- Overview
- Properties
- Genetics
- Related Genes
- Related Drugs
- Related Diseases
- Datasets
- Downloads/LinkOuts
Overview
| Generic Names: | EN 1530 Base; L-Naloxone; N-Allylnoroxymorphone; Nalossone [Dcit]; Naloxona [INN-Spanish]; Naloxone HCl; Naloxonum [INN-Latin] |
|---|---|
| Trade Names: | Nalone; Narcan; Narcanti; Narcon |
| PharmGKB Accession Id: | PA450586 |
Description
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors. PubChem (source: Drug Bank)
Indication
For the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids including natural and synthetic narcotics, propoxyphene, methadone and the narcotic-antagonist analgesics: nalbuphine, pentazocine and butorphanol. (source: Drug Bank)
ATC Therapeutic Category
- V03AB:Antidotes
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
While the mechanism of action of naloxone is not fully understood, the preponderance of evidence suggests that naloxone antagonizes the opioid effects by competing for the same receptor sites, especially the opioid mu receptor. Recently, naloxone has been shown to bind all three opioid receptors (mu, kappa and gamma) but the strongest binding is to the mu receptor. (source: Drug Bank)
Pharmacology
Naloxone is an opiate antagonist and prevents or reverses the effects of opioids including respiratory depression, sedation and hypotension. Also, it can reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine. Naloxone is an essentially pure narcotic antagonist, i.e., it does not possess the "agonistic" or morphine-like properties characteristic of other narcotic antagonists; naloxone does not produce respiratory depression, psychotomimetic effects or pupillary constriction. In the absence of narcotics or agonistic effects of other narcotic antagonists, it exhibits essentially no pharmacologic activity. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. (source: Drug Bank)
Absorption
Well absorbed following intramuscular injection. (source: Drug Bank)
Isomeric SMILES Code:
C=CCN1CC[C@]23c4c5ccc(c4O[C@H]2C(=O)CC[C@]3([C@H]1C5)O)O (source: Drug Bank)
Curated Annotations (
)
-
rs1799971
at chr6:154402490
in
OPRM1
Several studies found an enhanced cortisol response to naloxone among subjects with the Asp40 variant. A study in healthy individuals who were of European Americans or Asian ancestry found that participants with one or two Asp40 alleles had a significantly greater cortisol response to naloxone than Asn40 homozygotes, but the effect was limited to European Americans.- Variant Name:
- OPRM1: A118G; Asn40Asp
- Related Drugs:
- naloxone
- Evidence:
-
PMID:11751037
PMID:12627468
PMID:18004207
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
HTR1A |
|
Publications |
|
NR1I2 |
|
Publications |
|
|
OPRM1 |
|
Publications, Variants |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| CREB1 |
|
(source: Drug Bank) |
| ESR1 |
|
(source: Drug Bank) |
| OPRD1 |
|
(source: Drug Bank) |
| OPRM1 |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.