Giotrif 30mg obat Boehringer kanggo perawatan kanker paru-paru (4 blister x 7 tablet)

Bentuk sediaan Kothak 4 blister x 7 tablet
Spesifikasi Afatinib

Komposisi

Informasi komposisi	Isi
Afatinib	30 mg

Migunakake

Indikasi

Obat Giotrif sing digunakake ing terapi tunggal dituduhake kanggo perawatan kanker paru-paru sel non-small ing titik utawa metastase kanthi mutasi reseptor kanggo faktor pertumbuhan epidermis (EGFR) kanggo pasien diwasa sing durung diobati kanthi EGFR Tyrosine Kinase.

Pharmacokinatus

Klompok perawatan farmakologis: obat anti-kanker liyane - nyandhet protein kinase, kode ATC: L01xe13.

Mekanisme tumindak

Afatinib minangka inhibitor ErBB sing nduweni efek sing kuat, selektif lan ora bisa pulih. Afatinib ngiket sinyal non-recovery kovalen lan nyegah saka Homo - lan Heterodimer sing dibentuk dening anggota klompok ERBB: EGFR (ERBB1), Her2 (ERBB2), ERBB3 lan ERB4.

Efek farmakologis

Sinyal erbb bisa dipicu dening mutasi lan/utawa amplifier EGFR, amplifier utawa mutasi Her2 lan/utawa nambah ekspresi Ligand ERBB nyumbang kanggo nggawe karakteristik abnormal ing subkelompok pasien kanthi macem-macem jinis kanker.

Ing model patologis praklinis sing ilang kontrol rute ERBB, Afatinib nggunakake zat tunggal sing efektif nyegah transmisi sinyal reseptor ERBB sing nyegah pertumbuhan tumor utawa derajat tumor. Model NSCLC kanthi mutasi L858R utawa Del 19 EGFR utamané sensitif nalika diobati karo Afatinib. Afatinib njaga resistensi tumor sing signifikan ing garis sel in vitro NSCLC lan model tumor in vivo (transplantasi karo model sing ditransfer sacara genetis) sing ditemtokake dening persamaan mirip EGFR mutan kayata T790M sing ditemtokake tahan kanggo inhibitor EGFR karo Ellotinib lan Gefitinib.

farmakokinetik

penyerapan lan distribusi

Sawise njupuk Giotrif, konsentrasi maksimum (cmax) Afatinib diamati udakara 2 nganti 5 jam sawise njupuk obat kasebut. Rata-rata nilai CMAX lan AUC0-Avple rata-rata mundhak tinimbang rasio dosis afatinib saka 20 mg nganti 50 mg. Konsentrasi sistemik Afatinib mudhun 50% (CMAX) lan 39% (AUC0-fit), nalika dijupuk karo panganan sing sugih lemak dibandhingake nalika ngombe luwe. Adhedhasar data dinamis dinamis sing dipikolehi saka uji klinis kanthi macem-macem jinis tumor, weruh AUCτ, S nyuda rata-rata 26% nalika mangan sajrone 3 jam sadurunge utawa 1 jam sawise nggunakake Afatinib. Mulane, aja mangan paling sethithik 3 jam kepungkur lan sajrone 1 jam sawise njupuk Afatinib. Sawise nggunakake Afatinib, bioavailabilitas rata-rata rata-rata yaiku 92% (rasio rata-rata koreksi AUC0 -∞) yen dibandhingake karo solusi lisan.

In vitro afatinib disambungake karo protein ing plasma manungsa kira-kira 95%.

Metabolisme lan eliminasi

Reaksi metabolisme dening enzim katalitik nduweni peran sing bisa diabaikan kanggo Afatinib In Vivo. Produk sing nyambungake kovalen karo protein minangka metabolit utama Afatinib.

Sawise njupuk 15 mg Afatinib ing bentuk solusi, 85,4% dosis ditemokake ing feces lan 4,3% ing urin. Senyawa Afatinib wiwitan nyumbang 88% saka dosis sing dideteksi. Wektu sade eliminasi pungkasan yaiku 37 jam. Konsentrasi plasma ing negara stabil Afatinib digayuh sajrone 8 dina sawise njupuk pirang-pirang dosis Afatinib nyebabake akumulasi AUC 2,77 kaping lan CMAX 2,11 kaping.

