Anti-estrogen izidakamizwa: incazelo, isicelo

Estrogen-blocker kukhona zamakhemikhali ukuthi uvimbele isenzo estrogen. izidakamizwa Antiestrogen esetshenziswa ekwelashweni kwezifo ezihlukahlukene. Basuke kabanzi wokwelapha isifo somdlavuza webele izinqubo kuthiye ukukhula isimila noma lokubuya kwesifo lokuvikela. Njengoba kunjalo nezinye izidakamizwa ukuthi basebenzisane hormone emzimbeni, le mithi kufanele sisetshenziselwe ngaphansi kweso lwezokwelapha.

Izinzuzo kanye efanele ibe kuhlu lokuhlukumezeka estrogen

I-estrogen, noma i-hormone steroid kwemiqondo ngokuyinhloko ezikhiqiza amaqanda. Kuthinta eziningi izinqubo zomzimba. Abesifazane yokuzala kufanele ezingeni eliphakeme le-hormone zemvelo. Nokho, isamba ngokweqile, kungadala syndrome eyaziwa ngokuthi hyperestrogenia. Lesi sifo kungaholela inqubo somdlavuza webele futhi umdlavuza endometrial. Imishanguzo yama-estrogen bese estrogen blocker futhi aromatase inhibitor kungase silungise konke. Nokho, Le mithi, nemithelela emihle nemibi ku besilisa nabesifazane.

Izinhlobo estrogen-blocker kanye nokusetshenziswa yabo

Kunezindlela eziningana izinhlobo ezahlukene estrogen-blocker. aromatase inhibitor empeleni ukuvimba ukukhiqizwa estrogen. Okukhethwayo i-estrogen yokwamukela modulators, njengokuthi "Tamoxifen" "Clomiphene", eklanyelwe ukuvimba i-estrogen receptor, futhi ngendlela ehlukile ngoba izinhlobo ezahlukene lendwangu. Antiestrogens futhi ukuvimba i-estrogen receptor.

Antiestrogens ukuvimbela ukuguqulwa kwe-testosterone ukuba estradiol futhi hormone estrogen kuphele ukuqhuba noma ivaliwe.

Eyenziwe ekwelapheni umdlavuza, le mithi asetshenziswa ukubambezela ukuthuthukiswa izimila. Kulokhu, abakhethayo estrogen yokwamukela modulators kungenziwa okubhekiswe estrogen receptor ethize. Blocker, kuhlanganise "Clomiphene" ubizwa nangokuthi ngezinye izikhathi asetshenziswa ukwelapha ukungatholi abantwana, bangase abanye omama abanenkinga ekubeni ukhulelwe. Le mithi, zibuye zisetshenziswe ezinye odokotela ekwelapheni izingane ahambisana nokuthomba imisiwe ize sezikhule ngokwanele.

Phakathi bodybuilders kwenza ukusetshenziswa estrogen-blocker ngenxa umphumela estrogenic of amazinga aphezulu testosterone emzimbeni. Testosterone kuyinto eyandulela i-estrogen, aromatase inhibitor ingasetshenziswa ukuyeka kumiswa imisipha ngokweqile mass estrogen, nokugcina ezingeni eliphansi emzimbeni. Lo mkhuba uye ukhangwa eziningi, ikakhulukazi uma elwa ne-estrogen asetshenziswa ngokuyinhloko ngezinhloso ayeyisimonyo. Kulokhu, abantu basebenzisa amaphilisi kanye lwezakhamzimba ngaphandle kokubhekwa ngabezempilo.

side effects

Kunemiphumela emibi kwemishanguzo elwa estrogen. Zingadala isiyezi, ubuhlungu bekhanda, ukujuluka, ukushisa komzimba kanye ukudideka. endocrinology kuphela unganquma umthamo afanele isiguli kuye ngokuthi isimo, kanye nombundu eyamukelekayo amathuba okuba nemiphumela engemihle. I endocrinology ingase futhi linqume igazi njalo ukuhlolwa amazinga ama-hormone uma lokuhlola ukusebenza jikelele isiguli ukuqinisekisa ukuthi ukusetshenziswa anti-estrogens iphephile futhi ukusebenza for nesineke.

