Maprotiline (sold as Deprilept®, Ludiomil®, Psymion®) is a tetracyclic antidepressant. It is a stong norepinephrine reuptake inhibitor with only weak effects on serotonin and dopamine reuptake.

It exerts blocking effects at the following postsynaptic receptors:

Strong : alpha₁
Moderate : 5-HT₂, muscarinic, H₁, D₂
Weak : alpha₂
Extremely weak : 5-HT₁

The pharmacologic profile of Maprotiline explains its antidepressant, sedative, anxiolytic, sympatholytic, and anticholinergic activities. Additionally, it shows a strong antagonism against Reserpine-induced effects in animal studies, as the other 'cassical' antidepressants do. Although Maprotiline behaves in most regards as a 'first generation antidepressant' it is commonly referred to as 'second generation antidepressant'.

Sedation has a fast onset (the same day), while remission of the depression itself is noted usually after a latent period of 1 to 4 weeks.

Maprotiline does not brighten up the mood in nondepressed persons.

History

Maprotiline was developed and has been marketed by the Swiss manufacturer Geigy (now Novartis) since the early 1980's under the brand name Ludiomil®. Generics are widely available.

Indications

Treatment of depressions of all forms and severities (endogenous, psychotic, involutional, and neurotic)
Treatment of the depressive phase in bipolar depression
For the symptomatic relief of anxiety, tension or insomnia

N.B. The use of Maprotiline in the treatment of Enuresia in pediatric patients has so far not been systemetically explored and its use can therefore not be recommended.

Contraindications

Absolute

Hypersensitivity to Maprotiline or to other tri-/tetracyclic antidepressants
Hypertrophy of the prostate gland with urine hesitancy
Closed Angle Glaucoma

Special caution needed

Concomitant treatment with a MAO-Inhibitor
Serious impairment of liver and kidney function
Epilepsy and other conditions that lower the seizure threshold (active brain tumors, alcohol withdrawal, other medications)
Serious cardiovascular conditions (arrhythmias, heart insufficience, state after myocardial infarction etc.)
Treatment of patients under age 18

Pregnancy and nursing

If you are pregnant or thinking of becoming pregnant, before taking this medicine talk to your doctor about the benefits versus the risks to your pregnancy. Animal studies showed delayed bone development. Use this medicine only if it is clearly needed.

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