2018 Yakanakisisa-Kutengesa Kurasikirwa Kwehupfumi Kuwedzera Powder-Orlistat

 

Kuonda Drug History

 

Yokutanga kurasikirwa kwemishonga, iyo inonzi mafuta ekuchera panguva iyoyo, yakasvika pakupedzisira kwe1800s. Kunyange zvazvo mishonga iyi yakakonzera mamwe madhara akaipa, yakaramba ichiwanikwa kuti ishandiswe kusvikira ku1960s.
Mishonga mitsva inozivikanwa seDinroprophenol yakaiswa muZ1930 uye yakava yakakurumbira pakugadzirisa kurasikirwa. Iyo mishonga yakabudisa hutemogenic mukati momuviri, kuita kuti kurasikirwa kuwedzere.
Pakati pe-1950s, amphetamine yakavapo uye yakashanduka kuve kurasikirwa nemishonga yekusarudza. Yakaita kuti kurasikirwa kwemahombekombe kuve kukanganisa nekudzivisa kudya. Zvinosuruvarisa, yakawedzera ngozi yepemmonia yeupempersion, zvichiita kuti ibve kubva pamusika mu1968.

Mune 1970s, ephedrine yakave yakarongerwa kurapwa kwekurema. Mishonga iyi, zvisinei, yakakonzera kushushikana kwakashata kwakazoita kuti iziviswa kuti inotyisa.
Muna 1973, fenfluramine yakagamuchirwa sekuti kurasikirwa kwekureruka kuwedzera. Kuzivikanwa kwaro kwakasimudzirwa mu1992 apo yaisanganiswa ne phentermine kuumba kurasikirwa kwemazizi kunonzi fen-phen. Zvinosuruvarisa kuti mishonga iyi yakakonzera zvimwe zvinetso zvakashata, izvo zvakaita kuti zvibve pamusika mu1997. Muzana remakore reC21, kurasikirwa kwechiremera chemishonga, zvakawanda zvakabva pamaruva emiti, yakazara mumusika.

 


 

Kurema kwehutachiona hwechirwere chechirwere

 

Kurema kwekurasikirwa zvinodhaka zvinongororwa kuva zvikamu zvitatu zvakakura maererano nemaitiro avo ekuita uye zvinotevera:

 

(1) Appetite suppressant (Zvokudya)

 

Zvinodhaka zvinoderedza kudya zvokudya zvinonzi sympathomimetic agents. Vanowanzodzvinyirira chido apo vachiita kuti satiety isati yasvika. Satiety ndiyo "yakazara" kunzwa kana kugutsikana kunowanikwa pakutora zvokudya. Maitiro ekudzvinyirira anoshanda nekutevedzera neurotransmitter muhuropi hwemunhu inodzora chido, inozivikanwa sa noradrenaline (NA).

Iyi mishonga inobatanidza chimiro chakafanana neA NA uye inogona; semugumisiro kusunga kumabiro mamwechete se noradrenaline.

Chimiro chimiro che sympathomimetic agents.

Iyo mishonga zvakare inovandudza noradrenaline chiitiko mu "nzvimbo yekudyisa" yehuropi hwemunhu, iyo hypothalamus. Iyo hypothalamus yemunhu inodzora muyero wesimba mumuviri system. Ruzivo nezvezvimwe zvitoro zvemagetsi zvinogadzirwa muiyo hypothalamus iyo inodzora kudya uye kudya. Noradrenaline kusunga uye chiitiko mu hypothalamus ine kudzikisira mhedzisiro yekuda kudya. Mishonga yakadaro inosanganisira:

Sibutramine HCL (Meridia) CAS: 84485-00-7

Lorcaserin HCL (Belviq) CAS: 1431697-94-7

③ Rimonabant HCL CAS: 158681-13-1

DNP CAS: 119-26-6 

 

(2) Fat Burning

 

Mafuta anopisa kurasikirwa kwemishonga inogona kubatsira mafuta kurasikirwa kuburikidza nekuderedza zvido, kusimbisa metabolism, nekuchengetedza kudya kwakanaka. Vanogonawo kuwedzera kukwanisa kuita basa nekuwedzera simba nekuisa pfungwa. Mishonga yakadaro inosanganisira:

