Tedizolid
Jeneng merek: Sivextro
Kelas obat:
Agen Antineoplastik
Panganggone Tedizolid
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), 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), utawa Enterococcus faecalis.
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- Tedizolid
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- Tenex
- Terbinafine (Systemic)
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- 5-hydroxytryptophan, melatonin, and pyridoxine
Carane nggunakake Tedizolid
Administrasi
Kanggo oral utawa infus IV.
Administrasi oral
Administrasi oral tanpa preduli saka dhaharan.
Administrasi IV
Kanggo informasi kompatibilitas solusi lan obat, deleng Kompatibilitas ing Stabilitas.
Administrasi mung kanthi infus IV; Aja menehi injeksi IV kanthi cepet utawa langsung. Ora dimaksudake kanggo administrasi IM, intra-arteri, intrathecal, intraperitoneal, utawa sub-Q.
Kudu dilebokake maneh lan diencerake maneh sadurunge infus IV.
Aja nambah utawa infus bebarengan karo zat, aditif, utawa obat-obatan IV liyane.
Yen jalur IV sing padha digunakake kanggo infus berurutan saka sawetara obat sing beda, siram jalur IV kanthi injeksi natrium klorida 0,9% sadurunge lan sawise infus.
Botol ora ana pengawet; mung kanggo panggunaan siji.
ReconstitutionReconstitute vial ngemot 200 mg tedizolid fosfat kanthi nambah 4 mL banyu steril kanggo injeksi. Alon-alon swirl vial; ninggalake ngadeg nganti bubuk lyophilized utawa jajan larut lan umpluk dispersed. Aja agitasi utawa goyang sing kuat kanggo nyilikake busa.
Priksa kanggo mesthekake yen ora ana partikel, bubuk, utawa kue sing nempel ing sisih pinggir botol. Yen perlu, walik lan alon-alon swirl vial kanggo mbubarake bubuk sing isih ana. Solusi sing dikonstitusi kudu katon bening lan ora ana warna nganti kuning pucet.
CairanMiringake vial reconstituted lan tarik 4 ml larutan reconstituted saka sudhut ngisor vial nggunakake syringe; supaya inverting vial nalika mbatalake solusi. Alon-alon nambahake 4 ml larutan rekonstitusi menyang kantong IV sing ngemot 250 ml injeksi natrium klorida 0,9%. Alon-alon walik tas kanggo nyampur; aja goyangake.
Larutan IV sing diencerke lan diencerake kudu katon bening lan ora ana warna nganti kuning pucet. Priksa visual kanggo partikel partikel sadurunge administrasi; Mbuwang yen partikel diamati.
Tingkat AdministrasiAdministrasi kanthi infus IV liwat 1 jam.
Dosis
Kasedhiya minangka tedizolid fosfat (prodrug ora aktif saka tedizolid); dosis ditulis ing syarat-syarat tedizolid fosfat.
Dewasa
Infeksi Kulit lan Struktur Kulit Oral utawa IV200 mg sapisan saben dina kanggo 6 dina.
Populasi Khusus h3>
Panyesuaian dosis ora dibutuhake adhedhasar jender, ras, bobot awak, utawa indeks massa awak (BMI).
Gangguan Hepatik
Panyesuaian dosis ora dibutuhake ing pasien kanthi gangguan hepatik.
Gangguan Ginjal
Panyesuaian dosis ora dibutuhake kanggo pasien sing ngalami gangguan ginjel utawa ngalami hemodialisis.
Pasien Geriatrik
Panyesuaian dosis ora dibutuhake adhedhasar umur.
Pènget
Kontraindikasi
Pènget/PanandhapPasien karo Neutropenia
Keslametan lan khasiat ing pasien karo neutropenia (yaiku, jumlah neutrofil <1000 sel / mm3) ora dievaluasi. Ing model infèksi kéwan, aktivitas antibakteri saka tedizolid dikurangi amarga ora ana granulosit.
Pirsani terapi alternatif nalika ngobati infeksi kulit lan struktur kulit bakteri akut ing pasien neutropenia.
Efek Hematologis
Ing studi tahap 1 ing wong diwasa sing sehat sing nampa tedizolid sajrone 21 dina, ana bukti kemungkinan efek dosis lan durasi ing parameter hematologi sawise dina 6. Ing studi tahap 3 ing pasien kanthi bakteri akut infèksi kulit lan struktur kulit, tingkat owah-owahan hematologi sing penting sacara klinis umumé padha karo sing diobati karo tedizolid (regimen 6 dina) utawa linezolid (regimen 10 dina).
Neuropati
Neuropati perifer lan optik sing dilapurake ing pasien sing nampa perawatan > 28 dina karo anti-infektif oxazolidinone liyane (ora tedizolid). Ing fase 3 studi tedizolid ing pasien kanthi infeksi kulit lan struktur kulit bakteri akut, neuropati perifer lan kelainan saraf optik sing dilapurake ing frekuensi sing padha ing sing diobati karo tedizolid utawa linezolid. Data ora kasedhiya kanggo pasien sing ngalami >6 dina tedizolid.
Superinfection/Clostridium difficile-associated Diare and Colitis (CDAD)
Kamungkinan muncule lan tuwuh akeh bakteri utawa jamur sing ora rentan. Ngawasi kanthi teliti; institute terapi sing cocok yen superinfeksi dumadi.