Sadurunge njupuk Giotrif 30mg obat Boehringer kanggo perawatan kanker paru-paru (4 blister x 7 tablet)

How to use Giotrif drugs for oral use. If you cannot take the whole pill, you can mix Giotrif in about 100 ml of carbonate -free drinks. Do not use other solutions. Put the tablet into the water and not be crushed, occasionally stir for 15 minutes until the pill is disintegrated into very small particles and drink immediately. Should rinse with 100 ml of water and drink it afterwards. This solution can be used through the gastric catheter. Dosage Small cell lung cancer (NSCLC) Giotrif dose recommends that 40 mg oral once a day for step one or for patients who have not been treated earlier with EGFR Tyrosine Kinase inhibitors (patients have never used EGFR TKI). Should be treated with Giotrif continuously until the disease progresses or the patient is no longer tolerated. Dose increase It is possible to consider increasing the maximum dose of 50 mg daily in patients who have never used EGFR TKI and tolerated 40 mg daily (i.e. without diarrhea, rash, stomatitis and other drug -related events with a level of> 1 according to CTCAE) for the first 3 weeks. Do not increase the dose in patients who have reduced the previous dose. In any case, the maximum daily dose is 50 mg. Adjust the dose due to adverse reactions The adverse reaction that causes symptoms related to the drug (such as severe/prolonged diarrhea or adverse reactions on the skin) can be well treated by suspension of treatment and reduced giootrif dose. Information about the dose due to adverse reactions Adultery events due to ctcaea drugs Load) or level> 3 stopped the drug until the level of 0/1b continues to treat but reduced the dose of 10 mg B: In the case of diarrhea, should take anti -diarrhea drugs (such as looperamid) and if there is still diarrhea, continue to drink until the stool is over. c: diarrhea> 48 hours and/or rash> 7 days. D: If the patient is not tolerated by a dose of 20 mg per day, permanent giotrif should be considered. Think of interstitial lung disease (ILD) if a patient has acute or deteriorated respiratory symptoms, this case should temporarily suspend Giotrif while waiting for the assessment. If it is diagnosed with iLD, it is advisable to stop giotrif and conduct appropriate treatment. Patients with renal failure The observed giotrif concentration is increased in patients with medium or severe renal impairment. It is not necessary to adjust the starting dose in patients with mild renal impairment (EGFR 60 - 89 ml/min/1.73m2), average (EGFR 30 - 59 ml/min/1.73m2) or heavy (EGFR 15 - 29 ml/min/1.73m2). Monitor patients with severe renal impairment (EGFR 15 - 29 ml/min/1.73m2) and adjust the giotrif dose if not tolerated. Do not recommend giotrif treatment in patients with EGFR

Efek sisih

Unwanted effects (ADR) generally related to EGFR inhibitors in Afanitib activity. All unwanted effects are summarized below. The most unwanted effect is diarrhea and adultery events on the skin and stomatitis, inflammation around the nail. In general, reducing the dose leads to reduced frequency of common side effects. In patients treated with Giotrif 40 mg once a day, reducing the dose due to unwanted effects occurs in 57% of patients in Lux-Lung 3 clinical trial. Stop drugs due to unwanted effects of diarrhea and acne rashes are 1.3% and 0% in Lux-Lung 3 test. Reactions like interstitial lung disease are reported in 0.7% of patients treated with Afatinib. There has been a report on the case of water glossy, blistering, scales, including rare cases suggesting Stevens-Johnson syndrome and poisoned epidermal necrosis although these cases may be due to other causes. Summary of the frequency of unwanted effects from NSCLC tests and from experience used after Giotrif drugs circulate at a dose of 40 mg or 50 mg of monochromatic therapy. The following terms are used to classify unwanted effects by frequency: Very common (≥ 1/10); popular (≥ 1/100 to

Pènget

Sadurunge nggunakake obat kasebut, sampeyan kudu maca instruksi kasebut kanthi teliti lan deleng informasi ing ngisor iki.

contraindicated

Obat Giotrif contraindicated ing kasus ing ngisor iki:

Giotrif sing dikontraindikasi kanggo pasien hipersensitifitas marang Afatinib utawa bahan bantu apa wae.

