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Dapoxetine HCL ufa

mlingo:
5.00 kuchokera 5 kutengera 1 kasitomala mlingo
SKU: 129938-20-1. Category:

AASraw ili ndi kaphatikizidwe ndi kupanga kupanga kuchokera ku gramu kuti ikhale yaikulu ya Dapoxetine hydrochloride powder (129938-20-1), pansi pa malamulo a CGMP ndi dongosolo loyendetsa khalidwe labwino.

Dapoxetine hydrochloride ndi buku laling'ono lomwe limasankha serotonin reuptake inhibitor amaligwiritsa ntchito kuti asamangidwe msanga kwa amuna. Kuthamangira kusanayambe (PE) ndi vuto lodziwika kwambiri la kugonana kwa amuna, lomwe likuyenera kuti limakhudza anthu 30%. Dapoxetine hydrochloride ndi ndondomeko yowonongeka yomwe imagwiritsidwa ntchito ngati serotonin yowonjezeranso kubwezeretsa. Zimapereka kusintha kwa magawo angapo okhudzana ndi kuyamwa msanga msanga m'mayesero a zachipatala. Chogulitsira ichi chafunidwa kuti afufuze ndi ntchito zogwirira ntchito.

Mafotokozedwe Akatundu

Dapoxetine hydrochloride anesthesia powder kanema


Yaikulu Dapoxetine hydrochloride anesthesia powder zoyambirira otchulidwa

Name: Dapoxetine hydrochloride
CAS: 129938-20-1
Makhalidwe a Maselo: C9H7ClN2O5
Kulemera kwa maselo: 258.62
Melt Point: 175-179 ° C
Kusungirako nyengo: -20 ° C Freezer
mtundu; White crystalline powder


Dapoxetine ndi gulu lopangidwa ndi gulu la mankhwala omwe amawasankha a serotonin reuptake koma opanda anti-depressant effect. Mankhwalawa amapangidwa mwakhama kuti asamalidwe msanga pakati pa amuna akuluakulu pakati pa zaka za 18 ndi 64 omwe amakwaniritsa zofunikira izi:

1. Kupitilira kapena kubwereza mobwerezabwereza kwa mbolo musanayambe, pakapita nthawi, kapena mwamsanga mutalowa mukazi, ndipo kokha musanakhale osakhutira ndi kugonana;

2. Zovuta zaumwini zaumwini kapena zosiyana ndizokha chifukwa chokhazikika msanga (PE);

3. Kulephera koyendetsa kukakamiza.

Mankhwala a Dapoxetine

Puloteni ya Dapoxetine hydrochloride ndi piritsi yofiira, yomwe imakhala yoyera kapena yofiira pambuyo pochotsedwa.

Chofunika chachikulu: Dapoxetine hydrochloride.

IUPAC Name: (1S)-N,N-dimethyl-3-naphthalen-1-yloxy-1-phenylpropan-1-amine

Dapoxetine HCL ufa

1. Thupi la 2D:

2. 3D Conformer:

Fomu ya maselo: C21H23NO

Kulemera kwa maselo: 305.421 g / mol

CAS: 119356-77-3

Kulongosola kosavuta kwa Dapoxetine

Pakalipano, palibe lamulo lapadera la chithandizo cha mankhwala osakaniza msanga ndi mapiritsi a dapoxetine hydrochloride. Palibe malamulo enieni omwe mankhwalawa amagwiritsidwa ntchito pakamwa. Zimadalira kukula kwake kwa zizindikiro za kukwera msanga. Vuto la mankhwala ndi losiyana. Nthaŵi ya mankhwala siingakhoze kupangidwira. Komabe, mankhwalawa amatha kusintha zizindikiro za kukwera msanga, kotero odwala akhoza kumwa mankhwala malinga ndi zizindikiro zawo.

