Timolol (EENT)
Kelas obat: Agen Antineoplastik
Panganggone Timolol (EENT)
Hipertensi Okular lan Glaukoma
Timolol: Pengurangan IOP sing dhuwur ing pasien karo glaukoma sudut terbuka utawa hipertensi okular.
Data saiki nyaranake khasiat sing padha kanggo timolol maleate lan timolol minangka hemihidrat. Khasiat solusi Istalol timolol maleate (diformulasi karo kalium sorbate) sing diwenehake minangka larutan timolol 0,5% sapisan dina uga padha karo timolol maleate (diformulasi tanpa kalium sorbate) sing diwenehake minangka larutan timolol 0,5% kaping pindho saben dina.
Dorzolamide kombinasi tetep 2% lan timolol 0,5%: Ngurangi IOP munggah ing pasien karo glaukoma sudut terbuka utawa hipertensi okular sing durung nanggapi kanthi cukup (yaiku, gagal nggayuh target IOP sing ditemtokake sawise sawetara pangukuran liwat wektu) agen pamblokiran β-adrenergik topikal. Nalika ditrapake kaping pindho saben dina, efek nyuda IOP yaiku 1-3 mm Hg luwih gedhe tinimbang dorzolamide 2% sing diwenehake 3 kali dina utawa timolol 0,5% kaping pindho saben dina lan kira-kira 1 mm Hg kurang saka sing diraih kanthi nggunakake dorzolamide 2% bebarengan. 3 kali dina lan timolol 0,5% kaping pindho saben dina.
Kombinasi tetep brimonidine tartrate 0,2% lan timolol 0,5%: Pengurangan TIO munggah ing pasien glaukoma utawa hipertensi okular sing mbutuhake terapi tambahan utawa pengganti amarga ora cukup. kontrol IOP. Nalika diterbitake kaping pindho saben dina, efek nyuda IOP yaiku 1-3 mm Hg luwih gedhe tinimbang brimonidine tartrate 0,2% sing diwenehake 3 kali dina, 1-2 mm Hg luwih gedhe tinimbang timolol 0,5% sing diwenehake kaping pindho saben dina, lan kira-kira 1-2 mm. Hg kurang saka sing diraih kanthi nggunakake brimonidine tartrate 0,2% 3 kali dina lan timolol 0,5% kaping pindho saben dina. kahanan, lan karakteristik tamba (contone, frekuensi dosis, efek salabetipun, biaya). Kanthi regimen agen tunggal, pangurangan IOP kira-kira 25-33% kanthi analog prostaglandin topikal; 20-25% karo agen pamblokiran β-adrenergik topikal, agonis α-adrenergik, utawa agen miotik (parasympathomimetic); 20-30% karo inhibitor karbonik anhidrase oral; 18% karo inhibitor rho kinase topikal; lan 15-20% karo inhibitor karbonik anhidrase topikal.
Analog prostaglandin asring dianggep minangka terapi awal tanpa ana pertimbangan liyane (contone, kontraindikasi, pertimbangan biaya, intoleransi, efek samping, penolakan pasien) amarga aktivitas sing relatif luwih gedhe, administrasi sapisan dina, lan frekuensi kurang saka efek salabetipun sistemik; Nanging, efek salabetipun ocular bisa kelakon.
Tujuane kanggo njaga TIO ing ngendi mundhut lapangan visual ora bisa nyuda kualitas urip sajrone urip pasien.
Penurunan IOP pretreatment kanthi ≥25% ditampilake kanggo alon progresi glaukoma sudut terbuka primer. Setel target IOP awal (adhedhasar ombone karusakan saraf optik lan / utawa mundhut lapangan visual, IOP awal nalika karusakan, tingkat kemajuan, pangarep-arep urip, lan pertimbangan liyane) lan nyuda IOP menyang tujuan kasebut. Setel target IOP munggah utawa mudhun yen perlu sajrone penyakit.
