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Dapoxetine HCL powder

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ICHINYANYA ndechekugadzirisa uye kugadzira zvigadzirwa kubva ku gram kusvika pakukura kweDapoxetine hydrochloride powder (129938-20-1), pasi peCGMP mutemo uye trackable quality control system.

Dapoxetine hydrochloride ibhuku rinopfupika rinosarudza serotonin reuptake inhibitor rinotengeswa kurapwa kwemajaya asati asvika mumarume. Kupera kwemajeri (PE) ndiyo inowanzobatwa nehutachiona hwepabonde, inofungidzirwa kuchinja kusvika ku30% yevarume. Dapoxetine hydrochloride is an analytical reference standard inorongwa senototonin reuptake inhibitor. Inopa kuvandudzwa mumitambo yakasiyana-siyana inobatanidza kupera kusina nguva mumakiriniki. Ichi chigadzirwa chinogadzirirwa kutsvakurudza uye mapurisa ekuongorora.

Product Description

Dapoxetine hydrochloride anesthesia powder video


Raw Dapoxetine hydrochloride anesthesia powder zvinhu Characters

Name: Dapoxetine hydrochloride
CAS: 129938-20-1
Molecular Formula: C9H7ClN2O5
Molecular Weight: 258.62
Melt Point: 175-179 ° C
Storage Temp: -20 ° C Freezer
Color: White crystalline powder


Dapoxetine inhengo yehupenyu yekirasi ye selective inhibitors ye serotonin reuptake asi isina anti-depressant effect. Mushonga wacho unonyatsokurudzirwa kuti uite ejaculation isati yasvika kune varume vakuru pakati pemakore e18 ne64 vanoita zvose zvinotevera:

1. Kuenderera mberi kana kudzokorora kuwedzerwa kwepenisi musati, munguva, kana nguva pfupi mushure mokupinda mumudzimai, uye bedzi kusati kwavapo kusava nekugutsikana kwepabonde;

2. Zvinonyanya kukosha kumanikidziro kana kukanganisa kunokonzerwa nehutano husati hwasvika (PE);

3. Urombo hwekudzivirira kukwanisa mano.

Makemikari zvinhu zveDapoxetine

Dapoxetine hydrochloride tablet ndiyo gorosi yakafukidzwa nefirimu, iyo yakachena kana isina-yakachena pashure pokubviswa kwekupfeka.

Chinhu chikuru: Dapoxetine hydrochloride.

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

Dapoxetine HCL poda Kemikisi Yakagadzirwa

1. 2D Urongwa:

2. 3D Conformer:

Chirevo chemuumbi: C21H23NO

Molecular Weight: 305.421 g / mol

CAS: 119356-77-3

Tsanangudzo yakajeka yeDapoxetine

Parizvino, hapana mimwe mitemo yakananga yekurapa kwemajaya ejaculation nguva isati yasvika nemahwendefa e dapoxetine hydrochloride. Ikoko hapana mimwe mitemo yakananga yekushandisa mushonga kwenguva yakareba sei pakurapwa. Izvo zvinoenderana nekuoma kwezviratidzo zvekusati kwasvika. Matambudziko ekurapa akasiyana. Mishonga nguva haigone kuve yakawanda. Zvisinei, mishonga inogona kuvandudza zviratidzo zvekusati kwasvika, saka varwere vanogona kutora mishonga maererano nezviratidzo zvavo.

Dapoxetine inonyanya kurongerwa kurapwa kwe18 kusvika kune 64 gore rekare murume asati asvika ejaculation (PE) varwere vanoita zvose zvinotevera, kusanganisira:

1. Iyo peni iri shoma shoma kare, panguva, kana nguva pfupi mushure mokupinda mukati mechikadzi, uye vasati vagutsikana zvepabonde. Kuvhiringidza zvepabonde kunopfuurira kana kudzokorora kuwedzerwa;

2. Zvinonyanya kukosha kumanikidziro kana kukanganisa kunokonzerwa nehutano husati hwasvika (PE);

3. Urombo husina simba rekudzivirira.

Dapoxetine yakatove yakabvumirwa semishonga inopera muEurope uye United States seine hukuru hwekurapwa kwekugadzirira kusati kwatanga. Paunotora dapoxetine, serotonin, chinhu chiri muuropi, chakavanzwa. Iyi serotonin chinhu chinopisa kufara kweuropi kana kuti chinounza mhepo inofadza. Kukanganisa uye kufara kunogadziriswa, zvinoitika zveAdrenaline zvakaderedzwawo, kuitira kuti kuwedzerwa kwekugadzirisa nguva kunogona kunonoka.

