Zowonjezera Kulemera kwa Mtengo wa Padziko Lonse la 2018 Powder Supply-Orlistat

 

kuwonda Mbiri ya Mankhwala

 

Mankhwala oyamba kulemera koyambirira, omwe amatchedwa ochepetsa mafuta panthaŵiyo, anakhalapo kumapeto kwa 1800s. Ngakhale mankhwalawa adayambitsa mavuto akuluakulu, adapitiriza kupezeka kuti agwiritsidwe ntchito mpaka 1960s.
Chithandizo chatsopano chotchedwa Dinitrophenol chinayambitsidwa mu 1930s ndipo chinakhala chotchuka kwambiri poyesa kulemera. Mankhwalawa amachititsa kuti thupi likhale lopweteka kwambiri, kuwonetsa kuchepa kwa thupi.
Pakatikati mwa 1950s, amphetamines anakhalapo ndipo anapezeka kuti ndi mankhwala olemetsa. Icho chinathandiza kuchepetsa kulemera kwa kupondereza njala. Chomvetsa chisoni n'chakuti, chinawonjezereka chiopsezo cha kupatsirana kwapachipatala, zomwe zimapangitsa kuti asiye ku msika ku 1968.

Mu 1970s, ephedrine adayikidwa mankhwala operekera kulemera. Mankhwalawa, komabe, adayambitsa zowawa zomwe zinachititsa kuti adziwidwe kuti ndizoopsa.
Mu 1973, fenfluramine inavomerezedwa ngati chowonjezera cholemetsa. Kutchuka kwake kunafalikira mu 1992 pamene unaphatikizidwa ndi phentermine kuti apange mankhwala olemera omwe amatchedwa fen-phen. N'zomvetsa chisoni kuti mankhwalawa anabweretsa mavuto ena, zomwe zinapangitsa kuti achoke ku msika ku 1997. M'nthawi ya 21st, mankhwala osokoneza bongo, ambiri ochokera ku zitsamba zopangira zitsamba, anasefukira pamsika.

 


 

Kuchuluka kwa mankhwala ochepetsa thupi

 

Mankhwala osokoneza bongo amagawidwa m'magulu akuluakulu atatu malinga ndi momwe amachitira ndi awa:

 

(1) Kudya chakudya chokwanira (Zakudya)

 

Mankhwala osokoneza bongo amatchedwa sympathomimetic agents. Kawiri kaŵirikaŵiri amaletsa chilakolako chofuna kudya panthawi yomwe amachititsa kuti satiyambe. Chisangalalo ndi "kukhuta" kumverera kapena kukhutira komwe kumapezeka popeza chakudya. Zofuna zokhudzana ndi kudya zimagwira ntchito pomatsanzira khungu la ubongo mu ubongo wa umunthu lomwe limayambitsa chilakolako, lotchedwa noradrenaline (NA).

Mankhwalawa amagwiritsa ntchito mankhwala ofanana ndi NA ndipo angathe; Zotsatira zake zimamanga zovomerezeka zofanana ndi noradrenaline.

Mankhwala a sympathomimetic othandizira.

Mankhwalawa amathandizanso ntchito ya noradrenaline mu "malo odyetsera" aubongo wamunthu, hypothalamus. Hypothalamus ya munthu imayang'anira mphamvu zamagetsi mthupi. Chidziwitso chazogulitsa zamagetsi chimapangidwa mu hypothalamus yomwe imayang'anira kudya ndi kudya. Kumanga kwa Noradrenaline ndikuchita mu hypothalamus kumachepetsa njala. Mankhwalawa ndi monga:

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

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

③ Rimonabant HCL CAS: 158681-13-1

DNP CAS: 119-26-6 

 

(2) Fat Burning

 

Mafuta otentha kwambiri mankhwala angathe kuthandiza kutaya mafuta pochepetsa zilakolako, kupititsa patsogolo kagayidwe kake, ndi kukhala ndi chilakolako chabwino. Angathandizenso kuchita masewera olimbitsa thupi powonjezera mphamvu ndi kuganizira. Mankhwalawa ndi awa:

