Naloxone (Systemic)
Kelas obat: Agen Antineoplastik
Panganggone Naloxone (Systemic)
Depresi sing disebabake opioid lan Overdosis Opioid Akut
Pengobatan depresi sing disebabake opioid, kalebu depresi pernapasan, sing disebabake dening opioid alami lan sintetik (contone, kodein, diphenoxylate, Fentanyl, heroin, hydromorphone, Levorphanol, meperidin, metadon, morfin, oksimorfon, alkaloid Opium pekat, propoksifen).
Migunani kanggo perawatan depresi sing disebabake opioid, kalebu depresi pernapasan, sing disebabake dening agonis parsial opioid tartamtu kalebu butorphanol, Nalbuphine, lan Pentazocine. Nanging, mbalikke depresi pernapasan saka overdosis agonis parsial opioid bisa uga ora lengkap lan mbutuhake dosis Naloxone sing luwih dhuwur utawa luwih kerep.
Bisa digunakake ing setelan komunitas (nonmedis) kanggo perawatan darurat saka overdosis opioid sing dikawruhi utawa dicurigai, sing diwujudake kanthi depresi pernapasan lan/utawa CNS. Kasedhiya minangka jarum suntik sing wis diisi lan semprotan irung nggampangake administrasi dening anggota kulawarga utawa pengasuh liyane; perawatan kuwi ora sulih kanggo perawatan medical darurat. Nalika menehi naloxone ing njaba setelan medis sing diawasi, tansah golek bantuan medis darurat sawise dosis pisanan diwenehake.
Akeh ahli kalebu CDC, American Heart Association (AHA), lan American Society of Addiction Medicine nyaranake administrasi naloxone ing kasus overdosis opioid sing dikenal utawa dicurigai.
Pedoman praktik klinis CDC 2022 babagan resep opioid kanggo nyeri nyaranake supaya dokter ngrembug risiko cilaka sing ana gandhengane karo opioid karo pasien, kalebu strategi mitigasi risiko kayata naloxone kanggo pembalikan overdosis.
Dokter kudu menehi naloxone lan nyedhiyakake pendhidhikan pencegahan overdosis kanggo pasien sing nampa analgesik opioid sing duwe risiko overdosis opioid (contone, sing nampa terapi bebarengan karo benzodiazepine utawa depresan CNS liyane, sing duwe riwayat opioid utawa gangguan panggunaan zat, sing duwe riwayat medis. kahanan sing bisa nambah sensitivitas kanggo efek opioid, sing wis ngalami overdosis opioid sadurunge, sing njupuk dosis opioid sing luwih dhuwur [contone, ≥50 setara morfin mg / dina, lan sing duwe risiko bali menyang dosis dhuwur sing wis ilang. toleransi [contone, pasien sing ngalami tapering utawa bubar dibebasake saka pakunjaran]). Naloxone uga kudu ditawakake nalika pasien sing nampa opioid duwe anggota kluwarga sing beresiko ora disengaja utawa overdosis.
Diagnosis Overdosis Opioid Akut sing Dicurigai utawa Dikenal
Digunakake kanggo diagnosa overdosis opioid akut sing dicurigai utawa dikenal.
Septic Shock
Naloxone hydrochloride injection is FDA-labeled for adjunctive use in management of septic shock. Wis digunakake ing nomer winates saka patients ing setelan iki. Munggah ing BP bisa nganti sawetara jam, nanging ora ditampilake kanggo nambah kaslametané lan gadhah efek salabetipun (contone, agitasi, mual, mutahke, busung paru, hypotension, aritmia jantung, kejang).
Ngati-ati ing pasien sing nandhang kejut septik, utamane ing pasien sing nandhang lara utawa sadurunge nampa terapi opioid lan bisa uga ngalami toleransi opioid. Terapi naloxone ora kalebu ing Pedoman Internasional Kampanye Sepsis Surviving kanggo Manajemen Sepsis lan Septic Shock; resusitasi cairan lan vasopressor (contone, norepinephrine, Vasopressin) digunakake lini pertama ing manajemen hemodinamik.
