Delafloxacin
Jeneng merek: Baxdela
Kelas obat:
Agen Antineoplastik
Panganggone Delafloxacin
Infeksi Kulit lan Struktur Kulit
Pengobatan infeksi kulit lan struktur kulit akut bakteri (ABSSSI) sing disebabake dening Staphylococcus aureus sing rentan (kalebu S. aureus sing tahan methicillin [MRSA; uga dikenal minangka S. tahan oxacillin . aureus utawa ORSA] lan S. aureus sing rentan methicillin), S. haemolyticus, S. lugdunensis, Streptococcus pyogenes (grup A streptococci β-hemolytic, GAS), S. agalactiae (streptococci grup B, GBS), grup S. anginosus (kalebu S. anginosus, S. intermedius, lan S. constellatus), Enterococcus faecalis, EscheriChia coli, Enterobacter cloacae, Klebsiella pneumoniae, utawa Pseudomonas aeruginosa.
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Carane nggunakake Delafloxacin
Administrasi
Atur kanthi lisan utawa kanthi infus IV alon.
Administrasi Oral
Atur tablet kanthi lisan tanpa preduli saka dhaharan. (Deleng Panganan ing Farmakokinetik.)
Atur kanthi lisan paling ora 2 jam sadurunge utawa 6 jam sawise antasida sing ngemot magnesium utawa aluminium, kation logam (contone, wesi), sucralfate, multivitamin utawa suplemen panganan sing ngemot wesi utawa seng, utawa preparat didanosin buffered. (Deleng Obat Spesifik ing Interaksi.)
Infus IV
Kudu direkonstitusi lan diencerake maneh sadurunge infus IV. Tindakake teknik aseptik sing ketat nalika nyiapake solusi IV.
Aja infus bebarengan liwat selang sing padha karo obat liyane. Aja menehi solusi sing ngemot kation multivalen (contone, kalsium, magnesium).
Yen jalur IV umum digunakake kanggo administrasi obat liyane, siram karo injeksi natrium klorida 0,9% utawa injeksi Dextrose 5% sadurunge lan sawise saben. infus delafloxacin.
Botol bubuk lyophilized kanggo injeksi mung kanggo panggunaan siji.
Kanggo informasi kompatibilitas solusi lan obat, deleng Kompatibilitas ing Stabilitas.
ReconstitutionReconstitute vial ngemot 300 mg delafloxacin kanthi nambahake 10,5 ml injeksi natrium klorida 0,9% utawa injeksi dextrose 5% kanggo nyedhiyakake solusi sing ngemot 25 mg / mL. Solusi sing dikonstitusi kudu katon kuning bening nganti kuning.
CairanKanggo nyiapake dosis 300 mg delafloxacin ing kantong infus 250 ml sing ngemot 0,9% injeksi natrium klorida utawa injeksi dextrose 5%, copot 12 ml pelarut saka kantong infus, banjur injeksi 12 ml larutan delafloxacin sing direkonstitusi menyang tas. Konsentrasi solusi infus pungkasan yaiku 1,2 mg / mL.
Kanggo nyiapake 200 mg delafloxacin ing tas infus 250 ml sing ngemot 0,9% injeksi natrium klorida utawa 5% injeksi dextrose, copot 8 ml pengencer saka tas infus, banjur injeksi 8 ml larutan. solusi delafloxacin reconstituted menyang tas. Konsentrasi solusi infus pungkasan yaiku 0,8 mg / mL.
Tingkat AdministrasiAdministrasi kanthi infus IV liwat 1 jam.
Dosis
Kasedhiya minangka delafloxacin meglumine; dosis dituduhake ing istilah delafloxacin.
Dewasa
Infeksi Kulit lan Struktur Kulit Oral450 mg saben 12 jam suwene 5-14 dina.
IV300 mg saben 12 jam kanggo 5-14 dina.
Terapi IV bisa diowahi menyang terapi oral miturut kawicaksanan dokter. Total durasi terapi IV lan oral yaiku 5-14 dina.
