Lorcaserin

CMOAPI ili ndi zida zonse za lorcaserin, ndipo ili ndi pulogalamu yoyang'anira zonse.

Kuwonetsa 1-3 ya zotsatira za 6

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Kodi Lorcaserin ndi chiyani?

Lorcaserin (Belviq) ndi anti-kunenepa kwambiri. Ngati mukufuna kukweza thupi lanu popanda kukangana ndi zolimbitsa thupi, nazi zomwe muyenera kuzindikira musanagule mankhwala a serotonergic.
Lorcaserin hydrochloride idapangidwa ndi Arena Pharmaceuticals. Kwa zaka zambiri, akhala akugwiritsidwa ntchito ngati chithandizo chanthawi yayitali cha kunenepa kwambiri. Zowonjezerazo zimachepetsa chilakolako powonjezera kukhuta. Kuphatikiza apo, mphamvu ya lorcaserin sikutanthauza kuti muzitsatira zakudya zolimbitsa thupi kapena kuchita masewera olimbitsa thupi.
Chiyambireni pomwe, mankhwalawa adakumana ndi zovuta zingapo zamankhwala komanso maphunziro aumunthu kuti awonetsetse kuti ndiwothandiza komanso olekerera pochiza kunenepa kwambiri. Mu 2012, a FDA adavomereza lorcaserin (Belviq) kuti agwiritse ntchito zochiritsira koma mozama. Mwachitsanzo, mankhwalawa amangopezeka kwa anthu onenepa kwambiri komanso onenepa kwambiri omwe anali ndi zovuta zokhudzana ndi kulemera monga matenda oopsa, matenda ashuga, ndi dyslipidemia.
Pali mayina awiri otchuka a lorcaserin, ndiye kuti, Belviq ndi Belviq XR. Zonsezi ndizofanana, kukhala ndi lorcaserin hydrochloride ngati chinthu chogwira ntchito.
Makapisozi a Belviq ndi ocheperako pang'ono, ndipo kuchuluka kwa mlingowo kumagawika kawiri patsiku. Mosiyana ndi izi Belviq XR makapisozi ndi akulu kwambiri. Dzinalo la lorcaserin lili ndi mapiritsi otulutsa lalanje omwe amatengedwa kamodzi patsiku.


Ophunzira a Lorcaserin ndi Lorcaserin

Zamatsenga Chlorocaserin Hydrochloride

Mgwirizanowu umadziwika kuti lorcaserin hydrochloride. Komabe, dzina lake lasayansi ndi 8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine Hydrochloride (CAS: 1431697-94-7).
Racemic Chlorocaserin Hydrochloride powder amachokera pakuphatikiza dextrorotatory chlorocaserin hydrochloride ndi lev-rotator chlorocaserin hydrochloride. Lorcaserin wapakatikati amagwiritsidwa ntchito pophunzira ndikukonzekera mankhwala osokoneza bongo.

Dextrorotatory Chlorocaserin Hydrochloride

Mankhwalawa amadziwika kuti (R) -8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine hydrochloride (CAS no: 846589-98-8). Komabe, malinga ndi mawu a anthu wamba, ndi (R) lorcaserin hydrochloride.
Lorcaserin wapakatikatiyu ndiwofufuza zinthu zopangira mankhwala omwe amachititsa kuti munthu achepetse kunenepa. M'maphunziro am'mbuyomu omwe ali ndi mbewa, kompositiyo imawonetsa zovuta zina. Kuphatikiza apo, amachepetsanso kumwa ma analgesics ndi ma narcotic monga caffeine, amphetamine, ndi mankhwala ena ofanana nawo.

Green Casserole Wamanja

Mwasayansi, iyi ndi (R) -8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine yokhala ndi CAS no. 616202-92-7.
Casserole yobiriwira kumanja imapezeka pazifukwa zowunikira komanso zowerengera. Mankhwalawa ndi osagwirizana ndi ma 5-HT2C receptors, chifukwa chake, ndi othandiza pakufufuza zamankhwala osokoneza bongo.

