Mianserin

Abstract

Mianserin is a tetracyclic compound advocated for the treatment of depressive illness and depression associated with anxiety. It combines antidepressant activity with a sedative effect and has an EEG and clinical activity profile similar to that of amitriptyline. It has an overall efficacy comparable with amitriptyline and imipramine in depressive illness, but at dosages which have achieved a similar overall clinical improvement, mianserin causes significantly fewer anticholinergic side effects than amitriptyline or imipramine and also appears less likely than these drugs to cause serious cardiotoxicity on overdosage. Mianserin also has anti-anxiety activity, but its role in treating patients with anxiety associated with primary depression has still to be clarified. Mianserin appears to be well tolerated by the elderly and by patients with cardiovascular disease, including those recovering from a recent myocardial infarction, and does not appear to antagonise the action of adrenergic neurone blocking antihypertensive drugs or affect the anticoagulant action of phenprocoumon.

Three closely related dibenzazepine carboxylic acids: hydrogen-bonded aggregation in one, two and three dimensions

“…The dibenzo [b,e]azepine ring is an important pharmacophore in drug discovery and many of its derivatives exhibit a broad spectrum of biological activities (Van der Burg et al, 1970;Brogden et al, 1978;Nickolson & Wieringa, 1981;Berger et al, 1989;De Boer et al, 1996;Roeder et al, 1998;André s et al, 2002;Wikströ m et al, 2002). Consequently, a significant number of synthetic methods have been developed for the synthesis of new derivatives of this heterocyclic system (Moriconi & Maniscalco, 1972;Sasakura & Sugasawa, 1981;Stappers et al, 2002).…”

The Interaction of Heptakis (2,6-di-O-Methyl)-β-cyclodextrin with Mianserin Hydrochloride and Its Influence on the Drug Toxicity

“…They are supramolecules with a hydrophobic interior, which may include hydrophobic parts of the drug molecule and hydrophilic shells, consisting of primary and secondary hydroxyl groups that can interact with water molecules [13,14]. In pharmacological tests of the mianserin antidepressant effect [15], higher potency is found for the optical enantiomer (S)-(+)-mianserin. However, we chose the racemate for testing, since commercially available mianserin hydrochloride is a racemic mixture.…”

Quantum chemical study and isothermal titration calorimetry of β-cyclodextrin complexes with mianserin in aqueous solution

“…It blocks presynaptic receptors (α 2 -adrenoreceptors) responsible for the binding of serotonin and the mechanism of mianserin action allows for prolonged action of both hormones (noradrenaline and serotonin) improving the mood of a person suffering from depression. [4][5][6][7] In pharmacological tests of antidepressant activity 4 a higher potency is present for the (S)-(+)-mianserin optical enantiomer. A pharmacokinetic study with mianserin hydrochloride indicated that the maximum anticipated oral availability was calculated to be in the range of 34-49%.…”