorcaserin

I-CMOAPI inoluhlu olupheleleyo lwezixhobo eziluhlaza ze-lorcaserin, kwaye inolawulo olupheleleyo lwenkqubo.Also yadlula i-GMP kunye nesiqinisekiso se-DMF.

Ukubonisa 1-3 kweziphumo 6

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Yintoni iLorcaserin?

I-Lorcaserin (i-Belviq) yi-arhente echasene nokukhuluphala. Ukuba ufuna ukushukumisa ubunzima obongezelelekileyo bomzimba ngaphandle kokuxakaniseka malunga nokusebenza okunzima, nantsi into ekufuneka uyiqaphele ngaphambi kokuthenga iyeza le-serotonergic.
ILorcaserin hydrochloride yaphuhliswa yiArena Pharmaceuticals. Kule minyaka idlulileyo, ibisetyenziswa njengonyango lwexesha elide lokutyeba kakhulu. Isongezelelo sithintela ukutya ngokunyusa ukwanelisa. Ngaphandle koko, ukusebenza kakuhle kwe-lorcaserin akufuneki ukuba ulandele ukutya okungqongqo okanye iindlela zokuzilolonga.
Ukusukela oko yaqalwa, ichiza lifumene izilingo ezininzi kunye nezifundo zabantu ukuze kuqinisekiswe ukusebenza kwalo nokunyamezeleka kunyango lokutyeba kakhulu. Kwi-2012, i-FDA yamkele i-lorcaserin (Belviq) yokusetyenziswa konyango kodwa phantsi kwamanyathelo angqongqo. Umzekelo, amayeza kuphela-afunyanwa kubantu abadala abatyebe kakhulu kwaye abatyebe kakhulu ababene-comorbidities ezinxulumene nobunzima ezinje ngoxinzelelo lwegazi, isifo seswekile kunye nedyslipidemia.
Kukho amagama amabini e-lorcaserin, oko kukuthi, iBelviq kunye neBelviq XR. Zombini ziphantse zafana, ukuba ne-lorcaserin hydrochloride njengesithako esisebenzayo.
Iifomsile zeBelviq zincinci kancinci, kwaye uluhlu lwethamo lohlulwa kubini ngemini. Ngokuchasene ne-Belviq XR njengezingxobo zikhulu ngokuthe kratya. Le brand brand yelorcaserin ineepilisi zokukhupha ezandisiweyo eziza kuthathwa kanye ngemini.


I-Lorcaserin kunye neLorcaserin abaPhakathi

Uhlanga lweChlorocaserin Hydrochloride

Eli qela lidla ngokubizwa ngokuba yi-lorcaserin hydrochloride. Nangona kunjalo, igama layo lenzululwazi yi-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine Hydrochloride (CAS: 1431697-94-7).
I-Racemic Chlorocaserin Hydrochloride powder ivela ekuxubeni i-dextrorotatory chlorocaserin hydrochloride kunye ne-lev-rotator chlorocaserin hydrochloride. I-lorcaserin ephakathi isetyenziswa kufundo kunye nokulungiswa kwesiyobisi esisebenzayo sokulahleka kobunzima.

Ukuchasana neChlorocaserin Hydrochloride

Isiyobisi saziwa njengekhemikhali njenge (R) -8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine hydrochloride (CAS no: 846589-98-8). Nangona kunjalo, ngokwemiqathango yomntu, ngu (R) i-lorcaserin hydrochloride.
Le lorcaserin iphakathi yinto yohlalutyo eluhlaza ekufundeni iipropathi zeekhemesti zokunciphisa amayeza. Kwizifundo zangaphambi kokubhalwa kweempuku, ikhompawundi ibonisa iziphumo ze-anorectic. Ngaphandle koko, kunciphisa ukungeniswa kwee-analgesics kunye neziyobisi ezifana ne-caffeine, i-amphetamine, kunye neziyobisi ezinxulumene noko.

Isandla sasekunene saseCasserole

Ngokwesayensi, le (R) -8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine ene-CAS no. 616202-92-7.
I-casserole eluhlaza yasekunene iyafumaneka ngezizathu zohlalutyo kunye nesifundo. Into ikhetha ngokukhethekileyo i-agonistic kwii-5-HT2C receptors, yiyo loo nto iluncedo kuphando lweziyobisi ezingafunekiyo.