ukwelashwa amadoda

Njengoba bekhula, owesilisa amazinga testosterone lehle. Nokho, uma testosterone kuyehla ngokushesha noma kakhulu, kungaholela ukuthuthukiswa hypogonadism. Lesi simo libhekene ekuhlulekeni komzimba ukukhiqiza le hormone ezibalulekile, kungabangela izimpawu ezinhlobonhlobo, kuhlanganise:

• ukulahlekelwa libido;
• nokwehlisa ukukhiqizwa kanye nekhwalithi isidoda;
• ukungasebenzi Erectile;
• ukukhathala.

Uma sikhuluma i-estrogen, into abantu kuqala bacabanga ukuthi i-hormone besifazane, kodwa ubukhona balo kuqinisekisa ukuthi umzimba wesilisa nokusebenza ngendlela efanele. Kukhona izinhlobo ezintathu estrogens: estriol, estrone futhi estradiol. Estradiol - iyona ifomu main estrogen asebenzayo amadoda. Kufeza indima ebalulekile ekulondolozeni umsebenzi emalungeni besilisa ubuchopho izicubu. izidakamizwa Antiestrogen kubuye kwenze isidoda ukuze zikhule kahle.

ukungalingani hormone - ukhulisa izinga estrogen futhi kwehle testosterone - kudala izinkinga. estrogen omningi emzimbeni wesilisa kungaholela:

• gynecomastia (ukuthuthukiswa ngokweqile izigaxa ebeleni);
• izinkinga zenhliziyo;
• kwengozi unhlangothi;
• kwesisindo;
• Izinkinga wendlala.

Ungathatha izinyathelo ezimbalwa ukuze ubuyisele ukulingana ezingeni estrogen. Isibonelo, uma i-estrogen yakho ngokweqile lihlotshaniswa amazinga aphansi testosterone, ukuthi kungaba wusizo njengendlela yokukwenza testosterone esikhundleni estrogen blocker.

Pharmaceutical estrogen-blocker

Eminye imikhiqizo eyenza imithi angakhiqiza umphumela estrogen sokuvimbela ezingabantu. Njengomthetho, avame ahloselwe ukusetshenziswa abesifazane, kodwa ukuzuza in ukuthandwa phakathi kwabantu, ikakhulukazi labo abafisa ukuba babe nezingane. Testosterone Izithako kungaholela nenzalo. Kodwa i-estrogen blocker ezifana "Clomid" Ungakwazi ukubuyisela ibhalansi hormone ngaphandle kokuyekethisa okuzala.

izidakamizwa eziningana zaziwa ngokuthi abakhethayo estrogen yokwamukela modulators, ngokuvamile ithunyelwa njengoba izidakamizwa ekwelapheni umdlavuza webele. Kodwa lungasetshenziswa ukuvimba estrogen amadoda. Le mithi asetshenziselwa ezihlukahlukene izimo ezihlobene testosterone ongaphakeme, kuhlanganise:

• ukungazali;
• ongaphakeme isidoda ukubala;
• gynecomastia;
• kwamathambo.

Le mithi kufanele sisetshenziswe ngokukhetha, kuye ngokuthi isiguli. Ukusebenzisa izidakamizwa ezifana anti-estrogen. Ekhemisi ungathenga:

• "Tamoxifen".
• 'Arimidex'.
• "Letrozole."
• "Raloxifene".

Imiphumela enethambo

Ngokusho odokotela, ukuvezwa kwesikhathi eside i-estrogen izidakamizwa kungabangela umdlavuza endometrial kwabesifazane. "Raloxifene" - a abakhethayo estrogen yokwamukela modulator - kungavimbela emdlavuzeni, ngokukhetha amabhlogo ukumuncwa estrogen. Nokho, lokhu izidakamizwa, Kanti liyakwazi ezivimbela nemiphumela emihle estrogen ku kwamathambo. Umuthi omusha - "lasofoxifene" - kungenzeka ulungise le nkinga. It kuvimbela awohloke e abesifazane postmenopausal futhi kunciphisa brittleness ithambo izicubu. Ukusetshenziswa kwalesi izidakamizwa iphephile ngokuvamile, kodwa kungase kwandise amahlule.

