Nalbuphine (original) (raw)

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نالبوفين Nalbuphine أو Nubain هو مسكن أفيوني نصف صنعي. يكون فعال في النساء أكثر من الرجال، بل حتى يمكن أن يزيد الألم لدى الرجال. يُستَعمَل للتنويم خلال العمليات الجراحية كما يستخدم لتخفيف شدَّة الآلام.. يوجد على شكل ملحين بارابين أو سلفيت.

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dbo:abstract Nalbufin je opioidní analgetikum používané pro léčbu bolesti. Podává se injekčně do žíly, svalu nebo tuku. Mezi vedlejší účinky nalbufinu patří sedace, pocení, nevolnost, zvracení, závrať, sucho v ústech a bolest hlavy. Na rozdíl od většiny ostatních opioidů vyvolává Nalbufin jen slabou euforii a od určité dávky již dále nezesiluje útlum dýchacího centra. Je zde také téměř nulová incidence dysforie, disociativních stavů či halucinací, bere-li se lék v obvyklých terapeutických dávkách. Nalbufin je smíšený agonista-antagonista opioidových receptorů. Nalbufin byl objeven roku 1965 a v roce 1979 byl ve Spojených státech amerických schválen Úřadem pro kontrolu potravin a léčiv. (cs) نالبوفين Nalbuphine أو Nubain هو مسكن أفيوني نصف صنعي. يكون فعال في النساء أكثر من الرجال، بل حتى يمكن أن يزيد الألم لدى الرجال. يُستَعمَل للتنويم خلال العمليات الجراحية كما يستخدم لتخفيف شدَّة الآلام.. يوجد على شكل ملحين بارابين أو سلفيت. (ar) Nalbuphin ist ein Arzneistoff aus der Gruppe der Schmerzmittel vom Opioid-Typ. Er wirkt agonistisch an den κ-Opioidrezeptoren und partiell antagonistisch an den µ-Opioidrezeptoren. Die Vorteile des Partialantagonisten liegen darin, dass eine opioidbedingte Atemdepression, z. B. postoperativ nach dem Einsatz von Fentanyl während der Narkose, aufgehoben werden kann bei gleichzeitiger Fortführung der Schmerzbehandlung, da Nalbuphin selbst analgetisch wirkt. Die analgetische Potenz verglichen mit Morphin liegt bei 0,5–0,8. Es ist dem Pentazocin ähnlich, steigert jedoch den Blutdruck und die Herzfrequenz nicht.Bei opiatabhängigen Patienten kann der Einsatz von Nalbuphin allerdings sofort nach der Injektion ein Entzugssyndrom hervorrufen. Nalbuphin wird als Hydrochlorid in Injektionslösungen eingesetzt. Die Wirkung tritt rasch nach zwei bis drei Minuten ein. Die Halbwertszeit beträgt circa drei Stunden, die Wirkdauer bis zu sechs Stunden. Die gleichzeitige Gabe zu einer Behandlung mit μ-agonistischen Opioiden wie etwa Morphin oder Fentanyl ist kontraindiziert. (de) Nalbuphine, sold under the brand names Nubain among others, is an opioid analgesic which is used in the treatment of pain. It is given by injection into a vein, muscle, or fat. Side effects of nalbuphine include sedation, sweatiness, clamminess, nausea, vomiting, dizziness, vertigo, dry mouth, and headache. Unlike other opioids, it has little to no capacity for euphoria or respiratory depression. It also has little to no incidence of dysphoria, dissociation, hallucinations, and related side effects at typical therapeutic doses. Nalbuphine is a mixed agonist/antagonist opioid modulator. Specifically, it acts as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor (MOR) and as a high-efficacy partial agonist of the κ-opioid receptor (KOR), whereas it has relatively low affinity for the δ-opioid receptor (DOR) and sigma receptors. Nalbuphine was patented in 1963 and was introduced for medical use in the United States in 1979. It is marketed in many countries throughout the world. (en) La nalbuphine est un antalgique opiacé fort utilisé pour traiter les douleurs intenses ou rebelles aux autres antalgiques. Elle est susceptible d'entraîner une dépendance. Elle agit en bloquant les influx