Brimonidine (EENT)
Kelas obat: Agen Antineoplastik
Panganggone Brimonidine (EENT)
Hipertensi Okular lan Glaukoma
Brimonidine tartrate 0.1, 0.15, lan 0.2%: Pengurangan IOP munggah ing pasien karo glaukoma sudut terbuka utawa hipertensi okular. Efek hipotensi okular saka solusi 0,1 utawa 0,15% padha karo solusi 0,2%; nyuda IOP kira-kira 2-6 mm Hg ing studi klinis.
Brinzolamida kombinasi tetep 1% lan tartrat brimonidine 0,2%: Pengurangan TIO munggah ing pasien karo glaukoma sudut terbuka utawa hipertensi okular. Nalika diterbitake kaping telu saben dina, efek nyuda IOP 1-3 mm Hg luwih gedhe tinimbang obat sing diwenehake kanthi dosis sing padha karo monoterapi.
Brimonidine tartrate kombinasi tetep 0,2% lan timolol 0,5%: Digunakake topikal ing pasien glaukoma utawa hipertensi okular sing mbutuhake terapi tambahan utawa pengganti amarga IOP sing ora dikontrol. 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.
Kemacetan Konjungtiva
Brimonidine tartrate 0,025%: Pengobatan mandhiri kanggo ngilangi abang mata sementara amarga iritasi cilik.
Ora ana bukti tachyphylaxis ing studi klinis, lan okular rebound minimal. kemacetan diamati sawise mandheg obat.
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Carane nggunakake Brimonidine (EENT)
Umum
Administrasi
Administrasi Ophthalmic
Gunakake topikal menyang mripat sing kena pengaruh minangka solusi ophthalmic (brimonidine piyambak utawa ing kombinasi tetep karo timolol) utawa suspensi (kombinasi tetep Brinzolamide lan brimonidine).
Goyang suspensi ophthalmic sadurunge administrasi saben dosis.
Aja kontaminasi wadhah dispensing. (Deleng Keratitis Bakteri ing Ati-ati.)
Sawetara preparat ngandhut benzalkonium klorida. Copot lensa kontak sadurunge ngatur saben dosis persiapan kasebut; bisa masang maneh lensa 15 menit sawise dosis. Produsen brimonidine tartrate 0,025% solusi ophthalmic nyatakake lensa kontak bisa dipasang maneh 10 menit sawise dosis. (Deleng Gunakake karo Lensa Kontak ing Ati-ati.)
Yen luwih saka siji preparat ophthalmic topikal digunakake, gunakake preparat kasebut kanthi interval paling sethithik 5 menit.
Dosis
Pasien Pediatrik
Hipertensi Okular lan Glaukoma OphthalmicBrimonidine tartrate 0.1, 0.15, utawa 0.2% solusi ophthalmic ing pasien pediatrik ≥2 taun: Produsen ora menehi rekomendasi dosis tartamtu. (Deleng Panganggone Pediatrik ing Ati-ati.)
Brimonidine tartrate 0,2% lan solusi ophthalmic timolol 0,5% ing pasien pediatrik ≥2 taun: Siji tetes ing mripat sing kena pengaruh kaping pindho saben dina (kira-kira saben 12 jam). ).
Ophthalmic Conjunctival CongestionBrimonidine tartrate 0,025% larutan ophthalmic ing pasien pediatrik ≥5 taun: Siji tetes ing mripat sing kena pengaruh saben 6-8 jam.
Dewasa
Hipertensi Okular lan Glaukoma OphthalmicBrimonidine tartrate 0,1, 0,15, utawa 0,2% solusi ophthalmic: Siji tetes ing mripat sing kena pengaruh 3 kali dina (kira-kira saben 8 jam).
Brinzolamide 1% lan brimonidine tartrate 0,2% suspensi ophthalmic: Siji tetes ing mripat sing kena pengaruh 3 kali dina.
Brimonidine tartrate 0,2% lan timolol 0,5% larutan ophthalmic: Siji tetes ing sing kena pengaruh. mripat (s) kaping pindho saben dina (kira-kira saben 12 jam).