Terapi kombinasi karo obat saka kelas terapeutik sing beda asring dibutuhake kanggo ngontrol IOP.
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Carane nggunakake Timolol (EENT)
Umum
Administrasi
Ophthalmic Administration
Aplikasi topikal ing mripat minangka solusi ophthalmic sing ngandhut timolol piyambak utawa ing kombinasi tetep karo brimonidine utawa dorzolamide.
Singkirake kontaminasi wadhah solusi. (Deleng Keratitis Bakteri ing Ati-ati.)
Yen luwih saka siji preparat ophthalmic topikal digunakake, aturake preparat kasebut kanthi interval paling sethithik 5 menit (sawetara pabrikan nyaranake interval paling sethithik 10 menit). Nyedhiyakake preparat topikal liyane paling sethithik 10 menit sadurunge dosis larutan pembentuk gel timolol.
Balikake lan goyangake wadhah solusi pembentuk gel ophthalmic timolol sapisan sadurunge administrasi saben dosis.
Sawetara solusi ophthalmic timolol ngandhut benzalkonium klorida. Copot lensa kontak sadurunge ngatur saben dosis solusi kasebut; bisa masang maneh lensa 15 menit sawise dosis. (Deleng Lensa Kontak ing Ati-ati.)
Atur solusi tanpa pengawet saka timolol utawa kombinasi tetep dorzolamide lan timolol kanthi topikal menyang mripat siji utawa loro sanalika sawise mbukak wadhah, banjur langsung mbuwang solusi sing isih ana ing wadah sing mbukak. siji-nggunakake wadhah.
Dosis
Kasedhiya minangka timolol maleate utawa timolol (minangka hemihidrat); dosis ditulis ing syarat-syarat timolol.
Pasien Pediatrik
Hipertensi Okular lan Glaukoma OphthalmicSolusi ophthalmic Timolol (minangka timolol maleate) ing pasien pediatrik ≥2 taun: Kaping pisanan, 1 tetes larutan 0,25% ing sing kena pengaruh. mripat (s) kaping pindho saben dina. Bisa nambah dosis dadi 1 tetes solusi 0,5% ing mripat sing kena pengaruh kaping pindho saben dina yen perlu. Banjur bisa nyuda dosis dadi 1 tetes saka kekuatan efektif ing mripat sing kena pengaruh sapisan dina yen IOP tetep tetep.
Brimonidine tartrate 0,2% lan solusi ophthalmic timolol 0,5% ing pasien pediatrik ≥2 taun: 1 tetes ing mripat sing kena pengaruh kaping pindho saben dina (kira-kira saben 12 jam).
Dorzolamide 2% lan timolol 0,5% solusi ophthalmic ing pasien pediatrik ≥2 taun: 1 tetes ing mripat sing kena pengaruh kaping pindho saben dina.
Dewasa
Hipertensi Okular lan Glaukoma OphthalmicSolusi ophthalmic Timolol (minangka timolol maleate utawa hemihydrate): Kaping pisanan, 1 tetes larutan 0,25% ing mripat sing kena pengaruh kaping pindho saben dina. Bisa nambah dosis dadi 1 tetes solusi 0,5% ing mripat sing kena pengaruh kaping pindho saben dina yen perlu. Banjur bisa nyuda dosis dadi 1 tetes saka kekuatan efektif ing mripat sing kena pengaruh sapisan dina yen IOP tetep tetep.
Istalol (ngandhut kalium sorbate) solusi ophthalmic timolol: 1 tetes larutan 0,5% ing mripat sing kena pengaruh sapisan dina esuk. (Deleng Bioavailability ing Farmakokinetik.)
Solusi ophthalmic timolol sing mbentuk gel: 1 tetes larutan 0,25 utawa 0,5% ing mripat sing kena pengaruh sapisan dina.
Brimonidine tartrate 0,2 % lan timolol 0,5% larutan ophthalmic: 1 tetes ing mripat sing kena pengaruh kaping pindho saben dina (kira-kira saben 12 jam).