Dapoxetine hydrochloride inogona kuvharidzira 5-HT reuptake uye inowedzera huwandu hwe5-HT mumagetsi echinyakare nekudzivisa mutakuri we 5-HT. Zvidzidzo zvakaratidza kuti dapoxetine inopindira ejaculation reflex, uye giant cell lateral nucleus inhengo inokosha yehuropi. Apo kuiswa kwe dapoxetine kwakakwirira, monoamine protein yekutakura system inogona kudziviswa, uye reuptake ye dopamine inodziviswa zvakare. Dapoxetine inowedzera latency ye pudendal motor neuron reflexes uye inovandudza basa repabonde.

Zvinotora nguva yakareba sei kuti mahwendefa e-dapoxetine hydrochloride ave akabudirira haasi akawandisa. Kurapa kunoenderana nekuoma kwezviratidzo zvekusati kwasvika. Dambudziko rekurapa rakasiyana, uye nguva yekutora mishonga yakasiyana.

Chimiro cheDapoxetine

Iyo nzira yekuita dapoxetine mukurapa kwejeri yakasati yasvika ingave yakabatana nekudziviswa kwekudzokazve kwe serotonin neuroni, zvichidaro zvinokonzera kukanganisa kunogona kweveurotransmitter inobata pane zvakagadziriswa vasati vasvika uye mushure memasero esimba.

Dapoxetine inobatsira kushandiswa kwemajeri kwenguva isati yasvika nokuti ine simba rekuwedzera huwandu hwe serotonin inoderedza kufungidzirwa muuropi.

Serotonin inowanzobviswazve kubva ku synapse, asi nokutora dapoxetine inhibits reabsorption uye inoparadza serotonin.

Serotonin inodzvinyirira dopamine inokurudzira kufara, kunetseka, uye adrenaline inouya apo iwe unotya, saka iwe unogona kutowedzera nguva ye ejaculate.Dapoxetine inobatsira kuti isati yasvika ejaculation nokuti ine mhedziso yekuwedzera huwandu hwe serotonin inoderedza kushevedzera ubongo.

Serotonin inowanzobviswazve kubva ku synapse, asi nokutora dapoxetine inhibits reabsorption uye inoparadza serotonin.
Serotonin inodzvinyirira dopamine iyo inokurudzira kufara, kunetseka, uye adrenaline inouya apo iwe unotya, kuitira kuti iwe unogona kutowedzera nguva yekudzivirira.

Kubviswa kwevanhu kunonyanya kupindirana nehukama hwekunzwira tsitsi. Nzira inofungidzirwa yejeri inotorwa kubva mumugwagwa wepinini reflex, iyo inopindirana neuropiyo, iyo inotanga kukanganisa neuropi nuclei (inonzi preoptic nucleus uye hypoventricular paraventricular nucleus).

Dapoxetine HCL Pharmacokinetics

Mushure mokutaura kwemukanwa, dapoxetine inokurumidza kusvika uye inosvika pakugadziriswa kweplasma (Cmax) mushure memaawa anenge 1-2. Izvo zvachose bioavailability 42% (ibanga 15-176%). Mushure mekunge imwe yemutemo inotungamirirwa ne30 mg uye 60 mg ye dapoxetine munguva yekutsanya, nhamba yeplasma (297 ng / ml uye 498 ng / ml, maererano) yakasvika pashure pe1.01 uye 1.27 maawa, zvichienderana. Kuwedzerwa kwezvokudya zvakakosha kunogona kuderedza zvishoma nezvishoma Cmax (10%) ye dapoxetine uye kuwedzera zvishoma AUC (12%), uyewo zvishoma nezvishoma kunonoka kwepamusoro kwekutengesa dapoxetine; zvisinei, mafuta akawandisa anodya Diet haina kukanganisa kuwanda kwekudya. Hapana chimwe chezvinhu izvi chinenge chiine kliniki inokosha. Bentley inogona kushandiswa kana pasina kudya.