Diagnosis Penyalahgunaan Opioid Kronis (Tes Tantangan Naloxone)
Kanggo nyegah penarikan opioid sawise administrasi Naltrexone, naloxone wis digunakake minangka tes skrining (tes tantangan naloxone† [off-label]) kanggo nyathet ora ana katergantungan fisiologis lan nyuda risiko mundur total.
Tes tantangan naloxone ora dianjurake kanggo pasien sing ngandhut.
Terapi Kombinasi
Kombinasi pentazocine hydrochloride lan naloxone hydrochloride kanthi rasio 100:1 kasedhiya kanthi komersial kanggo panggunaan lisan minangka analgesik.
Kombinasi buprenorfin hidroklorida lan nalokson hidroklorida ing rasio 4: 1 kanggo administrasi sublingual utawa kira-kira 6: 1 kanggo administrasi intrabuccal kasedhiya kanthi komersial kanggo digunakake ing manajemen katergantungan opioid.
Opioid-Induced Pruritus
Nyegah saka opioid-induced pruritus† [off-label] ing bocah lan remaja.
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Carane nggunakake Naloxone (Systemic)
Umum
Pengawasan Pasien
Pertimbangan Umum Liyane
Administrasi
Administrasi kanthi injeksi IV, sub-Q, utawa IM; dening infus IV; utawa intranasally.
Aksi paling cepet digayuh kanthi administrasi IV, sing dianjurake ing kahanan darurat ing setelan sing diawasi sacara medis. Amarga panyerepan bisa uga ora mesthi utawa telat, AAP ora nyetujoni injeksi sub-Q utawa IM kanggo manajemen medis darurat mabuk opioid ing bocah-bocah utawa neonatus.
Yen akses IV ora bisa ditetepake ing kahanan darurat, wis diwenehake liwat tabung endotrakeal† [off-label] lan injeksi intraosseous† [off-label] (IO).
IV Infus
Infus IV sing terus-terusan bisa uga paling cocok kanggo pasien sing mbutuhake dosis sing luwih dhuwur, terus ngalami depresi pernapasan utawa CNS sing terus-terusan sawise terapi efektif kanthi dosis bola-bali, lan/utawa sing efek saka opioid long-acting lagi antagonis.
p> PengenceranKanggo infus IV sing terus-terusan, pabrikan nyatakake kanggo ngencerake 2 mg nalokson hidroklorida ing 500 mL natrium klorida 0,9% utawa injeksi Dextrose 5% kanggo ngasilake larutan sing ngemot 0,004 mg/mL (4 mcg/mL). Konsentrasi liyane wis disaranake (pirsani Standardize 4 Safety under DoSage and Administration).
Tingkat AdministrasiTitrasi sesuai karo respon pasien.
IM utawa Sub-Q Injection
Mungkin diwenehake dening anggota kulawarga utawa pengasuh liyane sadurunge tanggap darurat medis kanggo individu sing dikawruhi utawa dicurigai overdosis opioid. Pengasuh kudu njaluk perawatan medis darurat sanalika sawise menehi dosis awal.
Bisa ditindakake kanthi injeksi IM utawa sub-Q liwat jarum suntik sing wis diisi. Atur dosis awal jarum suntik sing wis diisi naloxone (Zimhi) IM utawa sub-Q menyang aspek anterolateral paha, liwat sandhangan yen perlu. Nalika diwènèhaké kanggo pasien pediatrik <1 taun, jiwitake otot paha nalika menehi obat kasebut.
Administrasi Intranasal
Bisa ditindakake dening anggota kulawarga utawa pengasuh liyane sadurunge tanggap darurat medis. kanggo individu sing dikenal utawa dicurigai overdosis opioid.
