Nebivolol Hydrochloride
Jeneng merek: Bystolic
Kelas obat:
Agen Antineoplastik
Panganggone Nebivolol Hydrochloride
Hipertensi
Manajemen hipertensi (piyambak utawa kombinasi karo kelas agen antihipertensi liyane).
B-Blockers umume ora disenengi kanggo terapi hipertensi lini pertama miturut pedoman hipertensi adhedhasar bukti saiki, nanging bisa uga dianggep ing pasien sing duwe indikasi sing kuat (contone, MI sadurunge, penyakit jantung iskemik, gagal jantung) kanggo panggunaan utawa minangka terapi tambahan ing wong sing ora nanggapi kelas obat sing disenengi (inhibitor ACE, antagonis reseptor angiotensin II, blocker saluran kalsium, utawa diuretik thiazide). Pedoman hipertensi multidisiplin ACC/AHA 2017 nyatakake yen β-blocker sing digunakake kanggo penyakit jantung iskemik sing uga efektif kanggo ngedhunake BP kalebu Bisoprolol, Carvedilol, metoprolol succinate, metoprolol tartrate, nadolol, propranolol, lan timolol.
Individualize pilihan saka therapy; nimbang karakteristik pasien (umpamane, umur, etnis / ras, komorbiditas, risiko kardiovaskular) uga faktor sing gegandhengan karo obat (contone, gampang administrasi, kasedhiyan, efek samping, biaya).
Pedoman hipertensi ACC/AHA 2017 nggolongake BP ing wong diwasa dadi 4 kategori: normal, dhuwur, hipertensi tahap 1, lan hipertensi tahap 2. (Deleng Tabel 1.)
Sumber: Whelton PK, Carey RM, Aronow WS et al. 2017 ACC/AHA/AAPA/ABC/ACPM/AGS/APhA/ASH/ASPC/NMA/PCNA guideline for the prevention, detection, evaluation, and management of high blood pressure in adults: a report of the American College of Cardiology/American Gugus Tugas Asosiasi Jantung babagan Pedoman Praktek Klinis. Hipertensi. 2018;71:e13-115.
Individu sing duwe SBP lan DBP ing 2 kategori beda (contone, SBP munggah pangkat lan DBP normal) kudu ditunjuk minangka kategori BP sing luwih dhuwur (yaiku, BP munggah pangkat).
Tabel 1. Klasifikasi ACC/AHA BP ing Dewasa1200Kategori
SBP (mm Hg)
DBP (mm Hg)
Normal
<120
lan
<80
Inggil
120–129
lan
<80
Hipertensi, Tahap 1
130–139
utawa
80–89
Hipertensi, Tahap 2
≥140
utawa
≥90
Tujuan manajemen hipertensi lan Nyegah yaiku kanggo nggayuh lan njaga kontrol BP sing optimal. Nanging, ambang BP digunakake kanggo nemtokake hipertensi, ambang BP paling luweh kanggo miwiti terapi obat antihipertensi, lan nilai BP target ideal tetep kontroversial.
Pedoman hipertensi ACC/AHA 2017 umume nyaranake target target BP (yaiku, BP kanggo digayuh kanthi terapi obat lan/utawa intervensi nonfarmakologi) <130/80 mm Hg ing kabeh wong diwasa tanpa preduli saka komorbiditas utawa tingkat risiko penyakit kardiovaskular aterosklerotik (ASCVD). Kajaba iku, target SBP <130 mm Hg umume dianjurake kanggo pasien ambulatory non-institusional ≥65 taun kanthi rata-rata SBP ≥130 mm Hg. Tujuan BP iki adhedhasar studi klinis sing nuduhake penurunan risiko kardiovaskular ing tingkat SBP sing luwih murah.
Pedoman hipertensi liyane umume duwe target target BP adhedhasar umur lan komorbiditas. Pedoman kayata sing ditanggepi dening panel ahli JNC 8 umume wis target target BP <140/90 mm Hg tanpa preduli saka risiko kardiovaskular lan nggunakake ambang BP sing luwih dhuwur lan target BP ing pasien tuwa dibandhingake karo sing disaranake dening ACC / AHA 2017. pedoman hipertensi.
Sawetara dokter terus ndhukung target BP sadurunge sing disaranake JNC 8 amarga kuwatir babagan kekurangan data umum saka sawetara uji klinis (contone, sinau SPRINT) sing digunakake kanggo ndhukung ACC/AHA 2017 pedoman hipertensi lan potensial cilaka (contone, efek tamba salabetipun, biaya therapy) versus keuntungan saka BP Mudhunake ing patients ing resiko penyakit jantung.