Dapoxetine makamaka amagwiritsidwa ntchito pochiza 18 kwa 64 wamwamuna wamwamuna wosakonzekera msanga (PE) omwe amakumana ndi mavuto onsewa, kuphatikizapo:

1. Penis ndi yaing'ono, isanafike, kapena itangotha ​​kumene kulowa mukazi, komanso asanakondweretse kugonana. Zokakamiza kugonana ndizopitilira kapena kubwereza kukweza;

2. Zovuta zaumwini zaumwini kapena zosiyana ndizokha chifukwa chokhazikika msanga (PE);

3. Kusokoneza kosavuta kutsegula.

Dapoxetine yatsimikiziridwa kale ngati mankhwala ku Ulaya ndi United States monga kukhala ndi zotsatira zabwino pa chithandizo cha kukwera msanga. Mukatenga dapoxetine, serotonin, chinthu chomwe chili mu ubongo, imabisika. Serotonin iyi ndi chinthu chomwe chimayambitsa chisangalalo cha ubongo kapena chimabweretsa zotsatira zosangalatsa. Kuvutitsa ndi chisangalalo zimathetsedwa, zotsatira za adrenaline zimachepetsanso, kotero kuti kutsegulira nthawi kumatha kuchedwa.

Dapoxetine hydrochloride ikhoza kulepheretsa 5-HT kubwezeretsa kachilomboko ndikuonjezeretsa 5-HT mu synaptic cleft poletsa 5-HT zotumiza. Kafukufuku wasonyeza kuti dapoxetine amalepheretsa kutentha kwajakisoni, ndipo chimake chachikulu chazitsulo ndizofunika kwambiri. Pamene dapoxetine imakhala yotalika kwambiri, njira yothetsera mapuloteni ya monoamine ikhoza kuimitsidwa, ndipo kubwezeretsedwa kwa dopamine kumatetezedwanso. Dapoxetine imachulukitsa nthawi ya pudendal motor neuron reflexes ndipo imapangitsa ntchito yogonana.

Kodi zimatengera nthawi yaitali bwanji kuti mapiritsi a dapoxetine hydrochloride akhale ogwira ntchito? Chithandizo chimadalira kukula kwake kwa zizindikiro za kukwera msanga. Kuvuta kwa mankhwala ndi kosiyana, ndipo nthawi ya kumwa mankhwala ndi yosiyana.

Njira yothandizira Dapoxetine

Mmene zochita za dapoxetine zimagwiritsira ntchito mankhwala ochizira msanga zingakhale zogwirizana ndi kulepheretsa kubwezeretsa serotonin ndi neuroni, motero zimakhudza kusiyana kwa odwala matenda opatsirana pogwiritsa ntchito mapuloteni asanayambe komanso pambuyo pa maselo.

Dapoxetine imathandizira kukwera msanga kwa nthawi yaying'ono chifukwa imakhala ndi zotsatira zowonjezera serotonin yowonjezera chisangalalo mu ubongo.

Serotonin kawirikawiri imabweretsedwanso kuchoka ku synapse, koma kutenga dapoxetine imalepheretsa kubwezeretsa kachilomboka ndi kudyetsa serotonin.

Serotonin imatsitsa dopamine yomwe imapangitsa chisangalalo, nkhawa, ndi adrenaline zomwe zimatuluka pamene mukuchita mantha, kotero mukhoza kutalikitsa nthawi yokwanira kuti ejaculate. Dapoxetine imatha kukwera msanga kwa nthawi yayitali chifukwa imapangitsa kuti serotonin iwonjezere chisangalalo mu ubongo.

Serotonin kawirikawiri imabweretsedwanso kuchoka ku synapse, koma kutenga dapoxetine imalepheretsa kubwezeretsa kachilomboka ndi kudyetsa serotonin.
Serotonin imatsitsa dopamine yomwe imapangitsa chisangalalo, nkhawa, ndi adrenaline zomwe zimatuluka pamene mukuchita mantha, kotero mukhoza kuchepetsa nthawi kuti mukhale ndi ejaculate.

Kuthamangitsidwa kwa anthu kumaphatikizidwa kwambiri ndi dongosolo lamanjenje lachisomo. Njira yowonongeka yopangidwira imachokera ku malo osungunuka a msana, omwe amayimira pakati pa ubongo, womwe umakhudzidwa ndi ubongo wa ubongo (chithunzithunzi chamkati choyamba ndi khungu la hypoventricular paraventricular).