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) Kukulitsa chimbudzi

 

Mankhwalawa amatayika chifukwa amatha kusokoneza zakudya zomwe zimadya zakudya. Mwachitsanzo, Orlistat imadziwika kuletsa kuwonongeka kwa mafuta ndipo imalepheretsa kutaya mafuta. Zakudya zina zambiri zakhala zikugwiritsidwa ntchito pochepetsa caloric absorption ndi kuletsa chimbudzi. M'nkhaniyi, tikambirana zambiri za mankhwala awa:

Chuma cha Orlistat: 96829-58-2

CAS Ceististat: 282526-98-1

 


 

Zowonjezera Kulemera kwa Mtengo wa Padziko Lonse la 2018 Powder Supply-Orlistat

 

Kulongosola kwa mankhwala ochepetsa thupi

 

M'munsimu muli tsatanetsatane mwachidule cha mankhwala onse otchulidwa pamwambapa.

 

(1) Kudya chakudya chokwanira (Zakudya)

 

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

Hutramirine HCL ndi imodzi mwa zovuta zowonongeka. Zimathandiza kuti tizilombo ta serotonin ndi NA mu ubongo, kenaka tizimangirira kuti tizilombo toyambitsa matenda tizilombo toyambitsa matenda.

Chithandizo cha Sibutramine pamodzi ndi zakudya ndi masewera olimbitsa thupi zingachititse 4.6 makilogalamu ambiri kulemera kuposa kuchita masewera olimbitsa thupi komanso zakudya zokha. Kuwonjezera pa kuchepetsa kudya, sibutramine wapezeka kuti:

• Limbikitsani thermogenesis
• Kukulitsa zoopsa za mtima
• Kuwonjezera kunenepa kwambiri
• Kukulitsa shuga m'magazi kwa odwala ali ndi matenda a shuga
• Kukulitsa mafilimu
• Kumachepetsa zigawo za C-peptide, insulini, ndi uric acid

Maonekedwe a mankhwala a HCL ya Sibutramine

 

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

Mankhwala a Lorcaserin HCL (Belviq)

Mankhwala a Lorcaserin HCl amagwira ntchito kuti athetse kuchepa kwa thupi ndi chilakolako. Mankhwalawa adavomerezedwa ndi FDA m'chaka cha 2012 kwa anthu omwe ali ndi BMI yoposa 30, komanso odwala omwe ali ndi Thupi la Mass Body la 27 kapena ena omwe ali ndi cholesterol, magazi, komanso matenda a shuga a 2. Mankhwalawa amagwiranso ntchito polimbikitsa serotonin 2CV receptor mu ubongo waumunthu umene ungathandize odwala kuti azikhala okhudzidwa atatha kumwa pang'ono.

M'mayesero a zachipatala, 38% akuluakulu (opanda mtundu wa 2 shuga) ataya zoposa 5% za kulemera kwa thupi, poyerekeza ndi 16% ya akuluakulu omwe amachitira mankhwalawa.

 

Rimonabant HCL CAS: 158681-13-1

Mankhwala a Rimonabant HCL

Mankhwala a Rimonabant HCL ndi osiyana chifukwa cha njira yake yatsopano yomwe imasankhidwa kuti ikhale yosakanikirana ndi mayina a cannabinoid-1 (CB-1). Endocannabinoids amamasulidwa mu CNS ndipo amachititsa lipogenesis, kudya, ndi mafuta kudzikundikira mu periphery. Rimonabant HCL ikugwira ntchito kuti zisawononge zotsatira za endocannabinoids.
Mankhwalawa amamwa mofulumira pambuyo poyendetsa pamlomo. Kupambana kwa mankhwalawa pochiza odwala olemera kwambiri kapena owonjezera kunenepa kunawerengedwa pulogalamu ya mayesero anayi osayenerera, omwe amadziwika kuti RIO (Rimonabant in Obesity). Mu mayesero awa, mankhwalawa amapezeka kuti ndi othandiza monga orlistat ndi sibutramine.