Pirsani keuntungan potensial saka manajemen hipertensi lan biaya obat, efek sing ora becik, lan risiko sing ana gandhengane karo panggunaan macem-macem obat antihipertensi nalika nemtokake tujuan perawatan BP pasien.
Kanggo pancasan babagan kapan kudu miwiti terapi obat (ambang BP), pedoman hipertensi ACC/AHA 2017 nggabungake faktor risiko kardiovaskular sing ndasari. Penilaian risiko ASCVD dianjurake dening ACC/AHA kanggo kabeh wong diwasa kanthi hipertensi.
ACC/AHA saiki nyaranake miwiti terapi obat antihipertensi saliyane modifikasi gaya urip/perilaku ing SBP ≥140 mm Hg utawa DBP ≥90 mm Hg ing wong diwasa sing ora duwe riwayat penyakit kardiovaskuler (yaiku, pencegahan utama) lan risiko ASCVD sing kurang (resiko 10 taun <10%).
Kanggo pencegahan sekunder ing wong diwasa kanthi penyakit kardiovaskular sing dikenal utawa kanggo Nyegah utama ing risiko ASCVD luwih dhuwur (resiko 10 taun ≥10%), ACC/AHA nyaranake miwiti terapi obat antihipertensi kanthi rata-rata SBP ≥130 mm Hg utawa DBP rata-rata ≥80 mm Hg.
Wong diwasa kanthi hipertensi lan diabetes mellitus, penyakit ginjel kronis (CKD), utawa umur ≥65 taun dianggep duwe risiko dhuwur kanggo penyakit kardiovaskular; ACC / AHA nyatakake yen pasien kasebut kudu duwe terapi obat antihipertensi sing diwiwiti ing BP ≥130/80 mm Hg. Terapi obat individu ing pasien hipertensi lan faktor risiko kardiovaskular utawa liyane.
Ing hipertensi tahap 1, para ahli nyatakake yen cukup kanggo miwiti terapi obat kanthi nggunakake pendekatan perawatan langkah sing siji obat diwiwiti lan dititrasi lan obat liyane ditambahake kanthi urutan kanggo nggayuh target BP. Miwiti terapi antihipertensi kanthi 2 agen lini pertama saka kelas farmakologi sing beda-beda sing disaranake kanggo wong diwasa kanthi hipertensi tahap 2 lan rata-rata BP> 20/10 mm Hg ing ndhuwur target BP.
Pasien hipertensi ireng umume cenderung nanggapi luwih apik. monoterapi karo blocker saluran kalsium utawa diuretik thiazide tinimbang β-blocker. Nanging, respon suda kanggo β-blockers umume diilangi nalika diwenehake bebarengan karo diuretik thiazide.
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Carane nggunakake Nebivolol Hydrochloride
Umum
Tujuan Pemantauan lan Perawatan BP
Administrasi
Administrasi Lisan
Administrasi lisan sapisan saben dina tanpa preduli saka dhaharan.
Sing kerep administrasi. (yaiku, dosis dibagi saben dina) ora mungkin luwih migunani tinimbang administrasi sapisan dina.
Dosis
Kasedhiya minangka nebivolol hidroklorida; dosis ditulis ing syarat-syarat nebivolol.
Dewasa
Hipertensi OralKaping pisanan, 5 mg sapisan dina, salah siji utawa ing kombinasi karo antihipertensives liyane. Tambah ing interval 2 minggu (nganti 40 mg saben dina) ing pasien sing BP ora dikontrol kanthi dosis awal. Sawetara ahli nyatakake kisaran dosis sing biasa yaiku 5-40 mg sapisan saben dina.
Batesan Resep
Dewasa
Hipertensi OralMaksimum 40 mg saben dina.
Populasi Khusus
Gangguan Hepatik
Kaping pisanan, 2,5 mg sapisan dina ing pasien kanthi gangguan hepatik moderat (kelas Child-Pugh B). Tambah dosis kanthi ati-ati, yen perlu.
Kontraindikasi ing pasien kanthi gangguan ati sing abot (Child-Pugh kelas C). (Deleng Kontraindikasi ing Caution.)
Gangguan Ginjal
Kaping pisanan, 2,5 mg sapisan dina ing pasien kanthi gangguan ginjel abot (Clcr <30 mL/menit). Tambah dosis kanthi ati-ati, yen perlu.
