Estropipate; Estrogens, Esterified
Kelas obat: Agen Antineoplastik
Panganggone Estropipate; Estrogens, Esterified
Panganggone estrogen mung ing wanita postmenopause umume diarani terapi sulih estrogen (ERT); nggunakake estrogen ing kombinasi karo progestin biasane diarani minangka terapi penggantian hormon (HRT) utawa terapi hormon postmenopausal.
Terapi Pengganti Estrogen
Manajemen gejala vasomotor moderat nganti abot sing gegandhèngan karo menopause. Esterified estrogen uga digunakake ing kombinasi tetep karo methyltestosteron ing wanita sing ora nanggepi cekap kanggo estrogen piyambak; FDA ngevaluasi maneh kombinasi iki.
Manajemen atrofi vulva lan vagina sing gegandhèngan karo menopause. Yen estrogen digunakake mung kanggo indikasi iki, nimbang nggunakake preparat vaginal topikal.
Osteoporosis
Nyegah osteoporosis postmenopausal. Digunakake bebarengan karo langkah-langkah liyane (contone, diet, kalsium, vitamin D, latihan bobot, terapi fisik) kanggo nyegah mundhut balung lan kemajuan osteoporosis ing wanita postmenopausal.
Estrogen efektif kanggo nyegah osteoporosis nanging digandhengake karo sawetara efek sing ora becik. Yen pencegahan osteoporosis postmenopausal minangka siji-sijine indikasi kanggo terapi, nimbang terapi alternatif (contone, alendronate, raloxifene, risedronate).
Wis efektif ing perawatan osteoporosis ing wanita postmenopause. Biyen dianjurake minangka terapi lini pertama; Nanging, rekomendasi babagan panggunaan HRT sing cocog wis direvisi adhedhasar temuan sinau WHI. (Deleng Warning Boxed.) Evaluasi risiko lan keuntungan saka panggunaan HRT jangka panjang ing manajemen osteoporosis, kanthi njupuk risiko tambah kanker payudara lan penyakit kardiovaskular, kasedhiyan modalitas farmakologis liyane (contone, alendronate, Calcitonin, calcium, raloxifene). , risedronate, vitamin D), lan faktor gaya urip sing bisa diowahi.
Wis digunakake ing sawetara wanita anorexic kanthi amenore kronis kanggo nyuda mundhut kalsium† [off-label] lan, kanthi mangkono, nyuda resiko osteoporosis.
Osteoporosis sing disebabake kortikosteroid
Wis digunakake kanggo nyegah mundhut balung ing wanita postmenopausal sing nampa terapi kortikosteroid dosis rendah nganti moderat† [off-label].
Hipoestrogenisme
Pengobatan hipoestrogenisme sekunder kanggo hipogonadisme, kastrasi, utawa gagal ovarium primer.
Karsinoma Payudara Metastatik
Pengobatan paliatif kanker payudara metastatik ing wanita lan pria sing dipilih. Salah siji saka sawetara agen baris kapindho.
Karsinoma Prostat
Pengobatan paliatif karsinoma prostat sing gumantung androgen lanjut.
Pengurangan Risiko Kardiovaskular† [off-label]
ERT utawa HRT ora nyuda kedadeyan penyakit kardiovaskular. AHA, American College of Obstetricians and Gynecologists, FDA, lan manufaktur nyaranake supaya terapi hormon ora digunakake kanggo nyegah penyakit jantung ing wanita sehat (pencegahan primer) utawa kanggo nglindhungi wanita kanthi penyakit jantung sing wis ana (pencegahan sekunder).
Penyakit Alzheimer
Sadurungé nggunakake HRT, nanging dudu HRT saiki kajaba panggunaan kasebut ngluwihi 10 taun, digandhengake karo nyuda resiko penyakit Alzheimer† [off-label]. Estrogen durung ditampilake kanggo nyegah perkembangan penyakit Alzheimer, lan American Academy of Neurology nyaranake supaya estrogen ora digunakake kanggo perawatan penyakit Alzheimer.
