Varenicline (Systemic)
Jeneng merek: Chantix
Kelas obat:
Agen Antineoplastik , Agen Antineoplastik
Panganggone Varenicline (Systemic)
Penghentian Rokok
Tambahan ing penghentian ngrokok.
Pedoman USPHS kanggo perawatan panggunaan tembakau lan ketergantungan nyaranake varenicline minangka salah siji saka sawetara obat lini pertama sing bisa kanthi andal ningkatake tingkat pantang rokok ing jangka panjang. Kanggo informasi tambahan, deleng Pedoman Praktek Klinis USPHS paling anyar sing kasedhiya ing [Web]
Ing studi klinis, terapi vareniklin nambah tingkat pantangan sing terus-terusan dibandhingake karo plasebo utawa komparator aktif (contone, Bupropion). Uga nyuda kepinginan kanggo ngrokok.
Ing panaliten ing pasien kanthi penyakit kardiovaskular sing stabil lan didokumentasikake lan pasien sing duwe COPD entheng nganti moderat, khasiat varenicline padha karo sing ana ing populasi umum sing ngrokok tanpa kondisi kasebut.
Uga dievaluasi ing pasien kanthi gangguan depresi utama sing stabil ing studi postmarketing; keuntungan uga diamati ing populasi iki tanpa bukti tambah efek neuropsyChiatric. (Deleng Gejala Neuropsychiatric lan Suicidality ing Ati-ati.)
Efikasi lan safety varenicline sing diwenehake bebarengan karo terapi mandheg ngrokok liyane (contone, bupropion, terapi pengganti nikotin) durung ditetepake.
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Carane nggunakake Varenicline (Systemic)
Administrasi
Administrasi Lisan
Atur tablet kanthi lisan sawise mangan, kanthi segelas banyu kebak.
Dosis
Kasedhiya minangka varenicline tartrate; dosis ditulis ing syarat-syarat varenicline.
Dewasa
Penghentian Rokok Oral0,5 mg sapisan dina ing dina 1-3, banjur 0,5 mg kaping pindho saben dina ing dina 4-7, lan banjur 1 mg kaping pindho saben dina saka dina 8 nganti pungkasan 12 minggu perawatan. Miwiti 1 minggu sadurunge tanggal target mandheg ngrokok. Utawa, pasien bisa miwiti perawatan karo varenicline lan banjur mandheg ngrokok antarane dina 8 nganti 35 perawatan.
Titrasi dosis sajrone minggu wiwitan perawatan kanggo nyuda kedadeyan mual sing ana gandhengane karo obat. Dosis bisa dikurangi sauntara utawa permanen ing pasien sing ngalami efek sing ora bisa ditrima.
Ing pasien sing wis sukses mandheg ngrokok ing pungkasan 12 minggu perawatan awal, nimbang terapi tambahan 12 minggu kanggo nambah kemungkinan. pantangan jangka panjang.
Anjurake pasien sing duwe motivasi, nanging ora bisa mandheg ngrokok sajrone perawatan awal 12 minggu (kanggo alasan liyane saka ora bisa ditolerir amarga efek samping) utawa sing wis kambuh sawise terapi varenicline. nyoba maneh kanggo mandheg ngrokok yen faktor-faktor sing nyebabake kegagalan kasebut wis diidentifikasi lan ditanggulangi.
Pendekatan Mungkasi Bertahap OralIng pasien sing ora gelem utawa ora bisa mandheg kanthi cepet, coba pendekatan bertahap kanggo mandheg ngrokok.
Miwiti varenicline nalika ngurangi jumlah rokok sing diisep nganti 50% sajrone 4 minggu pisanan; nyuda kanthi tambahan 50% ing 4 minggu sabanjure, lan banjur terus nyuda nganti pantang lengkap wis rampung nganti 12 minggu. Terusake varenicline kanggo tambahan 12 minggu kanggo total durasi terapi 24 minggu.
Anjurake pasien supaya nyoba mandheg luwih cepet yen dheweke rumangsa siap.
Watesan Resep
Dewasa
Oral1 mg kaping pindho saben dina.
Populasi Khusus
Gangguan Hepatik
Panyesuaian dosis ora perlu.
Gangguan Ginjal
Gagal ginjel entheng nganti moderat: Ora perlu pangaturan dosis.