Yen target IOP ora bisa digayuh, bisa miwiti agen hipotensi okular tambahan utawa alternatif. (Deleng Hipertensi Okular lan Glaukoma ing Panggunaan.)
Ophthalmic Conjunctival CongestionBrimonidine tartrate 0,025% larutan ophthalmic: Siji tetes ing mripat sing kena pengaruh saben 6-8 jam.
Prescribing Watesan
Pasien Pediatrik
Ophthalmic Conjunctival CongestionBrimonidine tartrate 0,025% larutan oftalmik: Maksimal 4 kali saben dina.
Dewasa
Ophthalmic Conjunctival CongestionBrimonidine tartrate 0,025% larutan ophthalmic: Maksimal 4 kali dina.
Pènget
Kontraindikasi
Pènget/PanandhapReaksi Sensitivitas
Reaksi Hipersensitivitas
Reaksi hipersensitivitas okular (contone, konjungtivitis alergi, hiperemia konjungtiva, pruritus okular). Yen ana reaksi sensitivitas, mandhegake brimonidine.
Kemungkinan sensitivitas silang parsial antarane brimonidine lan apraklonidine; nggunakake kanthi ati-ati ing pasien kanthi riwayat hipersensitivitas kanggo apraklonidine.
Panganggone Kombinasi Tetep
Yen digunakake ing kombinasi tetep karo timolol utawa brinzolamide, nimbang ati-ati, pancegahan, kontraindikasi, lan interaksi obat sing ana gandhengane karo saben agen ing kombinasi tetep.
Penyakit Kardiovaskular
Efek minimal ing BP ing studi klinis; Nanging, gunakake kanthi ati-ati ing pasien kanthi kondisi kardiovaskular sing abot.
Insufisiensi Vaskular
Bisa nyebabake sindrom sing ana gandhengane karo insufisiensi pembuluh darah; nggunakake kanthi ati-ati ing pasien kanthi depresi mental, hipotensi ortostatik, insufficiency serebral utawa koroner, fenomena Raynaud, utawa thromboangiitis obliterans.
IOP Monitoring
Efek ngedhunake IOP saka brimonidine bisa uga suda sajrone wektu; rutin ngawasi IOP.
Keratitis Bakteri
Keratitis bakteri dilapurake kanthi nggunakake wadhah pirang-pirang dosis preparat ophthalmic topikal. Wadah kasebut ora sengaja terkontaminasi dening pasien, sing umume ngalami penyakit kornea bebarengan utawa gangguan ing permukaan epitel okular.
Penanganan preparat ophthalmic sing ora bener bisa nyebabake kontaminasi preparat kasebut dening bakteri umum sing dikenal nyebabake infeksi okular. Kerusakan serius ing mripat lan mundhut sesanti sakteruse bisa disebabake nggunakake preparat ophthalmic sing kontaminasi. (Deleng Nasehat kanggo Pasien.)
Gunakake karo Lensa Kontak
Sawetara preparat ophthalmic brimonidine ngandhut benzalkonium klorida, sing bisa diserap dening lensa kontak alus. Copot lensa kontak sadurunge ngatur saben dosis persiapan kasebut; bisa masang maneh lensa 15 menit sawise dosis. Produsen brimonidine tartrate 0,025% larutan ophthalmic nyatakake lensa kontak bisa dipasang maneh 10 menit sawise dosis.
Populasi Tertentu
KandhutanKategori B.
Ing pasinaon ing kéwan, brimonidine nyabrang plasenta lan mlebu sirkulasi janin nganti winates; ora ana bukti teratogenisitas sing diamati.
Ora ana studi sing nyukupi lan dikontrol kanthi apik ing wanita ngandhut. Gunakake brimonidine mung yen keuntungan potensial mbecikake resiko kanggo jabang bayi.
LaktasiDistribusi menyang susu ing tikus; Ora dingerteni manawa disebarake menyang susu manungsa sawise aplikasi topikal menyang mripat. Mungkasi nyusoni utawa obat kasebut.