Pengobatan kanthi anti-infèksi ngubah flora usus normal lan bisa ngidinake overgrowth saka 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) dilapurake karo meh kabeh anti-infectives, kalebu tedizolid, lan bisa sawetara ing 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 yen bisa. Miwiti terapi dhukungan sing cocok (umpamane, manajemen cairan lan elektrolit, suplemen protein), terapi anti-infektif sing ditujokake marang C. difficile (umpamane, metronidazole, vancomycin), lan evaluasi bedah kaya sing dituduhake sacara klinis.
Pamilihan lan Panggunaan Anti-infèksi
Kanggo nyuda pangembangan bakteri sing tahan obat lan njaga efektifitas tedizolid lan antibakteri liyane, gunakake mung kanggo perawatan infeksi sing wis kabukten utawa diduga disebabake dening bakteri sing rentan. .
Nalika milih utawa ngowahi terapi anti-infèksi, 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.
Populasi Tertentu
KandhutanKategori C.
Gunakake nalika meteng mung yen keuntungan potensial mbenerake potensial risiko kanggo janin.
Ora ana studi sing nyukupi lan dikontrol kanthi apik ing wanita ngandhut; pasinaon kewan (tikus, tikus, terwelu) ngungkapake bobot janin sing suda, anomali tulang rawan kosta, variasi balung sing tambah, lan/utawa bobote ibu sing suda ing dosis paling sethithik 4 kaping kira-kira paparan manungsa.
LaktasiDistribusi menyang susu ing tikus; ora dingerteni manawa disebarake menyang susu manungsa.
Gunakake kanthi ati-ati ing wanita sing nyusoni.
Panggunaan PediatrikKeamanan lan khasiat ora ditetepake ing pasien pediatrik <18 taun.
Geriatrik GunakakeJumlah pasien sing umure ≥65 taun ora cukup ing studi klinis kanggo nemtokake manawa dheweke nanggapi beda karo wong diwasa sing luwih enom. Beda ing farmakokinetik ora diamati antarane pasien tuwa lan luwih enom; pangaturan dosis ora dibutuhake.
Gangguan HepatikGangguan ati moderat utawa abot (Child-Pugh kelas B utawa C): Ora ana owah-owahan farmakokinetik sing penting sacara klinis.
Gagal GinjalGangguan ginjel sing abot (Clcr < 30 mL/menit saben 1,73 m2): Ora ana owah-owahan farmakokinetik sing penting sacara klinis; ora ana penghapusan penting sacara klinis sajrone hemodialisis.
Efek Umum sing Sabar
Mul, sirah, diare, mutahke, pusing, kesel.
Apa obatan liyane bakal mengaruhi Tedizolid
Tedizolid fosfat lan tedizolid ora dadi substrat lan ora nyandhet utawa ngindhuksi isoenzim CYP (CYP1A2, 2B6, 2D6, 2C8, 2C9, 2C19, 3A4) ing vitro. Interaksi obat sing nglibatake metabolisme oksidatif lan isoenzim CYP ora mungkin.
Ora ana efek klinis sing penting ing penyerapan obat utawa transporter membran efluks obat (contone, transporter anion organik [OAT] 1, OAT3, polipeptida pengangkut anion organik [OATP] 1B1 , OATP1B3, transporter kation organik [OCT] 1, OCT2, P-glikoprotein [P-gp], protein tahan kanker payudara [BCRP]) in vitro.
Obat lan Panganan Spesifik
Obat
Interaksi
Komentar
Antibakteri (aztreonam, Ceftazidime, Ceftriaxone, ciprofloxacin, clindamycin, co-trimoxazole, daptomycin, Gentamicin, imipenem, minocycline, rifampisin , vankomisin)
Ora ana bukti in vitro saka efek sinergis utawa antagonis marang bakteri gram-positif utawa gram-negatif
Anti jamur (amphotericin B, ketokonazol, Terbinafine)
Ora ana bukti in vitro efek sinergis utawa antagonis marang bakteri gram-positif
Pakanan, sing ngandhut tyramine
Dosis sing disaranake (200 mg fosfat tedizolid saben dina) ora samesthine kanggo menehi respon pressor sing penting sacara klinis ing pasien sing nampa panganan sing sugih tyramine; palpitasi dilapurake ing 72% pasien sing nampa tedizolid karo tyramine dibandhingake karo 46% pasien sing nampa tyramine karo plasebo
Watesan panganan sing akeh tyramine ora dibutuhake
Inhibitor MAO
Tedizolid minangka inhibitor MAO sing bisa dibalikake kanthi in vitro; interaksi karo inhibitor MAO ora dievaluasi ing studi klinis
PseudoEphedrine
Ora ana paningkatan BP maksimal utawa denyut jantung nalika dosis dianjurake (200 mg tedizolid fosfat saben dina) digunakake karo pseudoephedrine (60 mg). ); ora ana pengaruh ing farmakokinetik obat kasebut
Obat serotonergik (SSRI, antidepresan trisiklik, serotonin tipe 1 [5-hydroxytryptamine; 5-HT1] agonis reseptor ["triptans"], Meperidine, Buspirone)
Ora ana bukti aktivitas serotonergik ing model tikus nggunakake dosis tedizolid nganti 30 kali luwih dhuwur tinimbang dosis manungsa sing padha; interaksi karo agen serotonergik ora dievaluasi ing studi klinis
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