nerveux véhiculant la douleur. (fr) Nalbufina é um fármaco utilizado como analgésico opióide, utilizado no tratamento da dor. Nalbufina é um analgésico narcótico agonista-antagonista. Relacionado quimicamente com naloxona, tem potência analgésica semelhante a morfina. Atua principalmente nos receptores kappa como agonista total e agonista parcial dos receptores mu. Produz depressao respiratória, porém diferente da morfina e outros opióides há efeito teto. Quando administrada concomitantemente com analgésicos opióides ou agonistas pode reverter parcialmente ou bloquear a depressao respiratória narcótico-induzida. utilizada em casos de intoxicação por hipnoanalgésicos. (pt) Налбуфін (англ. Nalbuphine, лат. Nalbuphinum) — синтетичний лікарський засіб, що належить до групи опіоїдних анальгетиків і є похідним фенантрену. Налбуфін застосовується переважно парентерально, як внутрішньовенно, так і внутрішньом'язово і підшкірно, вкрай рідко препарат застосовується перорально. Налбуфін уперше запатентовано у 1963 році в США і схвалено для клінічного застосування в 1979 році. (uk) 纳布啡是一种阿片类受体的镇静剂型精神药物,其镇静效果类似吗啡,有呼吸抑制作用但不明显。同时其抑制有封顶效应,无心血管副反应,临床上一般用于手术后镇痛。 (zh) Налбуфин (Nalbuphine) — опиоидный анальгетик. (ru)
dbo:alternativeName Nubain, Nalpain, Nalbuphin, others (en)
dbo:casNumber 20594-83-6
dbo:chEBI 7454
dbo:chEMBL 895
dbo:drugbank DB00844
dbo:fdaUniiCode L2T84IQI2K
dbo:medlinePlus a682668
dbo:pubchem 5311304
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dbp:alt Skeletal formula (en) Ball-and-stick model of nalbuphine (en)
dbp:atcPrefix N02 (en)
dbp:atcSuffix AF02 (en)
dbp:bioavailability • : 76% , 79% (en) • : 81% , 83% (en) • Oral: 11% , >44% (en)
dbp:c 21 (xsd:integer)
dbp:casNumber 20594 (xsd:integer)
dbp:chebi 7454 (xsd:integer)
dbp:chembl 895 (xsd:integer)
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dbp:drugbank DB00844 (en)
dbp:durationOfAction -21600.0
dbp:eliminationHalfLife 18000.0
dbp:excretion 21600.0
dbp:h 27 (xsd:integer)
dbp:image Nalbuphine molecule ball.png (en)
dbp:iupacName -3 (xsd:integer)
dbp:iupharLigand 1663 (xsd:integer)
dbp:legalAu S4 (en)
dbp:legalCa Schedule IV (en)
dbp:legalStatus Federally Uncontrolled , except in KY, C-IV (en)
dbp:legalUs Rx only Schedule IV in some states (en)
dbp:medlineplus a682668 (en)
dbp:metabolism Liver (en)
dbp:metabolites Glucuronide conjugates , others (en)
dbp:n 1 (xsd:integer)
dbp:o 4 (xsd:integer)
dbp:onset 1800.0 3600.0 900.0 -180.0
dbp:pregnancyCategory B (en)
dbp:proteinBound 50.0
dbp:pubchem 5311304 (xsd:integer)
dbp:routesOfAdministration dbr:Subcutaneous_injection dbr:Intramuscular dbr:Intravenous
dbp:smiles O[C@@H]4[C@@H]5Oc1c2cC[C@H]3NCC6CCC6 (en)
dbp:stdinchi 1 (xsd:integer)
dbp:stdinchikey NETZHAKZCGBWSS-CEDHKZHLSA-N (en)
dbp:synonyms EN-2234A; N-Cyclobutylmethyl-14-hydroxydihydronormorphine; 17-Cyclobutylmethyl-4,5α-epoxymorphinan-3,6α,14-triol; N-Cyclobutylmethyl-4,5α-epoxy-3,6α,14-morphinantriol (en)
dbp:tradename Nubain, Nalpain, Nalbuphin, others (en)
dbp:unii L2T84IQI2K (en)
dbp:verifiedfields verified (en)
dbp:verifiedrevid 459830736 (xsd:integer)
dbp:watchedfields verified (en)
dbp:width 225 (xsd:integer) 250 (xsd:integer)
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gold:hypernym dbr:Opioid
