Timolol (Systemic)
Kelas obat: Agen Antineoplastik
Panganggone Timolol (Systemic)
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). Timolol minangka salah siji saka sawetara β-blockers (kalebu bisoprolol, carvedilol, metoprolol succinate, metoprolol tartrate, nadolol, lan propranolol) sing disaranake dening pedoman hipertensi multidisiplin ACC/AHA 2017 minangka terapi lini pertama kanggo hipertensi ing pasien kanthi penyakit jantung iskemik sing stabil / angina.
Pilihan terapi individu; 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.
MI
Pencegahan sekunder sawise MI akut.
Administrasi sajrone 7-28 dina sawise MI digandhengake karo nyuda kematian kardiovaskular lan reinfark nonfatal.
Para ahli nyaranake terapi β-blocker ing kabeh pasien kanthi disfungsi sistolik ventrikel kiwa lan MI sadurunge; β-blocker kanthi manfaat kematian sing wis bukti (bisoprolol, carvedilol, utawa metoprolol succinate) luwih disenengi. Senajan keuntungan saka β-blockade jangka panjang ing pasien kanthi fungsi ventrikel kiwa normal kurang mantep, para ahli nyaranake nerusake terapi β-blocker paling sethithik 3 taun ing pasien kasebut.
Sakit vaskular
Profilaksis nyeri sirah migrain sing umum utawa klasik.
Angina Stabil Kronis
Wis digunakake ing manajemen angina pektoris stabil kronis† [off-label].
B-Blockers dianjurake minangka anti-iskemik lini pertama obatan ing umume pasien kanthi angina stabil kronis; sanajan beda ing kardioselektivitas, aktivitas simpatomimetik intrinsik, lan faktor klinis liyane, kabeh β-blocker katon padha efektif kanggo panggunaan iki.
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Carane nggunakake Timolol (Systemic)
Umum
Tujuan Pemantauan lan Perawatan BP
Administrasi
Oral Administration
Administrasi oral, biasane kaping pindho saben dina.
Kanggo manajemen hipertensi , dosis sapisan dina bisa uga ing sawetara pasien.
Ing pasien kanthi angina pectoris stabil kronis† [off-label], administrasi oral ing 3 utawa 4 dosis dibagi.
Sajrone therapy pangopènan ing patients karo ngelu vaskular (migrain), bisa ngatur dosis saben dina minangka dosis siji tinimbang dibagi.
Dosis
Kasedhiya minangka timolol maleate; dosis sing dituduhake ing syarat-syarat uyah.
Dewasa
Hipertensi OralKaping pisanan, 10 mg kaping pindho saben dina, kanthi mandiri utawa dikombinasikake karo diuretik.
Tambah dosis kanthi bertahap ing interval saben minggu (utawa luwih suwe) nganti entuk efek sing paling optimal.
Dosis pangopènan biasané yaiku 20-40 mg saben dina, diwenehake ing 2 dosis dibagi; dosis sepisan dina bisa uga ing sawetara pasien. Tambah nganti maksimal 60 mg saben dina (diwenehake ing 2 dosis dibagi). p>Durasi optimal terapi kanggo pencegahan sekunder tetep kudu ditetepake. Para ahli umume nyaranake terapi jangka panjang ing pasien pasca-MI kanthi disfungsi ventrikel kiwa, lan paling ora 3 taun terapi ing wong sing duwe fungsi ventrikel kiwa normal.
Angina Stabil Kronis† [off-label] Oral15-45 mg saben dina, diwenehi 3 utawa 4 dosis dibagi. Setel dosis miturut respon klinis lan njaga detak jantung istirahat 55-60 bpm.
Sakit Kepala Vaskular (Migrain) OralKaping pisanan, 10 mg kaping pindho saben dina. Nyetel dosis miturut respon klinis lan toleransi pasien; ora ngluwihi 30 mg saben dina, diwenehake ing dosis sing dibagi (contone, 10 mg ing wayah esuk lan 20 mg ing wayah sore).
Sajrone terapi pangopènan, bisa ngatur dosis saben dina 20 mg minangka dosis tunggal tinimbang dibagi; sawetara pasien bisa nanggapi kanthi cukup kanggo 10 mg sapisan dina.
