Inxight Drugs

Search results for "LiverTox|Substance abuse agent|Opiate addiction|Opiate antagonist" in comments (approximate match)

Showing 1 - 3 of 3 results

NALMEFENE

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TOV02TDP9I

Status:

US Approved Rx (2022)

First approved in 1995

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Nalmefene is the first medication approved for alcoholism with the primary goal of reducing alcohol intake in an as needed approach. Nalmefene received a marketing authorization valid throughout the European Union on February 25, 2013 and is under de...

NALTREXONE

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5S6W795CQM

Status:

US Approved Rx (2014)

First approved in 1984

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Naltrexone is marketed as its hydrochloride salt, naltrexone hydrochloride, under the trade names Revia and Depade. A once-monthly extended-release injectable formulation is marketed under the trade name Vivitrol. VIVITROL is indicated for the treatm...

NALOXONE

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36B82AMQ7N

Status:

US Approved Rx (2017)

First approved in 1971

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Naloxone, sold under the brand name Narcan among others, is a medication used to block the effects of opioids, especially in overdose. Naloxone has an extremely high affinity for μ-opioid receptors in the central nervous system (CNS). Naloxone is a μ...

-opioid receptor (MOR) inverse agonist, and its rapid blockade of those receptors often produces rapid onset of withdrawal symptoms. Naloxone also has an antagonist action, though with a lower affinity, at κ- (KOR) and δ-opioid receptors (DOR). If administered in the absence of concomitant opioid use, no functional pharmacological activity occurs (except the inability for the body to combat pain naturally). In contrast to direct opiate agonists, which elicit opiate withdrawal symptoms when discontinued in opiate-tolerant people, no evidence indicates the development of tolerance or dependence on naloxone. The mechanism of action is not completely understood, but studies suggest it functions to produce withdrawal symptoms by competing for opiate receptor sites within the CNS (a competitive antagonist, not a direct agonist), thereby preventing the action of both endogenous and xenobiotic opiates on these receptors without directly producing any effects itself. When administered parenterally (e.g. intravenously or by injection), as is most common, naloxone has a rapid distribution throughout the body. The mean serum half-life has been shown to range from 30 to 81 minutes, shorter than the average half-life of some opiates, necessitating repeat dosing if opioid receptors must be stopped from triggering for an extended period. Naloxone is primarily metabolized by the liver. Its major metabolite is naloxone-3-glucuronide, which is excreted in the urine. Naloxone is useful both in acute opioid overdose and in reducing respiratory or mental depression due to opioids. Whether it is useful in those in cardiac arrest due to an opioid overdose is unclear. Naloxone is poorly absorbed when taken by mouth, so it is commonly combined with a number of oral opioid preparations, including buprenorphine and pentazocine, so that when taken orally, just the opioid has an effect, but if misused by injecting, the naloxone blocks the effect of the opioid. In a meta-analysis of people with shock, including septic, cardiogenic, hemorrhagic, or spinal shock, those who received naloxone had improved blood flow. Naloxone is also experimentally used in the treatment for congenital insensitivity to pain with anhidrosis, an extremely rare disorder (one in 125 million) that renders one unable to feel pain or differentiate temperatures. Naloxone can also be used as an antidote in overdose of clonidine, a medication that lowers blood pressure.

Development Status

Primary Target

Highest Phase

Approval Year

Condition

Treatment Modality

CNS Activity

Originator

Substance Class

Code System

ATC Level 1

ATC Level 2

ATC Level 3

ATC Level 4

Substance Form

Search results for "LiverTox|Substance abuse agent|Opiate addiction|Opiate antagonist" in comments (approximate match)

NALMEFENE

TOV02TDP9I

NALTREXONE

5S6W795CQM

NALOXONE

36B82AMQ7N