 

DNP CAS: 119-26-6

2,4-Dinitrophenol (DNP kapena 2,4-DNP o) ndi mankhwala omwe amapangidwa ndi mankhwala awa: HOC6H3 (NO2) 2.

DNP imagwira ntchito monga protonophore, kulola kuti mapulotoni alowerere mkati mwa mimbachondrial membrane choncho amadutsa ATP synthase. Izi zimapangitsa ATP mphamvu kusakanikirana bwino. Zotsatira zake, mphamvu zina zomwe zimapangidwa kuchokera ku kupuma zimawonongedwa ngati kutentha.

Kulephera kwake kumagwirizana molingana ndi kuchuluka kwa mankhwala omwe atengedwa. Pamene kuchuluka kwa mankhwala kumawonjezeka, mphamvu zamagetsi zimayamba kukhala zosagwira ntchito, kuchuluka kwa kagayidwe kake kumakwera (ndipo mafuta ochulukirapo amawotchedwa) kuti akwaniritse zofunikira zamagetsi ndikubweza kusowa kwa ntchito. DNP ndi imodzi mwazida zodziwika bwino zosokoneza phosphorylation ya okosijeni. Phosphorylation ya ADP yolembedwa ndi ATP synthase imatha "kusungunuka kapena kutayilidwa ndi makutidwe ndi okosijeni.

 


 

(2) Njira Yopsa Moto

 

Synephrine CAS: 94-07-5

P-synephrine palimodzi ndi alkaloid. Izi zikutanthawuza kuti ndilo gulu lachilengedwe limene lingapezeke mwachilengedwe koma kuchepa kwakukulu. Kompositi ili ndi nayitrogeni monga maziko.

Mankhwala a synephrine

Kafeine, chikotini, ndi morphine zimakhalanso m'gulu la alkaloids malinga ndi ofufuza. Synephrine amawonekeratu mu zakudya zowonjezera zakudya zothandizira kulemera kwa thupi kapena kutayika ndi masewera.

Kodi Synephrine amagwira ntchito bwanji m'thupi lathu?
Mankhwala p-synephrine amakhudza dongosolo la mitsempha mwa kulimbikitsa β3 adrenergic receptors zomwe zimathandiza kwambiri mu thermogenesis ndi kuzimitsa mafuta obiriwira. Izi zikutanthauza kuti mapulogalamuwa amathandiza kuti maofesi anu aziwotcha mafuta.

 

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

1,3-Dimethylpentylamine

Dimethylamylamine ndi mankhwala opangidwa mwaluso mu labu. 1,3-dimethylamylamine (DMAA) ndi chivomezi cha amphetamine chomwe chagwiritsidwa ntchito mochulukira mu masewera olimbitsa masewera ogulitsa ku US Anali kugwiritsidwa ntchito poyamba ngati mankhwala osokoneza bongo. Masiku ano, dimethylamylamine imagulitsidwa ngati mankhwala osokoneza bongo omwe amagwiritsidwa ntchito polepheretsa kulemera, ADHD (kuchepa kwa matenda osokoneza bongo), kumangirira thupi, ndi kupititsa patsogolo ntchito.

 

Clenbuterol HCL CAS: 21898-19-1

Clenbuterol, Wodziwika kuti Clen, ndi decongestant ndi bronchodilator. Amagwiritsidwa ntchito kuteteza motsutsana ndi masewera a mphumu. Izi ndizigawo ngati steroid, koma osati steroid yeniyeni. Amagwera m'gulu la β2 agonists.