Populasi Khusus
Gangguan Hepatik
Gangguan hepatik entheng, moderat, utawa abot (Child-Pugh kelas A, B, utawa C): Penyesuaian dosis ora dibutuhake.
Gangguan Ginjal
OralGangguan ginjel entheng, moderat, utawa abot (kira-kira GFR [eGFR] 15–89 mL /menit saben 1,73 m2): Ora dibutuhake pangaturan dosis.
Penyakit ginjel tahap pungkasan (eGFR <15 mL/menit saben 1,73 m2): Ora dianjurake.
IVGangguan ginjel entheng utawa moderat (eGFR 30–89 mL/menit saben 1,73 m2): Ora perlu pangaturan dosis.
Gagal ginjel abot (eGFR 15–29 mL/menit saben 1,73 m2) : 200 mg saben 12 jam.
Penyakit ginjel tahap pungkasan (eGFR <15 mL/menit saben 1,73 m2): Ora dianjurake.
Pasien Geriatrik
Ora ana pangaturan dosis kajaba sing ana gandhengane karo gangguan ginjel. (Deleng Gagal Ginjal ing Dosis lan Administrasi.)
Pènget
Kontraindikasi
Pènget / PancegahanPènget
Mateni lan Reaksi Saleh Serius sing Potensi ora bisa dibalèkaké
Fluoroquinolones sistemik digandhengake karo mateni lan reaksi salabetipun serius sing ora bisa dibalèkaké (contone, tendinitis lan pecah tendon, neuropati perifer, efek CNS) sing bisa kedadeyan bebarengan ing pasien sing padha. Bisa kedadeyan sajrone jam nganti minggu sawise fluoroquinolone sistemik diwiwiti; wis kedaden ing kabeh klompok umur lan ing pasien tanpa faktor risiko sing wis ana sadurunge kanggo reaksi salabetipun.
Langsung nyetop ing tandha pisanan utawa gejala reaksi salabetipun serius.
Aja ngindhari fluoroquinolones sistemik, kalebu delafloxacin, ing pasien sing ngalami reaksi ala sing serius sing ana gandhengane karo fluoroquinolones.
Tendinitis lan Pecah TendonFluoroquinolones sistemik digandhengake karo tambah risiko tendinitis lan pecah tendon ing kabeh kelompok umur.
Risiko ngembangake tendinitis sing gegandhengan karo fluoroquinolone lan pecah tendon mundhak ing wong tuwa (biasane sing umure luwih saka 60 taun), individu sing nampa kortikosteroid bebarengan, lan panampa transplantasi ginjel, jantung, utawa paru-paru. (Deleng Panggunaan Geriatrik ing Cautions.)
Faktor liyane sing bisa nambah risiko pecah tendon kanthi bebas kalebu aktivitas fisik sing abot, gagal ginjel, lan kelainan tendon sadurunge kayata rheumatoid arthritis. Tendinitis lan pecah tendon wis dilapurake ing pasien sing nampa fluoroquinolones sing ora duwe faktor risiko kanggo reaksi salabetipun.
Tendinitis sing gegandhengan karo fluoroquinolone lan pecah tendon sing paling kerep nyangkut tendon Achilles; uga dilapurake ing rotator cuff (pundhak), tangan, biceps, jempol, lan situs tendon liyane.
Tendinitis lan pecah tendon bisa kedadeyan sajrone sawetara jam utawa dina sawise terapi diwiwiti utawa nganti pirang-pirang wulan sawise rampung. terapi; bisa kedadeyan bilateral.
Enggal-enggal mungkasi delafloxacin yen ana rasa nyeri, bengkak, inflamasi, utawa pecah tendon. (Deleng Saran kanggo Pasien.)
Aja ngindhari fluoroquinolones sistemik, kalebu delafloxacin, ing pasien sing duwe riwayat kelainan tendon utawa ngalami tendinitis utawa pecah tendon.
Neuropati PeriferFluoroquinolones sistemik yaiku digandhengake karo risiko tambah neuropati perifer.