Gagal ginjel abot (Clcr <30 mL / menit): Kaping pisanan, 0,5 mg sapisan dina; titrasi dosis sing dibutuhake nganti maksimal 0,5 mg kaping pindho saben dina.
Pasien kanthi penyakit ginjel tahap pungkasan sing ngalami hemodialisis: Maksimal 0,5 mg sapisan dina.
Pasien Geriatrik
Panyesuaian dosis ora dibutuhake; pilih dosis kasebut kanthi teliti lan ngawasi fungsi ginjel. (Deleng Panggunaan Geriatrik ing Caution.)
Pènget
Kontraindikasi
Pènget / PancegahanGejala Neuropsikiatri lan Suicidality
Kedadeyan neuropsikiatri sing serius, kalebu owah-owahan ing swasana ati (contone, depresi, mania), psikosis, halusinasi, paranoia, khayalan, ide homicidal, permusuhan, agitasi, agresi, kuatir, panik , lan suicidality (contone, ide bunuh diri, nyoba lan bunuh diri rampung), dilapurake sajrone pengalaman postmarketing karo varenicline lan bupropion (obat mandheg ngrokok liyane); wis kedadeyan ing pasien kanthi utawa tanpa riwayat psikiatri.
Analisis lan studi tambahan, kalebu studi sing dikontrol kanthi acak ing luwih saka 8000 pasien, nuduhake yen risiko luwih murah tinimbang sing dikira sadurunge lan bisa dibandhingake karo terapi penggantian nikotin utawa plasebo. Nanging, ana bukti sing nuduhake yen pasien sing duwe penyakit kejiwaan sing wis ana sadurunge (umpamane, depresi, gangguan kuatir, skizofrenia) bisa uga ngalami kedadeyan kasebut.
Sanajan risiko tetep, utamane ing wong sing nandhang penyakit kejiwaan saiki utawa kepungkur, pasien umume ora ngalami akibat sing serius (contone, rawat inap); mula, keuntungan saka mandheg ngrokok (contone, nyuda risiko ngembangake penyakit paru-paru, penyakit kardiovaskular, lan kanker) terus luwih gedhe tinimbang risiko obat-obatan penghentian kasebut.
Ngawasi pasien kanggo gejala neuropsikiatri utawa kahanan psikiatri sing luwih elek. . Mungkasi varenicline ing pasien sing ngalami agitasi, permusuhan, swasana ati sing depresi, utawa owah-owahan prilaku utawa pikiran sing ora khas kanggo pasien utawa sing ngalami ide bunuh diri utawa prilaku bunuh diri. Mungkasi terapi, nyuda dosis, utawa nerusake perawatan kanthi ngawasi kanthi teliti adhedhasar keruwetan gejala lan respon pasien marang terapi mandheg ngrokok.
Nyedhiyakake pemantauan pasien lan perawatan sing ndhukung nganti gejala kasebut ilang.
Sawetara efek neuropsikiatri, kalebu prilaku sing ora biasa lan kadhangkala agresif sing ditujokake marang awake dhewe utawa wong liya, bisa uga tambah parah amarga nggunakake alkohol bebarengan. (Deleng Obat Spesifik ing Interaksi.)
Kejang
Kejang dilapurake, biasane kedadeyan ing sasi pisanan terapi. Diamati ing pasien sing duwe lan tanpa riwayat kejang.
Timbang risiko versus keuntungan ing pasien sing duwe riwayat kejang utawa faktor liyane sing bisa nyuda ambang kejang. Mungkasi obat kasebut kanthi cepet yen kejang kedadeyan sajrone terapi. (Deleng Nasehat kanggo Pasien.)
Panganggone Alkohol bebarengan
Turun toleransi kanggo alkohol sing dilapurake sajrone pengalaman postmarketing, kadhangkala diiringi prilaku agresif sing ora biasa. (Waca Obat-obatan Khusus ing Interaksi.) Ing sawetara kasus, prilaku agresif nyebabake cilaka kanggo wong utawa properti. Pasien asring ora duwe memori utawa gangguan memori babagan acara kasebut.
Pasien kudu ngurangi konsumsi alkohol nganti efek varenicline ing toleransi alkohol dikenal. (Deleng Nasehat kanggo Pasien.)
