Lorcaserin

CMOAPI ine yakazara yakazara zvigadzirwa zveyakaora ye lorcaserin, uye ine yakazara mhando yehutariri system.Also yakapfuura GMP uye DMF chitupa.

Kuratidza 1-3 ye 6 migumisiro

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Chii chinonzi Lorcaserin?

Lorcaserin (Belviq) inorwisa-kufutisa mumiriri. Kana iwe uri kukwira kuzunza kurebesa kwehuremu hwemuviri pasina kupokana nezve kunetesa kushanda, hezvino izvo zvaunofanira kucherechedza usati watenga iyo serotonergic drug.
Lorcaserin hydrochloride yakagadzirwa neArena Pharmaceuticals. Kwemakore, yanga ichishandiswa sekurapwa kwenguva refu kwekurema. Iyo yekuwedzera inodzvinyirira kudya nekuwedzera satiation. Kunze kwezvo, lorcaserin kushanda hakudi kuti iwe uteedzere imwe yakaoma kudya kana kurovedza maitiro.
Kubvira payakatanga, mushonga uyu wakaitwa miedzo yakawanda yepamberi uye zvidzidzo zvevanhu kuti uone kushanda kwayo nekushivirira mukurapa kufutisa. Muna 2012, FDA yakabvumira lorcaserin (Belviq) yekurapa kushandiswa asi pasi pezviyero zvakaoma. Semuenzaniso, iyo yekunyora-chete yakazovepo kune vakafutisa uye vakafutisa vanhu vakuru vaive nehuremu-hwakanangana nehukama hwakadai sehypertension, chirwere cheshuga, uye dyslipidemia.
Kune maviri mazita anozivikanwa erorcaserin mazita, ndiko kuti, Belviq naBelviq XR. Ose ari maviri akafanana akafanana, aine lorcaserin hydrochloride sechinhu chinoshanda.
Belviq capsules madiki zvishoma, uye iyo dosi renji inopatsanurwa kuita maviri pazuva. Contrariwise Belviq XR ma capsules akakurisa. Iri zita rerorcaserin rine mahwendefa eorenji akawedzerwa-kuburitswa anotorwa kamwe pazuva.


Lorcaserin uye Lorcaserin Vapakati

Rudzi rweChlorocaserin Hydrochloride

Ichi chikamu chinowanzo kunzi lorcaserin hydrochloride. Zvisinei, zita rayo resainzi ndi8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine Hydrochloride (CAS: 1431697-94-7).
Racemic Chlorocaserin Hydrochloride powder inobva mukusanganisa dextrorotatory chlorocaserin hydrochloride uye lev-rotatory chlorocaserin hydrochloride. Iyo lorcaserin yepakati inoshandiswa mukudzidza uye kugadzirira kweiyo inoshanda inorema-kurasikirwa nemushonga.

Dextrorotatory Chlorocaserin Hydrochloride

Chinhu chacho chinozivikanwa semakemikari se (R) -8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine hydrochloride (CAS no: 846589-98-8). Zvisinei, mumashoko evanogona, iri (R) lorcaserin hydrochloride.
Iyi lorcaserin yepakati ndeye yekuongorora mbishi zvinhu zvekufunda izvo zvemishonga zvimiro zvekurema kurasikirwa nemishonga. Muzvidzidzo zvepamberi nemakonzo, iyo komponi inoratidza anorectic mhedzisiro Kunze kwezvo, zvinoderedza zvakare kudyiwa kweanorodza uye narcotic senge caffeine, amphetamine, uye zvimwe zvinodhaka.

Kurudyi-Ruoko Green Casserole

Sainzi, iyi (R) -8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine ine CAS kwete. 616202-92-7.
Iyo yekurudyi-ruoko girini casserole inowanikwa yekuongorora uye kudzidza zvikonzero. Icho chinhu chinosarudzika agonistic kune 5-HT2C receptors, nekudaro, inobatsira mukutsvagisa kudya-inodzvinyirira zvinodhaka.