Dorzolamide 2% lan solusi ophthalmic timolol 0,5%: 1 tetes ing mripat sing kena pengaruh( s) kaping pindho saben dina.
Yen target IOP ora digayuh, bisa miwiti agen hipotensi okular tambahan utawa alternatif. (Waca Hipertensi Okular lan Glaukoma ing Panggunaan.) Panggunaan bebarengan saka macem-macem agen pamblokiran β-adrenergik ophthalmic topikal ora dianjurake.
Batesan Resep
Pasien Anak
Hipertensi Okular lan Glaukoma OphthalmicSolusi ophthalmic Timolol (minangka timolol maleate): Dosis > 1 tetes larutan 0,5% ing mripat sing kena pengaruh kaping pindho saben dina umume ora ngasilake IOP maneh.
Dewasa
Hipertensi Okular lan Glaukoma OphthalmicSolusi ophthalmic Timolol (minangka timolol maleate utawa hemihydrate): Dosis > 1 tetes larutan 0,5% ing mripat sing kena pengaruh kaping pindho saben dina. ora ngasilake pangurangan luwih ing IOP.
Solusi pembentuk gel ophthalmic Timolol: Dosis > 1 tetes larutan 0,5% ing mripat sing kena pengaruh sapisan dina ora diteliti.
Pènget
Contraindications
Pènget/PanandhapReaksi Sensitivitas
Riwayat Reaksi Atopi utawa Anafilaksis
Pasien kanthi riwayat atopi utawa reaksi anafilaksis sing abot marang macem-macem alergen bisa uga luwih reaktif marang tantangan sing ora sengaja, diagnostik, utawa terapeutik sing bola-bali. alergen nalika njupuk agen pamblokiran β-adrenergik; patients kuwi bisa unresponsive kanggo dosis biasanipun saka epinephrine digunakake kanggo nambani reaksi anaphylactic.
Panganggone Kombinasi Tetep
Yen digunakake ing kombinasi tetep karo brimonidine utawa dorzolamide, nimbang ati-ati, pancegahan, kontraindikasi, lan interaksi obat sing ana gandhengane karo saben obat ing kombinasi tetep.
Efek Sistemik
Bisa diserap sacara sistemik sawise aplikasi topikal ing mripat; nimbang pancegahan biasa sing ana gandhengane karo panggunaan sistemik agen pamblokiran β-adrenergik nalika nggunakake timolol topikal.
Gagal Jantung
Reaksi jantung sing abot, kalebu pati sing ana gandhengane karo gagal jantung, dilapurake ing pasien sing nampa timolol sistemik utawa topikal (okular). Ing pasien sing nyuda kontraktilitas miokard, stimulasi simpatik bisa uga penting kanggo dhukungan sirkulasi.
Bisa nyebabake gagal jantung sing luwih abot ing pasien sing gagal jantung sing wis ana lan bisa nyebabake gagal jantung ing sawetara pasien tanpa riwayat gagal jantung.
Kontraindikasi kanggo pasien sing ngalami kejut kardiogenik utawa gagal jantung sing jelas. Ing pasien tanpa riwayat gagal jantung, mungkasi terapi kanthi tandha pisanan utawa gejala gagal jantung.
Penyakit Pernafasan
Reaksi pernapasan sing abot, kalebu pati amarga bronkospasme, dilapurake ing pasien asma sing nampa timolol sistemik utawa topikal (okular).
Kontraindikasi kanggo pasien asma, riwayat asma, utawa COPD abot (contone, bronkitis kronis utawa emfisema abot). Pasien karo COPD sing entheng utawa cukup abot, penyakit bronkospastik saliyane asma, utawa riwayat penyakit bronkospastik kasebut umume ora kudu nampa agen pamblokiran β-adrenergik.
