Налбуфин википедия

Налбуфин википедия

Налбуфин википедия

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Налбуфин википедия

Nalbuphine , sold under the brand names Nubain among others, is an opioid analgesic which is used in the treatment of pain. Side effects of nalbuphine include sedation , sweatiness , clamminess , nausea , vomiting , dizziness , vertigo , dry mouth , and headache. Nalbuphine was patented in and was introduced for medical use in the United States in Nalbuphine is indicated for the relief of moderate to severe pain. It can also be used as a supplement to balanced anesthesia, for preoperative and postoperative analgesia, and for obstetrical analgesia during labor and delivery. However, a Cochrane Systematic Review concluded that from the included studies, there was limited evidence to demonstrate that '0. Although nalbuphine possesses opioid antagonist activity, there is evidence that in nondependent patients it will not antagonize an opioid analgesic administered just before, concurrently, or just after an injection. Therefore, patients receiving an opioid analgesic, general anesthetics, phenothiazines, or other tranquilizers, sedatives, hypnotics, or other CNS depressants including alcohol concomitantly with Nalbuphine may exhibit an additive effect. When such combined therapy is contemplated, the dose of one or both agents should be reduced. In addition to the relief of pain, the drug has been studied as a treatment for morphine induced pruritus itching. Pruritus is a common side effect of morphine or other pure MOR agonist opioid administration. Kjellberg et al. The authors state that nalbuphine is an effective anti-pruritic agent against morphine induced pruritus. The effect may be mediated via central nervous system mechanisms. Pan summarizes the evidence that activation at the pharmacological level of the KOR antagonizes various MOR-mediated actions in the brain. The author states that the neural mechanism for this potentially very general MOR-antagonizing function by the KOR may have broad applications in the treatment of central nervous system mediated diseases. Morphine induced pruritus syndrome may also be caused by release of histamine from mast cells in the skin Gunion et al. Paus et al. Levy et al. Nalbuphine did not produce either a wheal or flare response. Both strengths contain 0. One mL of each strength contains 0. This is particularly true for the side effects of nausea, sedation and cognitive symptoms Jovey et al. These side effects can in many instances be ameliorated or avoided at the time of drug initiation by titrating the drug from a tolerable starting dose up to the desired therapeutic dose. Respiratory depression is a potentially fatal side effect from the use of pure MOR agonists. Nalbuphine has limited ability to depress respiratory function Gal et al. Other possible, but rare side effects include speech difficulty, urinary urgency, blurred vision, flushing and warmth. A Cochrane Systematic Review by Schnabel et al. In case of overdose or adverse reaction, the immediate intravenous administration of naloxone Narcan is a specific antidote. Oxygen, intravenous fluids, vasopressors and other supportive measures should be used as indicated. It is structurally related to the widely used opioid antagonists naloxone and naltrexone , and to the potent opioid analgesic oxymorphone. Nalbuphine is said to be more morphine -like at lower doses. However at higher doses, it produces more sedation , drunkenness , dysphoria , and dissociation. Nalbuphine is a potent analgesic. Its analgesic potency is essentially equivalent to that of morphine on a milligram basis, which is based on relative potency studies using intramuscular administration Beaver et al. Oral administered nalbuphine is reported to be three times more potent than codeine Okun et al. Clinical trials studied single dose experimental oral immediate release nalbuphine tablets for analgesic efficacy over a four- to six-hour time period following administration. Schmidt et al. Nalbuphine was first synthesized in and was introduced for medical use in the United States in In the search for opioid analgesics with less abuse potential than pure MOR agonist opioids, a number of semisynthetic opioids were developed. These substances are referred to as mixed agonist—antagonists analgesics. Nalbuphine belongs to this group of substances. The mixed agonists-antagonists drug class exerts their analgesic actions by agonistic activity at the KOR. While all drugs in this class possess MOR antagonistic activity leading to less abuse potential, nalbuphine is the only approved drug in the mixed agonist-antagonist class listed in terms of its pharmacological actions and selectivities on opioid receptors as a MOR partial agonist or antagonist as well as a KOR agonist Gustein et al. Nubain was approved for marketing in the United States in and remains as the only opioid analgesic of this type marketed in the U. Endo Laboratories, Inc. After receiving a medical and scientific review and a scheduling recommendation from the Department of Health, Education and Welfare, forerunner to the Department of Health and Human Services , nalbuphine was removed from schedule II of the CSA in Presently, nalbuphine is not a controlled substance under the CSA. Nubain, the Astra USA brand name for injectable nalbuphine HCL, was discontinued from being marketed in in the United States for commercial reasons Federal Register ; however, other commercial suppliers now provide generic injection formulation nalbuphine for the market. Nalbuphine is marketed primarily under the brand names Nubain, Nalpain, and Nalbuphin. Unlike many other opioids, nalbuphine has a limited potential for euphoria , and in accordance, is rarely abused. From Wikipedia, the free encyclopedia. Not to be confused with Nalorphine. This article includes a list of references , but its sources remain unclear because it has insufficient inline citations. Please help to improve this article by introducing more precise citations. December Learn how and when to remove this template message. IUPAC name. Interactive image. Waldman 9 June Pain Management E-Book. Elsevier Health Sciences. Pediatric Anesthesia. Section Anesthesiology. Lab Anim NY. Smith; Marco Pappagallo 6 September Cambridge University Press. Journal of Analytical Toxicology. Drug Alcohol Depend. Journal of Medicinal Chemistry. Robin Analogue-based Drug Discovery. Malamed 23 June Life Sci. Non-medical and illicit use of psychoactive drugs. American Psychiatric Pub. Bruno; Rick Csiernik 26 April Canadian Scholars. Analgesics N02A , N02B. Meloxicam Piroxicam. Meclofenamic acid Mefenamic acid. Cannabidiol Cannabis Nabilone Nabiximols Tetrahydrocannabinol dronabinol. Carbamazepine Lacosamide Local anesthetics e. Opioid receptor modulators. Hidden categories: Articles lacking in-text citations from December All articles lacking in-text citations Template:drugs. Namespaces Article Talk. Views Read Edit View history. By using this site, you agree to the Terms of Use and Privacy Policy. Intravenous , intramuscular , subcutaneous. Liver glucuronidation \\\\\\\\\\\\[1\\\\\\\\\\\\] \\\\\\\\\\\\[2\\\\\\\\\\\\]. Glucuronide conjugates inactive , others \\\\\\\\\\\\[4\\\\\\\\\\\\] \\\\\\\\\\\\[1\\\\\\\\\\\\] \\\\\\\\\\\\[2\\\\\\\\\\\\].

