Maprotiline
IUPAC: N-methyl- 9 ,10- ethanoanthracene -9 ( 10H) - propanamine
N06AA21
- 93 ° C ( maprotiline )
- 230-232 ° C ( maprotiline hydrochloride)
Attention
760 mg · kg -1 ( LD50, rat, oral)
Template: Infobox chemical / molecular formula search available
Maprotiline is a drug from the group of tetracyclic antidepressants, which is used in psychiatry for the treatment of depression.
Pharmacological properties
Maprotiline shows a strong reuptake inhibition of norepinephrine from the synaptic cleft, but no appreciable of serotonin. In addition, it blocks
- Strong histamine H1
- Moderate serotonin 5 -HT2A
- Weak α1 -adrenoceptors
- And very weak muscarinic M1 acetylcholine receptors.
The barely detectable anticholinergic activity provides an advantage over tricyclic antidepressants because it leads to less adverse effects on the autonomic nervous system. Maprotiline also acts as FIASMA ( functional inhibitors of acid sphingomyelinase ).
Indications
Maprotiline is approved for the treatment of depressive disorders.
Contraindications
Maprotiline may not be used in previously damaged heart ( conduction abnormalities), increased tendency to convulsions and in children and adolescents. After they had been MAOI treatment, a safety interval of at least 2 weeks must be maintained.
Use in pregnancy and lactation
There are insufficient Experience in the use of maprotiline in man before during pregnancy. The safety of use during pregnancy has not been established. Isolated cases that suggest a possible link between maprotiline and adverse effects on the human fetus have been reported. The use of maprotiline during pregnancy should be avoided unless the benefits of treatment outweigh the risks to the fetus. Since in newborns take their mothers to birth maprotiline, can potentially lead to symptoms such as dyspnoea, lethargy, irritability, tachycardia, hypotension, convulsions, tremor and hypothermia during the first hours or days, should - if it allows the clinical condition - be considered, maprotiline discontinued at least 7 weeks before the expected date of delivery.
Side effects
Among the common adverse effects of maprotiline
- Fatigue, drowsiness and dizziness
- Dry mouth, nausea and vomiting
- Accommodation disturbances, headache, hot flashes
- Constipation, urinary retention, weight gain
- Restlessness, agitation, insomnia and nightmares
- Anxiety, aggression
- Libido and impotence.
Rare but sometimes dangerous side effects of maprotiline are
- Fluctuations in blood pressure, conduction disturbances of the heart with ECG changes
- Pharmakogenes delirium, hallucinations and triggering manic or psychotic conditions
- Syncope, seizures, dyskinesias
- Alveolitis, vasculitis
- Drug skin and photosensitivity
- SIADH, galactorrhoea, gynaecomastia
- Disorder of hematopoiesis ( thrombocytopenia, agranulocytosis ), liver damage, and hepatitis.
Dosage forms, dosage
Maprotiline is available as a tablet for oral administration and as an injection solution. The active ingredient maprotiline hydrochloride in the tablets, while maprotiline mesilate, the salt of the methanesulfonic acid, is contained in the solutions for injection.
In order to avoid unpleasant side effects that increasing the dose should be einschleichend started with 3 × 25 mg and max. be increased: 150 mg ( 225 mg stationary). Discontinuation of therapy should be done tapered off over 4-6 weeks.
Trade names
Ludiomil (D, A, CH), Maprolu ( D) as well as a generic (D)