Mushure mekutungamirirwa kwemuviri womunhu kuburikidza nekujowa kwemukati, iyo inofungidzirwa kare, pakati, uye inotapudza hafu-upenyu hwe dapoxetine ndeye 0.10, 2.19, uye 19.3 maawa, zvichienderana.

Iyo metabolites ye dapoxetine yakanyanyisa inonyanya kubviswa nemurini mumamiriro ezvinhu emuganhu. Hapana chinhu chakashanda chakaonekwa mumugini. Dapoxetine inokurumidza kubviswa, uye uchapupu huri pasi pehutano hwemaawa maawa 24 mushure mekutungamira (pasi pe5% yepamusoro yepamusoro). Nhamba yezuva nezuva ye dapoxetine yakanyanya kuduku. Icho chinotapudza hafu-hupenyu hwehutano hwemashoko inenge maawa anenge 19. Iyo hafu yeupenyu ye desmethyl dapoxetine yakafanana neyoyo dapoxetine.

Kushandisa Dapoxetine

Kurapa kwevarume vevarume vane nguva isati yasvika (PE)

Dapoxetine hydrochloride mahwendefa anogona kubudirira kusimbisa kukwanisa kuwedzerwa kudzidzira; zvinonyanya kuvandudza kugutsikana kwepabonde; kunyatsokurudzira ejaculation latency.

Pavanenge vachishandisa mishonga, varwere vanogonawo kushandisa zvishoma zvishoma kuti vashandise zviratidzo zvekusarudzwa kwenguva refu, kugadzirisa mafungiro, kusimbisa kukurukurirana pakati pemurume nemudzimai, kudya kwemazuva ano, kusimbisa muviri wekurovedza muviri, kushanda kwezuva nezuva, uye kubatanidzwa mune basa remuviri vhiki rese. Ichowo chisarudzo chakanaka chekutamba nhabvu uye kutamba basketball kuti uwedzere muviri wakagadzikana uye kubvisa pfungwa mupfungwa.

Dosage yeDapoxetine

Muyero weDapoxetine hydrochloride mapiritsi ndeyomuromo, uye mahwendefa anofanira kunomedzwa asina kusimba; varwere vanorayirwa kuti vatore kamwe mukombe wakazara wemvura yemishonga; varwere vanofanira kuedza kudzivisa kukuvadzwa kunokonzerwa neprodromal zviratidzo zvakadai se syncope kana chirwere.

Kuwanda kwemapiritsi e-dapoxetine hydrochloride akakurudzirwa kuvarwere vose vari varume vakuru (18 kusvika kune 64 yemakore) ndeye 30 mg uye inoda kutorwa pamusoro pe1 kusvika maawa 3 vasati vaita zvepabonde. Kana mhinduro yacho isingagutsikani mushure mokutora 30mg uye migumisiro yemigumisiro ichiri mukati mechirongwa chinogamuchirwa, muyero unogona kuwedzerwa kusvika ku60mg yepamusoro purogiramu inorayirwa.

Nhamba yakakurudzirwa inoshandiswa inoshandiswa maawa ose e24.
Vakwegura (vakwegura vane 65 nepamusoro) Ichi chigadzirwa hachina kuongororwa mumakore e65 uye kuchengetedzwa nekubudirira kune varwere pamusoro peboka revanhu rakashandiswa, chikonzero chikuru che data pamusoro peiyo chigadzirirwe ichi muhuwandu hachina kukwana kune varwere vane unyoro renal impairment kana varwere vane utano hwepvo havafaniri kugadzirisa chirwere pavanotora chigadzirwa ichi, asi vanofanira kuchitora nokungwarira. Ichi chigadzirwa hachina kukurudzirwa kune varwere vane chirwere chakakomba chinorwadza.

Dapoxetine Zviratidzo:

Ichi chigadzirwa chinotarisirwa kuti kurapwa kwevarume vevarume vasati vasvika ejaculation (PE) pakati pemakore e18 ne64 vanosangana nemamiriro ezvinhu anotevera: chirume ichiripo kusvikira ichiiswa mukati memukadzi, panguva kana kuti nguva pfupi ichangobva kuiswa, uye mberi kugutsikana kwepabonde kunogadziriswa, chete nekuda kwekutsamwa kwakanyanya. Kana kudzokorora kuchinjwa; uye zvinokonzera kushungurudzika kwega kana kuti zvipingamupinyi zvepamweya nekuda kwekushanda kwejeri (PE); uye kushayiwa ejaculation control.