I-Dextrorotatory Chlorocaserin Hydrochloride Hemihydrate

Eli qela liyaziwa ngokuba yi-lorcaserin hydrochloride hemihydrate. Isazisi sayo (R) -8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine hydrochloride hemihydrate (CAS: 856681-05-5).
I-Dextrorotatory Chlorocaserin Hydrochloride yinto ekrwada yokuhlanganiswa kwe-lorcaserin.

Racemic Chlorocaserin Isiseko saSimahla

Igama layo leekhemikhali yi-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine (CAS no: 616201-80-0).
I-Racemic Chlorocaserin Isiseko sasimahla yimveliso ekumgangatho wamayeza ukuze isetyenziswe kuphando nakuhlalutyo lwenzululwazi.

IKhadi eliGreen Serin eliPhakathi

Igama layo lenzululwazi yi-1 - [[2- (4-Chlorophenyl) ethyl] amino] -2-chloropropane hydrochloride (CAS no: 953789-37-2). IGreen Card uSerin ikwangaphakathi ekulungiseleleni isongezelelo se-lorcaserin.
Kuya kufuneka uqaphele ukuba zonke ezi zinto ziphakathi zelorcaserin zenzelwe kuphela iinjongo zophando. Ezi khompawundi azikulungelanga ukusetyenziswa ngabantu okanye izilwanyana.


Usebenza njani uLorcaserin?

I-Lorcaserin (Belviq) ijolise kwiNkqubo ye-Nervous Central ngokusebenzisana ne-hypothalamic receptors ezithile. Isebenza ngokwenza i-serotonin 2C (5-HT2C) kwi-pro-opiomelanocortin neurons. Le nxalenye yengqondo inesandla ekuthandeni nasekutyeni. Nangona zikho ezinye ii-receptor subtypes ezinje nge-5-HT2A kunye ne-5-HT2B, eli chiza lineyona ndawo inxulumene ne-5-HT2C.
Isongezelelo sokulahleka kwesisindo seLorcaserin senza ii-5-HT2C receptors, kungoko, zibangela ukubonakaliswa kweehomoni ze-alpha-MSH. I-Alpha-MSH isebenza kwi-melanocortin-4-receptors, ethumela imiqondiso kwingqondo yokuba ugcwele.
Ipropathi ye-agonistic ye-lorcaserin kunye ne-5-HT2C receptor inyusa ukugcwala, kungoko, ukunciphisa ukutya kunye nokukhawulezisa ukunciphisa umzimba. Ngokwezinye iingcinga zesayensi, eli chiza le-serotonergic limodareyitha amanqanaba e-leptin, ihomoni edlala indima ekwehliseni ubunzima bomzimba. Ukudityaniswa kokusebenzisa esi songezelelo njengearhente yokulwa nokutyeba kakhulu kukuba ayisixholi isifo sentliziyo se-valvular. Isizathu kukuba kuncinci kwi-agonistic kwii-5-HT2B receptors.


Izibonelelo zeLorcaserin kunye neziphumo ebezingalindelekanga

benefits

Ukuthatha i-lorcaserin hydrochloride kwandisa uvakalelo lokuhlutha. Inceda ekuphazamiseni ukutya, okuqhelekileyo kubantu abadla ngokweemvakalelo kunye nokuzinkcinkca ngotywala. Ngokweempumelelo zezilingo zeklinikhi, umntu unokulahla ubuncinci i-5% yomzimba wabo kwiiveki ze-12.
Nangona kunqabile, ukulahlekelwa ngaphantsi kwe-5% yesisindo sakho ngelixa u-lorcaserin kuthetha ukuba awusoze ufezekise nasiphi na isiphumo esibalulekileyo nangonyango lwexesha elide. Okwangoku, abaphandi bacebisa ukuba uyeke ukulawula ukongezwa kwesisindo.
Sebenzisa le arhente ye-serotonergic ngokungathandabuzekiyo kuya kubangela inkqubo yokutshiswa kwamafutha. Nangona kunjalo, kuya kufuneka ubandakanye izinto ezithile zomzimba ngelixa unamathela kukutya okuneekhalori ezisezantsi. Ngaphandle koko, ukusebenza kwe-lorcaserin kulawulo lweentsimbi kuxhomekeke kulawulo oluqhubekayo. Ukuyekisa idosi kunokuba nefuthe elibi kwiziphumo.
Ngaphandle kolawulo lobunzima, i-lorcaserin ikwasebenza ngokuqhuba ngokusetyenziswa kakhulu kwe-dopamine ekuphenduleni kwizidakamizwa ezithile ezifana ne-caffeine, i-morphine, i-codeine, okanye i-amphetamines. Iziphumo ze-agonistic zokuncedisa kwii-serotonin receptors zenza ukuba zilungele ukulawula ukuphazamiseka kwengqondo.
Ngokwenzululwazi, i-lorcaserin inokunciphisa iimpawu zeschizophrenia kuba inciphisa ukukhutshwa kwe-dopamine.

