Dapoxetine hydrochloride anesthesia powder ividiyo

I-Raw Dapoxetine i-hydrochloride i-anesthesia powder esisiseko Abalinganiswa

I-Dapoxetine yinkomfa yendalo yeklasi ye-inhibitors ekhethiweyo ye-serotonin reuptake kodwa ngaphandle kwefuthe elichasayo. Isilwayo siphuhliswe ngokukodwa ukuphatha unyango olusenyakatho kumadoda amakhulu phakathi kweminyaka eyi-18 kunye ne-64 edibana nayo yonke imigaqo elandelayo:

1. Ukunyuka okuqhubekayo okanye okuphindaphindiweyo kwipenisi ngaphambi, ngexesha, okanye kungekudala emva kokufakela kwisini, kwaye kuphela ngaphambi kokusilela kokwaneliseka ngokwesondo;

2. Ubunzima bokubandezeleka okanye ukungqinelana ngokubambisana ngenxa ye-ejaculation yangaphambili (PE);

3. Ubunono bokulawula u-ejaculation.

Iipropati zeChimicals zeDapoxetine

I-Dapoxetine i-hydrochloride tablet ithebhulethi enefayili egciniweyo, emhlophe okanye emhlophe-emva kokususwa kwengubo.

Isithako esiyinhloko: Dapoxetine hydrochloride.

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

I-Dapoxetine i-HCL powder Isakhiwo seMachiza

1. Ulwakhiwo lwe2D:

2. 3D Conformer:

Ifomula ye-molecular: C21H23NO

Isisindo somzimba: 305.421 g / mol

I-CAS: 119356-77-3

Inkcazelo elula yeDapoxetine

Okwangoku, akukho mgaqo othe ngqo wokunyangwa kwe-ejaculation engaphambi kwendoda kunye namaphilisi e-dapoxetine hydrochloride. Akukho migaqo ethile malunga nokuba ixesha elide lisebenzisa ntoni unyango. Kuxhomekeke kubukhulu beempawu ze-ejaculation engaphambi kwesikhathi. Inkathazo yonyango iyahluke. Ixesha lonyango alinakwenziwa ngokubanzi. Nangona kunjalo, isilwanyana sinokuphucula iimpawu zokuhlaselwa kwangaphambili, ngoko ke izigulana zingathabatha unyango ngokwemiqondiso yazo.

I-Dapoxetine ngokuyinhloko ijoliswe kunyango lwe-18 ukuya kwi-64 ubudala elidala elidlulileyo le-Ejaculation (PE) ezihlangabezana nazo zonke iimeko ezilandelayo, eziquka:

1. I-penis yincinci encinci ngaphambi, ngexesha, okanye kungekudala emva kokufakwa kwisini, nangaphambi kokuneliswa ngokwesondo. Isishumo sezesondo siqhubeka ngokuphindaphindiweyo okanye ngokuphindaphindiweyo;

2. Ubunzima bokubandezeleka okanye ukungqinelana ngokubambisana ngenxa ye-ejaculation yangaphambili (PE);

3. Ukulawulwa kakubi kwe-ejaculation.

I-Dapoxetine sele ivunyiwe njengemveliso yezobisi kwiYurophu nakwi-United States njengefuthe eliphezulu kunyango lwe-ejaculation engaphambi kwexesha. Xa uthatha i-dapoxetine, i-serotonin, into ebonakala kwingqondo, ifihliwe. Le serotonin yinto evuyisa umonakalo wengqondo okanye ivelise umphumo wokuphumla. Ukuxhatshazwa kunye nenjabulo ixazululwa, umphumo we-adrenaline uyancitshiswa, ukwenzela ukuba ukukhawuleza kwexesha kunokulibaziseka.

I-Dapoxetine hydrochloride ingakwazi ukuvimbela ngokuphumelelayo i-5-HT yokuvuselela kwakhona kunye nokwanda kwe-5-HT kwi-synaptic cleft ngokuvimbela umthuthi we-5-HT. Ucwaningo luye lwabonisa ukuba i-dapoxetine igxininisa ngokubanzi i-ejaculation reflex, kwaye i-nucleus yesigxina yesalathisi enkulu kakhulu ibaluleke kakhulu kwisimo sengqondo. Xa uxinaniso lwe-dapoxetine luphakamileyo, inkqubo yokuthutha iprotoamine yeprotheyini ingavinjelwa, kwaye i-reuptake ye-dopamine nayo ivinjelwe. I-Dapoxetine yandisa i-latency ye-motor neuron reflexes kunye nokuphucula umsebenzi wesini.