(1) Varume vakuru (18 kusvika kumakore 64)

Batsira chirwere chekutanga che 30 mg kune varwere vose uye inoda kutora pamusoro pe1 kusvika maawa 3 vasati vaita zvepabonde. Kana mhinduro yacho isingagutsikani mushure mokutora 30mg uye migumisiro yemigumisiro ichiri mukati mechirongwa chinogamuchirwa, muyero unogona kuwedzerwa kusvika ku60mg yepamusoro purogiramu inorayirwa. Nhamba yakakurudzirwa inoshandiswa inoshandiswa maawa ose e24. Ichi chigadzirwa chinogona kutorwa kusati kwapera kana mushure mekudya.

Kana chiremba achisarudza chigadzirwa ichi kuti aite chirongwa chekuvhara nguva isati yasvika, anofanira kuongorora dambudziko uye murwere akarondedzera kubatsirwa kwemavhiki ekutanga e4 mushure mekushandisa mishonga, kana kuongorora mukana wehutano-kubhadharo mushure mekushandisa chirwere cheA6-nguva uye kuraira pasinei nekuramba uchishandisa chigadzirwa.

(2) Vakwegura (65 makore nemakore)

Kutsvakurudza hakugere kuongorora kuchengetedza uye kubudirira kwechigadzirwa ichi muvarwere vane makore gumi nemana kubva ku65 uye kupfuura. Chikonzero chikuru cheizvi ndechokuti data pamusoro pekushandiswa kwechigadzirwa ichi muhuwandu huwandu hushoma.

(3) Vana nevechidiki

Ichi chigadzirwa hachifanirwe kushandiswa nevanhu pasi pezera re 18.

Rimwe piritsi panguva imwe rinogona kutorwa nokusingaperi. Mushonga wacho unoda kuendeswa pane chisina chinhu chiri mudumbu. Zviri nani kunwa tiyi tisati tashandise zvakanaka musati mishonga iyi yakanakisisa kuita sangano rakazara rekuongorora, zvichienderana nehutano hwavo mune chiremba kana chiremba wezvemishonga akaudza uye kuchengeteka akaronga kuti mushonga wacho udzivise kushandiswa zvisina kukodzera kwemishonga, asi kwete kuwedzera zvisina kukodzera kuwanda kwekushandisa zvinodhaka panguva yaunofanira kutevera urongwa hwechiremba uye kunyadziswa.

Dapoxetine Overdose

Kazhinji, zviratidzo zvekuwedzererwa kwesarotonin reuptake inhibitor dzinosanganisira serotonin-miviri yakaipa miitiro yakadai seyetaria, kushaya kwepamuviri kusagadzikana zvakadai sekunyunyuta uye kurutsira, kufara, kudengenyeka, dutu uye tachycardia. Panyaya yekudarika, zviyero zvinotsigirwa zvinotsigira zvinofanira kutorwa sezvinodiwa. Iko pachako hakuna maitiro akazvidzivirira kune chigadzirwa ichi.

Dapoxetine HCL Kuchengetedzwa

1. Zvose zvinodzivirira. Dapoxetine inoshandiswa chete kune varume vane chirwere chine nguva isati yasvika. Kuchengetedzwa kweDapoxetine mune varume vasina kuiswa kwenguva isati yasvika haisi pachena. Panguva imwecheteyo, hapana deta pamusoro pemigumisiro yeDapoxetine pakurambidza kupererwa kwevanhu munzvimbo ino. Zvinokurudzirwa kuti varwere havafanire kutora Beverly uye "zvinodhaka zvinodhaka" panguva imwe chete nokuti zvinoitika hazvizivikanwe uye zviitiko zvakashata zvinogona kuitika.

2. Varwere vanorayirwa kuti vasatora zvinodhaka zvepfungwa zvepfungwa panguva vachizvitora.

3. Usatora doro paunotora Dapoxetine.

4. Shandisa Dapoxetine inogona kukonzera syncope kana chirwere

5. Uyewo tora modto cytochrome P450 3A4 inhibitors seyerythromycin, clarithromycin, fluconazole, verapamil uye diltiazem.