Dextrorotatory Chlorocaserin Hydrochloride Hemihydrate

Izi zimadziwika kuti lorcaserin hydrochloride hemihydrate. Kudziwika kwake kwasayansi ndi (R) -8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine hydrochloride hemihydrate (CAS: 856681-05-5).
Dextrorotatory Chlorocaserin Hydrochloride ndichinthu chopangira cha lorcaserin kaphatikizidwe.

Racemic Chlorocaserin Free Base

Dzina lake ndi 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine (CAS no: 616201-80-0).
Racemic Chlorocaserin Free Base ndi mankhwala omwe amagwiritsidwa ntchito pakafukufuku komanso kusanthula kwasayansi.

Green Card Serin Wapakati

Dzinalo la sayansi ndi 1 - [[2- (4-Chlorophenyl) ethyl] amino] -2-chloropropane hydrochloride (CAS no: 953789-37-2). Green Card Serin ndiwonso wapakatikati pokonzekera chowonjezera cha lorcaserin.
Muyenera kuzindikira kuti ma lorcaserin apakatikatiwa amangofufuza. Mankhwalawa sioyenera kudya anthu kapena nyama.


Kodi Lorcaserin Amagwira Ntchito Bwanji?

Lorcaserin (Belviq) imayang'ana Central Nervous System polumikizana ndi ma hypothalamic receptors. Imachita poyambitsa serotonin 2C (5-HT2C) pa pro-opiomelanocortin neurons. Gawo ili laubongo limakhala ndi chilakolako chofuna kudya komanso kudya. Ngakhale pali ma receptor ena amtundu wina monga 5-HT2A ndi 5-HT2B, mankhwalawa ali ndi chiyanjano chachikulu cha 5-HT2C.
Lorcaserin yolemetsa yowonjezera imathandizira ma 5-HT2C receptors, chifukwa chake, zomwe zimapangitsa chidwi cha mahomoni a alpha-MSH. Alpha-MSH imagwira pa melanocortin-4-receptors, yomwe imatumiza zikwangwani kuubongo kuti mwakhuta.
Katundu wa agonistic wa lorcaserin wokhala ndi 5-HT2C receptor augments satiety, chifukwa chake, amachepetsa kudya ndikuchepetsa kuchepa kwa thupi. Malinga ndi zomwe asayansi ena amaganiza, mankhwalawa amatulutsa milingo ya leptin, mahomoni omwe amathandizira kuchepetsa thupi. Kuphatikiza pakugwiritsa ntchito chowonjezerachi ngati cholimbana ndi kunenepa kwambiri ndikuti sikuyambitsa matenda amtima wa valvular. Cholinga chake ndikuti ndizovuta kwambiri kuzilandira za 5-HT2B.


Ubwino wa Lorcaserin ndi Zotsatira zoyipa

ubwino

Kutenga lorcaserin hydrochloride kumawonjezera kukhudzidwa kwa kukhuta. Zimathandiza pamavuto akudya, monga momwe zimakhalira kwa omwe amadya mwamphamvu komanso kudya kwambiri. Malinga ndi mayesero opambana a lorcaserin, munthu amatha kutaya osachepera 5% ya kulemera kwawo m'masabata a 12.
Ngakhale ndizosowa, kutaya kuchepa kwa 5% ya kulemera kwanu mukakhala pa lorcaserin kumatanthauza kuti mwina simungakhale ndi zotsatirapo zabwino ngakhale mutalandira chithandizo cha nthawi yayitali. Pakadali pano, ofufuza amalimbikitsa kuti musiye kupereka zowonjezera zowonjezera.
Kugwiritsira ntchito serotonergic agent mosakayikira kumayambitsa mafuta. Komabe, muyenera kuphatikiza zochitika zina zakuthupi mukumamatira ku zakudya zonenepetsa. Kuphatikiza apo, mphamvu ya lorcaserin pakuwongolera zolemera pamayendedwe mosalekeza. Kutaya mlingowo kumatha kusokoneza zotsatira zake.
Kuphatikiza pa kuwongolera kunenepa, lorcaserin imagwiranso ntchito poyendetsa kuchepa kwa dopamine poyankha mankhwala ena osokoneza bongo monga caffeine, morphine, codeine, kapena amphetamines. Zotsatira za agonistic zowonjezerazo pama serotonin receptors zimapangitsa kukhala koyenera kuthana ndi zovuta zama psychotic.
Malinga ndi asayansi, lorcaserin amathanso kuthana ndi matenda a schizophrenia chifukwa amachepetsa kutulutsa kwa dopamine.