Dextrorotatory Chlorocaserin Hydrochloride Hemihydrate

Ichi chikamu chinozivikanwa se lorcaserin hydrochloride hemihydrate. Kuzivikanwa kwayo kwesainzi ndeye (R) -8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine hydrochloride hemihydrate (CAS: 856681-05-5).
Dextrorotatory Chlorocaserin Hydrochloride chinhu chakasvibirira che lorcaserin synthesis.

Racemic Chlorocaserin Mahara Base

Yayo kemikari zita iri 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzazepine (CAS no: 616201-80-0).
Racemic Chlorocaserin Mahara Base chigadzirwa chemishonga-giredhi rekushandisa mukutsvaga uye kuongorora kwesainzi.

Green Kadhi Serin Pakati

Zita rayo resainzi ndi 1 - [[2- (4-Chlorophenyl) ethyl] amino] -2-chloropropane hydrochloride (CAS no: 953789-37-2). Green Kadhi Serin zvakare iri yepakati mukugadzirira kwe lorcaserin yekuwedzera.
Iwe unofanirwa kucherechedza kuti ese aya marorcaserin epakati ari chete ekutsvagisa zvinangwa. Iwo makomponi haana kukodzera kudyiwa nevanhu kana mhuka.


Lorcaserin Anoshanda Sei?

Lorcaserin (Belviq) inotarisana neCentral Nervous System nekudyidzana neakanyanya hypothalamic receptors. Inoita nekumisikidza serotonin 2C (5-HT2C) pane pro-opiomelanocortin neurons. Ichi chikamu cheuropi chine ruoko mukudya uye tsika dzekudya. Kunyangwe paine mamwe ekugamuchira madiki senge 5-HT2A uye 5-HT2B, uyu mushonga une hukama hwakanyanya hwe5-HT2C.
Lorcaserin uremu hwekuwedzera inowedzera inomutsa iyo 5-HT2C receptors, nekudaro, ichikurudzira kutaura kwealpha-MSH mahormone. Alpha-MSH inoshanda pane melanocortin-4-receptors, iyo inotumira mameseji kuuropi kuti waguta.
Iyo agonistic chivakwa che lorcaserin ine iyo 5-HT2C receptor inowedzera satiety, nekudaro, kudzikisa kudya kwekudya uye nekukurumidza kurasikirwa nekurema. Zvinoenderana nedzimwe fungidziro dzesainzi, iyi serotonergic drug inogadzirisa mwero weleptin, hormone inoita basa rekudzikisa uremu. Iyo yekuwedzera yekushandisa iyi yekuwedzera seanorwisa-kufutisa mumiriri ndeyekuti haibvise chirwere chevvalvular moyo Icho chikonzero ndechekuti haina kushomeka kune iyo 5-HT2B receptors.


Lorcaserin Makomborero uye Mativi Mhedzisiro

Benefits

Kutora lorcaserin hydrochloride kunowedzera kunzwa kwesatiety. Inobatsira nekunetseka kwekudya, senge kunozivikanwa kune vanonzwa uye vanodya zvinwiwa. Zvinoenderana nekubudirira kwema lorcaserin kiriniki miedzo, munhu anogona kurasikirwa kana 5% yehuremu hwemuviri wavo mumavhiki gumi nemaviri.
Kunyangwe zvisingawanzoitika, kurasikirwa pasi pe5% yehuremu hwako pa lorcaserin zvinoreva kuti haungatombowana chero mhedzisiro ine hunhu kunyangwe nekurapwa kwenguva refu. Panguva ino, vaongorori vanokurudzira kuti umise kupa huremu hwekuwedzera uremu.
Kushandisa iyi serotonergic mumiririri pasina mubvunzo kunokonzeresa kupisa-kupisa maitiro. Nekudaro, iwe unofanirwa kuisa zvimwe zviitiko zvepanyama uchinamatira kune yakaderera-koriori chikafu. Kunze kwezvo, lorcaserin inoshanda muhuremu manejimendi hinges pane inoenderera manejimendi. Kurega kuyerwa kunogona kukanganisa mhedzisiro.
Kunze kwekurema uremu, lorcaserin inoshandawo nekutyaira pasi kuwanda kwedopamine mukupindura kune mamwe maNarcotic akaita caffeine, morphine, codeine, kana amphetamines. Iwo agonistic mhedzisiro yeiyo yekuwedzera pane serotonin receptors inoita kuti ive yakakodzera kugadzirisa kusagadzikana kwepfungwa.
Sekureva kwesainzi, lorcaserin inogona zvakare kudzikamisa zviratidzo zvechichichiphrenia sezvo ichideredza kuburitswa kwedopamine.