6. Tora yakasimba cytochrome P450 2D6 inhibitor kana kuzivikanwa cytochrome P450 2D6 Varwere vane simba risina simba rekugadzirisa zvirwere vanofanira kuchenjerera pavanowedzera chiremba ku60 mg, sezvo izvi zvingaita kuti vawedzere kuwedzerwa, izvo zvingaguma zvichiita kuti pave nehuwandu hwakanyanya hunovhiringidza hunoita uye hutsinye.

7. Zvakakosha hazvifaniri kushandiswa pakuita mania / Varwere vane nhoroondo ye hypomanic kana bipolar disorder, panguva imwechete, chero murwere ane zviratidzo zvezvirwere zvinotaurwa pamusoro apa anofanira kuregererwa neDapoxetine.

8. Nokuti sarotonin yakagadziriswa inhibitori inhibitor inogona kuderedza chikumbaridzo chekufa. Kukosha, chero murwere anogumburwa anofanira kubviswa, uye varwere vane chirwere chisina kusimba chekufa vanofanira kudzivisa kushandisa Dapoxetine.

9. Dapoxetine haifaniri kushandiswa kune vanhu vari pasi pezera re 18.

10. Hazvikurudzirwi Kune varwere vane utachiona hwakakomba hwepvo, varwere vane runyoro kana kuti vane mwero kuora mwoyo kwemazino vanofanira kushandiswa nekuchenjerera. Kufanana nedzimwe sarotonin reuptake inhibitors inosarudza, kushandiswa kweDapoxetine kunosanganiswa nemamwe maziso ekuona. Semuenzaniso, mudzidzi kuwedzera uye kuchema kweziso. Varwere vane kukwidziridzwa kwepamusoro kwepisocular kana dambudziko rekona -vhavhara glaucoma inofanira kushandiswa nekuchenjerera.

Dapoxetine HCL powder Inorambidzwa

1. Dapoxetine inorambidzwa kune varwere vanozivikanwa kuti vane allergiki kune dapoxetine hydrochloride kana chero ipi zvayo.

2. Dapoxetine inorambidzwa kune varwere vane zviratidzo zvepfungwa zvinoratidza zviri mukati memoyo mumoyo [kunyanya mwoyo kusagadzikana (NYHA II-IV), kwete chekuita zvisina kufanira nekugadzirisa pacemaker therapy (grade 2 kana 3 atrioventricular block kana chirwere sinus syndrome), inokosha myocardial ischemia uye valvular chirwere]

3. Dapoxetine kana monoamine oxidase inhibitors (MAOIs)) Haifaniri kushandiswa pamwe mukati memazuva 14 mushure mokunge kurapwa kwemonoamine oxidase inhibitor kwakamira. Saizvozvowo, monoamine oxidase inhibitor haifaniri kushandiswa mukati mezuva re7 rekuregererwa kweBili (ona kushamwaridzana kwemishonga).

4. Dapoxetine haigone kushandiswa ne thioridazine kana kana mushure mekushaya thiodazine yakamira. Rinoshandiswa mukati memazuva. Saizvozvowo, thioridazine haifaniri kutorwa mukati mezuva re7 mushure mekuregererwa kweDapoxetine (ona chikamu chekubatana kwezvinodhaka).

5. Dapoxetine inorambidzwa kubva pakutora ketoconazole, itraconazole, ritonavir, saquin Varwere vane cytochrome yakasimba P450 3A4 inhibitors dzakadai seveve, telithromycin, nefazodone, naffenavir, uye atazanavir.

6. Dapoxetine inorambidzwa kune varwere vane uwandu hwakakomba uye hwakakomba hwechiropa.

Dapoxetine HCL powder Mhedziso

Paunenge uchishandisa mahwendefa e-dapoxetine hydrochloride, inofanirwa kutarisirwa pasi pekutungamirirwa kwechiremba, iyo inogona kuvandudza zviratidzo zvechirwere uye panguva imwechete zviri nani kushumira mushonga.


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CAS 129938-20-1 Dapoxetine hydrochloride HNMR

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