Zotsatira Zotsatira
  • litsipa
  • chizungulire
  • kutopa
  • nseru
  • nkhawa
  • Msana kapena kupweteka kwa minofu
  • kudzimbidwa
  • Kukodza pafupipafupi komanso kovuta
  • Kusagona
  • pakamwa youma
  • Masomphenya amasintha monga blurriness
  • Kukuda
  • Maso owuma

Zoposa theka la zizindikilo zoyipa za lorcaserin HCl zimachitika chifukwa cha bongo. Mutha kudutsa zotsatira zoyipa za lorcaserin mukamamatira ku njira zosamalirira mankhwala. Mwachitsanzo, simuyenera kupitirira mulingo wamasiku onse. Pankhani ya bongo, onetsetsani kuti mwapeza upangiri kuchipatala. Zina mwazomwe mungachite kuti muwone ngati izi zimaphatikizapo kuyerekezera zinthu m'maganizo, kusintha kwa malingaliro, kupweteka m'mimba, kugunda kwamtima mosasinthasintha, komanso kukwiya.

Zisamaliro:

Musanapereke mankhwala owonjezera a lorcaserin HCl, muyenera kuganizira zotsutsana ndi njira zotetezera mankhwala;

  • Ogwiritsa ntchito ena atha kukhala osagwirizana ndi zopangira za lorcaserin
  • Amayi apakati ndi amayi oyamwitsa sayenera kupereka lorcaserin chifukwa imakhudza mwanayo
  • Chowonjezeracho chimatha kulumikizana ndi mankhwala ena osalembedwa komanso kusokoneza zomwe ali nazo
  • Mankhwala amtundu wa Lorcaserin amatsutsana ndi odwala omwe ali ndi khansa kapena omwe ali ndi matenda

Ndani Angagwiritse Ntchito Lorcaserin?

Lorcaserin ndi othandiza pochiza kunenepa kwambiri. Malinga ndi lamulo la FDA, mankhwalawa a serotonergic amangoyenera anthu onenepa kwambiri omwe ali ndi BMI yopitilira 27kg / m2 komanso achikulire onenepa omwe ali ndi BMI yoposa 30kg / m2. Komabe, mankhwalawa ndi othandiza kwa odwala omwe ali ndi zovuta zokhudzana ndi matenda monga dyslipidemia, kuthamanga kwa magazi, matenda amtima, ndi matenda oopsa.
Odwala achikulire okha ndi omwe amatha kupanga lorcaserin kugula kuti azitha kuwongolera zolemera. Kuzungulira pamayesero azachipatala ndi mankhwalawa kumatsimikizira kuposa zomwe anthu anali nazo kuposa zaka 18. Kuphatikiza apo, chitetezo chake komanso mphamvu zake kwa odwala osakwana zaka 18 sizinatsimikizidwe.
Ngakhale wamkulu aliyense wonenepa kwambiri kapena wonenepa kwambiri atha kugwiritsa ntchito mankhwala owonjezera a lorcaserin, pali zotsutsana ndi magulu ochepa. Mwachitsanzo, amayi apakati sangatchulidwe. Kuphatikiza apo, sizikudziwika ngati mankhwalawa amadutsa mkaka wa m'mawere, chifukwa chake, amayi omwe akuyamwitsa satulutsidwa.


Kodi Pali Kusiyana Pati Pakati pa Lorcaserin, Cetilistat, ndi Orlistat?