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rdfs:comment نالبوفين Nalbuphine أو Nubain هو مسكن أفيوني نصف صنعي. يكون فعال في النساء أكثر من الرجال، بل حتى يمكن أن يزيد الألم لدى الرجال. يُستَعمَل للتنويم خلال العمليات الجراحية كما يستخدم لتخفيف شدَّة الآلام.. يوجد على شكل ملحين بارابين أو سلفيت. (ar) La nalbuphine est un antalgique opiacé fort utilisé pour traiter les douleurs intenses ou rebelles aux autres antalgiques. Elle est susceptible d'entraîner une dépendance. Elle agit en bloquant les influx nerveux véhiculant la douleur. (fr) Налбуфін (англ. Nalbuphine, лат. Nalbuphinum) — синтетичний лікарський засіб, що належить до групи опіоїдних анальгетиків і є похідним фенантрену. Налбуфін застосовується переважно парентерально, як внутрішньовенно, так і внутрішньом'язово і підшкірно, вкрай рідко препарат застосовується перорально. Налбуфін уперше запатентовано у 1963 році в США і схвалено для клінічного застосування в 1979 році. (uk) 纳布啡是一种阿片类受体的镇静剂型精神药物,其镇静效果类似吗啡,有呼吸抑制作用但不明显。同时其抑制有封顶效应,无心血管副反应,临床上一般用于手术后镇痛。 (zh) Налбуфин (Nalbuphine) — опиоидный анальгетик. (ru) Nalbufin je opioidní analgetikum používané pro léčbu bolesti. Podává se injekčně do žíly, svalu nebo tuku. Mezi vedlejší účinky nalbufinu patří sedace, pocení, nevolnost, zvracení, závrať, sucho v ústech a bolest hlavy. Na rozdíl od většiny ostatních opioidů vyvolává Nalbufin jen slabou euforii a od určité dávky již dále nezesiluje útlum dýchacího centra. Je zde také téměř nulová incidence dysforie, disociativních stavů či halucinací, bere-li se lék v obvyklých terapeutických dávkách. Nalbufin je smíšený agonista-antagonista opioidových receptorů. (cs) Nalbuphin ist ein Arzneistoff aus der Gruppe der Schmerzmittel vom Opioid-Typ. Er wirkt agonistisch an den κ-Opioidrezeptoren und partiell antagonistisch an den µ-Opioidrezeptoren. Die Vorteile des Partialantagonisten liegen darin, dass eine opioidbedingte Atemdepression, z. B. postoperativ nach dem Einsatz von Fentanyl während der Narkose, aufgehoben werden kann bei gleichzeitiger Fortführung der Schmerzbehandlung, da Nalbuphin selbst analgetisch wirkt. Die analgetische Potenz verglichen mit Morphin liegt bei 0,5–0,8. Es ist dem Pentazocin ähnlich, steigert jedoch den Blutdruck und die Herzfrequenz nicht.Bei opiatabhängigen Patienten kann der Einsatz von Nalbuphin allerdings sofort nach der Injektion ein Entzugssyndrom hervorrufen. (de) Nalbuphine, sold under the brand names Nubain among others, is an opioid analgesic which is used in the treatment of pain. It is given by injection into a vein, muscle, or fat. Side effects of nalbuphine include sedation, sweatiness, clamminess, nausea, vomiting, dizziness, vertigo, dry mouth, and headache. Unlike other opioids, it has little to no capacity for euphoria or respiratory depression. It also has little to no incidence of dysphoria, dissociation, hallucinations, and related side effects at typical therapeutic doses. Nalbuphine is a mixed agonist/antagonist opioid modulator. Specifically, it acts as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor (MOR) and as a high-efficacy partial agonist of the κ-opioid receptor (KOR), whereas it has relatively low (en) Nalbufina é um fármaco utilizado como analgésico opióide, utilizado no tratamento da dor. Nalbufina é um analgésico narcótico agonista-antagonista. Relacionado quimicamente com naloxona, tem potência analgésica semelhante a morfina. Atua principalmente nos receptores kappa como agonista total e agonista parcial dos receptores mu. Produz depressao respiratória, porém diferente da morfina e outros opióides há efeito teto. Quando administrada concomitantemente com analgésicos opióides ou agonistas pode reverter parcialmente ou bloquear a depressao respiratória narcótico-induzida. (pt)
rdfs:label نالبوفين (ar) Nalbufin (cs) Nalbuphin (de) Nalbuphine (fr) Nalbuphine (en) Налбуфин (ru) Nalbufina (pt) 纳布啡 (zh) Налбуфін (uk)
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