Chapter Ix 10 Reproductive Hormon

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HORMON SINH DỤC Phan Thị Như Quỳnh, MSc. Bộ môn Hóa Dược Khoa Dược, ĐHYD Huế

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Hóa Dược

Transcript of Chapter Ix 10 Reproductive Hormon

HORMON SINH DC

HORMON SINH DCPhan Th Nh Qunh, MSc.B mn Ha DcKhoa Dc, HYD HuHormon sinh dc nCc cht estrogenCc cht progestogen (progestin)Cc estrogen Estrogen thin nhin:Hormon chnh l estradiol do bung trng sinh raEstron, estriol l cht chuyn ha ca estradiol gan

EstradiolEstronEstriol3

Cc estrogenCc estrogen tng hp:C cu trc gn ging estrogen thin nhinu im: tng tc dng estrogen, gim tc dng ph, tng thi gian tc dng, dng c ng ungTc dng sinh l:Liu sinh l: pht trin c quan sinh dc n, cc c tnh th pht ca phi n; pht trin xng, tc. liu cao: c ch tit FSH, khng androgenEstradiol Thng dng di dng alcol hoc ester

EstradiolEstradiol monobenzoatDng ester benzoat bn gii phng dn estradiol trong c th Tc dng ko di do to cht chuyn ha c hot tnh6Estradiol Tc dng:Duy tr cu trc bnh thng ca da v thnh mch ph n.Gim tc tiu xng nhng khng kch thch to xng.Lm tng HDL, lm gim nh LDL, gim cholesterol, nhng lm tng nh triglycerid.Trn ng mu: estrogen lm tng ng mu, lm tng hm lng plasminogen v lm tng kt tp tiu cu.7Estradiol Ch nh:iu tr thay th: sau mn kinh, thiu nng bung trng, sau ct bung trngChm pht trin, suy gim bung trng tui dy thTc dng ph: Nguy c ung th (v, ni mc t cung), vim tc mch, thay i chuyn ha ng v lipid, tng huyt p, bnh ti mt (do tng cholesterol trong mt), bun nn, thay i tnh tnh.8Estradiol Chng ch nhTuyt i khng dng cho trc tui dy th, khi c thaiKhi u ph thuc vo estrogen nh carcinom ni mc t cung, v.Chy mu ng sinh dc, bnh gan ang trong giai on chn on, c tin s vim tc mch.

Ethinylestradiol iu ch: bn tng hp t estron

Tc dng:17-ethinyl ngn cn tc dng ca enzym chuyn ha gan gi c tc dng mnh theo ng ung:Tim: hiu lc tng ng estradiolUng: hiu lc gp 15-20 ln estradiolChng rng non, phi hp progestin chng th thai dng ng ung

10Ethinylestradiol Ch nh:iu tr thay th sau mn kinhPN thiu nng sinh dc, ung th v PN mn kinhUng th tuyn tin litC 2 nhm ch phm tng hp: nhm c nhn steroid ging estrogen t nhin nh ethinyl estradiol, mestranol, quinestrol; nhm khng c nhn steroid nh diethylstilbestrol (DES), mnh ngang estradiol nhng t/2 di), clorotrianisen, methallenestril. 11Thuc khng estrogen c im:Cht tng hp phi steroidC kch thc v v tr cc nhm chc tng quan vi estradiolC mch nhnhThuc:ClomiphenTamoxifen Clomiphen C ch tc dng:Clomiphen tranh chp vi estrogen ni sinh ti cc receptor vng di i v tuyn yn tng gii phng estrogen ca bung trng.Nu iu tr vo trc giai on phng non, s gy c phng non.Ch nhDng chn on d tr gonadotrophin ca tuyn ynDng trong iu tr v sinh do khng phng non.

13Tamoxifen Tamoxifen l dn xut ca triphenyl ethylen khng mang nhn steroid.

Ch nhUng th v ph thuc vo hormon trn ph n mn kinh

14Tamoxifen

15Tamoxifen C ch tc dng:Ngn cn phc hp estrogen - receptor gn vo v tr tc dng trn ADN ca t bo ch ngn cn s pht trin ca cc khi u ph thuc vo estrogen.