Clenbuterol ikhoza kuyambitsa zochitika za thupi monga zofanana ndi adrenaline. Zimayambitsa beta-2 receptor subtypes mu dongosolo la adrenergic. Izi zimapangitsa kuchuluka kwa cAMP (chotsatira cha ATP chomwe chimafunikira kuyankhula pamsewu). Chifukwa chake, puloteni kinase A ikuwonjezeka. Mapuloteni kinase A ndi mavitamini omwe amachititsa kuti lipiritsi, glycogen, ndi shuga zamagetsi zichitike. Kuwonjezeka kwake kumapangitsa mafuta kutentha thupi. Zimapanganso njira zina zomwe zimathandiza kutentha ma mafuta kudzera m'thupi lomwe limatchedwa mafuta a asidi okosijeni.

Mafutawa amatenthedwa ndiye amagwiritsidwa ntchito ngati magwero a mphamvu zogwira ntchito. Zimayambitsa mitochondria kumasula ATPs, zomwe zimapangitsa kuchuluka kwa kuchuluka kwa mankhwala. Ambiri amadziwika kuti kuwonjezeka kwa chiwerengero cha kagayidwe kamene kamathandizira kuchepetsa thupi.

 

Salbutamol (Albuterol) CAS: 18559-94-9

mankhwala a Salbutamol (Albuterol)

Salbutamol ndi mankhwala omwe amachititsa matenda osokoneza bongo ndi mphumu kapena zovuta zina zokhudzana ndi COPD. Momwe mankhwala amachitira ndikutsegula kapena kuchepetsa mapepala a kupuma m'mapapo panthawi yovutitsa mphumu. Popeza Salbutamol ili ndi mphamvu, anthu ena amagwiritsira ntchito mankhwalawa a pumu pofuna kulimbikitsa mafuta kapena kulemera.

Albuterol ndi yabwino kugwiritsa ntchito pulogalamu yochepetsera kulemera chifukwa imakhala ndi zotsatira zofanana pa njira ya androgenic monga machitidwe olimbitsa thupi. Zimamanga minofu ya minofu ndi kuchepetsa kulemera kwake.
Zagwiritsidwa ntchito ndi olimbikitsa thupi kuti azidula mafuta owonjezera kuchokera kumadera a thupi lawo zomwe zingakhale zovuta kulamulira kapena kutayika mafuta kudzera mwa njira zina. Pogwiritsa ntchito mankhwalawa pofuna kumanga thupi ndi kulemera kwa thupi, nthawi zambiri amatengedwa mu mapiritsi kapena mawonekedwe a madzi. Ngakhale mutagwiritsa ntchito Salbutamol kulemera kwake kutaya mafuta ngati ndi njira yokhayo yomwe ilipo.

 


 

(3) Kukulitsa chimbudzi

 

Chuma cha Orlistat: 96829-58-2

Orlistat ndipamwamba kwambiri paccatic ndi gastric lipase inhibitor. Zakudya zonse za triglycerides zimagwiritsidwa ntchito mothandizidwa ndi pancreatic ndi chapamimba lipases. Lipases limapangitsa kuti triglycerides iwononge mafuta omwe amatha kutengeka m'matumbo aang'ono. Gastric ndi pancreatic lipase inhibitors zimapanga mgwirizano ndi phulusa ndipo chapamimba chimatulutsa kuwala kwa m'mimba komanso m'mimba zimapangitsa kuti mavitaminiwa asagwire bwino ntchito.

Kupyolera mu chiopsezo cha ntchito ya lipases, zakudya zamagetsi zimayambanso kuthira, ndipo triglycerides zimatulutsidwa mu nyansi. Mankhwala osokoneza bongo amachititsa kuti pakhale peresenti ya 30 ya mafuta odya kuchokera ku chakudya cha thupi (pamene 30 peresenti ya mphamvu yodyera imaperekedwa ndi triglycerides). Kuchuluka kwa kuchepetsa kulemera kwa chaka chimodzi ndi kuphatikiza kwa Xenical (orlistat) ndi kusintha kwa moyo ndikuzungulira 8.5 kg.

Pamodzi ndi kuchepetsa kuyamwa kwa zakudya za triglycerides, orlistat weight loss powder yapezeka:
• Khalani ndi zotsatira zabwino zokhuza magazi;
• Kuchepetsa kuyamwa kwa kolesteroloni ndiyeno mafuta a cholesterol (pamodzi ndi LDL cholesterol);
• Kupititsa patsogolo kuteteza insulini; ndi
• Kuwonjezera kuyendetsa glycemic.