Polineuropati aksonal sensori utawa sensorimotor sing mengaruhi akson cilik lan/utawa gedhe sing nyebabake paresthesias, hypoesthesias, dysesthesias, lan kelemahan sing dilapurake karo fluoroquinolones, kalebu delafloxacin. Gejala bisa kedadeyan sanalika sawise wiwitan obat kasebut lan, ing sawetara pasien, bisa uga ora bisa dibatalake.
Enggal mungkasi delafloxacin yen gejala neuropati perifer (umpamane, nyeri, kobong, tingling, mati rasa, lan/utawa kekirangan) kedadeyan utawa yen ana owah-owahan liyane ing sensasi (umpamane, sentuhan entheng, nyeri, suhu, rasa posisi, sensasi geter, lan/utawa kekuatan motor).
Ngindhari fluoroquinolones sistemik, kalebu delafloxacin, ing pasien sing ngalami neuropati perifer.
Efek CNSFluoroquinolones sistemik digandhengake karo tambah risiko efek psikiatri sing saleh, kalebu psikosis beracun, halusinasi, paranoia, depresi, pikiran utawa tumindak suicidal, delirium, disorientasi, kebingungan, gangguan ing manungsa waé, kuatir, agitasi, nervousness, insomnia, ngipi elek, lan gangguan memori. Efek ala iki bisa kedadeyan sawise dosis pisanan.
Fluoroquinolones sistemik digandhengake karo tambah risiko kejang (kejang), tambah tekanan intrakranial (kalebu pseudotumor cerebri), pusing, lan tremor. Gunakake delafloxacin ing pasien sing duwe kelainan CNS sing dikenal utawa dicurigai (contone, arteriosclerosis serebral sing abot, epilepsi) utawa faktor risiko liyane sing predisposisi kanggo kejang utawa ambang kejang sing luwih murah mung yen keuntungan potensial ngluwihi risiko.
Yen psikiatri utawa CNS liyane efek kedadeyan, langsung mateni delafloxacin lan njupuk langkah-langkah sing cocog. (Deleng Saran kanggo Patients.)
Exacerbation saka Myasthenia GravisFluoroquinolones duwe aktivitas blocking neuromuscular lan bisa exacerbate kekirangan otot ing patients myasthenia gravis; pati utawa perlu kanggo dhukungan ventilasi dilaporake.
Aja nggunakake ing pasien kanthi riwayat myasthenia gravis sing dikenal. (Deleng Nasehat kanggo Pasien.)
Reaksi Sensitivitas
HipersensitivitasHipersensitivitas serius lan sok-sok fatal lan/utawa reaksi anafilaksis sing dilapurake ing pasien sing nampa fluoroquinolones. Reaksi kasebut bisa kedadeyan kanthi dosis pisanan utawa sakbanjure.
Sawetara reaksi hipersensitivitas sing dilapurake karo fluoroquinolones wis diiringi ambruk jantung, mundhut eling, tingling, edema (pharyngeal utawa facial), dyspnea, urtikaria, utawa pruritus.
Hipersensitivitas lan urticaria dilapurake ing pasien sing nampa delafloxacin.
Enggal-enggal mungkasi delafloxacin nalika muncul ruam utawa tandha hipersensitivitas liyane. (Deleng Saran kanggo Pasien.)
FotosensitifitasOra ana bukti potensial fototoksik.
Pènget lan Pancegahan Liyane
Risiko Aneurisma lan Diseksi AortaPecah utawa dissection aneurisma aorta sing dilapurake ing pasien sing nampa fluoroquinolones sistemik. Panaliten epidemiologis nuduhake risiko tambah aneurisma aorta lan dissection sajrone 2 wulan sawise nggunakake fluoroquinolones sistemik, utamane ing pasien tuwa. Panyebab risiko tambah iki ora dingerteni.