Kuthatha ixesha elingakanani ukuba amaphilisi e-dapoxetine hydrochloride asebenze ngempumelelo ayenzanga. Unyango luxhomekeke kubuqili beempawu zokuhlaselwa kwangaphambili. Ubunzima bonyango buhlukile, kwaye ixesha lokuthatha iyeza lihlukile.

Indlela yokusebenza yeDapoxetine

Inkqubo yesenzo se-dapoxetin ekwenzeni unyango lwe-ejaculation ngaphambi kokuba idibene nayo inxulumene nokuvinjelwa kokubuyiswa kwakhona kwe-serotonin nge-neurons, oko kuyachaphazela ukuhluka kweentlobo ze-neurotransmitters ezisebenza kwi-receptors ngaphambi nangemva kwe-synapses yeseli.

I-Dapoxetin isebenza ngokuphumelelayo kwimijondolo yexesha elide ngenxa yokuba inomphumela wokwandisa ukuxinwa kwe-serotonin ephazamisa ukuchulumiseka kwengqondo.

I-Serotonin idla ngokuphindaphindiwe kwi-synapse, kodwa ngokuthatha i-dapoxetine inqanda ukubuyisela kwakhona nokunciphisa i-serotonin.

I-Serotonin igxotha i-dopamine ephakamisa ukuzonwabisa, ukuxhalaba kunye ne-adrenaline ephuma xa unesifo, ngoko unako ukwandisa ixesha lo-ejaculate. I-Dapoxetine isebenza ngokukhawuleza kokunyuka kwe-ejaculation ngenxa yokuba inegalelo lokunyusa ukuxinwa kwe-serotonin ephazamisa ngengqondo.

I-Serotonin idla ngokuphindaphindiwe kwi-synapse, kodwa ngokuthatha i-dapoxetine inqanda ukubuyisela kwakhona nokunciphisa i-serotonin.
I-Serotonin igxotha i-dopamine ephakamisa ukuzonwabisa, ukuxhalaba, kunye ne-adrenaline ephuma xa unentshiseko, ngoko unokwandisa ixesha lokuba u-ejaculate.

Ukunyuswa kwabantu kubaluleke kakhulu kwinkqubo yesantya. Inkqubo yokucima i-ejaculation ivela kwiziko le-spinal reflex, elixhaswa yi-brainstem, echaphazelekayo yintsholongwane yengqondo yamanzi (i-nucleus yangaphambili kunye ne-nucleus ye-hypoventricular paraventricular).

I-Dapoxetine HCL Pharmacokinetics

Emva kokulawulwa komlomo, i-dapoxetine iyancipha ngokukhawuleza kwaye ifinyelele kwi-concentration yolwazi ye-plasma (Cmax) emva kweeyure ezingama-1-2. Ubuninzi bokuba yi-42% (udidi lwe-15-176%). Emva kokulawulwa komlomo omnye kwe-30 mg kunye ne-60 mg ye-dapoxetine kwisimo sokuzila, iiplumma ze-plasma (297 ng / ml kunye ne-498 Ng / ml, ngokulandelanayo) zafike emva kwe-1.01 kunye nee-1.27 iiyure, ngokulandelanayo. Ukutya kokutya okunamafutha aphezulu kunokunciphisa ngokwemodare i-Cmax (10%) ye-dapoxetine kwaye kwandiswe ngokukhawuleza i-AUC (12%), ngelixa ilibala ngokukhawuleza ukugxininiswa kwe-dapoxetine; Noko ke, ukunyuka kwamafutha amaninzi kuDiet akuchaphazeli umlinganiselo wokubamba. Akukho nanye kwezi nguqu zinekliniki ebalulekileyo. I-Bentley inokusetyenziswa kunye okanye ngaphandle kokutya.

Emva kokulawulwa komzimba womntu ngesilwanyana sangaphakathi, ukuqikelelwa kwangaphambili, kumaphakathi, kunye nokuphela kwesigamu-ubomi be-dapoxetine yi-0.10, 2.19, kunye nee-19.3 iiyure, ngokulandelanayo.

