obat hormon kelamin.pdf
TRANSCRIPT
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Hormon Kelamin
(Agen Sintetik & Inhibitor)
Akhmad Edy Purwoko
Bagian Farmakologi dan Toksikologi
Fakultas Kedokteran UMY
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Menjelaskan farmakodinamik, farmakokinetik, penggunaan klinis, cara pemberian, efek samping, efek toksik, dan penyalahgunaan obat androgenik
Menjelaskan farmakodinamik, farmakokinetik, penggunaan klinis, cara pemberian, efek samping, efek toksik obat estrogenik dan progestin
Menjelaskan sediaan obat, farmakodinamik, farmakokinetik, penggunaan klinis, cara pemberian, efek samping, efek toksik obat kontrasepsi hormonal
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Androgenik &
Anabolik steroid
FSH LH
Testis ~ Ovarium fungsi
gametogenik dan
endokrin
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Androgen !!! testosteron = 8 mg/hr [0,6 g /
dL] saat puber, menurun stl 50 th
95 % sel leydig, 5 % adrenal
Androgen lain <: (kuat) dehydrotestosterone ,
(lemah) androstenedion, dehydroepiandrosterone,
pregnenolon & progesteron + derivat 17-
hidroksilasi nya
65 % testosteron terikat SHBG, sisanya terikat
albumin & + 2 % bebas
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metabolisme
5 -reductase
Androstenedion,
Dehydroepiandrosteron
(DHEA)
Dehydroepiandrosteron
Sulfat (DHEAS)
aktif
Androsteron & etio-
chonanolon
inaktif
Androstenedion oleh
Enzym aromatase
P450 estron
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Efek fisiologik
testosteron, 5 -dehydrotestosteron perubahan
masa puber. Pertumbuhan jaringan umum + (penis,
skrotum), rambut pubis-aksila-jenggot, pengaktifan
Gl. Sebasea, kulit >tebal & berminyak, pita
suara tebal suara nada rendah. Efek lain
pertumbuhan prostat, vesikula seminalis,
penggelapan warna, peningkatan vaskularisasi
kulit.
Androgen stimulasi & menjaga fungsi sex pria
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Androgen meningkatkan bentuk otot
Efek metabolik: ikatan hormon protein,
sintesis faktor pembekuan darah (liver),
triglyseride lipase, 1-antitrypsin, haptoglobin,
dan sialic acid. Merangsang sekresi eritropoitin
ginjal, HDL.
DHEA & DHEAS memperbaiki emosi,
menghambat aterosklerosis.
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Steroid sintetis dg aksi androgenik & anabolik
Testosteron, testosteron cypionat, testosteron
enanthat, testosteron propionat, methyltestosteron,
fluoxymesteron, menthandrostenolon,
oxymetholon, ethylestrenol,oxandrolon, nandrolon
phenpropionat, nandrolon decanoate, stanozol,
dromostanolon propionat.
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Farmakokinetik: testosteron po absorpsi cepat,
metabolisme cepat, kadar aktif + 1/6. Parenteral
absorpsi lebih lambat.
Farmakodinamik: testosteron & dehydrotestosteron
berikatan dg reseptor androgen intraseluler
sintesis enzym, protein fungsional pertumbuhan
& diferensiasi
Efek: perkembangan karakteristik seks sekunder,
dosis besar menekan gnd-tropin atropi jar
interstitial & tubulus tetis, ekskresi nitrogen urin
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Penggunaan klinik:
Tx replacement androgen pd pria
Gangguan ginekologis
Digunakan sebagai agen anabolik kuat
Anemia
Osteoporosis
Perangsang pertumbuhan
Doping pd OR kekuatan & agresifitas
Aging
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Efek yang tidak dinginkan:
Efek maskulinisasi pd anak/wanita
Pendarahan endometrium
Aterosklerosis pd wanita
Retensi Na+ & udem !!! Pd decomp & peny ginjal
Steroid substitusi-17-alkyl disfungsi liver, AST-
bilirubin-ikterus kolestatis
Hiperplasi prostat retensi urin
Jerawat, sleep apne, eritrositosis, ginekomastia,
azoospermia
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Kontraindikasi & peringatan
Wanita hamil/mungkin hamil
Ca-prostat, Ca-payudara
Bayi/anak !!! Efek pertumbuhan otak belum jelas
Penyakit jantung & ginjal !!!