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Налбуфин википедия

Налбуфин : инструкция по применению

Nalbuphine , sold under the brand names Nubain among others, is an opioid analgesic which is used in the treatment of pain. Side effects of nalbuphine include sedation , sweatiness , clamminess , nausea , vomiting , dizziness , vertigo , dry mouth , and headache. Nalbuphine was patented in and was introduced for medical use in the United States in Nalbuphine is indicated for the relief of moderate to severe pain. It can also be used as a supplement to balanced anesthesia, for preoperative and postoperative analgesia, and for obstetrical analgesia during labor and delivery. However, a Cochrane Systematic Review concluded that from the included studies, there was limited evidence to demonstrate that '0. Although nalbuphine possesses opioid antagonist activity, there is evidence that in nondependent patients it will not antagonize an opioid analgesic administered just before, concurrently, or just after an injection. Therefore, patients receiving an opioid analgesic, general anesthetics, phenothiazines, or other tranquilizers, sedatives, hypnotics, or other CNS depressants including alcohol concomitantly with Nalbuphine may exhibit an additive effect. When such combined therapy is contemplated, the dose of one or both agents should be reduced. In addition to the relief of pain, the drug has been studied as a treatment for morphine induced pruritus itching. Pruritus is a common side effect of morphine or other pure MOR agonist opioid administration. Kjellberg et al. The authors state that nalbuphine is an effective anti-pruritic agent against morphine induced pruritus. The effect may be mediated via central nervous system mechanisms. Pan summarizes the evidence that activation at the pharmacological level of the KOR antagonizes various MOR-mediated actions in the brain. The author states that the neural mechanism for this potentially very general MOR-antagonizing function by the KOR may have broad applications in the treatment of central nervous system mediated diseases. Morphine induced pruritus syndrome may also be caused by release of histamine from mast cells in the skin Gunion et al. Paus et al. Levy et al. Nalbuphine did not produce either a wheal or flare response. Both strengths contain 0. One mL of each strength contains 0. This is particularly true for the side effects of nausea, sedation and cognitive symptoms Jovey et al. These side effects can in many instances be ameliorated or avoided at the time of drug initiation by titrating the drug from a tolerable starting dose up to the desired therapeutic dose. Respiratory depression is a potentially fatal side effect from the use of pure MOR agonists. Nalbuphine has limited ability to depress respiratory function Gal et al. Other possible, but rare side effects include speech difficulty, urinary urgency, blurred vision, flushing and warmth. A Cochrane Systematic Review by Schnabel et al. In case of overdose or adverse reaction, the immediate intravenous administration of naloxone Narcan is a specific antidote. Oxygen, intravenous fluids, vasopressors and other supportive measures should be used as indicated. It is structurally related to the widely used opioid antagonists naloxone and naltrexone , and to the potent opioid analgesic oxymorphone. Nalbuphine is said to be more morphine -like at lower doses. However at higher doses, it produces more sedation , drunkenness , dysphoria , and dissociation. Nalbuphine is a potent analgesic. Its analgesic potency is essentially equivalent to that of morphine on a milligram basis, which is based on relative potency studies using