Migumisiro Yechiri
  • Headaches
  • Chizutu
  • Kuneta
  • Nausea
  • kufunganya
  • Musana kana kurwadziwa kwemhasuru
  • Constipation
  • Kakawanda uye kwakaoma kuita weti
  • Kurara
  • Dry mouth
  • Zviratidzo zvinoshanduka zvakadai se-blurriness
  • Kukosora
  • Meso akaoma

Zvinopfuura hafu yezviratidzo zvisina kunaka zve lorcaserin HCl zvinokonzerwa nekuwedzeredza. Unogona kupfuudza iyo lorcaserin mhedzisiro nekunamatira kune zvekuchengetedza zvinodhaka. Semuenzaniso, iwe haufanire kupfuudza zuva reyero renji. Panyaya yekuwedzeredza, ita shuwa yekutsvaga rairo yekurapa. Zvimwe zvezviitiko zvekutarisa zvinosanganisira kuona zvisipo, kushanduka kwemanzwiro, kurwadziwa nemudumbu, kurova kwemoyo zvisina kujairika, uye kutsamwa.

Precautions:

Usati waisa lorcaserin HCl yekuwedzera, iwe unofanirwa kufunga zvinotevera zvinopesana uye zvekudzivirira zvinodhaka.

  • Vamwe vashandisi vanogona kunge vari allergiki kune lorcaserin zvigadzirwa
  • Vakadzi vane pamuviri uye amai vanoyamwisa havafanirwe kupa lorcaserin sezvo inogona kukanganisa mwana
  • Iyo yekuwedzera inogona kuwirirana neimwe mishonga yekunyora uye isina kunyoreswa uye inokanganisa yavo pharmacological zvivakwa
  • Lorcaserin kurasikirwa nemushonga mishonga inopesana nevarwere vanogona kubatwa nekenza kana avo vagara vaine chirwere

Ndiani Anogona Kushandisa Lorcaserin?

Lorcaserin ndeyekurapa kunobatsira pakurapa kufutisa. Zvinoenderana nemutemo weDFA, uyu serotonergic mushonga unokodzera chete vanhu vakafuta zvakanyanya vane BMI inopfuura 27kg / m2 uye vanhu vakafutisa vane BMI inopfuura 30kg / m2. Nekudaro, iwo mushonga unoshanda chete kune varwere vane mamiriro ane huremu hwakadai sedyslipidemia, kuwedzerwa kweropa, hosha yemoyo, uye neBP.
Varwere vakuru chete ndivo vanogona kuita kuti lorcaserin itenge yeusingaperi uremu manejimendi. Kufuratira kuburikidza nemakiriniki ekuedzwa nemushonga unosimbisa kupfuura izvo zvidzidzo zvevanhu zvaive pamusoro pemakore gumi nemasere. Uyezve, kuchengetedzeka kwayo pamwe nekubudirira kwevarwere vari pasi pemakore gumi nemasere hakuna kusimbiswa.
Kunyangwe chero munhu mukuru kana mukobvu anokwanisa kushandisa lorcaserin uremu hwekuwedzera, pane zvimwe zvinopesana nemapoka mashoma. Semuenzaniso, vakadzi vane nhumbu vari kunze kwemubvunzo. Kunze kwezvo, hazvizivikanwe kana mushonga uyu uchipfuura nemukaka wemukaka, nokudaro, vanaamai vanonwisa mvura vanosiiwa pakutora.


