Naloxone

Naloxone 속성

Naloxone MSDS

(5alpha)-3,14-Dihydroxy-17-prop-2-en-1-yl-4,5-epoxymorphinan-6-one

Naloxone C화학적 특성, 용도, 생산

개요

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.

용도

Naloxone is a specific opioid antagonist. Narcotic antagonist.

정의

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that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an all l group.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.

Biological Functions

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.

일반 설명

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.

Naloxone 준비 용품 및 원자재

원자재

준비 용품

Naloxone 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21689	55
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49391	58
Shaanxi Dideu Medichem Co. Ltd	+86-029-89586680 +86-18192503167	1026@dideu.com	China	9177	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	28812	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10523	58
LEAP CHEM CO., LTD.	+86-852-30606658	market18@leapchem.com	China	24738	58
Shanghai Acmec Biochemical Technology Co., Ltd.	+undefined18621343501	product@acmec-e.com	China	33349	58
Aladdin Scientific	+1-833-552-7181	sales@aladdinsci.com	United States	57511	58
Chemwill Asia Co.,Ltd.	86-21-51086038	chemwill_asia@126.com	CHINA	23931	58

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