Aja mbusak unit semprotan irung saka karton nganti wektu administrasi; aja prima utawa unit test sadurunge administrasi.
Teknik Administrasi IntranasalDelehake pasien ing posisi supine. Copot unit semprotan irung saka paket karton lan blister. Ngiringake sirah pasien, kanthi tangan siji ndhukung gulu. Aja prima utawa nyoba piranti sadurunge administrasi. Lebokake ujung unit semprotan irung alon-alon menyang siji bolongan irung nganti driji ing salah siji sisih nozzle nglawan irung pasien; pencet piranti plunger kuwat kanggo ngatur dosis.
Copot muncung saka bolongan irung sawise administrasi, lan pasang pasien ing posisi pemulihan; ngawasi pasien kanthi rapet.
Yen mbutuhake dosis tambahan, lebokake menyang bolongan irung alternatif nggunakake unit semprotan irung anyar.
Standar 4 Keamanan
Konsentrasi standar kanggo naloxone wis ditetepake liwat Standardize 4 Safety (S4S), inisiatif safety pasien nasional kanggo nyuda kesalahan obat, utamane sajrone transisi perawatan. Amarga rekomendasi saka panel S4S bisa uga beda karo informasi resep pabrikan, sampeyan kudu ati-ati nalika nggunakake konsentrasi sing beda karo label, utamane nalika nggunakake informasi tarif saka label. Kanggo informasi tambahan babagan S4S (kalebu nganyari sing kasedhiya), waca [Web].
Panel ngerteni yen konsentrasi 40 lan 400 mcg/mL sing kadhaptar ing standar pediatrik 10x beda; Nanging, iki mung rong konsentrasi sing ditliti kanggo stabilitas.
Tabel 1: Standarisasi 4 Standar Keamanan Naloxone Hydrochloride249250Populasi Pasien
Standar konsentrasi
Unit dosis
Pasien anak (<50 kg)
16 mcg/mL
40 mcg/mL
400 mcg/mL
mcg/kg/jam
Dewasa
16 mcg/mL
40 mcg/mL
mg/jam
mcg/kg/hr - pruritus† [off-label]
Dosis
Kasedhiya minangka naloxone hydrochloride; dosis ditulis ing syarat-syarat uyah.
Pasien Pediatrik
Depresi sing disebabake opioid ing Neonatus IV, IM, utawa Sub-QDosis awal biasa yaiku 0,01 mg / kg, diwenehake kanthi interval 2 nganti 3 menit menyang derajat kuwalikan sing dikarepake.
Overdosis Opioid ing Anak IV, IM, utawa Sub-QBocah-bocah bisa nampa dosis nalokson hidroklorida IV awal 0,01 mg/kg; yen dosis iki ora ngasilake tingkat respon sing dikarepake, dosis sabanjure 0,1 mg / kg bisa ditindakake.
IntranasalSiji semprotan (2, 4, utawa 8 mg [isi siji unit semprotan]); yen pasien gagal nanggapi utawa nanggapi nanging banjur bali menyang depresi pernapasan, baleni maneh yen perlu (yen kasedhiya unit semprotan tambahan) kanthi interval 2 nganti 3 menit nganti perawatan darurat teka. Prescribe kekuatan 2-mg kanggo pasien sing gumantung karo opioid sing samesthine bakal duwe risiko mundur opioid sing abot mung nalika risiko paparan opioid sing ora disengaja utawa disengaja dening kontak kluwarga kurang.
IO† utawa Endotrakeal†Anak < Umur 5 taun utawa bobote ≤20 kg: Sawetara ahli nyaranake dosis 0,1 mg/kg.
Bocah ≥5 taun utawa bobote>20 kg: Sawetara ahli nyaranake dosis 2 mg.
Dosis optimal kanggo administrasi liwat tabung endotrakeal† durung ditetepake (dosis sing luwih dhuwur dibandhingake karo rute liyane bisa uga perlu).