Ndeupi Musiyano Pakati peLorcaserin, Cetilistat, uye Orlistat?

Lorcaserin

Lorcaserin HCl chishuwo-chinodzvinyirira apo orlistat uye cetilistat inodzora hydrolysis ye triglycerides mumafuta asingabatike acids. Iyo yekuwedzera inotarisa iyo hypothalamic dunhu rehuropi iyo inodzora chishuwo uye kuzara. Kutora lorcaserin kunotanga kuguta uye kuratidza muviri kuti waguta zvisinei nemari shoma yawakadya. Naizvozvo, kurasikirwa kwehuremu kunorova mukati nekuda kwekuderedzwa kwekudya chikafu uye chikafu chikafu.
Na lorcaserin, murwere akafutisa anogona kurasikirwa neanopfuura 5% yehuremu hwemuviri wavo wekutanga uye kudzikisa saizi yechiuno ingangoita 3cm. Iyo mishonga inoratidza shanduko dzakakosha pane kana uchishandisa orlistat.
Mu2012, lorcaserin hydrochloride yakahwina mvumo yeDAA uye ikava mushonga wekunyorera kufutisa uye zvine chekuita nehuremu zvine hukama. Nekudaro, iyo Federal Agency yakaibvisa pamusika nekuda kwekuwedzera kwekuwedzera kwekenza pakati pevashandisi vayo.

Cetilistat

Kunge lorcaserin (Belviq), cetilistat inorwisa-kufutisa zvinodhaka. Kutora mushonga unodzivirira pancreatic lipases, inova nebasa rekutyora triglycerides. Nekuda kweizvozvo, iyo triglycerides haizopinze hydrolyze mune emahara emafuta acids ekunyatsoshanda kunyura mumuviri. Naizvozvo, mafuta anozoburitswa asina kudyiwa.
Cetilistat inogona kutungamira mukudzikira inosvika gumi muzana yehuremu hwemuviri uye kudzikisira kwakakosha muchiuno chakatenderedzwa.
Kusiyana ne lorcaserin mhedzisiro, izvo zvakashata zviratidzo zvecetilistat zvinonyanya kuenderana nekugaya. Semuenzaniso, mumwe achasangana nemafuta uye akasununguka zvituru, kubatikana, kugara uchiita ura, kana kusagadzikana kwetsvina.
Cetilistat haisati yakunda mvumo yeDFA nekuti parizvino iri muzvikamu zvekutanga zvezvidzidzo zvevanhu. Parizvino, iyo yekuwedzera ine anovimbisa mhedzisiro. Kufananidza pakati pemakiriniki stats eecetilistat uye orlistat yakaratidza kuti iyo yekutanga inowedzera kukurumidza kurasikirwa uye ine kushivirira zvirinani.
Iko kusanganisa kwecetilistat ndeyekuti haibate pane mamwe maenzyme emudumbu kana nehurongwa hwekutya. Chokwadi ichi chinotsanangura kuti nei chiine maitiro mashoma.

Orlistat

Ose maviri Lorcaserin uye orlistat rubatsiro mukurema uremu. Zvisinei, maitiro avo ekuita akasiyana.
Kungofanana necetilistat, Orlistat inodzivirira kwenguva pfupi gastric uye pancreatic lipases. Iyi inhibition inopesana neiyo hydrolysis ye triglycerides kubva pane yaunodya, nekudaro, ese mafuta anonwiwa anoburitswa asina kuchinjika.
Zvinoenderana neanowanikwa emakiriniki miedzo, zvidzidzo zvevanhu zvinogona kurasikirwa nekuremerwa nekukurumidza pavanenge vachishandisa orlistat pane avo vari panzvimbo. Pakupera kwemwedzi mitanhatu, pachave neshanduko dzinooneka mudenderedzwa rechiuno. Kunze kwezvo, kutora mushonga kunoderedza BP uye chiitiko cherudzi rwechipiri chirwere cheshuga.
Orlistat ndiyo yakanakira lorcaserin imwe nzira iyo inowanikwa seyachiremba mushonga yekurapa kufutisa asi iwe unogona zvakare kutenga pamusoro-e-iyo kondisiti. Kusiyana ne lorcaserin, uyu mushonga uchiri pane whitelist yeiyo FDA. Mazhinji matunhu aigona kutengesa iyo yekuwedzera pasina chikonzero chechokwadi chinonyorwa. Tora, semuenzaniso, muUS, European Union, neAustralia, kutenga orlistat kuri nyore sekubhadhara shangu shangu. Orlistat haina mhedzisiro pane mamwe maGN enzymes kana iyo system yehurongwa.