I-metabolites ye-dapoxetine ekhutshwe kakhulu ikhutshwe ngumchamo kwisimo se-conjugate. Akukho mveliso esebenzayo efunyenwe kumchamo. I-Dapoxetine ikhutshwe ngokukhawuleza, kwaye ubungqina bubungaphantsi kwimizuzu ye-24 iiyure emva kokulawulwa (ngaphantsi kwe-5% ye-concentration concentration). Umthamo wemihla ngemihla we-dapoxetine uncinci kakhulu. I-half half-life of administration of oral is about hours 19. Isiqingatha-ubomi se-desmethyl dapoxetine sifana ne-dapoxetine.

Ukusetyenziswa kweDapoxetine

Ukunyangwa kwezigulane zesilisa ezine-ejaculation engaphambi kwexesha (PE)

Amacwecwe e-Dapoxetine hydrochloride angaphumelela ukuphucula ikhono lokulawula u-ejaculation; ngokuphucula kakhulu ukwaneliseka kobomi bezesondo; ngokukhawuleza ukwandisa i-ejaculation latency.

Ngoxa usebenzisa iyeza, izigulana nazo zingasebenzisa amanyathelo amancinci okuphucula iimpawu zokubanjelwa kwangaphambili, ukuguqula isimo sengqondo, ukomeleza unxibelelwano phakathi kwendoda nomfazi, ukutya okunengqiqo, ukuqinisa umzimba, ukuqhuba imihla ngemihla, nokuthatha inxaxheba kwimisebenzi yenyama yonke iveki. Kwakhona kukhethwe kakuhle ukudlala ibhola kunye nokudlala ibhola yebhoksi ukuze kukhuliswe umzimba kunye nokunciphisa uxinzelelo lweengqondo.

Isisombululo seDapoxetine

Iilitha zamaphilisi e-dapoxetine i-hydrochloride ngomlomo, kwaye iipilisi kufuneka zigonywe kakuhle; Izigulane zikwacetyiswa ukuba zithathe ikhefu enye epheleleyo yamachiza; Izigulane kufuneka zizame ukukhusela ukulimala okubangelwa yimpawu ezibonakalayo ezifana ne-syncope okanye isisu.

Amanani amacwecwe e-dapoxetine hydrochloride anconywayo kuzo zonke izigulane kumadoda amakhulu (18 ukuya kwi-64 ubudala ubudala) ngu-30 mg kwaye kufuneka athathwe malunga ne-1 kwiiyure ze-3 ngaphambi kokuphila ngokwesondo. Ukuba umphumo awunelisekanga emva kokuthatha i-30mg kunye nemiphumo emibi kusekho kwibanga elimkelekileyo, i-dosage inganyuswa ibe yi-60mg yeyona dose ephakanyisiweyo.

I-dose ephakamileyo ephakanyisiweyo isetyenziselwa iiyure ze-24.
Abantu abadala (abaneminyaka eyi-65 nangaphezulu) Lo mveliso awuhloliswanga kwiminyaka ye-65 kwaye ukhuseleko kunye nokusebenza kwezigulane ngenxa yezihlwele ezisetyenzisiweyo, isizathu esiphezulu sedatha kule mveliso esetyenziswayo kuluntu sinqongophe kakhulu kwizigulane ezinobumnene Ukukhubazeka komzimba okanye izigulane ezinomonakalo wezintso akudingeki ukuba ulungelelanise umthamo xa uthatha le mveliso, kodwa kufuneka uyithathe ngokuqaphela. Le mveliso ayikhuthazwa izigulane ezinobungozi obukhulu beentso.

Izibonakaliso zeDapoxetine:

Le mveliso ijoliswe kunyango lwezigulane zesilisa ezine-ejaculation engaphambi kwexesha (PE) phakathi kwexesha le-18 kunye ne-64 edibana nazo zonke iimeko ezilandelayo: i-penis iyaqhubeka ide ibe ifakwe kwisini, ngexesha okanye emva nje kokufakela, nangaphambi ukuxhaswa ngokwesondo kufumaneka, kuphela ngenxa yokucaphukisa. Ukuphindaphinda okanye ukuphindaphinda; kunye noxinzelelo olubalulekileyo lomntu okanye imithintelo engavumelaniyo ngenxa ye-ejaculation yexesha elide (PE); kunye nokulawulwa kobuhlwempu.