Pasien Geriatrik
Panyesuaian dosis ora dibutuhake.
Metabolisme CYP2D6 sing ora apik
Ora ana pangaturan dosis sing dibutuhake ing metabolizer sing kurang saka substrat CYP2D6.
Pènget
Kontraindikasi
Pènget / PancegahanPènget
Pengunduran dadakan saka Terapi
Penghentian terapi dadakan ora dianjurake amarga bisa nambah gejala angina utawa nyebabake MI lan aritmia ventrikel ing pasien CAD. Alon-alon nyuda dosis sajrone udakara 1-2 minggu; ngawasi pasien kanthi ati-ati lan menehi saran supaya pasien mbatesi kegiatan fisik kanggo sementara sajrone mundur saka terapi. Yen exacerbation saka angina dumadi utawa insufficiency koroner akut berkembang, terapi reinstitute (paling ora sementara).
Gagal JantungKamungkinan udan gagal jantung.
Aja nggunakake ing pasien kanthi gagal jantung sing jelas; nggunakake kanthi ati-ati ing pasien kanthi fungsi jantung sing ora nyukupi lan, yen perlu, ing pasien kanthi gagal jantung sing dikompensasi kanthi apik. Yen gagal jantung saya tambah parah, coba mandhegake terapi.
Penyakit Jantung IskemikKeamanan lan khasiat ing pasien angina pectoris utawa MI anyar durung ditetepake.
Bedah UtamaMungkin risiko tambah sing ana gandhengane karo penyakit umum. anestesi (contone, hipotensi abot, kesulitan miwiti maneh utawa njaga denyut jantung) wis kedadeyan ing sawetara pasien sing nampa β-blocker. Gunakake kanthi ati-ati ing pasien sing ngalami operasi gedhe sing nglibatake anestesi umum, utamane karo anestesi miokard-depresan (umpamane, siklopropan, eter, trichloroethylene).
Efek β-blocker bisa dibalik kanthi administrasi β-agonis ( contone, dobutamine, isoproterenol).
Penyakit BronkospastikBronkospasme bisa. Umume ora bisa digunakake ing pasien kanthi penyakit bronkospastik.
Diabetes Mellitus lan HipoglikemiaMungkin nyuda pratandha lan gejala hipoglikemia (umpamane, tachycardia) lan paningkatan hipoglikemia sing disebabake dening insulin.
Gunakake kanthi ati-ati ing pasien kanthi riwayat hipoglikemia spontan lan ing pasien. karo diabetes sing nampa agen hipoglikemik.
TirotoksikosisTandha-tandha hipertiroidisme (contone, tachycardia) bisa ditutupi. Kamungkinan exacerbation saka hipertiroidisme utawa badai tiroid yen terapi tiba-tiba ditarik.
Penyakit Vaskular PeriferKamungkinan presipitasi utawa nambah insufisiensi arteri. Gunakake kanthi ati-ati.
InteraksiPanganggo bareng karo agen blocking saluran kalsium nondihydropyridine (kayata verapamil, diltiazem) mbutuhake ati-ati. (Deleng Obat Spesifik ing Interaksi.)
Panegahan Umum
Resiko Reaksi AnafilaksisPasien sing duwe riwayat reaksi anafilaksis marang macem-macem alergen bisa uga luwih reaktif marang tantangan sing ora disengaja, diagnostik, utawa terapeutik kanthi alergen nalika njupuk β-blocker. Pasien kasebut bisa uga ora nanggapi dosis epinefrin sing biasa.
PheochromocytomaGunakake kanthi ati-ati ing pasien sing dicurigai duwe pheochromocytoma; miwiti terapi karo agen blocking α-adrenergik sadurunge nggunakake β-blocker.
Populasi Tertentu
KandhutanKategori C.
LaktasiDistribusi menyang susu ing tikus; ora dingerteni manawa disebarake menyang susu manungsa. Mungkasi nyusoni utawa obat.
Panggunaan PediatrikKaamanan lan khasiat ora ditetepake ing bocah-bocah <18 taun.
Panggunaan GeriatrikOra ana bedane sing signifikan babagan safety utawa khasiat ing antarane wong diwasa sing luwih enom.
p> Kerusakan HepatikPenurunan reresik ing pasien kanthi gangguan hepatik moderat (kelas Anak-Pugh B); nggunakake kanthi ati-ati. (Deleng Gangguan Hepatik ing Dosis lan Administrasi.)
