I-Tadalafil 171596-29-5 yokwelapha i-Erectile Dysfunction emadodeni

I-Tadalafil (i-Tadalafil, i-Tadalafil) ine-formula ye-molecular ye-C22H19N3O4 kanye nesisindo se-molecule ye-389.4. Isetshenziswe kabanzi ekwelapheni ukungasebenzi kahle kwe-erectile kwabesilisa kusukela ku-2003, negama lokuhweba elithi Cialis (Cialis). NgoJuni 2009, i-FDA yagunyaza i-tadalafil e-United States yokwelashwa kweziguli ezine-pulmonary arterial hypertension (PAH) ngaphansi kwegama lokuhweba elithi Adcirca. I-Tadalafil yethulwa ku-2003 njengesidakamizwa sokwelashwa kwe-ED. Kuthatha ukusebenza imizuzu engu-30 ngemva kokuphatha, kodwa umphumela wawo omuhle kakhulu 2h ngemva kokuqala kwesenzo, futhi umphumela ungahlala for 36h, futhi umphumela wawo awuthintwa ukudla. Umthamo we-tadalafil yi-10 noma i-20 mg, umthamo wokuqala onconyiwe ngu-10 mg, futhi umthamo ulungiswa ngokuya ngempendulo yesiguli kanye nokusabela okubi. Ucwaningo lwangaphambi kwemakethe lubonise ukuthi ngemva kokuphathwa komlomo kwe-10 noma i-20 mg ye-tadalafil amasonto e-12, amanani asebenzayo angama-67% no-81%, ngokulandelana. Ucwaningo oluningi lubonise ukuthi i-tadalafil iyasebenza kangcono ekwelapheni i-ED.

I-Erectile Dysfunction: I-Tadalafil iwuhlobo olukhethiwe lwe-phosphodiesterase 5 (PDE5) njenge-sildenafil, kodwa isakhiwo sayo sihlukile kokugcina, futhi ukudla okunamafutha aphezulu akuphazamisi ukumuncwa kwayo. Ngaphansi kwesenzo sokugqugquzelwa ngokocansi, i-nitric oxide synthase (NOS) eziphethweni zenzwa ye-penile namaseli e-vascular endothelial akhamba ukuhlanganiswa kwe-nitric oxide (NO) kusuka ku-substrate L-arginine. I-NO ivula i-guanylate cyclase, eguqula i-guanosine triphosphate ibe yi-cyclic guanosine monophosphate (cGMP), ngaleyo ndlela isebenze i-cyclic guanosine monophosphate-dependent protein kinase, okuholela ekwehleni kokuhlangana kwama-calcium ion kumaseli emisipha ebushelelezi, okubangela ukuthi i-corpus cavernosum Ukumiswa kwenzeka ngenxa yokuxegiswa kwemisipha ebushelelezi. I-Phosphodiesterase type 5 (PDE5) yehlisa isithunzi i-cGMP ibe yimikhiqizo engasebenzi, okwenza umthondo ube buthakathaka. I-Tadalafil ivimbela ukuwohloka kwe-PDE5, okuholela ekuqoqweni kwe-cGMP, ekhulula imisipha ebushelelezi ye-corpus cavernosum, okuholela ekumiseni kwe-penile. Njengoba ama-nitrate AKUKHO abanikeli, ukusetshenziswa okuhlangene ne-tadalafil kuzokwandisa kakhulu izinga le-cGMP futhi kuholele ku-hypotension enzima. Ngakho-ke, ukusetshenziswa okuhlangene kokubili kuvinjelwa ekusebenzeni komtholampilo.

I-Tadalafil isebenza ngokuvimbela i-PDES. I-GMP yonakele, ngakho ukusetshenziswa okuhlangene ne-nitrate kungase kubangele ukwehla okukhulu komfutho wegazi futhi kwandise ingozi ye-syncope. Ama-CY3PA4 inducers azonciphisa i-bioavailability ye-tadanafil, futhi inhlanganisela ne-rifampicin, i-cimetidine, i-erythromycin, i-clarithromycin, i-itracon, i-ketocon, ne-HVI protease inhibitors ingase ikhulise ukugcwala kwegazi lomuthi kufanele kulungiswe. Kuze kube manje, ayikho imibiko yokuthi imingcele ye-pharmacokinetic yalo mkhiqizo ithintwa ukudla notshwala.