Kajaba ora ana pilihan perawatan liyane, aja nggunakake fluoroquinolones sistemik, kalebu delafloxacin, ing pasien sing duwe aneurisma aorta utawa duwe risiko tambah aneurisma aorta. Iki kalebu pasien lansia lan pasien sing nandhang penyakit pembuluh darah aterosklerotik perifer, hipertensi, utawa kondisi genetik tartamtu (contone, sindrom Marfan, sindrom Ehlers-Danlos).
Yen pasien nglaporake efek samping sing nuduhake aneurisma aorta utawa dissection, langsung mungkasi fluoroquinolone. (Deleng Saran kanggo Pasien.)
Hipoglikemia utawa HiperglikemiaFluoroquinolones sistemik digandhengake karo owah-owahan ing konsentrasi glukosa getih, kalebu hipoglikemia gejala lan hiperglikemia. Gangguan glukosa getih sajrone terapi fluoroquinolone biasane kedadeyan ing pasien diabetes mellitus sing nampa agen antidiabetik oral (umpamane, glyburide) utawa insulin.
Kasus hipoglikemia sing abot sing nyebabake koma utawa pati dilaporake karo sawetara fluoroquinolones sistemik. Sanajan umume kasus koma hipoglikemik sing dilapurake kalebu pasien sing duwe faktor risiko hipoglikemia (umpamane, umur tuwa, diabetes mellitus, insufisiensi ginjel, panggunaan obat antidiabetik bebarengan [utamane sulfonylureas]), sawetara pasien sing nampa fluoroquinolone sing ora diabetes lan ora nampa. agen antidiabetik oral utawa insulin.
Ngawasi konsentrasi glukosa getih kanthi ati-ati nalika fluoroquinolones sistemik, kalebu delafloxacin, digunakake ing pasien diabetes sing nampa agen antidiabetik.
Yen ana reaksi hipoglikemik, mandhegake fluoroquinolone lan langsung miwiti terapi sing cocog. (Deleng Saran kanggo Pasien.)
Diare lan Kolitis sing gegandhengan C. difficilePengobatan kanthi anti-infèksi ngowahi flora usus normal lan bisa ngidinaké tuwuhing Clostridioides difficile (sadurungé dikenal minangka Clostridium difficile). C. difficile infection (CDI) lan C. difficile-related diare and colitis (CDAD; uga dikenal minangka antibiotik-related diare lan colitis utawa pseudomembranous colitis) sing dilapurake karo meh kabeh anti-infèksi, kalebu delafloxacin, lan bisa sawetara saka keruwetan saka entheng. diare kanggo colitis fatal. C. difficile ngasilake racun A lan B sing nyumbang kanggo pangembangan CDAD; galur C. difficile sing ngasilake hipertoksin digandhengake karo tambah morbiditas lan mortalitas amarga bisa uga refrakter kanggo anti-infèksi lan kolektomi bisa uga dibutuhake.
Coba CDAD yen diare berkembang sajrone utawa sawise terapi lan ngatur kanthi bener. Entuk riwayat medis sing ati-ati amarga CDAD bisa kedadeyan nganti ≥2 sasi sawise terapi anti-infektif mandheg.
Yen CDAD dicurigai utawa dikOnfirmasi, mandhegake anti-infèksi sing ora ditujokake marang C. difficile sanalika bisa. Ngatur nggunakake terapi anti-infèksi sing cocog sing diarahake marang C. difficile (contone, vancomycin, Fidaxomicin, metronidazole), terapi sing ndhukung (contone, manajemen cairan lan elektrolit, suplemen protein), lan evaluasi bedah kaya sing dituduhake sacara klinis.
Pamilihan lan Panganggone Anti-infèksiKanggo nyuda pangembangan bakteri sing tahan obat lan njaga efektifitas delafloxacin lan antibakteri liyane, gunakake mung kanggo perawatan infeksi sing wis kabukten utawa dicurigai disebabake dening bakteri sing rentan.
p>Nalika milih utawa ngowahi terapi anti-infeksi, gunakake asil kultur lan tes kerentanan in vitro. Yen ora ana data kasebut, nimbang pola epidemiologi lan kerentanan lokal nalika milih anti-infèksi kanggo terapi empiris.
