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Antidepressant agents tranylcypromine

MAOI agents was synthesized and tested for antidepressant properties. Three MAOI agents are approved in the United States for use in major depression isocarboxazid (Marplan), phenelzine Nardil), and tranylcypromine (Parnate). [Pg.392]

Isocarboxazid, phenelzine, and tranylcypromine are irreversible nonselective inhibitors of both MAO-A and MAO-B. However, it appears that inhibition of MAO-A, not MAO-B, is important to the antidepressant action of these agents. [Pg.392]

Although clinical experience indicates tranylcypromine may be an effective antipanic agent, there are no controlled trials confirming this observation. Phenelzine, however, has been found to be very effective in both open and controlled designs ( 21, 116, 117). Onset of action is similar to that of other antidepressants, and although adverse effects tend to be less troublesome than with tricyclics, dietary restrictions may limit the usefulness of MAOIs in some patients. Unfortunately, the relapse rate may be comparable to that seen with BZDs and TCAs. For example, Kelly et al., in a follow-up of 246 patients, found that 50% who had discontinued MAOIs relapsed within 1 year (118). [Pg.260]

The MAO inhibitor tranylcypromine is amphetamine-like in structure but interacts only weakly at DA transporters. The phenylpiperazine nefazodone, and to a lesser extent, the structurally related trazodone have weak inhibitory actions on 5-HT transport nefazodone also may have a minor effect on NE transport. This agent also has a prominent direct antagonistic effect at S-HT receptors that may contribute to antidepressant and anxiolytic activity. Both drugs also may inhibit presynaptic 5-HTj subtype autoreceptors to enhance neuronal release of 5-HT, though they probably also exert at least partial-agonist effects on postsynaptic 5-HTj receptors. Trazodone also blocks cerebral and Hj receptors, possibly contributing to its tendency to induce priapism and sedation, respectively. [Pg.287]

MAO inhibitor tranylcypromine, for example, has been used since the 1960s as an antidepressant. A problem associated with many MAO inhibitors is that they are notoriously nonselective and can interfere with the metabolism of other neurotransmitters, amines found in certain foods, and exogenously administered amine-containing therapeutic agents. [Pg.595]

A number of new MAO inhibitors were described in 1971 however, because of the limited clinical utility of these agents in the treatment of depression, they will not be reviewed in detail. Nonetheless, several of these substances are noteworthy. Sydnophene ( ) was Included in a series of sydnonimines examined for MAO-inhibitory activity. It demonstrated mild stimulant and antidepressive actions in extensive clinical studies in Russia. Another MAO-inhibitor, clorgiline (32. M B 9302) had antidepressive activity its clinical effects were similar to those of imipramine. Proportions of two forms of MAO (Type A, B) were found to vary in different areas of rat brain. The type A enzyme, predominant in sympathetic nerves, acted on both 5-HT and tyramlne and was Inhibited by 32. whereas type B-MAO was insensitive to and acted on tyramine, but not 5-HT. In humans, tranylcypromine and isocarboxazid Increased 5HT, NE and dopamine levels in various brain areas however, the effect of tranylcypromine was significantly greater than that of the other two on dopamine in the caudate nucleus and hypothalamus. In vitro. Lilly 516 1 ( ), like harmaline, preferentially blocked MAO oxidation of 5-HT, whereas tranylcypromine and pargyline selectively inhibited the oxidation of tyramine. ... [Pg.22]


See other pages where Antidepressant agents tranylcypromine is mentioned: [Pg.157]    [Pg.148]    [Pg.301]    [Pg.148]    [Pg.127]    [Pg.870]    [Pg.208]    [Pg.364]    [Pg.220]    [Pg.176]    [Pg.115]    [Pg.729]    [Pg.17]    [Pg.418]    [Pg.467]    [Pg.565]    [Pg.701]    [Pg.215]    [Pg.42]    [Pg.189]    [Pg.285]   
See also in sourсe #XX -- [ Pg.121 , Pg.126 ]




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Antidepressant agents

Tranylcypromine

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