Cc progestinHormon t nhin: progesteronCc cht bn tng hp: cc cht progestin

Khung pregnanProgesteron iu ch:

PseudodiosgeninDehydropregnenolon acetatPregnenolon acetat18Progesteron Tc dng:Trn t cung: Lm chm giai on tng sinh ni mc t cung to iu kin cho trng lm tKhi c thai, progesteron c ch to vng kinh, c ch co bp t cung c tc dng gi thaiTrn tuyn v: Tng sinh chm nang tuyn v chun b cho vic tit saTrn thn nhit: Tng thn nhitTrn chuyn ha: Kch thch lipoproteinlipase lm tng ng m, gim LDH v gim tc dng c li ca estrogen trn chuyn ha m

19Progesteron Ch nh:Phi hp vi estrogen hoc dng ring trong "vin trnh thai" Liu php thay th hormon. Thng phi hp vi estrogen lm gim nguy c gy ung th v, t cung

20Cc progestin tng hp

Levonorgestrel Medroxyprogesteron Norethindron Hormon sinh dc namCc androgenHormon t nhin: Testosteron: hot tnh mnh c5 hydrotestosteron: hot tnh mnh trn tinh hon v tuyn tin litCht chuyn ha: androsteron, hot tnh bng 1/10 testosteronHormon tng hp:Dng ng ung, tc dng ko di, tc dng chuyn bitTestosteron propionat, methyltestosteron, fluoxymesteron c hot tnh androgen mnhNandrolon decanoat, nandrolon phenpropionat c hot tnh tng dng mnhTestosteron iu ch:

24Testosteron Chuyn ha:

Testosteron khng phi l dng c hot tnh mnh. Ti t bo ch, di tc dng ca 5 - reductase, n chuyn thnh dihydrotestosteron c hot tnh. C 2 cng gn vo receptor trong bo tng pht huy tc dng. Trong bnh lng tnh gi, tuy c th vn tit testosteron bnh thng, nhng t bo ch thiu 5 - reductase hoc thiu protein receptor vi testosteron v dihydrotestosteron (Griffin, 1982), nn testosteron khng pht huy c tc dng.Di tc dng ca aromatase mt s m (m, gan, h khu no), testosteron c th chuyn thnh estradiol, c vai tr iu ha chc phn sinh dc.

25Testosteron Tc dng:Tc dng androgen: Lm pht trin tuyn tin lit, ti tinh, c quan sinh dc nam v c tnh sinh dc th yu. i khng vi estrogen.Tc dng tng dng: Lm tng tng hp protein, pht trin xng, lm cho c th pht trin nhanh khi dy th (c bp n nang, xng di ra). Kch thch to hng cu, lm tng tng hp heme v globin.

Tc dngLm pht trin tuyn tin lit, ti tinh, c quan sinh dc nam v c tnh sinh dc th yu.i khng vi oestrogen.Lm tng tng hp protein, pht trin xng, lm cho c th pht trin nhanh khi dy th (c bp n nang, xng di ra). Sau sn ni b ct ha.Kch thch to hng cu, lm tng tng hp heme v globin.26Testosteron Ch nh:iu tr thay th i vi namPN ri lon TK, tun honUng th v, t cung, bung trng (liu cao)Ch :Ung mt tc dng v b ph hy ganTim bp dng ester, testosteron phng thch dn ko di tc dngGc acid ca chc ester cng ln thi gian tc dng cng di Methyltestosteron Androgen bn tng hp t DHEA

Tc dng:Nhm 17-methyl: t b chuyn ha gan hn testosteron Hot tnh sinh dc nam gim 4 ln so vi testosteron

Methyltestosteron Ch nh:Tng t testosteronPhi hp estrogen iu tr a kinh, ri lon kinh nguyt, cc triu chng thi k mn kinh, mt kinh, chng long xng, suy dinh dng, cai saChng ch nh:Nam ung th tuyn tin litPh n c thaiNgi c bnh ganCht khng androgenCht c ch androgenKetoconazol, liarozol, spironolacton Cht c ch 5-reductaseFinasterid Cht i khng androgen ti receptorCyproteron acetat, flutamid, bicalutamid Thank you!