Imiphumela
  • Intloko
  • Utywala
  • Ukukhathala
  • I sizathu
  • Ukuxhalabisa
  • Umqolo okanye iintlungu zemisipha
  • Ukutyunjwa
  • Ukuchama rhoqo kunye nobunzima
  • Ukulala
  • Umlomo omile
  • Umbono utshintsho olunjengobubungqina
  • Isiqhamo
  • Amehlo aname

Ngaphezu kwesiqingatha seempawu ezimbi ze-lorcaserin HCl ngenxa yokugqithisa. Ungagqitha kwimiphumo emibi ye-lorcaserin ngokunamathela kwizilumkiso zeziyobisi. Umzekelo, akufuneki udlule kwinqanaba ledosi yemihla ngemihla. Kwimeko yokugqithisa, qiniseka ukuba ufuna ingcebiso kwezonyango. Ezinye zeempendulo zokujonga ngaphandle zibandakanya ukubona izinto ezingekhoyo, ukutshintsha kwemozulu, iintlungu zesisu, ukubetha kwentliziyo okungaqhelekanga, kunye ne-hysteria.

Ukuqapha:

Ngaphambi kokulawula ukongezwa kwe-lorcaserin HCl, kufuneka uqwalasele oku kulandelwa kunye nokuthintela iziyobisi;

  • Abanye abasebenzisi banokuba ne-aleji kwizithako ze-lorcaserin
  • Abafazi abakhulelweyo kunye noomama abancancisayo akufuneki balawule i-lorcaserin njengoko inokuchaphazela umntwana
  • Isongezelelo sinokusebenzisana namanye amayeza kagqirha kunye nalawo angabhaliswanga kwaye siphazamisane nepropathi yazo
  • Amayeza okulahleka kobunzima beLorcaserin ayaphikiswa kwizigulana ezinomhlaza okanye abo sele benesifo

Ngubani onokusebenzisa iLorcaserin?

I-Lorcaserin iluncedo kunyango lokunyanyisa. Ngokomgaqo we-FDA, eli chiza le-serotonergic lilungele kuphela abantu abatyebileyo abane-BMI engaphezulu kwe-27kg / m2 kunye nabantu abadala abatyebe nge-BMI enkulu kune-30kg / m2. Nangona kunjalo, amayeza asebenza kuphela kwizigulana ezineemeko ezinxulumene nobunzima ezinje nge-dyslipidemia, uxinzelelo lwegazi, izifo zentliziyo, kunye noxinzelelo lwegazi.
Abaguli abadala kuphela abanokwenza i-lorcaserin ithenge kulawulo lobunzima obungapheliyo. I-flick kwiimvavanyo zeklinikhi kunye neziyobisi ziqinisekisa kunokuba izifundo zabantu zazingaphezulu kweminyaka eyi-18. Ngaphezu, ukhuseleko nokusebenza kwayo kwizigulana ezingaphantsi kweminyaka eli-18 akuqinisekiswanga.
Nangona nawuphi na umntu otyebileyo okanye otyebileyo angasebenzisa i-lorcaserin yokunciphisa umzimba, kukho ezinye izinto ezichasayo kumaqela ambalwa. Umzekelo, abasetyhini abakhulelweyo abekho kumbuzo. Ngaphandle koko, akucaci nokuba ichiza liyadlula kubisi lwebele, yiyo loo nto, oomama abancancisayo babandakanyiwe ekuthatheni.


Yintoni umahluko phakathi kweLorcaserin, iCetilistat, kunye ne-Orlistat?