Kekirangan Otot
Agen pamblokiran β-Adrenergic dilapurake kanggo potentiate kelemahan otot sing konsisten karo manifestasi myasthenic tartamtu (contone, diplopia, ptosis, lan kelemahan umum).
Timolol kacarita arang nambah kelemahan otot ing pasien kanthi gejala myasthenia gravis utawa myasthenia.
Diabetes Mellitus
Agen pamblokiran β-adrenergik bisa nutupi tandha lan gejala hipoglikemia akut; kanthi ati-ati ing pasien sing ngalami hipoglikemia spontan lan ing pasien diabetes (utamane sing duwe diabetes labil) sing nampa agen hipoglikemik.
Tirotoksikosis
Agen pamblokiran β-adrenergik bisa nutupi tandha-tandha hipertiroidisme (contone, takikardia).
Kamungkinan badai tiroid yen agen pamblokiran β-adrenergik tiba-tiba ditarik; kanthi ati-ati ngawasi pasien sing duwe utawa dicurigai ngalami tirotoksikosis.
Keratitis Bakteri
Keratitis bakteri dilapurake sawise kontaminasi sing ora disengaja saka wadah pirang-pirang dosis solusi ophthalmic topikal, utamane ing pasien sing nandhang penyakit kornea bebarengan utawa gangguan permukaan epitel okular.
Penanganan preparat ophthalmic sing ora bener bisa nyebabake kontaminasi solusi kasebut dening bakteri umum sing bisa nyebabake infeksi okular. Kerusakan serius ing mripat lan mundhut sesanti sakteruse bisa disebabake nggunakake preparat ophthalmic sing kontaminasi. (Deleng Nasehat kanggo Pasien.)
Bedah Utama
Kemungkinan tambah risiko sing ana gandhengane karo anestesi umum (contone, hipotensi abot, kesulitan miwiti maneh utawa njaga denyut jantung) amarga nyuda kemampuan jantung kanggo nanggapi rangsangan β-adrenergik refleks.
Perlu kanggo mundur saka agen pamblokiran β-adrenergik sadurunge operasi gedhe kontroversial; sawetara dokter nyaranake mundur bertahap saka agen pamblokiran β-adrenergik sadurunge operasi elektif.
Yen perlu sajrone operasi, bisa mbalikke efek saka agen pamblokiran β-adrenergik kanthi menehi dosis agonis adrenergik sing cukup.
Angle-closure Glaucoma
Timolol nduweni pengaruh cilik utawa ora ana ing ukuran pupil; Aja nggunakake dhewe ing pasien karo glaukoma sudut tertutup.
Insufisiensi serebrovaskular
Ati-ati disaranake ing pasien kanthi insufisiensi serebrovaskular amarga efek potensial saka agen pamblokiran β-adrenergik ing BP lan pulsa. Coba terapi alternatif yen ana pratandha utawa gejala sing nuduhake nyuda aliran getih serebral.
Detasemen Choroidal
Detasemen Choroidal sawise prosedur filtrasi dilaporake.
Lensa Kontak
Sawetara solusi ophthalmic timolol ngandhut benzalkonium klorida, sing bisa diserap dening lensa kontak alus. Copot lensa kontak sadurunge ngatur saben dosis solusi kasebut; bisa masang maneh lensa 15 menit sawise dosis.
Populasi Tertentu
KandhutanKategori C.
Gunakake mung yen keuntungan potensial mbenerake risiko sing bisa ditindakake kanggo janin.
LaktasiDisebarake menyang susu sawise aplikasi topikal menyang mripat. Mungkasi nyusoni utawa obat kasebut.
Panggunaan PediatrikSolusi ophthalmic Timolol maleate: Keamanan lan khasiat ing pasien pediatrik ≥2 taun ditetepake adhedhasar bukti saka studi sing nyukupi lan dikontrol kanthi apik ing bocah lan wong diwasa; safety lan khasiat ora ditetepake ing pasien pediatrik <2 taun. Keamanan lan khasiat Istalol (larutan timolol maleate sing diformulasikan karo kalium sorbate) ora ditetepake ing pasien pediatrik.
