lofepramine

Ligand id: 7551

Name: lofepramine

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Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 3
Hydrogen bond donors 0
Rotatable bonds 7
Topological polar surface area 23.55
Molecular weight 418.18
XLogP 7.1
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Used to treat major depressive disorder. However, there is no information regarding approval for clinical use of this drug on the US FDA or European Medicines Agency (EMA) websites. Individual national approval agencies may have granted marketing authorisation. For example, in 2002 the UK approved this drug for the treatment of symptoms of depressive illness and although some brands have been discontinued, the generic drug is still in use.
Mechanism Of Action and Pharmacodynamic Effects
Lofepramine acts as a norepinephrine and serotonin reuptake inhibitor [2], with little anticholinergic activity at muscarinic receptors [1]. Lofepramine is extensively metabolized to the active metabolite, desipramine, which also acts as a norepinephrine reuptake inhibitor (with low efficacy serotonin transporter inhibition).
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