Lorcaserin

I-Lorcaserin HCl ngumnqweno wokunciphisa ukutya ngelixa i-orlistat kunye ne-cetilistat ibamba i-hydrolysis ye-triglycerides kwi-fatty acids. Isongezelelo sijolise kwingingqi ye-hypothalamic yengqondo elawula ukutya kunye nokuzala. Ukuthatha i-lorcaserin kuya kuqalisa ukusuthisa kwaye kubonise umzimba ukuba ugcwele nokuba ungakanani na. Ke ngoko, ukunciphisa umzimba kuyakhaba ngenxa yokunciphisa ukutya kunye nokuthintela ukutya.
Nge-lorcaserin, isigulana esityebileyo sinokulahla ngaphezulu kwe-5% yesisindo sokuqala somzimba kunye nokunciphisa ubungakanani besinqe malunga ne-3cm. Amayeza abonisa utshintsho olukhulu kunokuba usebenzisa i-orlistat.
Ngo-2012, i-lorcaserin hydrochloride iphumelele ukuvunywa yi-FDA kwaye yaba sisiyobisi sokuyalelwa kukutyeba kunye ne-comorbidities enxulumene nobunzima. Nangona kunjalo, i-Arhente ye-Federal iyirhoxisile kwimarike ngenxa yokunyuka kokuqhubela phambili komhlaza phakathi kwabasebenzisi bayo.

Cetilistat

Njenge-lorcaserin (Belviq), i-cetilistat sisiyobisi esichasene nokukhuluphala. Ukuthatha iibhloko zamachiza iipancreatic lipases, ezinoxanduva lokophula i-triglycerides. Ngenxa yoko, i-triglycerides ayizukubangela i-hydrolyze kwii-acid zamahala zokufumana ukufakwa emzimbeni. Ke ngoko, amafutha aya kukhutshwa angatyiswanga.
I-Cetilistat ingakhokelela ekunciphiseni ukuya kuthi ga kwi-10% yobunzima bomzimba kunye nokwehliswa okubonakalayo kwinqanaba lesinqe.
Ngokungafaniyo neziphumo ebezingalindelekanga ze-lorcaserin, iimpawu ezimbi ze-cetilistat ikakhulu zihambelana nokugaya. Umzekelo, umntu uya kuba namafutha anamafutha kunye nezitulo ezikhululekileyo, ukuqumba, ukuhamba kwamathumbu rhoqo, okanye ukungalawuleki kwelindle.
I-Cetilistat ayikaphumeleli ukuvunywa kwe-FDA kuba kungokunje kwizigaba zokuqala zezifundo zabantu. Ukuza kuthi ga ngoku, isongezelelo sineziphumo ezithembisayo. Ukuthelekisa phakathi kwezibalo zeklinikhi ze-cetilistat kunye ne-orlistat kufakazele ukuba eyangaphambili inyusa kakhulu ukunciphisa umzimba kwaye inokunyamezeleka okungcono.
Ukudityaniswa kwecetilistat kukuba ayisebenzi kwezinye ii-enzymes zesisu okanye kwinkqubo yeemvakalelo. Le nyani ichaza ukuba kutheni ineempendulo ezimbalwa.

Orlistat

Zombini i-Lorcaserin kunye ne-orlistat yokunceda ekulahlekeni kwesisindo. Nangona kunjalo, indlela yokusebenza kwabo yahlukile.
Njenge-cetilistat, i-Orlistat inqanda okwethutyana isisu kunye nepancreatic lipases. Olu thintelo luphazamisa i-hydrolysis ye-triglycerides ekudleni komnye, yiyo loo nto onke amanqatha afunxiweyo engatshintshwanga.
Ngokweemvavanyo zeklinikhi ezikhoyo, izifundo zabantu zinokunciphisa umzimba ngokukhawuleza ngelixa zisebenzisa i-orlistat kunaleyo ikwi-placebo. Ekupheleni kweenyanga ezintandathu, kuya kubakho utshintsho olubonakalayo kumjikelezo wesinqe. Ngaphandle koko, ukuthatha iyeza kunciphisa uxinzelelo lwegazi kunye neziganeko zohlobo lweswekile II.
I-Orlistat yeyona ndlela ilungileyo ye-lorcaserin efumaneka njengeyeza lokunyanga ukutyeba kakhulu kodwa unokuthenga nakwi-counter. Ngokungafaniyo ne-lorcaserin, eli yeza lisekho kwi-whitelist ye-FDA. Uninzi lwamazwe luya kuthengisa isongezelelo ngaphandle kwemfuneko yonyango olusemthethweni. Thatha, umzekelo, e-US, European Union, nase-Australia, ukuthenga i-orlistat kulula njengokuhlawulela izihlangu. I-Orlistat ayinampembelelo kwezinye ii-enzymes ze-GIT okanye inkqubo ye-nervous.