1. Synephrine CAS: 94-07-5

2. DMAA / 1,3-Dimethylpentylamine CAS: 13803-74-2

3. Clenbuterol HCL CAS: 21898-19-1

4. Salbutamol (Albuterol) CAS: 18559-94-9

 

(3) Kuvandudza kudya

 

Izvi zvinorema kurasikirwa nemishonga zvinoshanda nekupindira nekwanisi yekugadzirisa chirongwa ichi kuti iwane zvimwe zvokudya muzvokudya. Somuenzaniso, Orlistat inozivikanwa kuvhiringidza kuparara kwemafuta uye naizvozvo inodzivisa kudya kwemafuta. Zvimwe zvidimbu zvakawanda zvakashandiswa mukuderedza caloric absorption uye kudzivisa kudya. Muchikamu ichi, tichakurukura zvakawanda pamusoro pemishonga yakadaro inotevera:

Orlistat CAS: 96829-58-2

Cetilistat CAS: 282526-98-1

 


 

2018 Yakanakisisa-Kutengesa Kurasikirwa Kwehupfumi Kuwedzera Powder-Orlistat

 

Kurema kwesirudzo yezvinodhaka zvinodhaka

 

Pasi pane tsanangudzo shomanana asi yakajeka yemishonga yose inotaurwa pamusoro apa.

 

(1) Appetite suppressants (Zvokudya)

 

Sibutramine HCL (Meridia) CAS: 84485-00-7

Sibutramine HCL ndechimwe chezvinonyanya kuda kudya zvinodhaka. Iyo inokurudzira zvose serotonin uye NA mazinga muuropi, ayo anotevera kusungira kune avo vanogamuchira kuti vatarise satiety uye kudya.

Sibutramine kurapwa pamwe chete nekudya uye kurovedza muviri kunogona kuita kuti 4.6 kg kuwedzere kurashikirwa kupfuura kurovedza muviri uye kudya chete. Pamwe nekuderedza kudya kwekudya, sibutramine akawanikwawo kune:

• Simbisa thermogenesis
• Kuvandudza hutano hwepfungwa
• Kuvandudza hutano hwakanyanya
• Kuvandudza glucose yeropa kune varwere vanorarama nekodhi diabetes
• Kuvandudza huwandu hwepombi
• Kuwedzera mazinga eC-peptide, insulini, uye uric acid

Chimiro chimiro cheSibutramine HCL

 

Lorcaserin HCL (Belviq) CAS: 1431697-94-7

Kemikari yakagadzirwa naLorcaserin HCL (Belviq)

Lorcaserin HCl zvinodhaka zvinoshanda kuti zvironge simba rekugadzirisa muviri uye chido. Mushonga wacho wakagamuchirwa neRDA mugore re2012 kune vanhu vane BMI yepamusoro pe30, uye kune varwere vane Body Mass Index ye27 kana vamwe vanowedzera cholesterol, ropa, uye chirwere cheshuga 2. Mushonga wacho unoshandawo kusimbisa serotonin 2CV receptor muuropi hwevanhu inogona kubatsira varwere kuti vanzwe vakaguta mushure mekutora zvishoma.

Mune miedzo yezvechiremba, 38% yevanhu vakuru (vasina chirwere chechirwere cheshuga 2) vakarasikirwa kupfuura 5% yemuviri wavo, pakuenzanisa ne16% yevakuru vakarapwa ne placebo.