Inisiasi ERT utawa HRT ing wanita ≥65 taun ora ana hubungane. kanthi paningkatan fungsi kognitif. Sawetara wanita sing nampa ERT utawa HRT (estrogen konjugasi khusus 0,625 mg bebarengan karo medroxyprogesterone acetate 2,5 mg saben dina utawa estrogen konjugasi 0,625 mg saben dina) ngalami efek ngrugekake. Insiden kemungkinan demensia ing wanita sing nampa ERT utawa HRT luwih dhuwur tinimbang wanita sing nampa plasebo. Panganggone ERT utawa HRT kanggo nyegah demensia utawa penurunan kognitif ing wanita ≥65 taun ora dianjurake.
Pembengkakan Payudara Postpartum
Digunakake ing jaman kepungkur kanggo nyegah pembengkakan payudara postpartum† [off-label]; FDA wis mbatalake persetujuan obat sing ngemot estrogen kanggo indikasi iki, amarga estrogen durung ditampilake aman kanggo panggunaan iki. (Deleng Lactation ing Cautions.)
Meteng
Ora efektif kanggo maksud apa wae nalika meteng; nggunakake contraindicated ing wanita ngandhut. (Deleng Pregnancy ing Cautions.)
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Carane nggunakake Estropipate; Estrogens, Esterified
Umum
ERT cocok kanggo wanita sing wis ngalami histerektomi (nyegah paparan progestin sing ora perlu).
Administrasi
Atur estropipat lan estrogen esterifikasi kanthi lisan.
Terapi estrogen umume ditindakake kanthi regimen dosis saben dina sing terus-terusan utawa, minangka alternatif, ing regimen siklik. Nalika ditrapake sacara siklus, estrogen biasane diwenehake sapisan saben dina kanggo 3 minggu banjur 1 minggu tanpa obat; regimen diulang yen perlu.
Administrasi Lisan
Administrasi lisan siji utawa luwih saben dina.
Yen estropipate utawa estrogen esterifikasi digunakake kanggo ngatur gejala vasomotor, miwiti perawatan kapan wae ing wanita sing durung menstruasi sajrone 2 sasi sadurunge; Yen pasien menstruasi, miwiti administrasi siklus ing dina kaping 5 siklus.
Dosis
Dosis individu miturut kondisi sing diobati lan toleransi lan respon terapeutik pasien.
Kanggo nyilikake risiko efek salabetipun, gunakake dosis efektif sing paling murah. Amarga potensial tambah risiko acara kardiovaskular, kanker payudara, lan acara thromboembolic vena, mbatesi terapi estrogen lan estrogen / progestin menyang dosis sing paling efektif lan durasi terapi paling cendhak sing cocog karo tujuan lan risiko perawatan kanggo wanita kasebut.
Evaluasi maneh terapi estrogen lan estrogen/progestin kanthi periodik (yaiku, kanthi interval 3 nganti 6 sasi).
Dewasa
Terapi Pengganti Estrogen Gejala Vasomotor OralEstropipate: 0,75–6 mg saben dina kanthi regimen siklik.
Estrogen esterifikasi: 1,25 mg saben dina ing regimen siklik.
Estrogen esterifikasi ing kombinasi tetep karo metiltestosteron: Esterifikasi estrogen 0,625 mg karo metiltestosteron 1,25 mg saben dina ing regimen siklik (3 minggu ing, 1 minggu off ). Utawa, estrogen esterifikasi 1,25 mg karo metiltestosteron 2,5 mg saben dina ing regimen siklik.
Vulvar lan Vaginal Atrophy OralEstropipate: 0,75-6 mg saben dina ing regimen siklik.
Esterifikasi estrogen: 0,3–≥1,25 mg saben dina ing regimen siklis.
Nyegah Osteoporosis ing Wanita Postmenopausal OralEstropipate: 0,75 mg saben dina ing regimen siklik (25 dina, 6 dina off).