(1) Abadala abadala (18 ukuya kwi-64 ubudala ubudala)

Ncoma umthamo wokuqala we-30 mg kuzo zonke izigulane kwaye kufuneka uthathe malunga ne-1 kwiiyure ze-3 ngaphambi kwesondo. Ukuba umphumo awunelisekanga emva kokuthatha i-30mg kunye nemiphumo emibi kusekho kwibanga elimkelekileyo, i-dosage inganyuswa ibe yi-60mg yeyona dose ephakanyisiweyo. I-dose ephakamileyo ephakanyisiweyo isetyenziselwa iiyure ze-24. Le mveliso inokuthathwa ngaphambi okanye emva kokutya.

Ukuba ugqirha ukhetha le mveliso ukunyanga ukuhlaselwa kwangaphambili, kufuneka ahlolisise umngcipheko kunye nokuxhamla kwengxelo yegulane kwiiveki zokuqala ze-4 emva kokuba isilwanyana sisetyenziswe, okanye ukuvavanya umgca-mali wokufumana ingozi emva kokusebenzisa i-dose ye-6 yonyango kunye nokwenza isigqibo ingaba uqhubeke usebenzisa le mveliso.

(2) Abantu abadala (iminyaka eyi-65 nangaphezulu)

Uphando alukavavanyanga ukhuseleko kunye nokusebenza kwalo mveliso kwizigulane ezineminyaka eyi-65 nangaphezulu. Isizathu esibalulekileyo salokhu kukuba idatha ekusebenziseni le mveliso kulolu nani iphela kakhulu.

(3) Abantwana nabaselula

Le mveliso ayilungiselelwe ukusetyenziswa ngabantu abangaphantsi kwe-18.

Elinye ipilisi ngexesha elithile lingathathwa ngonaphakade. Isiza kufuneka sithathwe kwisisu esingenalutho. Kungcono ukusela itiye phambi kokusetyenziswa kakuhle phambi kokuba eli liyeza lilungele ukwenza inkqubo epheleleyo yokuhlola, kuxhomekeke ekuguleni kwabo kugqirha okanye kwi-pharmist kuxelelwe kwaye ukhuseleko lulungiswe ukuba lugwenywe ukusetyenziswa kakubi kweziyobisi, kodwa kungabi nenyusa ixesha lokusetyenziswa kweziyobisi ngexesha kufuneka ulandele amalungiselelo ogqirha kunye neentloni.

Dapoxetine Overdose

Ngokuqhelekileyo, iimpawu zokugqithisileyo kwe-serotonin i-reuptake inhibitor ziquka i-serotonin-effects effects mediation, efana nokunyaniseka, ukungasebenzi kwesisu, kunye nokuhlanza, ukunwaba, ukuthuthumela, ukuzondla kunye ne-tachycardia. Kwimeko yokudlula ngaphezulu, amanyathelo okuxhasa amanyathelo kufuneka athathwe njengoko kufuneka. Kukho akakho i-antidote ethile yalo mveliso.

I-Dapoxetine HCL Iinkcukacha

1. I zi khuselo. I-Dapoxetine isetyenziselwa kuphela izigulane zesilisa ezine-ejaculation engaphambi kwesikhathi. Ukhuseleko lweDapoxetine kumadoda angenayo i-ejaculation yexesha elide alicaci. Ngelo xesha, akukho datha malunga nomphumo weDapoxetine ngokulibazisa ukunyuka kwelo xesha. Kucetyiswa ukuba izigulane akufanele zithathe i-Beverly kunye "nezidakamizwa zokuzonwabisa" ngexesha elifanayo kuba umphumo awunakwenzeka kwaye iziganeko ezimbi ziyakwenzeka.

2. Izigulane zikwacetyiswa ukuba zingathathi iziyobisi zengqondo xa zithatha.

3. Gwema ukusela utywala xa uthatha i-Dapoxetine.

4. Sebenzisa i-Dapoxetine inokubangela ukuba i-syncope okanye i-syzziness

5. Kwakhona thabatha i-cytochrome ephakathi kwe-P450 3A4 inhibitors njenge-erythromycin, i-clarithromycin, i-fluconazole, i-verapamil kunye ne-diltiazem.

