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Psychotropic Use during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Maprotiline is a tetracyclic antidepressant. The frequency of congenital anomalies was not increased among 107 pregnancies exposed to maprotiline during the first trimester (McElhatton et al., 1996; see Table 10.3). The frequency of birth defects was not increased among experimental animals (Esaki et al., 1976; Hirooka et al., 1978).
Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Maprotiline is a tricyclic antidepressant acting as a highly selective norepinephrine reuptake inhibitor with very weak inhibitory effect on dopamine and 5-HT reuptake (Pinder et al. 1977b). It is metabolized extensively, with only 2% of the total dose being excreted unchanged in urine (Alkalay et al. 1980). Maprotiline is mainly metabolized by CYP2D6 (~83%) and 1A2 (~17%) to its major active metabolite desmethylmaprotiline (Figure 3.8) (Brachtendorf et al. 2002). Desmethylmaprotiline is further acetylated (Baumann et al. 1988). Formation of hydroxylated metabolites including 3-OH-maprotiline, 2-OH-maprotiline, and 2,3-dihydrodiol to a lesser extent accounts for most of the remaining fraction (Breyer-Pfaff et al. 1985). Secondary metabolic steps generate a number of other metabolites. Several clinical inhibition studies indicate the important role of CYP2D6 in the metabolism of maprotiline. In depressed patients, fluvoxamine inhibits maprotiline’s N-demethylation (Hartter et al. 1993). Risperidone also increases the plasma concentrations of maprotiline (Normann et al. 2002). In studies with therapy-resistant depressive patients treated with maprotiline, coadministration of moclobemide significantly increases maprotiline plasma levels (25%) (Konig et al. 1997). Moclobemide is a known inhibitor of CYP2D6, 1A2, and 2C19 (Gram et al. 1995).
Depression
Published in Ethan Russo, Handbook of Psychotropic Herbs, 2015
Harrer and colleagues compared LI 160 at 900 mg per day to 75 mg per day of maprotiline, a quadricyclic antidepressant, more popular in Germany than in the United States (Harrer, Hübner, and Podzu-weit, 1994). The study involved 102 patients meeting ICD-10 criteria of depression who were examined over four weeks. HAMD scores dropped 50 percent in both treatment arms, with similar changes in von Zerssen Depression Scale and CGI, such that no significant differences were ascertained between hypericum and maprotiline. However, hypericum was favored, according to patients’ characterizations. Of those calling themselves“very much improved,” hypericum-treated patients outpolled the maprotiline patients 23:16, while it was touted by those“no longer ill,” 22:12. Of maprotiline patients, 22 percent noted fatigue versus 4 percent for hypericum patients.
A systematic review of second line therapies in toxic seizures
Published in Clinical Toxicology, 2021
Meghan L. Fletcher, Preeyaporn Sarangarm, Jacob Nash, Susan C. Smolinske, Robert L. Alunday, Steven A. Seifert, Brandon J. Warrick
This case series from two inpatient intensive care units included 43 cases involving 41 patients (27 female and 14 male) aged 20–66 years with maprotiline overdose [9]. Co-ingestions included benzodiazepines (19), ethanol (13), tricyclic antidepressants (6) and others (4). Fifteen patients experienced seizures, the majority (14) classified as “typical grand mal convulsions”. The authors implied that all seizure patients received diazepam. Two of these patients received phenytoin as second-line therapy. Seven out of the 43 total overdose cases received physostigmine as a toxicological antidote and seizures occurred in six of the patients who received this antidote (five after administration). The authors described patient outcomes as a whole and thus did not report individual seizure patient (15) outcomes.
The pharmacological management of chronic lower back pain
Published in Expert Opinion on Pharmacotherapy, 2021
Filippo Migliorini, Nicola Maffulli, Jörg Eschweiler, Marcel Betsch, Giovanni Catalano, Arne Driessen, Markus Tingart, Alice Baroncini
TCAs have been employed in the management of chronic LBP thanks to various actions which produce an analgesic effect: TCAs interfere with serotonin reuptake and serotonin binding to receptors (serotoninergic system), interact with α2-adrenoreceptors (noradrenergic system), modify the density of opioid receptors, and increase opioid levels in the opioidergic system of the brain [37]. Furthermore, TCAs bind N-methyl-D-aspartate (NMDA) and amino-3-hydroxy-5-methyl-4-isoxazoleproprionic acid (AMPA) glutamate receptors, activate A1 receptors to inhibit peripheral adenosine uptake, and block sodium channels [37]. According to the finding of the present study, which results from five articles trialing nortryptiline, maprotiline, imipramine, and amytriptiline [38–42], TCAs were not effective as a single therapy in the management of chronic LBP. This finding is coherent with current guidelines recommending the use of these compounds only as co-therapy [36], and with studies observing that TCAs did not score better than placebo in the treatment of chronic LBP [43]. Three studies reported information regarding the rate of AE: up to 90% of patients reported at least one AE during a trial with maprotiline, with the most frequent AE being dry mouth, insomnia, and sedation [38]. Schliessbach et al. observed nausea and dizziness occurring at low rate after using imipramine [41], while 12% of patients withdrew from an amitryptiline trial following AE [42].
Effect of Imipramine on radiosensitivity of Prostate Cancer: An In Vitro Study
Published in Cancer Investigation, 2019
Songul Barlaz Us, Fatma Sogut, Metin Yildirim, Derya Yetkin, Serap Yalin, Sakir Necat Yilmaz, Ulku Comelekoglu
In this study, to understand the cytotoxic effect of the IMI, RAD and combination of IMI and RAD, we measured cell proliferation, apoptosis, cell cycle parameters, EAG1 channel currents and oxidative stress in all groups. In the 72th h, cell proliferation in the IMI group was reduced 7.7 fold with compared to RAD group and was reduced 1.32 fold compared to IMI plus RAD group. According to our results, the inhibitor effect of RAD and IMI plus RAD on cell proliferation was weaker than effect of IMI administed alone. Previous studies suggested that IMI has antiproliferative effects for some cancer cell lines. Biber et al. investigated seven tricyclic (IMI, clomipramine, amitriptyline, opipramol, desipramine, protriptyline, nortriptyline) and two tetracyclic (maprotiline, mianserin) antidepressants for their effects on the viability of the U266 multiple myeloma cell line. They found that, except mianserin, all tested tricyclic antidepressant and maprotiline showed significant inhibitory effects on cell growth (24). Jahchan et al. treated the small cell lung cancer lines with IMI, clomipramine, promethazine and bepridil, significantly inhibited the growth of mouse and human small cell lung cancer but this effect was not seen using tranylcypromine and pargyline (35). Our findings regarding the antiproliferative effect of IMI are consistent with previous studies.