GAMANIL Film-coated tablet Ref.[49943] Active ingredients: Lofepramine

Source: Health Products Regulatory Authority (IE)  Revision Year: 2021  Publisher: Zentiva k.s., U kabelovny 130, 102 37 Prague 10, Czech Republic

5.1. Pharmacodynamic properties

Pharmacotherapeutic group: Antidepressant, non-selective monoamine reuptake inhibitor
ATC Code: N06AA07

Mechanism of action

Gamanil 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.

Pharmacodynamic effects

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.

5.2. Pharmacokinetic properties

Absorption

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.

Distribution

From the plasma it is distributed throughout the body notably to the brain, lungs, liver and kidney.

Biotransformation

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.

Elimination

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.

5.3. Preclinical safety data

Not applicable.

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