Stereochemistry | ABSOLUTE |
Molecular Formula | C21H25NO3.ClH.2H2O |
Molecular Weight | 411.92 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.O.Cl.[H][C@@]12OC3=C4C(C[C@H]5N(CC6CC6)CC[C@@]14[C@@]5(O)CCC2=C)=CC=C3O
InChI
InChIKey=XOBQQQVDLSMXCE-JVRGSUDVSA-N
InChI=1S/C21H25NO3.ClH.2H2O/c1-12-6-7-21(24)16-10-14-4-5-15(23)18-17(14)20(21,19(12)25-18)8-9-22(16)11-13-2-3-13;;;/h4-5,13,16,19,23-24H,1-3,6-11H2;1H;2*1H2/t16-,19+,20+,21-;;;/m1.../s1
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | H2O |
Molecular Weight | 18.0153 |
Charge | 0 |
Count |
MOL RATIO
2 MOL RATIO (average) |
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C21H25NO3 |
Molecular Weight | 339.4281 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
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 development
in Asia. Nalmefene is an opioid system modulator with a
distinct μ, δ, and κ receptor profile. In vitro studies have demonstrated
that Nalmefene is a selective opioid receptor ligand
with antagonist activity at the μ and δ receptors and partial
agonist activity at the κ receptor. In vivo studies have demonstrated
that nalmefene reduces alcohol consumption, possibly
by modulating cortico-mesolimbic functions. In the US, immediate-release injectable nalmefene was approved in 1995 as an antidote for opioid overdose. It was sold under the trade name Revex. The product was discontinued by its manufacturer around 2008. Currently Nalmefene is sold under the trade name Selincro. Selincro is indicated for the reduction of alcohol consumption in adult patients with alcohol dependence who have a high drinking-risk level, without physical withdrawal symptoms and who do not require immediate detoxification.
CNS Activity
Originator
Approval Year
AUC
T1/2
Doses
AEs
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Tox targets
Sourcing
PubMed
Patents
Sample Use Guides
How much to take
- The recommended dose is one tablet on days when you think there is a risk you will drink alcohol
- The maximum dose is one tablet per day.
How and when to take
- You should take the tablet 1-2 hours before you start drinking alcohol.
- Swallow the tablet whole, do not crush or divide the tablet.
- You can take Selincro (Nalmefene) with or without food.
Each film-coated tablet contains 18.06 mg nalmefene (as hydrochloride dihydrate).
Route of Administration:
Oral