 

Rimonabant HCL CAS: 158681-13-1

Chimiro chimiro cheRimonabant HCL

Rimonabant HCL zvinodhaka zvakajeka nokuda kwomuitiro wayo wekuita sechisarudzo chisingaenzaniswi chinokonzerwa ne-cannabinoid-1 (CB-1) chinogamuchirwa. Endocannabinoids inosunungurwa muCSS uye inokurudzira lipogenesis, chido chekudya, uye kuunganidza mafuta mumhepo. IRimonabant HCL inoshanda kuti igadzirire endocannabinoids madhara.
Mushonga wacho unopinza nokukurumidza mushure mekutaura kwemuromo. Kubudirira kwechirwere ichi mukurapa vanyoro kana kuti kunyanya kuwandisa varwere kwakadzidzwa mune purogiramu yemayeri mana akachengetedzwa, anoromized, anozivikanwa seRIO (Rimonabant in Obesity) purogiramu. Mune miedzo iyi, Chirwere ichi chakawanikwa sechishanda se orlistat uye sibutramine.

 

DNP CAS: 119-26-6

2,4-Dinitrophenol (DNP kana 2,4-DNP o) inonzi organic makemikari ine chimiro uye chimiro chimiro: HOC6H3 (NO2) 2.

DNP inoshanda seprotonophore, ichiita kuti maprotoni adye mukati maro mukati memitochondrial membrane saka inodarika ATP synthase. Izvi zvingaita kuti ATP energy isanyanya kuderera. Somugumisiro, mamwe emasimba anoshandiswa kubva kumhepo inoputika anoparadzwa nenzira yehuni.

Iko kusashanda kwakanangana zvakananga nedosi yemushonga wakatorwa. Sezvo chinodhaka chemushonga chichiwedzera, kugadzirwa kwesimba kunova kusinganyanyi kushanda, mwero wemagetsi unokwira (uye huwandu hwakawanda hwemafuta hwatsva) kusangana nezvinodiwa nesimba uye kuripa kusashanda. DNP ndeimwe yeakanakisa mumiririri anozivikanwa nekusunungura oxidative phosphorylation. Phosphorylation yeADP neATP synthase inowana “kusabatanidzwa kana kubviswa kubva mukusanganiswa.

 


 

(2) Fat Burning Mechanism

 

Synephrine CAS: 94-07-5

Compound p-synephrine is alkaloid. Izvi zvinoreva kuti iyo inhengo yehupenyu inogona kuwanika mumasikirwo asi kuderera zvakanyanya. Iyo kemikari ine nitrogen senheyo.

Chimiro chimiro che synephrine

Caffeine, nicotine, uye morphine zvakare ndeyekirasi yealkaloids maererano nevatsvakurudzi. Synephrine inowanzoonekwa muzvokudya zvekudya zvinokonzera kuyerwa nekurema kana kurasikirwa uye mitambo yekuita.

Synephrine anoshanda sei mumuviri wedu?
Makemikari mu-p-synephrine anokonzera hurongwa hwemagetsi nekukurudzira β3 adrenergic receptors iyo inobatsira zvikuru mu thermogenesis uye inopolysis mumafuta ane mavara. Izvi zvinoreva kuti izvi zvinogamuchirwa zvichaita kuti hurongwa hwako hutsve mafuta nekuda kwesimba.

 

DMAA / 1,3-Dimethylpentylamine CAS: 13803-74-2

1,3-Dimethylpentylamine

Dimethylamylamine chirongwa chinogadzirwa zvakagadziridzwa mubazi. 1,3-dimethylamylamine (DMAA) inogadzirwa nemamphetamine yakashandiswa zvakanyanya mumitambo inowedzera inotengeswa muUnited States Yakanga iri kushandiswa pakutanga sechirongestantine yemasine. Mazuva ano, dimethylamylamine inoshambadzirwa semishonga inoshandiswa pakurasikirwa, ADHD (kucherechedza dambudziko rehutachiona hwehutano), kuvaka muviri, nekuvandudza kushanda.

 

Clenbuterol HCL CAS: 21898-19-1

Clenbuterol, Uyewo anozivikanwa seClen, inonzi decongestant uye bronchodilator. Inowanzoshandiswa kuchengetedza kurwisana nechirwere chemafi. Iyi iyi steroid-like compound, asi kwete steroid chaiyo. Inowira muboka re β2 agonists.