6. Thatha i-cytochrome eqinile i-cytochrome i-P450 2D6 inhibitor okanye i-cytochrome eyaziwayo I-P450 2D6 Izigulane ezinobuthakathaka obuthakathaka kufuneka ziqaphele xa ukwandisa umthamo kwi-60 mg, njengoko oku kunokukhokelela ekunyuseni okukhulu, ekugqibeleni ekukhokelela ekusebenziseni okuphezulu okuxhomekeke kumthamo.

7. Inzuzo ayifanele isetyenziselwe imania / izigulane ezineembali ze-hypomanic okanye i-bipolar disorder, ngexesha elifanayo, nasiphi na isigulane esinempawu zesifo esichazwe apha ngasentla kufuneka sipheliswe nge-Dapoxetine.

8. Ngenxa yokuba i-serotonin ekhethiweyo i-inhibitor inganciphisa umyinge wokuthintela ukuxabisa Ixabiso, naluphi na isigulane esinokuthintela kufuneka siyeke, kwaye izigulane ezinokuhluthwa okungaqiniseki kufuneka ziphephe ukusebenzisa i-Dapoxetine.

9. I-Dapoxetine ayifanele isetyenziswe kubantu abangaphantsi kwe-18.

10. Azinconywa Izigulane ezinobungozi obunzima beentliziyo, izigulane ezinokukhubazeka komnxeba omncinci okanye olinganisiweyo kufuneka zisetyenziswe ngokuqapha. Njengezinye i-serotonin e-reuptake inhibitors ekhethiweyo, ukusebenzisa i-Dapoxetine kudibaniswa nokujonga kwamehlo. Umzekelo, ukunyuka komfundi kunye nentlungu yeso. Izigulane ezineengcinezelo eziphezulu ze-intraocular okanye umngcipheko we-glaucoma yokuvalwa kwe-angle kufuneka zisetyenziswe ngokuqaphela.

I-Dapoxetine i-HCL powder Inqatshelwe

1. I-Dapoxetine iyanqatshelwe izigulane eziyaziwayo ukuba ziyingozi kwi-dapoxetine hydrochloride okanye nayiphi na i-excipients.

2. I-Dapoxetine iyanqatshelwe izigulane ezineemeko zesifo se-pathological entliziyweni [isib. Ukungaphumeleli kwentliziyo (NYHA II-IV), akukho ukuqhuba okungavumelekanga kunye neyeza eziqhubekayo ze-pacemaker (ibakala le-2 okanye i-3 kwibrioventricular block okanye isifo se-sinus syndrome), i-myocardial ischemia kunye nesifo se-valvular]

3. I-Dapoxetine kunye ne-monoamine oxidase inhibitors (MAOIs)) Akufanele isetyenziswe kunye phakathi kweentsuku ze-14 emva kokuba unyango lwe-monoamine oxidase inhibitors lugqityiwe. Ngokufanayo, i-monoamine oxidase inhibitors ayifanele isetyenziswe kwiintsuku ze-7 zokunqanyulwa kweBili (jonga ukusebenzisana kwezidakamizwa).

4. I-Dapoxetine ayinakusetyenziswa kunye ne-thioridazine okanye emva kokuba unyango lwe-thiodazine lugqityiwe. Se tyenziswe kwiintsuku. Ngokufanayo, i-thioridazine akufanele ithathwe kwiintsuku ze-7 emva kokucima i-Dapoxetine (jonga isigaba sokusebenzisana kweziyobisi).

5. I-Dapoxetine ivinjelwe ukuthatha i-ketoconazole, i-itraconazole, i-ritonavir, i-saquin Izigulane ezine-cytochrome ezinamandla i-P450 3A4 inhibitors njenge-nave, i-telithromycin, i-nefazodone, i-naffenavir, ne-atazanavir.

6. I-Dapoxetine inqatshelwe izigulane ezinobungozi obunzima kunye nobunzima besibindi.

I-Dapoxetine i-HCL powder Ukuphela

Xa usebenzisa amacwecwe e-dapoxetine i-hydrochloride, kufuneka ilawulwe phantsi kolawulo lugqirha, oluya kuphucula iimpawu zesifo kwaye ngexesha elifanayo lisebenzise le nkunkuma.

Indlela yokuthenga I-Dapoxetine hydrochloride powder (129938-20-1) kwiAASraw

1.Qhagamshelana nathi nge-imeyile yethu inkqubo yophando, okanye i-skype ye-intanethiummeli wenkonzo yamakhasimende (CSR).
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