Dapoxetine HCL Pharmacokinetics

Pambuyo pa mauthenga a m'kamwa, dapoxetine imadziwika mofulumira ndipo imatha kufika pamtundu wambiri wa mankhwala a plasma (Cmax) pambuyo pa maola pafupifupi 1-2. Mtheradi wa bioavailability ndi 42% (wosiyana 15-176%). Pambuyo poyendetsa kamodzi kamodzi ka 30 mg ndi 60 mg ya dapoxetine mu nthawi ya kusala, chiwerengero cha plasma (297 ng / ml ndi 498 ng / ml, mwachitsanzo) chinafikira pambuyo pa 1.01 ndi ma 1.27 maola. Kusakaniza kwa zakudya zamtengo wapatali kungathe kuchepetsa Cmax (10%) ya dapoxetine ndi kuwonjezera moyenera AUC (12%), komanso kuchepetsa kuchepa kwa dapoxetine; Komabe, kudya kwambiri mafuta Zakudya sizimakhudza momwe mungathere. Palibe kusintha kumeneku kumakhala ndi tanthauzo lachipatala. Bentley ikhoza kutumikiridwa ndi kapena popanda chakudya.

Pambuyo polamulidwa ndi thupi la munthu mwa jekeseni wothandizira, miyeso yoyambirira, pakati, ndi yotsiriza ya moyo wa dapoxetine ndi 0.10, 2.19, ndi ma 19.3 maola.

Ma metabolites a dapoxetine excreted amachotsedwa kwambiri ndi mkodzo mu conjugate mkhalidwe. Palibe mankhwala ogwira ntchito omwe anapezeka mu mkodzo. Dapoxetine imachotsedwa mofulumira, ndipo umboni uli pansi pazigawo zamagazi maola 24 pambuyo pa maulamuliro (osachepera 5% ya chiwerengero chapamwamba). Mlingo wa tsiku ndi tsiku wa dapoxetine ndi wochepa kwambiri. Nthenda ya moyo yotsiriza ya mauthenga oyamwa ndi pafupifupi maola 19. Theka la moyo wa desmethyl dapoxetine ndi ofanana ndi dapoxetine.

Kugwiritsira ntchito Dapoxetine

Kuchiza kwa odwala amuna omwe ali ndi vuto loyamba msanga (PE)

Ma pulogalamu ya Dapoxetine hydrochloride angathe kuthandizira kuyanjanitsa mphamvu; kulimbikitsa kwambiri moyo wokhudzana ndi kugonana; Kuwonjezera kutalika kwa ejaculation latency.

Pamene akugwiritsa ntchito mankhwala, odwala angagwiritsenso ntchito njira zochepetsera zizindikiro zowonongeka msanga, kusintha maganizo, kulimbitsa mgwirizano pakati pa mwamuna ndi mkazi, chakudya chamaganizo, kulimbitsa thupi, kuchita masewera olimbitsa thupi, komanso kuchita nawo masewera olimbitsa thupi sabata iliyonse. Ndibwinonso kusewera mpira ndi kusewera mpira wa basketball kuti mukhale ndi thupi labwino komanso kuchepetsa nkhawa.

Mlingo wa Dapoxetine

Mlingo wa mapulogalamu a dapoxetine hydrochloride ndi olankhula, ndipo mapiritsi ayenera kumeza bwino; odwala amalangizidwa kuti atenge kapu imodzi yamadzi kuti amwe mankhwala; odwala ayenera kuyesetsa kupeŵa kuvulala chifukwa cha zizindikiro za prodromal monga syncope kapena chizungulire.

Mapiritsi a dapoxetine hydrochloride analimbikitsa odwala onse akuluakulu (18 mpaka 64) ali ndi 30 mg ndipo ayenera kuthandizidwa pa 1 maola 3 asanayambe kugonana. Ngati zotsatirazi sizikhutiritsa mutatenga 30mg ndipo zotsatira zake zimakhalabe pamtundu woyenera, mlingo ukhoza kuwonjezeka kufika ku 60mg ya mlingo woyenera kwambiri.

Mankhwala otsimikiziridwa oterewa amagwiritsidwa ntchito maola onse a 24.
Okalamba (okalamba a 65 ndi apamwamba) Katunduyu sanaganizidwe zaka za 65 komanso chitetezo ndi chithandizo kwa odwala pazogwiritsidwa ntchito, chifukwa chachikulu chomwe chidziwitso cha mankhwalawa chikugwiritsidwa ntchito mwa anthuwa n'chochepa kwambiri kwa odwala omwe ali ofatsa Kuwonongeka kwa chiwerewere kapena Odwala omwe ali ndi vuto la impso sayenera kusintha mlingo podula mankhwalawa, koma ayenera kusamala. Chida ichi sichiri chovomerezeka kwa odwala okhala ndi vuto lalikulu la impso.