Clenbuterol inogona kutanga maitiro ehupenyu akafanana neAdrenaline. Iyo inobatsira beta-2 receptor subtypes mune imwe chirongwa chedrenergic. Izvi zvinokonzera kuwedzera kwemugomba (ATP's inogadziriswa inoda kuti mutauriri-mutauriri wehurukuro). Somugumisiro, protein kinase A inowedzera. Protein kinase A is enzyme inoronga lipid, glycogen, uye shuga metabolism. Kuwedzera kwayo kunoita kuti mafuta aipise mumuviri. Inokurudzira dzimwe nzira dzinobatsira pakupisa mafuta kuburikidza nehutano hwehupenyu hunozivikanwa se fatty acid oxidation.

Mafuta akapiswa zvino inoshandiswa senzvimbo ye simba yekuita mabasa emuviri. Iko inokurudzira mitochondria kusunungura ATPs, zvichiita kuti kuwedzerwa kwehuwandu hwemagetsi. Inonyanya kuzivikanwa kuti kuwedzerwa kwehuwandu hwemetabolism inobatsira mukurema kwekukura.

 

Salbutamol (Albuterol) CAS: 18559-94-9

kemikari yakagadzirwa naSalbutamol (Albuterol)

Salbutamol imishonga inobata chirwere chisingaperi chinoparadza zvirwere uye chirwere cheputi uye zvimwe zvirwere zvine chokuita neCOPD. Mishonga yemararamiro ekuvhura iri kuzarura kana kuputika mapapu 'kufema kufema panguva yekurwadza kwechirwere chemafi. Sezvo Salbutamol ine simba rinokurudzira, vamwe vanhu vanoshandisa ichi chirwere chechirma kukurudzira mafuta kana kuora muviri.

Albuterol yakakosha kuti ishandiswe mukurema kweprogram purogiramu nokuti ine zvimwe zvakafanana pane uyerogenic system sekuita muviri. Iyo inovaka huwandu hwemisungo uye inoderedza huwandu huwandu.
Yakashandiswa nevarimi vemiti kuti vape mafuta akawanda kubva munzvimbo dzomuviri wavo izvo zvingave zvakaoma kudzora kana kurasikirwa mafuta kuburikidza nemamwe nzira. Paunotora ichi chirwere chekuvaka muviri nekurema kwekuita mabasa, inowanzotorwa mupiritsi kana mazai emvura. Kunyangwe iwe ungashandisa Salbutamol inhaler kurema kana mafuta kurasikirwa kana ihwo chete sarudzo inowanikwa.

 


 

(3) Kuvandudza kudya

 

Orlistat CAS: 96829-58-2

Orlistat inonyanyisa pancreatic uye gastric lipase inhibitor. Zvose zvekudya zvinonzi triglycerides zvinogadziriswa nemubatsiro we pancreatic uye gastric lipases. Iyo inopisa enzymatically inoputsa pasi triglycerides muhusununguko husina mafuta acids iyo inogona kuve yakabatwa mumatumbo maduku. Gastric uye pancreatic lipase inhibitors zvakagadzikana nesangano repancreatic uye gastric lipases mu lumen yemukati muduku uye mudumbu zvichiita kuti ma enzymes aregone kushanda zvakanaka.

Kuburikidza nekudzivisa kwechiito chezviputika izvi, kudya kwemafuta kunodya kunodzivirirwawo, uye triglycerides inowedzerwa mumucheka. Orlistat kurasikirwa nemishonga kunodzivirira kumativi ose 30 muzana yemafuta ane utano kubva pakudya kubva pakupinda mumuviri wemunhu (apo 30 muzana yezvokudya muzvokudya zvinopiwa ne triglycerides). Ivhareji inorema kuderedza mushure megore rimwe nekubatanidzwa kweXenical (orlistat) uye kuchinja mumararamiro ehupenyu kune kambani 8.5 kg.

Pamwe nekudzikisa kudyidzana kwezvokudya zvinonzi triglycerides, orlistat kurasikirwa kwehupfu kwakawanikwa ku:
• Iva nemigumisiro yakanaka pamubhadharo weropa;
• Kuderedza cholesterol kunyanya uye saka cholesterol mazinga (pamwe neLDL cholesterol);
• Kuvandudza insulin kudzivisa; and
• Kukurudzira glycemic control.