Ati-ati nalika nggunakake

evaluasi kahanan mutasi EGFR

Nalika netepake kondisi mutasi EGFR ing pasien, penting kanggo milih cara sing akurat lan wis dievaluasi kanthi ati-ati kanggo ngindhari asil negatif palsu utawa palsu.

diare

diare, kalebu diare parah, wis dilaporake nalika perawatan karo Giotrif. Diare bisa nyebabake dehidrasi utawa ora ana gagal ginjal, ing kasus langka sing bisa nyebabake pati. Diare biasane katon ing 2 minggu pisanan perawatan. Diare level 3 biasane katon ing 6 minggu pisanan perawatan. Penting kanggo proaktif ngobati diare kalebu banyu sing cukup kanggo digabungake karo obat anti-diare sajrone perawatan 6 minggu pisanan lan diwiwiti sanalika ana tandha-tandha diare pisanan. Anti-diare kudu digunakake (kayata Loperamid) lan yen perlu, dosis sing paling dhuwur kudu disetujoni. Anti-diare kudu kasedhiya supaya pasien bisa diobati nalika nandhang diare sing pisanan lan kudu diobati terus-terusan nganti 12 jam metu saka bangkekan. Pasien sing nandhang diare abot bisa uga kudu nundha obat kasebut lan nyuda dosis utawa mungkasi perawatan kanthi permanen karo Giotrif. Pasien dehidrasi mbutuhake infus intravena lan elektrolit.

Kulit jina

Ana laporan babagan kukul / kukul ing pasien sing diobati karo giotrif. Umumé, papan kasebut katon ing wangun eritema cahya utawa medium lan ruam kaya kukul sing bisa katon utawa saya tambah parah ing wilayah sing kena sinar srengenge. Pasien sing kena sinar srengenge kudu disaranake nggunakake sandhangan sing ditutupi, lan / utawa tabir surya. Intervensi awal saka reaksi kulit (kayata krim pelunak kulit, antibiotik) bisa nggampangake perawatan terus-terusan karo giotrif.

Pasien kanthi reaksi kulit sing dawa utawa serius bisa uga kudu dihentikan sementara, dosis, perawatan tambahan, lan pemeriksaan dermatologist kanggo nambani efek kulit. Ana laporan babagan banyu nggilap, blistering, flaking, kalebu kasus langka sing nuduhake sindrom Stevens-Johnson lan nekrosis epidermal beracun. Giotrif kudu dilereni utawa mandheg kanthi permanen yen pasien nuduhake pratandha banyu, blistering utawa kulit sing abot.

Pasien wanita, bobot entheng lan gagal ginjal: Diamati konsentrasi wektu dhuwur Afatinib ing pasien wanita, bobot entheng lan pasien gagal ginjal. Iki bisa nambah risiko kedadeyan ala liwat perantara EGFR kayata diare, ruam / kukul lan stomatitis. Sampeyan kudu ngawasi pasien kanthi faktor risiko kasebut.

Penyakit paru-paru interstisial (ILD)

Ana laporan ILD utawa kedadeyan kaya ILD (kayata infeksi paru-paru, radhang paru-paru, sindrom insufisiensi ambegan akut, alveoli alergi), kalebu pati ing pasien sing nggunakake Giotrif kanggo nambani NSCLC. Acara kaya ILD sing ana gandhengane karo obat-obatan dilaporake ing 0,7% luwih saka 3800 pasien sing diobati. Acara kaya ILD yaiku ≥3 miturut CTCAE, tanpa preduli saka sabab lan akibat, dilaporake ing 1% pasien. Ora ana riset ing pasien kanthi riwayat ILD. Evaluasi kanthi ati-ati kabeh pasien kanthi gejala ing paru-paru (sesak ambegan, batuk, mriyang) nuduhake perkembangan akut lan / utawa ala amarga alasan sing ora dingerteni kanggo ngilangi iLD. Perawatan Giotrif kudu ditundha nalika ngenteni kanggo ngevaluasi gejala. Giotrif kudu mandheg kanthi permanen yen diagnosis ILD lan perawatan sing cocok yen perlu.

Gagal ati sing abot

Gagal hepatik, kalebu pati, wis dilaporake sajrone perawatan Giotrif kurang saka 1% pasien. Ing pasien kasebut, faktor jamming kalebu penyakit ati sing wis ana sadurunge lan / utawa penyakit sing teka kanthi perkembangan tumor ganas. Fungsi ati kudu dipriksa sacara periodik kanggo pasien sing nandhang penyakit ati luwih dhisik. Giotrif bisa digantung ing pasien kanthi fungsi ati. Giotrif kudu mandheg kanthi permanen yen pasien katon gagal ati sing serius nalika ngobati.

Cerematitis

Perlu langsung menyang spesialis mata yen ana gejala inflamasi akut utawa ala, berair, sensitivitas cahya, penglihatan kabur, nyeri mripat lan/utawa mripat abang. Yen didiagnosis ulkus kornea, dianjurake kanggo nundha utawa mungkasi perawatan kanthi permanen karo giotrif. Yen diagnosis keratitis kudu ati-ati ing antarane keuntungan lan risiko perawatan terus. Ati-ati nalika nggunakake Giotrif kanggo pasien sing duwe riwayat keratitis, ulkus kornea utawa mata garing sing abot. Nggunakake lensa kontak uga dadi faktor risiko kanggo keratitis lan ulcer.