Yen tanggepan sing nyukupi ora digayuh sawise 6-8 minggu ing dosis maksimal sing disaranake, mandhegake terapi.
Watesan Resep h3> Dewasa
Hipertensi Oral
Maksimum 60 mg saben dina.
Sakit Kepala Vaskular (Migrain) OralMaksimum 30 mg saben dina.
Populasi Khusus
Gangguan Hepatik
Kudu ngowahi dosis lan/utawa frekuensi administrasi kanggo nanggepi tingkat gangguan hepatik.
Genal. Kerusakan
Kudu ngowahi dosis lan/utawa frekuensi administrasi kanggo nanggepi tingkat gangguan ginjel.
Pasien Geriatrik
Pilih dosis kanthi ati-ati amarga ana hubungane karo umur. nyuda fungsi hepatik, ginjel, lan / utawa jantung lan penyakit bebarengan lan terapi obat. Miwiti ing pungkasan kisaran dosis.
Pènget
Kontraindikasi
Pènget/PanandhapPènget
Gagal Jantung
Kamungkinan presipitasi gagal jantung.
Aja nggunakake ing pasien kanthi gagal jantung sing jelas; bisa digunakake kanthi ati-ati ing pasien kanthi fungsi miokard sing ora nyukupi lan, yen perlu, ing pasien kanthi gagal jantung sing dikompensasi kanthi apik (umpamane, sing dikontrol karo glikosida jantung lan/utawa diuretik).
Pengobatan sing nyukupi (contone, karo glikosida jantung lan / utawa diuretik) lan pengamatan sing cedhak dianjurake yen ana pratandha utawa gejala gagal jantung sing bakal teka; yen gagal jantung terus, mungkasi terapi, mboko sithik yen bisa.
Penarikan dadakan saka TerapiPenolakan terapi kanthi tiba-tiba ora dianjurake amarga bisa nambah gejala angina utawa precipitate MI ing pasien sing nandhang penyakit arteri koroner.
Turunake dosis kanthi bertahap sajrone 1-2 minggu lan ngawasi pasien kanthi ati-ati; menehi saran marang pasien supaya mbatesi aktivitas fisik kanggo sementara nalika mundur saka terapi.
Yen ana exacerbation angina utawa insufficiency koroner akut berkembang, reinstitute terapi kanthi cepet, paling ora kanggo sementara, lan miwiti langkah-langkah sing cocok kanggo manajemen angina pectoris sing ora stabil.
Penyakit bronkospastikKamungkinan inhibisi bronkodilatasi sing diprodhuksi dening katekolamin endogen.
Umume ora bisa digunakake ing pasien sing nandhang penyakit bronkospastik, nanging bisa digunakake kanthi ati-ati ing pasien sing ora nanggapi utawa ora bisa nanggapi. ngidinke perawatan alternatif. Gunakake kanthi ati-ati ing pasien karo bronkospasme sing ora alergi (contone, bronkitis kronis, emfisema) utawa riwayat bronkospasme sing ora alergi. (Deleng Kontraindikasi ing Caution.)
Bedah UtamaKemungkinan tambah risiko sing ana gandhengane karo anestesi umum (contone, hipotensi abot, kesulitan miwiti maneh utawa njaga denyut jantung) amarga nyuda kemampuan jantung kanggo nanggapi refleks β-adrenergik. stimulus.
Sawetara dokter nyaranake mundur bertahap sadurunge operasi elektif. Produsen nyaranake administrasi β-agonis (contone, dopamin, dobutamine, isoproterenol) kanggo mbalikke blokade β-adrenergik yen perlu nalika operasi.
Diabetes lan HipoglikemiaMungkin nyuda tandha lan gejala hipoglikemia (contone, tachycardia, nanging ora kringet utawa pusing). Gunakake kanthi ati-ati ing pasien diabetes mellitus sing nampa obat hipoglikemik.
TirotoksikosisBisa nutupi tandha-tandha hipertiroidisme (contone, tachycardia). Kemungkinan badai tiroid yen terapi tiba-tiba ditarik; ngawasi kanthi ati-ati pasien sing duwe utawa dicurigai ngalami tirotoksikosis.
