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It exerts blocking effects at the following postsynaptic receptors:
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 do the other 'classical' antidepressants. 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 one to four weeks.
Maprotiline does not brighten up the mood in nondepressed persons.
Additional recommended knowledge
Maprotiline was developed and has been marketed by the Swiss manufacturer Geigy (now Novartis) since the early 1980s under the brand name Ludiomil®. Generics are widely available.
N.B. The use of maprotiline in the treatment of enuresis in pediatric patients has so far not been systematically explored and its use can therefore not be recommended.
Special caution needed
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.
Maprotiline should not be given to nursing mothers. If you have any questions, ask your doctor or pharmacist.
The side-effect profile is comparable to other tri-/tetracyclic antidepressants. Most often seen are:
Other uncommon side effects may be seen. Consult your doctor, if these are more than mild.
Maprotiline causes a strong initial sedation (first 2 to 3 weeks of therapy) and is therefore indicated to treat agitated patients or those with suicidal risks. It causes anticholinergic side effects with a lower incidence than Amitritypline. Originally, the manufacturer claimed that Maprotiline is better tolerated than other tri-/tetrcyclic drugs. This is not the case because seizures, leukopenia and skin reactions occur more often with Maprotiline than with comparable drugs like Amitriptyline.
Necessary examinations during therapy
All patients should have frequent blood pressure checks and periodic white blood cell counts. Risk patients need also regular EKG and EEG monitoring as well.
Patients with suicidal thoughts, or those with previous suicidal attempts, should be monitored closely under treatment with Maprotiline. Perhaps, the decision is made to hospitalize high risk patients until remission or to prescribe an additional sedating drug like a benzodiazepine or Chlorprothixene for 2-4 weeks of initial treatment with Maprotiline (until significant remission). At least, the smallest amount of Maprotiline should be prescribed at one time to minimize the risk of deliberate overdose.
Generally, many antidepressants (SSRIs, other tricyclic drugs) have been shown to cause a significant higher rate of suicidal thoughts and suicidal attempts in patients under 18 yrs. of age compared to placebo. It is not known if Maprotiline shares this risk. If Maprotiline treatment is considered essentially in these patient group, all persons so-treated should be monitored closely for signs of suicidal risk.
Drug abuse and dependence
Maprotiline has no known potential for abuse and psychological dependence.
Withdrawal symptoms frequently seen when treatment with Maprotiline is stopped abruptly (agitation, anxiety, insomnia, sometimes activation of mania or rebound depression) are not indicative of addiction and can be avoided by reducing the daily dose of Maprotiline gradually by approximately 25% each week. If treatment has to be stopped at once due to medical reasons, the use of a benzodiazepine (e.g. Lorazepam, Clonazepam, or Alprazolam) for a maximum of 4 weeks as needed will usually suppress withdrawal symptoms.
Maprotiline may worsen psychotic conditions like schizophrenia and should be given with caution. The antipsychotic treatment should be continued.
Bipolar patients during acute manic phase should not be treated.
Maprotiline has a wide range of possible interactions. Some are typical for tri-/tetracyclic antidepressants, others are caused by specific metabolic effects (e.g. high plasma-protein-binding) of Maprotiline:
Increased drug actions:
Decreased drug actions:
Other types of interaction:
If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US national poison hotline at 1-800-222-1222.
Canadian residents should call their local poison control center directly. Symptoms of overdose may include flushing, fast or irregular heartbeat, dry mouth, drowsiness, confusion, agitation, enlarged pupils, seizures, and loss of consciousness.
Drugs commonly used to treat overdose are Physostigmine (N.B. increased risk of seizures in Physostigmine treated patients) to counteract central and peripher anticholinergic effects and Diazepam (cautiously, may deepen central depression!) against convulsion. Symptomatic measures are stabilization of blood pressure and correction of water- and electrolyt-deficits. Lidocaine can be given intravenously in cautious doses against cardial arrhythmias. The patient should be treated and monitored in an intensive care unit for several days.
Due to milder anticholinergic and cardiotoxic effects of Maprotiline the acute lethal dose may be higher compared with other classical antidepressants (e.g. Amitriptyline, Doxepin). Maprotiline is definitely more toxic than the other tetracyclic drugs Mianserin and Mirtazapine.
|This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Maprotiline". A list of authors is available in Wikipedia.