izidakamizwa ekuhlanganyeleni

Estrogen blocker "Tamoxifen" kungasiza ekuvimbeleni umdlavuza. iziguli ezinomdlavuza ngokuvamile nokucindezeleka, futhi leli qembu kungase kuyenze ithathe uxhumana omubi imithi, nemithi yokunciphisa ukucindezeleka. Kufanele sisebenzise "Paroxetine", ngenxa yokuthi abesifazane ukuthatha "Tamoxifen" futhi "Paroxetine", nengozi kancane lokufa lungcono abesifazane abathatha "Tamoxifen" futhi iyiphi enye antidepressant. Lokhu kungenxa yokuthi "Paroxetine" izenzo ngokukhetha.

ejenti Antiestrogen nezidakamizwa

I ukuveza zonke lezi zimali abonisa ukuthi izidakamizwa ngamunye isetshenziswa ngamunye endabeni ethile.

"Clomid" noma "clomiphene citrate" Lesi esinye sezenzakalo izidakamizwa yokuqala isetshenziswe ekwelapheni gynecomastia, ngoba kuphakamisa izinga somzimba kwe-testosterone zemvelo. Kukhona ezinye imiphumela emibi evela ukusetshenziswa eside, ezifana izinkinga umbono. Kukhona izinto zisebenze kakhulu emakethe, okuyinto isinyathelo ngendlela efanayo kodwa "Clomid" namanje ukuxubana ngempumelelo futhi engabizi nganoma yisiphi umsubathi.

Lena akuyona steroid Anabolic, umuthi ngokuvamile ebekiwe njengento esizayo abesifazane nge ukungazali, ngoba ikhono evelele ukuze sikhuthaze nge-ovulation, okuyinto ibangelwa ekuvimbeni / ukunciphisa imiphumela estrogen emzimbeni. Ukuze ucacise kabanzi, "Clomid" - chemical izakhiwo zokwenziwa estrogen agonist / omelene. Ngo target izicubu ezithile kungenza ukuvimba ikhono estrogen ukuhlanganisa uxhumano nomsebenzisi kwezinga yokwamukela okuhambisanayo. Ukusetshenziswa Its sokucindezeleka yokulwisana ngempendulo negative estrogen uhlelo ngxenye-pituitary-wesibeletho, athuthukisa ukukhululwa kwe LH futhi FSH. Konke lokhu kuholela ukukhiqizwa kwamaqanda.

Ngezinhloso yezemidlalo "clomiphene citrate" abesifazane azinamphumela. Nokho, ngo-amadoda, kukhulile ukukhiqizwa FSH futhi (ngokuyinhloko) luteinizing hormone kuvusa testosterone zemvelo. Lo mphumela kuyazuzisa ikakhulu ukuba lo msubathi ekupheleni umjikelezo steroid lapho amazinga testosterone endogenous bacindezelekile. Ngaphandle kwe-testosterone (noma ezinye androgens), "cortisol" Liyanqoba futhi sithinta amaprotheni zamagama ezicutshini. Kepha ngokushesha "odla" iningi imisipha asanda kuluthola ngemva yokukhansela. Clomid Ungadlala indima ebalulekile ukugwema lokhu ukwehluleka ukufeza imiphumela ezemidlalo. Ukuze abesifazane, izinzuzo isinyathelo Clomid - Amandla ukulawula endogenous estrogen ezingeni. Lokhu kuzokhulisa ukulahlekelwa amafutha kanye muscle, ikakhulukazi ezindaweni ezifana emathangeni nezinqe. "Clomiphene citrate" Nokho, ngokuvamile ikhiqiza imiphumela eminingi engemihle njengezindlela kwabesifazane, kodwa, nokho, funa phakathi leli qembu abasubathi.

"Tamoxifen" ivimbela i-estrogen zemizwa amaseli umdlavuza webele. Lokhu okuvimba estrogen kusukela yokuxoxisana nabo futhi kuvimbela ukukhula nokuhlukana kwamangqamuzana. Nakuba "Tamoxifen" izenzo njengenhlangano antiestrogen kumaseli mammary ndlala ke uba i-estrogen kwamanye amathishu: amathambo kwesibeletho.