Panggunaan PediatrikEfek sing bisa nyebabake serius, kalebu apnea, bradikardia, koma, hipotensi, hipotermia, hipotonia, lesu, pucet, depresi pernapasan, lan ngantuk, sing dilapurake ing bayi; contraindicated ing bayi <2 taun.
Aman lan khasiat brimonidine topikal kanggo perawatan glaukoma sudut terbuka utawa hipertensi okular sing ora ditetepake ing pasien pediatrik <2 taun. Ing bocah-bocah umur 2-7 taun kanthi glaukoma, efek samping sing paling umum saka brimonidine (solusi 0,2% sing diwenehake 3 kali saben dina) yaiku ngantuk lan nyuda kewaspadaan mental; kira-kira 16% bocah mandheg terapi amarga ngantuk. 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.
Komponèn individu saka brinzolamide lan Brimonidine ophthalmic suspension wis diteliti ing bocah-bocah umur 4 minggu nganti 5 taun (brinzolamide) lan 2-7 taun (brimonidine).
Keamanan lan khasiat solusi ophthalmic brimonidine lan timolol sing ditetepake ing pasien pediatrik umur 2-16 taun adhedhasar bukti saka studi sing cukup lan dikontrol kanthi apik babagan kombinasi tetep ing wong diwasa lan data tambahan saka panaliten sing ngevaluasi obat-obatan 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 karo glaukoma. ditetepake ing bocah-bocah <5 taun. Safety lan khasiat ing pasien pediatrik ≥5 taun didhukung dening bukti saka uji klinis sing dikontrol ing wong diwasa lan data tambahan saka studi safety ing wong diwasa lan pasien pediatrik ≥5 taun.
Panggunaan GeriatrikOra ana substansial. beda ing safety lan khasiat relatif kanggo wong diwasa enom.
Gangguan HepatikOra diteliti ing pasien sing duwe gangguan hepatik; nggunakake kanthi ati-ati.
Gagal GinjalOra ditliti ing pasien kanthi gangguan ginjel.
Efek Samsaya Awon
Brimonidine tartrate 0.1–0.2% larutan ophthalmic: Oral dryness, ocular or conjunctival hyperemia, burning and stinging, allergic conjunctivitis, headache, kabur, sensasi benda asing, lemes/ngantuk , folikel konjungtiva, reaksi alergi okular, pruritus okular.
Brimonidine tartrate 0,2% larutan ophthalmic ing bocah-bocah umur 2-7 taun kanthi glaukoma: Ngantuk sing gegandhengan karo umur lan bobot lan kewaspadaan mental sing mudhun. (Deleng Panganggone Pediatrik ing Ati-ati.)
Brimonidine tartrate 0,025% larutan ophthalmic ing wong diwasa lan pasien pediatrik: Suda ketajaman visual, hiperemia konjungtiva utawa okular, mripat garing, nyeri situs instilasi, sirah.
Apa obatan liyane bakal mengaruhi Brimonidine (EENT)
Ora ana studi interaksi obat resmi sing ditindakake.
Obat Spesifik
Obat
Interaksi
Komentar
Agen pamblokiran β-adrenergik (topikal utawa sistemik)
Kamungkinan aditif IOP-mudhunake lan efek kardiovaskuler
Gunakake kanthi ati-ati
Efek IOP-mudhun sing tambah digunakake kanggo keuntungan terapeutik
Antidepresan, trisiklik (TCAs)
TCA sing mengaruhi metabolisme lan penyerapan amina sirkulasi bisa ngganggu efek nyuda IOP saka brimonidine
Gunakake kanthi ati-ati
Glikosida jantung
Kamungkinan efek aditif kardiovaskular
Gunakake kanthi ati-ati
Depresan CNS (contone, alkohol, barbiturat, anestesi umum, opiat, obat penenang)
Kamungkinan efek aditif CNS depresan
Agen hipotensi
Kamungkinan aditif nyuda IOP lan efek kardiovaskular
Gunakake kanthi ati-ati
MAO inhibitor
Potensi teoritis kanggo interferensi metabolisme brimonidine, bisa uga nyebabake efek samping sistemik (contone, hipotensi)
Gunakake kanthi ati-ati
Disclaimer
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