Active Ingredients

Maprotiline – Effect, Application & Risks

Maprotiline

Maprotiline is one of the antidepressants . The drug is used to treat depressive disorders .

What is maprotiline?

Maprotiline is a tetracyclic antidepressant (TCA). Antidepressants are drugs that are used to effectively treat depression. However, they can also be used for other mental illnesses such as panic disorders or chronic pain .

Tetracyclic antidepressants such as maprotiline are a further development of tricyclic antidepressants. In their chemical structure, for example, they have four carbon rings instead of three.

Maprotiline, also known as maprotilinum or maprotiline hydrochloride , has been used in Europe since the early 1970s. Psychiatry uses the drug to treat depression. In Germany it is marketed under the product names Maprolu® and Ludiomil®.

Pharmacological action

Maprotiline has the property of acting on the central nervous system (CNS). In doing so, it ensures the inhibition of norepinephrine reuptake from the synaptic cleft . The inhibition of the neurotransmitter serotonin , on the other hand, is hardly worth mentioning. In this way, an anxiolytic and drive-increasing effect is achieved.

In the initial stages of treatment, there is a weakening of adrenaline and histamine within the nervous system, resulting in an arousal-dampening and calming effect. After a few weeks of treatment, however, this effect is increasingly replaced by mood elevation and increased drive.

The anticholinergic effect of maprotiline can hardly be proven. It is considered to be more advantageous than tricyclic antidepressants, since the autonomic nervous system is less affected by undesirable effects.

A disadvantage of the maprotiline effect, however, is that the antidepressant can also bind to adrenoceptors, serotonin receptors and histamine receptors. This increases the likelihood of various undesirable side effects . However, they are weaker than tricyclic antidepressants.

Furthermore, maprotiline can act as a FIASMA. This is a “functional inhibitor of acidic phosphomyelinase”. Maprotiline is taken orally, intravenously or intramuscularly. The bioavailability of the active ingredient reaches up to 90 percent. Up to 88 percent of it is bound to plasma proteins in the blood . Maprotiline is metabolized in the liver . On average, its plasma half-life reaches 36 hours. The active substance is then broken down via the liver and kidneys .

Medical Application & Use

Maprotiline is given to treat depression, dysphoria, or anxiety disorders. The drug is used to counteract depressive moods and to relieve anxiety and agitation. Another area of ​​application for maprotiline is somatic or psychosomatic complaints associated with anxiety disorders.

Maprotiline is usually taken in the form of film-coated tablets with a little water. The usual daily dose is 1 to 3 tablets containing 25 to 75 milligrams of maprotiline hydrochloride. The daily dose can also be administered as a single dose in the evening hours.

Depending on how the patient tolerates maprotiline, the dosage increases after two weeks by another film-coated tablet per day until the patient is taking two to three tablets per day. The recommended maximum dose is six tablets a day. If the symptoms improve, the patient gradually reduces the dose to one or two tablets per day.

How long the treatment with maprotiline lasts varies and is decided individually by the doctor. It usually takes 4 to 6 weeks for the antidepressant to have a positive effect.

Risks & side effects

Some patients may experience side effects from the use of maprotiline. In most cases, these include dry mouth , dizziness , lightheadedness , tiredness , nausea , vomiting , hot flashes , headaches , urinary problems, constipation , weight gain , trouble sleeping , nightmares , blurred vision , anxiety , and aggressive behavior . Also disorders of sexual potencyand loss of libido are within the realm of possibility.

Some patients may experience major side effects, but these are very rare. These include cardiac conduction disorders , fluctuations in blood pressure , seizures , vasculitis , gynecomastia , manic or psychotic states, hallucinations , liver damage , disorders of blood formation or liver inflammation ( hepatitis ).

If the patient is hypersensitive to maprotiline or other tetracyclic or tricyclic antidepressants, the drug must not be administered. The same applies to severe kidney and liver dysfunction, mania or psychosis, acute drug or alcohol poisoning, a tendency to seizures, intestinal paralysis, glaucoma , constrictions within the gastrointestinal tract, an enlargement of the prostate , which is associated with urinary drainage disorders, as well as severe cardiac arrhythmia .

During pregnancy , the use of maprotiline must be administered only after a careful assessment between risk and benefit by the doctor. Damage to the unborn child by the active substance cannot be completely ruled out. There is also a possibility that maprotiline passes into breast milk during breastfeeding . This can also affect the baby’s health. Maprotiline is not suitable for children.

Taking maprotiline and MAO inhibitors at the same time is problematic. Since there is a risk of serious side effects, simultaneous use should be avoided. Interactions are also possible through parallel therapy with maprotiline and other tetra- or tricyclic antidepressants. In this way, the effects of the remedies can increase each other. The effects of maprotiline are increased by the administration of cimetidine , methylphenidate or neuroleptics . In addition, simultaneous treatment with neuroleptics increases the risk of seizures.

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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.