Cedera Sengaja
Kacilakan lalu lintas, kedadean cedhak-celaka ing lalu lintas, utawa ciloko ora sengaja liyane sing dilaporake. Ing sawetara kasus, somnolence, pusing, mundhut eling utawa kangelan musataken kacarita. (Deleng Nasehat kanggo Pasien.)
Efek Kardiovaskular
Ing pasien kanthi penyakit kardiovaskular sing stabil sing wis nampa varenicline, kedadeyan kardiovaskular tartamtu (yaiku, angina pectoris, MI nonfatal, stroke nonfatal, perlu kanggo revaskularisasi koroner, rawat inap kanggo angina pectoris, TIA, diagnosa anyar saka penyakit pembuluh darah perifer, diakoni rumah sakit kanggo prosedur penyakit pembuluh darah perifer) kacarita. A meta-analisis ngandhakake yen acara jantung sing ora becik (mati kardiovaskuler, MI nonfatal, stroke nonfatal) kedadeyan luwih kerep sajrone perawatan lan 30 dina sawise perawatan ing pasien sing nampa varenicline yen dibandhingake karo pasien sing nampa plasebo, dene mortalitas sakabèhé lan kardiovaskular luwih murah. varenicline. Asil ora signifikan sacara statistik nanging konsisten; daya diwatesi amarga tarif acara kurang.
Ora ditliti ing pasien sing nandhang penyakit kardiovaskular sing ora stabil utawa ing pasien sing ngalami acara kardiovaskular sajrone 2 wulan sadurunge screening.
Timbang risiko nglawan keuntungan panggunaan varenicline ing perokok kanthi penyakit kardiovaskular. . Rokok minangka faktor risiko inDependen lan utama kanggo penyakit kardiovaskular, lan mandheg penting banget ing populasi pasien iki.
Anjurake pasien supaya menehi kabar marang panyedhiya kesehatan yen ngalami gejala penyakit kardiovaskular sing anyar utawa saya tambah parah.
Somnambulism
Somnambulism, kadhangkala nyebabake cilaka kanggo awake dhewe, wong liya, utawa properti, dilaporake. (Deleng Nasehat kanggo Pasien.)
Reaksi Sensitivitas
Reaksi hipersensitivitas, kalebu angioedema, dilaporake. Manifestasi kalebu bengkak ing pasuryan, tutuk (ilat, lambe, lan gusi), ekstremitas, lan gulu (pharynx lan laring). Angioedema sing ngancam nyawa sing mbutuhake perhatian medis amarga kompromi ambegan jarang dilapurake.
Nyetop varenicline langsung yen gejala kasebut kedadeyan. (Deleng Nasehat kanggo Pasien.)
Efek Dermatologis
Reaksi dermatologis sing serius, kalebu sindrom Stevens-Johnson lan erythema multiforme, dilapurake; potensial ngancam nyawa. Anjurake pasien kanggo mungkasi varenicline lan langsung hubungi panyedhiya kesehatan nalika katon ruam kanthi lesi mukosa utawa tandha hipersensitivitas.
Mual
Mul iku paling umum dilapurake efek salabetipun; biasane entheng utawa moderat, gegayutan karo dosis, lan asring transient (sanajan bisa tahan nganti pirang-pirang wulan).
Titrasi awal dosis varenicline nyuda kedadeyan mual (pirsani Dosis ing Dosis lan Administrasi). Coba nyuda dosis ing pasien sing ngalami mual sing ora bisa ditoleransi.
Populasi Tertentu
KandhutanData manungsa sing kasedhiya ora cukup kanggo nemtokake risiko sing ana gandhengane karo obat. Ora ana malformasi utama sing diamati ing studi reproduksi kewan, nanging sawetara bukti keracunan ibu, keracunan perkembangan, lan bobot janin sing mudhun.
Ngrokok nalika meteng digandhengake karo risiko sing dikenal kanggo ibu, janin, lan bayi sing nembe lair; ora dingerteni manawa mandheg ngrokok kanthi varenicline bisa nyuda risiko kasebut.