Amaqokobhe enathi

I-Cetilistat kunye ne-orlistat zezinye iindlela zelorcaserin zokunyanga ukutyeba nokutyeba kakhulu. Nangona kunjalo, ukusebenza kwabo ngokufanelekileyo kuya kunyuka kuphela ngemisebenzi yomzimba kunye nokutya okuneekhalori ezisezantsi. I-Lorcaserin kunye ne-orlistat banciphisa ubunzima kunye nobukhulu besinqe kodwa ukuyeka iidosi zabo kuya kwenza ukuba umsebenzisi abuyele kwi-35% yento ebephulukene nayo.
Ukuza kuthi ga ngoku, kuphela sisongezelelo seCetilistat esingakhange siyenze kugunyaziso lwe-US FDA njengoko isesekulingweni lwezonyango. Ngokumalunga ne-orlistat, ukuyifumana kufana nokuthenga iparacetamol yakho yesiqhelo. Ngokuchaseneyo, ukwenza i-lorcaserin yokuthenga phantse ayinakwenzeka okoko i-Arhente yase-US yachitha ukuvunywa kwayo kwangoko kwi-2020.
Omathathu la machiza asebenza ngokufanelekileyo kodwa i-cetilistat ineziphumo ezibonakalayo. Ngaphandle koko, ineziphumo ebezingalindelekanga ezimbalwa kwaye inyamezeleka kakuhle emzimbeni.


Kuphi ukuthenga iLorcaserin kunye nabaPhakathi bayo?

Unokwenza i-lorcaserin ithenge kwiivenkile ezikwi-intanethi. Umgubo ufumaneka ngesixa esikhulu kubaphandi nakwabahlalutyi. Xa injongo yakho kukulahla iipawundi ezongezelelekileyo ngenxa yokutyeba kakhulu, unokujonga i-lorcaserin ethengiswa kwi-Intanethi. Nangona kunjalo, unokufuna amayeza ngenxa yesikhokelo esingqongqo yi-FDA.
Ukuba ujonga i-lorcaserin okanye i-intermediates yayo, kuya kufuneka ungene kunye ne-CMOAPI ngonikezelo olusebenzayo lweemveliso ezihlambulukileyo. Amakhompawundi ethu afumene isiqinisekiso somgangatho.


Ucaphulo
  1. UTaylor, J., uDetretr, uE, kunye noPowell, J. (2013). I-Lorcaserin yoLawulo loBunzima. Iswekile, iMetabolic Syndrome, kunye nokuTyeba kakhulu.
  2. IHoy, SM (2013). I-Lorcaserin: Uphengululo loSetyenziso lwayo kuLawulo lweSisindo esingapheliyo. Iziyobisi.
  3. IHess, R., kunye noMnqamlezo, i-LB (2013). Ukhuseleko kunye nokusebenza kweLorcaserin kuLawulo lokuTyeba kakhulu. Unyango lwasemva kwesidanga.
  4. UBrashier, DB, Sharma, AK, Dahiya, N., kunye no-Singh, SK (2014). I-Lorcaserin: Inoveli yokulwa nesiyobisi. Ijenali yeFarmacology kunye neFarmacotherapeutics.
  5. UChan, EW okqhubekayo. (2013). Ukusebenza kunye noKhuseleko lweLorcaserin kubantu abadala abatyebileyo: Uhlalutyo lweMeta yoNyaka o-1 woLingo oluLungelelanisiweyo (RCTs) kunye noPhononongo lokuBalisa kwiiRCTs zeXesha elifutshane. Ukutyeba kakhulu.
  6. INigro, SC, Luon, D., kunye no-Baker, WL (2013). I-Lorcaserin: Inoveli yeSerotonin 2C Agonist yoNyango lokuTyeba kakhulu. Uphando lwangoku lwezoNyango kunye neMbono.