Hypoestrogenism Female Hypogonadism OralEstropipate: 1.5-9 mg saben dina kanggo 3 minggu banjur 8-10 dina tanpa obat; yen menstruasi ora kedadeyan ing pungkasan periode 8 nganti 10 dina tanpa obat, baleni jadwal dosis sing padha. Jumlah kursus sing dibutuhake kanggo ngrangsang menstruasi beda-beda gumantung saka respon endometrium. Yen ora ana getihen sing ora bisa ditindakake, progestin bisa diwènèhaké bebarengan ing minggu katelu siklus.
Esterifikasi estrogen: 2,5-7,5 mg saben dina ing dosis dibagi kanggo 20 dina, banjur 10 dina tanpa tamba. Jumlah kursus sing dibutuhake kanggo ngrangsang menstruasi beda-beda gumantung saka respon endometrium. Yen menstruasi ora kedadeyan ing pungkasan siklus lengkap pisanan, baleni jadwal dosis sing padha. Yen menstruasi kedadeyan sadurunge pungkasan periode bebas obat 10 dina, miwiti regimen estrogen-progestin kanthi estrogen esterifikasi 2.5-7.5 mg sing diwenehake saben dina ing dosis dibagi kanggo 20 dina; ngatur progestin lisan sajrone 5 dina pungkasan administrasi estrogen esterifikasi. Yen menstruasi diwiwiti sadurunge regimen estrogen-progestin rampung, mungkasi terapi lan banjur bali maneh ing dina kaping lima menstruasi.
Kastrasi Wanita utawa Gagal Ovarium Utama OralEstropipate: 1,5-9 mg saben dina suwene 3 minggu, banjur diterusake. dening 8-10 dina tanpa tamba. Setel dosis miturut keruwetan gejala lan respon terapeutik.
Esterifikasi estrogen: 1,25 mg saben dina ing regimen siklik. Setel dosis miturut keruwetan gejala lan respon terapeutik.
Karsinoma Payudara Metastatik OralEsterifikasi estrogen: 10 mg 3 kali dina kanggo ≥3 sasi.
Karsinoma Prostat OralEsterifikasi estrogen: 1,25–2,5 mg 3 kali dina.
Pènget
Kontraindikasi
Pènget/PanandhapPènget
Gangguan Kardiovaskular
Terapi estrogen/progestin sing gegandhèngan karo tambah risiko MI, stroke, DVT, lan emboli paru. Terapi estrogen digandhengake karo tambah risiko stroke lan DVT. (Deleng Warning Boxed.) Mungkasi estrogen langsung yen ana kedadeyan kasebut utawa dicurigai. Panganggone ERT utawa HRT ora dianjurake kanggo wanita sing duwe riwayat stroke utawa serangan iskemik transien. (Deleng Contraindications ing Cautions.)
Ngatur faktor risiko penyakit kardiovaskular kanthi tepat (contone, hipertensi, diabetes mellitus, panggunaan tembakau, hiperkolesterolemia, obesitas) lan/utawa tromboembolisme vena (riwayat tromboembolisme vena pribadi utawa kulawarga, obesitas, lupus eritematosus sistemik). (Deleng Contraindications ing Cautions.)
Nyetop estrogen, sawayah-wayah, paling sethithik 4-6 minggu sadurunge operasi sing digandhengake karo tambah risiko thromboembolism utawa sajrone imobilisasi sing suwe.
Kanker EndometriumPanganggone terapi estrogen tanpa lawan ing wanita sing duwe uterus digandhengake karo tambah risiko kanker endometrium. Pengawasan lan evaluasi klinis penting. Nindakake tes diagnostik kanggo ngilangi ganas ing wanita kanthi pendarahan vagina sing ora didiagnosis, terus-terusan utawa bola-bali.
Kedadeyan saka hiperplasia endometrium suda sacara substansial nalika progestin digunakake bebarengan.
Kanker PayudaraHRT sing digandhengake karo tambah risiko kanker payudara.
Kabeh wanita postmenopause kudu nampa pemeriksaan payudara saben taun dening dokter lan nindakake pemeriksaan diri saben wulan. Jadwal mammography periodik adhedhasar umur pasien lan faktor risiko.