Informasi babagan metode tes lan standar kontrol kualitas kanggo tes kerentanan in vitro saka agen antibakteri lan kriteria interpretasi khusus kanggo tes kasebut sing diakoni dening FDA kasedhiya ing [Web].
Populasi Spesifik
KandhutanData sing kasedhiya babagan panggunaan ing wanita ngandhut ora cukup kanggo menehi informasi babagan risiko keguguran sing ana gandhengane karo obat utawa cacat lair utama.
Yen diwènèhaké sacara lisan marang tikus sing ngandhut, ora malformasi utawa pati janin sing diamati ing konsentrasi delafloxacin 7 kaping kira-kira paparan klinis. Toksisitas ibu lan bobot awak janin sing suda diamati ing dosis paling dhuwur (1,6 g / kg saben dina); telat ossification janin diamati ing kabeh dosis. Sawise administrasi intravena kanggo tikus ing pungkasan meteng liwat laktasi, ora ana efek ngaruh marang turunane sing diamati ing konsentrasi klinis sing relevan.
LaktasiDistribusi menyang susu ing tikus lactating; ora dikawruhi yen disebarake menyang susu manungsa, mengaruhi bayi sing disusui, utawa mengaruhi produksi susu.
Pertimbangake keuntungan pangembangan lan kesehatan saka nyusoni bebarengan karo kabutuhan klinis ibu kanggo delafloxacin; uga nimbang potensial efek salabetipun ing bayi-disusun bayi saka tamba utawa ndasari kondisi ibu.
Pediatric PanganggoneSafety lan khasiat ora ditetepake ing bocah utawa cah cilik <18 taun; digunakake ing pasien pediatrik ora dianjurake.
Kuinolon nyebabake arthropathy ing kewan remaja.
Produsen nyatakake uji klinis sing ngevaluasi delafloxacin kanggo perawatan infeksi kulit lan struktur kulit bakteri ora kalebu pasien <18 taun. umur amarga risiko versus keuntungan ora ndhukung nggunakake tamba kanggo infèksi kuwi ing kelompok umur iki.
AAP nyatakake nggunakake fluoroquinolone sistemik bisa sabdho ing bocah-bocah <18 taun ing kahanan tartamtu nalika ora ana alternatif sing aman lan efektif lan obat kasebut dikenal efektif.
Panggunaan GeriatrikKira-kira 15% pasien sing nampa delafloxacin ing studi klinis umure ≥65 taun. Tingkat respon klinis ing jam 48-72 kira-kira 76% ing pasien ≥65 taun dibandhingake karo 82% ing umur <65 taun.
Risiko kelainan tendon sing abot, kalebu pecah tendon, yaiku tambah ing wong diwasa lawas (biasane sing umure luwih saka 60 taun). Risiko iki luwih tambah ing wong sing nampa kortikosteroid bebarengan. (Deleng Tendinitis lan Tendon Rupture ing Cautions.) Gunakake ati-ati ing wong diwasa geriatrik, utamane sing nampa kortikosteroid bebarengan.
Risiko aneurisma aorta lan diseksi bisa tambah ing pasien geriatrik. (Deleng Resiko Aneurisma Aorta lan Diseksi ing Ati-ati.)
Gangguan HepatikOra ana prabédan klinis penting ing farmakokinetik ing wong diwasa kanthi gangguan hepatik entheng, moderat, utawa abot (kelas Anak-Pugh A, B, utawa C) ; pangaturan dosis ora dibutuhake ing pasien kasebut.
Gagal GinjalGangguan ginjel sing abot (eGFR 15–29 mL/menit saben 1,73 m2): Akumulasi kendaraan delafloxacin IV, sulfobutylether-β-cyclodextrin (SBECD), dumadi. Ngurangi dosis (pirsani Gagal Ginjal ing Dosis lan Administrasi) lan ngawasi Scr lan eGFR kanthi rapet ing pasien sing nampa delafloxacin IV. Coba ngalih menyang delafloxacin oral yen Scr mundhak sajrone perawatan delafloxacin IV. Yen eGFR mudhun dadi <15 mL/menit saben 1,73 m2, mandhegake delafloxacin.