Fungsi ventrikel kiwa

disfungsi ventrikel kiwa digandhengake karo inhibisi HER2. Adhedhasar data klinis sing ana, ora ana saran sing nuduhake yen Giotrif duweni efek ngrugekake ing kontraksi jantung. Nanging, ora ana panaliten babagan Giotrif ing pasien kanthi pembuluh getih LVEF abnormal (LVEF) utawa riwayat penyakit jantung sing abot. Ing pasien kanthi faktor risiko jantung lan pasien sing bisa mengaruhi LVEF, pemantauan kardiovaskular kudu dianggep, kalebu evaluasi LVEF ing wiwitan lan sajrone perawatan Giotrif. Yen pasien katon pratandha / gejala sing ana gandhengane karo jantung sajrone perawatan, pemantauan kardiovaskular kalebu review LVEF. Ing pasien hematoma sing luwih murah tinimbang wates ngisor tingkat normal kaya sing diwènèhaké, spesialis kardiovaskular kudu diteliti uga penundaan sementara utawa suspensi permanen giotrif.

Interaksi karo inhibitor P-Glycoprotein (P-GP)

Nggunakake inhibitor P-GP sing kuwat sadurunge nggunakake Giotrif bisa nyebabake paningkatan konsentrasi sajrone wektu afatinib lan kanthi ati-ati. Yen sampeyan kudu nggunakake inhibitor P-GP, sampeyan kudu nggunakake ing wektu sing padha utawa sawise giotrif. Pangobatan simultan karo obat induksi P-GP sing kuat bisa nyuda konsentrasi saka wektu Afatinib.

Digabungake karo Vinorelbin ing kanker payudara metastatik kanthi dheweke2 positif

Ing analisis mid-term saka kabeh kaslametané sak pisanan sinau phase III ing kanker payudara metastatik karo Her2 positif nuduhake Tambah ing tingkat kematian ing patients nggunakake Giotrif ing kombinasi karo Vinorelbin dibandhingake nggunakake Trastuzumab lan Vinorelbin. Nggabungake Giotrif karo Vinorelbin uga nambah tingkat efek saleh (kayata diare, ruam) lan kedadeyan fatal sing ana gandhengane karo infeksi bakteri lan kanker sing progresif. Giotrif ora kena digunakake ing kombinasi karo vinorelbin kanggo pasien kanker payudara metastatik kanthi Her2 positif.

laktosa

Giotrif ngandhut laktosa. Pasien sing nandhang penyakit genetik langka yaiku intoleransi galaktosa, kayata defisiensi Lapp Lactase utawa Glucose-Galactose, sing ora kudu dijupuk.

Efek obat kasebut ing nyopir lan ngoperasikake mesin

Ora ana panaliten babagan kemampuan nyopir lan ngoperasikake mesin.

Gunakake obat kanggo wanita nalika meteng lan laktasi

Wanita ngandhut:

Pasinaon klinis karo Afatinib nuduhake yen ora ana tandha teratogenisitas nalika nggunakake ibune. Owah-owahan sing ala mung katon ing dosis sing jelas beracun. Ora ana panaliten babagan wanita ngandhut sing nggunakake Giotrif. Mulane, risiko potensial ing wong ora dingerteni. Wanita sing duwe kemampuan kanggo nglairake kudu menehi saran supaya ora ngandhut nalika perawatan giotrif. Langkah-langkah kontrasepsi sing cocog kudu digunakake sajrone periode pengobatan lan paling ora 2 minggu sawise dosis pungkasan obat kasebut. Yen Giotrif digunakake nalika meteng utawa yen pasien ngandhut nalika giotrif, luwih becik menehi kabar marang pasien babagan bebaya potensial kanggo janin.

wanita sing nyusoni:

Adhedhasar data non-klinis, kemampuan Afatinib ora kalebu ing susu ibu. Ora bisa ngilangi risiko nyusoni. Para ibu ora kena nyusoni nalika nggunakake giotrif.

Reproduksi:

Ora ana riset Giotrif babagan kesuburan manungsa. Data beracun non-klinis klinis wis ditampilake mengaruhi organ reproduksi nalika dosis dhuwur. Mulane, ora bisa ngilangi efek samping ing kesuburan ing manungsa nalika diobati karo giotrif.