Zvinonyanya kufungidzirwa kuti orlistat yemavhu inokonzera matambudziko anoshanda nenzira yakafanana nekusimudzira kusagadzikana, izvo zvinokurudzira avo vari pamishonga iyi kuti vateerere zvakakwana kudya kwakaderera-mafuta.

 

Cetilistat CAS: 282526-98-1

Cetilistat inomirira mumuromo, inova, pancreatic uye muviri lipase inhibitor.

Cetilistat kurasikirwa nekurasikirwa kwemishonga chirwere chinogadzirwa kurapa kuneta. Inoshanda nenzira imwecheteyo sezvakaita mishonga inokurukurwa kare inonzi Xenical (orlistat) nekudzora pancreatic lipase, iyo enzyme inoputsa triglycerides mumatumbo edu. Pasina idzi enzymes, triglycerides kubva kuzvokudya zvedu inodziviswa kuti irege kudyiwa muhurukuro yemafuta inogona kushandiswa uye inobviswa kubva mumuviri usina kupfuura.

Mumakiriniki ekuedzwa kunosanganisira varwere vanorema vasina chirwere cheshuga 2 uye mune varwere vakanyanya vanorarama nechirwere cheshuga 2. Apo Cetilistat kurasikirwa kwemafuta kwakapiwa kwemavhiki gumi nemaviri, zvakakosha zvikuru kuderedza muviri, huwandu hwecholesterol, serum low-density lipoprotein cholesterol nokukurumidza pakuenzanisa ne placebo.

Izvo zviyero zvevarwere vanorema zvakaratidza kuderedzwa kukuru muhutano hwekutanga hwemuviri wehutori huwandu hwe5 hwepamusoro hwakanga hwapamusoro pane zvese zvakashanda zvichienzaniswa ne placebo. Mukuwedzera kwehuwandu hwevanhu vane chirwere cheshuga, HbA1c (glycosylated hemoglobin) mazinga akanyanyawo kuderedzwa. Cetilistat kuora kurasikirwa kwemishonga kwakaratidza kuenzanisa kusvika kune zvinorwadza zvakanyanya, zvinowanzokonzera steatorrhea (kushaya muviri) uye ine chirwere chakanyanya kupfuura icho chiri mu orlistat. Iyi mishonga yakanga ichangobva kugamuchirwa muJapan kunobata kuneta nekumwe matambudziko.

 


 

2018 Yakanakisisa-Kutengesa Kurasikirwa Kwehupfumi Kuwedzera Powder-Orlistat

 

Kurema kwehupfumi kupfupiswa kwehupfu

 

Sezviri kuonekwa kubva pane zvatakanyatsokurukurirana, pane zvakawanda zvinorema kurasikirwa nemishonga kunze uko izvo zvakabva kune dzakawanda zvakasiyana-siyana masangano. Mishonga yemishonga iyi yakawanikwa ichibudirira, uye dzimwe dzadzo dzakagamuchirwa nemitemo dzakasiyana-siyana dzakadai seDefA neJapane, kutaura zvishomanana, pakurapa kuneta.

Mushure mekupedza maawa mazhinji tichitsvaga nezvekudzora uremu zvinodhaka, isu takakwanisa kuona mashoma e2018 World's Best-Selling Weight Loss Powder Supplements. Aya ekuremerwa kurasikirwa nehupfu zvinowedzera zvinosanganisira orlistat uremu hwekurasikirwa hupfu uye lorcaserin uremu hwekurasikirwa hupfu. Kusiyana nehurema hwekureruka zvekuwedzera zvinowanwa pane chero chitoro chezvinodhaka, iyi yekuremerwa uremu mishonga iyo yakatemwa nevezvehunyanzvi vakapfuura makore ekuyedzwa kuti vawane chitambi chekubvumidzwa kubva kuDFA nedzimwe nzvimbo dzinoverengeka. Isu tinokurudzira zvikuru kuti uedze iyi mishonga nekuti yakaratidza kuti haina kungoshanda chete asi zvakare yakachengeteka kushandisa.

 

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