Diagnosis Overdosis Opioid IVOra ana rekomendasi khusus ing wektu iki. Yen ora ana respon sawise administrasi 10 mg naloxone, diagnosis keracunan sing disebabake opioid kudu ditakoni.
Depresi Opioid Pascaoperasi IVKanggo mbalikke wiwitan depresi ambegan, naloxone hydrochloride kudu diwènèhaké kanthi tambahan 0,005-0,01 mg ing interval 2 nganti 3 menit nganti respon sing dikarepake (yaiku, ventilasi lan kewaspadaan sing nyukupi tanpa perlu. nyeri utawa rasa ora nyaman) dipikolehi.
Perawatan Opioid-Induced Pruritus IV†Dosis ing bocah lan remaja antara 0.25-1.0 mcg / kg saben jam liwat infus IV terus-terusan.
Dewasa
Postoperative Opioid Depression IVDosis awal: Biasane, 0.1-0.2 mg, diwenehake ing interval 2 nganti 3 menit nganti respon sing dikarepake (yaiku, ventilasi lan kewaspadaan sing nyukupi tanpa penting. nyeri utawa rasa ora nyaman) dipikolehi; dosis tambahan bisa uga dibutuhake ing interval 1-2 jam gumantung saka respon lan dosis lan durasi tumindak opioid sing diwenehake.
Kanggo infus IV sing terus-terusan, tingkat titrasi infus sesuai karo respon pasien.
Overdosis Opioid IVDosis awal: Biasane, 0,4-2 mg IV, diwenehake kanthi interval 2 nganti 3 menit yen perlu; yen ora ana respon sing diamati sawise total 10 mg obat kasebut diwenehake, kondisi depresi bisa disebabake dening proses obat utawa penyakit sing ora responsif marang naloxone.
Durasi tumindak opioid asring ngluwihi nalokson; efek depresan opioid bisa bali amarga efek naloxone suda, lan dosis nalokson tambahan bisa uga dibutuhake.
Ngawasi pasien kanthi ati-ati kanggo kambuh efek depresan opioid.
IM utawa Sub-Q2 mg (isi siji jarum suntik sing wis diisi) utawa 5 mg (isi siji jarum suntik sing wis diisi; Zimhi); yen pasien ora nanggapi utawa nanggapi nanging banjur kambuh dadi depresi pernapasan, baleni maneh yen perlu ing interval 2-3 menit nganti perawatan darurat teka.
IntranasalSiji semprotan (2, 4, utawa 8 mg [isi siji unit semprotan]); yen pasien ora nanggapi utawa nanggapi nanging banjur kambuh dadi depresi pernapasan, baleni maneh yen perlu ing interval 2-3 menit nganti perawatan darurat teka. Prescribe kekuatan 2-mg kanggo pasien sing gumantung karo opioid sing samesthine bakal duwe risiko mundur opioid sing abot mung nalika risiko paparan opioid sing ora disengaja utawa disengaja dening kontak kluwarga kurang.
IO† utawa Endotracheal†Dosis optimal ora ditetepake; dosis khas sing diwenehake dening rute endotrakeal yaiku 2-2,5 kaping dosis IV sing disaranake.
Diagnosis Overdosis Opioid IVOra ana rekomendasi khusus ing wektu iki. Yen ora ana respon sawise administrasi 10 mg naloxone, diagnosis keracunan sing disebabake opioid kudu ditakoni.
Tes Tantangan NaloxoneAdministrasi naloxone hydrochloride 0.4–0.8 mg sadurunge miwiti perawatan karo naltrexone bisa mbantu ndokumentasikake ora ana katergantungan fisiologis lan nyuda resiko mundur.
Septic Shock IVOptimal dosis lan regimen perawatan ora ditetepake.
Populasi Khusus
Gangguan Hepatik
Ora ana rekomendasi dosis khusus.
Gagal ginjal
Ora ana rekomendasi dosis khusus.