Timolol (minangka hemihidrat) solusi ophthalmic: Keamanan lan khasiat ora ditetepake ing pasien pediatrik.
Solusi ophthalmic brimonidine lan timolol: Keamanan lan khasiat ditetepake ing pasien pediatrik umur 2-16 taun adhedhasar bukti saka studi sing nyukupi lan dikontrol kanthi apik babagan kombinasi tetep ing wong diwasa lan data tambahan saka panaliten sing ngevaluasi obat sing diwenehake kanthi individu (brimonidine). tartrate 0,2% diterbitake kaping 3 saben dina minangka tambahan kanggo terapi timolol) ing bocah-bocah umur 2-7 taun kanthi glaukoma. Insiden ngantuk katon ana hubungane karo umur lan bobot, kedadeyan ing 50-83% bocah umur 2-6 taun lan 25% saka umur 7 taun sing bobote > 20 kg.
Dorzolamide lan timolol Solusi ophthalmic: Keamanan lan khasiat ditetepake (minangka obat-obatan sing diwenehake sacara individu) ing pasien pediatrik ≥2 taun adhedhasar bukti saka studi sing cukup lan dikontrol kanthi apik ing bocah lan wong diwasa. Keamanan lan khasiat ora ditetepake ing pasien pediatrik <2 taun.
Panggunaan GeriatrikOra ana bedane sakabèhé ing safety lan khasiat relatif marang pasien sing luwih enom.
Efek Umum sing Sabar
Kobong lan nyenyet nalika instilasi.
Apa obatan liyane bakal mengaruhi Timolol (EENT)
Katon dimetabolisme sebagian dening CYP2D6.
Obat-obatan sing Ngaruhi Enzim Mikrosomal Hepatik
Inhibitor CYP2D6: Bisa nambah konsentrasi timolol plasma lan nambah blokade β-adrenergik sistemik (contone, nyuda denyut jantung, depresi).
Obat Spesifik
Obat
Interaksi
Komentar
Agen pamblokiran β-adrenergik, sistemik utawa topikal
Efek sistemik lan okular aditif sing bisa ditrapake
Panjaluk bebarengan agen pamblokiran β-adrenergik ophthalmic topikal ora dianjurake
Agen pamblokiran saluran kalsium
Potensi hipotensi, gangguan konduksi AV, lan gagal ventrikel kiwa
Ati-ati disaranake
Aja nggunakake bebarengan ing pasien kanthi fungsi jantung cacat
Glikosida jantung
Kamungkinan efek aditif ing prolonging wektu konduksi AV nalika pamblokiran β-adrenergik agen, glikosida jantung, lan agen pamblokiran saluran kalsium (diltiazem, verapamil) digunakake bebarengan
Obat sing nyuda katekolamin (umpamane, reserpine)
Efek aditif sing bisa ditindakake
Amati kanthi teliti kanggo bukti bradikardia utawa hipotensi sing nyata (bisa uga diwujudake minangka vertigo, sinkop, utawa hipotensi postural)
Cimetidine
Mungkin ngurangi aditif ing detak jantung istirahat lan TIO
Klonidin
Agen pamblokiran β-adrenergik oral bisa nambah hipertensi rebound sawise mungkasi clonidine
Ora dilapurake kanthi nggunakake ophthalmic timolol
Epinefrin
Midriasis bisa kedadeyan sawise bebarengan administrasi okular
Individu atopik lan sing duwe riwayat reaksi anafilaksis abot bisa uga ora nanggapi dosis epinefrin sing biasa digunakake kanggo perawatan reaksi anafilaksis
Quinidine
Potensi paningkatan konsentrasi timolol plasma lan ing β-blockade (bradikardia)
SSRI
Potensi peningkatan konsentrasi timolol plasma lan ing β-blockade
Disclaimer
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