Abesifazane kanye engaphansi webele "Tamoxifen" umdlavuza koda ingasetshenziswa emva kokuhlinzwa 5-10 kweminyaka, ukuze unciphise amathuba ukusabalalisa Ukudlulela. Iphinde kunciphisa ingozi yokuba nesifo somdlavuza kwesinye webele. Ukuze usaqala lokhu ukulungiselela isetshenziswa ngokuyinhloko ukuze iziguli abangamkhonzi nambili kuya kwabadala. Aromatase inhibitor ukuphathwa oluncamelayo abesifazane menopausal.

"Tamoxifen" naye angayeka ukukhula noma oluhlehlela izimila in iziguli metastatic zabasiza abathile abanomdlavuza. Ingase futhi ingasetshenziswa ukwehlisa ingozi yokuba webele onkologicheskihz izinqubo.

Lesi sidakamizwa esithathwayo ngomlomo, ngokuvamile ngesimo amaphilisi.

imiphumela emibi anti-estrogen izidakamizwa ahlanganisa ukukhathala, ukushisa komzimba, isitho sowesifazane somile noma ezinkulu kanye nokuguquguquka kwemizwelo.

Abanye besifazane metastases e bone izicubu kungenzeka ubuhlungu nokuvuvuka imisipha namathambo. Lokhu ngokuvamile Asihlali isikhathi eside, kodwa kwezinye izimo ezingavamile, abesifazane ingase futhi ukuthuthukisa amazinga aphezulu calcium egazini, okungasekelwe prokontroliruesh. Uma lokhu kwenzeka, impatho ke kungenziwa okwesikhashana isikhathi esithile.

Ezingavamile, kodwa kakhulu emibi nazo zingaba khona. Le mithi kungase kwandise amathuba okuthola i-nomdlavuza myometrium besifazane nge nambili kuya kwabadala. igazi Ukwandiswa ekunqandeni kungulenye indlela eyaba nemiphumela emibi. Deep vein thrombosis kwenzeka, kodwa ngezinye izikhathi ucezu igazi ihlule kungaba phuma futhi ekugcineni ukuvimba Umthambo emaphashini (embolism yamaphaphu).

Akuvamile "Tamoxifen" ombangela yokufa uhlangothi nokumelwa yinhliziyo kwabesifazane postmenopausal.

Kuye ngokuthi isimo menopausal abesifazane "Tamoxifen" kungaba nemiphumela ehlukene enethambo. Ngo abesifazane premenopausal, "Tamoxifen" kungabangela thinning amathambo, kodwa abesifazane post-menopausal kwandisa izinga calcium, ezidingekile enamandla.

Izinzuzo lokhu izidakamizwa zinkulu izingozi ngoba cishe bonke abesifazane nge-hormone engaphansi koda umdlavuza webele.

Ngokufanayo, umuthi "Toremifene", okuyinto ivunyelwe ukuze kwelashwe metastatic umdlavuza webele. Nokho, lokhu imithi angeke isebenze uma esetshenziswa "Tamoxifen", kodwa singanyakazi.

"Fulvestrant" kuyinto umuthi amabhlogo we-estrogen yokwamukela kuqala, bese futhi kususa yokwamukela umthamo esibophezelayo. It uba i anti-estrogen wonke umzimba.

"Fulvestrant" isetshenziswa ukwelapha egijima metastatic yomdlavuza webele, futhi kuvame kakhulu ukuba kusetshenziswe emva nezinye izidakamizwa hormone ( "Tamoxifen" futhi aromatase inhibitor) okuyinto kuyekile ukusebenza.

Common side effects kungafaka phakathi komzimba, ukujuluka ebusuku, isicanucanu omnene futhi babekhathele kakhulu. Kwakucatshangwa ukuthi kungaba buthaka amathambo (kwamathambo), uma wamukelwe isikhathi eside.