Pasien Geriatrik
Ora ana rekomendasi dosis khusus; ati-ati nalika milih dosis.
Pènget
Kontraindikasi
Pènget/PanandhapTindakan Resusitasi Liyane
Yen digunakake kanggo ngatur overdosis opioid akut, langkah resusitasi liyane (contone, pangopènan saluran napas sing nyukupi, respirasi buatan, pijet jantung, agen vasopressor) kudu kasedhiya lan digunakake nalika perlu.
Dosis Kakehan ing Pasien Pasca Operasi
Dosis sing berlebihan ing pasien pasca operasi nyebabake agitasi lan mbalikke analgesia.
Gunakake ing Pasien karo Gangguan Kardiovaskular
Hipotensi, hipertensi, takikardia / fibrilasi ventrikel, edema paru, lan serangan jantung sing dilapurake ing pasien pasca operasi sing nampa naloxone, kadhangkala nyebabake pati, koma, utawa encephalopathy. Dilaporake utamane ing pasien sing duwe kelainan kardiovaskular sing wis ana sadurunge utawa nampa obat liya kanthi efek kardiovaskular sing padha.
Gunakake kanthi ati-ati ing pasien sing duwe penyakit kardiovaskular sing wis ana sadurunge utawa sing nampa obat-obatan sing duweni potensi kardiotoksik; ngawasi pasien kasebut kanggo hipotensi, tachycardia ventrikel utawa fibrilasi, lan edema paru.
Efikasi Terbatas karo Agonis Parsial utawa Agonis/Antagonis Campuran
Pembalikan depresi pernapasan amarga overdosis agonis parsial opioid (umpamane, Buprenorphine, pentazocine) bisa uga ora lengkap lan mbutuhake dosis nalokson sing luwih dhuwur utawa bola-bali.
Presipitasi Penarikan Opioid Parah
Bisa nyebabake gejala mundur opioid sing abot. Pembalikan efek opioid sing tiba-tiba bisa nyebabake mual, muntah, kringet, tremor, tachycardia, hipotensi, hipertensi, kejang, takikardia / fibrilasi ventrikel, edema paru, lan serangan jantung, sing bisa nyebabake pati.
Ngatur kanthi ati-ati kanggo pasien sing dikenal utawa dicurigai gumantung sacara fisik marang opioid (kalebu neonatus sing lair saka wanita sing gumantung karo opioid), utamane ing pasien sing nandhang penyakit kardiovaskular. (Deleng Panganggone ing Patients with Cardiovascular Disorders ing Cautions.)
Risiko Pernafasan Ambalan lan Depresi SSP
Durasi tumindak umume opioid bisa ngluwihi naloxone sing nyebabake bali saka ambegan lan/utawa depresi CNS sawise perbaikan awal. Ngawasi pasien kanthi rapet lan ngatur dosis naloxone sing bola-bali yen perlu. Pasien kanthi overdosis opioid sing dawa tumindak utawa dibebasake bisa uga mbutuhake wektu pengamatan sing luwih suwe. Ngawasi pasien pediatrik sing wis nanggapi naloxone paling ora 24 jam.
Risiko Ciloko Jarum Tanpa Sengaja
Cedera jarum suntik bisa kedadeyan ing kahanan darurat kanthi nggunakake jarum suntik sing wis diisi naloxone (Zimhi). Yen ana jarum suntik sing ora disengaja, golek bantuan medis. Kaku pasien pentinge familiarize dhewe karo piranti sadurunge kahanan darurat.
Populasi Tertentu
KandhutanData winates babagan panggunaan ing wanita ngandhut. Gunakake mung yen cetha perlu. Coba rasio resiko-manfaat sadurunge menehi naloxone kanggo wanita ngandhut sing wis dikenal utawa dicurigai katergantungan opioid. Naloxone ngliwati plasenta; risiko mundur opioid ing wanita ngandhut lan janin. Monitor distress janin.
