Chemical formula: C₂₆H₂₇ClN₂O Molecular mass: 418.97 g/mol
Lofepramine is a tricyclic antidepressant. It exerts its therapeutic effect by blocking the uptake of noradrenaline by the nerve cell thus increasing the amine in the synaptic cleft and hence the effect on the receptors.
There is evidence to suggest that serotonin may also be involved. Other pharmacological effects are due to anti-cholinergic activity, but less sedation is observed than with other tricyclics.
Lofepramine is a tertiary amine, similar in structure to imipramine but with improved lipophilicity and lower base strength. It is readily absorbed when given orally.
From the plasma it is distributed throughout the body notably to the brain, lungs, liver and kidney.
It is metabolised in the liver by cleavage of the p-chlorophenacyl group from the lofepramine molecule leaving desmethylimipramine (DMI). The latter is pharmacologically active.
The p-chlorobenzoyl portion is mainly metabolised to p-chlorobenzoic acid which is then conjugated with glycine. The conjugate is excreted mostly in the Urine. DMI has been found excreted in the faeces. In a study of protein binding capability it has been found that lofepramine is up to 99% protein bound.
Not applicable.
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