Anthu ambiri amaganiza kuti mankhwala a orlistat amachititsa kuti azikhala olimbikitsana, zomwe zimalimbikitsa anthu omwe amamwa mankhwalawa kuti azigwiritsira ntchito zakudya zochepa.

 

CAS Ceististat: 282526-98-1

Cetilistat ndi ammimba, buku, pancreatic ndi m'mimba lipase inhibitor.

Mankhwala osokoneza bongo a mankhwalawa ndi mankhwala omwe amapangidwa kuti athetse kunenepa kwambiri. Zimagwiranso ntchito mofananamo monga mankhwala omwe atchulidwa kale kuti Xenical (orlistat) mwa kulamulira pancreatic lipase, puloteni yomwe imaphwanya triglycerides m'matumbo athu. Popanda mavitamini awa, triglycerides kuchokera ku chakudya chathu saloledwa kudyetsedwa mu mafuta omwe amatha kutengeka ndi kuchotsedwa ku thupi losagwiritsidwa ntchito.

M'mayesero am'chipatala odwala ochepa omwe alibe mtundu wa shuga wa 2 komanso odwala ambiri omwe ali ndi matenda a shuga a 2. Pamene Cetilistat kutayika kwa ufa kunkaperekedwa kwa milungu khumi ndi iwiri, iyo imachepa kwambiri thupi, cholesterol chokwanira, serum yothamanga lipoprotein cholesterol mofulumira poyerekezera ndi placebo.

Chiwerengero cha odwala kwambiri omwe akuwonetsa kuchepa kwakukulu kulemera kwake kwa thupi kwa osachepera 5 peresenti chinali chapamwamba mu mikono yonse yogwira poyerekeza ndi placebo. Odwala odwala kwambiri a shuga, ma HbA1c (ma glycosylated hemoglobin) anagwedezeka kwambiri. Mankhwala osokoneza bongo amachititsa kuti thupi likhale lopweteka kwambiri, ndipo limayambitsa steatorrhea (chibadwa cha m'mimba) chokhala ndi chiwerengero chocheperapo kusiyana ndi chomwe chimapangika mu orlistat. Mankhwala awa adalandiridwa posachedwapa ku Japan kuti athetse kunenepa ndi mavuto ena.

 


 

Zowonjezera Kulemera kwa Mtengo wa Padziko Lonse la 2018 Powder Supply-Orlistat

 

Kuchepetsa kuperewera kwa mpweya wofiira

 

Monga momwe tawonera pamakambirano athu, pali mankhwala ambiri ochepetsa kulemera komwe kumachokera ku mitundu yosiyanasiyana ya mankhwala. Ambiri mwa mankhwalawa apezeka kuti ali othandiza, ndipo ena avomerezedwa ndi maulamuliro osiyanasiyana monga FDA ndi Japan, kutchula owerengeka, kuti athetse kunenepa kwambiri.

Pambuyo pokhala maola ochuluka tikufufuza za mankhwala ochepetsa kunenepa, tinatha kuzindikira zowonjezerapo za 2018 Zogulitsa Zabwino Kwambiri Padziko Lonse. Izi zowonjezera kulemera kwa ufa zimaphatikizapo orlistat kuwonda kwa ufa ndi lorcaserin kuwonda kwa ufa. Mosiyana ndi zoperewera zamafuta ochepetsa thupi omwe amapezeka m'sitolo iliyonse, mankhwala ochepetsa thupi omwe adalamulidwa ndi akatswiri azachipatala adutsa zaka zoyesedwa kuti apeze chidindo chovomerezedwa ndi a FDA ndi madera ena angapo. Tikukulimbikitsani kuti muyesere mankhwalawa chifukwa atsimikiziridwa kuti siwothandiza komanso otetezeka kugwiritsa ntchito.

 

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