Lesi sidakamizwa unqobile ukuqashelwa ukuze isetshenziswe abesifazane postmenopausal ngubani ungaphenduli "Tamoxifen" noma "Toremifene." It ngezinye izikhathi isetshenziselwa inhloso yazo kwabesifazane premenopausal, ngokuvamile lihambisana luteinizing-hormone okuthiwa i-ukukhulula agonist ukucisha amaqanda.

"Raloxifene" esetshenziswa abesifazane ngoba nokwelashwa zokuphela kwamathambo noma kwamathambo ngemva kokuma ukuya esikhathini. Kuyasiza silondoloze amathambo eqinile, ekunciphiseni ingozi waphuka.

"Raloxifene" futhi kungavimbela okuvela koda yomdlavuza webele ngemva kokuma ukuya esikhathini. Akayena hormone i-estrogen, kodwa Unjengomahluleli estrogen ezinye izingxenye zomzimba, ezifana kwamathambo. Ngamanye izingxenye zomzimba (webele kanye kwesibeletho), "Raloxifene" izenzo njengenhlangano blocker estrogen. Yena awusho ezihlukahlukene menopausal syndrome. Raloxifene siphathelene isigaba izidakamizwa eyaziwa ngokuthi abakhethayo estrogen yokwamukela modulators-SERMs (estrogenic nezidakamizwa antiestrogenic).

Imishanguzo yama-estrogen bese Ezemidlalo

Eminye imithi kabanzi bodybuilders ukwakha kwemisipha.

"Cyclofenil" - kuyinto neanabolichesky / steroid androgenic. Isebenza njengenhlangano anti-estrogen ne-testosterone njengoba ivuselela. "Cyclofenil" kuyinto estrogen enganamandla kakhulu nobumnene, kodwa sibopha estrogen receptor iphinde ivimbele yokubopha zemvelo estrogen receptor. Eqinisweni, it isebenza kahle kangangokuthi abanye abadlali thatha izidakamizwa ngesikhathi ukwelashwa kwama-steroid ukuze silondoloze amazinga aphansi estrogen. Umphumela - kuncishiswe inani uketshezi emzimbeni, obadalwa nge ama kanye nokuncipha gynecomastia. Umsubathi has a Ingaphandle ezinzima, elokusebenzisa izidakamizwa ezifana, okuyinto engase ezithathwe ngesikhathi belungiselela umncintiswano. Nokho, bodybuilders, ulisebenzise kancane kaningi ngoba bakhetha a ethengekayo 'Nolvadex' futhi 'Proviron. "

"Njengokuhlaba Clomid", "Cyclofenil" kuyinto bahluleka abesifazane, njengoba kunomthelela omuhle kuphela ekukhiqizweni kwama-hormone ezingabantu. Ukukhulisa izinga kwe-testosterone odalwe lolu izidakamizwa akwanele ukukhuluma mayelana ngcono kakhulu impela nje, kodwa lilomlilo inzuzo, ngisho nje ukwenyuka kancane isisindo somzimba, nokwanda okuphawulekayo amandla nokwenyuka ukuvuselelwa kungenzeka. Le miphumela ibonakala ikakhulukazi abasubathi eziphambili abanesipiliyoni noma ngokubonisana okuncane nalabo steroid. Sebenzisa imiphumela kuzobonakala kuphela ngemva kwesonto.

Kwezinye izimo, abasubathi ababukele nokuqhuma ezifana induna, kukhuphuke ubulili drive futhi ukufikelwa ukushisa. Lezi zimpawu yilezi ubufakazi Indlela ikakhulukazi ukuthi kwakwakhe empeleni ngempumelelo. Ngemva ukuqedwa kwezinye isimo sokucindezeleka futhi ukwehla okuncane nje kwamazinga amandla. Labo thatha izidakamizwa njengoba i anti-estrogen ngesikhatsi ukwelashwa kwama-steroid, zingabuka nomphumela ophambene lapho umphumela agent imisiwe.

"Proviron" ingenye omdala Anabolic steroid androgenic emakethe. Ngokusemthethweni yaziwa abantu bakhona njenge- "Mesterolone", luhlala luwuhlamvu lunye we engaphiwanga kakhulu phakathi abasebenzisi Anabolic steroid.