DemensiaERT utawa HRT ing wanita ≥65 taun wis digandhengake karo tambah risiko ngembangake kemungkinan demensia. Apa temuan kasebut ditrapake kanggo wanita sing luwih enom ora dingerteni. (Deleng Penyakit Alzheimer ing Panggunaan.)
Penyakit Kandung EmpeduERT sing gegandhengan karo tambah risiko penyakit kandung empedu sing mbutuhake operasi.
HiperkalsemiaEstrogen bisa nyebabake hiperkalsemia abot ing pasien kanker payudara lan metastase balung. Mungkasi obat kasebut lan miwiti terapi sing cocog kanggo nyuda konsentrasi kalsium serum yen ana hiperkalsemia.
Efek OkularTrombosis retina kacarita. Mungkasi pemeriksaan sing ditundha yen mundhut sesanti parsial utawa lengkap, utawa tiba-tiba muncul proptosis, diplopia, utawa migren. Mungkasi estrogen yen papilledema utawa lesi pembuluh darah retina kacathet nalika pemeriksaan.
Pancegahan Umum
Peningkatan BPArang banget, kenaikan BP sing signifikan amarga reaksi idiosinkratik marang estrogen. ERT umume ora digandhengake karo BP munggah pangkat. Monitor BP kanthi interval biasa.
HypertriglyceridemiaTerapi estrogen bisa uga digandhengake karo paningkatan konsentrasi trigliserida plasma sing nyebabake pankreatitis ing wanita kanthi lipid serum sing tambah.
Retensi CairanEstrogen bisa nyebabake sawetara tingkat retensi cairan; nggunakake kanthi ati-ati lan ngawasi kanthi ati-ati ing pasien kanthi kahanan sing bisa saya tambah amarga retensi cairan (contone, gagal jantung utawa ginjel).
HypocalcemiaGunakake kanthi ati-ati ing pasien kanthi hipokalsemia abot.
Kanker OvariumTerapi estrogen jangka panjang sing digandhengake karo tambah insiden kanker ovarium ing sawetara studi epidemiologi. Panaliten liyane ora nuduhake asosiasi sing penting sacara klinis.
EndometriosisEstrogen bisa nambah endometriosis.
Transformasi ganas saka sisa implan endometrium kacarita arang banget ing wanita sing nampa estrogen tanpa lawan sawise histerektomi. Coba tambahan progestin ing wanita kanthi endometriosis residual sawise histerektomi.
Kahanan LiyaneEstrogen bisa nambah panandhang asma, diabetes mellitus, epilepsi, migren, porfiria, lupus eritematosus sistemik, lan hemangioma hepatik; nggunakake kanthi ati-ati ing pasien kanthi kondisi kasebut.
Terapi KombinasiYen estrogen esterifikasi digunakake ing kombinasi tetep karo metiltestosteron utawa estrogen digunakake bebarengan karo progestin, nimbang pancegahan, ati-ati, lan kontraindikasi saka agen sing bebarengan.
Populasi Tertentu
KandhutanKategori X. (Deleng Kontraindikasi ing Ati-ati.)
Paparan ing utero wanita kanggo diethylstilbestrol (DES [ora kasedhiya kanggo komersial maneh ing AS]) digandhengake kanthi risiko tambah adenosis vagina, displasia sel skuamosa ing cervix, lan kanker vagina sel jernih ing umur sabanjure.
Paparan ing utero wong lanang kanggo DES digandhengake karo tambah risiko kelainan genital lan bisa uga testis. kanker ing salawas-lawase.
Wong wadon sing nampa DES nalika meteng bisa nambah risiko kanker payudara; hubungan sebab-akibat ora kabukten.
LaktasiAdministrasi estrogen kanggo wanita sing nyusoni wis digandhengake karo penurunan jumlah lan kualitas susu sing luwih murah. Jumlah estrogen sing bisa dideteksi wis diidentifikasi ing susu wanita sing nampa obat kasebut. Ati-ati menehi saran.