LaktasiDistribusi menyang susu ing kewan; ora dikawruhi manawa disebarake menyang susu manungsa utawa yen obat duweni pengaruh marang bayi sing disusui utawa ing produksi susu. Coba manfaat sing dikawruhi saka nyusoni bebarengan karo kabutuhan klinis ibu kanggo varenicline lan efek samping potensial saka obat kasebut utawa kondisi ibu sing ndasari ing bayi.
Panggunaan PediatrikKeamanan lan khasiat ora ditetepake ing bocah-bocah <18 taun. umur. (Deleng Populasi Khusus miturut Farmakokinetik.)
Panggunaan GeriatrikOra ana bedane signifikan ing safety lan khasiat relatif marang wong diwasa sing luwih enom, nanging tambah sensitivitas ora bisa ditolak.
Pilih dosis kanthi ati-ati amarga umur. -related sudo ing fungsi ginjel. Muga-muga bisa migunani kanggo ngawasi fungsi ginjel ing pasien geriatrik.
Gagal GinjalPaparan obat kasebut tambah akeh ing pasien kanthi gangguan ginjel moderat nganti abot lan ing pasien penyakit ginjel tahap pungkasan sing ngalami hemodialisis.
Panyesuaian dosis dianjurake kanggo pasien sing nandhang gagal ginjel abot utawa penyakit ginjel tahap pungkasan sing ngalami hemodialisis. (Deleng Gagal Ginjal ing Dosis lan Administrasi.)
Efek Sabar sing Umum
Mual, impen ora normal (nyata, ora biasa, aneh), konstipasi, kembung, muntah.
Apa obatan liyane bakal mengaruhi Varenicline (Systemic)
Owah-owahan fisiologis amarga mandheg ngrokok (nganggo utawa tanpa varenicline) bisa ngowahi farmakokinetik utawa farmakodinamik sawetara obat (umpamane, insulin, theophylline, warfarin); pangaturan dosis bisa uga dibutuhake.
Varenicline ora nyandhet isoenzim CYP 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4/5 in vitro; ora ngindhuksi isoenzim CYP 1A2 utawa 3A4 in vitro.
Obat-obatan sing Ngaruhi utawa Dimetabolisme dening Enzim Mikrosomal Hepatik
Interaksi farmakokinetik sing ora mungkin karo obat sing dimetabolisme utawa mengaruhi isoenzim CYP.
Obat sing diilangi dening Sekresi Renal
Interaksi farmakokinetik sing penting sacara klinis sing mbutuhake pengurangan dosis varenicline ora mungkin.
Inhibitor Pengangkut Kation Organik
Interaksi farmakokinetik potensial (konsentrasi plasma mundhak. varenicline minangka asil saka nyuda reresik ginjel). Panggunaan bebarengan karo inhibitor OCT2 bisa uga ora mbutuhake pangaturan dosis varenicline; tambah akeh paparan sistemik kanggo varenicline ora samesthine sacara klinis penting.
Obat Spesifik
Obat
Interaksi
Komentar
Alkohol
Potensi tambah efek mabuk saka alkohol; prilaku sing ora biasa lan kadhangkala agresif sing dilapurake ing pasien sing ngombe alkohol nalika njupuk varenicline
Kurangi konsumsi alkohol nganti efek varenicline ing toleransi alkohol dikenal
Bupropion
Interaksi farmakokinetik ora mungkin
Keamanan panggunaan gabungan ora ditetepake
Cimetidine
Konsentrasi plasma varenicline sing luwih dhuwur bisa uga amarga nyuda reresik ginjal
Interaksi sing ora dikarepake sacara klinis penting; pangaturan dosis bisa uga ora dibutuhake
Digoxin
Interaksi farmakokinetik ora mungkin
Metformin
Interaksi farmakokinetik ora mungkin
Nikotin
Interaksi farmakokinetik ora mungkin; tambah insiden efek samping (mual, sirah, mutahke, pusing, dyspepsia, lemes) lan tambah tingkat penghentian terapi kombinasi (varenicline lan pengganti nikotin transdermal) dibandhingake karo sing nampa nikotin transdermal lan plasebo
Keamanan lan khasiat varenicline ing kombinasi karo terapi mandheg ngrokok liyane ora ditetepake
Warfarin
Interaksi farmakokinetik ora mungkin; Farmakokinetik warfarin bisa uga kena pengaruh saka mandheg ngrokok
Disclaimer
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