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Statements

Subject Item
dbr:Diprenorphine
rdf:type
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rdfs:label
Diprenorphin Diprenorphine Diprénorphine 地利洛非
rdfs:comment
地利洛非也称为二丙诺啡，是（MOR），（KOR）和阿片受体（DOR）（三者具有相同的亲和力）的非选择性，高亲和力，弱部分激动剂，同时在兽医学中用作。它用于逆转超强效阿片类镇痛药的作用，例如用于镇静大型动物的和。该药物未被批准用于人类。 地利洛非是市场上最强的阿片类拮抗剂（作为拮抗剂的效力比纳洛芬高100倍），并且用于逆转非常强的阿片类物质的作用是，其结合亲和力如此之高以至于纳洛酮不能有效或可靠地逆转麻醉作用。这些超强效的阿片类药物，除了丁丙诺啡以外（由于其部分激动作用而具有改善的安全性），因为人体剂量太小难以正确测量，因此不会用于人体。 因此过量服用的风险会导致致命的呼吸抑制。然而，常规阿片类衍生物的镇静强度不足以使大型动物（如大象和犀牛）迅速镇静，因此埃托啡和卡芬太尼等药物可用于此目的。 因为地利洛非是阿片受体的弱部分激动剂而不是沉默拮抗剂，可以在没有其他足够剂量的阿片类药物的情况下产生一些阿片类药物作用。此外，由于具有KOR的部分激动作用，它似乎相对于MOR具有显着更大的内在活性，因此地利洛非可以产生镇静作用，并且在人类中也可以产生幻觉。 Diprenorphin (Revivon, M5050) ist ein Opioid-Antagonist. Es wird eingesetzt, um die Wirkung extrem potenter Opioide, wie Etorphin oder Carfentanyl aufzuheben, die in der Tiermedizin eingesetzt werden, um große Tiere zu betäuben. Diprenorphin ist der stärkste kommerziell verfügbare Opioidantagonist. Es wird benutzt, um Tiere, die mit den genannten Opioiden betäubt worden sind, wieder aufzuwecken. Weil Diprenorphin eine zum Teil auch agonistische Wirkung hat, wird es nicht beim Menschen angewandt, wo Naloxon oder Naltrexon Mittel der Wahl sind.Die Wirkungsstärke als Antagonist wird mit 100-mal der von (N-Allylnormorphin, einem schon seit Langem nicht mehr eingesetzten Opioidantagonisten) angegeben. In Deutschland sind keine Tierarzneimittel auf der Basis von Diprenorphin zugelassen. Diprenorphine (brand name Revivon; former developmental code name M5050), also known as diprenorfin, is a non-selective, high-affinity, weak partial agonist of the μ- (MOR), κ- (KOR), and δ-opioid receptor (DOR) (with equal affinity) which is used in veterinary medicine as an opioid antagonist. It is used to reverse the effects of super-potent opioid analgesics such as etorphine and carfentanil that are used for tranquilizing large animals. The drug is not approved for use in humans. La diprénorphine, ou diprénorfine, est un agoniste partiel faible non sélectif dont l'affinité très élevée est égale pour les récepteurs opioïdes mu (μ), delta (δ) et kappa (κ). Elle est employée en médecine vétérinaire comme antagoniste des opioïdes pour stopper l'effet des sédatifs très puissants comme l'étorphine et le carfentanil utilisés pour tranquilliser les gros animaux. L'usage de cette molécule sur les humains n'est pas autorisé.