LaktasiOra dingerteni manawa naloxone disebarake menyang susu utawa duweni pengaruh marang bayi sing disusui utawa ing produksi susu, gunakake naloxone kanthi ati-ati ing wanita sing nyusoni. Ora mengaruhi konsentrasi prolaktin utawa oxytocin ing wanita sing nyusoni, lan bioavailabilitas oral minimal.
Badhak wadon lan Lanang saka Potensi ReproduksiPanaliten kewan ora ana bukti yen kesuburan cacat.
Panggunaan PediatrikNaloxone bisa digunakake kanggo mbalikke efek opioid ing bayi lan bocah-bocah. Keamanan lan khasiat jarum suntik sing wis diisi kanggo panggunaan IM utawa Sub-Q (Zimhi) utawa semprotan irung (contone, Narcan, Kloxxado) sing ditetepake ing pasien pediatrik kabeh umur kanggo perawatan darurat saka overdosis opioid sing dikenal utawa dicurigai. Panggunaan kasebut ing pasien pediatrik sing didhukung dening studi bioequivalence diwasa lan bukti saka produk naloxone liyane.
Panyerepan sawise administrasi intranasal utawa injeksi IM utawa sub-Q ing pasien pediatrik bisa uga ora mesthi utawa telat; kanthi ati-ati ngawasi pasien pediatrik ≥24 jam.
Aman lan khasiat ing manajemen hipotensi sing gegandhèngan karo kejut septik ora ditetepake ing pasien pediatrik. Ing panaliten babagan 2 neonatus kanthi kejut septik, perawatan karo naloxone ngasilake respon pressor positif; Nanging, siji pasien banjur tiwas sawise kejang sing ora bisa ditindakake.
Panggunaan GeriatrikPengalaman sing ora cukup ing pasien ≥65 taun kanggo nemtokake manawa pasien geriatrik nanggapi beda karo wong diwasa sing luwih enom. Pilih dosis kanthi ati-ati amarga nyuda fungsi ati, ginjel, lan / utawa jantung sing gegandhengan karo umur lan potensial kanggo penyakit bebarengan lan terapi obat.
Gangguan HepatikKeamanan lan khasiat ora ditetepake; nggunakake kanthi ati-ati.
Gagal GinjalKeamanan lan khasiat ora ditetepake; nggunakake kanthi ati-ati.
Efek Samsaya Awon
Naloxone intranasal: nyeri abdomen, asthenia, pusing, sirah, tekanan getih mundhak, konstipasi, lara untu, kram otot, nyeri muskuloskeletal, hidung tersumbat, irung ora nyaman, irung garing, edema irung, inflamasi irung, presinkop, rhinalgia, xeroderma.
Naloxone parenteral (nggunakake sawise operasi): Hipotensi, hipertensi, takikardia ventrikel lan fibrilasi, dyspnea, edema paru, lan serangan jantung dilaporake; sequelae kalebu pati, koma, lan encephalopathy. Efek kardiovaskuler sing paling umum ing pasien sing nandhang penyakit kardiovaskular sing wis ana utawa sing nampa obat liya sing nyebabake efek kardiovaskular sing padha.
Injeksi naloxone kanggo panggunaan IM utawa sub-Q (Zimhi): pusing, bilirubin sing dhuwur, pusing, lan mual.
Pemulihan efek opiat sing tiba-tiba bisa nyebabake mundur akut lan prilaku agresif.
Apa obatan liyane bakal mengaruhi Naloxone (Systemic)
Dimetabolisme ing ati utamane kanthi konjugasi glukuronida.
Obat Spesifik
Obat
Interaksi
Komentar
Buprenorphine
Buprenorphine dawa tumindak; wiwitan efek pembalikan naloxone bertahap.
Dosis gedhe saka naloxone dibutuhake kanggo antagonize buprenorfin.
Methohexital
Methohexital katon kanggo mblokir onset akut gejala penarikan sing disebabake dening naloxone ing pecandu opioid
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