Reaksi Sensitivitas
Reaksi AnafilaksisPasien kanthi riwayat atopi utawa reaksi anafilaksis marang macem-macem alergen bisa uga luwih reaktif marang tantangan sing bola-bali, ora sengaja, diagnostik, utawa terapeutik karo alergen kasebut nalika njupuk β-blocking. agen; pasien kasebut bisa uga ora nanggapi dosis epinefrin sing biasa.
Pancegahan Umum
Kelemahan OtotBlockade β-Adrenergik sing dilapurake kanggo potentiate kelemahan otot sing konsisten karo gejala miastenia tartamtu (contone, diplopia, ptosis, kelemahan umum). Kekirangan otot sing tambah jarang dilaporake ing sawetara pasien kanthi myasthenia gravis utawa gejala myasthenia.
Insufisiensi serebrovaskularKamungkinan efek kardiovaskuler (umpamane, hipotensi, bradikardia) sing bisa nyebabake aliran getih serebral. Gunakake kanthi ati-ati ing pasien kanthi insufficiency serebrovaskular. Yen ana pratandha utawa gejala sing nuduhake nyuda aliran getih serebral, nimbang mandheg.
Pancegahan LiyaneNuduhake potensi beracun saka β-blocker; mirsani pancegahan biasa saka agen kasebut.
Populasi Tertentu
KandhutanKategori C.
LaktasiDistribusi menyang susu. Mungkasi nyusoni utawa obat kasebut.
Panggunaan PediatrikKeamanan lan khasiat durung ditetepake.
Panggunaan GeriatrikPengalaman sing ora cukup ing pasien umur ≥65 taun kanggo nemtokake manawa pasien geriatrik nanggapi beda karo wong diwasa sing luwih enom.
Diilangi sacara substansial dening ginjel; netepake fungsi ginjel sacara periodik lan nyetel dosis amarga pasien geriatrik luwih cenderung ngalami penurunan fungsi ginjel. (Deleng Pasien Geriatrik ing Dosis lan Administrasi.)
Gangguan HepatikGunakake kanthi ati-ati; pangaturan dosis bisa uga dibutuhake. (Deleng Gangguan Hepatik ing Dosis lan Administrasi.)
Gagal GinjalGunakake kanthi ati-ati; pangaturan dosis bisa uga dibutuhake. (Deleng Gagal Ginjal ing Dosis lan Administrasi.)
Efek Sabar sing Umum
Kesel, sirah, bradikardia, aritmia, pruritus, pusing, dyspnea, iritasi mata.
Apa obatan liyane bakal mengaruhi Timolol (Systemic)
Katon dimetabolisme sebagian dening CYP2D6.
Obat sing Ngaruhi Enzim Mikrosomal Hepatik
Inhibitor CYP2D6: Potensi farmakodinamik (tambah blokade β-adrenergik) lan interaksi farmakokinetik (tambah konsentrasi timolol plasma).
Obat Spesifik
Obat
Interaksi
Komentar
Agen pamblokiran saluran kalsium
Potensi hipotensi, gangguan konduksi AV, lan gagal ventrikel kiwa
Aja nggunakake bebarengan ing pasien sing duwe gangguan fungsi jantung
Clonidine
Blokade β-adrenergik bisa nambah. hipertensi rebound sing bisa kedadeyan sawise mandheg clonidine
Nyetop β-blocker sawetara dina sadurunge mundur bertahap saka clonidine
Yen terapi klonidin diganti karo β-blocker, tundha administrasi sawetara dina sawise clonidine mandheg
Digoxin
Kamungkinan efek aditif ing prolonging wektu konduksi AV nalika digunakake bebarengan karo diltiazem utawa verapamil
Agen hypotensive (hydralazine, methyldopa)
Mungkin nambah efek hipotensi
Panyesuaian dosis sing ati-ati dianjurake
NSAIA
Potensi blunting efek hipotensi
Ngawasi pasien kanthi ati-ati
Quinidine
Kamungkinan potensiasi blokade β-adrenergik (contone, nyuda denyut jantung)
Reserpine
Mungkin efek aditif
Priksa kanthi teliti kanggo bukti bradikardia utawa hipotensi sing nyata (bisa uga diwujudake minangka vertigo, presinkop utawa sinkop, utawa owah-owahan ortostatik ing BP tanpa tachycardia kompensasi)
Disclaimer
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