naloxone

Ligand id: 1638

Name: naloxone

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Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 3
Hydrogen bond donors 2
Rotatable bonds 2
Topological polar surface area 70
Molecular weight 327.15
XLogP 0.61
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Used to reverse narcotic depression, including respiratory depression induced by opioids. Also indicated for the diagnosis of acute opioid overdose and as an adjunctive agent to increase blood pressure following septic shock.
Naloxone is sometimes combined in fixed-mixture brands with opioid analgesics as a method of deterring abuse of opioid medications. Naloxone blocks the euphoric effects of the opioid, making it less attractive to drug abusers. Examples of such combinations are Targiniq ER® which contains oxycodone hydrochloride and naloxone hydrochloride and Suboxone® and Zubsolv® which contain naloxone and buprenorphine. Targiniq ER® is used as a pain medication in specific patients, whereas Suboxone® and Zubsolv® are used to treat opiate dependence.
In September 2014 the US FDA approved Contrave® (bupropion and naloxone), a fixed-mixture medication, to be used in conjunction with reduced-calorie intake and physical activity, as a treatment for chronic weight management.
Mechanism Of Action and Pharmacodynamic Effects
The exact mechanism of action of naloxone is unknown, but its properties are believed to arise from its antagonism of opioid receptors.
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