Maprotiline belongs to the group of antidepressants. The drug is used for the treatment of depressive disorders.
What is maprotiline?
Maprotiline is one of the antidepressants. The drug is used for the therapy of depressive disorders. Maprotiline is a tetracyclic antidepressant (TCA). Antidepressants are drugs that can be used to treat depression effectively. However, they can also be used to treat other mental illnesses such as panic disorders or chronic pain. Tetracyclic antidepressants such as maprotiline are a further development of tricyclic antidepressants. Thus, within their chemical structure, they have four carbon rings instead of three. Maprotiline, which is also called maprotilinum or maprotiline hydrochloride, has been used in Europe since the early 1970s. Psychiatry uses the drug to treat depression. In Germany, it is sold under the preparation names Maprolu and Ludiomil.
Pharmacological action
Maprotiline has the property of acting on the central nervous system (CNS). In doing so, it provides inhibition of norepinephrine reuptake from the synaptic cleft. In contrast, the inhibition of the neurotransmitter serotonin is hardly worth mentioning. In this way, an anxiety-relieving and drive-increasing effect is achieved. In the initial stage of treatment, there is an attenuation of adrenaline and histamine within the nervous system, which results in an excitement-dampening and calming effect. However, after a few weeks of treatment, this effect is increasingly replaced by mood elevation and increased drive. The anticholinergic effect of maprotiline can hardly be demonstrated. It is considered more advantageous over tricyclic antidepressants because the autonomic nervous system is less affected by adverse effects. However, a disadvantage of maprotiline action is that the antidepressant can also bind to adrenoreceptors, serotonin receptors, and histamine receptors. This increases the likelihood of various adverse side effects. However, compared with tricyclic antidepressants, they are weaker. Furthermore, maprotiline may act as a FIASMA. This is a “functional inhibitor of acid phosphomyelinase”. Maprotiline is taken orally, intravenously or intramuscularly. The bioavailability of the active substance reaches up to 90 percent. In the blood, it is present bound to plasma proteins up to 88 percent. Maprotiline is metabolized by the liver. On average, its plasma half-life reaches 36 hours. Subsequently, the drug is broken down by the liver and kidneys.
Medical use and application
Maprotiline is administered to treat depression, dysphoria, or anxiety disorders. In this context, the drug is used to counteract depressive moods and relieve anxiety and states of 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 is increased by one additional film-coated tablet per day after two weeks until the patient is taking two to three tablets daily. The maximum recommended 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 treatment with maprotiline lasts varies and is decided individually by the doctor. It usually takes 4 to 6 weeks before the positive effect of the antidepressant sets in.
Risks and side effects
The use of maprotiline may result in side effects in some patients. In most cases, these include dry mouth, dizziness, lightheadedness, fatigue, nausea, vomiting, hot flashes, headache, problems urinating, constipation, weight gain, sleep disturbances, nightmares, vision problems, anxiety, and aggressive behavior. Disorders of sexual potency and loss of libido are also in the range 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, hematopoiesis disorders, or hepatitis. If the patient is hypersensitive to maprotiline or other tetracyclic or tricyclic antidepressants, the drug must not be administered. The same applies in cases of severe renal and hepatic dysfunction, mania or psychosis, acute drug or alcohol intoxication, a tendency to seizures, intestinal paralysis, glaucoma, narrowing within the gastrointestinal tract, enlargement of the prostate associated with urinary dysfunction, and severe cardiac arrhythmias. During pregnancy, the use of maprotiline should be administered only after a careful review between risk and benefit by the physician. Thus, damage to the unborn child by the active substance cannot be completely ruled out. There is also the possibility that maprotiline passes into breast milk during breastfeeding. This can also affect the health of the baby. Maprotiline is not suitable for children. Simultaneous use of maprotiline and MAO inhibitors is problematic. Since there is a risk of severe side effects, concomitant use should be avoided. Interactions are also possible with parallel therapy of maprotiline and other tetra- or tricyclic antidepressants. Thus, the effects of the agents may increase each other. The effects of maprotiline are enhanced by the administration of cimetidine, methylphenidate or neuroleptics. In addition, concurrent treatment with neuroleptics increases the risk of seizures.