Muchidimbu

Cetilistat uye orlistat ndeimwe nzira dze lorcaserin dzekurapa kufutisa uye kufutisa. Nekudaro, kugona kwavo kunongowedzera chete nemabasa epanyama uye kudya kwakaderera-koriori. Lorcaserin uye orlistat inoderedza huremu uye kukura kwechiuno asi kuregedza madhiri avo kuchaita kuti mushandisi awanezve kusvika ku35% yezvavakange varasikirwa nazvo.
Parizvino, ingori iyo yeCetilistat yekuwedzera iyo isina kuzviita kuUS FDA whitelist sezvo ichiri mumakiriniki ekuedzwa. Kana iri orlistat, kuitora kwakafanana nekutenga yako chaiyo paracetamol. Kupesana, kugadzira lorcaserin kutenga zvinenge zvisingaite sezvo iyo US Federal Agency yakabvisa kubvumidzwa kwayo mukutanga 2020.
Mishonga mitatu iyi inoshanda nemazvo asi cetilistat ine mhedzisiro inoshamisa. Kunze kwezvo, ine mashoma mhedzisiro uye inoregererwa-mumuviri.


Ndekupi Kwokutenga Lorcaserin neVapakati vayo?

Iwe unogona kugadzira lorcaserin kutenga pazvitoro zvepamhepo. Iyo poda inowanikwa yakawanda kune vaongorori nevanoongorora. Kana chinangwa chako kuri kurasikirwa nemapaundi ekuwedzera nekuda kwekufutisa, unogona kutarisa lorcaserin iri kutengeswa online. Nekudaro, iwe ungangoda mushonga semhedzisiro yemitemo yakaoma neDFA.
Kana iwe uchitsvaga lorcaserin kana ayo epakati, iwe unofanirwa kutarisa neCMOAPI kuti uwane unovimbika hwezvakachena zvigadzirwa. Makomputa edu akawana vimbiso yemhando yepamusoro.


References
  1. Taylor, J., Dietrich, E., uye Powell, J. (2013). Lorcaserin yeUremu Management. Chirwere cheshuga, Metabolic Syndrome, uye Kufutisa.
  2. Hoy, SM (2013). Lorcaserin: Ongororo Yekushandisa Kwayo muKusingaperi Kurema Management. Zvinodhaka.
  3. Hess, R., uye Muchinjikwa, LB (2013). Iko Kuchengeteka uye Kubudirira kweLorcaserin mu Management yeKufutisa. Postgraduate mushonga.
  4. Brashier, DB, Sharma, AK, Dahiya, N., uye Singh, SK (2014). Lorcaserin: A Novel Antiobesity Zvinodhaka. Zvinyorwa zveFarmacology & Pharmacotherapeutics.
  5. Chan, EW uye al. (2013). Kubudirira uye Kudzivirirwa kwaLorcaserin muVakuru Vakuru: Meta-Ongororo ye1-Year Randomized Kudzora Miedzo (RCTs) uye Rondedzero Ongororo paPfupi-Nguva RCTs. Kuwedzeredza Ongororo.
  6. Nigro, SC, Luon, D., uye Baker, WL (2013). Lorcaserin: A Novel Serotonin 2C Agonist ye Kurapa Kufutisa. Ikozvino Kurapa Kwekutsvaga uye Maonero.