Interaksi obat

Efek saka inhibitor P-GP lan inhibitor protein anti-narkoba ing kanker payudara (BCRP) ing Afatinib: Panliten in vitro nuduhake yen Afatinib minangka substrat P-GP lan BCRP. Nalika nggunakake inhibitor P-GP lan BCRP sing kuat yaiku Ritonavir (200 mg kaping pindho dina telung dina) sak jam sadurunge nggunakake dosis siji 20 mg Giotrif, konsentrasi Afatinib mundhak 48% (wilayah ing kurva (AUC0 -∞)) lan 39% (konsentrasi puncak cmax (CMAX)). Ing sisih liya, nalika nggunakake Ritonavir bebarengan utawa 6 jam sawise nggunakake 40 mg Giotrif, bioavailabilitas relatif saka Afatinib yaiku 119% (AUC0 -∞), 104% (cmax) lan 111% (AUC0-fit), 105% (cmax). Mulane, dianjurake kanggo nggunakake inhibitor P-GP sing kuwat (kalebu nanging ora mung winates ing ritonavir, cyclosporine A, ketoconazole, iTraconazole, erythromycin, verapamil, quinidine, tacrolimus, nelfinavir, saquavir, lan amiodarone) SO LE Dibandhingake karo giotrif (deleng dosis lan panggunaan).

Efek obat induksi P-GP ing Afatinib: perawatan sadurunge karo Rifampicin (600 mg sapisan dina kanggo 7 dina) minangka stimulan kuat P-GP sing nyuda tingkat Afatinib 34% (AUC0 -∞) lan 22% (CMAX) sawise dosis siji Giotrif 40 mg. Obat induksi P-GP sing kuwat (kalebu nanging ora mung winates ing rifampicin, carbamazepine, phenytoin, fenobarbital utawa jamu St. John (Hypericum Perforatum) sing bisa nyuda tingkat Afatinib.

Pengaruh Afatinib ing substrat P-GP: Adhedhasar in vitro, data Afatinib minangka inhibitor P-GP rata-rata, nanging adhedhasar data klinis, perawatan karo Giotrif dianggep ora ngganti konsentrasi plasma substrat P-GP.

Interaksi karo BCRP: Panliten in vitro nuduhake yen Afatinib minangka substrat lan inhibitor transportasi BCRP. Afatinib bisa nambah bioavailabilitas substrat BCRP lisan (kalebu nanging ora mung winates ing rosuvastatin lan sulfasalazine).

Efek panganan ing Afatinib: njupuk Giotrif kanthi panganan sing sugih lemak sing nyuda konsentrasi Afatinib kanthi signifikan sajrone wektu Afatinib, utamane CMAX mudhun 50% lan AUC0-∞ mudhun udakara 39%. Mulane, Giotrif kudu karo panganan.

Panyimpenan

Ninggalake papan sing adhem, aja nganti cahya, suhu ngisor 30⁰C.

Obat liyane

Disclaimer

Kabeh upaya wis ditindakake kanggo mesthekake yen informasi sing diwenehake dening Drugslib.com akurat, nganti -tanggal, lan lengkap, nanging ora njamin kanggo efek sing. Informasi obat sing ana ing kene bisa uga sensitif wektu. Informasi Drugslib.com wis diklumpukake kanggo digunakake dening praktisi kesehatan lan konsumen ing Amerika Serikat lan mulane Drugslib.com ora njamin sing nggunakake njaba Amerika Serikat cocok, kajaba khusus dituduhake digunakake. Informasi obat Drugslib.com ora nyetujoni obat, diagnosa pasien utawa menehi rekomendasi terapi. Informasi obat Drugslib.com minangka sumber informasi sing dirancang kanggo mbantu praktisi kesehatan sing dilisensi kanggo ngrawat pasien lan / utawa nglayani konsumen sing ndeleng layanan iki minangka tambahan, lan dudu pengganti, keahlian, katrampilan, kawruh lan pertimbangan babagan perawatan kesehatan. praktisi.

Ora ana bebaya kanggo kombinasi obat utawa obat sing diwenehake kanthi cara apa wae kudu ditafsirake kanggo nuduhake yen obat utawa kombinasi obat kasebut aman, efektif utawa cocok kanggo pasien tartamtu. Drugslib.com ora nanggung tanggung jawab kanggo aspek kesehatan apa wae sing ditindakake kanthi bantuan informasi sing diwenehake Drugslib.com. Informasi sing ana ing kene ora dimaksudake kanggo nyakup kabeh panggunaan, pituduh, pancegahan, bebaya, interaksi obat, reaksi alergi, utawa efek samping. Yen sampeyan duwe pitakon babagan obat sing sampeyan gunakake, takon dhokter, perawat utawa apoteker.