intramuscular administration Beaver et al. Oral administered nalbuphine is reported to be three times more potent than codeine Okun et al. Clinical trials studied single dose experimental oral immediate release nalbuphine tablets for analgesic efficacy over a four- to six-hour time period following administration. Schmidt et al. Nalbuphine was first synthesized in and was introduced for medical use in the United States in In the search for opioid analgesics with less abuse potential than pure MOR agonist opioids, a number of semisynthetic opioids were developed. These substances are referred to as mixed agonist—antagonists analgesics. Nalbuphine belongs to this group of substances. The mixed agonists-antagonists drug class exerts their analgesic actions by agonistic activity at the KOR. While all drugs in this class possess MOR antagonistic activity leading to less abuse potential, nalbuphine is the only approved drug in the mixed agonist-antagonist class listed in terms of its pharmacological actions and selectivities on opioid receptors as a MOR partial agonist or antagonist as well as a KOR agonist Gustein et al. Nubain was approved for marketing in the United States in and remains as the only opioid analgesic of this type marketed in the U. Endo Laboratories, Inc. After receiving a medical and scientific review and a scheduling recommendation from the Department of Health, Education and Welfare, forerunner to the Department of Health and Human Services , nalbuphine was removed from schedule II of the CSA in Presently, nalbuphine is not a controlled substance under the CSA. Nubain, the Astra USA brand name for injectable nalbuphine HCL, was discontinued from being marketed in in the United States for commercial reasons Federal Register ; however, other commercial suppliers now provide generic injection formulation nalbuphine for the market. Nalbuphine is marketed primarily under the brand names Nubain, Nalpain, and Nalbuphin. Unlike many other opioids, nalbuphine has a limited potential for euphoria , and in accordance, is rarely abused. From Wikipedia, the free encyclopedia. Not to be confused with Nalorphine. This article includes a list of references , but its sources remain unclear because it has insufficient inline citations. Please help to improve this article by introducing more precise citations. December Learn how and when to remove this template message. IUPAC name. Interactive image. Waldman 9 June Pain Management E-Book. Elsevier Health Sciences. Pediatric Anesthesia. Section Anesthesiology. Lab Anim NY. Smith; Marco Pappagallo 6 September Cambridge University Press. Journal of Analytical Toxicology. Drug Alcohol Depend. Journal of Medicinal Chemistry. Robin Analogue-based Drug Discovery. Malamed 23 June Life Sci. Non-medical and illicit use of psychoactive drugs. American Psychiatric Pub. Bruno; Rick Csiernik 26 April Canadian Scholars. Analgesics N02A , N02B. Meloxicam Piroxicam. Meclofenamic acid Mefenamic acid. Cannabidiol Cannabis Nabilone Nabiximols Tetrahydrocannabinol dronabinol. Carbamazepine Lacosamide Local anesthetics e. Opioid receptor modulators. Hidden categories: Articles lacking in-text citations from December All articles lacking in-text citations Template:drugs. Namespaces Article Talk. Views Read Edit View history. By using this site, you agree to the Terms of Use and Privacy Policy. Intravenous , intramuscular , subcutaneous. Liver glucuronidation \\\\\\\\\\\\\\[1\\\\\\\\\\\\\\] \\\\\\\\\\\\\\[2\\\\\\\\\\\\\\]. Glucuronide conjugates inactive , others \\\\\\\\\\\\\\[4\\\\\\\\\\\\\\] \\\\\\\\\\\\\\[1\\\\\\\\\\\\\\] \\\\\\\\\\\\\\[2\\\\\\\\\\\\\\].

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