Malanga obusebenzayo Proviron has imisebenzi emine esemqoka, okuyinto zinquma Yiqiniso yayo senzo. Okokuqala, yena ingenye ama ezinamandla kakhulu Anabolic, ngoba kwandisa umthamo afundwa testosterone khulula, okuyinto ebaluleke kakhulu Anabolic izinqubo bodybuilders. Indlela elula uyibuke: uma uphuza ama steroid, mass imisipha liyakhuphuka.

"Proviron®" futhi unekhono ukuze uxhumane aromatase enzyme, okuyinto unomthwalo ukuguqulwa kwe-testosterone ukuze estrogen. Ngu sesibopho ukuthobisa aromatase, "Proviron®" empeleni zivimbela umsebenzi wayo, ngaleyo ndlela bathola isivikelo kusuka imiphumela emibi estrogen.

On "Mesterolone" Ubuye ziyezwana enamandla yokwamukela androgen. Lokhu steroid Anabolic okungahambisani ukucindezela gonadotropins kuyafana nezinye Ama-anabolic steroid. Lokhu kwenza kube nokwenzeka ukwandisa ukukhiqizwa kwesidoda kanye androgens zibalulekile ukukhuthazwa spermatogenesis. Lokhu kwandisa hhayi kuphela isibalo isidoda, kodwa kuthuthukisa izinga layo.

Side Effects "Proviron" ungafaki gynecomastia noma uketshezi ngokweqile. Lokhu kuzophinde kakhulu ukunciphisa ingozi high blood pressure elihlobene ne ukuthatha ama steroid. Eqinisweni, "Proviron" has umphumela anti-estrogenic ngovimba ukuguqulwa kwe-testosterone ukuba i-estrogen, noma okungenani ukubambezela le nqubo.

Izidakamizwa oshiwo ngenhla musa ukwehlisa izinga estrogen kodwa kuthinta umzimba jikelele.

Iqembu izidakamizwa antiestrogenic futhi zihlanganisa agonists ukukhulula izici hormone gonadotropic ( "Buserelin" futhi analogs yayo), megestrol acetate ( "Megeys") "Parlodel" futhi "Dostinex" asetshenziswa njengoba izidakamizwa asimise prolactin uketshezi. Ukusebenzisa kwabo siqu ekwelapheni non-okunengqondo.

Wokwelapha isifo somdlavuza

Ngaphezu "Tamoxifen" Okulandelayo estrogen yokwamukela blocker.

izidakamizwa ezintathu ukuthi sime ukukhiqiza estrogen abesifazane postmenopausal, sivunyiwe ukwelapha kokubili ekuseni sezihambile umdlavuza webele: "Letrozole" ( "Femara"), "Anastrozole" ( 'Arimidex') kanye "Exemestane" ( "AROMASIN") .

Lo mshini wezenzo kwemishanguzo elwa estrogen leli qembu - the Ukuvinjwa of enzyme (aromatase) kwezicubu adipose, okuyinto unomthwalo nengcosana estrogen abesifazane post-menopausal. Abanaso kuthinte amaqanda, ngakho kuphela ngempumelelo labo abesifazane izindlala zabo ezikhiqiza amaqanda azisebenzi, kungaba ngenxa menopause noma ngenxa umthelela luteinizing-hormone okuthiwa i-analog. Le mithi zithathwa nsuku zonke ifomu iphilisi. Basebenza kahle ngokufanayo ekwelapheni izinqubo oncological ebeleni bese wendlala.

Ngezinye izikhathi ekwelapheni umdlavuza webele kudinga wesibeletho wezokwelapha. Lokhu kungenziwa nge izidakamizwa analogue of luteinizing-hormone okuthiwa i-ukukhulula ama-hormone (LHRH), isibonelo, "Goserelin" ( "Zoladex") noma "leuprolide" ( "Lyupron"). Le mithi ukuvimba isignali okuthumela emzimbeni ezikhiqiza amaqanda ukukhiqiza estrogen kubo. Zingasetshenziswa eyedwa noma "tamoxifen", aromatase inhibitor, "Fulvestrant" ukulapha hormone kwabesifazane premenopausal.