China
Africa
Explore chapters and articles related to this topic
Adrenergic Agonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Tranylcypromine resembles dextroamphetamine, a weak MAO inhibitor. It is absorbed readily after an oral dose and is metabolized extensively. Both the in vivo and in vitro experiments reveal tranylcypromine as one potent MAO inhibitor. It shows a long duration of activity (Britain, 2008; Katzung et al., 2014).
Common/useful drugs
Published in Jonathan P Rogers, Cheryl CY Leung, Timothy RJ Nicholson, Pocket Prescriber Psychiatry, 2019
Jonathan P Rogers, Cheryl CY Leung, Timothy RJ Nicholson
Interactions:↓P450 (CYP2A6); ☠ ↑risk of severe toxic reaction with serotonergics, dopaminergics and noradrenergics: SSRIs, SNRIs, NARIs, TCAs (and related drugs), other MAOIs (inc for Parkinson's), carbamazepine, linezolid, triptans, pethidine, tramadol. ☠Do not start tranylcypromine until these drugs have been stopped and they have cleared: 5 wk for fluoxetine, 3 wk for clomipramine/imipramine, at least 7–14 days for other drugs.Wait 2 wk after stopping tranylcypromine before starting any of these medicines. ↑risk of hypertensive crisis with sympathomimetics, dopamine agonists, CNS stimulants, buspirone. ↑fx of CNS depressants, antimuscarinics, antidiabetics, antihypertensives.
Molecular Aspects of the Activity and Inhibition of the FAD-Containing Monoamine Oxidases
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Tranylcypromine (TCP) inactivation of MAO has been studied in depth using a variety of cyclopropylamine derivatives. TCP itself modifies the flavin at the C4a position (Fig. 10.4) but N-cyclo-α-methylbenzylamine modifies a cysteine. Chemical and mechanistic studies of the inactivation support a radical mechanism in which one electron passes from the substrate amino group to the oxidized flavin to give the amine radical cation and the flavosemiquinone, followed by opening of the cyclopropyl ring and adduct formation (Silverman, 1995). Where adduct formation does not occur, further oxidation gives the iminium ion which can either leave the active site or react with nearby cysteines. Reversible inhibition by TCP is weak at around 100 μM for both MAO A and B (Table 10.5) (Bonivento et al., 2010; Malcomson et al., 2015). Inactivation with low partition ratios in both forms, is marginally better in MAO B (kinact/Kinact is 0.2 compared to 0.1 min−1 · μM−1 in MAO A). Interestingly, in MAO B the covalently bound TCP stabilizes the entrance cavity residues to favour binding of 2-BFI, an imidazoline site ligand (Bonivento et al., 2010; McDonald et al., 2010). The clinical pharmacology for tranylcypromine use in depression has recently been reviewed in a meta-analysis which found that, when administered with dietary restriction of tyramine, it is a safe and effective antidepressant (Ricken et al., 2017).
Review and meta-analysis of add-on tranylcypromine with antipsychotic drugs for the treatment of schizophrenia with predominant negative symptoms: a restoration of evidence
Published in Current Medical Research and Opinion, 2021
Tranylcypromine (TCP) is an irreversible and non-selective MAO-A/B inhibitor prescribed mainly in treatment resistant depression. Increased levels of serotonin, norepinephrine, dopamine, and trace amines (e.g. phenylethylamine) in brain resulting from MAO inhibition, as well as norepinephrine reuptake inhibition at doses higher than 40 mg/day are considered as a unique combination of two primary pharmacological mechanisms10,11. The therapeutic limitation to a third-line antidepressant treatment comes from MAO inhibition in liver and gut. Patients suffer a relative tyramine incompatibility and risk of hypertensive crisis (“cheese reaction”) when eating tyramine rich food. A mandatory tyramine restricted diet is therefore applied. Cases of hypertensive crisis in TCP-treatment were reported decades ago before the introduction of the diet or, more recently, after neglect of dietary restrictions12,13. On the other hand, it was discussed that modern food has an improved quality with lower tyramine content14–16. Some authors have criticized current practice where MAOIs are prescribed only after 10 or more failed antidepressant trials17.
Marine natural products with monoamine oxidase (MAO) inhibitory activity
Published in Pharmaceutical Biology, 2020
Ahreum Hong, Le Cam Tu, Inho Yang, Kyung-Min Lim, Sang-Jip Nam
There are several classes of MAOI drugs on the market based on reversibility and selectivity (Shulman et al. 2013; Entzeroth and Ratty 2017). Reversibility means the way of the inhibitor binding into the enzyme whether covalently or non-covalently. Selectivity is a preference for one of the MAO subtypes. Non-selective and irreversible MAOI such as isocarboxazid, phenelzine and tranylcypromine were approved to treat depression in the US (Shulman et al. 2013). Selective MAO-A inhibitors with reversibility such as brofaromin and moclobemide were employed to treat social anxiety disorder (Entzeroth and Ratty 2017). However, the results were contradictory that these were not approved in the US. Irreversible MAO-B inhibitors, selegiline and rasagiline, were used to treat the symptoms of Parkinson's disease (Dezsi and Vecsei 2017). At present, the development of reversible, specific and safe MAOIs is required.
Pharmacotherapy and nutritional supplements for seasonal affective disorders: a systematic review
Published in Expert Opinion on Pharmacotherapy, 2018
Olivia Cools, Kaat Hebbrecht, Violette Coppens, Laurence Roosens, Andy De Witte, Manuel Morrens, Hugo Neels, Bernard Sabbe
With regard to monoamine-oxidase (MAO) inhibitors, moclobemide, a MAO-A inhibitor, showed a similar effect on mood as fluoxetine’s, although it is found to be comparable to placebo in another DB-RCT [40,47]. Tranylcypromine, a nonselective MAO inhibitor, resulted in significant improvement in 91% of the subjects (n = 14) in an open-label study. However, we question the reliability of these results as, on the one hand, the Carroll Rating Scale for Depression (CRS) was used; on the other, the study design was aimed at including only the least depressive score of the full five test weeks in the final data processing [48].