Lorcaserin

Lorcaserin HCl ndi chilakolako chofuna kudya pamene orlistat ndi cetilistat amaletsa hydrolysis ya triglycerides kukhala mafuta omwe amatha kuyamwa. Chowonjezeracho chimayang'ana dera la hypothalamic laubongo lomwe limayang'anira kudya ndi chidzalo. Kutenga lorcaserin kuyambitsa kukhuta ndikuwonetsa thupi kuti mwadzaza mosasamala kuchuluka kwa zomwe mwadya. Chifukwa chake, kuchepa thupi kumayambira chifukwa chakuchepa kwakudya komanso kusapeza chakudya.
Ndi lorcaserin, wodwala wonenepa amatha kutaya kuposa 5% ya thupi lawo loyambirira ndikuchepetsa kukula kwa chiuno pafupifupi 3cm. Mankhwalawa akuwonetsa kusintha kwakukulu kuposa momwe amagwiritsira ntchito orlistat.
Mu 2012, lorcaserin hydrochloride idapambana kuvomerezedwa ndi FDA ndikukhala mankhwala osokoneza bongo okhudzana ndi kunenepa kwambiri komanso zovuta zokhudzana ndi kulemera. Komabe, Federal Agency idachotsa pamsika chifukwa cha kuchuluka kwa khansa pakati pa ogwiritsa ntchito.

Cetilistat

Monga lorcaserin (Belviq), cetilistat ndi mankhwala oletsa kunenepa kwambiri. Kutenga mankhwalawa kumatsegula ma pancreatic lipases, omwe amachititsa kuti triglycerides iwonongeke. Zotsatira zake, ma triglycerides sadzasungunuka kukhala mafuta amtundu wamafuta kuti alowerere mthupi. Chifukwa chake, mafuta amamasulidwa osagayidwa.
Cetilistat imatha kubweretsa kuchepa mpaka 10% ya kulemera kwa thupi ndikuchepetsa kwakukulu m'chiuno.
Mosiyana ndi zoyipa za lorcaserin, zizindikilo zoyipa za cetilistat zimakhudzana makamaka ndi chimbudzi. Mwachitsanzo, munthu amakumana ndimatope amafuta ndi otayirira, kukhathamira, kuyenda matumbo pafupipafupi, kapena kusadziletsa.
Cetilistat sanalandirebe kuvomerezedwa ndi FDA chifukwa pakadali pano koyambirira kwamaphunziro aumunthu. Pakadali pano, chowonjezeracho chili ndi zotsatira zabwino. Kuyerekeza pakati pa ziwerengero zamatenda a cetilistat ndi orlistat kunatsimikizira kuti choyambacho chimathandizira kwambiri kuwonda ndipo chimatha kulolerana.
Kuphatikiza kwa cetilistat ndikuti sichimagwira ma enzyme ena am'mimba kapena dongosolo lamanjenje. Izi zikufotokozera chifukwa chomwe zimakhalira ndi zovuta zochepa.

Orlistat

Onse awiri a Lorcaserin ndi orlistat amathandizira kuwonda. Komabe, momwe amagwirira ntchito amasiyana.
Monga cetilistat, Orlistat imalepheretsa kwakanthawi m'mimba ndi kapamba lipases. Kuletsa uku kumalepheretsa hydrolysis ya triglycerides kuchokera pazakudya zanu, chifukwa chake, mafuta onse oyamwa amasinthidwa osasinthika.
Malinga ndi mayeso azachipatala omwe amapezeka, anthu amatha kuonda mwachangu akamagwiritsa ntchito orlistat kuposa omwe ali pa placebo. Pakutha pa miyezi isanu ndi umodzi, padzakhala kusintha kwakukulu m'mbali mwake. Kuphatikiza apo, kumwa mankhwalawa kumachepetsa kuthamanga kwa magazi komanso kuchuluka kwa matenda ashuga amtundu wachiwiri.
Orlistat ndi njira yabwino kwambiri ya lorcaserin yomwe imapezeka ngati mankhwala ochiritsira kunenepa koma mutha kugulanso pa-counter. Mosiyana ndi lorcaserin, mankhwalawa akadali pa whitelist a FDA. Mayiko ambiri amatha kugulitsa zowonjezerazo popanda kufunikira chiphaso chovomerezeka. Tengani, mwachitsanzo, ku US, European Union, ndi Australia, kugula orlistat ndikosavuta monga kulipira nsapato. Orlistat ilibe vuto lililonse ndi michere ina ya GIT kapena dongosolo lamanjenje.