Dapoxetine Zizindikiro:

Chogulitsira mankhwalachi ndicholinga chochizira odwala amuna omwe ali ndi msinkhu wosapitirira msinkhu (PE) pakati pa zaka za 18 ndi 64 omwe amakumana ndi zovuta zonsezi: mbolo ikupitirira mpaka italowetsedwa mukazi, nthawi kapena posakhalitsa, komanso kukondweretsa kugonana kumatheka, kokha chifukwa cha kukwiya kochepa. Kapena kubwereza mobwerezabwereza; ndi zovuta zenizeni zaumunthu kapena zosiyana siyana chifukwa chokhazikika msanga (PE); komanso kulamulira kosavuta kutsegula.

(1) Amuna akuluakulu (18 kwa zaka 64)

Limbikitsani mlingo woyamba wa 30 mg kwa odwala onse ndipo muyenera kutenga 1 maola 3 musanagonane. Ngati zotsatirazi sizikhutiritsa mutatenga 30mg ndipo zotsatira zake zimakhalabe pamtundu woyenera, mlingo ukhoza kuwonjezeka kufika ku 60mg ya mlingo woyenera kwambiri. Mankhwala otsimikiziridwa oterewa amagwiritsidwa ntchito maola onse a 24. Chida ichi chingatengedwe asanadye kapena pambuyo pa chakudya.

Ngati dokotala asankha mankhwalawa kuti asamangidwe msanga, ayenera kuwonetsa chiopsezo ndipo wodwala atsimikiziridwa kuti apindula kwa masabata oyambirira a 4 mutagwiritsa ntchito mankhwalawa, kapena kuyesa kulandira phindu la wodwalayo atagwiritsa ntchito mlingo wa mankhwala a 6 ndi kusankha kaya apitirize kugwiritsa ntchito mankhwalawa.

(2) Okalamba (zaka 65 ndi zaka zambiri)

Kafukufuku sanayambe kuwonetsa kuti mankhwalawa ndi otetezeka ndi ogwira mtima kwa odwala omwe ali ndi zaka 65 ndi kupitirira. Chifukwa chachikulu cha izi ndikuti chidziwitso chogwiritsira ntchito chida ichi chiwerengerochi n'chochepa kwambiri.

(3) Ana ndi achinyamata

Chogulitsira ichi sichinagwiritsidwe ntchito ndi anthu osasinkhu wa 18.

Pulogalamu imodzi panthawi ingatengedwe kosatha. Mankhwalawa amafunika kutengedwa pamimba yopanda kanthu. Ndi bwino kumwa tiyi musanagwiritse ntchito bwino mankhwalawa asanayambe ntchito yabwino yoyendera, malinga ndi matenda awo kwa dokotala kapena wamasitolo omwe amauza ndi chitetezo chokonzekera mankhwala kuti asagwiritse ntchito molakwika mankhwala osokoneza bongo, koma osawonjezereka mopanda malire Kugwiritsa ntchito mankhwala mobwerezabwereza Muyenera kutsatira ndondomeko ya dokotala komanso manyazi.

Kuchuluka kwa Dapoxetine

Kawirikawiri, zizindikiro zowonjezereka kwa serotonin reuptake inhibitor zikuphatikizapo serotonin-zosokoneza zomwe zimakhala zovuta monga kutaya thupi, kuchepa kwa m'mimba, kutaya, kusanza, kusangalala, chizungulire ndi tachycardia. Pankhani yowonjezereka, njira zothandizira ziyenera kuchitidwa ngati pakufunika. Pakalipano palibe mankhwala enieni a mankhwalawa.

Malangizo a Dapoxetine HCL

1. Zisamaliro zonse. Dapoxetine imagwiritsidwa ntchito kwa odwala omwe ali ndi vuto loti asanamalize msanga. Chitetezo cha Dapoxetine mwa amuna omwe alibe msambo wosamba msanga sichimveka bwino. Panthawi imodzimodziyo, palibe deta potsatira zotsatira za Dapoxetine pochedwa kuchepetsa kukwera kwa anthu. Ndikoyenera kuti odwala sayenera kutenga Beverly ndi "zosokoneza bongo" panthawi imodzimodzi chifukwa zotsatira zake sizidziwika ndipo zochitika zovuta zimachitika.

2. Odwala amalangizidwa kuti asatenge mankhwala osokoneza maganizo a m'maganizo pamene akuwutenga.

3. Pewani kumwa mowa mukatenga Dapoxetine.

4. Gwiritsani ntchito Dapoxetine kungayambitse syncope kapena chizungulire

5. Tengani cytochrome yochepa P450 3A4 inhibitors monga erythromycin, clarithromycin, fluconazole, verapamil ndi diltiazem.