Ca-hepatoseluler anemi aplastik
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Supresi androgen
Estrogen dosis besar
GRH analogs
(goserelin, nafarelin,
buserelin, leuprolid
acetat) kadar
berkesinambungan
menekan gonad
Antagonis GnRH
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Antiandrogen
Penghambat sintesa
steroid
Konversi prekursor
steroid menjadi
androgen (Finasterid menghambat 5 -
reductase konversi testosteron dihydrotestosteron, Tx
BPH, SE penurunan libido, disfungsi ereksi
Penghambat
reseptor (Flutamide, antagonis kompetitif
reseptor androgen, Tx kanker prostat, ES GI upset,
ginekomastia, gg fungsi liver)
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Estrogen & progestin
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Estrogen sintetik:
Steroidal synthetic
Ethinyl estradiol
Mestranol
Quinestrol
Nonsteroidal synthetic
Diethylstilbestrol
Chlorotrianisene
methallenestril
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Farmakokinetik: estrogen alami setelah dirilis ke
sirkulasi akan terikat SHBG globulin- 2 &
albumin dg afinitas rendah. Dlm liver & jaringan
Estradiol estrone & estriol
Estrogen catecol 2-&4-methoxy via cathecol-O-
methyltransferase
Estrogen PO rasio hepatis tinggi sintesis
faktor pembekuan darah & substrat renin plasma
Rasio hepatis diminimalkan via rute pervaginal,
transdermal atau suntikan
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Efek Fisiologis
Mekanisme aksi terikat EREs (estrogen respon
elements) pengaturan transkripsi gen
Maturasi wanita
Efek-efek endometrial
Efek-efek metabolik & kardiovaskular
Efek pada koagulasi darah
Efek-efek lain
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Penggunaan klinis:
Hipogonadisme primer
Terapi hormon pascamenopause
Penggunaan lain
Efek yang tidak diinginkan: pendarahan rahim
pascamenopause, mual, breast tenderness,
hiperpigmentasi, Ca-payudara, Adeno Ca-vagina
(wanita 14-44 th) pd pemakaian diethylstilbestrol
pd ibunya
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Kontraindikasi:
neoplasma (Ca-Endometrium, Ca payudara
Perdarahana genital
Penyakit liver
Gangguan tromboembolik
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Progestin
Sintetis:
Hydroxyprogesteron, medroxyprogesteron
Megestrol, dimethisteron
Desogestrel, gestoden, norgestimate
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Farmakokinetik:
Absorpsi cepat semua rute, t ½ plasma + 5 menit, <
disimpan dlm lemak tbh
Progesteron pregnaediol konjugasi glukoronide
eliminasi lewat urin
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Efek fisiologis:
Mekanisme aksi: mirip steroid yang lain
Efek: metabolisme protein, lemak, karbohidrat
Penggunaan klinis
Aplikasi terapeutik: replacement hormonal therapy
Diagnostik: uji sekresi estrogen
Kontraindikasi: hipertensi, Ca-payudara
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Kontrasepsi hormonal
Mekanisme kerja
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Efek yang tidak diinginkan:
Ringan:
Mual mastalgia, breaktrough blleeding
Perubahan protein serum
Sakit kepala ringan
Withdrawl bleeding
Sedang:
Breaktrough bleeding infeksi vagina
Penambahan BB amenorea
Pigmentasi kulit
Jerawat
Hirsutisme
Dilatasi uretra
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Berat:
Gangguan vaskular
Peny. Tromboembolik
Infark myocardium
Penyakit serebrovaskular
Gangguan gastrointestinal
Depresi
Kanker
Kontraindikasi: peny tromboflebitis, fenomena
tromboembolik, gangguan kardiovaskular, Ca-
payudara, decomp. cordis
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Kontrasepsi dg progestin saja
Kontrasepsi pascakoitus
Kontrasepsi kimia untuk pria: gossypol (no RCT)
Inhibitor & antagonis estrogen + progesteron
Tamoxiphen: antagonis partial estradiol
Raloxiphen: antagonis partial estrogen
Clomiphene: id
Mifepristone: antagonis progesteron
Danazol:
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Penginduksi ovulasi:
Clomiphene
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Baca: Gonadal Hormon & Inhibitor
dalam bab Endocrine (Katzung)