Keamanan lan khasiat ora ditetepake ing pasien kanthi gangguan hepatik sing abot (kelas Child-Pugh); nggunakake contraindicated ing patients iki. (Deleng Kontraindikasi.)
Gagal GinjalPenurunan reresik ing pasien kanthi gangguan ginjel abot (Clcr <30 mL/menit); nggunakake kanthi ati-ati. (Deleng Gangguan Renal ing Dosis lan Administrasi.)
Ora diteliti sacara khusus ing pasien sing ngalami dialisis; gunakake kanthi ati-ati ing pasien kasebut.
Efek Umum sing Sabar
Sakit sirah, kesel, pusing, diare, mual.
Apa obatan liyane bakal mengaruhi Nebivolol Hydrochloride
Metabolisme dening CYP2D6; ora nyandhet isoenzim CYP ing konsentrasi klinis sing relevan.
Obat-obatan sing Ngaruhi Enzim Mikrosomal Hepatik
Inhibitor CYP2D6: Potensi peningkatan konsentrasi nebivolol plasma; ngawasi pasien kanthi ati-ati lan nyetel dosis miturut respon BP.
Obat Spesifik
Obat
Interaksi
Komentar
Agen antiarrhythmic (contone, amiodarone, disopyramide)
Kemungkinan gangguan konduksi
Gunakake kanthi ati-ati
Agen antidiabetik (oral)
Bisa nutupi gejala hipoglikemia (contone, tachycardia)
Gunakake bebarengan kanthi ati-ati
B-Blockers
Kamungkinan efek aditif
Panganggo bareng karo β-blocker liyane ora dianjurake
Agen pamblokiran saluran kalsium, nondihydropyridine (contone, diltiazem, verapamil)
Kamungkinan gangguan konduksi
Gunakake kanthi ati-ati; monitor BP lan ECG kanthi nggunakake bebarengan
Agen depleting katekolamin (contone, guanethidine, reserpine)
Efek aditif potensial (contone, hipotensi, bradikardia)
Monitor kanggo gejala (contone, vertigo, sinkop, hipotensi postural)
Arang (diaktifake)
Interaksi farmakokinetik ora mungkin
Cimetidine
Potensi konsentrasi nebivolol plasma sing tambah
Ora ana owah-owahan farmakodinamika sing nyata. nebivolol (contone, BP, detak jantung)
Clonidine
Potensi tambah hipertensi rebound sawise mungkasi clonidine
Yen digunakake bebarengan, mungkasi terapi nebivolol sawetara dina sadurunge Terapi klonidin kudu diendhegake kanthi bertahap
Digoxin
Kamungkinan efek negatif aditif ing konduksi AV lan detak jantung; tambah risiko bradikardia
Panganggone bebarengan ora mengaruhi farmakokinetik digoxin utawa nebivolol
Gunakake kanthi ati-ati
Diuretik (contone, furosemide, Hydrochlorothiazide, spironolactone)
Interaksi farmakokinetik ora mungkin
Fluoxetine
Potensi peningkatan konsentrasi nebivolol plasma
Gunakake kanthi ati-ati
Insulin
Mungkin gejala topeng hipoglikemia (contone, tachycardia)
Gunakake kanthi ati-ati
Losartan
Interaksi farmakokinetik ora mungkin
Anestetik umum miokardial-depresan (umpamane, siklopropana, eter, trichloroethylene)
Tambah risiko hipotensi lan kesulitan miwiti maneh utawa njaga denyut jantung
Ngawasi kanthi rapet kanthi nggunakake bebarengan
Paroxetine
Potensi konsentrasi nebivolol plasma sing tambah
Gunakake kanthi ati-ati
Propafenone
Potensi peningkatan konsentrasi nebivolol plasma
Gunakake bebarengan kanthi ati-ati
Quinidine
Potensi peningkatan konsentrasi nebivolol plasma
Gunakake kanthi ati-ati
Ramipril
Interaksi farmakokinetik ora mungkin
Ranitidine
Interaksi farmakokinetik ora mungkin; ora ana owah-owahan nyata ing farmakodinamika nebivolol (contone, BP, denyut jantung)
Sildenafil
Efek aditif ing BP lan pulsa
Potensi nyuda konsentrasi plasma puncak sildenafil; efek sederhana ing konsentrasi plasma puncak lan AUC d-nebivolol
Warfarin
Ora ana efek ing farmakokinetik PT utawa warfarin sing diamati
Disclaimer
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