6. Tengani mankhwala amphamvu a cytochrome P450 2D6 inhibitor kapena odziwika bwino a cytochrome P450 2D6 Odwala omwe ali ofooka a metabolism ayenera kukhala osamala poonjezera mlingo ku 60 mg, chifukwa izi zingapangitse kuwonjezereka, zomwe zingathe kutsogolera kuchitidwa choipa kwambiri chokhudzidwa ndi mlingo.

7. Zopindulitsa siziyenera kugwiritsidwa ntchito kwa mania / odwala omwe ali ndi mbiri ya matenda a hypomanic kapena bipolar, panthawi yomweyi, wodwalayo ali ndi zizindikiro za matenda otchulidwa pamwambawa ayenera kuthetsedwa ndi Dapoxetine.

8. Chifukwa chakuti serotonin yochepetsanso kachilombo koyambitsa matenda imatha kuchepetsa chifuwa cha khunyu Mtengo, wodwala aliyense amene akudwala matendawa ayenera kusiya, ndipo odwala omwe ali ndi khunyu osakhazikika ayenera kupeŵa kugwiritsa ntchito Dapoxetine.

9. Dapoxetine sayenera kugwiritsidwa ntchito kwa anthu osapitirira zaka 18.

10. Osatonthozedwa Kwa odwala opweteka kwambiri a impso, odwala omwe ali ndi vuto lopweteka kwambiri la nkhumba ayenera kugwiritsidwa ntchito mosamala. Mofanana ndi zina zoteteza serotonin reuptake inhibitors, kugwiritsidwa ntchito kwa Dapoxetine kumagwirizanitsidwa ndi machitidwe ena a maso. Mwachitsanzo, kupweteka kwa mwana ndi kupweteka kwa diso. Odwala omwe ali ndi vuto la kuthamanga kwa m'mimba kapena chiopsezo cha glacoma yoyenera kutsekedwa ayenera kugwiritsidwa ntchito mosamala.

Dapoxetine HCL ufa wotsutsidwa

1. Dapoxetine imaletsedwa kwa odwala omwe amadziwika kuti amatsutsana ndi dapoxetine hydrochloride kapena excipients.

2. Dapoxetine imaletsedwa kwa odwala omwe ali ndi zizindikiro zomvetsa chisoni m'mtima [mwachitsanzo, mtima wosagonjetsedwa (NYHA II-IV), osati kutentha kwapadera kwa pacemaker therapy (kalasi ya 2 kapena 3 atrioventricular block kapena matenda odwala matenda a sinus syndrome), chofunika kwambiri cha myocardial ischemia ndi valvular disease]

3. Dapoxetine ndi monoamine oxidase inhibitors (MAOIs)) Sayenera kugwiritsidwa ntchito limodzi mkati mwa masiku a 14 chithandizo cha monoamine oxidase chitetezo chitayimitsidwa. Mofananamo, monoamine oxidase inhibitors sayenera kugwiritsidwa ntchito mkati mwa masiku 7 atasiya Bili (onani kuyanjana kwa mankhwala).

4. Dapoxetine sichitha kugwiritsidwa ntchito ndi thioridazine kapena mankhwala a thiodazine amaletsedwa. Inagwiritsidwa ntchito masiku angapo. Mofananamo, thioridazine sayenera kutengedwa m'kati mwa masiku a 7 pambuyo posiya Dapoxetine (onani gawo loyanjana ndi mankhwala).

5. Dapoxetine imaletsedwa kutenga ketoconazole, itraconazole, ritonavir, saquin Odwala okhala ndi cytochrome amphamvu P450 3A4 inhibitors monga nave, telithromycin, nefazodone, naffenavir, ndi atazanavir.

6. Dapoxetine imaletsedwa kwa odwala omwe amavutika kwambiri ndi chiwindi.

Dapoxetine HCL ufa Kutsitsa

Pogwiritsira ntchito mapiritsi a dapoxetine hydrochloride, ayenera kuyang'aniridwa motsogoleredwa ndi dokotala, omwe angathe kusintha zizindikiro za matendawa ndipo nthawi yomweyo amatha kugwiritsa ntchito mankhwalawa.


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CAS 129938-20-1 Dapoxetine hydrochloride HNMR

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