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dbo:wikiPageWikiLink
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dbp:synonyms
Diprenorfin; M5050
dbp:tradename
Revivon
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1
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changed
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dbo:abstract
Diprenorphin (Revivon, M5050) ist ein Opioid-Antagonist. Es wird eingesetzt, um die Wirkung extrem potenter Opioide, wie Etorphin oder Carfentanyl aufzuheben, die in der Tiermedizin eingesetzt werden, um große Tiere zu betäuben. Diprenorphin ist der stärkste kommerziell verfügbare Opioidantagonist. Es wird benutzt, um Tiere, die mit den genannten Opioiden betäubt worden sind, wieder aufzuwecken. Weil Diprenorphin eine zum Teil auch agonistische Wirkung hat, wird es nicht beim Menschen angewandt, wo Naloxon oder Naltrexon Mittel der Wahl sind.Die Wirkungsstärke als Antagonist wird mit 100-mal der von (N-Allylnormorphin, einem schon seit Langem nicht mehr eingesetzten Opioidantagonisten) angegeben. In Deutschland sind keine Tierarzneimittel auf der Basis von Diprenorphin zugelassen. 地利洛非也称为二丙诺啡，是（MOR），（KOR）和阿片受体（DOR）（三者具有相同的亲和力）的非选择性，高亲和力，弱部分激动剂，同时在兽医学中用作。它用于逆转超强效阿片类镇痛药的作用，例如用于镇静大型动物的和。该药物未被批准用于人类。 地利洛非是市场上最强的阿片类拮抗剂（作为拮抗剂的效力比纳洛芬高100倍），并且用于逆转非常强的阿片类物质的作用是，其结合亲和力如此之高以至于纳洛酮不能有效或可靠地逆转麻醉作用。这些超强效的阿片类药物，除了丁丙诺啡以外（由于其部分激动作用而具有改善的安全性），因为人体剂量太小难以正确测量，因此不会用于人体。 因此过量服用的风险会导致致命的呼吸抑制。然而，常规阿片类衍生物的镇静强度不足以使大型动物（如大象和犀牛）迅速镇静，因此埃托啡和卡芬太尼等药物可用于此目的。 因为地利洛非是阿片受体的弱部分激动剂而不是沉默拮抗剂，可以在没有其他足够剂量的阿片类药物的情况下产生一些阿片类药物作用。此外，由于具有KOR的部分激动作用，它似乎相对于MOR具有显着更大的内在活性，因此地利洛非可以产生镇静作用，并且在人类中也可以产生幻觉。 La diprénorphine, ou diprénorfine, est un agoniste partiel faible non sélectif dont l'affinité très élevée est égale pour les récepteurs opioïdes mu (μ), delta (δ) et kappa (κ). Elle est employée en médecine vétérinaire comme antagoniste des opioïdes pour stopper l'effet des sédatifs très puissants comme l'étorphine et le carfentanil utilisés pour tranquilliser les gros animaux. L'usage de cette molécule sur les humains n'est pas autorisé. Diprenorphine (brand name Revivon; former developmental code name M5050), also known as diprenorfin, is a non-selective, high-affinity, weak partial agonist of the μ- (MOR), κ- (KOR), and δ-opioid receptor (DOR) (with equal affinity) which is used in veterinary medicine as an opioid antagonist. It is used to reverse the effects of super-potent opioid analgesics such as etorphine and carfentanil that are used for tranquilizing large animals. The drug is not approved for use in humans. Diprenorphine is the strongest opioid antagonist that is commercially available (some 100 times more potent as an antagonist than nalorphine), and is used for reversing the effects of very strong opioids for which the binding affinity is so high that naloxone does not effectively or reliably reverse the narcotic effects. These super-potent opioids, with the single exception of buprenorphine (which has an improved safety-profile due to its partial agonism character), are not used in humans because the dose for a human is so small that it would be difficult to measure properly, so there is an excessive risk of overdose leading to fatal respiratory depression. However conventional opioid derivatives are not strong enough to rapidly tranquilize large animals, like elephants and rhinos, so drugs such as etorphine and carfentanil are available for this purpose. Diprenorphine is considered to be the specific reversing agent/antagonist for etorphine and carfentanil, and is normally used to remobilise animals once veterinary procedures have been completed. Since diprenorphine also has partial agonistic properties of its own, it should not be used on humans if they are accidentally exposed to etorphine or carfentanil. Naloxone or naltrexone is the preferred human opioid receptor antagonist. In theory, diprenorphine could also be used as an antidote for treating overdose of certain opioid derivatives which are used in humans, particularly buprenorphine for which the binding affinity is so high that naloxone does not reliably reverse the narcotic effects. However, diprenorphine is not generally available in hospitals; instead a vial of diprenorphine is supplied with etorphine or carfentanil specifically for reversing the effects of the drug, so the use of diprenorphine for treating a buprenorphine overdose is not usually carried out in practice. Because diprenorphine is a weak partial agonist of the opioid receptors rather than a silent antagonist, it can produce some opioid effects in the absence of other opioids at sufficient doses. Moreover, due to partial agonism of the KOR, where it appears to possess significantly greater intrinsic activity relative to the MOR, diprenorphine can produce sedation as well as, in humans, hallucinations.
dbp:atcvet
yes
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Revivon
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14357-78-9
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