Drug intelligence / Profile preview

lofepramine

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Lofepramine is a tricyclic antidepressant (TCA) used primarily for the treatment of depression. It is structurally related to imipramine and is extensively metabolized to desipramine, which may contribute to its pharmacological effects[5][8]. Lofepramine acts mainly as a strong inhibitor of norepinephrine reuptake and as a moderate inhibitor of serotonin reuptake in the central nervous system[3][6][8]. It also exhibits weak-to-intermediate antagonism at muscarinic acetylcholine receptors, resulting in fewer anticholinergic side effects compared to some other TCAs[3][5]. Its therapeutic efficacy is considered comparable to other tricyclic antidepressants such as imipramine and amitriptyline. Lofepramine has been noted for a more favorable cardiac safety profile than many other TCAs and is licensed for use in the United Kingdom for unipolar depression[7][8].

Brand names
GamanilLomontTymelyt
02

Targets

mAChR (Muscarinic acetylcholine receptors)SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)

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