Penyakit ginjel tahap pungkasan (eGFR <15 mL/menit saben 1,73 m2): Akumulasi kendaraan delafloxacin IV (SBECD) kedadeyan. Panganggone delafloxacin (oral utawa IV) ora dianjurake.
Efek Umum sing Sabar
Efek GI (mual, diare, muntah), sirah, konsentrasi aminotransferase sing dhuwur.
Apa obatan liyane bakal mengaruhi Delafloxacin
Ora nyandhet CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, utawa 3A4/5 in vitro ing konsentrasi klinis sing relevan; ora nuduhake potensial kanggo induksi CYP1A2, 2B6, 2C19, utawa 2C8. Induksi entheng CYP2C9 lan 3A4 in vitro.
Obat-obatan sing Ngaruhi utawa Dipengaruhi dening Pengangkut Membran
Substrat transportasi P-glikoprotein (P-gp) lan protein tahan kanker payudara (BCRP) in vitro; penting klinis saka panggunaan bebarengan karo inhibitor P-gp lan/utawa inhibitor BCRP ora dingerteni.
Ora nyandhet multidrug-resistance gene (MDR) 1, BCRP, transporter anion organik (OAT) 1, OAT3, organik polipeptida pengangkut anion (OATP) 1B1, OATP1B3, pompa ekspor uyah empedu (BSEP), utawa transporter kation organik (OCT) 1 utawa OCT2 kanthi konsentrasi sing cocog sacara klinis.
Ora substrat OAT1, OAT3, OCT1, OCT2, OATP1B1, utawa OATP1B3.
Obat Spesifik
Obat
Interaksi
Komentar
Antacid (ngandhut aluminium utawa magnesium)
Kamungkinan nyuda penyerapan oral lan nyuda konsentrasi sistemik saka delafloxacin; efek ing IV delafloxacin ora dingerteni
Administrasi oral delafloxacin paling ora 2 jam sadurunge utawa 6 jam sawise antacid sing ngemot aluminium utawa magnesium
Antibakteri
Aztreonam, Ceftazidime, colistin (kasedhiya komersil ing AS minangka natrium colitimethate), co-trimoxazole, daptomycin, linezolid, Meropenem, tigecycline, utawa vankomisin: Ora ana bukti in vitro antibakteri sinergis utawa antagonis efek
Didanosine
Kamungkinan nyuda penyerapan oral lan nyuda konsentrasi sistemik delafloxacin yen digunakake bebarengan karo buffered didanosine (bubuk pediatrik kanggo solusi lisan); efek ing IV delafloxacin ora dingerteni
Administrasi oral delafloxacin paling sethithik 2 jam sadurunge utawa 6 jam sawise buffered didanosine
Olahan wesi
Kamungkinan nyuda penyerapan oral lan nyuda konsentrasi sistemik. saka delafloxacin; efek ing IV delafloxacin ora dingerteni
Administrasi oral delafloxacin paling sethithik 2 jam sadurunge utawa 6 jam sawise persiapan wesi
Midazolam
Ora ana efek substansial ing konsentrasi plasma puncak utawa AUC midazolam utawa metabolité (1-hydroxymidazolam)
Multivitamin lan suplemen diet
Kamungkinan nyuda penyerapan oral lan nyuda konsentrasi sistemik delafloxacin; efek ing IV delafloxacin ora dingerteni
Administrasi oral delafloxacin paling sethithik 2 jam sadurunge utawa 6 jam sawise multivitamin utawa suplemen diet sing ngemot wesi utawa seng
Sucralfate
Mungkin ngurangi oral panyerepan lan nyuda konsentrasi sistemik delafloxacin; efek ing IV delafloxacin ora dingerteni
Administrasi oral delafloxacin paling ora 2 jam sadurunge utawa 6 jam sawise sucralfate
Disclaimer
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