Panggunaan PediatrikTerapi estrogen wis digunakake kanggo induksi pubertas ing remaja kanthi sawetara bentuk wektu tundha pubertas. Keamanan lan khasiat estrogen ing bocah-bocah sing durung ditetepake.
Gunakake terapi estrogen kanthi ati-ati lan ngawasi kanthi ati-ati yen wutah balung durung rampung, amarga estrogen bisa nyebabake penutupan epifisis prematur.
Panggunaan GeriatrikPengalaman sing ora cukup karo estrogen esterifikasi ing kombinasi tetep karo methyltestosteron (Estrast, Estratest HS) ing pasien geriatrik kanggo nemtokake manawa pasien geriatrik nanggapi beda karo wanita sing luwih enom. Pilih dosis kanthi ati-ati amarga nyuda fungsi ati, ginjel, lan/utawa sing gegandhengan karo umur lan potensial penyakit bebarengan lan terapi obat.
Risiko tambah kemungkinan ngalami demensia ing wanita ≥65 taun. (Deleng Demensia ing Ati-ati.)
Gangguan HepatikEstrogen bisa uga kurang metabolisme ing pasien sing duwe gangguan hepatik. (Deleng Contraindications ing Cautions.)
Ati-ati disaranake ing pasien kanthi riwayat jaundice kolestatik sing ana gandhengane karo panggunaan estrogen sadurunge utawa nalika meteng; mandheg yen jaundice kambuh.
Gagal GinjalGunakake kanthi ati-ati. (Deleng Cairan Retensi ing Cautions.)
Efek Umum sing Sabar
Pendarahan vagina, moniliasis vagina.
Apa obatan liyane bakal mengaruhi Estropipate; Estrogens, Esterified
Katon dimetabolisme sebagian dening CYP3A4.
Obat sing Ngaruhi Enzim Mikrosomal Hepatik
Inhibitor CYP3A4: Potensi interaksi farmakokinetik (konsentrasi estrogen plasma mundhak).
Induser CYP3A4: Potensi interaksi farmakokinetik (mudhun konsentrasi estrogen plasma).
Obat lan Panganan Spesifik
Obat utawa Pangan
Interaksi
Komentar
Antikoagulan, oral
Kamungkinan ngurangi tumindak antikoagulan
Monitor; tambah dosis warfarin yen perlu
Anti jamur, azoles (itrakonazol, ketokonazol)
Konsentrasi estrogen plasma bisa tambah; tambah potensial kanggo efek salabetipun
Kamungkinan nyuda konsentrasi estrogen plasma; potensial kanggo nyuda efek terapeutik lan / utawa owah-owahan ing pendarahan uterus
Kortikosteroid (hydrocortisone)
Efek anti-inflamasi sing luwih apik saka hidrokortison ing pasien kanthi penyakit kulit inflamasi kronis
Amati tandha-tandha efek kortikosteroid sing berlebihan; nyetel dosis kortikosteroid nalika miwiti utawa mungkasi estrogen
Jus jeruk bali
Konsentrasi estrogen plasma bisa tambah; tambah potensial kanggo efek salabetipun
Antibiotik Macrolide (clarithromycin, erythromycin)
Kamungkinan nambah konsentrasi estrogen plasma; tambah potensial kanggo efek salabetipun
Phenobarbital
Konsentrasi estrogen plasma sing bisa mudhun; potensial ngurangi efek terapeutik lan/utawa owah-owahan ing getihen uterus
Rifampin
Konsentrasi estrogen plasma bisa mudhun; potensial kanggo ngurangi efek terapeutik lan/utawa owah-owahan ing getihen uterus
Ritonavir
Kamungkinan nambah konsentrasi estrogen plasma; tambah potensial kanggo efek salabetipun
St. John's wort (Hypericum perforatum)
Konsentrasi estrogen plasma sing bisa mudhun; potensial kanggo ngurangi efek terapeutik lan/utawa owah-owahan pendarahan uterus
Agen tiroid
Nambah konsentrasi globulin pengikat tiroid
Tambahan dosis agen pengganti tiroid bisa uga dibutuhake; monitor fungsi tiroid
Disclaimer
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