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Налоксон
- английское имяNaloxone
- CAS №465-65-6
- CBNumberCB5728727
- ФормулаC19H21NO4
- мольный вес327.37
- EINECS207-365-7
- номер MDLMFCD00242634
- файл Mol465-65-6.mol
химическое свойство
Температура плавления | 184° (Lewenstein), 177-178° (Sankyo Co.) |
альфа | D20 -194.5° (c = 0.93 in CHCl3) |
Температура кипения | 465.27°C (rough estimate) |
плотность | 1.2223 (rough estimate) |
показатель преломления | 1.5000 (estimate) |
Fp | 9℃ |
температура хранения | 2-8°C |
растворимость | Chloroform (Slightly, Heated, Sonicated), DMSO (Slightly), Methanol (Slightly), |
форма | Solid |
пка | pKa 7.94/7.82(H2O,t =20/37,I<0.01) (Uncertain) |
цвет | White to Off-White |
ИнЧИКей | UZHSEJADLWPNLE-GRGSLBFTSA-N |
Словарь онкологических терминов NCI | naloxone |
FDA UNII | 36B82AMQ7N |
Код УВД | A06AH04,V03AB15 |
Система регистрации веществ EPA | Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, (5.alpha.)- (465-65-6) |
Коды опасности | F,T |
Заявления о рисках | 11-23/24/25-39/23/24/25 |
Заявления о безопасности | 7-16-36/37-45 |
РИДАДР | UN1230 - class 3 - PG 2 - Methanol, solution |
WGK Германия | 3 |
кода HS | 2939190000 |
Банк данных об опасных веществах | 465-65-6(Hazardous Substances Data) |
Токсичность | An opiate antagonist devoid of agonist activity except for mild, specific effects at very high doses. Naloxone displays a high affinity for the μ-opioid receptor, a lesser affinity for the kopioid receptor and has some affinity for δ-opioid receptor subtypes. Naloxone produces a rapid and profound reversal of the effects of opioid administration (e.g., 1 mg, i.v., blocks the effects of 25 mg of heroin). Naloxone also antagonizes the analgesia induced by placebo, acupuncture, and stress, and in animals the hypotension due to hypovolemia or spinal cord injury. Naloxone has a short half-life (about 1 h in plasma) and is not administered orally because of rapid, “first-pass” metabolism. |
рисовальное письмо(GHS)
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рисовальное письмо(GHS)
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сигнальный язык
предупреждение
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вредная бумага
H302:Вредно при проглатывании.
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оператор предупредительных мер
P264:После работы тщательно вымыть кожу.
P270:При использовании продукции не курить, не пить, не принимать пищу.
P301+P312:ПРИ ПРОГЛАТЫВАНИИ: Обратиться за медицинской помощью при плохом самочувствии.
P501:Удалить содержимое/ контейнер на утвержденных станциях утилизации отходов.
Налоксон химические свойства, назначение, производство
Описание
It is worth mentioning that N-allylic substitution in a number of morphine derivatives, as a rule, leads to antagonistic properties. Naloxone is a few times stronger than nalorphine as an antagonist. It blocks opiate receptors. It eliminates central and peripheral action of opioids, including respiratory depression. Naloxone is used upon overdose of narcotic analgesics.Использование
Naloxone is a specific opioid antagonist. Narcotic antagonist.Определение
ChEBI: A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an all l group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.Биологические функции
Because of its fast onset (minutes), naloxone (Narcan) administered IV is used most frequently for the reversal of opioid overdose. However, it fails to block some side effects of the opioids that are mediated by the δ- receptor, such as hallucinations. The rapid offset of naloxone makes it necessary to administer the drug repeatedly until the opioid agonist has cleared the system to prevent relapse into overdose. The half-life of naloxone in plasma is 1 hour. It is rapidly metabolized via glucuronidation in the liver and cleared by the kidney. Naloxone given orally has a large first-pass effect, which reduces its potency significantly. Often an overshoot will follow the administration of naloxone for overdose. The heart rate and blood pressure of the patient may rise significantly. The overshoot is thought to be due to precipitation of acute withdrawal signs by naloxone. Given alone to nonaddicts, naloxone produces no pharmacological effects.Naloxone is approved for use in neonates to reverse respiratory depression induced by maternal opioid use. In addition, naloxone has been used to improve circulation in patients in shock, an effect related to blockade of endogenous opioids. Other experimental and less well documented uses for naloxone include reversal of coma in alcohol overdose, appetite suppression, and alleviation of dementia from schizophrenia. Side effects of naloxone are minor.
Общее описание
Naloxone (Narcan) is a pure antagonist at allopioid receptor subtypes. Structurally, it resembles oxymorphoneexcept that the methyl group on the nitrogen isreplaced by an allyl group. This minor structural change retains high binding affinity to the receptor, but no intrinsicactivity. It is used to reverse the respiratory depressant effectsof opioid overdoses.Naloxone is administered intravenously with an onset ofaction within 2 minutes. Because it is competing with theopioid for the receptor sites, the dose and frequency of administrationwill depend on the amount and type of narcoticbeing antagonized. Overdoses of long-acting opioids(methadone) may require multiple IV doses of naloxone orcontinuous infusions. Neonates born to opioid-exposedmothers may be given IV naloxone at birth to reverse the effectsof opiates.
Very few metabolism studies on naloxone have beenconducted, although the major metabolite found in the urineis naloxone-3-glucuronide.
Налоксон запасные части и сырье
сырьё
- (5alpha)-6,7,8,14-tetradehydro-4,5-epoxy-6-methoxy-17-methylmorphinan-3-ol
- Morphinan-6-one, 3-(acetyloxy)-4,5-epoxy-14-hydroxy-17-methyl-, (5α)-
- 6,11b-Ethano-7H-furo[2',3',4',5':4,5]phenanthro[9,8a-d]oxazol-11(11aH)-one, 2-(acetyloxy)-5,5a,9,10-tetrahydro-, (5aR,6R,8aS,11aR,11bS)-
- Morphinan-3,14-diol, 4,5-epoxy-6,6-dimethoxy-17-(2-propen-1-yl)-, (5α)-
- IDDUCSVQXOGMNE-GVVUEQADSA-N
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запасной предмет
Налоксон поставщик
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