Mwachidule

Cetilistat ndi orlistat ndi njira zina za lorcaserin zochizira kunenepa kwambiri komanso kunenepa kwambiri. Komabe, kuyendetsa bwino kwawo kumangokulira ndi zochitika zathupi komanso zakudya zochepa. Lorcaserin ndi orlistat amachepetsa kulemera ndi kukula m'chiuno koma kusiya mankhwala ake kumapangitsa kuti wogwiritsa ntchitoyo apezenso 35% yazomwe adataya.
Pakadali pano, ndizowonjezera za Cetilistat zokha zomwe sizinafike ku US FDA yoyera popeza ikadali m'mayesero azachipatala. Ponena za orlistat, kuchipeza kuli ngati kugula paracetamol yanu. Mosiyana ndi izi, kupanga lorcaserin kugula ndizosatheka kuyambira pomwe US ​​Federal Agency idaletsa kuvomereza kwawo koyambirira kwa 2020.
Mankhwala atatuwa amagwira ntchito bwino koma cetilistat ili ndi zotsatira zabwino. Kuphatikiza apo, ili ndi zovuta zoyipa zochepa ndipo imaloledwa bwino mthupi.


Kodi Mungagule Kuti Lorcaserin ndi Ophatikizira Ake?

Mutha kupanga lorcaserin kugula m'masitolo apaintaneti. Ufa umapezeka wochuluka kwa ofufuza ndi akatswiri. Pamene cholinga chanu ndikutaya mapaundi owonjezera chifukwa cha kunenepa kwambiri, mutha kuwona lorcaserin yogulitsa pa intaneti. Komabe, mungafunike mankhwala chifukwa chotsatira malangizo okhwima a FDA.
Ngati mukuyang'ana lorcaserin kapena oyimira pakati, muyenera kufunsa ndi CMOAPI kuti mupeze zogulitsa zenizeni. Makampani athu adalimbikitsidwa.


Zothandizira
  1. Taylor, J., Dietrich, E., ndi Powell, J. (2013). Lorcaserin ya Kunenepa. Matenda a shuga, Metabolic Syndrome, ndi Kunenepa Kwambiri.
  2. Hoy, SM (2013). Lorcaserin: Kuwunikiranso Momwe Amagwiritsidwira Ntchito Mukusamalira Kunenepa Kwambiri. Mankhwala osokoneza bongo.
  3. Hess, R., ndi Cross, LB (2013). Chitetezo ndi Kuchita Bwino kwa Lorcaserin mu Management of Obesity. Mankhwala Omaliza Maphunziro.
  4. Brashier, DB, Sharma, AK, Dahiya, N., ndi Singh, SK (2014). Lorcaserin: Mankhwala Osokoneza Bongo Osadziwika. Zolemba za Pharmacology & Pharmacotherapeutics.
  5. Chan, EW ndi al. (2013). Kuchita bwino ndi Chitetezo cha Lorcaserin mwa Achikulire Olemera: Meta-Analysis of 1-Year Randomized Controlled Trials (RCTs) ndi Ndemanga Yowunikira pa RCTs Yaifupi. Ndemanga Zakudya Zambiri.
  6. Nigro, SC, Luon, D., ndi Baker, WL (2013). Lorcaserin: A Novel Serotonin 2C Agonist a Chithandizo cha Kunenepa Kwambiri. Kafukufuku Wamakono Wazachipatala ndi Maganizo.